DUPIXENT is given as an injection under the skin (subcutaneous injection).
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They settled on the SM-88 treatment, which involved simply taking a pill and doing a subcutaneous injection once a day, every day.
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"For them, whether it comes as a subcutaneous injection or whether it comes as an IV infusion that they take four times per year, that's very appealing for them," he told Cramer.
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Reconstitution in sterile diluent produces a solution for subcutaneous injection.
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Although nandrolone decanoate is usually administered by intramuscular injection, it has been found to be similarly effective when administered by subcutaneous injection. The pharmacokinetics of nandrolone decanoate via subcutaneous injection closely resemble those of intramuscular injection. However, subcutaneous injection is considered to be easier, more convenient, and less painful compared to intramuscular injection. In addition, research suggests that most intramuscular injections in practice are in fact subcutaneous injections.
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Product Information: TINDAMAX(R) oral tablets, tinidazole oral tablets. Mission Pharmacal Company, San Antonio, TX, 2007. The GLP-1 receptor agonist lixisenatide may slow down the absorption and activity of benznidazole, presumably due to delayed gastric emptying.Product Information: ADLYXIN(TM) subcutaneous injection, lixisenatide subcutaneous injection.
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It is approved for use in CSII pumps and Flexpen, Novopen delivery devices for subcutaneous injection.
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Erenumab is indicated for the prevention of migraine in adults. It is administered by subcutaneous injection.
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Buserelin is available in the form of a 1 mg/mL solution for use as a nasal spray or subcutaneous injection once every 8 hours (three times per day) and as 6.3 mg and 9.45 mg implants for subcutaneous injection once every two and three months, respectively.
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The LD50 of subcutaneous injection of the venom of Buthus eupeus in mice is 1.45 mg/kg.
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Testosterone esters like testosterone enanthate and testosterone cypionate can be given by subcutaneous injection instead of intramuscular injection. Studies have shown that subcutaneous injection of testosterone and closely related esters in oil like testosterone cypionate, testosterone enantate, and nandrolone decanoate is effective and has similar pharmacokinetics to intramuscular injection.
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The bioavailability of bremelanotide with subcutaneous injection is about 100%. Following a subcutaneous injection of bremelanotide, maximal levels occur after about one hour, with a range of 0.5 to 1.0 hours. The plasma protein binding of bremelanotide is 21%. Bremelanotide is metabolized via hydrolysis of its peptide bonds.
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Alomone labs: Taipoxin (pdf) Median lethal dose (LD50) for mice is around 1–2 μg/kg (subcutaneous injection).
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The albumin used is a medicinal product approved in several countries, and is indicated for subcutaneous injection therapy.
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Estradiol cypionate in a microcrystalline aqueous suspension has been found to have equivalent effectiveness and virtually identical pharmacokinetics when administered by subcutaneous injection versus intramuscular injection. However, subcutaneous injection is considered to be easier and less painful relative to intramuscular injection, and for these reasons, may result in comparatively greater satisfaction and compliance.
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The protein is prepared in a lyophilized 1 microgram dose. Reconstitution in sterile diluent produces a solution for subcutaneous injection.
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A lower strength product is available for children. Intramuscular injection can be complicated in that the depth of subcutaneous fat varies and may result in subcutaneous injection, or may be injected intravenously in error, or the wrong strength used. Intramuscular injection does give a faster and higher pharmacokinetic profile when compared to subcutaneous injection.
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The dose recommended is 80mcg subcutaneous injection once a day, administered in the periumbilical area using a prefilled pen device containing 30 doses.
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The drug is administered by monthly intravenous infusions. An infusion takes about an hour. An alternative formulation for subcutaneous injection was approved in October 2013.
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Rebif; July 29, 2016EMD Serono Takes on Exclusive Promotion of Rebif (interferon beta-1a) in the US; January 19, 2016 Rebif is administered via subcutaneous injection.
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After subcutaneous injection, asfotase alfa has a bioavailability of 46–98% and reaches highest blood plasma concentrations after 24 to 48 hours. Elimination half life is five days.
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The pharmacokinetics and distribution of hexestrol have been studied with intravenous injection of aqueous solution in women and with subcutaneous injection of oil solution in female goats and sheep.
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3D animation of a subcutaneous injection A subcutaneous injection is administered as a bolus into the subcutis, the layer of skin directly below the dermis and epidermis, collectively referred to as the cutis. Subcutaneous injections are highly effective in administering medications such as insulin, morphine, diacetylmorphine and goserelin. Subcutaneous (as opposed to intravenous) injection of recreational drugs is referred to as "skin popping." Subcutaneous administration may be abbreviated as SC, SQ, sub-cu, sub-Q, SubQ, or subcut.
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For the treatment and prevention of DVT, the drug is administered as a subcutaneous injection (under the skin), usually around the stomach. Injections are given once or twice daily depending on the condition.
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Estradiol esters like estradiol valerate and estradiol cypionate can be given by subcutaneous injection instead of intramuscular injection. Subcutaneous and intramuscular injection of estradiol cypionate in an aqueous suspension has been found to result in levels of estradiol and other pharmacokinetic parameters (e.g., duration) that were virtually identical. Studies have shown that subcutaneous injection of closely related steroid esters in oil like the androgen esters testosterone cypionate, testosterone enantate, and nandrolone decanoate is effective and has similar pharmacokinetics to intramuscular injection as well.
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There are ongoing efforts to develop sublingual epinephrine to treat anaphylaxis. Subcutaneous injection of the anti-IgE antibody omalizumab is being studied as a method of preventing recurrence, but it is not yet recommended.
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Hydroxocobalamin at standard conditions is a solid composed of dark red crystals. Hydroxocobalamin injection USP (1000 mcg/mL) is a clear red liquid solution. Shown is 500 mcg B-12 prepared for subcutaneous injection.
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OHPH shows a pronounced depot effect when administered by subcutaneous injection in animals, similarly to the closely related medication hydroxyprogesterone caproate. The oral activity of OHPH in animals does not appear to have been assessed.
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Absorption: Bioavailability (subcutaneous injection) ~ 100% Distribution: Volume of distribution (anti-Factor Xa activity) = 4.3 liters Metabolism: Enoxaparin is metabolized in the liver into low molecular weight species by either or both desulfation and depolymerization. Elimination: A single dose of a subcutaneous injection of enoxaparin has an elimination half-life of 4.5 hours. Approximately 10–40% of the active and inactive fragments from a single dose are excreted by the kidneys. Dose adjustments based on kidney function are necessary in persons with reduced kidney function.
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Amylin agonist analogues slow gastric emptying and suppress glucagon. They have all the incretins actions except stimulation of insulin secretion. , pramlintide is the only clinically available amylin analogue. Like insulin, it is administered by subcutaneous injection.
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The practice of "skin-popping" or subcutaneous injection predisposes to necrotizing fasciitis or necrotizing cellulitis from Clostridium perfringens, while deep intramuscular injection predisposes to necrotizing myositis. Tar heroin injection can also be associated with Clostridium botulinum infection.
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An insulin pump with a subcutaneous injection site A person with insulin-dependent (either type 1 or type 2) diabetes mellitus typically injects insulin subcutaneously. The injection should be given under the skin, into the fat layer.
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Conversely, testosterone and testosterone esters in oil solution or crystalline aqueous suspension administered by intramuscular or subcutaneous injection have much longer half- lives, in the range of days to months, due to slow release from the injection site.
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Mipomersen (INN; trade name Kynamro) is used to treat homozygous familial hypercholesterolemia and is administered by subcutaneous injection. There is a serious risk of liver damage from this drug and it can only be prescribed in the context of a risk management plan.
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The skeletal effects of parathyroid hormone depend upon the pattern of systemic exposure. Transient elevations in parathyroid hormone levels after subcutaneous injection of Preotact stimulates new bone formation on trabecular and cortical bone surfaces by preferential stimulation of osteoblastic activity over osteoclastic activity.
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Reconstitution in sterile diluent produces a solution for subcutaneous injection. It is unknown what LTCI is in terms of its sequence. It is not interleukins 1-7 nor G-CSF. The manufacturer verifies its potency by checking for stimulation of IL-2 production.
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Angiotensin II causes blood vessels to constrict, and drives blood pressure up. CYT006-AngQb consists of virus-like particles covalently coupled to angiotensin II. Subcutaneous injection causes the immune system to produce antibodies which reduce angiotensin II blood levels, lowering blood pressure.
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When used at a higher dose of 100 mg per injection in men with prostate cancer, estradiol undecylate has been given usually once a month. After a single subcutaneous injection of estradiol undecylate in rats, its duration of effect was 80 days (about 2.5 months).
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After subcutaneous injection, mipomersen reaches highest blood levels after 3 to 4 hours. It accumulates in the liver, which is convenient since apolipoprotein B predominantly acts there. Protein binding is over 90%. The molecule is slowly broken up by endonucleases and subsequently by exonucleases.
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Preliminary studies in bladder carcinoma, carcinoma of the urothelium and lymphomas are also promising. Another interesting schedule of subcutaneous injection with low doses of gallium nitrate has been proposed, especially for the treatment of bone metastases, but the definitive results have not yet been published.
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Progesterone can be administered by subcutaneous injection, with Prolutex, an aqueous solution of progesterone marketed in Europe, being intended for once-daily administration by this route. This formulation is rapidly absorbed and has been found to result in higher peak levels of progesterone relative to progesterone in oil solution by intramuscular injection. In addition, subcutaneous injection of progesterone is considered to be easier, safer due less risk of injection site reactions, and less painful compared to intramuscular injection of progesterone. The elimination half-life of this formulation is 13 to 18 hours, compared to 20 to 28 hours for intramuscular injection of progesterone in oil solution.
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The affected persons are then switched to a preparation that does not contain the specific agent they are reacting to or undergo desensitization. Cutaneous adverse effects Repeated subcutaneous injection without site rotation can lead to lipohypertrophy and amyloidomas, which manifest as firm palpable nodules under the skin.
