Clinical pharmacokinetics of dorzolamide.

Abstract:

:Dorzolamide is a carbonic anhydrase inhibitor for topical ophthalmic application. It is used in the treatment of glaucoma to lower the intraocular pressure. After absorption via the cornea and stroma, it inhibits carbonic anhydrase in the ciliary process, which leads to a reduction of aqueous humour production and therefore to the desired therapeutic effect. In the systemic circulation, dorzolamide is bound mainly to carbonic anhydrase in red blood cells. It is slowly metabolised to N-de-ethyldorzolamide, which in turn is also stored in red blood cells. The very slow elimination (half-life >4 months) of both substances takes place via the renal route. However, the inhibition of carbonic anhydrase in red blood cells is moderate in the course of a topical treatment, avoiding systemic adverse effects. This review summarises the pharmacokinetic and pharmacodynamic properties of dorzolamide and its metabolite in eye tissues and in the systemic circulation.

journal_name

Clin Pharmacokinet

authors

Martens-Lobenhoffer J,Banditt P

doi

10.2165/00003088-200241030-00004

keywords:

subject

Has Abstract

pub_date

2002-01-01 00:00:00

pages

197-205

issue

3

eissn

0312-5963

issn

1179-1926

pii

410304

journal_volume

41

pub_type

杂志文章,评审
  • Clinical pharmacokinetics of nabumetone. The dawn of selective cyclo-oxygenase-2 inhibition?

    abstract::Nabumetone is a nonsteroidal anti-inflammatory drug (NSAID) of the 2,6-disubstituted naphthyl-alkanone class. Nabumetone is metabolised to an active metabolite 6-methoxy-2-napthylacetic acid (6-MNA) which is a relatively selective cyclo-oxygenase-2 inhibitor that has anti-inflammatory and analgesic properties. Nabumet...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.2165/00003088-199733060-00001

    authors: Davies NM

    更新日期:1997-12-01 00:00:00

  • Clinical pharmacokinetics of sevoflurane.

    abstract::Sevoflurane is a comparatively recent addition to the range of inhalational anaesthetics which has been recently released for clinical use. In comparison to older inhalational agents such as isoflurane or halothane, the most important property of sevoflurane is its low solubility in the blood. This results in a more r...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.2165/00003088-199936010-00002

    authors: Behne M,Wilke HJ,Harder S

    更新日期:1999-01-01 00:00:00

  • Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib.

    abstract::Nintedanib is an oral, small-molecule tyrosine kinase inhibitor approved for the treatment of idiopathic pulmonary fibrosis and patients with advanced non-small cell cancer of adenocarcinoma tumour histology. Nintedanib competitively binds to the kinase domains of vascular endothelial growth factor (VEGF), platelet-de...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.1007/s40262-019-00766-0

    authors: Wind S,Schmid U,Freiwald M,Marzin K,Lotz R,Ebner T,Stopfer P,Dallinger C

    更新日期:2019-09-01 00:00:00

  • An updated comparison of drug dosing methods. Part IV: Vancomycin.

    abstract::The resurgence of the use of and interest in vancomycin, in conjunction with the high degree of interpatient variability in its pharmacokinetic profile, has prompted the development of many and varied dosing methods. Several dosing nomograms have been proposed and evaluated, methods which are useful for initial dosing...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.2165/00003088-199120060-00003

    authors: Pryka RD,Rodvold KA,Erdman SM

    更新日期:1991-06-01 00:00:00

  • Pharmacology of anticancer drugs in the elderly population.

    abstract::Modifications to bodily functions and physiology are known to occur with age. These changes can have a considerable impact on the pharmacokinetic processes of absorption, distribution, metabolism and excretion and the pharmacodynamic properties of administered drugs. For many drugs with a high therapeutic index, this ...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.2165/00003088-200342140-00003

    authors: Wildiers H,Highley MS,de Bruijn EA,van Oosterom AT

    更新日期:2003-01-01 00:00:00

  • Clinical Pharmacokinetics and Pharmacodynamics of Evolocumab, a PCSK9 Inhibitor.

    abstract::Proprotein convertase subtilisin/kexin type 9 (PCSK9) increases plasma low-density lipoprotein cholesterol (LDL-C) by decreasing expression of the LDL receptor on hepatic cells. Evolocumab is a human monoclonal immunoglobulin G2 that binds specifically to human PCSK9 to reduce LDL-C. Evolocumab exhibits nonlinear kine...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.1007/s40262-017-0620-7

    authors: Kasichayanula S,Grover A,Emery MG,Gibbs MA,Somaratne R,Wasserman SM,Gibbs JP

