Abstract：
:Carboxylesterases (CESs) play major roles in catalyzing the hydrolysis of a wide range of ester- and amide-containing compounds. CESs dominate both the biotransformation of numerous therapeutic drugs and the detoxification of environmental toxicants, and the activity alteration of CESs may be a determinant reason for modification of the resultant pharmacokinetic/pharmacodynamic profile when two or more drugs are concurrently used. Herein, we provide a comprehensive review of the current literature involving of induction and inhibition on CESs by both exogenous and endogenous compounds. In particular, the inhibition constant and inhibition pattern of inhibitors on CESs in studies using animal microsomes or human recombinant CESs are summarized. Further studies are needed to clarify the underlying regulation mechanism, and alterations in CESs activity should be taken into consideration for safe clinical therapy.
journal_name
Eur J Drug Metab Pharmacokinetjournal_title
European journal of drug metabolism and pharmacokineticsauthors
Xu Y,Zhang C,He W,Liu Ddoi
10.1007/s13318-016-0326-5subject
Has Abstractpub_date
2016-08-01 00:00:00pages
321-30issue
4eissn
0378-7966issn
2107-0180pii
10.1007/s13318-016-0326-5journal_volume
41pub_type
杂志文章,评审abstract：:Sertraline potently inhibits cytochrome P450 2B6 (CYP2B6) in vitro. Bupropion is commonly co-prescribed with sertraline and is exclusively metabolized by CYP2B6 to its major active metabolite hydroxybupropion. Putatively the co-administration of bupropion and sertraline could lead to a significant pharmacokinetic drug...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s13318-011-0065-6
更新日期：2012-03-01 00:00:00
abstract：:This study describes an approach permitting the determination of compartmental concentration and drug kinetics in the case of chronobiological variations of elimination rate. ...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03190035
更新日期：1999-10-01 00:00:00
abstract：BACKGROUND AND OBJECTIVE:Polyethylene glycol-modified canine uricase (PEG-UHC) prepared with a lower-molecular-weight (5 kDa) PEG is used to treat gout. This study investigated the comparative pharmacokinetics of single and multiple doses of PEG-UHC administered intravenously and a single dose of uricase (UHC) administ...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s13318-020-00612-w
更新日期：2020-08-01 00:00:00
abstract：:The aim of the present study was to investigate the relative bioavailability and bioequivalence of a new tablet formulation of metformin hydrochloride with reference to a standard product in healthy Chinese adult male volunteers. Two randomized, comparative, two-way crossover studies were therefore conducted. In study...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章,随机对照试验
doi：10.1007/BF03190986
更新日期：2007-01-01 00:00:00
abstract：:Angiogenesis is integral to tumour growth and invasion, and is a key target for cancer therapeutics. However, for many of the licensed indications, only a modest clinical benefit has been observed for both monoclonal antibody and small-molecule tyrosine kinase inhibitor anti-angiogenic therapy. Pre-clinical and clinic...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章,评审
doi：10.1007/s13318-017-0442-x
更新日期：2018-04-01 00:00:00
abstract：:This study examined the effects of the absorption enhancers, acylcarnitines, on efflux transporting systems, including P-glycoprotein (P-gp) and other efflux transporters, and elucidated the importance of acyl chain length and the concentration of acylcarnitine on the activity of efflux transport. The effects of two a...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s13318-010-0001-1
更新日期：2010-09-01 00:00:00
abstract：:A bioequivalence study compares the bioavailability between a test and a reference drug product in terms of the rate and extent of drug absorption. Area under the plasma concentration-time curve (AUC) and maximum plasma concentration (Cmax) are the pharmacokinetic parameters that serve as characteristics for the asses...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03190024
更新日期：1999-07-01 00:00:00
abstract：BACKGROUND AND OBJECTIVES:Lidocaine 5% medicated plaster is the first lidocaine containing product for chronic use. As no previous investigations have been conducted to evaluate the population pharmacokinetics of long-term exposure to lidocaine 5% medicated plasters, further insights into the evaluation of the pharmaco...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章,多中心研究,随机对照试验
doi：10.1007/s13318-017-0400-7
更新日期：2017-10-01 00:00:00
