Pharmacodynamics of ticlopidine in man in relation to plasma and blood cell concentration.

Abstract:

:In 6 normal volunteers given single oral doses of 250,500 and 1000 mg ticlopidine (T), the peak plasma level of unchanged drug was reached after about 2 h. There was no correlation between the plasma T level and its inhibitory effect on platelet function, expressed as % inhibition of ADP-induced aggregation. By means of HPLC and GC/MS significant concentrations of T were demonstrated in washed red cells, platelets and neutrophils, with a marked difference in the time course of the appearance of cell-associated drug. The time course of platelet-associated T very accurately fitted that of the antiaggregatory activity. After subacute oral administration (250 mg b.d. for 7 days), the maximum effect on platelet function was observed after 3 to 4 days, when a significant concentration of platelet-associated T had been reached. The pharmacological effect persisted as long as drug was detectable in platelet. An in vitro study strongly suggested that the antiaggregating effect was retained by treated washed platelets but not by treated plasma. It is suggested that the platelet compartment represents the pharmacological target of T via a specific uptake system.

journal_name

Eur J Clin Pharmacol

authors

DiPerri T,Pasini FL,Frigerio C,Blardi P,Centini F,Messa GL,Ghezzi A,Volpi L

doi

10.1007/BF00626364

subject

Has Abstract

pub_date

1991-01-01 00:00:00

pages

429-34

issue

5

eissn

0031-6970

issn

1432-1041

journal_volume

41

pub_type

杂志文章
  • Variability of coumarin 7- and 3-hydroxylation in a Jordanian population is suggestive of a functional polymorphism in cytochrome P450 CYP2A6.

    abstract:OBJECTIVE:To determine the variability of coumarin 7- and 3-hydroxylation in a human population and to evaluate the evidence for the existence of genetic polymorphism in these pathways. 7-Hydroxylation of coumarin is considered to be a detoxication pathway, whilst 3-hydroxylation, which predominates in rats, leads to h...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/s002280050489

    authors: Hadidi H,Irshaid Y,Vågbø CB,Brunsvik A,Cholerton S,Zahlsen K,Idle JR

    更新日期:1998-07-01 00:00:00

  • Studies of the agonist and antagonist activity of cicloprolol in man.

    abstract::To assess the partial agonist activity of cicloprolol in man, four studies were carried out in normal male volunteers. I and II. Open dose escalating studies of the effects of oral doses of the drug on exercise tachycardia and sleeping heart rate. III and IV. Double-blind randomized studies of the effects of placebo, ...

    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/BF00615219

    authors: McCaffrey PM,Burke M,Riddell JG,Shanks RG

    更新日期:1988-01-01 00:00:00

  • Systolic time intervals in evaluation of the negative inotropic effect after single oral doses of mexiletine and disopyramide.

    abstract::A placebo-controlled, single blind, crossover study was done to evaluate the inotropic effects of single oral doses of mexiletine and disopyramide assessed by the measurement of Systolic Time Intervals (STI). Each of 8 healthy volunteers received five treatments in random order: 200 and 400 mg mexiletine, 100 and 200 ...

    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/BF00541525

    authors: Rousson D,Piolat C,Galleyrand J,Ferry S,Boissel JP

    更新日期:1986-01-01 00:00:00

  • Quality and impact of problem-oriented drug information: a method to change clinical practice among physicians?

    abstract:OBJECTIVES:Problem-oriented drug information is characterised by health professionals actively seeking drug information through various sources. In this study our objective was to determine the quality and impact of problem-oriented drug information among physicians. METHODS:Evaluation forms accompanying 163 written a...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/s00228-001-0386-5

    authors: Schjøtt J,Pomp E,Gedde-Dahl A

    更新日期:2002-02-01 00:00:00

  • Effect of atrial natriuretic factor on platelet function in whole blood ex-vivo in man.

    abstract::Atrial natriuretic factor (ANF) binding sites have been shown to be present on human platelet membranes. We investigated the effect of an infusion of ANF 5 pmol.kg-1.min-1 on platelet aggregation in whole blood ex-vivo in 8 normal volunteers. Spontaneous platelet aggregation, collagen (0.6-2 micrograms.m.-1)-induced o...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00316102

    authors: Lang CC,Lau CS,Belch JJ,Struthers AD

    更新日期:1990-01-01 00:00:00

  • Medication and medical diagnosis as risk factors for falls in older hospitalized patients.