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After subcutaneous injection, the erenumab has an estimated bioavailability of 82%. Highest blood plasma concentrations are reached after four to six days. Like other proteins, the substance is degraded by proteolysis to small peptides and amino acids. It has an elimination half-life of 28 days.
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A dart injection is used to give a single intramuscular or subcutaneous injection to livestock without restraining the animal. It can be contrasted with hand injection. These injections are usually administered by a tranquilliser gun, if in the wild, or sometimes a blowgun if in captivity.
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After subcutaneous injection, mepolizumab has an estimated bioavailability of 80% and reaches highest blood plasma concentrations after four to eight days. Like other antibodies, it is degraded by proteolytic enzymes. Its biological half-life is 20 days on average, ranging from 16 to 22 days in different individuals.
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The affected animal should be left in the pasture, and not forced to come back to stall because excitation can darken the prognosis, even after adequate treatment. Intravenous mixed calcium and magnesium injection are used. Subcutaneous injection of magnesium sulfate (200 ml of 50% solution) is also recommended.
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Megestrol caproate, abbreviated as MGC, is a progestin medication which was never marketed. It was developed in Russia in 2002. In animals, MGC shows 10-fold higher progestogenic activity compared to progesterone when both are administered via subcutaneous injection. In addition, MGC has no androgenic, anabolic, or estrogenic activity.
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The targets of pitrakinra action are inflammatory cells (dendritic cells, Th2 cells, B cells) and structural cells (smooth muscle, endothelium, epithelium) that express IL-4Rα. The drug has been applied both as a subcutaneous injection and as an inhalation, but the latter formulation proved to be more effective.
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Naloxone can also be administered via intramuscular or subcutaneous injection. The onset of naloxone provided through this route is 2 to 5 minutes with a duration of around 30-120min.Naloxone for Treatment of Opioid Overdose Oct. 2016 Naloxone administered intramuscularly are provided through pre-filled syringes, vials, and auto-injector.
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The leaves contain an essential oil and the coumarins, ayapanin and ayapin, stigmasterol, esculetin methylene ether (the Methylene ether of esculetin), vitamin C and carotene. Ayapanin and ayapin are non-toxic and possess pronounced haemostatic properties and are effective when applied locally or when administered by subcutaneous injection or orally.
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Injectable medications can produce irritation or bruises at injection site. The bruise depicted was produced by a subcutaneous injection. Interferon beta-1b is available only in injectable forms, and can cause skin reactions at the injection site that may include cutaneous necrosis. Skin reactions vary greatly in their clinical presentation.
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Oxycodone can be administered orally, intranasally, via intravenous, intramuscular, or subcutaneous injection, or rectally. The bioavailability of oral administration of oxycodone averages within a range of 60 to 87%, with rectal administration yielding the same results; intranasal varies between individuals with a mean of 46%.Analgesic Expert Group. Therapeutic Guidelines: Analgesic.
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Hydroxyprogesterone heptanoate benzilic acid hydrazone (OHPHBH), also known as 17α-hydroxyprogesterone 17α-heptanoate 3-benzilic acid hydrazone, is a progestin medication which was never marketed. It is the C3 benzilic acid hydrazone of hydroxyprogesterone heptanoate (OHPH). The medication has a longer duration of action than OHPH when administered by subcutaneous injection in animals.
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Some formulations, intended for use against coughing and the like, have other active ingredients such as antihistamines, decongestants and others. Other oral formulations, such as packets of effervescent powder, sublingual drops, elixirs and the like are also available in many locations. Injectable dihydrocodeine is most often given as a deep subcutaneous injection.
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Injectable medications can produce irritation or bruises at injection site. The bruise depicted was produced by a subcutaneous injection. Irritation zone after injection of glatiramer acetate. Both the interferons and glatiramer acetate are available only in injectable forms, and both can cause skin reactions at the injection site, specially with subcutaneous administration.
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Transdermal progesterone is poorly effective, owing to absorption issues. Progestins are usually taken orally. In contrast to progesterone, most progestins have high oral bioavailability, and can produce full progestogenic effects with oral administration. Some progestins, such as medroxyprogesterone acetate and hydroxyprogesterone caproate, are or can be used by intramuscular or subcutaneous injection instead.
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By virtue of its peptide nature, enfuvirtide is marketed in injectable form. The lyophilised enfuvirtide powder must be reconstituted by the patient and administered twice daily by subcutaneous injection. Due to the chronic nature of this kind of therapy, this dosage form may be a major problem for the patient's adherence to this drug regimen.
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MFA is a convulsant poison. It causes severe convulsions in poisoned victims. Death results from respiratory failure. For a variety of animals, the toxicity of methyl fluoroacetate has been determined orally and through subcutaneous injection. The dosage ranges from 0.1 mg/kg in dogs to 10-12 mg/kg in monkeys indicating considerable variation.
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Daratumumab/hyaluronidase, sold under the brand name Darzalex Faspro, is a combination drug for the treatment of adults with newly diagnosed or relapsed/refractory multiple myeloma. It is a combination of daratumumab and hyaluronidase. It is administered via subcutaneous injection. The most common adverse reaction using daratumumab/hyaluronidase as monotherapy is upper respiratory tracts infection.
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Estradiol is well-absorbed regardless of route of administration. However, the bioavailability of estradiol differs substantially with different routes of administration. Oral estradiol has an average bioavailability of around 5%, requiring relatively high dosages of estradiol for effects. Estradiol administered in the form of an ester by intramuscular or subcutaneous injection has complete bioavailability.
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OHPH is a progestin, or a synthetic progestogen, and hence is an agonist of the progesterone receptor, the biological target of progestogens like progesterone. The progestogenic potency of OHPH in the uterus is equal to or greater than that of progesterone when administered by subcutaneous injection in animals.Junkmann, K. (1959). Über Entwicklungen auf dem Gestagengebiet. 15.
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In veterinary anesthesia, medetomidine is often used in combinations with opioids (butorphanol, buprenorphine etc.) as premedication (before a general anesthetic) in healthy cats and dogs. It can be given by intramuscular injection (IM), subcutaneous injection (SC) or intravenous injection (IV). When delivered intravenously, a significantly decreased dose is used. Some authors suggest a sublingual route is also effective.
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After subcutaneous injection, ixekizumab has a bioavailability of 54–90%. Highest blood plasma concentrations are reached after four to seven days after a single dose. With the usual dosing scheme (loading plus a dose every two weeks), steady state concentrations are reached in the eighth week on average. Like other antibodies, ixekizumab is probably degraded by proteolysis.
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Cefovecin is a broad-spectrum, third-generation cephalosporin antibiotic administered by subcutaneous injection. It is used to treat skin and soft tissue infections in dogs and cats. The antimicrobial effects last for 14 days following administration. In drug studies, cefovecin administered to dogs was 92.4% effective against skin infections (secondary superficial pyoderma, abscesses, and infected wounds).
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Tumor progression was observed after subcutaneous injection into the dorsal subcutis for 107 wild type, 129/Black Swiss mice. These mice were selected for their genetic background proximity to C57BL/6J mice. They observed the progression as being characterized by skin ulceration followed by ulcer hemorrhaging. Not only that, there was also basal hemorrhaging and/or edema.
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After subcutaneous injection, fremanezumab has a bioavailability of 55–66%. Highest concentrations in the body are reached after five to seven days. Like other proteins, the substance is degraded by proteolysis to small peptides and amino acids, which are reused or excreted via the kidney. The elimination half-life is estimated to be 30 to 31 days.
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Testosterone can be taken by a variety of different routes of administration. These include oral, buccal, sublingual, intranasal, transdermal (gels, creams, patches), rectal suppositories), by intramuscular or subcutaneous injection (in oil or aqueous), and as a subcutaneous implant. The pharmacokinetics of testosterone, including its bioavailability, circulating testosterone levels, metabolism, biological half-life, and other parameters, differ by route of administration.
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It contains 69% of the MPA found in the original intramuscular DMPA formulation. It can be injected using a smaller injection needle inserting the medication just below the skin, instead of into the muscle, in either the abdomen or thigh. This subcutaneous injection claims to reduce the side effects of DMPA while still maintaining all the same benefits of the original intramuscular DMPA.
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The oral activity of nandrolone has been studied. With oral administration of nandrolone in rodents, it had about one-tenth of the potency of subcutaneous injection of nandrolone. Nandrolone has very low affinity for human serum sex hormone-binding globulin (SHBG), about 5% of that of testosterone and 1% of that of DHT. It is metabolized by the enzyme 5α-reductase, among others.
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Injectable medications can produce irritation or bruises at injection site. The bruise depicted was produced by a subcutaneous injection. Interferon beta-1a is available only in injectable forms, and can cause skin reactions at the injection site that may include cutaneous necrosis. Skin reactions with interferon beta are more common with subcutaneous administration and vary greatly in their clinical presentation.
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Several dosage forms for sumatriptan have been approved, including tablets, solution for injection, and nasal inhalers. In July 2009, the US FDA approved a single-use jet injector formulation of sumatriptan. The device delivers a subcutaneous injection of 6 mg sumatriptan, without the use of a needle. Autoinjectors with needles have been previously available in Europe and North America for several years.
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Acyline (developmental code name MER-104) is a gonadotropin-releasing hormone analogue (GnRH analogue) and gonadotropin-releasing hormone antagonist (GnRH antagonist) which was never marketed. It has been shown to suppress gonadotropin and testosterone levels in men. Acyline is a peptide and under normal circumstances is not orally active. For this reason, it has instead been administered by subcutaneous injection.
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Tildrakizumab was approved by the Food and Drug Administration in March 2018, and the European Medicines Agency in September 2018, for the treatment of moderate-to-severe plaque psoriasis in adult patients who are candidates for systemic therapy. Tildrakizumab is administered via subcutaneous injection. It is available as a single-dose prefilled syringe containing 100 mg of tildrakizumab in 1 ml of solution.
