Sumatriptan

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Sumatriptan belongs to the group of anti-migraine preparations. It is a 5-HT (types 5-HT1D and 5-HT1B) receptor agonist.

Migraine headaches are thought to result from the dilatation of blood vessels. Sumatriptan constricts these blood vessels, thus relieving the migraine headache.

Sumatriptan is used to treat migraine attacks with or without aura (a warning sensation that usually involves visual distortions, such as light-flashes, zigzag lines, stars, or waves).

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[edit] BRAND NAMES

[edit] STRUCTURE

Sumatriptan.jpg

[edit] MECHANISM OF ACTION

Theories on the etiology of migraine headache suggest that symptoms are due to local cranial vasodilatation and/or to the release of vasoactive and pro-inflammatory peptides from sensory nerve endings in an activated trigeminal system.

Sumatriptan bind with high affinity to two serotonin (5-HT) subtypes, the 5HT1B and 5HT1D.
The agonist effects of Sumatriptan on these receptors results in extracerebral intracranial blood vessels constriction and in the inhibition of pro-inflammatory neuropeptide release from nerve endings.

[edit] INDICATIONS

  • Acute treatment of migraine attacks with or without aura in Adults

[edit] DOSAGE

  • Tablets:
    • Adults (18-65 years of age): 50 mg as early as possible after the onset of migraine, may repeat after 2 hours if headache returns. Maximum daily dose 100 mg
  • Subcutaneous injection:
    • Single 6 mg dose administered to an injection site with adequate skin and subcutaneous thickness (e.g. lateral thigh or upper arm). The maximum recommended dose that may be given in 24 hours is two doses separated by at least 1 hour. Benefit of second dose in patients who have failed to respond to a first dose has not been established.
  • Iontophoretic transdermal system (ZECUITY):
    • Single transdermal system (TDS) applied to dry, intact, non-irritated skin of upper arm or thigh. No more than two TDS should be used in any 24 hour period; second TDS should be used no sooner than 2 hours after activation of first TDS. TDS should not be applied to a previous application site until that site remains erythema free for at least 3 days.

[edit] DOSAGE FORMS AND STRENGTHS

  • Tablets: 25, 50, and 100 mg of sumatriptan
  • Injection: 0.5 mL of solution containing 6 mg sumatriptan (Alsuma)
  • Iontophoretic transdermal system: 6.5 mg over 4 hours (Zecuity)

[edit] CONTRAINDICATIONS

  • Ischemic heart disease, coronary artery vasospasm, Previous myocardial infarction, or other significant underlying cardiovascular disease (Triptans may cause coronary artery vasospasm)
  • Cerebrovascular syndromes (e.g. history of stroke or transient ischaemic attack)
  • Peripheral Vascular Disease (including ischemic bowel disease)
  • Hemiplegic or basilar migraine
  • Uncontrolled hypertension
  • Concomitant administration within 24 hours of an ergotamine derivative or another triptan [e.g. Almotriptan (AXERT®), Eletriptan (RELPAX®) , Frovatriptan (FROVA®), Naratriptan (AMERGE®), Rizatriptan (MAXALT®, MAXALT-MLT®), Sumatriptan/Naproxen (TREXIMET®), ergotamines (CAFERGOT®, ERGOMAR®, MIGERGOT®), dihydroergotamine (D.H.E. 45®, MIGRANAL®)]
  • Use of monoamine oxidase-A inhibitor (MAO-A inhibitor) in past 2 weeks
  • Hepatic or renal impairment
  • Hypersensitivity to sumatriptan

[edit] WARNINGS AND PRECAUTIONS

  • Perform cardiac evaluation in patients with multiple cardiovascular risk factors (e.g., hypertension, hypercholesterolemia, smoker, obesity, diabetes, strong family history of coronary artery disease (CAD), female with surgical or physiological menopause, male over 40 years of age).
  • In case of chest discomfort, including pain, pressure, heaviness and tightness following Sumatriptan administration, patients should be evaluated for the presence of Coronary artery disease (CAD) or a predisposition to Prinzmetal variant angina before receiving additional doses.
  • Arrhythmias: Discontinue Sumatriptan if occurs
  • Cerebral hemorrhage, subarachnoid hemorrhage, and stroke: Discontinue Sumatriptan if occurs
  • Medication overuse headache: Overuse of acute migraine drugs for 10 or more days per month may lead to exacerbation of headache. Medication overuse headache may present as migraine-like daily headaches or as a marked increase in frequency of migraine attacks. Detoxification of patients, including withdrawal of the overused drugs, and treatment of withdrawal symptoms (which often include

a transient worsening of headache) may be necessary.

[edit] INTERACTIONS

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category C (US). Sumatriptan should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
  • Sumatriptan is excreted into breast milk. Infant exposure can be minimised by avoiding breast feeding for 24 hours after treatment.

[edit] SIDE EFFECTS

Tablets: The most common side effects were: nausea, vomiting, paresthesia, dizziness, malaise/fatigue and pressure sensation in the chest or throat

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

[edit] REFERENCES

Antimigraine preparations
5 HT1 agonists (Triptans) Almotriptan (Almogran, Axert)   Eletriptan (Relpax)   Frovatriptan (Frova, Migard, Menatriptan)   Rizatriptan (Maxalt)   Sumatriptan (Imigran)   Zolmitriptan (Zomig)
Ergot alkaloids Dihydroergotamine   Ergotamine
NSAIDs/ Analgesics Indometacin   Acetylsalicylic acid (Aspirin)   Diclofenac (Voltaren)   Ibuprofen (Advil, Brufen, Dolgit, Nurofen)   Ketorolac (Toradol)   Naproxen (Naprosyn, Aleve)   Nimesulide   Paracetamol (Efferalgan, Panadol...)
Prophylaxis Cinnarizine (Stugeron, Stugeron forte)   Flunarizine (Sibelium)   Nifedipine (Adalat)   Pizotifen   Propranolol (Inderal)   Topiramate (Topamax)