    更新日期:2018-07-01 00:00:00

  • Pharmacokinetics of taurolidine following repeated intravenous infusions measured by HPLC-ESI-MS/MS of the derivatives taurultame and taurinamide in glioblastoma patients.

    abstract:BACKGROUND AND OBJECTIVE:Taurolidine is known to have antimicrobial activity. Furthermore, at lower concentrations, it has been found to exert a selective antineoplastic effect in vitro and in vivo. The aim of this study was to investigate the pharmacokinetics of taurolidine in vivo following repeated intravenous infus...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章

    doi:10.2165/00003088-200746060-00005

    authors: Stendel R,Scheurer L,Schlatterer K,Stalder U,Pfirrmann RW,Fiss I,Möhler H,Bigler L

    更新日期:2007-01-01 00:00:00

  • Drug absorption in gastrointestinal disease with particular reference to malabsorption syndromes.

    abstract::There is a considerable range in the dose of many drugs that is required to produce a given pharmacological effect in an individual patient. This individual variation in dose requirement is sometimes reflected in the wide scatter in the steady state plasma concentration that follows the same oral dose of a drug given ...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.2165/00003088-197702010-00004

    authors: Parsons RL

    更新日期:1977-01-01 00:00:00

  • Predicting Drug Extraction in the Human Gut Wall: Assessing Contributions from Drug Metabolizing Enzymes and Transporter Proteins using Preclinical Models.

    abstract::Intestinal metabolism can limit oral bioavailability of drugs and increase the risk of drug interactions. It is therefore important to be able to predict and quantify it in drug discovery and early development. In recent years, a plethora of models-in vivo, in situ and in vitro-have been discussed in the literature. T...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.1007/s40262-015-0351-6

    authors: Peters SA,Jones CR,Ungell AL,Hatley OJ

    更新日期:2016-06-01 00:00:00

  • Cellular and clinical pharmacology of fludarabine.

    abstract::In the past decade, fludarabine has had a major impact in increasing the effectiveness of treatment of patients with indolent B-cell malignancies. This has come about in a variety of clinical circumstances, including use of fludarabine alone as well as in combinations with DNA-damaging agents or membrane-targeted anti...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.2165/00003088-200241020-00002

    authors: Gandhi V,Plunkett W

    更新日期:2002-01-01 00:00:00

  • Drug interactions with cisapride: clinical implications.

    abstract::Cisapride, a prokinetic agent, has been used for the treatment of a number of gastrointestinal disorders, particularly gastro-oesophageal reflux disease in adults and children. Since 1993, 341 cases of ventricular arrhythmias, including 80 deaths, have been reported to the US Food and Drug Administration. Marketing of...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.2165/00003088-200039010-00004

    authors: Michalets EL,Williams CR

    更新日期:2000-07-01 00:00:00

  • Clinical pharmacokinetics of alpha 1-antitrypsin in homozygous PiZ deficient patients.

    abstract::A pharmacokinetic study of alpha 1-antitrypsin (ATT) was performed in 2 groups of homozygous PiZ-deficient patients (treated and untreated) and 1 group of healthy volunteers. The distribution of the 131I-labelled protein corresponds to a 3-compartment model. The intravenously administered protein diffused quickly to t...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章

    doi:10.2165/00003088-199223020-00007

    authors: Constans J,Carles P,Boneu A,Arnaud J,Tufenkji AE,Pujazon MC,Tavera C

    更新日期:1992-08-01 00:00:00

  • Therapeutic drug monitoring in oncology. Problems and potential in antineoplastic therapy.

    abstract::Therapeutic drug monitoring is now widely used in many areas of medicine. With its proliferation has come an understanding of the clinical situations in which it is likely to be of value. Factors that can limit the usefulness of therapeutic drug monitoring and situations where it is less likely to be of benefit have a...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.2165/00003088-198713040-00001

    authors: Moore MJ,Erlichman C

    更新日期:1987-10-01 00:00:00

  • Dosage adjustment from simple nortriptyline spot level predictor tests in depressed patients.

    abstract::20 routine patients with endogenous depression were investigated in a kinetic and 4 week treatment study. Steady-state plasma nortriptyline concentrations above 200 microgram/L were associated with a highly significant poorer therapeutic outcome. The correlations between the 24, 48 and 72 hour concentrations and stead...

    journal_title:Clinical pharmacokinetics

    pub_type: 临床试验,杂志文章

    doi:10.2165/00003088-197904020-00005

    authors: Montgomery SA,McAuley R,Montgomery DB,Braithwaite RA,Dawling S

    更新日期:1979-03-01 00:00:00

  • Clinical pharmacokinetics of pravastatin.

