Abstract：
:Platelets contribute significantly to arterial-occlusive thrombosis, one of the major causes of death and disease throughout the world. Consequently, inhibiting platelet function is a potentially important therapeutic goal. Among agents that inhibit platelet function, ticlopidine shows a wide spectrum of antiplatelet activity. There have been a limited number of studies investigating the pharmacokinetic profile of the drug. However, it has been demonstrated that absorption of ticlopidine after oral administration is rapid, is improved when the drug is administered with food, but reduced by the coadministration of antacid. Ticlopidine is extensively metabolised, with little unchanged drug present in the plasma. After administration of a single dose, unchanged ticlopidine can be detected for up to 96 hours postdose. Repeated administration of ticlopidine 250mg twice daily results in 3- to 4-fold accumulation of the drug after 2 weeks. The terminal elimination half-life is between 20 and 50 hours. Dosage selection is not determined by the pharmacokinetic profile of the drug, but rather by determination of the effect of the drug on bleeding time. The clearance of theophylline and phenazone (antipyrine) are reduced by ticlopidine, resulting in increased plasma drug concentrations. In contrast, the plasma concentration of cyclosporin is reduced. Aspirin (acetylsalicylic acid) increases the bleeding time in patients receiving ticlopidine concurrently, while corticosteroids reduce bleeding time. Ticlopidine use is discouraged in patients with severe organ failure. Furthermore, ticlopidine should be discontinued 2 weeks before surgery and dental intervention. Most importantly, the blood cell count should be monitored regularly during the 3 first months of treatment with ticlopidine because 1% of patients receiving ticlopidine may experience agranulocytosis.
journal_name
Clin Pharmacokinetjournal_title
Clinical pharmacokineticsauthors
Desager JPdoi
10.2165/00003088-199426050-00003subject
Has Abstractpub_date
1994-05-01 00:00:00pages
347-55issue
5eissn
0312-5963issn
1179-1926journal_volume
26pub_type
杂志文章,评审abstract：:All of the commonly used anticonvulsants drugs, except possibly primidone, are cleared from the human body mainly by metabolism. The metabolites of phenytoin, phenobarbital and ethosuximide have so far not been shown to possess significant pharmacological activity. However, carbamazepine-10,11-epoxide, derived from ca...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/00003088-199121010-00003
更新日期：1991-07-01 00:00:00
abstract：:Few of the articles published on antibiotics and pregnancy are concerned with pharmacokinetics. It is particularly difficult to evaluate possible alterations in pharmacokinetic parameters that may be due to pregnancy. Most data available have been obtained in connection with abortion or delivery. Such data may not be ...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/00003088-197904040-00003
更新日期：1979-07-01 00:00:00
abstract：BACKGROUND AND OBJECTIVE:Losmapimod is an orally available, potent p38 mitogen-activated protein kinase inhibitor. It is in development as an anti-inflammatory drug in different therapeutic areas. Clinical studies have shown that losmapimod is well tolerated and safe in humans and several studies have shown its pharmac...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,随机对照试验
doi：10.1007/s40262-012-0025-6
更新日期：2013-03-01 00:00:00
abstract：BACKGROUND:Ovarian cancer is the leading cause of gynaecological cancer-related death in Western countries. Intraperitoneal (IP) peroperative chemotherapy is an interesting therapeutic option. However, very few data are available regarding pharmacokinetics and especially population pharmacokinetics. PATIENTS AND METHO...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章
doi：10.2165/00003088-200948030-00003
更新日期：2009-01-01 00:00:00
abstract：:The results of research studies conducted to date in vitro and in healthy volunteers are practically all concordant in demonstrating the lack of any kind of interference between famotidine and microsomal oxidative metabolism. The pharmacokinetics (elimination half-life, area under the plasma concentration-time curve, ...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章
doi：10.2165/00003088-199324030-00006
更新日期：1993-03-01 00:00:00
abstract：:The isoenzymes which catalyse the polymorphic hydroxylations of debrisoquine/sparteine and S-mephenytoin are cytochromes P450 2D6 and P450 2C19 (CYP2D6 and CYP2C19), respectively. CYP2D6 is involved in the stereospecific metabolism of several important groups of drugs, for example antiarrhythmics, antidepressants and ...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/00003088-199529030-00005
