Frovatriptan SuccinateFrovatriptan has been studied in healthy male and female subjects, in subjects with renal or hepatic impairment, in elderly subjects, and in individuals with migraine headache during and between attacks.

Healthy Subjects

Following oral administration of frovatrip-tan, 2.5-mg mean maximum blood concentrations in patients are achieved in approximately 2 to 4 hours. With regard to age, the area under the curve (AUC) in healthy subjects aged 65 to 77, compared with subjects aged 21 to 37, was 1.5-fold to twofold higher in the older individuals. Blood concentrations and the AUC were greater in healthy women (7.0 ng/ml, 94 ng/ml per hour) than in healthy men (4.25 ng/ml, 42.9 ng/ml per hour). The absolute bioavailability in healthy subjects is about 20% in males and 30% in females. Protein binding of frovatriptan is low (approximately 15%). online canadian pharmacy

Elderly Populations

Blood concentrations were higher in older women than in older men and higher in both older men and women than in younger subjects. Mean values of maximum concentration (Cmax) and the AUC were ranked in the following order: (1) elderly women, (2) young women, (3) elderly men, and (4) young men.

Subjects with Renal Impairment

No significant difference was noted in subjects with renal impairment compared to healthy subjects. Less than 10% of frova-triptan is excreted renally after an oral dose, thus making it unlikely that the kinetics of frovatriptan would be affected by renal impairment.

Subjects with Hepatic Impairment

Four men and four women were given a single oral dose, or 2.5 mg of frovatriptan. Of these four subjects, two men and two women had mild impairment (Child-Pugh score A) and two men and two women had moderate impairment (Child-Pugh score B). The AUC in women with moderate impairment appeared higher than that in women with mild impairment. No relationship was seen in the men, and there appeared to be no correlation between the degree of hepatic impairment and the kinetics of frova-triptan. In addition, these values were consistent with studies comparing the young and elderly, with mean concentrations in both young and elderly women being higher than those in the men. Furthermore, the mean AUC and Cmax were nearly twice as high in hepatically impaired subjects, when compared with the data in young subjects (aged 21 to 37). However, the mean AUC and Cmax were just as high in hepatically impaired women as in women taking combined oral contraceptives (COCs). In short, decreased hepatic function affects the ki­netics of frovatriptan in a similar manner as concurrent administration of COCs. 

Subjects with Migraine

Twelve patients (six of both sexes) were given frovatriptan 2.5 mg as a single oral dose and were examined during a migraine attack and during a migraine-free period. Blood concentrations were twofold higher in women than men, with no significant differences apparent in either sex. In addition, there appeared to be little difference in blood concentrations or kinetics during a migraine or during a migraine-free period.

In sum, as a result of increased bioavailability, blood concentrations of frovatrip-tan were higher in women than in men during migraine attacks. Further, the presence of migraine headache does not seem to affect the kinetics of frovatriptan.