Abstract：
AIMS:The pharmacokinetics and dose proportionality of rizatriptan single oral doses from 2.5 to 15 mg administered as solutions to healthy volunteers were studied. METHODS:In a randomized, crossover study with four periods, twenty-four healthy volunteers (12 males and 12 females) took single oral doses of 2.5, 5, 10, and 15 mg rizatriptan in Periods 1-4. In a fifth period, subjects received 4 mg intravenous (i.v.) rizatriptan as a reference. Plasma and urine rizatriptan concentrations were determined at several timepoints/intervals for 12 and 24 h, respectively. RESULTS:The arithmetic mean AUC values following single oral doses of 2.5, 5, 10, and 15-mg rizatriptan were 16, 33, 72, and 127 ng ml-1 h, respectively, in males; and 19, 42, 97, and 161 ng ml-1 h, respectively, in females. The overall bioavailability (F ) of rizatriptan was approximately 40% in males. Following the 4 mg reference i.v. dose, the apparent plasma clearance (CL) and renal clearance (CLr ) were 1042 and 225 ml min-1, respectively, in males; and 821 and 174 ml min-1, respectively, in females. CONCLUSIONS:The disposition kinetics of oral rizatriptan were linear for doses of 2. 5-10 mg in males, and for doses of 2.5-5 mg in females. However, the degree of nonlinearity for higher doses was minor for both genders. The plasma concentrations of rizatriptan were slightly greater in women compared to men but the difference was not considered to be clinically meaningful. Also, the clearance of rizatriptan appeared to be mainly nonrenal.
journal_name
Br J Clin Pharmacoljournal_title
British journal of clinical pharmacologyauthors
Lee Y,Conroy JA,Stepanavage ME,Mendel CM,Somers G,McLoughlin DA,Olah TV,De Smet M,Keymeulen B,Rogers JDdoi
10.1046/j.1365-2125.1999.00917.xkeywords:
subject
Has Abstractpub_date
1999-04-01 00:00:00pages
373-8issue
4eissn
0306-5251issn
1365-2125journal_volume
47pub_type
临床试验,杂志文章,随机对照试验abstract：AIMS:The present pharmacokinetic study was undertaken to determine the dose proportionality of three different doses of budesonide-400 microg, 800 microg or 1600 microg administered twice daily by a dry-powder inhaler (Turbuhaler ) in adult patients with mild asthma. METHODS:A total of 38 patients received budesonide ...
journal_title：British journal of clinical pharmacology
pub_type： 临床试验,杂志文章,多中心研究,随机对照试验
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更新日期：1999-09-01 00:00:00
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journal_title：British journal of clinical pharmacology
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journal_title：British journal of clinical pharmacology
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journal_title：British journal of clinical pharmacology
pub_type： 临床试验,杂志文章,随机对照试验
doi：
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pub_type： 临床试验,杂志文章,随机对照试验
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pub_type： 杂志文章
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pub_type： 临床试验,杂志文章,随机对照试验
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journal_title：British journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1111/j.1365-2125.1985.tb02611.x
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pub_type： 临床试验,杂志文章,随机对照试验
doi：
更新日期：1995-09-01 00:00:00