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Buserelin is ineffective via oral administration due to first-pass metabolism in the gastrointestinal tract. Its bioavailability is 2.5 to 3.3% by intranasal administration and 70% by subcutaneous injection. The plasma protein binding of buserelin is approximately 15%. The metabolism of buserelin occurs in the liver, kidneys, and gastrointestinal tract and is mediated by peptidases, specifically pyroglutamyl peptidase and chymotrypsin-like endopeptidase.
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Commonly the drug is given as a carefully titrated intravenous infusion with a syringe pump or volumetric pump. Because of its vasoconstrictive effect, phenylephrine can cause severe necrosis if it infiltrates the surrounding tissues. Because of this, it should be given through a central line if at all possible. Damage may be prevented or mitigated by infiltrating the tissue with the alpha blocker phentolamine by subcutaneous injection.
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The MMR vaccine is administered by a subcutaneous injection. The second dose may be given as early as one month after the first dose. The second dose is a dose to produce immunity in the small number of persons (2–5%) who fail to develop measles immunity after the first dose. In the U.S. it is done before entry to kindergarten because that is a convenient time.
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Insulin aspart can be used in an insulin pump and insulin pen for subcutaneous injection. Additionally, it can be used with an injection port such as the I-port. Insulin aspart has a more rapid onset, and a shorter duration of activity than normal human insulin. Therefore, insulin aspart given by injection should normally be used in a regimen with long-acting or intermediate insulin.
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TVOR is typically performed after ovarian hyperstimulation, where oocytes are pharmacologically stimulated to mature. When the ovarian follicles have reached a certain degree of development, induction of final oocyte maturation is performed, generally by an intramuscular or subcutaneous injection of human chorionic gonadotropin (hCG). TVOR is typically performed 3436 hours after hCG injection, when the eggs are fully mature but just prior to rupture of the follicles.
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The bioavailability of nafarelin with intranasal administration is 2.8% on average, with a range of 1.2 to 5.6%. The plasma protein binding of nafarelin is 80%. It is metabolized primarily by peptidases and not by cytochrome P450 enzymes. The elimination half-life of nafarelin is 2.5 to 3.0 hours by intranasal administration, whereas the half-life of nafarelin and its metabolites by subcutaneous injection is 85.5 hours.
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As with all hormonal therapies, degarelix is commonly associated with hormonal side effects such as hot flashes and weight gain. Due to its mode of administration (subcutaneous injection), degarelix is also associated with injection-site reactions such as injection-site pain, erythema or swelling. Injection-site reactions are usually mild or moderate in intensity and occur predominantly after the first dose, decreasing in frequency thereafter. Less common: Anemia.
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A study finds a correlation between the presence of MGL and an increase in mice survival after subcutaneous injection of the bacteria. In B. linens, a cheese ripening bacterium, MGL activity is tightly linked with carbohydrate metabolism. In plants, MGL mRNA is found in dry seeds although the protein itself is not. However, the enzyme is highly expressed in wet seeds, suggesting that MGL is a vital part of early germination.
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This is in contrast to estradiol, which is an agonist of this receptor. Like other estrogens, estriol does not importantly interact with other steroid hormone receptors. Estriol is a much less potent estrogen than is estradiol, and is somewhat weak and atypical in its properties. Given by subcutaneous injection in mice, estradiol is about 10-fold more potent than estrone and about 100-fold more potent than estriol.
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Lewin was very successful in his profession. He introduced several new methods in the treatment of syphilis and in dermatology, among which may be mentioned the subcutaneous injection of mercuric chloride and the spray application in diseases of the throat. His mercury sublimate injections for the treatment of syphilis were to be administered daily. Carriage horses delivered the costly therapy, and were referred to as "Sublimatsschimmel" [sublimate greys].
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In 1997 researchers from Gilead and the University of California, San Francisco demonstrated that tenofovir exhibits anti-HIV effects in humans when dosed by subcutaneous injection. The initial form of tenofovir used in these studies had limited potential for widespread use because it poorly penetrated cells and was not absorbed when given by mouth. Gilead developed a pro-drug version of tenofovir, tenofovir disoproxil. This version of tenofovir is often referred to simply as "tenofovir".
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This causes them to form a depot with intramuscular or subcutaneous injection and gives them a long duration when administered by these routes. Some estradiol esters have other moieties instead of fatty acids as the esters. Such esters include sulfuric acid (as in estradiol sulfate), sulfamic acid (as in estradiol sulfamate), phosphoric acid (as in estradiol phosphate), glucuronic acid (as in estradiol glucuronide, and others (e.g., estramustine phosphate (estradiol 3-normustine 17β-phosphate)).
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After subcutaneous injection of a single dose, daclizumab has a bioavailability of about 90% and reaches highest blood plasma levels after 5 to 7 days. Given every four weeks, steady state concentrations are found after the fourth dose. It is expected that daclizumab, like other antibodies, is degraded by proteases to peptides and finally amino acids, and that it does not interact with cytochrome P450 liver enzymes. The biological half-life is 21 days.
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Pitrakinra is associated with few adverse effect, whether administered by subcutaneous injection or by inhalation in participants with atopic asthma or atopic eczema. The most common adverse event after subcutaneous administration is injection site-related discomfort, a common event with most injectable drugs. However, these events are neither associated with the development of antibodies nor with any discernible pattern (i.e., they were not more common at the end of the 4 weeks of exposure).
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Distribution of hexestrol radioactivity in blood and tissues after a subcutaneous injection of a physiological dose of tritium- labeled hexestrol in oil solution in five juvenile female goats. Points are one animal each. With the exception of skeletal muscle, tissues with a radioactivity concentration of less than 15% of that of the endometrium are not shown. Hexestrol is concentrated in target tissues such as the uterus and vagina due to binding to estrogen receptors.
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Anakinra is administered at home by subcutaneous injection. It is used as a second line treatment to manage symptoms of rheumatoid arthritis after treatment with a disease-modifying antirheumatic drug (DMARD) has failed. It can be used in combination with some DMARDs. For label updates see FDA index page for BLA 103950 It is used to treat anyone from infants to adults with a cryopyrin-associated periodic syndrome, including neonatal-onset multisystem inflammatory disease.
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Tildrakizumab is available as a single-use, pre-filled syringe and is administered via subcutaneous injection. The recommended dose of tildrakizumab in the United States and in the European Union is 100 mg at weeks 0, and 4 and every 12 weeks thereafter. In the European Union, a 200 mg dose is also approved. For patients with certain characteristics (high disease burden, body weight ≥ 90 kg) the 200 mg may provide greater efficacy.
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One 150 mg subcutaneous injection, usually needed every two weeks, costs over $16,700. On August 27, 2017, the results of the CANTOS trial were announced at the European Society of Cardiology and published in The Lancet and The New England Journal of Medicine. Those treated in CANTOS had a 15% reduction in deaths from heart attacks, stroke and cardiovascular disease combined. However, there were serious side-effects and no statistically significant overall survival benefit.
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The trial was conducted at 24 sites in Australia, Europe, South America, and the United States. The benefits and side effects of inotersen were evaluated in one clinical trial that enrolled patients with hereditary transthyretin-mediated amyloidosis. Patients were randomly assigned to receive inotersen or placebo by subcutaneous injection given once a week for 65 weeks. During the first week of treatment, patients received three doses of treatment, followed by once weekly subcutaneous injections for 64 weeks.
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Injections of insulin – via subcutaneous injection using either a syringe or using an insulin pump – are necessary for those living with type 1 diabetes because it cannot be treated by diet and exercise alone. Insulin dosage is adjusted taking into account food intake, blood glucose levels and physical activity. Untreated type 1 diabetes can commonly lead to diabetic ketoacidosis which can result in death. Diabetic ketoacidosis can cause cerebral edema (accumulation of liquid in the brain).
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It is also used to treat relapsing-remitting multiple sclerosis. It is administered by subcutaneous injection. It is a mixture of random-sized peptides that are composed of the four amino acids found in myelin basic protein, namely glutamic acid, lysine, alanine, and tyrosine. Myelin basic protein is the antigen in the myelin sheaths of the neurons that stimulates an autoimmune reaction in people with MS, so the peptide may work as a decoy for the attacking immune cells.
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Urofollitropin is a purified form of follicle-stimulating hormone (FSH) that is manufactured by extraction from human urine and then purified to remove various proteins and other substances. FSH is important in the development of follicles (eggs) produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility.Drugs.com: Urofollitropin (Intramuscular route, Subcutaneous route, Injection route) It is also used with in vitro fertilization methods.
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The vaccine itself can be administered differently depending on the species. The route of administration for most animals is subcutaneous injection, while injections are administered intramuscularly to pigs and in the wing membrane to birds. The dose can also vary depending on the animal and disease. The usual method is either three doses of the same volume but increasing density, three doses of the same density with the last two as booster doses, or one dose only.
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However, oral progesterone has very low bioavailability, and produces relatively weak progestogenic effects even at high doses. In accordance, and in contrast to progestins, oral progesterone has no antigonadotropic effects in men even at high doses. Progesterone can also be taken by various parenteral (non-oral) routes, including sublingually, rectally, and by intramuscular or subcutaneous injection. These routes do not have the bioavailability and efficacy issues of oral progesterone, and accordingly, can produce considerable antigonadotropic and other progestogenic effects.
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Following subcutaneous injection, albiglutide reaches highest blood concentrations after three to five days. Steady-state concentrations are achieved after three to five weeks. The substance is most likely broken down by protease enzymes to small peptides and amino acids. Being resistant to dipeptidyl peptidase-4 (DPP-4), the enzyme that breaks down GLP-1, albiglutide has a biological half-life of five (four to seven) days, which is considerably longer than the older GLP-1 analogs exenatide and liraglutide.
