SUMATRIPTAN

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DRUGS
SUMATRIPTAN

Sumatriptan belongs to the class of medications called as selective serotonin receptor agonists. Sumatriptan is used to treat the symptoms of migraine headaches (severe, throbbing headaches that sometimes are accompanied by nausea or sensitivity to sound and light). 

Introduction

Sumatriptan belongs to the class of medications called as selective serotonin receptor agonists. Sumatriptan is used to treat the symptoms of migraine headaches (severe, throbbing headaches that sometimes are accompanied by nausea or sensitivity to sound and light).

Pharmacological class: Selective serotonin receptor agonist

Indications

  • Migraine

Pharamcological Action

Sumatriptan, an antimigraine drug, is a selective agonist of vascular serotonin (5hydroxytryptamine; 5-HT) type 1-like receptors, likely the 5-HT1D and 5-HT1B subtypes. The 5-HT1B and 5-HT1D receptors function as auto receptors, which inhibit the firing of serotonin neurons and a reduction in the synthesis and release of serotonin upon activation.

After sumatriptan binds to these receptors, adenylate cyclase activity is inhibited via regulatory G proteins, increases intracellular calcium, and affects other intracellular events. This results in vasoconstriction and inhibition of sensory nociceptive (trigeminal) nerve firing and vasoactive neuropeptide release.

 

Dosage

Adult Dose for Migraine

Oral:

Initial dose: 25 mg, 50 mg, or 100 mg orally, once

Maximum dose: 200 mg per 24 hours

Subcutaneous:

Initial dose: 1 to 6 mg subcutaneously, once

Maximum dose: 12 mg per 24 hours

Intranasal:

Nasal spray: Initial dose: 5 mg, 10 mg, or 20 mg into one nostril, once

Pharmacokinetics

Sumatriptan shows 15% absorption. It shows 14%-21% protein binding. Sumatriptan is metabolized by monoamine oxidase (MAO), predominantly the A isoenzyme. Only 3% of the dose is excreted in the urine as unchanged sumatriptan; 42% of the dose is excreted as the major metabolite, the indole acetic acid analogue of sumatriptan. The half-life of sumatriptan is 2.5 hours.

 

Contraindications

  • Contraindicated in patients with known allergy to sumatriptan.

  • Contraindicated in patients with history of angina pectoris, myocardial infarction and documented silent ischemia

  • Contraindicated in patients with history of stroke or transient ischemic attack

Drug Interactions

  • Concomitant administration of sumatriptan with monoamine oxidase inhibitors such as phenelzine, isocarboxazid, can cause a severe condition called serotonin syndrome.

  • Concomitant administration of sumatriptan with ergot containing drugs like dihydroergotamine may raise the risk of side effects like chest tightness or pressure.

  • Co-administration of Sumatriptan and other 5-HT1 agonists may add to the vasospastic effect.

Side effects

Common (affecting between 1 in10 to 1 in 100)

  • Injection site reaction

  • Dizziness

  • Vertigo

  • Nausea and vomiting

  • Tingling sensation

  • Flushing sensation

  • Unpleasant taste

Uncommon (affecting 1 in 100 to 1 in 1000)

  • Abdominal Pain

  • Anxiety

  • Blurred Vision

  • Changes in Patterns and Rhythms of Speech

  • Chest Pain or Tightness

  • Chills

  • Confusion

  • Dizziness

  • Irregular Heartbeat

  • Headache

  • Muscle Cramps and Stiffness

  • Neck, Throat, or Jaw Pain

  • Nightmares

  • Shivering

  • Sweating

  • Swelling of fingers, hands, feet, or lower legs

  • Trouble Breathing

Very rare (affecting less than 1 in 10,000)

  • Blindness

  • Chest pain

  • Chest tightness

  • Flushing or redness of the skin

  • Increased blinking or spasms of the eyelid

  • Itching, pain, redness, or swelling

  • Lightheadedness, dizziness, or fainting

  • Nerve pain

  • Severe numbness

  • Stomach pain

  • Trouble speaking or swallowing

  • Twitching

  • Unusual bleeding or bruising

  • Vomiting of blood

  • Weakness of arms and legs

Precautions

  • Avoid in patients with severe heart problems.

  • Avoid in patients with a previous stroke or mini-stroke

  • Avoid in patients with problems related to circulation

  • Avoid in with serious bowel disorders

 

Clinic Evidence

  • Data from 6 randomized, double-blind, placebo-controlled, early-intervention studies of sumatriptan tablets 50 mg and 100 mg were pooled for analysis. These constitute all the studies conducted to date of sumatriptan tablets prospectively given early for mild pain. In this analysis of pooled data from 6 clinical trials, sumatriptan tablets 50 mg and 100 mg administered early in a migraine attack while the pain was mild were well tolerated and significantly more effective than placebo. The 100-mg dose of sumatriptan was significantly more effective than the 50-mg dose.1

  • The efficacy and tolerability of oral sumatriptan were assessed in 187 migraineurs enrolled in a randomized, double-blind, parallel-group, placebo-controlled study. In the clinic, patients received oral sumatriptan 25 mg, 50 mg, or 100 mg, or placebo, for the treatment of a migraine attack. The results demonstrate that by 2 hours post dose, 52 to 57% of patients treated with sumatriptan 25 mg, 50 mg, 100 mg compared with 17% of patients treated with placebo achieved relief of headache (p < 0.05 for each sumatriptan group vs placebo). By 4 hours post dose, 65 to 78% of sumatriptan-treated patients compared with 19% of placebo-treated patients achieved relief of headache (p < 0.05 for each sumatriptan group vs placebo). Oral sumatriptan also effectively relieved nausea and photophobia and improved clinical disability.2

References

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