abstract：BACKGROUND AND OBJECTIVES:Ketoprofen, a potent nonsteroidal anti-inflammatory drug, is clinically administered as a racemic mixture. One of the possible metabolism routes of ketoprofen is the inversion of the R- to S-enantiomer in the gastrointestinal tract. Ketoprofen, as a weak acid drug, might undergo recirculation ...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 临床试验,杂志文章,随机对照试验
doi：10.1007/s13318-015-0313-2
更新日期：2016-12-01 00:00:00
abstract：:Benzo[alpha]pyrene (B[a]P) is a product derived from incomplete combustion of organic material and is considered responsible for chemically-induced cancer in humans. In the present study, the levels of noradrenaline (NA), dopamine (DA), dihydroxyphenylacetic acid (DOPAC), homovanillic acid (HVA), 5-hydroxytryptamine (...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03189998
更新日期：1998-10-01 00:00:00
abstract：:Diabetes mellitus is becoming an increasingly prevalent disease that concerns patients and healthcare professionals worldwide. Among many anti-diabetic agents in clinical uses, numerous reports are available on their altered pharmacokinetics because of changes in the expression of drug transporters and metabolic enzym...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章,评审
doi：10.1007/s13318-015-0306-1
更新日期：2016-06-01 00:00:00
abstract：:Pharmacokinetics of ketoprofen (KTP) enantiomers has been studied in patients with rheumatoid arthritis (RA) following administration of a single oral dose of 100 mg rac-KTP during multidrug therapy taking into consideration the genotype of RA patients Concentrations of (-)-R and (+)-S enantiomers of KTP in plasma, ur...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s13318-011-0041-1
更新日期：2011-09-01 00:00:00
abstract：:The present investigation was designed and undertaken in order to substantiate further contention concerning the universality of the utilization of PEG polymers as matrix carriers. This study could then be considered an attempt to enhance the dissolution rate of triamterene, with the subsequent enhancement in its abso...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03188855
更新日期：1994-10-01 00:00:00
abstract：:Urodynamic model was developed which, in conjunction with a compartmental pharmacokinetic model, was used for study of factors influencing drug concentrations in urine: urine flow rate, residual bladder urine, maximal bladder urine, stage of renal failure, and elimination kinetics of drugs. Norfloxacin (NOR) was used ...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：
更新日期：1991-01-01 00:00:00
abstract：:IdB 1016 is a complex of silybin (the main active component of silymarin) and phosphatidylcholine, which in animal models shows greater oral bioavailability and therefore greater pharmacological activity compared with pure silybin and silymarin. In order to assess its pharmacokinetic profile in man, plasma silybin lev...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 临床试验,杂志文章,随机对照试验
doi：10.1007/BF03190223
更新日期：1990-10-01 00:00:00
abstract：:The effects of potassium ethylxanthogenate (PEX) and 2,3-Dimercaptopropane sulphonate sodium (Unithiol) on the pentobarbital (40 mg/kg, body weight i.v.) (PB) sleeping time, pharmacokinetics, and metabolism, were studied in comparative experiments on male albino mice. It was established that the pretreatment of animal...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03189539
更新日期：1982-01-01 00:00:00
abstract：:The transdermally applied dopamine receptor agonist rotigotine is extensively metabolized in the liver. An open-label, parallel-group study was conducted to evaluate the effects of moderate hepatic impairment on the pharmacokinetics, safety and tolerability of rotigotine. Eight subjects with normal hepatic function an...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章,多中心研究
doi：10.1007/s13318-013-0153-x
更新日期：2014-09-01 00:00:00
abstract：:This study developed a physiologically based pharmacokinetic (PBPK) model in intraabdominally infected rats and extrapolated it to humans to predict the levofloxacin pharmacokinetics and penetration into tissues. Twelve male rats with intraabdominal infections induced by Escherichia coli received a single dose of 50 m...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s13318-015-0271-8
更新日期：2016-08-01 00:00:00
abstract：:The co-administration of lidocaine and propranolol leads to significant drug-drug interactions. Beta-blockers decrease liver perfusion and inhibit the activity of hepatic microsomal lidocaine metabolizing enzymes of the P450_2D subfamily. Hence, there is a resulting reduction in the hepatic breakdown of lidocaine and ...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03191006
