Grapefruit-drug interactions: can interactions with drugs be avoided?

abstract：:Disease states such as liver cirrhosis and chronic kidney disease can lead to altered pharmacokinetics (PK) of drugs by influencing drug absorption, blood flow to organs, plasma protein binding, apparent volume of distribution, and drug-metabolizing enzyme and transporter (DMET) abundance. Narrow therapeutic index dru...

journal_title：Journal of clinical pharmacology

authors： Sharma S,Suresh Ahire D,Prasad B

更新日期：2020-10-01 00:00:00

abstract：:The primary albumin binding site of indomethacin is remote from the bilirubin binding site. Indomethacin is, at most, a weak displacer of bilirubin at low serum drug concentrations. When administered at dosages less than 1 mg/kg, indomethacin would appear to be safe with respect to serum binding of bilirubin in premat...

journal_title：Journal of clinical pharmacology

authors： Rasmussen LF,Ahlfors CE,Wennberg RP

更新日期：1978-10-01 00:00:00

abstract：:GS-9667, a new selective, partial agonist of the A(1) adenosine receptor (AR), may represent an effective therapy for Type 2 diabetes (T2DM) and dyslipidemia via lowering of free fatty acids (FFA). The objectives of the studies were to evaluate the effects of single and multiple doses of GS-9667 on plasma FFA concentr...

journal_title：Journal of clinical pharmacology

authors： Staehr PM,Dhalla AK,Zack J,Wang X,Ho YL,Bingham J,Belardinelli L

更新日期：2013-04-01 00:00:00

abstract：:The aim of this study was to test the usefulness of the metabolite/caffeine ratio for the evaluation of hepatic dysfunction. Subjects with liver cirrhosis and chronic hepatitis, as well as healthy volunteers, were given the oral dose of 300 mg caffeine. Blood samples were collected after 4, 8, and 12 hours. Concentrat...

journal_title：Journal of clinical pharmacology

authors： Jodynis-Liebert J,Flieger J,Matuszewska A,Juszczyk J

更新日期：2004-04-01 00:00:00

abstract：:Essential oil compounds such as found in thyme extract are established for the therapy of chronic and acute bronchitis. Various pharmacodynamic activities for thyme extract and the essential thyme oil, respectively, have been demonstrated in vitro, but availability of these compounds in the respective target organs ha...

journal_title：Journal of clinical pharmacology

authors： Kohlert C,Schindler G,März RW,Abel G,Brinkhaus B,Derendorf H,Gräfe EU,Veit M

更新日期：2002-07-01 00:00:00

abstract：:The cancer stem cell paradigm, the epithelial-to-mesenchymal transition and its converse, the mesenchymal-to-epithelial transition, have reached convergence. Implicit in this understanding is the notion that cancer cells can change state, and with such change come bidirectional alterations in motility, proliferative a...

journal_title：Journal of clinical pharmacology

authors： Donnenberg VS,Donnenberg AD

更新日期：2015-06-01 00:00:00

abstract：:The need for clinical pharmacology in research and education, drug development, and health care delivery is well known. However, a current profile of those working in the field is not available. The ACCP authorized a survey of clinical pharmacologists to provide such a profile. Members of the ACCP or ASCPT were solici...

journal_title：Journal of clinical pharmacology

authors： Wilson JT,Brown RD,Kimura KK,Whelton A

更新日期：1989-08-01 00:00:00

abstract：:The principal causes of digitalis toxicity are overdose, reduced volume of distribution, reduced renal elimination, and increased myocardial sensitivity. The metabolic mechanism of digitalis toxicity is intense inhibition of sarcolemma Na-K ATPase, which leads to increases of intracellular Na+ and Ca2+ and arrhythmoge...

journal_title：Journal of clinical pharmacology

authors： Bigger JT Jr

更新日期：1985-10-01 00:00:00

abstract：:The objective of this study was to evaluate the effect of the acute administration of marijuana (MJ) on cardiovascular (CV) function and CNS pharmacokinetics (PK) of [(15)O]water in occasional (O) versus chronic (C) MJ users. Each subject received four injections of [(15)O]water (one prior and three postsmoking) on tw...

journal_title：Journal of clinical pharmacology

authors： Ponto LL,O'Leary DS,Koeppel J,Block RI,Watkins GL,Richmond JC,Ward CA,Clermont DA,Schmitt BA,Hichwa RD

更新日期：2004-07-01 00:00:00

abstract：:Varenicline is a novel selective α4β2 nicotinic acetylcholine partial agonist developed for smoking cessation. Single- and multiple dose studies were conducted to investigate pharmacokinetics, safety, and tolerability of varenicline in healthy male Japanese smokers. The single-dose study was conducted as a double-blin...