    abstract::The hypolipidaemic agent pravastatin differs from other US Food and Drug Administration (FDA)-approved HMG-CoA reductase inhibitors (e.g. lovastatin and simvastatin) because it has greater hydrophilicity, as a result of the hydroxyl group attached to its decalin ring. The hydrophilic nature of pravastatin accounts for...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.2165/00003088-199427020-00002

    authors: Quion JA,Jones PH

    更新日期:1994-08-01 00:00:00

  • Population pharmacokinetic analysis of tesamorelin in HIV-infected patients and healthy subjects.

    abstract:BACKGROUND AND OBJECTIVES:Tesamorelin is a synthetic analogue of growth hormone-releasing factor (GRF), which increases basal and pulsatile growth hormone (GH) secretion and subsequently increases insulin-like growth factor (IGF)-1. Limited information is available about the pharmacokinetics of this compound. Consequen...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,随机对照试验

    doi:10.1007/s40262-014-0202-x

    authors: González-Sales M,Barrière O,Tremblay PO,Nekka F,Mamputu JC,Boudreault S,Tanguay M

    更新日期:2015-03-01 00:00:00

  • Pharmacokinetic and pharmacodynamic properties of histamine H2-receptor antagonists. Relationship between intrinsic potency and effective plasma concentrations.

    abstract::Histamine H2-receptor antagonists are a unique class of compounds. Pharmacologically they are characterised as a family by their ability to inhibit the secretion of gastric acid, and kinetically they are classified as a family by their similarity in absorption, distribution and elimination. All the H2-receptor antagon...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.2165/00003088-199120030-00004

    authors: Lin JH

    更新日期:1991-03-01 00:00:00

  • Elucidating the Plasma and Liver Pharmacokinetics of Simeprevir in Special Populations Using Physiologically Based Pharmacokinetic Modelling.

    abstract::The disposition of simeprevir (SMV) in humans is characterised by cytochrome P450 3A4 metabolism and hepatic uptake by organic anion transporting polypeptide 1B1/3 (OATP1B1/3). This study was designed to investigate SMV plasma and liver exposure upon oral administration in subjects infected with hepatitis C virus (HCV...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/s40262-016-0476-2

    authors: Snoeys J,Beumont M,Monshouwer M,Ouwerkerk-Mahadevan S

    更新日期:2017-07-01 00:00:00

  • Reliability of antiarrhythmic drug plasma concentration monitoring.

    abstract::Measurement of drug levels is becoming increasingly popular to optimise the dosage of various drugs. In the case of antiarrhythmic drugs, the narrow therapeutic margin of most of these agents and a direct relationship between their pharmacological effects and plasma concentrations would justify more widespread use of ...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.2165/00003088-198308010-00004

    authors: Follath F,Ganzinger U,Schuetz E

    更新日期:1983-01-01 00:00:00

  • Pharmacokinetic considerations in the treatment of inflammatory bowel disease.

    abstract::This review describes the pharmacokinetics of the major drugs used for the treatment of inflammatory bowel disease. This information can be helpful for the selection of a particular agent and offers guidance for effective and well tolerated regimens. The corticosteroids have a short elimination half-life (t1/2beta) of...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.2165/00003088-200140100-00003

    authors: Schwab M,Klotz U

    更新日期:2001-01-01 00:00:00

  • Pharmacokinetic Studies in Neonates: The Utility of an Opportunistic Sampling Design.

    abstract:BACKGROUND AND OBJECTIVE:The use of an opportunistic (also called scavenged) sampling strategy in a prospective pharmacokinetic study combined with population pharmacokinetic modelling has been proposed as an alternative strategy to conventional methods for accomplishing pharmacokinetic studies in neonates. However, th...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/s40262-015-0291-1

    authors: Leroux S,Turner MA,Guellec CB,Hill H,van den Anker JN,Kearns GL,Jacqz-Aigrain E,Zhao W,TINN (Treat Infections in NeoNates) and GRiP (Global Research in Paediatrics) Consortiums.

