Frovatriptan, sold under the brand name Frova among others, is a triptan medication developed by Vernalis plc for the treatment of migraine
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
| + |
|
50–62 (Ki)
759–>10,000 ()
38% () |
2.5–46 (Ki)
6.3–20 ()
92% () |
1.7–10 (Ki)
2–5 ()
98% () |
>1,000 (Ki)
6,610–>10,000 ()
44% () |
63–120 (Ki)
79–447 ()
46% () |
>10,000 (Ki)
>10,000 () |
>10,000 (Ki)
>10,000 () |
>5,000 (Ki)
() |
| >1,000 (mouse/rat) |
| |
| |
| |
107–200 (Ki)
38 () |
| >10,000 (rat) |
| |
| |
| |
| >10,000 |
| >10,000 |
| >10,000 |
| |
| >10,000 (guinea pig) |
| |
| |
| |
| |
| |
| |
| |
| |
Notes: The smaller the value, the more avidly the drug binds to the site. All proteins are human unless otherwise specified. Refs:
|
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.
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
, 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-
cyclic compound derivative of
N-methyltryptamine (NMT).
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.
[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).] 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.
See also
-
Triptan
-
Tetrahydrocarbazolamine
-
LY-344864
