Frovatriptan


Frovatriptan, sold under the brand name Frova among others, is a triptan medication developed by Vernalis for the treatment of migraine headaches and for short term prevention of menstrual migraine. The product is licensed to Endo Pharmaceuticals in North America and Menarini in Europe.

Medical uses

Frovatriptan is used in the treatment of migraine.

Available forms

It is available as 2.5 mg tablets.

Contraindications

Frovatriptan should not be given to patients with:
Rare, but serious cardiac events have been reported in patients with risk factors predictive of CAD. These include: coronary artery vasospasm, transient myocardial ischemia, myocardial infarction, ventricular tachycardia and ventricular fibrillation.

Pharmacology

Pharmacodynamics

Frovatriptan is a serotonin receptor agonist, with high affinity for the serotonin 5-HT1B and 5-HT1D receptors and with weaker activity at the serotonin 5-HT1F receptor. It has no significant effects on the GABAA mediated channel activity and benzodiazepine binding sites. Frovatriptan inhibits excessive dilation of arteries that supply blood to the head. Uniquely among most triptans, frovatriptan is also a relatively potent serotonin 5-HT7 receptor agonist. It is inactive at the serotonin 5-HT2A and 5-HT2B receptors.

Pharmacokinetics

Frovatriptan has a terminal elimination half-life of approximately 26 hours, making it the longest within its class.

Chemistry

Frovatriptan's chemical structure is unusual among triptans, with other triptans being simple tryptamines or closely related compounds but frovatriptan instead being a tricyclic cyclized tryptamine and tetrahydrocarbazolamine derivative. It can be thought of as a 5-substituted and side chain-cyclized derivative of N-methyltryptamine.
The experimental log P of frovatriptan is 0.9 and its predicted log P is 1.2.

History

Frovatriptan was first described in the scientific literature by 1997. It was approved for medical use in the United States in 2001.

Society and culture

Legal status

Frovatriptan is available only by prescription in the United States and Canada.