Eletriptan

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Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Eletriptan.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.

Eletriptan is a triptan drug. it binds with high affinity to three serotonin (5-HT) subtypes, the 5HT1B, 5HT1D and 5HT1F. The agonist effects on these receptors results in extracerebral intracranial blood vessels constriction and in the inhibition of pro-inflammatory neuropeptide release from nerve endings.

Peak plasma levels occurs approximately 1.5 hours after dosing to healthy subjects and elimination half-life is approximately 4 hours.

[edit] INDICATIONS

  • Acute treatment of migraine with or without aura in adults.

Eletriptan should not be used for migraine prophylaxis.

[edit] DOSAGE

Eletriptan comes in 20 mg and 40 mg tablets

  • Adults: 20-40 mg as early as possible after the onset of migraine, may repeat after 2 hours if headache returns. Maximum daily dose 80 mg

[edit] CONTRAINDICATIONS

  • Ischemic heart disease, coronary artery vasospasm, or other significant underlying cardiovascular disease (Triptans can produce a small contraction of human coronary arteries)
  • Cerebrovascular syndromes (e.g. history of stroke or transient ischaemic attack)
  • Peripheral Vascular Disease (including ischemic bowel disease)
  • Uncontrolled hypertension
  • Concomitant administration within 24 hours of an ergotamine derivative or another triptan.
  • Severe hepatic impairment
  • Hemiplegic or basilar migraine

[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 Eletriptan 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 Eletriptan if occurs
  • Cerebral hemorrhage, subarachnoid hemorrhage, and stroke: Discontinue Eletriptan 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

[edit] SIDE EFFECTS

The most common side effects of Eletriptan are: Dizziness, nausea, weakness, tiredness and pressure sensation in the chest or throat

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

http://labeling.pfizer.com/ShowLabeling.aspx?id=621

[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)