Abstract:
:The bioavailability and pharmacologic activity of tablets containing micronized spironolactone chemical (median particle size 2.21 micrometers) were compared to those of tablets made from standard spironolactone chemical (median particle size 78.8 micrometers) in healthy men. Apart from particle size, all features of these tablets were identical. After 200-mg single doses, the bioavailability of micronized tablets was significantly higher than that of standard tablets. Furthermore, as assessed by 24-hour urine log10 10 Na/K ratio, the pharmacologic activity of micronized spironolactone was significantly greater than that of the standard formulation. The significant influence on renal antimineralocorticoid activity of raised plasma and urinary levels of canrenone, quantitatively the major active metabolite of spironolactone in man, emphasizes the clinical importance of the bioavailability of spironolactone preparations. Since this study, the process used in the manufacture of spironolactone (Aldactone) tablets has been under review.
journal_name
J Clin Pharmacoljournal_title
Journal of clinical pharmacologyauthors
McInnes GT,Asbury MJ,Ramsay LE,Shelton JR,Harrison IRdoi
10.1002/j.1552-4604.1982.tb02694.xsubject
Has Abstractpub_date
1982-08-01 00:00:00pages
410-7issue
8-9eissn
0091-2700issn
1552-4604journal_volume
22pub_type
杂志文章abstract::The pharmacokinetics and pharmacodynamics of verapamil were investigated in six chronic hemodialysis patients. A single oral 120-mg dose was administered both on a non-hemodialysis day and a hemodialysis day separated by greater than or equal to 7 days. Blood pressure and PR interval were measured simultaneously with ...
journal_title:Journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1002/j.1552-4604.1988.tb03224.x
更新日期:1988-09-01 00:00:00
abstract::Nonlinearities are commonplace in pharmacokinetics and most frequently occur because of a limited concentration of biological material available for interaction with relatively high concentrations of drugs. The Michaelis-Menten-type function can be applied to metabolism, transport, and binding phenomena that display c...
journal_title:Journal of clinical pharmacology
pub_type: 杂志文章,评审
doi:10.1002/j.1552-4604.1989.tb03369.x
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abstract::This study outlines the attempts of four states (Louisiana, Kansas, Wisconsin, and Michigan) to restrict anorectic prescriptions. The actions in these four states exemplify the various mechanisms used in regulating anorectics, ranging from educational efforts to legislative enactments. We examine the evidence used in ...
journal_title:Journal of clinical pharmacology
pub_type: 杂志文章,评审
doi:
更新日期:1988-05-01 00:00:00
abstract::Experiments were performed on humans to study the blunting on the diuretic action of furosemide by prostaglandin synthetase inhibitors. Maximal water diuresis was instituted. At the peak of urine flow, clearance periods were performed during baseline conditions and repeated after the injection of aspirin and, subseque...
journal_title:Journal of clinical pharmacology
pub_type: 杂志文章
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abstract::Recent initiatives calling for changes in medical education, such as the General Professional Education of the Physician and Robert Wood Johnson Reports, have recommended alternative teaching approaches to the lecture format. The Patient-Oriented Problem-Solving (POPS) exercises, sponsored by the Upjohn Company (Kalam...
journal_title:Journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1002/j.1552-4604.1995.tb04999.x
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abstract::The effect of epoprostenol on the pharmacokinetics of furosemide was investigated in 23 patients with end-stage congestive heart failure (CHF) receiving conventional therapy alone or conventional therapy plus epoprostenol. Estimates of the apparent oral clearance, volume of distribution, and absorption rate constant f...
journal_title:Journal of clinical pharmacology
pub_type: 临床试验,杂志文章
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更新日期:1996-03-01 00:00:00
abstract::This trial was conducted to evaluate the pharmacokinetics and safety of a sodium oxybate (gamma-hydroxybutyrate [GHB]) oral solution in narcoleptic patients after acute and chronic treatment. An open-label, two-period, two-treatment study design was used. Trial subjects included 13 patients with polysomnographically c...
journal_title:Journal of clinical pharmacology
pub_type: 临床试验,杂志文章
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journal_title:Journal of clinical pharmacology
pub_type: 杂志文章,随机对照试验
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更新日期:2017-09-01 00:00:00
abstract::In a placebo-controlled, randomized, double-blind cross-over study in 12 healthy volunteers the effect of acute alcohol intake during treatment with transdermally administered scopolamine (TTS-scopolamine) was investigated. One group of six subjects reached maximal blood alcohol concentrations (BAC) of 80 mg/dL and an...
journal_title:Journal of clinical pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
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更新日期:1988-12-01 00:00:00
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journal_title:Journal of clinical pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
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更新日期:1995-09-01 00:00:00
abstract::Sixteen essential hypertensive patients were entered into a protocol assessing the effect of Spirapril, an angiotensin-converting enzyme (ACE) inhibitor, on blood pressure, the renin-aldosterone system, and renal function. Specifically monitored before, during 6 weeks, and 6 months of Spirapril therapy were plasma ren...
