imitrex
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imitrex
SumatriptanSystematic (IUPAC) name1-- N-methyl-methanesulfonamideIdentifiersCAS number103628-46-2ATC codeN02CC01PubChem5358DrugBankAPRD00379ChemSpider5165Chemical dataFormulaC14H21N3O2S Mol. mass295.402 g/molSMILESeMolecules & PubChemPharmacokinetic dataBioavailability15% (oral)/ 96% (s.c)Protein binding14%-21%MetabolismMAOHalf life2.5 hoursExcretion60% urine; 40% fecesTherapeutic considerationsLicence dataUS FDA:linkPregnancy cat.CLegal statusRoutestablet, subcutaneous injection, nasal spraySumatriptan (trade names Imitrex, Imigran, Imigran recovery) is a triptan drug including a sulfonamide group for the treatment of migraine headaches. It is marketed and manufactured by GlaxoSmithKline.// Approval and availabilityThis section may require copy-editing for grammar, style, cohesion, tone or spelling. You can assist by editing it now. A how-to guide is available. (November 2008)Several dosage forms for sumatriptan have been approved, including tablets, solution for injection, and nasal inhalers. Sumatriptan was the first triptan available (in 1991), and, in the United States and most developed countries, is available only by medical prescription. In the United Kingdom, sumatriptan is available over the counter, under the name Imigran Recovery. It is sold in packs of two 50mg tablets for approximately £7.99 (about $15 US). Larger pack sizes, the nasal spray, and the liquid preparation for injection are still only available by prescription. Originally covered by UK Patent GB2162522, extended by supplementary protection certificate SPC/GB93/071, protection in the UK (as well as the rest of Europe), expired on 16 May 2006. Through patent litigation, Glaxo was able to extend their US patent considerably beyond this date. However, as the result of a lawsuit by the maker of a generic version of the injectable version of Imitrex, a settlement should allow this generic to come to the market in the US in August 2008.On April 15, 2008, the US FDA approved a combination of sumatriptan and naproxen, an NSAID, which will be marketed under the brand name Treximet. This combination has shown a benefit over either medicine used separately. Mode of actionSumatriptan is structurally similar to serotonin (5HT), and is a 5-HT (types 5-HT1D and 5-HT1B) agonist. The specific receptor subtypes it activates is present in the cerebral arteries. Dilation of these arteries is thought to be a major cause of headache pain, and activating these receptors causes vasoconstriction. Sumatriptan was also shown to decrease the activity of the trigeminal nerve, which may partially explain sumatriptan's efficacy in treating cluster headaches. The injectable form of the drug has been shown to abort a cluster headache within fifteen minutes in 96% of cases. PharmacokineticsSumatriptan is administered in several forms; tablets, subcutaneous injection, and nasal spray. Oral administration (as succinate) 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. Sumatriptan is metabolised primarily by monoamine oxidase A into an indole acetic acid analogue, part of which is further conjugated with glucuronic acid. These metabolites are excreted in the urine and bile. Side EffectsLarge doses of sumatriptan (200 mg/day) can cause sulfhemoglobinemia, a rare condition in which the blood changes from red to greenish-black, due to the integration of sulfur into the hemoglobin molecule. If sumatriptan is discontinued, the condition reverses within a few weeks.Serious cardiac events, including some that have been fatal, have occurred following the use of Imitrex Injection or Tablets. Events reported have included coronary artery vasospasm, transient myocardial ischemia, myocardial infarction, ventricular tachycardia, and ventricular fibrillation.Atypical Sensations Frequent were burning sensation and numbness. Infrequent was tight feeling in head. Rare were dysesthesia.Cardiovascular Frequent were palpitations, syncope, decreased blood pressure, and increased blood pressure. Infrequent were arrhythmia, changes in ECG, hypertension, hypotension, pallor, pulsating sensations, and tachycardia. Rare were angina, atherosclerosis, bradycardia, cerebral ischemia, cerebrovascular lesion, heart block, peripheral cyanosis, thrombosis, transient myocardial ischemia, and vasodilation.Ear, Nose, and Throat Frequent were sinusitis, tinnitus; allergic rhinitis; upper respiratory inflammation; ear, nose, and throat hemorrhage; external otitis; hearing loss; nasal inflammation; and sensitivity to noise. Infrequent were hearing disturbances and otalgia. Rare was feeling of fullness in the ear(s).Endocrine and Metabolic Infrequent was thirst. Rare were elevated thyrotropin stimulating hormone (TSH) levels; galactorrhea; hyperglycemia; hypoglycemia; hypothyroidism; polydipsia; weight gain; weight loss; endocrine cysts, lumps, and masses; and fluid disturbances.Eye Rare were disorders of sclera, mydriasis, blindness and low vision, visual disturbances, eye edema and swelling, eye irritation and itching, accommodation