Pharmacokinetics of chlordesmethyldiazepam after single-dose oral administration in humans.

Abstract:

:The pharmacokinetics of chlordemethyldiazepam--a pharmacologically very active new 1,4-benzodiazepine derivative--in healthy subjects after administration of a single oral dose of 2 mg, was studied. Peak concentrations were reached in 1.2 +/- 0.2 hours. Plasma levels declined with a biphasic pattern, and the elimination phase had a half-life of 82.9 +/- 14.1 hours. The concentrations of the main metabolite of chlordemethyldiazepam, lorazepam, were about 7% of those of the parent compound. In urine only conjugated lorazepam could be found its 96 hour excretion reaching about 15% of the administered dose of parent drug.

authors

Bareggi SR,Pirola R,Leva S,Zecca L

doi

10.1007/BF03189844

subject

Has Abstract

pub_date

1986-07-01 00:00:00

pages

171-4

issue

3

eissn

0378-7966

issn

2107-0180

journal_volume

11

pub_type

杂志文章
  • Bioequivalency evaluation by comparison of in vitro dissolution and in vivo absorption using reference equations.

    abstract::Using in vitro dissolution and in vivo absorption of different generics or batches for an appropriate drug and dosage form, a reference equation of form: ka = a+bkd+dkd2 can be proposed. In the case of availability of standardised in vitro-in vivo data for a specific drug, a Level A a correlation of this type containi...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/BF03188930

    authors: Kayali A

    更新日期:1994-07-01 00:00:00

  • Prediction of Half-Life Extension of Peptides via Serum Albumin Binding: Current Challenges.

    abstract::The development of peptide therapeutics has increased enormously in recent decades. Many of the peptide drugs and antibody fragments that lack Fc backbone have a short half-life in circulation. In general, the half-life supports the design of the dosing regimen and frequency of administration, which are key aspects in...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/s13318-020-00664-y

    authors: Hijazi Y

    更新日期:2021-01-01 00:00:00

  • Determination of the Pharmacokinetics and Tissue Distribution of Methyl 3,4-Dihydroxybenzoate (MDHB) in Mice Using Liquid Chromatography-Tandem Mass Spectrometry.

    abstract:BACKGROUND AND OBJECTIVES:Methyl 3,4-dihydroxybenzoate (MDHB) has the potential to prevent neurodegenerative diseases (NDDs). The present work aims to reveal the pharmacokinetics and tissue distribution characteristics of MDHB. METHODS:The pharmacokinetics and tissue distribution of MDHB were analyzed using LC-MS/MS a...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/s13318-018-0512-8

    authors: Wang JH,Hu SH,Su JY,Pan JP,Mi XN,Geng HJ,Zhang W,Cai L,Su CF,Hong AH,Luo HM

    更新日期:2019-04-01 00:00:00

  • Metabolism of ticlopidine in rats: identification and quantitative determination of some its metabolites in plasma, urine and bile.

    abstract::The fate of Ticlopidine, a new inhibitor of platelet aggregation, has been studied in rats following single oral doses. The compound was quickly absorbed as evaluated by the time of the peak plasma concentration. The metabolism of Ticlopidine involved N-oxidation, cleavage of the N-C bond, oxidation of aliphatic carbo...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/BF03189474

    authors: Tuong A,Bouyssou A,Paret J,Cuong TG

    更新日期:1981-01-01 00:00:00

  • Pharmacokinetic study of multiple active constituents after oral gavage of Guizhi decoction in rats using a LC-MS/MS method.

    abstract::Guizhi decoction (GZD) is a classic traditional Chinese medicine formula, clinically used for the treatment of influenza, common cold, and other pyretic conditions. A sensitive, specific, and validated liquid chromatography-tandem mass spectrometric (LC-MS/MS) method was developed to investigate the pharmacokinetic pr...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/s13318-013-0121-5

    authors: Chen Y,Gao C,Ma Y,Qiu F

    更新日期:2013-12-01 00:00:00

  • Parameterization of Microsomal and Cytosolic Scaling Factors: Methodological and Biological Considerations for Scalar Derivation and Validation.

    abstract::Mathematical models that can predict the kinetics of compounds have been increasingly adopted for drug development and risk assessment. Data for these models may be generated from in vitro experimental systems containing enzymes contributing to metabolic clearance, such as subcellular tissue fractions including micros...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/s13318-020-00666-w

    authors: Doerksen MJ,Jones RS,Coughtrie MWH,Collier AC

    更新日期:2020-12-19 00:00:00

  • Deuterium isotope effects on caffeine metabolism.

