Frovatriptan Succinate

(BANM, USAN, rINNM)
Synonyms: Frovatriptan, Succinate de; Frovatriptani Succinas; SB-209509AX VML-251 (frovatriptan or frovatriptan succinate).
Cyrillic synonym: Фроватриптана Суксинат.

💊 Chemical information

Chemical formula: C14H17N3O,C4H6O4,H2O = 379.4.
CAS — 158930-17-7.
ATC — N02CC07.
ATC Vet — QN02CC07.

💊 Adverse Effects and Precautions

As for Sumatriptan. Frovatriptan should not be used in patients with severe hepatic impairment. No dosage adjustment is needed in mild or moderate hepatic impairment.

💊 Interactions

As for Sumatriptan. Fluvoxamine is a potent inhibitor of the cytochrome P450 isoenzyme CYP1A2 and has been shown to increase the blood levels of frovatriptan by 27 to 49%.

💊 Pharmacokinetics

After oral doses, peak plasma-frovatriptan concentrations are attained in 2 to 4 hours, and bioavailability is about 20% in men and 30% in women. Food may delay the time to peak plasma concentrations by about 1 hour. Frovatriptan is 15% protein bound. It is primarily metabolised by the hepatic cytochrome P450 isoenzyme CYP1A2. About 32% of an oral dose is excreted in the urine and 62% in faeces. The plasma elimination half-life of frovatriptan is about 26 hours.
Distribution into milk has been found in studies in rats.
1. Buchan P, et al. Clinical pharmacokinetics of frovatriptan. Headache 2002; 42 (suppl 2): S54–S62
2. Elkind AH, et al. Pharmacokinetics of frovatriptan in adolescent migraineurs. J Clin Pharmacol 2004; 44: 1158–65.

💊 Uses and Administration

Frovatriptan is a selective serotonin (5-HT 1 ) agonist with actions and uses similar to those of sumatriptan. It is used for the acute treatment of the headache phase of migraine attacks. It should not be used for prophylaxis. Frovatriptan is given orally as the succinate although doses are expressed in terms of the base; frovatriptan succinate 3.9 mg is equivalent to about 2.5 mg of frovatriptan. The recommended dose is 2.5 mg; if this is ineffective, a second dose should not be taken for the same attack. If symptoms recur after an initial response, the dose may be repeated after an interval of at least 2 hours. The maximum dose of frovatriptan in 24 hours is 5 mg in the UK although, in the USA, a maximum daily dose of 7.5 mg is allowed.
1. Goldstein J. Frovatriptan: a review. Expert Opin Pharmacother 2003; 4: 83–93.

Migraine.

For comparison of the relative benefits of different triptans in migraine, see under Sumatriptan. Further references.
1. Rapoport A, et al. Dose range-finding studies with frovatriptan in the acute treatment of migraine. Headache 2002; 42 (suppl 2): S74–S83
2. Ryan R, et al. Clinical efficacy of frovatriptan: placebo-controlled studies. Headache 2002; 42 (suppl 2): S84–S92
3. Poolsup N, et al. Efficacy and tolerability of frovatriptan in acute migraine treatment: systematic review of randomized controlled trials. J Clin Pharm Ther 2005; 30: 521–32.

💊 Preparations

Proprietary Preparations

Austria: Eumitan; Cz.: Fromen; Recur; Fin.: Migard; Fr.: Tigreat; Ger.: Allegro; Gr.: Migard; Migralin; Irl.: Frovex; Ital.: Auradol; Rilamig; Neth.: Fromirex; Migard; Port.: Dorlise; Migard; Spain: Forvey; Perlic; Switz.: Menamig; UK: Migard; USA: Frova.
Published October 23, 2018.