更新日期：1995-09-01 00:00:00
abstract：:Calcineurin inhibitors, the primary immunosuppressive therapy used to prevent alloreactivity of transplanted organs, have a narrow therapeutic index. Currently, treatment is individualized based on clinical assessment of the risk of rejection or toxicity guided by trough concentration monitoring. Advances in immune mo...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.1007/s40262-020-00923-w
更新日期：2020-11-01 00:00:00
abstract：:Metformin is widely used for the treatment of type 2 diabetes mellitus. It is a biguanide developed from galegine, a guanidine derivative found in Galega officinalis (French lilac). Chemically, it is a hydrophilic base which exists at physiological pH as the cationic species (>99.9%). Consequently, its passive diffusi...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/11534750-000000000-00000
更新日期：2011-02-01 00:00:00
abstract：:In the last 15 years the role of opioids in anaesthesia management has undergone dramatic change. Initially used as premedicants, or adjuvants to inhalation anaesthetic agents or as analgesics for postoperative pain relief, narcotics have now evolved into primary anaesthetic agents, primarily because of their ability ...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/00003088-198611010-00002
更新日期：1986-01-01 00:00:00
abstract：:The overall reporting rate of drug-drug interactions with fluvoxamine is very low: only 73 cases have been identified from an estimated exposure of over 8 million patients worldwide. The reporting rate is similar in men and women, and most events relate to the use of fluvoxamine in conjunction with psychotropic compou...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/00003088-199500291-00006
更新日期：1995-01-01 00:00:00
abstract：:The effects of liver disease on pharmacokinetics and pharmacodynamics are highly variable, and difficult to predict as the mechanisms of these effects are not well understood. Since the majority of the published literature is concerned with cirrhotic liver disease, this review also focuses mainly on this area. Four di...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/00003088-199529050-00005
更新日期：1995-11-01 00:00:00
abstract：:Although activity of cytochrome P450 isoenzymes (CYPs) plays a major role in the fate of anticancer agents in patients, there are relatively few clinical studies that evaluate drug metabolism with therapeutic outcome. Nevertheless, many clinical reports in various non-oncology fields have shown the dramatic importance...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/00003088-200544040-00002
更新日期：2005-01-01 00:00:00
abstract：:Etodolac is a chiral nonsteroidal anti-inflammatory drug (NSAID) that is marked as the racemate. Currently, the drug is available in several countries for the treatment of arthritis and the alleviation of pain. Etodolac possesses several unique disposition features mainly due to its stereoselective pharmacokinetics. I...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/00003088-199426040-00003
更新日期：1994-04-01 00:00:00
abstract：:Although individualised antihypertensive therapy is widely recommended, prospective methods for optimising treatment are hampered by the paucity of basic information about dose-plasma concentration-response relationships for commonly used drugs. Concentration-effect analysis has been applied to a number of therapeutic...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/00003088-199426060-00005
更新日期：1994-06-01 00:00:00
abstract：BACKGROUND AND OBJECTIVES:Therapeutic hypothermia can influence the pharmacokinetics and pharmacodynamics of drugs, the discipline which is called thermopharmacology. We studied the effect of therapeutic hypothermia on the pharmacokinetics of phenobarbital in asphyxiated neonates, and the clinical efficacy and the effe...
journal_title：Clinical pharmacokinetics
pub_type： 临床试验,杂志文章
doi：10.1007/s40262-012-0004-y
更新日期：2012-10-01 00:00:00
abstract：:Due to concern and debate in the epilepsy medical community and to the current interest of the US Food and Drug Administration (FDA) in revising approaches to the approval of generic drugs, the FDA is currently supporting ongoing bioequivalence studies of antiepileptic drugs, the EQUIGEN studies. During the design of ...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s40262-013-0103-4
更新日期：2013-12-01 00:00:00
abstract：BACKGROUND AND OBJECTIVE:Preterm and term newborn infants show wide interindividual variability (IIV) in pharmacokinetic parameters of gentamicin. More extensive knowledge and use of predictive covariates could lead to faster attainment of therapeutic concentrations and a reduced need for concentration monitoring. This...
