Sumatriptan
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Trade names | Imitrex, Imigran, others |
AHFS/Drugs.com | Monograph |
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subcutaneous injection) | |
Protein binding | 14–21% |
Metabolism | Monoamine oxidase (MAO) |
Elimination half-life | 2.5 hours |
Excretion | 60% urine; 40% feces |
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Sumatriptan, sold under the brand name Imitrex among others, is a
Its primary effect as a serotonin
Sumatriptan was patented in 1982 and approved for medical use in 1991.
Medical uses
Sumatriptan is effective for ending or relieving the intensity of migraine and cluster headaches.[9] It is most effective when taken early after the start of the pain.[9] Injected sumatriptan is more effective than other formulations.[10]
Oral sumatriptan can be used also in the treatment of post-dural puncture headache.[11]
Adverse effects
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.[12] If sumatriptan is discontinued, the condition reverses within a few weeks.[citation needed]
Serious cardiac events, including some that have been fatal, have occurred following the use of sumatriptan injection or tablets. Events reported have included
The most common side effects[14] 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 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 the placebo group to 2% in the sumatriptan group.
Mechanism of action
Sumatriptan is molecularly similar to
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 the drug has been shown to abort a cluster headache within 30 minutes in 77% of cases.[19]
Pharmacokinetics
Sumatriptan is administered in several forms: tablets,
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.[20][21]
History
In 1991, Glaxo received approval for sumatriptan, which 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.[22]
Phase III studies with an
Society and culture
Legal status
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 a pharmacist and is only available in packs of two without a medical prescription.[28] However, it can be bought over the counter in the UK[29] and Sweden.[30]
In Russia versions of sumatriptan, which are not registered in the National registry of medications, may be regarded as narcotic drugs (derivatives of dimethyltryptamine).[31]
Generics
Glaxo patents for sumatriptan expired in February 2009. At that time, Imitrex sold for about $25 a pill.
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 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.[34]
Controversy
According to the
References
- ^ ISBN 9780857113382.
- ^ a b c d e f g "Sumatriptan Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 3 March 2019.
- S2CID 25060147.
- ^ "Sumatriptan Use During Pregnancy". Drugs.com. Retrieved 3 March 2019.
- ISBN 9783527607495.
- hdl:10665/345533. WHO/MHP/HPS/EML/2021.02.
- ^ "The Top 300 of 2021". ClinCalc. Archived from the original on 15 January 2024. Retrieved 14 January 2024.
- ^ "Sumatriptan - Drug Usage Statistics". ClinCalc. Retrieved 14 January 2024.
- ^ PMID 24865446.
- from the original on 17 February 2017. Retrieved 16 July 2016.
- ISSN 1110-1849.
- ^ "Patient bleeds dark green blood". BBC News. 8 June 2007. Archived from the original on 5 August 2010. Retrieved 6 March 2010.
- S2CID 35168945.
- ^ "Tablets". fda.gov. Retrieved 19 February 2018.
- ^
Razzaque Z, Heald MA, Pickard JD, Maskell L, Beer MS, Hill RG, et al. (January 1999). "Vasoconstriction in human isolated middle meningeal arteries: determining the contribution of 5-HT1B- and 5-HT1F-receptor activation". British Journal of Clinical Pharmacology. 47 (1): 75–82. PMID 10073743.
- S2CID 13007101.
- PMID 28653227.
- S2CID 25689799.
- PMID 1647496.
- S2CID 25587940.
- S2CID 20755695.
- S2CID 25696109.
- ^ Clinical trial number NCT00724815 for "The Efficacy and Tolerability of NP101 Patch in the Treatment of Acute Migraine (NP101-007)" at ClinicalTrials.gov
- ^ "SmartRelief -electronically assisted drug delivery (iontophoresis)". nupathe.com. Archived from the original on 7 January 2016. Retrieved 19 February 2018.
- S2CID 205683188.
- ^ "Zecuity Approved by the FDA for the Acute Treatment of Migraine". nupathe.com. Archived from the original on 7 January 2016. Retrieved 19 February 2018.
- ^ "Teva pulls migraine patch Zecuity on reports of burning, scarring". FiercePharma. 13 June 2016. Archived from the original on 21 March 2017. Retrieved 10 April 2017.
- ^ "Poisons Standard June 2017". 18 May 2017. Archived from the original on 31 July 2017. Retrieved 22 July 2017.
- ^ "Press release: First Over The Counter (OTC) migraine pill made available". Medicines and Healthcare Products Regulatory Agency. Archived from the original on 5 December 2014. Retrieved 28 January 2015.
- ^ European Medicines Agency (23 November 2011). "Assessment Report: Sumatriptan Galpharm 50 mg Tablets" (PDF). European Medicines Agency. p. 20. Archived (PDF) from the original on 7 January 2016. Retrieved 28 January 2015.
- ^ "Постановление Правительства РФ от 30 июня 1998 г. N 681 "Об утверждении перечня наркотических средств, психотропных веществ и их прекурсоров, подлежащих контролю в Российской Федерации" (с изменениями и дополнениями)" (in Russian). Гарант. Retrieved 28 April 2019.
ДМТ (диметилтриптамин) и его производные, за исключением производных, включенных в качестве самостоятельных позиций в перечень
- ^ "GlaxoSmithKline sets out to dupe migraine sufferers with Treximet smoke and mirrors". Community Catalyst. 24 April 2008. Retrieved 22 March 2019.
- ^ "Par Pharmaceutical begins shipment of sumatriptan injection". Par Pharmaceutical. 6 November 2008. Archived from the original on 10 December 2008. Retrieved 25 November 2008.
- ^ LaMattina J (2 March 2015). "If You 'Want To Make A Good Drug Great' Cost Must Be Factored In". Forbes. Archived from the original on 14 February 2017. Retrieved 13 February 2017.
- S2CID 42239120
- S2CID 80167113, retrieved 26 June 2022