Abstract:
PURPOSE:Sitagliptin, a dipeptidyl peptidase (DPP)-IV inhibitor approved for the treatment of type 2 diabetes, is reported to be more efficacious in Indian patients than non-Indian patient population. The objective of the study was to evaluate pharmacokinetic and pharmacodynamic (PK/PD) parameters of single-dose sitagliptin 100 mg (Januvia) in healthy Indian male participants. METHOD:In a randomised, single-dose, open-label, three-treatment, three-period, three-sequence, crossover bioavailability study, 18 healthy male participants received single-dose of sitagliptin under fasted and fed conditions. PK parameters (Cmax, Tmax, AUC0-∞ and t1/2) were determined using Phoenix WinNonlin software. PD parameters [DPP-IV inhibition, active glucagon-like peptide-1 (GLP-1) and insulin] were determined using established methods. RESULTS:PK parameters expressed in mean (SD) were Cmax 491.7 (135.9) ng/mL; AUC0-∞ 4256.1 (509.9) ng· hr/mL, Tmax 2.9 (1.0) hr and t1/2 10.4 (3.0) hr. The weighted average (WA) plasma DPP-4 inhibition over 24 h was 89.6% and WA of plasma active GLP-1 over 2 h after standardised meal (geometric mean ratio) was 11.1 (9.9) pM/L which is two- to- four fold higher compared to that reported in other populations. The mean average (SD) AUC of plasma insulin over 2 h of standardised meal was 47.9 (24.9) μIU/mL. CONCLUSION:Although, there are differences in pharmacokinetic parameters, no clinically meaningful differences were observed with respect to DPP-IV inhibition between Indian and non-Indian population.
journal_name
Eur J Clin Pharmacoljournal_title
European journal of clinical pharmacologyauthors
Sangle GV,Patil M,Deshmukh NJ,Shengule SA,Kamble S,Vuppalavanchu KK,Kale S,Baig MLA,Singh G,Shaikh J,Tripathi J,Aravindababu Pdoi
10.1007/s00228-018-2433-5subject
Has Abstractpub_date
2018-05-01 00:00:00pages
561-569issue
5eissn
0031-6970issn
1432-1041pii
10.1007/s00228-018-2433-5journal_volume
74pub_type
杂志文章,随机对照试验abstract:OBJECTIVE:To compare the efficacy and safety of repaglinide, a novel oral prandial glucose regulator, with that of glibenclamide, an oral hypoglycaemic agent, in the treatment of patients with type 2 diabetes. METHODS:This was a 14-week, double-blind, parallel-group trail in which a total of 195 type 2 diabetic patien...
journal_title:European 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
doi:10.1007/s002280050613
更新日期:1999-05-01 00:00:00
abstract::Levosimendan is a new calcium-sensitiser intended for the treatment of congestive heart failure. The results of preclinical studies indicate it has positive inotropic and vasodilator effects. In the open study reported here up to 5 mg levosimendan and vehicle were administered to 8 healthy male volunteers at one- to 2...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF02570507
更新日期:1994-01-01 00:00:00
abstract:PURPOSE:Some reports have described arterial hypertension (AH) in patients treated by serotonin reuptake inhibitor (SRI) or serotonin-norepinephrine reuptake inhibitor (SNRI) antidepressants. The mechanism remains discussed, some authors suggesting a role of SERT (SERotonin Transporter) inhibition whereas others discus...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s00228-020-02913-0
更新日期:2020-09-01 00:00:00
abstract::Recently, interactions of herbal medicines with synthetic drugs came into focus of particular interest. In the past 3 years, more than 50 papers were published regarding interactions between St. John's wort (Hypericum perforatum L.; SJW) and prescription drugs. Co-medication with SJW resulted in decreased plasma conce...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章,评审
doi:10.1007/s00228-006-0096-0
更新日期:2006-03-01 00:00:00
abstract::Procaine esterase activity in plasma from patients with renal failure is decreased by 40%. Since cyanate is formed from urea and readily carbamylates certain blood proteins, a possible role for cyanate in the depression of plasma esterase activity in uraemic patients was considered. However, in vitro carbamylation of ...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00609899
更新日期:1983-01-01 00:00:00
abstract:BACKGROUNDS AND AIMS:Development of safe and effective rescue regimens for eradication failure of Helicobacter pylori infection by standard regimens is an urgent task. We designed the prospective study to compare the efficacy of two rescue regimens after eradication failure by the standard triple therapy. METHODS:One ...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章,随机对照试验
doi:10.1007/s00228-007-0302-8
更新日期:2007-08-01 00:00:00
abstract::A phamacokinetic study in man has been made of a new dosage form of diclofenac hydroxyethylpyrrolidine (DIEP); soluble salt packed in sachets was compared with diclofenac sodium as enteric coated tablets. Oral DIEP 2 X 50 mg showed a significant difference in absorption kinetics (ka, lag time and tmax) as compared to ...
