Journal ArticleDOI
Pharmacokinetics and pharmacodynamics of zolmitriptan in patients with mild to moderate hypertension: a double-blind, placebo-controlled study.
Deborah A. Smith,Elena W. Cleary,Stephanie Watkins,Cameron S. Huffman,Stacy C. Dilzer,Kenneth C. Lasseter +5 more
TLDR
It is indicated that zolmitriptan can be administered for treatment of migraine in patients with controlled hypertension without dose adjustment and was well tolerated in both groups.Abstract:
Zolmitriptan is a potent selective 5HT1B/1D receptor agonist for acute migraine therapy. Zolmitriptan has vasoconstrictor activity in cerebral vessels and may cause slight elevations of blood pressure in subjects without hypertension. Therefore, the pharmacokinetics and pharmacodynamics of zolmitriptan (5, 10, and 20 mg) were evaluated in 16 patients with mild to moderate hypertension (controlled by hydrochlorothiazide 50 mg once daily) and 17 healthy age- and sex-matched control subjects in a randomized, placebo-controlled, double-blind, four-period crossover study. The pharmacokinetics of zolmitriptan and its metabolites were dose proportional. Although area under the concentration-time curve (AUC0-infinity) and maximum concentration (Cmax) were slightly higher in patients with hypertension at all doses, this was only statistically significant for AUC at the 20-mg dose. Differences between subjects with and without hypertension were not clinically significant. Zolmitriptan produced a small increase in blood pressure, but this was similar in subjects with and without hypertension and was of no clinical significance. Zolmitriptan was well tolerated in both groups. Zolmitriptan plasma concentrations were higher in women than in men, with higher values of AUC and Cmax and lower total clearance in women. These results indicate that zolmitriptan can be administered for treatment of migraine in patients with controlled hypertension without dose adjustment.read more
Citations
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Journal ArticleDOI
Pharmacokinetics and pharmacodynamics of the triptan antimigraine agents: a comparative review.
TL;DR: The pharmacological properties of the triptans (time to peak plasma concentration, half-life, bioavailability and receptor binding) are reviewed and related to efficacy and time of onset and the effects of concomitant medication, food, age and disease are considered.
Journal ArticleDOI
Zolmitriptan: a review of its use in migraine.
TL;DR: Zolmitriptan is effective across a wide range of migraine subtypes, maintains efficacy when used in the long term and is generally well tolerated.
Journal ArticleDOI
Preliminary studies of the pharmacokinetics and tolerability of zolmitriptan nasal spray in healthy volunteers.
TL;DR: Plasma concentrations of zolmitriptan and its active metabolite, 183C91, were broadly dose proportional, and there was no statistically significant difference for AUC or Cmax values between the two nasal spray solutions or between nasal spray and oral formulations.
Journal ArticleDOI
Zolmitriptan intranasal: a review of the pharmacokinetics and clinical efficacy.
Peter J. Goadsby,Roger Yates +1 more
TL;DR: A nasal formulation of zolmitriptan with clear evidence for local absorption, resulting in plasma drug concentrations within 2 minutes of dosing, central nervous system penetration 3 minutes later, and a significant efficacy benefit versus placebo 10 to 15 minutes after dosing.
Journal ArticleDOI
High-performance liquid chromatographic analysis of zolmitriptan in human plasma using fluorescence detection.
TL;DR: A simple, rapid and sensitive high-performance liquid chromatographic (HPLC) method to quantify zolmitriptan in plasma using an isocratic system with fluorescence detection was developed and yielded good results regarding linearity, precision, accuracy, specificity and recoveries.
References
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Journal ArticleDOI
Sumatriptan. A reappraisal of its pharmacology and therapeutic efficacy in the acute treatment of migraine and cluster headache
Greg L. Plosker,Donna McTavish +1 more
TL;DR: Oral administration of sumatriptan 100mg consistently achieved significantly greater response rates than a fixed combination of ergotamine 2mg plus caffeine 200mg during 3 consecutive migraine attacks and was also more effective than aspirin 900mg plus metoclopramide 10mg orally in a similar study.
Journal ArticleDOI
Inhibition of trigeminal neurons by intravenous administration of the serotonin (5HT)1B/D receptor agonist zolmitriptan (311C90): are brain stem sites therapeutic target in migraine?
Peter J. Goadsby,Karen L. Hoskin +1 more
TL;DR: It is demonstrated that systemically administered zolmitriptan can inhibit evoked trigeminovascular activity within the trigeminal nucleus, which may play a role in the anti‐migraine actions of this compound and offers the prospect of a third pathophysiologically consistent target site for anti‐Migraine drug effects.
Journal ArticleDOI
311C90, A new central and peripherally acting 5-HT1D receptor agonist in the acute oral treatment of migraine A double-blind, placebo-controlled, dose-range finding study
TL;DR: Oral 311C90 (5 and 25 mg) is highly effective and well tolerated in the acute treatment of migraine and the response rates and treatment differences compared with placebo suggest possible superiority over existing antimigraine therapies.
Journal ArticleDOI
The tolerability and pharmacokinetics of the novel antimigraine compound 311C90 in healthy male volunteers
TL;DR: 311C90 showed no clinically significant effects on blood pressure, heart rate, ECG or laboratory variables at any dose and demonstrated a tolerability and pharmacokinetic profile compatible with an acute oral migraine treatment.
Journal ArticleDOI
The absolute bioavailability and metabolic disposition of the novel antimigraine compound zolmitriptan (311C90)
Emma J. Seaber,N. On,Ruth Dixon,M. Gibbens,W. J. Leavens,J. Liptrot,G. Chittick,John Posner,Paul Rolan,Richard Peck +9 more
TL;DR: The data suggest that zolmitriptan undergoes first-pass metabolism and this is more extensive in men than in women, and there are no significant unidentified metabolites in man.