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Sumatriptan

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39-605: Sumatriptan , sold under the brand name Imitrex among others, is a medication used to treat migraine headaches and cluster headaches . It is taken orally , intranasally , or by subcutaneous injection . Therapeutic effects generally occur within three hours. Its primary effect as a serotonin 5-HT1B / 5-HT1D receptor agonist can create common side effects such as chest pressure , fatigue, vomiting, tingling, and vertigo . Serious side effects may include serotonin syndrome , heart attacks , strokes , and seizures . With excessive use, medication overuse headaches may occur. It

78-435: A critical role, often then selling the rights to larger companies that have the resources to run the clinical trials. Drug discovery is different from Drug Development. Drug Discovery is often considered the process of identifying new medicine. At the same time, Drug development is delivering a new drug molecule into clinical practice. In its broad definition, this encompasses all steps from the basic research process of finding

117-575: A group of 2245 elderly Americans (average age of 71) surveyed over the period 2010 – 2011, those percentages were 88%, 38%, and 64%. One of the key classifications is between traditional small molecule drugs; usually derived from chemical synthesis and biological medical products ; which include recombinant proteins , vaccines , blood products used therapeutically (such as IVIG ), gene therapy , and cell therapy (for instance, stem cell therapies). Pharmaceuticals or drugs or medicines are classified into various other groups besides their origin on

156-410: A limit on the amount of pills available to a patient per month, which has been called "arbitrary and unfair." Medication A medication (also called medicament , medicine , pharmaceutical drug , medicinal drug or simply drug ) is a drug used to diagnose , cure , treat, or prevent disease. Drug therapy ( pharmacotherapy ) is an important part of the medical field and relies on

195-505: A list of essential medicines . A sampling of classes of medicine includes: Pharmaceuticals may also be described as "specialty", independent of other classifications, which is an ill-defined class of drugs that might be difficult to administer, require special handling during administration, require patient monitoring during and immediately after administration, have particular regulatory requirements restricting their use, and are generally expensive relative to other drugs. Drugs affecting

234-569: A pharmacist and is only available in packs of two without a medical prescription. However, it can be bought over the counter in the UK and Sweden. In Russia, versions of sumatriptan which are not registered in the State Register of Medicines may be regarded as narcotic drugs (derivatives of dimethyltryptamine ). Glaxo patents for sumatriptan expired in February 2009. At that time, Imitrex sold for about $ 25

273-461: A pill. Par Pharmaceutical then introduced generic versions of sumatriptan injection (sumatriptan succinate injection) 4- and 6-mg starter kits and 4- and 6-mg filled syringe cartridges, and 6-mg vials soon after. Mylan Laboratories Inc. , Ranbaxy Laboratories , Sandoz (a subsidiary of Novartis ), Dr. Reddy's Laboratories , and other companies have been producing generic versions of sumatriptan tablets in 25-, 50-, and 100-mg doses. Generic forms of

312-612: A pre-programmed microchip to deliver a single dose of sumatriptan through the skin within 30 minutes. Zecuity was approved by the US FDA in January 2013. Sales of Zecuity have been stopped following reports of skin burns and irritation. In the United States, it is available only by medical prescription. It is available over the counter in many states in Australia. The product requires labelling by

351-452: A process known as reverse pharmacology . Hits from these screens are then tested in cells and then in animals for efficacy . Even more recently, scientists have been able to understand the shape of biological molecules at the atomic level and to use that knowledge to design (see drug design ) drug candidates. Modern drug discovery involves the identification of screening hits, medicinal chemistry , and optimization of those hits to increase

390-411: A process of identifying a new medicine. Development: Chemicals extracted from natural products are used to make pills, capsules, or syrups for oral use. Injections for direct infusion into the blood drops for eyes or ears. Preclinical research : Drugs go under laboratory or animal testing, to ensure that they can be used on Humans. Clinical testing: The drug is used on people to confirm that it

429-499: A suitable molecular target to supporting the drug's commercial launch. Drug development is the process of bringing a new drug to the market once a lead compound has been identified through the process of drug discovery . It includes pre-clinical research (microorganisms/animals) and clinical trials (on humans) and may include the step of obtaining regulatory approval to market the drug. Drug Development Process Discovery: The Drug Development process starts with Discovery,

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468-595: A vein , or by drops put into the ear or eye . A medication that does not contain an active ingredient and is used in research studies is called a placebo . In Europe, the term is "medicinal product", and it is defined by EU law as: In the US, a "drug" is: Drug use among elderly Americans has been studied; in a group of 2,377 people with an average age of 71 surveyed between 2005 and 2006, 84% took at least one prescription drug, 44% took at least one over-the-counter (OTC) drug, and 52% took at least one dietary supplement ; in