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In a clinical context the route of administration is most commonly intravenous injection; it may also be given by intramuscular or subcutaneous injection, as well as orally in the form of tablets. The onset of effects is usually rapid and lasts for a few hours. Common side effects include respiratory depression (decreased breathing), dry mouth, drowsiness, impaired mental function, constipation, and addiction. Side effects of use by injection can include abscesses, infected heart valves, blood-borne infections, and pneumonia.
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The oil mentioned in the Ayurvedic texts was determined to be from the tree Hydnocarpus wightiana, known as Tuvakara in Sanskrit and chaulmugra in Hindi and Persian. The first parenteral administration was given by the Egyptian doctor Tortoulis Bey, personal physician to the Sultan Hussein Kamel of Egypt. He had been using subcutaneous injections of creosote for tuberculosis. In 1894 he administered subcutaneous injection of chaulmoogra oil to a 36-year- old Egyptian Copt who had been unable to tolerate oral treatment.
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Treatment with iron-chelating drugs such as deferoxamine reduces mortality in persons with sickle cell disease or β‐thalassemia who are transfusion dependent. Administration for chronic conditions is generally accomplished by subcutaneous injection over a period of 8–12 hours each day. Administration of deferoxamine after acute intoxication may color the urine a pinkish red, a phenomenon termed "vin rosé urine". Apart from iron toxicity, deferoxamine can be used to treat aluminium toxicity (an excess of aluminium in the body) in select patients.
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The recommended dose is 100 micrograms of Preotact administered once-daily as a subcutaneous injection into the abdomen, during 18 months (data support treatment up to 24 months). The injections are given using a specially designed injection device (Preotact(TM)Pen). The PreotactPen is specifically designed to allow osteoporosis patients to administer the injections, despite challenges of vision impairment and limited strength of hands and digits tributable to high age. Patients should receive supplemental calcium and vitamin D during treatment with parathyroid hormone.
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Medication: For those unable to tolerate routine blood draws, there are chelating agents available for use. The drug deferoxamine binds with iron in the bloodstream and enhances its elimination in urine and faeces. Typical treatment for chronic iron overload requires subcutaneous injection over a period of 8–12 hours daily. Two newer iron-chelating drugs that are licensed for use in patients receiving regular blood transfusions to treat thalassaemia (and, thus, who develop iron overload as a result) are deferasirox and deferiprone.
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NPH (Neutral Protamine Hagedorn) insulin is an intermediate-acting insulin with delayed absorption after subcutaneous injection, used for basal insulin support in diabetes type 1 and type 2. NPH insulins are suspensions that require shaking for reconstitution prior to injection. Many people reported problems when being switched to intermediate acting insulins in the 1980s, using NPH formulations of porcine/bovine insulins. Basal insulin analogs were subsequently developed and introduced into clinical practice to achieve more predictable absorption profiles and clinical efficacy.
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Given by subcutaneous injection in mice, estradiol is about 10-fold more potent than estrone and about 100-fold more potent than estriol. The ERs are expressed widely throughout the body, including in the breasts, uterus, vagina, fat, skin, bone, liver, pituitary gland, hypothalamus, and other parts of the brain. In accordance, estradiol has numerous effects throughout the body. Among other effects, estradiol produces breast development, feminization, changes in the female reproductive system, changes in liver protein synthesis, and changes in brain function.
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The medication was approved in September 2001, by the US Food and Drug Administration for treatment of anemia in patients with chronic kidney failure by intravenous or subcutaneous injection. In June 2001, it had been approved by the European Medicines Agency for this indication as well as the treatment of anemia in cancer patients undergoing chemotherapy. Dr. Reddy's Laboratories launched darbepoetin alfa in India under the brand name ‘Cresp’ in August 2010. This is the world's first follow-on biologic of darbepoetin alfa.
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While in New York, his daughter, Charlotte Maria was born. Finally, he went back to Paris to succeed Claude Bernard in 1878 as professor of experimental medicine in the Collège de France, and he remained there until his death, which occurred in 1894 at Sceaux, France. He was buried in Paris at the Cimetière du Montparnasse. Brown-Séquard was quite a controversial and eccentric figure, and is also known for self-reporting, at age 72, "rejuvenated sexual prowess after subcutaneous injection of extracts of monkey testis".
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MPA is marketed under a large number of brand names throughout the world. Its most major brand names are Provera as oral tablets and Depo-Provera as an aqueous suspension for intramuscular injection. A formulation of MPA as an aqueous suspension for subcutaneous injection is also available in the United States under the brand name Depo-SubQ Provera 104. Other brand names of MPA formulated alone include Farlutal and Sayana for clinical use and Depo-Promone, Perlutex, Promone-E, and Veramix for veterinary use.
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Pertuzumab/trastuzumab/hyaluronidase, sold under the brand name Phesgo, is a fixed-dose combination medication to treat adults with HER2-positive breast cancer that has spread to other parts of the body, and for treatment of adults with early HER2-positive breast cancer. It contains pertuzumab, trastuzumab, and hyaluronidase–zzxf. It is injected under the skin via subcutaneous injection in the thigh. The most common side effects include alopecia (hair loss), nausea, diarrhea, anemia (reduced number of red blood cells) and asthenia (lack of energy).
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Two forms of "cytotoxin II" (cardiotoxin) were found in the venom of this species. The crude venom of this species produced the lowest known lethal dose (LCLo) of 0.005 mg/kg, the lowest among all cobra species, derived from an individual case of poisoning by intracerebroventricular injection. A 1992 extensive toxinology study gave a value of 0.18 mg/kg (range of 0.1 mg/kg - 0.26 mg/kg) by subcutaneous injection. According to Brown (1973), the subcutaneous value is 0.4 mg/kg, while Ernst and Zug et al.
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Abaloropatide was known as BIM-44058 when it was first discovered at Ipsen and as BA058 while under development. The anabolic effects of abaloparatide on bone were demonstrated in two preclinical studies conducted in ovariectomized rats. Both studies showed increased cortical and trabecular bone volume and density, and trabecular microarchitecture improvement in vertebral and nonvertebral bones after short-term and long-term daily subcutaneous injection of abaloparatide compared to controls. Recent studies indicated a dose-dependent increased in bone mass and strength in long-term abalorapatide treatment.
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Testosterone can be taken by a variety of different routes of administration. These include oral, buccal, sublingual, intranasal, transdermal (gels, creams, patches, solutions), vaginal (creams, gels, suppositories), rectal (suppositories), by intramuscular or subcutaneous injection (in oil solutions or aqueous suspensions), and as a subcutaneous implant. The pharmacokinetics of testosterone, including its bioavailability, metabolism, biological half-life, and other parameters, differ by route of administration. Likewise, the potency of testosterone, and its local effects in certain tissues, for instance the liver, differ by route of administration as well.
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Sumatriptan is administered in several forms: tablets, subcutaneous injection, and nasal spray. Oral administration (as the succinate salt) suffers from poor bioavailability, partly due to presystemic metabolism—some of it gets broken down in the stomach and bloodstream before it reaches the target arteries. A new rapid-release tablet formulation has the same bioavailability, but the maximum concentration is achieved on average 10–15 minutes earlier. When injected, sumatriptan is faster-acting (usually within 10 minutes), but the effect lasts for a shorter time.
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Indole-3-carbinol causes proliferation arrest and apoptosis in human melanoma cells. Kim YS et al showed that the master regulator of melanoma biology, microphthalmia-associated transcription factor (MITF-M) was downregulated by Indole-3-carinol to induce apoptosis. Kundu A et al demonstrated that the anticancer property of Indole-3-carbinol is driven by specific targeting of oncogenic pathways. In two different studies using xenografted mouse model of melanoma, they observed that subcutaneous injection of Indole-3-carbinol could bring down tumor burden significantly.
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Insulin glargine differs from human insulin by replacing asparagine with glycine in position 21 of the A-chain and by carboxy-terminal extension of B-chain by 2 arginine residues. The arginine amino acids shift the isoelectric point from a pH of 5.4 to 6.7, making the molecule more soluble at an acidic pH and less soluble at physiological pH. The isoelectric shift also allows for the subcutaneous injection of a clear solution. The glycine substitution prevents deamidation of the acid-sensitive asparagine at acidic pH.
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Estradiol can be taken by a variety of different routes of administration. These include oral, buccal, sublingual, intranasal, transdermal (gels, creams, patches), vaginal (tablets, creams, rings, suppositories), rectal, by intramuscular or subcutaneous injection (in oil or aqueous), and as a subcutaneous implant. The pharmacokinetics of estradiol, including its bioavailability, metabolism, biological half-life, and other parameters, differ by route of administration. Likewise, the potency of estradiol, and its local effects in certain tissues, most importantly the liver, differ by route of administration as well.
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It is administered by subcutaneous injection. The most common side effects include hypoglycaemia (low blood glucose). Side effects on the digestive system include nausea (feeling sick), diarrhea, vomiting, constipation, dyspepsia (indigestion), gastritis (inflammation of the stomach), abdominal pain (stomach ache), flatulence (wind), gastroesophageal reflux disease (passage of stomach acid back up towards the mouth), and distension (swelling) of the belly. Insulin degludec is a replacement insulin that acts in the same way as naturally produced insulin and helps glucose enter cells from the blood.
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The pharmacokinetics of progesterone are dependent on its route of administration. The medications is approved in the form of oil- filled capsules containing micronized progesterone for oral administration, termed oral micronized progesterone or OMP. It is also available in the form of vaginal or rectal suppositories or pessaries, topical creams and gels, oil solutions for intramuscular injection, and aqueous solutions for subcutaneous injection. Routes of administration that progesterone has been used by include oral, intranasal, transdermal/topical, vaginal, rectal, intramuscular, subcutaneous, and intravenous injection.