    abstract:OBJECTIVE:To examine the impact of medication and medical conditions on the fall risk in older hospitalized patients. DESIGN:Matched case-control study. SETTING:Large regional hospital in a mid-sized German city. SUBJECTS:Four hundred eighty-one inpatients aged ≥ 65 years who fell during hospitalization ("cases") an...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/s00228-019-02668-3

    authors: Wedmann F,Himmel W,Nau R

    更新日期:2019-08-01 00:00:00

  • Effect of rifampicin on the pharmacokinetics of itraconazole in normal volunteers and AIDS patients.

    abstract:OBJECTIVE:To investigate the effects of rifampicin on the pharmacokinetics of itraconazole in humans. METHODS:Our study was conducted with six healthy normal volunteers and three AIDS patients. All subjects received a 200 mg single dose of oral itraconazole on day 1 and day 15 and 600 mg of oral rifampicin once daily ...

    journal_title:European journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1007/s002280050437

    authors: Jaruratanasirikul S,Sriwiriyajan S

    更新日期:1998-04-01 00:00:00

  • Antagonism by domperidone of the ocular hypotensive effect of pergolide.

    abstract::1. The effect of pre-dosing with 15 mg domperidone, a relatively selective dopamine 2-receptor antagonist, on the ocular hypotensive action of a single oral dose of 25 micrograms pergolide, a dopamine 2-receptor agonist, was studied in 9 normal human volunteers, using a non-invasive method. 2. Compared with domperidon...

    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/BF02336684

    authors: al-Sereiti MR,Quik RF,Hedges A,Turner P

    更新日期:1990-01-01 00:00:00

  • Stimulation of renin secretion by potassium-channel activation with cromakalim.

    abstract::The cardiovascular and endocrine profile of cromakalim has been studied in 8 healthy men (age 25 +/- 2 years: means SEM) and its influence on renin release from cultured rat juxtaglomerular cells in vitro has also been examined. According to a double-blind, randomized sequence the subjects received placebo or cromakal...

    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/BF00558067

    authors: Ferrier CP,Kurtz A,Lehner P,Shaw SG,Pusterla C,Saxenhofer H,Weidmann P

    更新日期:1989-01-01 00:00:00

  • Relationship between renal function and disposition of oral cefixime.

    abstract::The pharmacokinetics of cefixime following a single oral dose of 200 mg have been investigated in 6 normal subjects and in 22 patients with various degrees of renal insufficiency. Serum and urine samples were collected between 0 and 72 h and were subjected to two methods of analysis: bioassay and HPLC. There was a lin...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00314988

    authors: Dhib M,Moulin B,Leroy A,Hameau B,Godin M,Johannides R,Fillastre JP

    更新日期:1991-01-01 00:00:00

  • Statistical interpretation of the antisecretory effect of famotidine measured by intragastric pH-metry.

    abstract:OBJECTIVE:Intragastric pH-metry is widely used to evaluate the efficacy of antisecretory drugs, but statistical interpretation of the measurements has not yet been standardised. METHODS:The effects of single morning (N = 9) or evening (N = 7) doses of the H2-receptor antagonist famotidine, 20 mg (QUAMATELR. Gedeon Ric...

    journal_title:European journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1007/s002280050139

    authors: Hunyady B,Juricskay I,Nagy L,Garamszegi M,Vincze A,Mózsik G

    更新日期:1996-01-01 00:00:00

  • High prevalence of cytochrome P450 2A6*1A alleles in a black African population of Ghana.

    abstract:OBJECTIVE:We investigated the frequencies of the functionally important variants of the CYP2A6 gene in black African populations. METHODS:Using genomic DNA sequencing, polymerase chain reaction (PCR)-restriction fragment length polymorphism and allele-specific PCR, the allele frequencies of CYP2A6 *1A, *1B, *2, *4A, *...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/s00228-004-0854-9

    authors: Gyamfi MA,Fujieda M,Kiyotani K,Yamazaki H,Kamataki T

    更新日期:2005-02-01 00:00:00

  • Drug-associated non-pyrogenic hyperthermia: a narrative review.

    abstract:PURPOSE:Hyperthermia occurs when heat accumulation surpasses the body's ability for heat dissipation. Many drugs may affect thermoregulation. This narrative review aimed to provide an overview of the current literature concerning reports of drug-associated non-pyrogenic hyperthermia. METHODS:A comprehensive search was...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1007/s00228-019-02763-5

    authors: Bongers KS,Salahudeen MS,Peterson GM

    更新日期:2020-01-01 00:00:00

  • Influence of hyperlipidic food on the kinetics of slow-release formulations of theophylline.

    abstract::A cross-over study of kinetics has been undertaken in 12 healthy adults volunteers using two sustained-release theophylline products that allow once a day dosing (Theo-Dur tablets and Dilatrane A.P. bead filled capsules) to compare the i.v. pharmacokinetic profiles when taken with an hyperlipidic meal and a balanced s...