507-493: Is a medicine or a chemical compound used to treat or cure illness. According to Encyclopædia Britannica , medication is "a substance used in treating a disease or relieving pain ". As defined by the National Cancer Institute , dosage forms of medication can include tablets , capsules , liquids, creams , and patches. Medications can be administered in different ways, such as by mouth , by infusion into

546-511: Is between traditional small molecule drugs, usually derived from chemical synthesis , and biopharmaceuticals , which include recombinant proteins , vaccines , blood products used therapeutically (such as IVIG ), gene therapy , monoclonal antibodies and cell therapy (for instance, stem cell therapies). Other ways to classify medicines are by mode of action, route of administration , biological system affected, or therapeutic effects . An elaborate and widely used classification system

585-428: Is molecularly similar to serotonin (5-HT), and is a 5-HT receptor (types 5-HT 1D and 5-HT 1B ) agonist . Sumatriptan's primary therapeutic effect is related in its inhibition of the release of Calcitonin gene-related peptide (CGRP), likely through its 5-HT 1D/1B receptor-agonist action. This has been substantiated by the efficacy of more recently developed CGRP targeting drugs and antibodies developed for

624-422: Is safe to use. FDA Review: drug is sent to FDA before launching the drug into the market. FDA post-Market Review: The drug is reviewed and monitored by FDA for the safety once it is available to the public. The regulation of drugs varies by jurisdiction. In some countries, such as the United States, they are regulated at the national level by a single agency. In other jurisdictions, they are regulated at

663-523: Is still a lengthy, "expensive, difficult, and inefficient process" with a low rate of new therapeutic discovery. In 2010, the research and development cost of each new molecular entity (NME) was approximately US$ 1.8 billion. Drug discovery is done by pharmaceutical companies, sometimes with research assistance from universities. The "final product" of drug discovery is a patent on the potential drug. The drug requires very expensive Phase I, II, and III clinical trials, and most of them fail. Small companies have

702-778: Is the Anatomical Therapeutic Chemical Classification System . The World Health Organization keeps a list of essential medicines . Drug discovery and drug development are complex and expensive endeavors undertaken by pharmaceutical companies , academic scientists, and governments. As a result of this complex path from discovery to commercialization, partnering has become a standard practice for advancing drug candidates through development pipelines. Governments generally regulate what drugs can be marketed, how drugs are marketed , and in some jurisdictions, drug pricing . Controversies have arisen over drug pricing and disposal of used Medicine . Medication

741-475: Is unclear if use during pregnancy or breastfeeding is safe. The mechanism of action is not entirely clear. It is in the triptan class of medications. Sumatriptan was patented in 1982 and approved for medical use in 1991. It is on the World Health Organization's List of Essential Medicines . It is available as a generic medication . In 2022, it was the 95th most commonly prescribed medication in

780-406: Is used for euthanasia and physician-assisted suicide . Euthanasia is not permitted by law in many countries, and consequently, medicines will not be licensed for this use in those countries. A single drug may contain single or multiple active ingredients . The administration is the process by which a patient takes medicine. There are three major categories of drug administration: enteral (via

819-469: Is used per day (e.g., four times a day). It may include event-related information (e.g., 1 hour before meals, in the morning, at bedtime), or complimentary to an interval, although equivalent expressions may have different implications (e.g., every 8 hours versus 3 times a day). In the fields of medicine, biotechnology , and pharmacology , drug discovery is the process by which new drugs are discovered. Historically, drugs were discovered by identifying

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858-506: The affinity , selectivity (to reduce the potential of side effects), efficacy/ potency , metabolic stability (to increase the half-life ), and oral bioavailability . Once a compound that fulfills all of these requirements has been identified, it will begin the process of drug development prior to clinical trials . One or more of these steps may, but not necessarily, involve computer-aided drug design . Despite advances in technology and understanding of biological systems, drug discovery

