Naratriptan

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[edit] BRAND NAMES

[edit] STRUCTURE

Naratriptan.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.

Naratriptan is a triptan drug. Triptans are 5-HT receptor agonists, they bind with high affinity to 5HT1B and 5HT1D receptors.

The agonist effects of Naratriptan 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 2-3 hours after dosing to healthy subjects and elimination half-life is approximately 6 hours.

[edit] INDICATIONS

  • Naratriptan is indicated for the acute treatment of migraine attacks with or without aura in adults.

Naratriptan is not intended for the prophylactic therapy of migraine or for use in the management of hemiplegic or basilar migraine

[edit] DOSAGE

Naratriptan comes in 1 mg and 2,5 mg tablets.

The recommended dose is 1 mg-2,5mg taken orally with fluids as early as possible after the onset of migraine. The choice of dose should be made on an individual basis, weighing the possible benefit of the 2.5 mg dose with the potential for a greater risk of adverse events

If the headache recurs after initial relief, a second tablet may be taken, providing there is an interval of at least 4 hours between doses. The total daily dose of Naratriptan should not exceed 5 mg per day.

[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 (Naratriptan may increase blood pressure)
  • Severe renal impairment (creatinine clearance, <15 mL/min)
  • Severe hepatic impairment
  • Concomitant administration within 24 hours of an ergotamine derivative (e.g. Dihydroergotamine, ergotamine) or another Triptan.
  • Hemiplegic or basilar migraine

[edit] WARNINGS AND PRECAUTIONS

  • In case of chest discomfort, including pain, pressure, heaviness and tightness following Naratriptan administration, patients should be evaluated for the presence of Coronary artery disease (CAD) or a predisposition to Prinzmetal variant angina before receiving additional doses of Naratriptan
  • 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).
  • Arrhythmias: Discontinue Naratriptan if occurs
  • Cerebral hemorrhage, subarachnoid hemorrhage, and stroke: Discontinue Naratriptan 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), Naratriptan should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
  • Naratriptan is excreted in the milk of rats. Therefore, caution should be exercised when considering the administration to a nursing woman.

[edit] SIDE EFFECTS

Naratriptan is generally well tolerated. The most common side effects were: Dizziness, paresthesia, drowsiness, fatigue, flushing, sensitivity to light, dry mouth, hot or cold sensation and pressure sensation in the chest or throat.

  • In very rare cases, coronary vasospasm and myocardial infarction have been reported.
  • Increase in Blood Pressure: At the recommended doses, the increases in systemic blood pressure are generally small and may be more pronounced in the elderly and hypertensive patients. Significant elevation in blood pressure, including hypertensive crisis, has been reported only on rare occasions.

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

http://us.gsk.com/products/assets/us_amerge.pdf

[edit] REFERENCES