journal_title:Journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1002/j.1552-4604.1993.tb04668.x
更新日期:1993-04-01 00:00:00
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journal_title:Journal of clinical pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1002/j.1552-4604.1982.tb02158.x
更新日期:1982-04-01 00:00:00
abstract::The aim of these two studies was to evaluate the safety and pharmacokinetics of oral nalmefene, a new orally effective opioid antagonist. In the first study, single ascending doses of 50, 100, 200, and 300 mg of nalmefene HCl were administered in double-blind fashion to four groups of healthy men. There were six subje...
journal_title:Journal of clinical pharmacology
pub_type: 临床试验,杂志文章
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更新日期:1987-03-01 00:00:00
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journal_title:Journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1002/j.1552-4604.1991.tb03648.x
更新日期:1991-10-01 00:00:00
abstract::Propafenone and its 5-hydroxy metabolite exhibit different electrophysiological properties. Objectives of the CAQ-PAF study were (1) to develop a strategy favoring propafenone instead of 5-hydroxypropafenone in plasma following oral administration of propafenone and (2) to evaluate the potential of low-dose quinidine ...
journal_title:Journal of clinical pharmacology
pub_type: 杂志文章,随机对照试验
doi:10.1177/0091270011399574
更新日期:2012-02-01 00:00:00
abstract::Controlled-onset extended-release verapamil (COER-V) is designed so drug concentrations rise sharply in the early morning to coincide with the peak incidence of cardiovascular events. The primary objective of this study was to compare the diurnal pattern of forearm vascular resistance (FVR) between hypertensives and n...
journal_title:Journal of clinical pharmacology
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doi:
更新日期:2000-12-01 00:00:00
abstract::Six obese (mean weight 92 kg) and five normal (60 kg) subjects received 2 mg diazepam nightly for 30 nights. Determination of diazepam and desmethyldiazepam plasma concentrations during the dosing period and for a withdrawal period indicated that accumulation half-life for both diazepam (7.8 days in obese vs. 3.1 days...
journal_title:Journal of clinical pharmacology
pub_type: 杂志文章
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更新日期:1983-08-01 00:00:00
abstract::Effective and practical preventive procedures for postflight orthostatic intolerance are highly desirable. The current practice of attempts to expand plasma volume by ingestion of salt and fluids before reentry has proven benefits. This study evaluated alternative options using fludrocortisone (F) to expand plasma vol...
journal_title:Journal of clinical pharmacology
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journal_title:Journal of clinical pharmacology
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abstract::Raltegravir is a novel HIV-1 integrase inhibitor with potent in vitro activity (95% inhibitory concentration = 33 nM in 50% human serum). In vitro characterization of raltegravir inhibition potential was assessed against a panel of cytochrome P450 (CYP) enzymes. An open-label, 2-period study was conducted to assess th...
journal_title:Journal of clinical pharmacology
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journal_title:Journal of clinical pharmacology
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abstract::As documented in national surveys, for the past several years, marijuana has been the most commonly abused drug in the United States, with approximately 6% of the population 12 years and older having used the drug in the month prior to interview. The use of marijuana is not without significant health hazards. Marijuan...
journal_title:Journal of clinical pharmacology
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doi:10.1002/j.1552-4604.2002.tb05997.x
更新日期:2002-11-01 00:00:00
abstract::Calcium channel blocker therapy has proved protective in certain models of ischemic-induced acute renal failure. This effect may be related to the prevention of calcium influx into injured cells or by the vasodilatory effects of verapamil that may result in an improvement in renal blood flow. In the current study, the...
journal_title:Journal of clinical pharmacology
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doi:10.1002/j.1552-4604.1987.tb03076.x
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journal_title:Journal of clinical pharmacology
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abstract::Vitamin B6 has been known to possess antiemetic effects since 1942. This water soluble compound has several forms in the circulation including pyridoxine, pyridoxal, and pyridoxal phosphate. The active antiemetic form of vitamin B6 is unknown. This was a pre-specified substudy of a randomized, placebo-controlled trial...
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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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abstract::Bile acid sequestrants can potentially bind to concomitant drugs. Single-dose studies evaluated the effects of colesevelam on the pharmacokinetics of glimepiride, glipizide extended-release (ER), and olmesartan medoxomil. Each study enrolled healthy subjects aged 18-45 years. The olmesartan medoxomil study used a rand...
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abstract::To determine the elimination of high-molecular-weight hydroxyethyl starch (HES, Mw 450,000) in normal subjects, ten volunteers were given 500 ml 6% HES solution by intravenous infusion, and serial blood and urine samples were collected for nonglucose total carbohydrate determination. On the average, 46 and 64 per cent...
journal_title:Journal of clinical pharmacology
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doi:10.1002/j.1552-4604.1982.tb02164.x
更新日期:1982-04-01 00:00:00
abstract::Isosorbide dinitrate is one of the most commonly prescribed medications for the treatment of ischemic heart disease. It has been demonstrated to be ineffective relative to placebo when taken inappropriately. This study objectively documents the magnitude and nature of compliance in 68 ambulatory patients who were pres...
journal_title:Journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1002/j.1552-4604.1996.tb04222.x
更新日期:1996-07-01 00:00:00