disorders, external ocular muscle disorders, eye hemorrhage, eye pain, and keratitis and conjunctivitis.Gastrointestinal Frequent were diarrhea and gastric symptoms. Infrequent were constipation, dysphagia, and gastroesophageal reflux. Rare were gastrointestinal bleeding, hematemesis, melena, peptic ulcer, gastrointestinal pain, dyspeptic symptoms, dental pain, feelings of gastrointestinal pressure, gastritis, gastroenteritis, hypersalivation, abdominal distention, oral itching and irritation, salivary gland swelling, and swallowing disorders.Hematological Disorders Rare was anemia.Musculoskeletal Frequent was myalgia. Infrequent was muscle cramps. Rare were tetany; muscle atrophy, weakness, and tiredness; arthralgia and articular rheumatitis; acquired musculoskeletal deformity; muscle stiffness, tightness, and rigidity; and musculoskeletal inflammation.Neurological Frequent were phonophobia and photophobia. Infrequent were confusion, depression, difficulty concentrating, disturbance of smell, dysarthria, euphoria, facial pain, heat sensitivity, incoordination, lacrimation, monoplegia, sleep disturbance, shivering, syncope, and tremor. Rare were aggressiveness, apathy, bradylogia, cluster headache, convulsions, decreased appetite, drug abuse, dystonic reaction, facial paralysis, hallucinations, hunger, hyperesthesia, hysteria, increased alertness, memory disturbance, neuralgia, paralysis, personality change, phobia, radiculopathy, rigidity, suicide, twitching, agitation, anxiety, depressive disorders, detachment, motor dysfunction, neurotic disorders, psychomotor disorders, taste disturbances, and raised intracranial pressure.Respiratory Frequent was dyspnea. Infrequent was asthma. Rare were hiccoughs, breathing disorders, cough, and bronchitis.Skin Frequent was sweating. Infrequent were erythema, pruritus, rash, and skin tenderness. Rare were dry/scaly skin, tightness of skin, wrinkling of skin, eczema, seborrheic dermatitis, and skin nodules.Breasts Infrequent was tenderness. Rare were nipple discharge; breast swelling; cysts, lumps, and masses of breasts; and primary malignant breast neoplasm.Urogenital Infrequent were dysmenorrhea, increased urination, and intermenstrual bleeding. Rare were abortion and hematuria, urinary frequency, bladder inflammation, micturition disorders, urethritis, urinary infections, menstruation symptoms, abnormal menstrual cycle, inflammation of fallopian tubes, and menstrual cycle symptoms.Miscellaneous Frequent was hypersensitivity. Infrequent were fever, fluid retention, and overdose. Rare were edema, hematoma, lymphadenopathy, speech disturbance, voice disturbances, contusions. GenericsOn November 6, 2008, Par Pharmaceutical announced that it would begin shipping generic versions of Imitrex Injection (sumatriptan succinate injection) 4mg and 6mg starter kits and 4mg and 6mg pre-filled syringe cartridges to the trade immediately. In addition, Par anticipates launching the 6mg vials early in 2009. Mylan Laboratories Inc. has received FDA approval for its generic version of Imitrex tablets in 25, 50, and 100 milligram doses. The drug will soon be available, or is already available, in European markets since Glaxo's patent protections have expired in those jurisdictions. However, sales of the generic drug are still restricted in the U.S. since Glaxo won an extension on their patent until 2009. A generic version of the drug in tablet form became available December 2008 in the United States and is distributed by Ranbaxy.
. The effectiveness of the amount 4mg of injection of Imitrex was established in three studies.. Pharmaceutical company Zogenix has developed an alternate delivery method for administration of sumatriptan, the active ingredient in Imitrex.Combining two commonly used medications can provide faster, long-lasting relief of migraine pain than using either drug alone, concludes a new study. The study compared the use of a new combination pill that includes sumatriptan (brand name Imitrex) and naproxen sodium (Aleve) to use of either drug alone and to a placebo for moderate to severe[. I'm now 43 and the last two years I've been able to control them without medication ( such as imitrex ).. As this Fall rolls in, change your Imitrex prescription to the generic Sumatriptans and Naproxen.Of course, the ones who've read this article will have the option of saving at least 2/3 of the cost on the migraine abortives. Here's what migraine sufferers should know about this bait-and-switchEven without an ability to time-travel (one looses it as one grows older, as you know) it was made possible by combining.]. Generic Imitrex at last! Cheap!Generic Sumatriptan (Imitrex) just hit the market..GlaxoSmithKline just recently got FDA approval for a new migraine medication, Treximet -- but it's
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Imitrex Sumatriptan Succinate
Learn about IMITREX, a medicine used to treat migraines. ... RT Technology TM to dissolve quickly after swallowing.* Current IMITREX Tablets, formulated with RT Technology ...
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