    abstract::The aim of this work was to study the influence of labelling on caffeine metabolism according to the incubation mode. It has been observed that labelling induces an isotopic effect on metabolisation speed: apparent half-lives are systematically increased. Moreover, isotopic effects are in agreement with those previous...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/BF03189795

    authors: Benchekroun Y,Dautraix S,Desage M,Brazier JL

    更新日期:1997-04-01 00:00:00

  • Impact of Efavirenz Metabolism on Loss to Care in Older HIV+ Africans.

    abstract::BACKGROUND AND OBJECTIVE: Efavirenz is commonly used in Africa and is frequently associated with neurocognitive toxicity, which may compromise clinical outcomes. Older individuals are at increased risk for drug toxicity and clinical outcomes may be worse in older age, particularly among those individuals with cytochro...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/s13318-018-0507-5

    authors: Torgersen J,Bellamy SL,Ratshaa B,Han X,Mosepele M,Zuppa AF,Vujkovic M,Steenhoff AP,Bisson GP,Gross R

    更新日期:2019-04-01 00:00:00

  • Disposition of paclitaxel (Taxol) and its metabolites in patients with advanced breast cancer (ABC) when combined with trastuzumab (Hercpetin).

    abstract::Monoclonal antibodies are capable of modulating drug metabolising enzymes resulting in unexpected plasma concentrations of a drug when given concomitantly. Therefore plasma concentration of paclitaxel (PTX) and its metabolites has been monitored in 10 patients with advanced breast cancer during treatment with PTX alon...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/BF03190613

    authors: Furtlehner A,Schueller J,Jarisch I,Ostermann E,Czejka M

    更新日期:2005-07-01 00:00:00

  • The Effect of Verapamil, a P-gp Inhibitor, on the Pharmacokinetics, Safety, and Tolerability of Omadacycline in Healthy Adults: A Phase I, Open-Label, Single-Sequence Study.

    abstract:BACKGROUND:Omadacycline is a semisynthetic aminomethylcycline antibacterial derived from the tetracycline class. It is approved in the USA to treat adults with acute bacterial skin and skin-structure infections and community-acquired bacterial pneumonia. OBJECTIVES:This phase I, open-label study evaluated the effect o...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/s13318-020-00651-3

    authors: Hunt TL,Tzanis E,Bai S,Manley A,Chitra S,McGovern PC

    更新日期:2021-01-01 00:00:00

  • Pharmacodynamic and Pharmacokinetic Markers For Anti-angiogenic Cancer Therapy: Implications for Dosing and Selection of Patients.

    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

    authors: Morotti M,Dass PH,Harris AL,Lord S

    更新日期:2018-04-01 00:00:00

  • Age-related changes in mRNA levels of hepatic transporters, cytochrome P450 and UDP-glucuronosyltransferase in female rats.

    abstract::Hepatic transporters and metabolic enzymes affect drug pharmacokinetics. Limited information exists on the alteration in mRNA levels of hepatic transporters and metabolic enzymes with aging. We examined the effects of aging on the mRNA levels of representative hepatic drug transporters and metabolic enzymes by analyzi...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/s13318-014-0208-7

    authors: Kawase A,Ito A,Yamada A,Iwaki M

    更新日期:2015-06-01 00:00:00

  • Pharmacokinetics of the Urokinase Receptor-Derived Peptide UPARANT After Single and Multiple Doses Administration in Rats.

    abstract:BACKGROUND AND OBJECTIVES:UPARANT has emerged as a novel therapeutic agent with the potential to treat ocular diseases as assessed by studies in animal models. Since limited information is available on the pharmacokinetics of UPARANT, the aim of this study is to evaluate its pharmacokinetics after single and multiple a...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/s13318-020-00654-0

    authors: Ciccone M,D'Alonzo D,Cangiano AM,De Fenza M,Pavone V,Mancinelli A

    更新日期:2021-01-01 00:00:00

  • Fate and disposition of bromocriptine in animals and man. I: structure elucidation of the metabolites.

    abstract::A total of 16 metabolites of bromocriptine could be isolated from rat bile and incubates of rat liver cell preparations using [6-methyl-14C]bromocriptine as substrate. Separation and purification was achieved by reversed-phase liquid chromatography and preparative thin-layer chromatography in conjunction with radioact...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/BF03189631

    authors: Maurer G,Schreier E,Delaborde S,Loosli HR,Nufer R,Shukla AP

    更新日期:1982-10-01 00:00:00

  • The design of potential antidiabetic drugs: experimental investigation of a number of beta-D-glucose analogue inhibitors of glycogen phosphorylase.