    更新日期:2015-12-01 00:00:00

  • Evaluation of Tobramycin Exposure Predictions in Three Bayesian Forecasting Programmes Compared with Current Clinical Practice in Children and Adults with Cystic Fibrosis.

    abstract:BACKGROUND AND OBJECTIVES:Bayesian forecasting (BF) methods for tobramycin dose individualisation has not seen widespread clinical adoption, despite being endorsed by clinical practice guidelines. Several freeware and commercial programmes using BF methods are available to support personalised dosing. This study evalua...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/s40262-017-0610-9

    authors: Burgard M,Sandaradura I,van Hal SJ,Stacey S,Hennig S

    更新日期:2018-08-01 00:00:00

  • Warfarin withdrawal. Pharmacokinetic-pharmacodynamic considerations.

    abstract::Warfarin, like all the 4-hydroxycoumarin compounds, has an asymmetric carbon atom. The clinically available warfarin preparations consist of a racemic mixture of equal amounts of 2 distinct S and R isomers, the former being 4-times more potent as anticoagulant and more susceptible to drug interaction. Warfarin is high...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.2165/00003088-199630040-00003

    authors: Palareti G,Legnani C

    更新日期:1996-04-01 00:00:00

  • Population pharmacokinetics and pharmacodynamics for treatment optimization in clinical oncology.

    abstract::Population pharmacokinetic and pharmacodynamic analysis is an important tool to support optimal treatment in clinical oncology. The population approach is suitable to explain variability between patients and to establish relationships between drug exposure and a relevant pharmacodynamic parameter. This can facilitate ...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.2165/00003088-200847080-00001

    authors: Zandvliet AS,Schellens JH,Beijnen JH,Huitema AD

    更新日期:2008-01-01 00:00:00

  • Antiretroviral therapy : pharmacokinetic considerations in patients with renal or hepatic impairment.

    abstract::Hepatic and renal insufficiency due to co-infection, alcoholism, diabetes mellitus, family history, adverse effects of antiretrovirals and other factors are commonly seen in HIV-infected patients. Therefore, the use of antiretrovirals in this patient setting requires attention to the pharmacokinetic issues that clinic...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.2165/00003088-200847030-00002

    authors: McCabe SM,Ma Q,Slish JC,Catanzaro LM,Sheth N,DiCenzo R,Morse GD

    更新日期:2008-01-01 00:00:00

  • Higher Febuxostat Exposure Observed in Asian Compared with Caucasian Subjects Independent of Bodyweight.

    abstract:BACKGROUND AND OBJECTIVE:Febuxostat is a xanthine oxidase inhibitor indicated for gout and hyperuricemia. This work investigates potential clinically relevant covariates for febuxostat pharmacokinetics with a special focus on Asian race and bodyweight. METHODS:Febuxostat plasma concentrations from 141 male subjects we...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/s40262-020-00943-6

    authors: Rekić D,Johansson S,Leander J

    更新日期:2020-09-19 00:00:00

  • Pharmacokinetics in the elderly.

    abstract::The elderly are generally considered to be different from young people in terms of drug response and this applies particularly to quantitative differences. While altered drug handling is a major potential source of difference in responsiveness to drugs, the relative contribution of pharmacokinetics and pharmacodynamic...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.2165/00003088-197601040-00003

    authors: Crooks J,O'Malley K,Stevenson IH

    更新日期:1976-01-01 00:00:00

  • Therapeutic drug monitoring of clozapine treatment. Therapeutic threshold value for serum clozapine concentrations.

    abstract::It has been suggested that the minimum effective serum clozapine concentration for an acceptable clinical response (threshold value) is about 400 micrograms/L. This article argues against the use of therapeutic drug monitoring (TDM) as a tool to obtain clozapine concentrations of > or = 400 micrograms/L in the individ...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.2165/00003088-199834060-00005

    authors: Olesen OV

    更新日期:1998-06-01 00:00:00

  • Relevance of absorption rate and lag time to the onset of action in migraine.

    abstract:OBJECTIVE:The objective of this analysis was to simulate the performance of oral triptan formulations with varying absorption characteristics and their impact on the onset and magnitude of the antimigraine effect using a Markov model for migraine attacks. ANALYSIS:Sumatriptan pharmacokinetic data were obtained from cl...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章

    doi:10.2165/00003088-200847020-00007

    authors: Maas HJ,Spruit MA,Danhof M,Della Pasqua OE

    更新日期:2008-01-01 00:00:00

  • Routine plasma anti-Xa monitoring is required for low-molecular-weight heparins.

    abstract::Low-molecular-weight heparins are anticoagulants used in the treatment of thrombosis. They have effectiveness and safety profiles similar to those of unfractionated heparin but are considered an attractive alternative because of their predictable pharmacokinetic characteristics. In this article, we demonstrate the nee...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章

    doi:10.2165/11532960-000000000-00000

    authors: Al-Sallami HS,Barras MA,Green B,Duffull SB

    更新日期:2010-09-01 00:00:00