Frovatriptan
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Frovatriptan, sold under the brand name Frova among others, is a triptan medication developed by Vernalis for the treatment of migraine headaches[1] and for short term prevention of menstrual migraine.[2][3] The product is licensed to Endo Pharmaceuticals in North America and Menarini in Europe.[4]
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:
- Ischemic heart disease
- Cerebrovascular syndrome
- Peripheral vascular disease
- Uncontrolled hypertension
- Hemiplegic or basilar migraine
Side effects
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
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| Target | Affinity (Ki, nM) |
|---|---|
| 5-HT1A | 50–62 (Ki) 759–>10,000 (EC50) 38% (Emax) |
| 5-HT1B | 2.5–46 (Ki) 6.3–20 (EC50) 92% (Emax) |
| 5-HT1D | 1.7–10 (Ki) 2–5 (EC50) 98% (Emax) |
| 5-HT1E | >1,000 (Ki) 6,610–>10,000 (EC50) 44% (Emax) |
| 5-HT1F | 63–120 (Ki) 79–447 (EC50) 46% (Emax) |
| 5-HT2A | >10,000 (Ki) >10,000 (EC50) |
| 5-HT2B | >10,000 (Ki) >10,000 (EC50) |
| 5-HT2C | >5,000 (Ki) ND (EC50) |
| 5-HT3 | >1,000 (mouse/rat) |
| 5-HT4 | ND |
| 5-HT5A | ND |
| 5-HT6 | ND |
| 5-HT7 | 107–200 (Ki) 38 (EC50) |
| α1 | >10,000 (rat) |
| α1A–α1D | ND |
| α2A–α2C | ND |
| β1–β3 | ND |
| D1 | >10,000 |
| D2 | >10,000 |
| D3 | >10,000 |
| D4–D5 | ND |
| H1 | >10,000 (guinea pig) |
| H2–H4 | ND |
| M1–M5 | ND |
| I1, I2 | ND |
| σ1, σ2 | ND |
| TAAR1 | ND |
| SERT | ND |
| NET | ND |
| DAT | ND |
| Notes: The smaller the value, the more avidly the drug binds to the site. All proteins are human unless otherwise specified. Refs: [5][6][7][8][3][9][10] [11][12][13][14][15] | |
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.[12] It has no significant effects on the GABAA mediated channel activity and benzodiazepine binding sites.Script error: No such module "Unsubst". Frovatriptan inhibits excessive dilation of arteries that supply blood to the head.Script error: No such module "Unsubst". Uniquely among most triptans, frovatriptan is also a relatively potent serotonin 5-HT7 receptor agonist.[12] It is inactive at the serotonin 5-HT2A and 5-HT2B receptors.[12]
Pharmacokinetics
Frovatriptan has a terminal elimination half-life of approximately 26 hours, making it the longest within its class.[16]
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.[17] It can be thought of as a 5-substituted and side chain-cyclized derivative of N-methyltryptamine (NMT).[17]
The experimental log P of frovatriptan is 0.9 and its predicted log P is 1.2.[18]
History
Frovatriptan was first described in the scientific literature by 1997.[19][20][21] It was approved for medical use in the United States in 2001.[22]
Society and culture
Legal status
Frovatriptan is available only by prescription in the United States and Canada.[23]
See also
References
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- ↑ Brown, A. M., Parsons, A. A., Raval, P., Porter, R., Tilford, N. S., Gager, T. L., ... & King, F. D. (1996, October). SB 209509 (VML 251), a potent constrictor of rabbit basilar artery with high affinity and selectivity for human 5-HT1D receptors. In BRITISH JOURNAL OF PHARMACOLOGY (Vol. 119, pp. P110-P110).
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