Oral medium-dosed metoclopramide versus placebo as highly effective antiemetic prophylaxis in in- and outpatients on noncisplatin chemotherapy.

The antiemetic effect of oral medium-dosed metoclopramide (MCL, 3.5 mg/kg b.w.

Minimal biliary excretion and enterohepatic recirculation of metoclopramide in patients with extrahepatic cholestasis.

The biliary excretion and apparent oral clearance of metoclopramide (MCL) were determined after oral administration of 1 mg MCL/kg body weight to 10 patients suffering from extrahepatic cholestasis with nasobiliary tube for drainage of the common bile duct. A bilioduodenal endoprosthesis was subsequently fitted in 6 of these patients, i.e.

Pharmacokinetics and relative bioavailability of prajmalium bitartrate after single oral dosing.

Pharmacokinetics and relative bioavailability of the marketed prajmalium bitartrate tablet (Neo-Gilurytmal, CAS 2589-47-1) compared to an oral solution were investigated in an open, randomized, single-dose two-fold crossover study in 20 healthy male volunteers. One subject was identified to be a poor metabolizer. In the study population with normal metabolic status the two oral formulations proved to be bioequivalent with regard to the pharmacokinetic parameters Cmax, AUC(0-Tlast), AUC(0-infinity) and Ae(24h).

Transfer of metaclazepam and its metabolites into breast milk.

Ten young women took part in this study a few days after delivery (day 3 and day 5 post partum). Lactation had developed normally but the newborn infants were not breast-fed. The study was intended to investigate whether metaclazepam (Talis), a new 1,4-benzodiazepine, and some of its metabolites were present in breast milk.

Pharmacokinetics and metabolism of 14C isobytylnaphtyl acetic acid in rat.

After oral administration to rats, absorption of INAA was slow but complete. Plasma level curves reached a plateau for INAA as well as for the two metabolites, which were rapidly formed (MI and MII). The plateau concentration led to an increase of the apparent elimination half-life, which was short after i.

Absolute bioavailability of metoclopramide given orally or by enema in patients with normal liver function or with cirrhosis of the liver.

Single dose studies were performed with three different dosage forms of metoclopramide (0.25 mg/kg body weight) in patients with normal liver function (i.v.

Pharmacokinetics of n-propyl-ajmaline-bitartrate in elderly patients with ventricular ectopic activity.

11 patients (9m, 2f, median age 59 years) with ventricular ectopic activity of at least Lown grade III received 20 mg N-Propyl-ajmaline-bitartrate (N-PAB) p.o. Plasma concentrations of N-PAB were determined with HPLC from blood samples within 26 hours after administration.

Pharmacokinetic profile of metaclazepam (Talis), a new 1.4-benzodiazepine. Influence of different dosage regimens on the pharmacokinetic profile of metaclazepam and its main metabolite under steady-state conditions.

The pharmacokinetic parameters of the new 1.4-benzodiazepine metaclazepam (Talis) were investigated. In particular, the question of whether the drug and/or its main metabolite accumulates in the body under steady-state conditions was studied.

[Dose-effect relation of N-prajmalium bitartrate with control of plasma levels].

15 patients with ventricular ectopic beats classified to at least Lown class III with more than 100 ventricular ectopic beats in one hour were treated with N-prajmalium bitartrate (NPAB) in increasing dosages. The first dosage of 4 X 5 mg/d has been increased by 5 mg in three steps of three days to a level of 4 X 20 mg/d. A resting ECG, the systolic time intervals and a 24 h ECG were registered before treatment and after every dose.

Pharmacokinetics of N-propylajmaline in relation to polymorphic sparteine oxidation.

In order to determine whether the metabolism of the antiarrhythmic drug N-propylajmaline is under the same genetic control as sparteine metabolism, the pharmacokinetics of this antiarrhythmic drug were studied in a groups of six extensive and four poor metabolizers of sparteine. Pronounced differences in terminal half-life, total plasma clearance, metabolic clearance and urinary excretion of N-propylajmaline were observed between extensive and poor metabolizers. A close relationship between the total clearance and metabolic clearance of N-propylajmaline and sparteine could be demonstrated.

Comparison of the pharmacokinetic profile of metaclazepam in old and young volunteers.

A single-centre, open, Phase I-study comparison of the pharmacokinetics of a single dose of metaclazepam 10 mg, a new 1,4-benzodiazepine has been done in 10 older and 20 younger volunteers. No important age-related effect was found on the kinetics of metaclazepam or its N-desmethyl derivative, the principal metabolite in man.

Metoclopramide kinetics at high-dose infusion rates for prevention of cisplatin-induced emesis.

Eleven male subjects aged 24 to 58 yr received cisplatin, 90 to 120 mg/m2 iv, in combination with other cytostatic drugs such as doxorubicin HCl and bleomycin. To prevent emesis, two high-dose metoclopramide regimens were started 2 hr before cytostatic therapy. Regimen A (n = 7) consisted of a loading dose infusion of 1 mg/kg/hr over 2 hr, followed by a maintenance infusion of 0.

Metabolism and pharmacokinetics of metaclazepam (Talis), Part III: Determination of the chemical structure of metabolites in dogs, rabbits and men.

The metabolism of 7-bromo-1-methyl-2-methoxymethyl-5-(2'-chlorophenyl)-2, 3-dihydro-1H-1,4-benzodiazepine (metaclazepam, Talis) in animals and men is described. Based upon mass spectrometry fifteen metabolites could be identified. Qualitative and quantitative differences in the biotransformation products of metaclazepam in comparison with the well known metabolites of other drugs in the 1,4-benzodiazepine class could be demonstrated.

[Pharmacokinetics and biotransformation of N-propylajmaline hydrogen tartrate in man].

10 and 20 mg of N-Propyl-ajmalin-hydrogentartrate (N-PAB, Neo-Gilurytmal) were administered i.v. and orally respectively to healthy volunteers.