    abstract::alpha-D-glucose is a weak inhibitor (Ki = 1.7 mM) of glycogen phosphorylase (GP) and acts as physiological regulator of hepatic glycogen metabolism; it binds to GP at the catalytic site and stabilizes the inactive T state of the enzyme promoting the action of protein phosphatase 1 and stimulating glycogen synthase. Th...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/BF03188920

    authors: Oikonomakos NG,Kontou M,Zographos SE,Tsitoura HS,Johnson LN,Watson KA,Mitchell EP,Fleet GW,Son JC,Bichard CJ

    更新日期:1994-07-01 00:00:00

  • Differences in Intestinal Metabolism of Ginseng Between Normal and Immunosuppressed Rats.

    abstract:BACKGROUND AND OBJECTIVE:Ginseng is usually consumed as a dietary supplement for health care in the normal state or prescribed as a herbal medicine in pathologic conditions. Although metabolic studies of ginseng are commonly performed on healthy organisms, the metabolic characteristics in pathologic organisms remain un...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/s13318-020-00645-1

    authors: Zhu JH,Xu JD,Zhou SS,Zhang XY,Zhou J,Kong M,Mao Q,Zhu H,Li SL

    更新日期:2021-01-01 00:00:00

  • Phenobarbital-digitoxin interaction in the guinea pig liver.

    abstract::The influence of phenobarbital pretreatment on liver concentration of digitoxin and its metabolites was studied in guinea-pigs after i.p. administration of the cardiac glycoside. During the first hour an increase in liver uptake was observed in pretreated animals. The differences detected in the hepatic subcellular di...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/BF03189562

    authors: Carvalhas ML,Figueira MA,Maya MR

    更新日期:1982-01-01 00:00:00

  • First pass effect of pinazepam in the rabbit liver.

    abstract::The liver first pass effect of pinazepam in four anaesthetized rabbits was determined by measuring the concentrations of this compound and those of its metabolite N-desmethyldiazepam in the plasma from the portal and hepatic veins. Anaesthesia was induced with an i.p. injection of urethane (1.5 g/kg). Portal and hepat...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/BF03188728

    authors: Pacifici GM,Placidi GF

    更新日期:1982-01-01 00:00:00

  • Metabolism of (-)-(S)-nicotine in the isolated perfused rabbit lung.

    abstract::The metabolism of (-)-(S)-nicotine has been investigated following intratracheal administration to the recirculating perfused rabbit lung model. The metabolic products present in the perfusate were identified by co-chromatography (HPLC and GC) with authentic standards and quantified by HPLC. After the 180 min perfusio...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/BF03190976

    authors: Aislaitner G,Bello A,Tan SC,Hutt AJ,Marriott C,Gorrod JW

    更新日期:1997-10-01 00:00:00

  • Acceleration of in vitro dissolution studies of sustained release dosage form of theophylline and in vitro-in vivo evaluations in terms of correlations.

    abstract::The aim of the study was to accelerate the dissolution of the sustained release dosage forms using both elevated temperature and high rpm rates. Teokap(®) SR 200 mg pellets were tested by in vitro sustained and accelerated dissolution studies using USP XXIII rotating paddle method. Sustained dissolution studies were c...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/s13318-011-0049-6

    authors: Ertan G,Karasulu E,Ozgüney I,Karasulu Y,Apaydın S,Kantarcı G,Yurdasiper A,Ege MA

    更新日期:2011-12-01 00:00:00

  • Liver Perfusion Modifies Gd-DTPA and Gd-BOPTA Hepatocyte Concentrations Through Transfer Clearances Across Sinusoidal Membranes.

    abstract:BACKGROUND AND OBJECTIVES:Gadobenate dimeglumine (Gd-BOPTA) is a commercialised hepatobiliary contrast agent used during liver magnetic resonance imaging (MRI) to detect liver diseases. It enters into human hepatocytes through organic anion transporting polypeptides (OATP1B1/B3) and crosses the canalicular transporter ...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/s13318-016-0382-x

    authors: Daire JL,Leporq B,Vilgrain V,Van Beers BE,Schmidt S,Pastor CM

    更新日期:2017-08-01 00:00:00

  • Pharmacokinetics of nefazodone in the dog following single oral administration.

    abstract::The pharmacokinetics of nefazodone (NEF) and two of its pharmacologically active metabolites viz hydroxynefazodone (HO-NEF) and m-chlorophenylpiperazine (mCPP) were determined following single oral administration of 100, 200 and 400 mg NEF to 6 beagle dogs in a three-way crossover study. Blood samples were collected f...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/BF03190163

    authors: Shukla UA,Marathe PH,Labudde JA,Pittman KA,Barbhaiya RH

    更新日期:1992-10-01 00:00:00

  • In vivo metabolism of 4-fluorobenzoic acid [(5-nitro-2-furanyl)methylene] hydrazide in rats.

