Limits...
Frovatriptan: a review of pharmacology, pharmacokinetics and clinical potential in the treatment of menstrual migraine.

Balbisi EA - Ther Clin Risk Manag (2006)

Bottom Line: Frovatriptan treatment is generally well tolerated.Its selectivity for cerebral vessels lessens the potential for undesirable peripheral effects.Frovatriptan does not alter cytochrome P450 (CYP450) isoenzymes, as such it is unlikely to affect the metabolism of other drugs.

View Article: PubMed Central - PubMed

Affiliation: St. John's University, College Of Pharmacy & Allied Health Professions Jamaica, New York, USA Ambulatory Medicine, Queens Hospital Center Jamaica, New York, USA.

ABSTRACT
Frovatriptan is an orally active 5-hydroxytryptamine (5-HT) receptor agonist which binds with high affinity to 5-HT(1B) and 5-HT(1D) receptors. Earlier clinical trials demonstrated that frovatriptan 2.5 mg is significantly more effective than placebo in the acute management of migraine and its associated symptoms. More recently, frovatriptan was shown to be effective in the management of menstrual migraine. The incidence of menstrual migraine in subjects receiving frovatriptan 2.5 mg twice daily during the six day perimenstrual period was 41% compared with 67% with placebo. Frovatriptan treatment is generally well tolerated. The most commonly reported adverse effects were dizziness, paresthesia, dry mouth, and fatigue. Pharmacologic studies demonstrated that frovatriptan is cerebroselective. Its selectivity for cerebral vessels lessens the potential for undesirable peripheral effects. Frovatriptan has a terminal deposition half-life of approximately 26 hours, which appears to be independent of age, gender, and renal function. This imparts that frovatriptan may be particularly well suited to patients with prolonged migraines and those who suffer migraine recurrence. Frovatriptan does not alter cytochrome P450 (CYP450) isoenzymes, as such it is unlikely to affect the metabolism of other drugs. No dosage adjustments are necessary based on age, renal, or mild to moderate hepatic impairment. Apart from its efficacy in the acute management of migraine, frovatriptan is an effective agent when used as either acute therapy or as intermittent prophylaxis therapy of menstrual migraines, particularly in women who do not respond to conventional therapies.

No MeSH data available.


Related in: MedlinePlus

Structure of frovatriptan.
© Copyright Policy
Related In: Results  -  Collection


getmorefigures.php?uid=PMC1936266&req=5

fig1: Structure of frovatriptan.

Mentions: Frovatriptan (Figure 1) is a 5-HT receptor agonist which binds with high affinity to 5-HT1B and 5-HT1D receptors (Comer 2002). In vitro, frovatriptan shows moderate affinity for the receptor 5-HT7, which is believed to contribute to its distinctive pharmacologic properties (Brown et al 1998). Frovatriptan demonstrated higher binding affinity than sumatriptan at human 5-HT1B receptor (∼4-fold) and a comparable affinity at human 5-HT1D receptor (Comer 2002). Frovatriptan was shown to be the most potent 5-HT1B agonist in vitro −log10 of the concentration causing 50% maximal stimulation (pEC50) of 8.2 as compared with sumatriptan, pEC50 of 7.0 (Stewart et al 1999).


Frovatriptan: a review of pharmacology, pharmacokinetics and clinical potential in the treatment of menstrual migraine.

Balbisi EA - Ther Clin Risk Manag (2006)

Structure of frovatriptan.
© Copyright Policy
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC1936266&req=5

fig1: Structure of frovatriptan.
Mentions: Frovatriptan (Figure 1) is a 5-HT receptor agonist which binds with high affinity to 5-HT1B and 5-HT1D receptors (Comer 2002). In vitro, frovatriptan shows moderate affinity for the receptor 5-HT7, which is believed to contribute to its distinctive pharmacologic properties (Brown et al 1998). Frovatriptan demonstrated higher binding affinity than sumatriptan at human 5-HT1B receptor (∼4-fold) and a comparable affinity at human 5-HT1D receptor (Comer 2002). Frovatriptan was shown to be the most potent 5-HT1B agonist in vitro −log10 of the concentration causing 50% maximal stimulation (pEC50) of 8.2 as compared with sumatriptan, pEC50 of 7.0 (Stewart et al 1999).

Bottom Line: Frovatriptan treatment is generally well tolerated.Its selectivity for cerebral vessels lessens the potential for undesirable peripheral effects.Frovatriptan does not alter cytochrome P450 (CYP450) isoenzymes, as such it is unlikely to affect the metabolism of other drugs.

View Article: PubMed Central - PubMed

Affiliation: St. John's University, College Of Pharmacy & Allied Health Professions Jamaica, New York, USA Ambulatory Medicine, Queens Hospital Center Jamaica, New York, USA.

ABSTRACT
Frovatriptan is an orally active 5-hydroxytryptamine (5-HT) receptor agonist which binds with high affinity to 5-HT(1B) and 5-HT(1D) receptors. Earlier clinical trials demonstrated that frovatriptan 2.5 mg is significantly more effective than placebo in the acute management of migraine and its associated symptoms. More recently, frovatriptan was shown to be effective in the management of menstrual migraine. The incidence of menstrual migraine in subjects receiving frovatriptan 2.5 mg twice daily during the six day perimenstrual period was 41% compared with 67% with placebo. Frovatriptan treatment is generally well tolerated. The most commonly reported adverse effects were dizziness, paresthesia, dry mouth, and fatigue. Pharmacologic studies demonstrated that frovatriptan is cerebroselective. Its selectivity for cerebral vessels lessens the potential for undesirable peripheral effects. Frovatriptan has a terminal deposition half-life of approximately 26 hours, which appears to be independent of age, gender, and renal function. This imparts that frovatriptan may be particularly well suited to patients with prolonged migraines and those who suffer migraine recurrence. Frovatriptan does not alter cytochrome P450 (CYP450) isoenzymes, as such it is unlikely to affect the metabolism of other drugs. No dosage adjustments are necessary based on age, renal, or mild to moderate hepatic impairment. Apart from its efficacy in the acute management of migraine, frovatriptan is an effective agent when used as either acute therapy or as intermittent prophylaxis therapy of menstrual migraines, particularly in women who do not respond to conventional therapies.

No MeSH data available.


Related in: MedlinePlus