Sumatriptan

BRAND NAMES:

Zembrace SymTouch: Zembrace SymTouch is used for migraines and cluster headaches in adults. This medication exclusively treats headaches. 

Treximet: Treximet is a combination medication. The first ingredient is sumatriptan, a triptan. Triptans are frequently referred to as selective serotonin receptor agonists. The second medication is naproxen, a nonsteroidal anti-inflammatory (NSAID). It is available in tablets with strengths of 85 mg sumatriptan/ 500 mg naproxen and 10 mg sumatriptan/ 60 mg naproxen.

Tosymra: Tosymra is a nasal spray device that holds a liquid solution. The medicine comes in a package of six nasal spray devices. Each device contains a single dose. After you have used the device, you will trash it available in strength of 10 mg.

Sumavel DosePro: Sumavel DosePro is a needle-free, single-dose subcutaneous delivery system that provides 0.5 mL of sterile fluid containing 6 mg of sumatriptan.

MECHANISM OF ACTION:

Sumatriptan (1-{3-[2-(Dimethylamino)ethyl]-1H-indol-5-yl}-N-methylmethane sulfonamide) is a selective agonist of 5-HT1-like receptors, inhibiting plasma leakage from the dura and venous sinus. Perivascular trigeminal fibers cause this inhibition by releasing substance P, calcitonin gene-related peptide, and neurokinin A. This pain mechanism could be the final unifying pathway for multiple cephalgias and migraines, given the overlap and similarity observed among headache syndromes. Sumatriptan administered subcutaneously resulted in fast obtaining peak plasma concentrations.

By acting as an agonist on 5-HT1B/1D receptors, sumatriptan narrows blood channels in the dura mater and the basilar artery. The drug modifies trigeminovascular nerves or selectively constricts cerebral blood vessels to reduce peripheral nociception. Neurogenic plasma extravasation indicates that sumatriptan blocks peripheral trigeminal vascular nerves. By obstructing the trigeminal nucleus caudalis presynaptic terminal, the medication effectively reduces face allodynia.

Triptans function by reducing the release of inflammatory mediators from trigeminal neurons and obstructing the passage of pain signals to the trigeminal nucleus caudalis. The calcitonin gene-related peptide's vasodilation is lowered by this procedure. The middle cerebral artery (MCA) dilatation that causes migraine pain lowers the regional cerebral blood flow rate. Because sumatriptan reverses MCA dilation, this shows that the etiology of migraines involves the 5-HT receptor system.

PHARMACOKINETICS:

Absorption: Sumatriptan is readily absorbed when taken orally or subcutaneously. However, oral sumatriptan has a bioavailability of just 14%, compared to nearly 100% when administered subcutaneously.

Distribution: The volume of distribution of sumatriptan is 50L for a subcutaneous dose of 6 mg, or 2.7L/kg.

Metabolism: Monoamine oxidase A (MAO-A) mainly metabolizes sumatriptan.

Elimination: Sumatriptan has a plasma half-life of about two hours. The medication is removed primarily by metabolism, which produces an inactive analogue of indoleacetic acid. Sumatriptan's pharmacokinetics and pharmacodynamics remain unaffected in the presence of alcohol, preventative migraine therapies, or dihydroergotamine.

DOSAGE AND ADMINISTRATION:

Sumatriptan is available in several dose forms, including oral pills, intranasal sprays, subcutaneous injections, and rectal suppositories. Sumatriptan is most effective at relieving pain when used shortly following the onset of migraine symptoms. 

• Intranasal sprays: 5 mg, 10 mg, and 20 mg per actuation nasal solution formulations of sumatriptan are available, along with an 11 mg per actuation nasal powder formulation. Compared to the oral tablet form, the nasal powder form of sumatriptan exhibits quicker relief from pain intensity and migraine-related impairment.
• Sumatriptan is available in subcutaneous injectable formulations with concentrations of 3 mg/0.5 mL, 4 mg/0.5 mL, and 6 mg/0.5 mL. Subcutaneous administration of the medicine has been shown to be the most effective treatment for both pain and accompanying autonomic symptoms during the acute phase of migraine attacks. Furthermore, if migraine recurs after the initial sumatriptan injection treatment, patients can be given sumatriptan succinate tablets at a dose of up to 100 mg/d two hours later.
• Rectal suppositories: Giving sumatriptan succinate rectally at a dose of 25 mg is helpful for treating acute migraine attacks and significantly lowers symptoms within 2 hours.
• Sumatriptan is available in tablets form with strengths of 25, 50, and 100 mg.

CONTRAINDICATIONS:

• Sumatriptan should not be administered orally, intranasally, or subcutaneously to patients with severe hepatic impairment. 
• Sumatriptan should not be taken by patients who are presently on MAO-A inhibitors or have stopped taking them within the last two weeks owing to contraindications.
• Sumatriptan is contraindicated in patients with ischaemic heart disease, which includes disorders like coronary artery vasospasm, myocardial infarction, Prinzmetal angina, and angina pectoris. 
• Sumatriptan should not be used in combination with ergotamine or another 5-HT1 agonist. 
• Sumatriptan should not be used if the patient is allergic to the medicine or its excipients, as anaphylaxis has been documented in such cases. Clinicians should exercise caution when prescribing other triptans to patients who have a history of hypersensitivity responses to sumatriptan.

DRUG INTERACTIONS:

Severe interactions of sumatriptan include:

• Citalopram
• Linezolid
• Methylene blue
• Desvenlafaxine
• cyclobenzaprine
• Ondansetron
• Lorcaserin
• Duloxetine
• Sertraline
• Fluoxetine

SIDE EFFECTS:

Common side effects of sumatriptan include:

• Eye irritation
• Palpitations
• Burning sensation
• Sore throat
• Agitation
• Abdominal distress
• Nasal discomfort
• Weakness
• Pain urination
• Heart attack

TOXICITY:

There are few data on sumatriptan toxicity and overdose that are currently accessible. A 36-year-old male patient is included in a case report who self-reported using sumatriptan excessively, giving himself 66 subcutaneous injections of 6 mg over the course of four weeks. No adverse reactions were clinically observed, and laboratory parameters remained unaffected.