更新日期：2007-10-01 00:00:00
abstract：:The pharmacokinetics of flumecinol (Zixoryn) a new hepatic enzyme inducer has been studied in four beagle dogs and six healthy volunteers. The beagle dogs and the volunteers received the drug orally in a dose of 40 mg/kg of body weight and of 100 mg single dose respectively. Flumecinol was extracted from plasma with d...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03188725
更新日期：1982-01-01 00:00:00
abstract：:The pharmacokinetic-pharmacodynamic (PK-PD) relationship of the proton pump inhibitor rabeprazole in healthy Chinese volunteers was characterized via a population approach. Healthy Chinese male volunteers were enrolled in the clinical trial. Subjects were divided into three groups by their CYP2C19 genotype. Serum conc...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03190639
更新日期：2006-01-01 00:00:00
abstract：BACKGROUND AND OBJECTIVES:Clopidogrel is an antiplatelet and antithrombotic prodrug. It has poor oral bioavailability due to poor dissolution and possible premature degradation in the intestine. Accordingly, the objective of this study was to enhance clopidogrel dissolution rate and to reduce its premature degradation ...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s13318-015-0311-4
更新日期：2016-12-01 00:00:00
abstract：:The effects of aluminium, manganese, ferrous and ferric iron, cobalt, nickel, copper, zinc, cadmium, barium, mercury and lead ions on the rat hepatic UDPglucuronosyltransferase activity with regard to 4-methylumbelliferone, 4-nitrophenol, bilirubin, and 2-aminophenol were investigated in vitro. Conjugation of bilirubi...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03189441
更新日期：1980-01-01 00:00:00
abstract：:This study compared some pharmacokinetic parameters of DL-lysine-acetyl salicylate administered intravenously (i.v.) and intramuscularly (i.m.) at a dose of 20 mg/kg in camels, sheep and goats. The data was analyzed using a non-compartmental model. In camels, sheep and goats given the drug i.v., the t1/2 values were 4...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03190500
更新日期：2003-04-01 00:00:00
abstract：:Hepatic distributional volumes were investigated in the in situ perfused rat liver. Perfusion experiments were conducted using Krebs bicarbonate buffer delivered via the portal vein in single-pass mode at a total flow rate of 15 mL/min. A bolus dose of normal erythrocytes (RBC, vascular marker) and Evans blue (EB, ext...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03190469
更新日期：2006-10-01 00:00:00
abstract：:In a single dose, randomized, cross-over study, with one week of wash-out period, the relative bioavailability of Dopegyt tablets containing 250 mg alpha-methyldopa (AMD) and Presinol film tablets with identical active ingredient content was examined in 24 healthy volunteers. Since technologically two completely diffe...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03190372
更新日期：2001-01-01 00:00:00
abstract：:The pharmacokinetics, biotransformation, protein binding and tissue distribution of mitonafide and pinafide were studied after single i.v. and oral administration of each drug (20 mg/Kg) in female rats. In pregnant rats a study of cross placental-barrier after i.v. administration of the two drugs was also performed. T...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03189110
更新日期：1986-10-01 00:00:00
abstract：:Bioavailability of lansoprazole, a new gastric proton pump inhibitor, was investigated in 12 healthy subjects. Each subject received in random order, lansoprazole (30 mg) alone or associated with standard meal or with antacids (aluminium and magnesium hydroxides) or one hour later than antacids. Lansoprazole and metab...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 临床试验,杂志文章,随机对照试验
doi：
更新日期：1991-01-01 00:00:00
abstract：:Vitexin-4″-O-glucoside (VOG), being a main component in the leaves of Crataegus pinnatifida Bge. var. major, was isolated and then three different doses (20, 40, and 60 mg/kg) of VOG were administered intravenously to rats. To study its pharmacokinetics, a simple and rapid HPLC method was developed using hesperidin as...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s13318-011-0071-8
更新日期：2012-06-01 00:00:00
abstract：:A major biotransformation pathway for many NSAIDs from the group of optically active 2-arylpropionic acids is the conjugation with D-glucuronic acid, forming diastereomers. These conjugates of the S-(+)-and the R-(-)-enantiomers can be separated directly, e.g., by ion-pair chromatography on a C18-column using a mixtur...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03189905
更新日期：1987-10-01 00:00:00