journal_title：Journal of clinical pharmacology

authors： Kikkawa H,Maruyama N,Fujimoto Y,Hasunuma T

更新日期：2011-04-01 00:00:00

abstract：:As the United States seeks a greater presence in space, physiologic changes associated with space flight become of greater concern. Exposure to a weightless environment has been shown to have numerous effects on body composition and organ function. Alterations include decreases in muscle and liver mass, changes in bon...

journal_title：Journal of clinical pharmacology

authors： Feldman S,Brunner LJ

更新日期：1994-06-01 00:00:00

abstract：:R(+)-alpha-lipoic acid is a natural occurring compound that acts as an essential cofactor for certain dehydrogenase complexes. The redox couple alpha-lipoic acid/dihydrolipoic acid possesses potent antioxidant activity. Exogenous racemic alpha-lipoic acid orally administered for the symptomatic treatment of diabetic p...

journal_title：Journal of clinical pharmacology

authors： Teichert J,Hermann R,Ruus P,Preiss R

更新日期：2003-11-01 00:00:00

abstract：:Migraine is a common and debilitating disorder of uncertain pathogenesis. Recent research into the pathophysiology of migraine and serotonin receptors has revolutionized the approach to pharmacotherapy. New medications, such as sumatriptan, and new dosage forms of older medications, including dihydroergotamine, NSAIDs...

journal_title：Journal of clinical pharmacology

authors： Solomon GD

更新日期：1993-03-01 00:00:00

abstract：:The extension of the previously developed integrated models for glucose and insulin (IGI) to include the oral glucose tolerance test (OGTT) in healthy volunteers could be valuable to better understand the differences between healthy individuals and those with type 2 diabetes mellitus (T2DM). Data from an OGTT in 23 he...

journal_title：Journal of clinical pharmacology

authors： Silber HE,Frey N,Karlsson MO

更新日期：2010-03-01 00:00:00

abstract：:The most recent International Conference on Harmonisation E14 Q&A document states that a separate positive control would not be necessary provided sufficiently high exposures are achieved in the early-phase studies. Realistically, a phase 1 study is unlikely to include a pharmacological positive control, and in cases ...

journal_title：Journal of clinical pharmacology

authors： Ferber G,Fernandes S,Täubel J

更新日期：2018-01-01 00:00:00

abstract：:Peginterferon beta-1a was efficacious in a Phase 3 relapsing multiple sclerosis trial, and its safety profile was consistent with other beta interferons. This study evaluated the impact of renal impairment on the pharmacokinetics and pharmacodynamics (neopterin elevation; a biomarker of pharmacological activity induce...

journal_title：Journal of clinical pharmacology

authors： Hu X,Seddighzadeh A,Stecher S,Zhu Y,Goyal J,Matson M,Marbury T,Smith W,Nestorov I,Hung S

更新日期：2015-02-01 00:00:00

abstract：:A double-blind controlled trial was carried out to compare the effects of chenodeoxycholic acid (CDCA), ursodeoxycholic acid (UDCA), and placebo on cholesterol and triglyceride levels in patients with endogenous hypertriglyceridemias. The dose of both bile acids was four 150-mg capsules day. Total serum cholesterol le...

journal_title：Journal of clinical pharmacology

authors： Carulli N,Ponz de Leon M,Podda M,Zuin M,Strata A,Frigerio G,Digrisolo A

更新日期：1981-10-01 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

authors： O'Hara GE,Philippon F,Gilbert M,Champagne J,Michaud V,Charbonneau L,Pruneau G,Hamelin BA,Geelen P,Turgeon J

更新日期：2012-02-01 00:00:00

abstract：:The impact of a microgravity simulation using a head-down tilt (-6 degrees) on lidocaine pharmacokinetics used as a probe to evaluate hepatic blood flow is discussed. Eight healthy male subjects were selected for a 7-day study, including a 4-day head-down tilt from day 2 to day 5. Subjects were given 1 mg/kg of lidoca...

journal_title：Journal of clinical pharmacology

authors： Saivin S,Pavy-Le Traon A,Cornac A,Güell A,Houin G

更新日期：1995-07-01 00:00:00

abstract：:This multicenter, open-label study evaluated the effects of multiple doses of peginterferon alfa-2b on the steadystate pharmacokinetics of methadone in 20 adults with hepatitis C virus infection who were enrolled in a methadone maintenance program. All subjects received peginterferon alfa-2b 1.5 mug/kg/wk for 4 weeks ...

journal_title：Journal of clinical pharmacology

authors： Gupta SK,Sellers E,Somoza E,Angles L,Kolz K,Cutler DL

更新日期：2007-05-01 00:00:00

abstract：:To evaluate the population pharmacokinetics of valproic acid in children, 97 steady-state serum valproate concentration measurements were gathered during normal, routine, outpatient care of 52 children with epilepsy (1.2-16 years of age). Levels were obtained from patients receiving valproate monotherapy (49%) or valp...

