Pharmacokinetic evaluation of frovatriptan

被引:16
|
作者
Negro, Andrea [2 ]
Lionetto, Luana [1 ]
Casolla, Barbara [1 ]
Lala, Noemi [2 ]
Simmaco, Maurizio [1 ]
Martelletti, Paolo [2 ]
机构
[1] Univ Roma La Sapienza, St Andreas Hosp, Sch Hlth Sci, Adv Mol Diagnost Unit,NESMOS Dept, I-00189 Rome, Italy
[2] Univ Roma La Sapienza, Reg Referral Headache Ctr, Sch Hlth Sci, Dept Med & Mol Sci, I-00189 Rome, Italy
关键词
cluster headache; frovatriptan; menstrual migraine; migraine; pharmacodynamics; pharmacokinetics; triptans; 5-HT1B/1D RECEPTOR AGONIST; ACUTE MIGRAINE TREATMENT; MENSTRUAL MIGRAINE; POSTMARKETING SURVEILLANCE; TRIPTAN FORMULATIONS; ORAL SUMATRIPTAN; DOUBLE-BLIND; EFFICACY; TOLERABILITY; ALMOTRIPTAN;
D O I
10.1517/17425255.2011.622265
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Introduction: Migraine is the most common painful neurological disorder, affecting 13% of the general population. Triptans represent a powerful pharmacological tool in acute migraine treatment, however, a significant portion of treated patients cannot have access to this class due to possible adverse affects. Today, a total of seven triptan molecules are available, representing a commonly prescribed migraine treatment. Although there is a need of extensive use of triptans, only 25% of migraine patients are using triptans. Areas covered: This review includes triptans and evidence for the use of frovatriptan. A systematic approach is used to discuss the pharmacodynamic and pharmacokinetic aspects of frovatriptan, considering the emerging data on the clinical efficacy of frovatriptan in the treatment of migraine and cluster headaches. The data were obtained by searching the following key words in MEDLINE: pharmacokinetic, pharmacodynamic, triptans, frovatriptan, migraine, menstrual migraine, relatively to the period 1988 - 2011. Expert opinion: Frovatriptan has been developed in order to improve safety and efficacy of triptans. It shows a favorable tolerability and efficacy profile, limited to 24/48-h headache recurrence, when compared with other triptans. Preclinical data suggest that the pharmacokinetic profile of frovatriptan may differ from other available triptans. In fact, among triptans, frovatriptan showed the highest potency at the 5-HT1B receptor (8.2) and the longer half-life (26 h). These parameters determine the clinical properties of frovatriptan; in particular the lowest rate of headache recurrence in comparison with other triptans.
引用
收藏
页码:1449 / 1458
页数:10
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