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QuickView for Frovatriptan (compound)
PubChem
| Name: | frovatriptan |
|---|---|
| PubChem Compound ID: | 152943 |
| Molecular formula: | C18H25N3O6 |
| Molecular weight: | 379.408 g/mol |
| Synonyms: |
Frovatriptan succinate [USAN]; Frova; Frovatriptan succinate hydrate; 158930-17-7; 1H-Carbazole-6-carboxamide, 2,3,4,9-tetrahydro-3-(methylamino)-, (R)-, butanedioate (1:1), monohydrate; Butanedioic acid, compd. with (R)-2,3,4,9-tetrahydro-3-(methylamino)-1H-carbazole-6-carboxamide (1:1), monohydrate
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DrugBank
Identification
| Name: | frovatriptan |
|---|---|
| Name (isomeric): | DB00998 |
| Drug Type: | small molecule |
| Synonyms: |
Frovatriptan succinate
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| Brand: | Miguard, Frova, Frovelan |
| Category: | Serotonin Agonists, Vasoconstrictor Agents, Anti-migraine Agents, Anti-inflammatory Agents |
| CAS number: | 158747-02-5 |
Pharmacology
| Indication: | For the acute treatment of migraine attacks with or without aura in adults. |
|---|---|
| Pharmacology: |
Frovatriptan is a second generation triptan 5-HT receptor agonist that binds with high affinity for 5-HT1B and 5-HT1D receptors. It is structurally distinct from, but pharmacologically related to other selective 5-HT1B/1D receptor agonists. Frovatriptan has no significant effects on GABAA mediated channel...
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| Mechanism of Action: |
Three distinct pharmacological actions have been implicated in the antimigraine effect of the triptans: (1) stimulation of presynaptic 5-HT1D receptors, which serves to inhibit both dural vasodilation and inflammation; (2) direct inhibition of trigeminal nuclei cell excitability via 5-HT1B/1D receptor agonism in the brainstem ...
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| Absorption: | Frovatriptan is rapidly absorbed from the duodenum, but has low oral bioavailability. |
| Protein binding: | Binding to serum proteins is low (approximately 15%). Reversible binding to blood cells at equilibrium is approximately 60%. |
| Biotransformation: | In vitro, cytochrome P450 1A2 appears to be the principal enzyme involved in the metabolism of frovatriptan to several metabolites including hydroxylated frovatriptan, N-acetyl desmethyl frovatriptan, hydroxylated N-acetyl desmethyl frovatriptan and desmethyl frovatriptan, and several other minor metabolites. Desmethyl frovatriptan has lower affinity for 5-HT1B/1D receptors compared to the parent compound. The N-acetyl desmethyl metabolite has no significant affinity for 5-HT receptors. The activity of the other metabolites is unknown. |
| Route of elimination: | Radiolabeled compounds excreted in urine were unchanged frovatriptan, hydroxylated frovatriptan, N-acetyl desmethyl frovatriptan, hydroxylated N-acetyl desmethyl frovatriptan and desmethyl frovatriptan, together with several other minor metabolites. Less than 10% of frovatriptan was excreted in urine after an oral dose. |
| Half Life: | 26 hours |
| Clearance: | 220 mL/min [male receiving IV dose of 0.8 mg] 130 mL/min [Female receiving IV dose of 0.8 mg] |
| Toxicity: | There is no direct experience of any patient taking an overdose of Frovatriptan. The maximum single dose of frovatriptan given to male and female patients with migraine was 40 mg (16 times the clinical dose) and the maximum single dose given to healthy male subjects was 100 mg (40 times the clinical dose) without significant adverse events. |
| Affected organisms: | Humans and other mammals |
Interactions
| Food interaction: |
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Targets
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