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The four major naturally occurring estrogens in women are estrone (E1), estradiol (E2), estriol (E3), and estetrol (E4). Estradiol is the predominant estrogen during reproductive years both in terms of absolute serum levels as well as in terms of estrogenic activity. During menopause, estrone is the predominant circulating estrogen and during pregnancy estriol is the predominant circulating estrogen in terms of serum levels. Given by subcutaneous injection in mice, estradiol is about 10-fold more potent than estrone and about 100-fold more potent than estriol.
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King cobra skull, lateral view, showing fangs The king cobra's venom consists of cytotoxins and neurotoxins, including alpha-neurotoxins and three-finger toxins. Other components have cardiotoxic effects. It can deliver up to 420 mg venom in dry weight per bite, with a toxicity in mice of 1.28 mg/kg through intravenous injection, 1.5 to 2.18 mg/kg through subcutaneous injection, and 1.644 mg/kg through intraperitoneal injection. The toxins affect the victim's central nervous system, resulting in severe pain, blurred vision, vertigo, drowsiness, and eventually paralysis.
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Because the inflammatory cells of chalazia are sensitive to steroids, intralesional or subcutaneous injection of steroids, commonly triamcinolone acetonide (TA) is considered a simple and effective treatment option with high success rates. It may give the same results as surgical treatment (I&C;). Considering the surgical risks, steroid injection is believed as a safer procedure in marginal lesions and lesions close to lacrimal punctum. One injection alone has a success rate about 80%, if requested a second injection can be given 1-2 weeks later.
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Ganirelix is administered by a subcutaneous injection of 250 µg once per day during the mid to late follicular phase of a patient's menstrual cycle. Treatment should start on the 5th or 6th day after the start of ovarian stimulation, and the mean duration for its use is five days. Preferably, the subcutaneous injections are delivered in the upper leg, and the patient can be trained to do this themself. Continued use of the drug should take place until the administration of hCG begins.
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Efalizumab (trade name Raptiva, Genentech, Merck Serono) is a formerly available medication designed to treat autoimmune diseases, originally marketed to treat psoriasis. As implied by the suffix -mab, it is a recombinant humanized monoclonal antibody administered once weekly by subcutaneous injection. Efalizumab binds to the CD11a subunit of lymphocyte function-associated antigen 1 and acts as an immunosuppressant by inhibiting lymphocyte activation and cell migration out of blood vessels into tissues. Efalizumab was associated with fatal brain infections and was withdrawn from the market in 2009.
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The pharmacokinetics of progesterone are dependent on its route of administration. The medication is approved in the form of oil-filled capsules containing micronized progesterone for oral administration, termed "oral micronized progesterone" ("OMP") or simply "oral progesterone". It is also available in the form of vaginal or rectal suppositories, vaginal gels, oil solutions for intramuscular injection, and aqueous solutions for subcutaneous injection, among others. Routes of administration that progesterone has been used by include oral, intranasal, transdermal, vaginal, rectal, intramuscular, subcutaneous, and intravenous injection.
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The pharmacokinetics of DHPA have been studied, albeit limitedly. One study in women observed an elimination half- life of DHPA and its metabolites of 24 days and found that it remained detectable in the circulation for up to 60 days following a single intramuscular injection. In another study, the duration of action of DHPA was reported to be more than 100 days after a single subcutaneous injection, although it was unspecified as to whether this was in humans or animals. DHPA is excreted preferentially in feces via the biliary route.
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Depo-Provera is the brand name for a 150 mg microcrystalline aqueous suspension of DMPA that is administered by intramuscular injection. The shot must be injected into thigh, buttock, or deltoid muscle four times a year (every 11 to 13 weeks), and provides pregnancy protection instantaneously after the first injection.Stacey, Dawn. Depo Provera: The Birth Control Shot Accessed October 13, 2009 Depo-subQ Provera 104 is a variation of the original intramuscular DMPA that is instead a 104 mg microcrystalline dose in aqueous suspension administered by subcutaneous injection.
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No differences have been detected in the route of administration of UFH (subcutaneous or intravenous). LMWH is usually administered by a subcutaneous injection, and a person's blood clotting factors do not have to be monitored as closely as with UFH. Once the diagnosis is confirmed, a decision needs to be made about the nature of the ongoing treatment and its duration. USA recommendations for those without cancer include anticoagulation (medication that prevents further blood clots from forming) with the DOACs dabigatran, rivaroxaban, apixaban, or edoxaban rather than warfarin or low molecular weight heparin (LMWH).
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An estrogen ester is an ester of an estrogen, most typically of estradiol but also of other estrogens such as estrone, estriol, and even nonsteroidal estrogens like diethylstilbestrol. Esterification renders estradiol into a prodrug of estradiol with increased resistance to first-pass metabolism, slightly improving its oral bioavailability. In addition, estrogen esters have increased lipophilicity, which results in a longer duration when given by intramuscular or subcutaneous injection due to the formation of a long-lasting local depot in muscle and fat. Conversely, this is not the case with intravenous injection or oral administration.
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The acute toxicity of snake venom is conventionally tested on laboratory animals and is evaluated in terms of the median lethal dose (LD50), that is, the dose required to kill half the members of a tested population divided by the weight of the tested animal. The LD50 depends on the animal. Rabbits are about twice as sensitive to sea snake venom as mice, and fish and frogs are even more susceptible. The LD50 for subcutaneous injection of A. duboisii venom into mice is 0.044 mg/kg of body weight.
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The substance is intended for subcutaneous injection and intravenous infusion, and indirectly inhibits aggregation, adhesion, and release of thrombocytes mediated through the action of a fibrinogen degradation product (FDP). It also cleaves and therefore inactivates a significant part of circulating plasma fibrinogen. Fibrinogen is often found in increased concentrations in arteriae with impaired circulation. This leads to a pathologically increased blood viscosity and thereby to a worsening of symptoms of the circulation disorder (more intense pain, decreased mobility of the limb and decreased temperature, need for partial or even total limb amputation).
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Injection into the subcutaneous tissue is a route of administration used for drugs such as insulin: because it is highly vascular, the tissue absorbs drugs quickly. Subcutaneous injection is believed to be the most effective manner to administer some drugs, such as human growth hormones. Just as the subcutaneous tissue can store fat, it can also provide good storage space for drugs that need to be released gradually because there is limited blood flow. "Skin popping" is a slang term that includes this method of administration, and is usually used in association with recreational drugs.
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Steroid esters may be naturally occurring/endogenous like DHEA sulfate or synthetic like estradiol valerate. Esterification is useful because it is often able to render the parent steroid into a prodrug of itself with altered chemical properties such as improved metabolic stability, water solubility, and/or lipophilicity. This, in turn, can enhance pharmacokinetics, for instance by improving the steroid's bioavailability and/or conferring depot activity and hence an extended duration with intramuscular or subcutaneous injection. Esterification of steroids with fatty acids was developed to prolong the duration of effect of steroid hormones.
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Most injector pens are designed for subcutaneous injection just under the skin, but some are designed for injection into muscle. The desired injection site and the skin profile at the injection site will determine what needle length is appropriate for a person to use. For products with included needles, such as epinephrine pens, different brands may have different included needle lengths, which must be taken into account. Multiple studies have shown that many people prefer the use of injector pens over other forms of injectable medication, such as vial and syringe.
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9,11-Dehydrocortexolone 17α-butyrate (developmental code name CB-03-04) is a synthetic steroidal antiandrogen that was developed for use as a topical medication but was never marketed. It is the C17α butyrate (butanoate) ester of the 9,11-dehydrogenated analogue of 11-deoxycortisol (cortexolone). C17α esters of 11-deoxycortisol were unexpectedly found to possess antiandrogen activity, and 9,11-dehydrocortexolone 17α-butyrate was selected for development based on its optimum drug profile. In rats, the drug has been found to possess strong local antiandrogen activity and to also be active systemically upon subcutaneous injection.
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Insulin analog The first biosynthetic insulin analog was developed for clinical use at mealtime (prandial insulin), Humalog (insulin lispro), it is more rapidly absorbed after subcutaneous injection than regular insulin, with an effect 15 minutes after injection. Other rapid-acting analogues are NovoRapid and Apidra, with similar profiles. All are rapidly absorbed due to amino acid sequences that will reduce formation of dimers and hexamers (monomeric insulins are more rapidly absorbed). Fast acting insulins do not require the injection-to-meal interval previously recommended for human insulin and animal insulins.
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DMPA, under brand names such as Depo-Provera and Depo-SubQ Provera 104, is used in hormonal birth control as a long-lasting progestogen-only injectable contraceptive to prevent pregnancy in women. It is given by intramuscular or subcutaneous injection and forms a long-lasting depot, from which it is slowly released over a period of several months. It takes one week to take effect if given after the first five days of the period cycle, and is effective immediately if given during the first five days of the period cycle. Estimates of first-year failure rates are about 0.3%.
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ShK-186 also displays a low toxicity profile in rats. Daily administration of ShK-170 or ShK-186 (100 µg/kg/day) by subcutaneous injection over 4 weeks in rats does not induce any changes in blood counts, blood chemistry or histopathology. By virtue of suppressing only TEM and TEMRA cells, ShK-186 did not compromise protective immune responses to influenza virus and chlamydial infection in rats, most likely because naïve and TCM cells unaffected by Kv1.3 blockade mounted effective immune responses. ShK-186 is poorly immunogenic and did not elicit anti-ShK antibodies in rats repeatedly administered the peptide.
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For mice, the dose at which acute toxicity occurs for intravenous administration is 40 mg/kg and for subcutaneous injection (injection in the layer of skin directly below the dermis and epidermis) this is 380 mg/kg. The lethal dose of dimethocaine for a mouse is 0.3 g per kilogram body weight. An abdominal constriction test was performed in mice, using doses of 5, 10, and 20 mg/kg of dimethocaine which were administered subcutaneously. This test showed induced dose-dependent antinociceptive responses, which are processes that block detection of a painful or injurious stimulus by sensory neurons.
