Frovatriptan Succinate (frovatriptan succinate)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Frovatriptan succinate is a selective agonist of serotonin (5-hydroxytryptamine; 5-HT) type 1B and 1D receptors (''triptan'').
Frovatriptan succinate is a selective agonist of serotonin (5-hydroxytryptamine; 5-HT) type 1B and 1D receptors. Frovatriptan is structurally distinct from, but pharmacologically related to, other selective 5-HT1B/1D receptor agonists (e.g., almotriptan, eletriptan, naratriptan, rizatriptan, sumatriptan, zolmitriptan). Current data suggest that 5-HT1 receptor agonists, including frovatriptan, may ameliorate migraine through selective constriction of certain intracranial blood vessels, inhibition of neuropeptide release, and/or reduced transmission in the trigeminal pain pathway.
Frovatriptan is incompletely absorbed from GI tract, with an absolute bioavailability of 20 and 30% in males and females, respectively. The peak plasma concentrations of frovatriptan are attained approximately 2-4 hours after oral administration. Food does not affect bioavailability but may delay time to peak plasma concentration by 1 hour.
Frovatriptan distributes into the cellular fraction of blood, principally erythrocytes (approximately 60% reversibly bound). Plasma protein binding is low (approximately 15%). Animal studies indicate limited capacity of the drug to cross the blood-brain barrier.
Frovatriptan is distributed into milk in rats; it is not known whether the drug is distributed into human milk.
In vitro, frovatriptan is metabolized principally by cytochrome P-450 (CYP) isoenzyme 1A2 to numerous metabolites, including desmethyl frovatriptan, which exhibits a lower affinity for 5-HT1B/1D receptors compared with the parent drug. The activity of other metabolites (e.g., hydroxylated frovatriptan, N-acetyl desmethyl frovatriptan, hydroxylated N-acetyl desmethyl frovatriptan) has not been fully elucidated. Following oral administration of a single 2.5-mg dose of radiolabeled frovatriptan, 32 and 62% of the dose is excreted in urine and feces, respectively, as unchanged drug and metabolites.
The elimination half-life of frovatriptan is reportedly 26 hours in healthy individuals.
In patients with mild to moderate hepatic impairment, the AUC of frovatriptan is 2-fold higher than in healthy individuals. In geriatric patients, the AUC of frovatriptan is 1.5- to 2-fold higher than in younger adults; half-life and time to peak plasma concentrations are unchanged.
USES: Frovatriptan is used to treat migraines. It helps to relieve headache, pain, and other migraine symptoms (including nausea, vomiting, sensitivity to light/sound). Prompt treatment helps you return to your normal routine and may decrease your need for other pain medications.
Frovatriptan belongs to a class of drugs known as triptans. It affects a certain natural substance (serotonin) that causes narrowing of blood vessels in the brain. It may also relieve pain by affecting certain nerves in the brain.
Frovatriptan does not prevent future migraines or lessen how often you get migraine attacks.
Generic name: frovatriptan succinate
Pronunciation: (FROE-va-TRIP-tan)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Frovatriptan Succinate
Indications
The following indications are listed for Frovatriptan Succinate:
- Migraine
Dosing
Available as frovatriptan succinate; dosage is expressed in terms of frovatriptan.
Frovatriptan is available in a tablet formulation for oral administration.
Frovatriptan should be administered with fluids.
Tablets should be stored at 20-25degreesC with excursions permitted between 15-30degreesC; protect from moisture.
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Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Ischemic coronary artery disease (e.g., angina pectoris, history of myocardial infarction, documented silent ischemia), coronary artery vasospasm (e.g., Prinzmetal variant angina), or uncontrolled hypertension.
*Wolff-Parkinson-White syndrome or arrhythmias associated with other cardiac accessory conduction pathway disorders.
*Cerebrovascular syndromes (e.g., history of stroke, transient ischemic attack, or hemiplegic or basilar migraine), peripheral vascular disease, or ischemic bowel disease.
*Recent (i.e., within 24 hours) treatment with another 5-HT1 receptor agonist or an ergotamine-containing or ergot-type drug.
*Known hypersensitivity to frovatriptan; angioedema and anaphylaxis reported.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
The most common adverse effects occurring in >=2% of patients receiving frovatriptan and more frequently than with placebo include dizziness, fatigue, headache, paresthesia, flushing, dry mouth, hot or cold sensation, skeletal pain, dyspepsia, and chest pain.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and efficacy of frovatriptan have not been established in children younger than 18 years of age.
Frovatriptan produced embryofetal lethality, fetal abnormalities, and reduced embryofetal growth in animal studies at doses greater than those used clinically. There are no adequate and well-controlled studies of the developmental risk associated with frovatriptan therapy in pregnant women.
Frovatriptan and/or its metabolites are distributed into milk in rats; it is not known whether frovatriptan is distributed into human milk, its effects on the breastfed infant, or on milk production. The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for frovatriptan and any adverse effects on the breastfed infant from the drug or from the underlying maternal condition.
No dosage adjustment is necessary in geriatric patients.
Plasma concentrations of frovatriptan are substantially (1.5- to 2-fold) higher in geriatric patients than in younger adults. No adjustment in frovatriptan dosage appears to be necessary in geriatric patients.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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