    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/BF00609431

    authors: Brazier JL,Benchekroun Y,Gillet A,Andre C

    更新日期:1989-01-01 00:00:00

  • Effects of the alpha-glucosidase inhibitor 1 desoxynojirimycin (Bay m 1099) on postprandial blood glucose, serum insulin and C-peptide levels in type II diabetic patients.

    abstract::Bay m 1099 is a newly developed inhibitor of intestinal alpha-glucosidase. Its ability to lower postprandial plasma glucose, serum insulin and C-peptide levels in Type II diabetics has been investigated. Fifteen obese Type II diabetic patients with inadequate metabolic control during sulphonylurea treatment received a...

    journal_title:European journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1007/BF00607953

    authors: Schnack C,Röggla G,Luger A,Schernthaner G

    更新日期:1986-01-01 00:00:00

  • Effect of ciprofloxacin on the pharmacokinetics of ropivacaine.

    abstract:OBJECTIVE:To assess the effect of ciprofloxacin on the pharmacokinetics of ropivacaine. METHODS. In a double-blind, randomised, cross-over study, nine healthy volunteers were treated for 2.5 days with 500 mg oral ciprofloxacin or placebo twice daily. On day 3, they received a single dose of 0.6 mg/kg ropivacaine intrav...

    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/s00228-002-0540-8

    authors: Jokinen MJ,Olkkola KT,Ahonen J,Neuvonen PJ

    更新日期:2003-02-01 00:00:00

  • Comparison of nicardipine and propranolol in the treatment of mild and moderate hypertension.

    abstract::In a double-blind controlled trial 22 patients with mild or moderate essential hypertension were treated with nicardipine 30 mg t.d.s. and 19 patients with propranolol 80 mg t.d.s. as monotherapy for 24 weeks. Blood pressure in both groups at the end of trial was equally and significantly reduced; systolic pressure 22...

    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/BF00544554

    authors: Naukkarinen VA,Karppinen K,Sarna S

    更新日期:1987-01-01 00:00:00

  • Comparative bioavailability of diclofenac hydroxyethylpyrrolidine vs diclofenac sodium in man.

    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

    authors: Maggi CA,Lualdi P,Mautone G

    更新日期:1990-01-01 00:00:00

  • Pharmacokinetics of TZU-0460, a new H2-receptor antagonist, in patients with impaired renal function.

    abstract::We have studied pharmacokinetics of a new H2-receptor antagonist, TZU-0460, in patients with varying degrees of renal impairment. The apparent volume of distribution at steady-state was 1.70 l/kg, and the plasma protein binding of TZU-0460 or its active metabolite, desacetyl TZU-0460 was less than 10% in normal subjec...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00608220

    authors: Takabatake T,Ohta H,Yamamoto Y,Ishida Y,Hara H,Nakamura S,Ushiogi Y,Satoh S,Hattori N

    更新日期:1986-01-01 00:00:00

  • Impact of CYP3A5 polymorphism on trough concentrations and outcomes of tacrolimus minimization during the early period after kidney transplantation.

    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

    authors: Yaowakulpatana K,Vadcharavivad S,Ingsathit A,Areepium N,Kantachuvesiri S,Phakdeekitcharoen B,Sukasem C,Sra-Ium S,Sumethkul V,Kitiyakara C

    更新日期:2016-03-01 00:00:00

  • Pharmacokinetics of the placental transfer and distribution of clorazepate and its metabolite nordiazepam in the feto-placental unit and in the neonate.

    abstract::Clorazepate 20 mg was given i.m. to 49 mothers during the first stage of labour. The elimination of the drug was studied in 27 newborns produced by these mothers. The same dose was given to 13 women who underwent amniocentesis and to 7 women who were breast-feeding. "Total nordiazepam", i.e. the sum of clorazepate and...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00563103

    authors: Rey E,Giraux P,d'Athis P,Turquais JM,Chavinie J,Olive G

    更新日期:1979-04-17 00:00:00

  • Effect of lithium treatment on the GH-clonidine test in affective disorders.

    abstract::The effects of short-term lithium (Li) administration on alpha 2-adrenoceptor sensitivity was studied in 10 healthy volunteers and in 15 patients with normothymic, phasic depressive disorders. The GH-clonidine test was used to examine alpha 2-adrenoceptor sensitivity, administered before and after Li treatment (600 mg...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00637595

    authors: Brambilla F,Catalano M,Lucca A,Smeraldi E

    更新日期:1988-01-01 00:00:00

  • The geographic relationship between the use of antimicrobial drugs and the pattern of resistance for Streptococcus pneumoniae in Italy.