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European Medicines Agency (EMA) has approved the use of golimumab as a treatment for rheumatoid arthritis, psoriatic arthritis and ankylosing spondylitis. Golimumab was approved for the treatment by the US Food and Drug Administration (FDA) as well as the European Medicines Agency (EMA) in 2013 for the treatment of ulcerative colitis. Golimumab can either be used via a self administered subcutaneous injection or intravenous injection. Golimumab is approved in Canada and the United StatesFDA Approves Simponi as a once monthly subcutaneous treatment for adults with moderately to severely active rheumatoid arthritis, psoriatic arthritis, and ankylosing spondylitis.
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Romiplostim treatment is generally administered at weekly intervals via subcutaneous injection. Prior to injection, a complete blood count (CBC) is obtained, as the dosage is dependent on the individual's body weight and platelet count at the time of treatment. The goal of treatment is to maintain the count above 50,000 per cubic millimeter (mm3) of blood, not to achieve a normal count--defined as 150,000-450,000 per mm3 in most healthy individuals. If a count of 200,000 or higher is achieved for two consecutive weeks a reduced dose is administered or treatment is suspended until the count decreases below 200,000.
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Lymphography is a medical imaging technique in which a radiocontrast agent is injected, and then an X-ray picture is taken to visualize structures of the lymphatic system, including lymph nodes, lymph ducts, lymphatic tissues, lymph capillaries and lymph vessels. Lymphangiography is the same procedure, used only to visualize the lymph vessels. The X-ray film or image of the vessels and nodes is called a lymphogram or a lymphangiogram. Radiographs can be taken after injection of a radiopaque contrast medium into small lymphatic vessels (these are made visible by prior subcutaneous injection of patent blue dye).
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Estrone is an estrogen, specifically an agonist of the estrogen receptors ERα and ERβ. It is a far less potent estrogen than is estradiol, and as such, is a relatively weak estrogen. Given by subcutaneous injection in mice, estradiol is about 10-fold more potent than estrone and about 100-fold more potent than estriol. According to one study, the relative binding affinities of estrone for the human ERα and ERβ were 4.0% and 3.5% of those estradiol, respectively, and the relative transactivational capacities of estrone at the ERα and ERβ were 2.6% and 4.3% of those of estradiol, respectively.
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Virtually all infections with rabies resulted in death until two French scientists, Louis Pasteur and Émile Roux, developed the first rabies vaccination in 1885. Nine-year-old Joseph Meister (1876–1940), who had been mauled by a rabid dog, was the first human to receive this vaccine. The treatment started with a subcutaneous injection on 6 July 1885, at 8:00 PM, which was followed with 12 additional doses administered over the following 10 days. The first injection was derived from the spinal cord of an inoculated rabbit which had died of rabies 15 days earlier.
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Following administration, estradiol benzoate acts as a prodrug of estradiol via cleavage by esterases into estradiol and the natural fatty acid benzoic acid. This cleavage occurs not only in the liver, but also in the blood and in tissues. Esters of estradiol like estradiol benzoate are readily hydrolyzed to estradiol, but have an extended duration when administered in via intramuscular or subcutaneous injection due to a depot effect afforded by their fatty acid ester moiety and consequent high lipophilicity. A long-lasting local tissue depot is formed by the injection that slowly releases estradiol benzoate into the circulation.
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Insulin glargine is formulated at an acidic pH 4, where it is completely water-soluble. After subcutaneous injection of the acidic solute (which can cause discomfort and a stinging sensation), when a physiologic pH (approximately 7.4) is achieved the increase in pH causes the insulin to come out of solution resulting in the formation of higher order aggregates of insulin hexamers. The higher order aggregation slows the dissociation of the hexamers into insulin monomers, the functional and physiologically active unit of insulin. This gradual process ensures that small amounts of insulin glargine are released into the body continuously, giving an almost peakless profile.
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All marketed triptans are available in oral form; some in form of sublingual tablets. Sumatriptan and zolmitriptan are also available as nasal sprays. For sumatriptan, a number of other application forms are marketed: suppositories, a subcutaneous injection, an iontophoretic transdermal patch, which uses low voltage controlled by a pre-programmed microchip to deliver a single dose of sumatriptan through the skin within 30 minutes; a drug-device combination containing sumatriptan powder that is "breath powered" allowing the user to blow sumatriptan powder in to their nostrils; as well as a needle-free injection system that works with air pressure.
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In 1934, while working at St Alfege's Hospital, Walker discovered that the subcutaneous injection of physostigmine could temporarily reverse the muscle weakness found in patients suffering from myasthenia gravis. She had noted that the symptoms and signs of myasthenia were similar to those found in curare poisoning, and physostigmine was used as an antidote to curare poisoning at that time. The first case of myasthenia gravis successfully treated with physostigmine was published in the Lancet in June 1934. In 1935, Walker was the first to recognise the association between the condition familial periodic paralysis and hypokalaemia (low blood potassium levels).
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Progesterone is available in a variety of different forms, including oral capsules; sublingual tablets; vaginal capsules, tablets, gels, suppositories, and rings; rectal suppositories; oil solutions for intramuscular injection; and aqueous solutions for subcutaneous injection. A 1% topical progesterone gel is approved for local application to the breasts to treat breast pain, but is not indicated for systemic therapy. Progesterone was previously available as an intrauterine device for use in hormonal contraception, but this formulation was discontinued. Progesterone is also limitedly available in combination with estrogens such as estradiol and estradiol benzoate for use by intramuscular injection.
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Due to its differing effects from those of estradiol, estriol may be considered a safer estrogen in certain regards. Nuclear retention of the receptor estrogen complex in the uterus with a single short-acting subcutaneous injection of 0.1 μg estradiol (E2), 1.0 μg estriol (E3), or a combination of 0.1 μg estradiol and 1.0 μg estriol in aqueous solution in rats. Estriol displaces estradiol from the estrogen receptors and, due to the shorter nuclear retention of estriol, it thereby antagonizes overall nuclear retention. No antagonism occurs when long-acting subcutaneous pellets of estriol are used instead.
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Estrone is an estrogen, specifically an agonist of the estrogen receptors (ERs) ERα and ERβ. It is a far less potent estrogen than is estradiol, and as such is a relatively weak estrogen. Given by subcutaneous injection in mice, estradiol is about 10-fold more potent than estrone and about 100-fold more potent than estriol. According to one study, the relative binding affinities of estrone for the human ERα and ERβ were 4.0% and 3.5% of those estradiol, respectively, and the relative transactivational capacities of estrone at the ERα and ERβ were 2.6% and 4.3% of those of estradiol, respectively.
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The elimination half-life of MPA via oral administration has been reported as both 11.6 to 16.6 hours and 33 hours, whereas the elimination half-lives with intramuscular and subcutaneous injection of microcrystalline MPA in aqueous suspension are 50 and 40 days, respectively. The metabolism of MPA is mainly via hydroxylation, including at positions C6β, C21, C2β, and C1β, mediated primarily via CYP3A4, but 3- and 5-dihydro and 3,5-tetrahydro metabolites of MPA are also formed. Deacetylation of MPA and its metabolites (into, e.g., medroxyprogesterone) has been observed to occur in non-human primate research to a substantial extent as well (30 to 70%).
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Psoriasis is a severe autoimmune disease of the skin that afflicts many people worldwide. Despite the success of recent biologics in ameliorating disease, there is still a search for safe and effective drugs for psoriasis. KV1.3 inhibitors (ShK, PAP-1) have been reported to treat disease in psoriasiform (psoriasis-like) SCID (severe combined immunodeficiency) mouse model. In a Phase 1b placebo-controlled clinical study in patients with plaque psoriasis, ShK-186 administered twice a week (30 or 60 mg/dose/patient) by subcutaneous injection caused improvements with a statistically significant reduction in their PASI (Psoriasis Area and Severity Index) score between baseline and day 32.
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The progestin is a long-acting progestogen ester, which may or may not act as a prodrug. Progesterone derivatives including medroxyprogesterone acetate, algestone acetophenide (dihydroxyprogesterone acetophenide), hydroxyprogesterone caproate, and megestrol acetate are active themselves and are not prodrugs, whereas the testosterone derivative norethisterone enantate is a prodrug of norethisterone. Regardless of whether they are prodrugs or not, steroid esters form a depot and have an extended duration of action due to a depot effect when administered by intramuscular or subcutaneous injection. Because CICs are administered parenterally, they bypass the first-pass effect in the liver and intestines that occurs with oral administration of estrogens.
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Conjugated estrogens (Premarin), which are used in menopausal hormone therapy, and ethinylestradiol, which is used in birth control pills, have been used in transgender women in the past, but are no longer recommended and are rarely used today due to their higher risks of blood clots and cardiovascular problems. Estrogens may be administered orally, sublingually, transdermally/topically (via patch or gel), rectally, by intramuscular or subcutaneous injection, or by an implant. Parenteral (non-oral) routes are preferred, owing to a minimal or negligible risk of blood clots and cardiovascular issues. In addition to producing feminization, estrogens have antigonadotropic effects and suppress gonadal sex hormone production.
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English scientist Robert Robinson was also working on the synthesis of physostigmine, but surprisingly Julian, a relatively unknown scientist at the time, was the successful one. In 1934, while working at St Alfege's Hospital in London, Dr Mary Walker discovered that a subcutaneous injection of physostigmine could temporarily reverse the muscle weakness found in patients suffering from myasthenia gravis. She had noted that the symptoms and signs of myasthenia were similar to those found in curare poisoning, and physostigmine was used as an antidote to curare poisoning at that time. Her article explaining the first case of myasthenia gravis being successfully treated with physostigmine was published in The Lancet in June 1934.