    abstract::It is known that substituted hydrazide hydrazone derivatives have several biological and pharmacological activities; there is limited literature on the metabolism of hydrazide hydrazones in rats. In our previous study, 4-fluorobenzoic acid [(5-nitro-2-furanyl)methylene]hydrazide (S) was found active against Staphyloco...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/BF03190075

    authors: Gülerman NN,Oruç EE,Kartal F,Rollas S

    更新日期:2000-04-01 00:00:00

  • The effect of molecular weight on the biodistribution of hyaluronic acid radiolabeled with 111In after intravenous administration to rats.

    abstract::Hyaluronic acid (HA), is a high molecular weight (HMW) glucosaminoglycan with significant acitivity, and which influences a number of physiological and pathological processes such as tumorogenesis, arthritis, etc. The aim of this study was to determine the difference in the biodistributional pathways of 111In-labeled ...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/BF03191112

    authors: Svanovsky E,Velebny V,Laznickova A,Laznicek M

    更新日期:2008-07-01 00:00:00

  • Physiologically based modeling of lisofylline pharmacokinetics following intravenous administration in mice.

    abstract::Lisofylline (LSF), is the R-(-) enantiomer of the metabolite M1 of pentoxifylline, and is currently under development for the treatment of type 1 diabetes. The aim of the study was to develop a physiologically based pharmacokinetic (PBPK) model of LSF in mice and to perform simulations in order to predict LSF concentr...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/s13318-015-0260-y

    authors: Wyska E,Świerczek A,Pociecha K,Przejczowska-Pomierny K

    更新日期:2016-08-01 00:00:00

  • Pharmacokinetic and pharmacodynamic data and models in clinical trials.

    abstract::There is current emphasis for extended integration of pharmacokinetics (PK) and pharmacodynamics (PD) into all phases of new drug development, including large-scale clinical trials. In this paper, we focus on study design and data analysis issues for the investigation of pharmacokinetic/pharmacodynamic and blood level...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.1007/BF03220009

    authors: Steimer JL,Ebelin ME,Van Bree J

    更新日期:1993-01-01 00:00:00

  • Disposition of [3H]cloflumide, a new neuroleptic drug, in rats.

    abstract::The disposition of cloflumide (VUFB 15496), 2-chloro-7-fluoro-10 [4-(carbamoylethyl)piperazino]-10,11-dihydrodibenzo [b,f] thiepin methansulfonate, a new neuroleptic agent, following single oral and intravenous dose was studied in the rat using radiotracer techniques. [3H]Cloflumide was almost completely absorbed from...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/BF03189883

    authors: Lapka R,Franc Z,Smolík S

    更新日期:1987-04-01 00:00:00

  • One-compartmental biometric blood loss calculation after cesarean section.

    abstract::Blood loss during cesarean section was calculated based on post-operative decrement of hemoglobin (Hb) and hematocrit (Hct) level. The model used for pregnant women was previously validated for non-pregnant women who underwent gynecological surgery. 1,068 pregnant women who underwent cesarean section and 517 women who...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/s13318-011-0042-0

    authors: Milosevic N,Popovic J,Grujic Z,Rapaic M

    更新日期:2011-09-01 00:00:00

  • Clinical Pharmacokinetics of a Lipid-Based Formulation of Risperidone, VAL401: Analysis of a Single Dose in an Open-Label Trial of Late-Stage Cancer Patients.

    abstract:BACKGROUND AND OBJECTIVES:A clinical trial was conducted to measure and analyse the pharmacokinetic parameters of a lipid formulation of risperidone, VAL401. The VAL401 formulation is designed to repurpose risperidone from an antipsychotic to an adenocarcinoma treatment, with the lipid formulation altering the cellular...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/s13318-018-00538-4

    authors: Dilly SJ,Morris GS,Taylor PC,Parmentier F,Williams C,Afshar M

    更新日期:2019-08-01 00:00:00

  • Quinine distribution in mice with Plasmodium berghei malaria.

    abstract::The disposition of a single 80 mg/kg injection of quinine base was compared in control and Plasmodium berghei-infected mice. Pharmacokinetic parameters were determined on repeated whole blood samples from caudal vein (experiment 1) and quinine distribution was evaluated in tissues and blood fractions from mice sacrifi...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/BF03190862

    authors: Pussard E,Bernier A,Fouquet E,Bouree P

    更新日期:2003-01-01 00:00:00