897-3535: The central nervous system include psychedelics , hypnotics , anaesthetics , antipsychotics , eugeroics , antidepressants (including tricyclic antidepressants , monoamine oxidase inhibitors , lithium salts , and selective serotonin reuptake inhibitors (SSRIs)), antiemetics , anticonvulsants /antiepileptics, anxiolytics , barbiturates , movement disorder (e.g., Parkinson's disease ) drugs, nootropics , stimulants (including amphetamines ), benzodiazepines , cyclopyrrolones , dopamine antagonists , antihistamines , cholinergics , anticholinergics , emetics , cannabinoids , and 5-HT (serotonin) antagonists . The main classes of painkillers are NSAIDs , opioids , and local anesthetics . For consciousness (anesthetic drugs) Some anesthetics include benzodiazepines and barbiturates . The main categories of drugs for musculoskeletal disorders are: NSAIDs (including COX-2 selective inhibitors ), muscle relaxants , neuromuscular drugs , and anticholinesterases . Antibiotics , sympathomimetics , antihistamines , anticholinergics , NSAIDs , corticosteroids , antiseptics , local anesthetics , antifungals , and cerumenolytics. Bronchodilators , antitussives , mucolytics , decongestants , inhaled and systemic corticosteroids , beta2-adrenergic agonists , anticholinergics , mast cell stabilizers , leukotriene antagonists . Androgens , antiandrogens , estrogens , gonadotropin , corticosteroids , human growth hormone , insulin , antidiabetics ( sulfonylureas , biguanides / metformin , thiazolidinediones , insulin ), thyroid hormones , antithyroid drugs, calcitonin , diphosphonate , vasopressin analogues . Antifungal , alkalinizing agents , quinolones , antibiotics , cholinergics , anticholinergics , antispasmodics , 5-alpha reductase inhibitor , selective alpha-1 blockers , sildenafils , fertility medications . NSAIDs , anticholinergics , haemostatic drugs , antifibrinolytics , Hormone Replacement Therapy (HRT), bone regulators, beta-receptor agonists , follicle stimulating hormone , luteinising hormone , LHRH , gamolenic acid , gonadotropin release inhibitor , progestogen , dopamine agonists , oestrogen , prostaglandins , gonadorelin , clomiphene , tamoxifen , diethylstilbestrol . Emollients , anti-pruritics , antifungals , antiseptics , scabicides , pediculicides , tar products, vitamin A derivatives , vitamin D analogues , keratolytics , abrasives , systemic antibiotics , topical antibiotics , hormones , desloughing agents, exudate absorbents, fibrinolytics , proteolytics , sunscreens , antiperspirants , corticosteroids , immune modulators. Antibiotics , antifungals , antileprotics , antituberculous drugs , antimalarials , anthelmintics , amoebicides , antivirals , antiprotozoals , probiotics, prebiotics, antitoxins , and antivenoms. Vaccines , immunoglobulins , immunosuppressants , interferons , and monoclonal antibodies . Anti-allergics , antihistamines , NSAIDs , corticosteroids . Tonics, electrolytes and mineral preparations (including iron preparations and magnesium preparations ), parenteral nutrition , vitamins , anti-obesity drugs , anabolic drugs , haematopoietic drugs, food product drugs. Cytotoxic drugs , therapeutic antibodies , sex hormones , aromatase inhibitors , somatostatin inhibitors, recombinant interleukins , G-CSF , erythropoietin . Contrast media . A euthanaticum

936-410: The human gastrointestinal tract ), injection into the body, and by other routes ( dermal , nasal , ophthalmic , otologic , and urogenital ). Oral administration , the most common form of enteral administration, can be performed using various dosage forms including tablets or capsules and liquid such as syrup or suspension. Other ways to take the medication include buccally (placed inside

975-411: The United States, with more than 6   million prescriptions. It is also available as the combination product sumatriptan/naproxen . Sumatriptan is effective for ending or relieving the intensity of migraine and cluster headaches . It is most effective when taken early after the start of the pain. Injected sumatriptan is more effective than other formulations. Oral sumatriptan can be used also in

1014-643: The active ingredient from traditional remedies or by serendipitous discovery. Later chemical libraries of synthetic small molecules , natural products , or extracts were screened in intact cells or whole organisms to identify substances that have a desirable therapeutic effect in a process known as classical pharmacology . Since sequencing of the human genome which allowed rapid cloning and synthesis of large quantities of purified proteins, it has become common practice to use high throughput screening of large compound libraries against isolated biological targets which are hypothesized to be disease-modifying in

1053-399: The basis of pharmacological properties like mode of action and their pharmacological action or activity, such as by chemical properties , mode or route of administration , biological system affected, or therapeutic effects . An elaborate and widely used classification system is the Anatomical Therapeutic Chemical Classification System (ATC system). The World Health Organization keeps

1092-400: The cheek), sublingually (placed underneath the tongue), eye and ear drops (dropped into the eye or ear), and transdermally (applied to the skin). They can be administered in one dose, as a bolus . Administration frequencies are often abbreviated from Latin, such as every 8 hours reading Q8H from Quaque VIII Hora . The drug frequencies are often expressed as the number of times a drug