journal_title:European journal of clinical pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1007/BF00265987
更新日期:1990-01-01 00:00:00
abstract::The time-courses of plasma carbamazepine concentrations were followed in six apparently healthy adult subjects who, at different times, took single oral drug doses of 200, 400, 500, 600, 700, 800 and 900 mg. There were some suggestions of impaired bioavailability of the drug when given in tablet form. The following va...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00561065
更新日期:1977-12-28 00:00:00
abstract::In 8 social drinkers, the effect of a single dose of Liv.52 or placebo on ethanol absorption has been studied after ingestion of 30 ml whisky in 5 min. The t1/2 absorption with Liv.52 was 3.62 min, significantly less than after placebo, 6.29 min. The peak concentration after Liv.52 (49.9 mg.100 ml-1) was significantly...
journal_title:European journal of clinical pharmacology
pub_type: 临床试验,杂志文章
doi:10.1007/BF00280076
更新日期:1991-01-01 00:00:00
abstract:PURPOSE:The 388A>G and the 521T>C polymorphism of the SLCO1B1 gene affect the activity of the uptake transporter OATP1B1, thus influencing kinetics, safety, and efficacy of substrate drugs. To evaluate the impact of these polymorphisms in populations of different ethnic origins, it is important to know their frequencie...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s00228-011-1065-9
更新日期:2011-11-01 00:00:00
abstract::The effects of an oral dose of atropine (0.03 mg/kg body weight) and an IM (0.02 mg/kg) dose on the heart rate and salivary flow in seven healthy adult volunteers were compared to see whether the oral dose was sufficient to inhibit vagal reflexes of the heart. Atropine concentrations in plasma were determined by an M2...
journal_title:European journal of clinical pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1007/BF00192357
更新日期:1995-01-01 00:00:00
abstract::Caffeine metabolites in urine from premature infants were analysed by TLC and HPLC. Caffeine, dimethyluric acids, mono- and dimethylxanthines and, for the first time, a uracil derivative (6-amino-5-[N-methylformylamino]-1,3-dimethyluracil) were identified. ...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00613531
更新日期:1986-01-01 00:00:00
abstract:OBJECTIVE:Withdrawal of a drug from the market for safety reasons is a serious and sometimes complex decision. The scientific evidence supporting drug withdrawals in the past years is critically appraised. METHODS:With data provided by the Spanish Medicines Agency, all drugs withdrawn from the Spanish market for safet...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章,评审
doi:10.1007/s002280100265
更新日期:2001-04-01 00:00:00
abstract:PURPOSE:Our aim was to observe the impact of CYP3A4*1G genetic polymorphism on lipid-lowering efficacy of statins. METHODS:We studied 217 unrelated hyperlipidemic patients who prospectively received atorvastatin and 199 patients who received simvastatin as a single-agent therapy (20 mg day(-1) p.o.) for 4 weeks. Genot...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s00228-008-0502-x
更新日期:2008-09-01 00:00:00
abstract:OBJECTIVES:Methantheline is a strong muscarinic receptor blocking drug used in the treatment of overactive bladder syndrome, hypersalivation and hyperhidrosis. To provide basic information on the pharmacokinetics, magnitude of pharmacodynamic (PD) effects and their correlations with plasma concentrations, we performed ...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章,随机对照试验
doi:10.1007/s00228-012-1286-6
更新日期:2012-11-01 00:00:00
abstract:OBJECTIVES:Evidence exists to suggest that diclofenac is metabolised by CYP2C9. The present study was undertaken in order to evaluate the effect of the single CYP2C9*3 variant on drug metabolism using diclofenac as a probe drug. METHODS:A single dose of diclofenac was administered orally to 12 healthy subjects in whom...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s002280050722
更新日期:2000-04-01 00:00:00
abstract::Hemodynamic changes for 30 min after intravenous administration of molsidomin 4 mg were studied in 10 patients. Pulmonary artery pressure, pulmonary wedge pressure, right atrial pressure and aortic pressure decreased significantly after 15 min, and after 30 min they were still below the control level. Heart rate incre...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00716357
更新日期:1978-06-19 00:00:00
abstract:OBJECTIVE:The aim of this study was to define the pharmacokinetic profile of free carbamazepine (F-CBZ) in adult Omani epileptic patients in order to improve on dosing schedules through population pharmacokinetic analysis using the NONMEM program. METHOD:Steady-state trough F-CBZ serum concentrations, carbamazepine (C...
