Frovatriptan succinate, a 5-HT1B/1D receptor agonist for migraine

被引:32
|
作者
Balbisi, EA
机构
[1] St Johns Univ, Coll Pharm & Allied Hlth Profess, Jamaica, NY 11439 USA
[2] Queens Hosp Ctr, Jamaica, NY USA
关键词
D O I
10.1111/j.1368-5031.2004.00218.x
中图分类号
R5 [内科学];
学科分类号
1002 ; 100201 ;
摘要
Frovatriptan succinate is one of the most recent serotonin receptor agonists to receive FDA, approved labelling for use in the acute management of migraine with or without aura in adults. The mechanism of action of frovatriptan is thought to be similar to that of a serotonin agonist. However, frovatriptan has distinctive pharmacokinetic and pharmacologic properties, chiefly, a high affinity for serotonin receptors 1B and ID and a long elimination half-life; frovatriptan was shown to be more selective for cerebral than coronary arteries, a property which makes frovatriptan more favourable in patients at risk of coronary artery disease. Additionally, frovatriptan has a half-life of approximately 25 h, substantially longer than that of any other agent within its class. This property makes frovatriptan suitable for patients who typically suffer migraines of long duration and/or those who suffer migraine recurrence. The efficacy of frovatriptan in the treatment of acute migraine was demonstrated in five double-blind, randomised, placebo-controlled trials. At 2 h, headache response rates for frovatriptan 2.5 mg ranged from 38 to 40% compared to 22-35% for placebo. Headache recurrence for frovatriptan 2.5 mg at 24 h ranged from 9 to 14% compared with 18% in placebo subjects. Frovatriptan has no clinically significant pharmacokinetic interactions with drugs used for migraine prophylaxis or with commonly prescribed medications. Adverse effects of frovatriptan including dizziness, paresthesia, dry mouth, fatigue and flushing were generally mild and well tolerated. Given the fact that patient response to serotonin agonists is individualised, and selecting an effective agent may involve trial and error, frovatriptan is a welcome alternative in the acute management of migraine.
引用
收藏
页码:695 / 705
页数:11
相关论文
共 50 条
  • [41] 5-HT1B/1D as a potential target for antidepressants/anxiolytics
    Stenfors, C
    EUROPEAN NEUROPSYCHOPHARMACOLOGY, 2004, 14 : S116 - S117
  • [42] Patient treatment preferences and the 5-HT1B/1D agonists
    Ryan, RE
    ARCHIVES OF INTERNAL MEDICINE, 2001, 161 (21) : 2545 - 2553
  • [43] Familial migraine with aura:: Association study with 5-HT1B/1D,5-HT2C, and hSERT polymorphisms
    Racchi, M
    Leone, M
    Porrello, E
    Rigamonti, A
    Govoni, S
    Sironi, M
    Montomoli, C
    Bussone, G
    HEADACHE, 2004, 44 (04): : 311 - 317
  • [44] Porcine carotid vascular effects of eletriptan (UK-116,044): a new 5-HT1B/1D receptor agonist with anti-migraine activity
    Edwin Willems
    Peter De Vries
    Jan P. C. Heiligers
    P. R. Saxena
    Naunyn-Schmiedeberg's Archives of Pharmacology, 1998, 358 : 212 - 219
  • [45] Rizatriptan, a novel 5-HT1B/1D agonist for migraine:: Single- and multiple-dose tolerability and pharmacokinetics in healthy subjects
    Goldberg, MR
    Lee, Y
    Vyas, KP
    Slaughter, DE
    Panebianco, D
    Ermlich, SJ
    Shadle, CR
    Brucker, MJ
    McLoughlin, DA
    Olah, TV
    JOURNAL OF CLINICAL PHARMACOLOGY, 2000, 40 (01): : 74 - 83
  • [46] The anti-migraine 5-HT1B/1D agonist rizatriptan inhibits neurogenic dural vasodilation in anaesthetized guinea-pigs
    Williamson, DJ
    Hill, RG
    Shepheard, SL
    Hargreaves, RJ
    BRITISH JOURNAL OF PHARMACOLOGY, 2001, 133 (07) : 1029 - 1034
  • [47] 311C90 ('Zomig', or zolmitriptan), a novel 5-HT1B/1D agonist for treatment of acute migraine: Mechanism of action
    Martin, GR
    Goadsby, PJ
    NEUROLOGY, 1997, 48 (03) : 1131 - 1131
  • [48] Conformationally constrained 5-(thienyl)tryptamine derivatives as serotonin 5-HT1B/1D receptor agonists:: Potential treatments for migraine
    Slassi, A
    Meng, CQ
    Dyne, K
    Wang, X
    Lee, DKH
    Kamboj, R
    McCallum, KL
    Mazzacco, L
    Rakhit, S
    MEDICINAL CHEMISTRY RESEARCH, 1999, 9 (09) : 668 - 674
  • [49] Porcine carotid vascular effects of eletriptan (UK-116,044):: a new 5-HT1B/1D receptor agonist with anti-migraine activity
    Willems, E
    De Vries, P
    Heiligers, JPC
    Saxena, PR
    NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY, 1998, 358 (02) : 212 - 219
  • [50] 5-HT1B/1D AGONIST CGS-12066B ATTENUATES CLASP KNIFE REFLEX IN THE CAT
    MILLER, JF
    PAUL, KD
    RYMER, WZ
    HECKMAN, CJ
    JOURNAL OF NEUROPHYSIOLOGY, 1995, 74 (01) : 453 - 456