Abstract:
:Beta-adrenoceptor antagonists are among the most commonly prescribed classes of drugs. They are indicated for the treatment of diseases such as hypertension and angina pectoris, in which long term therapy is often required. Since many beta-adrenoceptor antagonists have short plasma elimination half-lives, divided daily dosing has often been necessary in order to provide continuous beta-blockade throughout the day. However, such multiple-dose schedules may promote patient non-compliance and failure of the prescribed regimen. Long acting propranolol is a sustained release formulation of propranolol which has been developed to maintain therapeutic plasma propranolol concentrations throughout a 24-hour period while allowing once-daily dosing. Compared with conventionally formulated propranolol, long acting propranolol has a prolonged terminal half-life (8 to 11 hours), due to slower absorption from the gut. Systemic bioavailability of long acting propranolol is 30 to 50% less than that of the conventional formulation. This difference may result from increased hepatic metabolism. Peak drug concentrations are significantly lower than following identical doses of conventional propranolol, and the time to peak drug concentrations following administration is delayed. Relatively constant plasma concentrations and clinically significant inhibition of exercise-induced tachycardia are maintained throughout a 24-hour dosing interval following once-daily long acting propranolol. Once-daily long acting propranolol is as effective as divided doses of conventional propranolol for the treatment of hypertension and angina pectoris. Efficacy also appears comparable with once-daily administration of long acting conventional beta-adrenoceptor antagonists such as atenolol and nadolol. Once-daily long acting propranolol provides clinically significant sustained beta-adrenoceptor blockade and offers the potential for improved patient compliance due to once-daily dosing. Since provision of sustained beta-adrenoceptor blockade appears to be particularly important in the treatment of angina, this may be the principal indication for which long acting propranolol has a therapeutic advantage independent of its potential to improve compliance.
journal_name
Clin Pharmacokinetjournal_title
Clinical pharmacokineticsauthors
Nace GS,Wood AJdoi
10.2165/00003088-198713010-00003subject
Has Abstractpub_date
1987-07-01 00:00:00pages
51-64issue
1eissn
0312-5963issn
1179-1926journal_volume
13pub_type
杂志文章,评审abstract:BACKGROUND:Antihistamines (histamine H(1) receptor antagonists) are effective and convenient drugs for the treatment of allergic conjunctivitis. Because of the short duration of action generally observed for drugs administered topically to the eye, the oral route is often preferred. However, the presence of a selective...
journal_title:Clinical pharmacokinetics
pub_type: 临床试验,杂志文章
doi:10.2165/00003088-200241070-00006
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abstract:BACKGROUND AND OBJECTIVES:Two phase I drug interaction studies were performed with oral enzalutamide, which is approved for the treatment of metastatic castration-resistant prostate cancer (mCRPC). METHODS:A parallel-treatment design (n = 41) was used to evaluate the effects of a strong cytochrome P450 (CYP) 2C8 inhib...
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pub_type: 杂志文章,多中心研究,随机对照试验
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journal_title:Clinical pharmacokinetics
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.2165/00003088-200039001-00004
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journal_title:Clinical pharmacokinetics
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journal_title:Clinical pharmacokinetics
pub_type: 杂志文章,评审
doi:10.2165/00003088-198611010-00002
更新日期:1986-01-01 00:00:00
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更新日期:1986-03-01 00:00:00
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更新日期:1988-06-01 00:00:00
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更新日期:1999-02-01 00:00:00
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更新日期:1998-08-01 00:00:00
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更新日期:1994-07-01 00:00:00
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更新日期:2018-07-01 00:00:00
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journal_title:Clinical pharmacokinetics
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更新日期:1999-09-01 00:00:00
abstract:BACKGROUND AND OBJECTIVE:Tegafur is an oral fluorouracil prodrug used in the treatment of colorectal cancer. The aim of this phase II, crossover, bioequivalence study was to compare the pharmacokinetics (primary objective) and tolerability (secondary objective) of tegafur-uracil (UFT) given as three daily doses (tid, r...
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更新日期:2007-01-01 00:00:00
abstract:BACKGROUND:Febuxostat is a novel non-purine selective inhibitor of xanthine oxidase currently being developed for the management of hyperuricemia in patients with gout. OBJECTIVE:To investigate the pharmacokinetics, pharmacodynamics and safety of febuxostat over a range of oral doses in healthy subjects. METHODS:In a...
journal_title:Clinical pharmacokinetics
pub_type: 杂志文章,随机对照试验
doi:10.2165/00003088-200645080-00005
更新日期:2006-01-01 00:00:00
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journal_title:Clinical pharmacokinetics
pub_type: 杂志文章
doi:10.2165/00003088-198106040-00006
更新日期:1981-07-01 00:00:00
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journal_title:Clinical pharmacokinetics
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更新日期:1997-05-01 00:00:00
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journal_title:Clinical pharmacokinetics
pub_type: 杂志文章,评审
doi:10.2165/00003088-198611010-00003
更新日期:1986-01-01 00:00:00
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journal_title:Clinical pharmacokinetics
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更新日期:1993-03-01 00:00:00
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更新日期:2018-08-01 00:00:00
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