1131-561: The drug are available in U.S. and European markets after Glaxo's patent protections expired in the respective countries. A nasal spray form of sumatriptan known as AVP-825 has been developed by Avanir and is generically available in some countries. According to the American Headache Society , "Patients frequently state that they have difficulty accessing triptans prescribed to them." In the U.S. triptans cost from $ 12 to $ 120 each, and more than 80% of U.S. health insurance plans place

1170-432: The drug has been shown to abort a cluster headache within 30 minutes in 77% of cases. Sumatriptan is administered in several forms: tablets, subcutaneous injection , and nasal spray. Oral administration (as succinate salt) has low bioavailability , partly due to presystemic metabolism —some of it gets broken down in the stomach and bloodstream before it reaches the target arteries. A rapid-release tablet formulation with

1209-455: The placebo group and 5–6% in the sumatriptan groups, pain and other pressure sensations (including chest pain) reported by 4% in the placebo group and 6–8% in the sumatriptan groups, neurological events ( vertigo ) reported by less than 1% in the placebo group and less than 1% to 2% in the sumatriptan groups. Malaise/fatigue occurred in less than 1% of the placebo group and 2–3% of the sumatriptan groups. Sleep disturbance occurred in less than 1% in

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1248-429: The placebo group to 2% in the sumatriptan group. Concurrent use with other triptans or ergot-containing medications within 24 hours can result in additive vasoconstriction . Increased systemic exposure to sumatriptan can occur if used within 2 weeks after a monoamine oxidase inhibitor . Cases of serotonin syndrome have been reported with co-administration of triptans and serotonin reuptake inhibitors . Sumatriptan

1287-439: The preventive treatment of migraine. How agonism of the 5-HT 1D/1B receptors inhibits CGRP release is not fully understood. CGRP is believed to cause sensitization of trigeminal nociceptive neurons, contributing to the pain experienced in migraine. Sumatriptan is also shown to decrease the activity of the trigeminal nerve , which presumably accounts for sumatriptan's efficacy in treating cluster headaches. The injectable form of

1326-463: The same bioavailability but a high concentration can achieve therapeutic effects on average 10–15 minutes earlier than other oral forumulations. 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 2-{5-[(methylsulfamoyl)methyl]-indole-3-yl}acetic acid, which is then conjugated to glucuronic acid . These metabolites are excreted in

1365-451: The science of pharmacology for continual advancement and on pharmacy for appropriate management. Drugs are classified in many ways. One of the key divisions is by level of control , which distinguishes prescription drugs (those that a pharmacist dispenses only on the order of a physician, physician assistant , or qualified nurse ) from over-the-counter drugs (those that consumers can order for themselves). Another key distinction

1404-464: The state level, or at both state and national levels by various bodies, as is the case in Australia. The role of therapeutic goods regulation is designed mainly to protect the health and safety of the population. Regulation is aimed at ensuring the safety, quality, and efficacy of the therapeutic goods which are covered under the scope of the regulation. In most jurisdictions, therapeutic goods must be registered before they are allowed to be marketed. There

1443-844: The treatment of post-dural puncture headache. Overdose of sumatriptan can cause sulfhemoglobinemia , a rare condition in which the blood changes from red to green, 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 sumatriptan injection or tablets. Events reported have included coronary artery vasospasm , transient myocardial ischemia, myocardial infarction , ventricular tachycardia , and ventricular fibrillation . The most common side effects reported by at least 2% of patients in controlled trials of sumatriptan (25-, 50-, and 100-mg tablets) for migraine are atypical sensations (paresthesias and warm/cold sensations) reported by 4% in

1482-488: The urine and bile. Only about 3% of the active drug may be recovered unchanged. There is no simple, direct relationship between sumatriptan concentration (pharmacokinetics) per se in the blood and its anti-migraine effect (pharmacodynamics). This paradox has, to some extent, been resolved by comparing the rates of absorption of the various sumatriptan formulations, rather than the absolute amounts of drug that they deliver. In 1991, Glaxo received approval for sumatriptan, which

1521-548: Was the first available triptan . In July 2009, the US FDA approved a single-use jet injector formulation of sumatriptan. The device delivers a subcutaneous injection of sumatriptan, without the use of a needle. Autoinjectors with needles have been previously available in Europe and North America. Phase III studies with an iontophoretic transdermal patch (Zelrix/Zecuity) started in July 2008. This patch uses low voltage controlled by

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