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The receptor belongs to the Class I cytokine family and signals the JAK/STAT pathway. It is available as 11.3 mg powder in a vial for subcutaneous injection upon reconstitution and needs to be protected from the light. For treatment, patients and their doctors need to be enrolled and certified in the Myalept' Risk Evaluation and Mitigation Strategy (REMS) Program because people on this treatment has a risk of developing anti-metreleptin antibodies that decrease the effectiveness of metreleptin, and increased risk of lymphoma. Clinical study with GL patients who took metreleptin had increased insulin sensitivity, as indicated by decreased HbA1c and fasting glucose level, and reduced caloric intake as well as fasting triglyceride levels.
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Cetrorelix (, ), or cetrorelix acetate (, ), sold under the brand name Cetrotide, is an injectable gonadotropin-releasing hormone (GnRH) antagonist. A synthetic decapeptide, it is used in assisted reproduction to inhibit premature luteinizing hormone surges The drug works by blocking the action of GnRH upon the pituitary, thus rapidly suppressing the production and action of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). In addition, cetrorelix can be used to treat hormone-sensitive cancers of the prostate and breast (in pre-/perimenopausal women) and some benign gynaecological disorders (endometriosis, uterine fibroids and endometrial thinning). It is administered as either multiple 0.25 mg daily subcutaneous injections or as a single-dose 3 mg subcutaneous injection.
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Pitrakinra protects allergic cynomolgus monkeys from allergen-induced airways hyper-responsiveness and lung eosinophilia in both prophylactic and therapeutic model settings. Subcutaneous injection of pitrakinra in human patients with severe atopic eczema for 4 weeks or more decreases the eczema clinical score and circulating IgE concentrations, and normalized T-cell subsets. Decreases in Forced Expiratory Volume in 1 s (FEV1) after allergen challenge after 4 weeks of inhalation of pitrakinra supports the hypothesis that dual inhibition of IL-4 and IL-13 can affect the course of the late asthmatic response after experimental allergen challenge. The reduced frequency of spontaneous asthma attacks requiring rescue medication use suggests that the use of pitrakinra improves the control over asthma symptoms.
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Apomorphine, which is a dopamine agonist not orally administered, may be used to reduce off periods and dyskinesia in late PD. Since secondary effects such as confusion and hallucinations are not rare, patients under apomorphine treatment should be closely monitored. Apomorphine can be administered by subcutaneous injection using a small pump which is carried by the patient. A low dose is automatically administered throughout the day, reducing the fluctuations of motor symptoms by providing a steady dose of dopaminergic stimulation. After an initial "apomorphine challenge" in hospital to test its effectiveness and brief patient and primary caregiver (often a spouse or partner), the latter of whom takes over maintenance of the pump.
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A few small studies have also assessed the suppression of testosterone levels with buserelin nasal spray twice a day instead of three times a day. One such study found that testosterone levels in men with prostate cancer were suppressed during treatment with buserelin from 332 ng/dL to 215 ng/dL (28.9% lower than controls) with 200 μg by nasal spray twice a day (400 μg/day total), from 840 ng/dL to 182 ng/dL (71.4% lower than controls) with 500 μg by nasal spray twice a day (1,000 μg/day total), and from 598 ng/dL to 126 ng/dL (80.4% lower than controls) with 50 μg by subcutaneous injection once a day.
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Alirocumab is used as a second-line treatment to lower LDL cholesterol for adults who have a severe form of hereditary high cholesterol and people with atherosclerosis who require additional lowering of LDL cholesterol when diet and statin treatment have not worked. See FDA index page for BLA 125559 It is administered by subcutaneous injection. As of July 2015, it is not known whether alirocumab prevents early death from cardiovascular disease or prevents heart attacks; a clinical trial to determine outcomes was ongoing at that time, the results of which were expected in 2017. The New England journal of medicine published on the 7th of November 2018 positive results from a clinical trial with Alirocumab (Praluent).
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However, it is inactive orally and must be administered via subcutaneous injection. Remarkably, despite having a very short half-life of only 15–30 minutes, in most or all studies assessing its efficacy nemifitide has been administered merely once daily via the subcutaneous route and yet is effective for depression. The mechanism of action of nemifitide is unclear, but since MIF-1 has been demonstrated to have similar antidepressant effects it may act in an analogous manner. Possibly of interest however is that nemifitide binds to several receptors including 5-HT2A (where it has been shown to act as an antagonist), NPY1, bombesin, and MC4 and MC5, though at only micromolar concentrations.
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Brown also wrote, 'At first this new hypodermic method was employed exclusively for the administration of morphia and preparations of opium, but it is important to note that, from the outset, Dr Wood pointed to a far wider application.' In referring to the preface of a paper on '"New Method of Treating Neuralgia by Subcutaneous Injection," separately published in 1855', Brown quotes Wood as saying, 'In all probability, what is true in regard to narcotics would be found to be equally true in regard to other classes of remedies.' Wood was elected President of the Royal College of Physicians of Edinburgh in 1858. In 1863 he was elected a Fellow of the Royal Society of Edinburgh his proposer being James David Forbes.
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"Single-Dose PRO 140 Has Lasting Effects". 21 Sept 2007. POZ.com. Compared to highly-active antiretroviral therapy which has been shown to have treatment-related toxicities for HIV-infected patients, PRO140 has no multi- drug resistance or toxicities. In February 2018 CytoDyn Inc reported that the primary endpoint has been achieved in the PRO 140 pivotal combination therapy trial in HIV infection and will continue for an additional 24 weeks (end of August 2018) with PRO 140 weekly subcutaneous injections and optimized ART. The report discloses that a single 350 mg subcutaneous injection of PRO 140 resulted in a HIV-1 RNA viral load reduction greater than 0.5log or 68% within one week compared with those who received a placebo.
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Like all other species in the genus Bothrops, the jararacussu has rather potent venom, potent enough to kill sixteen people. The venom is citotoxic, hemotoxic and myotoxic, one study with 29 bites of jararacussu in the state of São Paulo, Brazil showed symptoms like severe local necrosis, shock, spontaneous systemic bleeding, renal failure, coagulopathy, local abscesses, respiratory and circulatory failure, acute renal tubular necrosis, cerebral edema, haemorrhagic rhabdomyolysis at the site of the bite and disseminated intravascular coagulation. Cerebral hemorrhage and kidney failure have already been reported, in a man bitten by a young jararacussu. The LD50 value is 0.14 mg/kg (intravenous injection), 4.92 mg/kg (subcutaneous injection) and 2.73 mg/kg (intraperitoneal injection), while the venom yield is 1000 mg, enough to kill 10,163 rats.
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Although estriol is an efficacious agonist of the ERs, it is reported to have mixed agonist–antagonist (partial agonist) activity at the ER; on its own, it is weakly estrogenic, but in the presence estradiol, it is antiestrogenic. Given by subcutaneous injection in mice, estradiol is about 10-fold more potent than estrone and about 100-fold more potent than estriol. It is notable that unlike estriol, estrone can be metabolized into estradiol, and most of its potency in vivo is in fact actually due to conversion into estradiol. In addition to acting as an agonist of the nuclear ERs, estriol at high concentrations (~1,000–10,000 nM) also acts as an antagonist of the GPER, a membrane estrogen receptor where, conversely, estradiol acts as an agonist.
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Sex hormone levels, including those of estradiol and progesterone, are similarly profoundly suppressed in premenopausal women. The suppression of estradiol levels is 95% and progesterone levels are less than 1 ng/mL (normal range during the luteal phase approximately 10–20 ng/mL); the resulting levels are equivalent to those in postmenopausal women. Buserelin has been found to suppress testosterone levels in men with prostate cancer from 426 ng/dL to 28 ng/dL (by 93.4%) with 200 μg by subcutaneous injection once per day and from 521 ng/dL to 53 ng/dL (by 89.8%) with 400 μg by nasal spray once every 8 hours (1,200 μg/day total). The difference in suppression may have been due to poor compliance.
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Estradiol is an estrogen, or an agonist of the nuclear estrogen receptors (ERs), the estrogen receptor alpha (ERα) and the estrogen receptor beta (ERβ). In one study, the value of estradiol for the human ERα was 50 pM (0.05 nM) and for the human ERβ was 200 pM (0.2 nM). Estradiol is also an agonist of the membrane estrogen receptors (mERs), including the G protein- coupled estrogen receptor (GPER) (3–6 nM), Gq-coupled membrane estrogen receptor (Gq-mER), ER-X, and ERx. It is far more potent as an estrogen than are other natural and bioidentical estrogens like estrone and estriol. Given by subcutaneous injection in mice, estradiol is about 10-fold more potent than estrone and about 100-fold more potent than estriol.
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Triphenylchloroethylene (TPCE; brand names Gynosone, Oestrogyl), or triphenylchlorethylene, also known as chlorotriphenylethylene or as phenylstilbene chloride, is a synthetic nonsteroidal estrogen of the triphenylethylene group that was marketed in the 1940s for the treatment of menopausal symptoms, vaginal atrophy, lactation suppression, and all other estrogen-indicated conditions. The estrogenic effects of triphenylethylene, the parent compound of triphenylchloroethylene, were discovered in 1937. Triphenylchloroethylene was first reported in 1938 and was found to have 20 to 100 times the estrogenic activity of the relatively weak triphenylethylene, a potentiation of effect that was afforded by its halogen substituent. The drug has a relatively long duration of action when administered via subcutaneous injection but a duration similar to that of diethylstilbestrol or estradiol benzoate when administered orally.
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However, the dosages of spironolactone used in animals to produce progestogenic effects were very high (50–200 mg/kg/day in rabbits, 400 mg/day in rhesus monkeys). In one study, the threshold dose by subcutaneous injection for endometrial transformation in rabbits was 0.003–0.01 mg for cyproterone acetate, 0.1–0.3 mg for drospirenone, 0.5 mg for progesterone, and 10–20 mg for spironolactone. Spironolactone orally at 40 mg/kg/day failed to show an antigonadotropic effect or decrease testosterone levels in male cynomolgus monkeys, whereas oral drospirenone at 4 mg/day was effective and strongly suppressed testosterone levels. In addition, no evidence of progestogenic nor antiprogestogenic effects (as assessed by endometrial changes) have been observed in women even with high doses of spironolactone.