journal_title:European journal of clinical pharmacology
pub_type: 临床试验,杂志文章
doi:10.1007/s002280100300
更新日期:2001-06-01 00:00:00
abstract:AIM:Our aim was to characterize utilization patterns for drugs used to treat attention deficit/hyperactivity disorder (ADHD) on the level of the individual patient among Danish users, focusing on treatment duration, doses used, and concurrent use of ADHD and non-ADHD drugs. METHODS:Using the Danish Registry of Medicin...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s00228-012-1344-0
更新日期:2013-03-01 00:00:00
abstract:OBJECTIVE:To investigate the influence of theophylline on erythropoiesis in chronic obstructive pulmonary disease (COPD) and explore the potential underlying mechanisms. METHODS:We evaluated the haematological parameters and erythropoietin (EPO) values in 38 COPD patients, 18 of which had been treated with theophyllin...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s00228-003-0640-0
更新日期:2003-09-01 00:00:00
abstract::An expert meeting to discuss population pharmacokinetic/pharmacodynamic software was held in Brussels in November 1993 under the auspices of the European Co-operation in Science and Technology (COST), Medicine (B1) programme. Recently developed statistical methods offer the possibility of gaining integrated informatio...
journal_title:European journal of clinical pharmacology
pub_type:
doi:10.1007/BF00191898
更新日期:1994-01-01 00:00:00
abstract::Pharmacokinetic interactions between antipyrine and acetaminophen were evaluated in 7 healthy volunteers. On 3 occasions subjects received: 1, antipyrine 1.0 g intravenously (i.v.); 2, acetaminophen 650 mg i.v.; 3, antipyrine 1.0 g and acetaminophen 650 mg i.v. simultaneously. Between Trials 1 and 3, antipyrine elimin...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00561374
更新日期:1988-01-01 00:00:00
abstract::Plasma aspirin, salicylate and salicyluric acid concentrations were monitored in young, elderly and alcoholic subjects after ingestion of a single 1.2 g dose of soluble aspirin. The plasma aspirin, salicylate and unbound salicylate concentration-time profiles varied considerably between individual subjects. Most of th...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00543800
更新日期:1983-01-01 00:00:00
abstract:PURPOSE:A variety of diagnostic methods are available to validate the performance of population pharmacokinetic models. Internal validation, which applies these methods to the model building dataset and to additional data generated through Monte Carlo simulations, is often sufficient, but external validation, which req...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s00228-020-03036-2
更新日期:2020-11-11 00:00:00
abstract::The effect of menstrual cycle on the pharmacokinetics of theophylline has been studied in 9 female asthmatic patients. At three different times during the cycle (first, tenth and twentieth days) each subject received an i.v. infusion of 240 mg theophylline. Significant changes were found in the kinetics of theophyllin...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF02657059
更新日期:1990-01-01 00:00:00
abstract:PURPOSE:The purpose of this study is to determine the impacts of CYP3A5 polymorphism on tacrolimus concentration and the proportion of patients within a target therapeutic range during the first week after transplantation together with the 3-month acute rejection rate in kidney transplant patients receiving a minimized...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s00228-015-1990-0
更新日期:2016-03-01 00:00:00
abstract:OBJECTIVE:This study was performed to investigate whether it is possible to use saliva instead of blood usually used for therapeutic drug monitoring (TDM) of disopyramide. METHODS:Six healthy male volunteers ingested 200 mg of disopyramide base, and the disopyramide concentrations in saliva and plasma (total and unbou...
journal_title:European journal of clinical pharmacology
pub_type: 临床试验,杂志文章
doi:10.1007/s002280050250
更新日期:1997-01-01 00:00:00
abstract::The comparative enzyme inducing effects of rifabutin and the chemically related drug rifampicin have been investigated in 8 normal subjects. Rifampicin 600 mg daily for 7 days caused considerable shortening of the antipyrine half-life and a marked increase in antipyrine clearance, associated with an increased rate of ...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00615223
更新日期:1988-01-01 00:00:00
abstract:OBJECTIVE:To quantify the relation between local and systemic magnitudes of effects of inhaled formoterol and salbutamol. METHODS:Twenty-eight stable asthmatic patients completed this double-blind, randomised crossover study. Pre-drug administration FEV1 (mean 2.08 L) was 49-93% of predicted and reversibility 16-82% a...
journal_title:European journal of clinical pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
doi:
更新日期:2002-07-01 00:00:00
abstract::The four sulphonamides studied--furosemide, tolbutamide, sulfafurazole and sulfonamidochlorobenzoic acid--bind to human albumin at the same sites but with decreasing affinity. These sites are also common to other drugs, namely acenocoumarin, chlorophenoxyisobutyric acid, phenylbutazone and warfarin. In plasma, the fou...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00609473
更新日期:1976-06-15 00:00:00