journal_title：Clinical pharmacokinetics
pub_type： 临床试验,杂志文章
doi：10.2165/00003088-200948040-00003
更新日期：2009-01-01 00:00:00
abstract：:For the past 300 years antimalarial dosage regimens have not been based on pharmacokinetic information. However, now that this information is available, it is appropriate to examine current recommendations for prophylaxis and treatment. In healthy subjects, the cinchona alkaloids (quinine and quinidine), primaquine an...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/00003088-198510030-00001
更新日期：1985-05-01 00:00:00
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
更新日期：2000-07-01 00:00:00
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
更新日期：2010-09-01 00:00:00
abstract：:Carbamazepine is one of the most commonly prescribed antiepileptic drugs and is also used in the treatment of trigeminal neuralgia and psychiatric disorders, particularly bipolar depression. Because of its widespread and long term use, carbamazepine is frequently prescribed in combination with other drugs, leading to ...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/00003088-199631030-00004
更新日期：1996-09-01 00:00:00
abstract：INTRODUCTION:Renal impairment may have a significant impact on the pharmacokinetics of drugs. Ad hoc studies in subjects with renal impairment are required by the regulatory authorities to propose dose adjustments in these subjects, to find a dosing regimen able to provide a systemic exposure similar to those in subjec...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s40262-017-0574-9
更新日期：2018-04-01 00:00:00
abstract：BACKGROUND AND OBJECTIVES:Imeglimin (IMEG) is the first in a novel class of oral glucose-lowering agents with a unique mechanism of action targeting mitochondrial bioenergetics. We assessed whether repeated co-administration of IMEG and either metformin (MET) or sitagliptin (SITA) would influence the pharmacokinetics o...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s40262-020-00886-y
更新日期：2020-10-01 00:00:00
abstract：:Sulphonylureas have remained the mainstay of oral therapy for type 2 (non-insulin-dependent) diabetes mellitus (NIDDM). They stimulate insulin release from pancreatic beta cells. Pharmacokinetic differences between the various sulphonylureas are of clinical importance in terms of the time to onset of action, timing of...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/00003088-199834030-00001
更新日期：1998-03-01 00:00:00
abstract：OBJECTIVE:To assess any pharmacokinetic interactions between loperamide and saquinavir. DESIGN:Double-blind, double-dummy, randomised, placebo-controlled, three-way crossover trial. PARTICIPANTS:Twelve healthy male and female volunteers, aged 24-46 years. METHODS:Saquinavir and loperamide pharmacokinetics were deter...
journal_title：Clinical pharmacokinetics
pub_type： 临床试验,杂志文章,随机对照试验
doi：10.2165/00003088-200443140-00004
更新日期：2004-01-01 00:00:00
abstract：BACKGROUND:Fat-free mass (FFM)-based dose scaling is increasingly being adopted in clinical pharmacology. Given the complexities with the measurement of FFM in clinical practice, choosing an appropriate equation for FFM is critical for accurate dose scaling. Janmahasatian's FFM model (FFMJan) has largely remained the p...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s40262-020-00883-1
更新日期：2020-09-01 00:00:00
abstract：BACKGROUND AND OBJECTIVE:Vicriviroc is a small-molecule CCR5 antagonist currently in development for the treatment of HIV in patients on a regimen containing a ritonavir-boosted protease inhibitor. As renal disease and renal dysfunction are prevalent in the HIV-infected population, patients with varying degrees of rena...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,随机对照试验
doi：10.2165/11319470-000000000-00000
更新日期：2010-06-01 00:00:00
abstract：:The effects of anaesthesia and surgery on the pharmacokinetics of ketobemidone were studied in 12 patients. Plasma ketobemidone concentrations were assayed with a mass-fragmentographic method. The peroperative Vd(area) was 5.9 +/- 2.6L/kg and the terminal half-life was 3.9 +/- 1.7 h. In the postoperative period Vd(are...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章
doi：10.2165/00003088-198207030-00005
更新日期：1982-05-01 00:00:00
abstract：BACKGROUND AND OBJECTIVE:Daclatasvir is a potent, pangenotypic once-daily hepatitis C virus (HCV) NS5A inhibitor that is approved for the treatment of chronic HCV infection. The objective of this analysis was to characterize the pharmacokinetics of daclatasvir in subjects with chronic HCV infection. METHODS:A populati...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s40262-016-0504-2
更新日期：2017-10-01 00:00:00
abstract：:Many antiarrhythmic drugs introduced into the market during the past three decades have a chiral centre in their structure and are marketed as racemates. Most of these agents, including disopyramide, encainide, flecainide, mexiletine, propafenone and tocainide, belong to class I antiarrhythmics, whereas verapamil is a...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/00003088-200241080-00001
更新日期：2002-01-01 00:00:00