journal_title：Journal of clinical pharmacology

authors： Botha JH,Gray AL,Miller R

更新日期：1995-10-01 00:00:00

abstract：:The pharmacokinetics, pharmacodynamics, and safety of fosinopril sodium (SQ 28,555), a new orally active angiotensin-converting enzyme (ACE) inhibitor, was evaluated in 73 healthy men in two separate studies. In study I, doses ranging from 10 to 640 mg were administered once daily for 3 days to seven groups of five su...

journal_title：Journal of clinical pharmacology

authors： Duchin KL,Waclawski AP,Tu JI,Manning J,Frantz M,Willard DA

更新日期：1991-01-01 00:00:00

abstract：:A double-blind, placebo-controlled trial was performed to establish the duration of action of antihistamines and their ability to attenuate the adverse affects associated with histamine release. Thirty volunteers were assigned randomly to receive either placebo or a combination of the H1 blocker dimetindene maleate (0...

journal_title：Journal of clinical pharmacology

authors： Doenicke A,Moss J,Toledano A,Hoernecke R,Lorenz W,Ostwald P

更新日期：1997-02-01 00:00:00

abstract：:A clinical study of bumetanide, a new diuretic, was conducted in outpatients of a cardiology clinic to determine its long-term effectiveness and safety in the treatment of peripheral edema due to congestive heart failure. The drug was administered for at least 24 weeks on a selected group of 34 patients. The patients ...

journal_title：Journal of clinical pharmacology

authors： Handler B,Dhingra RC,Rosen KM

更新日期：1981-11-01 00:00:00

abstract：:This study was undertaken to determine whether rofecoxib can interfere with CYP1A2 activity in humans using theophylline as a probe substrate. Single oral doses of theophylline were administered to each of three panels of 12 healthy subjects receiving daily doses of rofecoxib for 7 days to examine the effect of rofeco...

journal_title：Journal of clinical pharmacology

authors： Bachmann K,White D,Jauregui L,Schwartz JI,Agrawal NG,Mazenko R,Larson PJ,Porras AG

更新日期：2003-10-01 00:00:00

abstract：:A population pharmacokinetic (PPK) model of pomalidomide was developed and the influence of demographic and disease-related covariates on PPK parameters was assessed based on data from 6 clinical trials of pomalidomide (dose range, 0.5-10 mg) in healthy participants (n = 96) and patients with multiple myeloma (MM; n =...

journal_title：Journal of clinical pharmacology

authors： Li Y,Xu Y,Liu L,Wang X,Palmisano M,Zhou S

更新日期：2015-05-01 00:00:00

abstract：:Twenty-three normal volunteers who received morphine sulphate (MS Contin) with naltrexone completed this randomized, analytically blinded, two-way crossover comparison of the bioavailability of one 200-mg oral controlled-release morphine sulfate tablet with two 100-mg MSC tablets. Morphine effects were blocked by thre...

journal_title：Journal of clinical pharmacology

authors： Kaiko RF,Grandy RP,Reder RF,Goldenheim PD,Sackler RS

更新日期：1995-05-01 00:00:00

abstract：:Antibody-drug conjugates (ADCs) represent an innovative therapeutic approach that provides novel treatment options and hope for patients with cancer. By coupling monoclonal antibodies (mAbs) to cytotoxic small-molecule payloads with a plasma-stable linker, ADCs offer the potential for increased drug specificity and fe...

journal_title：Journal of clinical pharmacology

authors： Vezina HE,Cotreau M,Han TH,Gupta M

更新日期：2017-10-01 00:00:00

abstract：:To test the effects of fluvastatin on low-density lipoprotein (LDL) receptor activity in patients with heterozygous familial hypercholesterolemia, the authors measured LDL receptor activity in stimulated T-lymphocytes prepared from 34 patients before and after treatment with 40 mg fluvastatin daily for 12 weeks. Maxim...

journal_title：Journal of clinical pharmacology

authors： Raungaard B,Brorholt-Petersen JU,Jensen HK,Faergeman O

更新日期：2000-04-01 00:00:00

abstract：:Renal electrolyte excretion patterns were determined in nonedematous healthy volunteers following bumetanide and furosemide in two separate clinical studies. In study 1, intravenous bumetanide was administered to 24 subjects at four dose levels. In study 2, bumetanide (1 or 2 mg) or furosemide (40 or 80 mg) was admini...

journal_title：Journal of clinical pharmacology

authors： Hutcheon DE,Vincent ME,Sandhu RS

更新日期：1981-11-01 00:00:00