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However, whereas fulvestrant is not orally active and must be administered via intramuscular injection, ZB716 is less susceptible to first-pass metabolism, and in relation to this, is orally active. A single oral dose of 8.3 mg/kg ZB716 to mice has been found to result in an over 160 ng/mL maximal concentration of the drug in circulation, a level far in excess of the 15.2 ng/mL concentration achieved with subcutaneous injection of fulvestrant in mice. As such, not only may ZB716 be more convenient to administer in humans, it has far greater bioavailability compared to fulvestrant and hence may allow for greater systemic exposure and therapeutic benefit. ZB716 produces fulvestrant as an active metabolite in vivo in mice, with approximately 10 to 15% of the drug being converted into it.
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A jet injector being used in mass vaccinations, 1976 swine flu outbreak, United States. A jet injector is a type of medical injecting syringe device used for a method of drug delivery known as jet injection, in which a narrow, high-pressure stream of liquid penetrates without needle the outermost layer of the skin (stratum corneum) to deliver medication to targeted underlying tissues of the epidermis or dermis ("cutaneous" injection, also known as classical "intradermal" injection), fat ("subcutaneous" injection), or muscle ("intramuscular" injection). The jet stream is usually generated by the pressure of a piston in an enclosed liquid-filled chamber. The piston is usually pushed by the release of a compressed metal spring, although investigational devices may use piezoelectric effects and other novel technologies to pressurize the liquid in the chamber.
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An injectable form of glucagon may be part of first aid in cases of low blood sugar when the person is unconscious or for other reasons cannot take glucose orally or by intravenous. The glucagon is given by intramuscular, intravenous or subcutaneous injection, and quickly raises blood glucose levels. To use the injectable form, it must be reconstituted prior to use, a step that requires a sterile diluent to be injected into a vial containing powdered glucagon, because the hormone is highly unstable when dissolved in solution. When dissolved in a fluid state, glucagon can form amyloid fibrils, or tightly woven chains of proteins made up of the individual glucagon peptides, and once glucagon begins to fibrilize, it becomes useless when injected, as the glucagon cannot be absorbed and used by the body.
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Insulin degludec (INN/USAN) is an ultralong-acting basal insulin analogue that was developed by Novo Nordisk under the brand name Tresiba. It is administered via subcutaneous injection once daily to help control the blood sugar level of those with diabetes. It has a duration of action that lasts up to 42 hours (compared to 18 to 26 hours provided by other marketed long-acting insulins such as insulin glargine and insulin detemir), making it a once-daily basal insulin, that is one that provides a base insulin level, as opposed to the fast- and short-acting bolus insulins. Insulin degludec is a modified insulin that has one single amino acid deleted in comparison to human insulin, and is conjugated to hexadecanedioic acid via gamma-L-glutamyl spacer at the amino acid lysine at position B29.
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It was approved in Europe in 1999.Roche. March 04, 1999 Roche Press Release: Zenapax (daclizumab), The First Humanized Monoclonal Antibody To Prevent Organ Rejection, Approved In The European Union PDL began clinical trials of daclizumab on its own, and in September 2004 after the drug had shown promise in a Phase II trial, PDL and Roche agreed to expand their relationship to include codevelopment of daclizumab for asthma and other respiratory conditions.Candace Hoffmann for First Word Pharma. September 16, 2004 Roche in new deal to co-development asthma drug In August 2005, PDL and Biogen Idec agreed to collaborate to develop daclizumab in indications outside the fields of organ rejection and respiratory disease. In November 2005 Roche and PDL agreed to try to develop a formulation of daclizumab that would be useful as a subcutaneous injection for longterm maintenance in organ transplant.
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Racemic synephrine, given intramuscularly, or by instillation, was found to significantly reduce the inflammation caused by instillation of mustard oil into the eyes of rabbits. Subcutaneous injection of racemic synephrine into rabbits was reported to cause a large rise in blood sugar. In experiments on anesthetized cats, Papp and Szekeres found that synephrine (stereochemistry unspecified) raised the thresholds for auricular and ventricular fibrillation, an indication of anti-arrhythmic properties. Evidence that synephrine might have some central effects comes from the research of Song and co-workers, who studied the effects of synephrine in mouse models of anti-depressant activity. These researchers observed that oral doses of 0.3 – 10 mg/kg of racemic synephrine were effective in shortening the duration of immobility produced in the assays, but did not cause any changes in spontaneous motor activity in separate tests.
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MPA is available alone in the form of 2.5, 5, and 10 mg oral tablets, as a 150 mg/mL (1 mL) or 400 mg/mL (2.5 mL) microcrystalline aqueous suspension for intramuscular injection, and as a 104 mg (0.65 mL of 160 mg/mL) microcrystalline aqueous suspension for subcutaneous injection. It has also been marketed in the form of 100, 200, 250, 400, and 500 mg oral tablets; 500 and 1,000 mg oral suspensions; and as a 50 mg/mL microcrystalline aqueous suspension for intramuscular injection. A 100 mg/mL microcrystalline aqueous suspension for intramuscular injection was previously available as well. In addition to single-drug formulations, MPA is available in the form of oral tablets in combination with conjugated estrogens (CEEs), estradiol, and estradiol valerate for use in menopausal hormone therapy, and is available in combination with estradiol cypionate in a microcrystalline aqueous suspension as a combined injectable contraceptive.
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The muscular lightweight body of the Taipan allows it to hurl itself forwards or sideways and reach high off the ground, and such is the speed of the attack that a person may be bitten several times before realizing the snake is there. This snake is considered to be one of the most venomous in the world. Ernst and Zug et al. 1996 and the Australian venom and toxin database both list a value of 0.106 mg/kg for subcutaneous injection. Engelmann and Obst (1981) list value of 0.12 mg/kg SC, with an average venom yield of 120 mg per bite and a maximum record of 400 mg. To demonstrate just how deadly this species is, an estimate was made on the number of mice and adult human fatalities it is capable of causing in a single bite that yields the maximum dose of 400 mg.
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The Murphy drip was invented by Wisconsin surgeon John Benjamin Murphy, for the purpose of administering a proctoclysis for hydration and replenishment of electrolytes, via a sodium and calcium chloride solution. This would be used when administration by mouth was not possible because of the condition of the patient.Morgenstern, Leon, "John Benjamin Murphy (1857-1916): An American Surgical Phenomenon", Surgical Innovation, vol 13, No 1, pp1-3, Sage Publications, March 2006 The Murphy drip was described in the April 1909 issue of the Journal of the American Medical Association.Journal of the American Medical Association (April 17, 1909) Proctoclysys in the Treatment of Peritonitis (the Murphy Drip). By as early as July 1928, the Murphy drip was considered an auxiliary method of injection behind intravenous therapy and subcutaneous injection, the two principal methods of injection at that time.Homer R. Spence (November 3, 1933) California Courts of Appeal, First District, Division 2.
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The report discloses that a single 350mg subcutaneous injection of PRO 140 resulted in a HIV-1 RNA viral load reduction greater than 0.5log or 68% within one week compared with those who received a placebo. The primary efficacy endpoint results were presented at ASM Microbe 2018. In the pivotal trial of Leronlimab in combination with standard anti-retroviral therapies in HIV- infected treatment-experienced patients, 81% of patients completing trial achieved HIV viral load suppression of < 50 cp/mL. Recent approved drugs for this population range from 43% after 24 weeks to 45% after 48 weeks with viral load suppression of < 50 cp/mL. In March 2019 CytoDyn filed with the US FDA the first part of the BLA for leronlimab (PRO140) as a combination therapy with HAART in HIV. In December 2019, the company affirmed plans to complete the BLA in January 2020 with potential FDA approval in 2Q'20.
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In 1993, interferon beta-1b was the first drug to ever be approved for MS, being soon followed by interferon beta-1a and glatiramer acetate. Interferon beta-1a is injected either weekly (intramuscular injection) or three times a week (subcutaneous injection) depending on commercial formulations, while interferon beta-1b is injected subcutaneously every second day. In 2014, a pegylated form of interferon beta-1a was introduced with the brand name Plegridy, which is available as a subcutaneous injection.Plegridy Prescribing Information Biogen Idec Inc. Plegridy Prescribing Information (August 2014). Retrieved on 31 October 2014 This peginterferon beta 1-a attaches polyethylene glycol to the interferon molecules allowing longer lasting biological effects in the body while decreasing the frequency of administration to once every two weeks.Peginterferon beta-1a description National Multiple Sclerosis Society (15 August 2014). Retrieved on 27 October 2014 Interferon beta balances the expression of pro- and anti-inflammatory agents in the brain, and reduces the number of inflammatory cells that cross the blood–brain barrier.
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Estetrol levels following a single dose of different doses of oral estetrol (E4) in postmenopausal women. Estetrol shows high oral bioavailability. Its oral bioavailability in rats was 70% relative to subcutaneous injection. The high oral bioavailability of estetrol is in contrast to estradiol, estrone, and estriol (all very low, in the range of 5% and below), but is more similar to ethinylestradiol (38–48%). Estetrol shows a high and linear dose–response relationship across oral doses of 0.1 to 100 mg in humans, and shows low interindividual variability. Upon oral administration, estetrol is very rapidly absorbed, with maximal levels occurring within 15 to 80 minutes. At a dosage of 20 mg/day estetrol, peak levels of estetrol of 3,490 pg/mL and trough levels of 2,005 pg/mL have been reported. The high water solubility of estetrol makes it optimal for passage of the blood–brain barrier, and the drug may be expected to have effects in the central nervous system.
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