    abstract:OBJECTIVES:A temporal relationship between the increasing use of antibiotics and the increasing levels of antibiotic resistance has been established for Streptococcus pneumoniae. There are also data that support the presence of a geographic correlation between the level of resistance and the pattern of use among differ...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/s00228-003-0724-x

    authors: Boccia D,Alegiani SS,Pantosti A,Moro ML,Traversa G

    更新日期:2004-04-01 00:00:00

  • Pharmacokinetics of temocapril hydrochloride, a novel angiotensin converting enzyme inhibitor, in renal insufficiency.

    abstract::The pharmacokinetics of temocapril hydrochloride, a novel prodrug-type angiotensin-I converting enzyme (ACE) inhibitor, has been studied in patients with mild (Group II) to severe (Group III) renal insufficiency in comparison with subjects with normal renal function (Group I). The pharmacokinetic parameters of the act...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF02284968

    authors: Nakashima M,Yamamoto J,Shibata M,Uematsu T,Shinjo H,Akahori T,Shioya H,Sugiyama K,Kawahara Y

    更新日期:1992-01-01 00:00:00

  • Paracetamol disposition and metabolite kinetics in patients with chronic renal failure.

    abstract::The disposition of paracetamol following an oral dose of 1.0 g was compared in 10 healthy volunteers, 7 patients with moderate chronic renal failure and 6 patients with end stage renal failure on maintenance haemodialysis. Paracetamol absorption was normal in the patients with renal failure. The mean plasma half-life ...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00558162

    authors: Prescott LF,Speirs GC,Critchley JA,Temple RM,Winney RJ

    更新日期:1989-01-01 00:00:00

  • Cost evaluation of a new iv device in an Israeli hospital.

    abstract::A new device for IV admixtures has been developed in Israel, the Vialink minibag. It consists of a partly filled minibag, attached by rubber tubing to a sterile receptable into which various types of vials containing drugs can be firmly inserted. Time and motion studies were conducted to determine the time and cost as...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00194973

    authors: Lustig A

    更新日期:1994-01-01 00:00:00

  • Humoral and haemodynamic effects of idrapril calcium, the prototype of a new class of ACE-inhibitors, in essential hypertensive patients.

    abstract::Idrapril is the prototype of a new class of ACE inhibitors, characterised by the presence of a hydroxdmic group. Six untreated in-patients with essential hypertension were given single oral doses of the calcium salt of idrapril, idrapril calcium (200 mg) and placebo according to a double blind, randomised experimental...

    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/BF00194948

    authors: Taddei S,Ghiadoni L,Mattei P,Sudano I,Duranti P,Favilla S,Virdis A,Romagnoli A,Criscuoli M,Coppini A

    更新日期:1995-01-01 00:00:00

  • Paracetamol test: modification by renal function, urine flow and pH.

    abstract::Factors which might affect paracetamol disposition have been studied in a heterogenous group of patients in need of mild analgesia in an intensive care unit. Following oral administration of 1 g of paracetamol, plasma and urinary concentrations of the parent compound and metabolites were assessed by HPLC. The renal cl...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00315104

    authors: Kietzmann D,Bock KW,Krähmer B,Kettler D,Bircher J

    更新日期:1990-01-01 00:00:00

  • Evaluation of the safety of fexofenadine from experience gained in general practice use in England in 1997.

    abstract:BACKGROUND:Fexofenadine is the active metabolite of the non-sedating anti-histamine terfenadine. Pre-licensing clinical trials in over 6000 patients suggested it was effective and well tolerated. OBJECTIVE:To assess the tolerability and safety of fexofenadine immediately after its availability on the UK market in Marc...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/s002280100292

    authors: Craig-McFeely PM,Acharya NV,Shakir SA

    更新日期:2001-07-01 00:00:00

  • Effects of sumatriptan and eletriptan on diseased epicardial coronary arteries.

    abstract:BACKGROUND:Triptans are contraindicated in patients with known or suspected coronary artery disease (CAD); however, few studies have evaluated triptans in patients with obstructive CAD to quantify the vasoconstrictive effect on diseased coronary vessels. METHODS:Patients undergoing percutaneous transluminal coronary a...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章,随机对照试验

    doi:10.1007/s00228-005-0988-4

    authors: Newman CM,Starkey I,Buller N,Seabra-Gomes R,Kirby S,Hettiarachchi J,Cumberland D,Hillis WS

    更新日期:2005-11-01 00:00:00