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At least 109 records · Page 6Linked to original sources
PubMed1979

Evaluation of clinical efficacy and plasma levels of aprindine.

The clinical efficacy of Aprindine, a new antiarrhythmic agent was tested in 37 patients with ventricular and supraventricular arrhythmias. The drug was shown to be effective - disappearance or prevention of relapse of the arrhythmia - in 80% of the cases with ventricular tachycardia, and in 67.7% of the cases with premature ventricular beats. No judgement was possible for supraventricular tachycardia due to the small number of patients. Effectivness of Aprindine was found to be related more closely to the administered dose expressed in mg/kg body weight than to plasma level in steady-state. Discontinuation of therapy was necessary in 5 cases due to the appearance of side effects (tremor and dizziness). Side effects were not found to be in relation with plasma levels or administered dose. In the period of observation (2 months) no effects on blood cells were noticed.

Adult↗
PubMed1995

Determination of aprindine in human plasma using reversed phase HPLC.

A rapid, simple, accurate method is presented for the determination of aprindine in human plasma. Liquid-liquid extraction of aprindine was carried out using diethyl ether. Amiodarone was applied as an internal standard. The samples were chromatographed on LiChrosorb RP-18 (10 microns) column and the mobile phase was methanol/acetonitrile/phosphate buffer pH 2.5 (80:15:5). The detection was carried at 254 nm. The method was tested for linearity (range from 0.5 to 2.5 micrograms/ml), recovery (ca. 90%) and precision (CV = 3.7%).

Amiodarone↗
PubMed1994

Chromatographic analysis (TLC) aprindine and nadoxolol in human plasma.

Aprindine and nadoxolol extracted from plasma were separated by TLC method on silica gel by ascending technique on 5 x 20 cm and 2.5 x 7.5 cm microscopic slides and also by horizontal development, using suitable mobile phases. The substances were identified by reaction with Kiefer reagent (up to the amount 100 ng of aprindine and 300 ng of nadoxolol).

Anti-Arrhythmia Agents↗
PubMed1998

Prediction of catalepsies induced by amiodarone, aprindine and procaine: similarity in conformation of diethylaminoethyl side chain.

Recently, clinical cases of parkinsonism due to antiarrhythmics drugs amiodarone and aprindine and a local anesthetic drug procaine have been reported. We performed both in vivo and in vitro experiments to quantitatively predict the intensity of catalepsy by these drugs and haloperidol in mice. Haloperidol showed the most potent relative intensity of catalepsy, followed by aprindine, metoclopramide, tiapride, amiodarone and procaine, in that order. In vivo dopamine D1 and D2 receptor occupancies of the six drugs to the striatum were observed. In vitro binding affinity (Ki) of these drugs to the D1 and D2 receptors in the striatum synaptic membrane was within the range of 60 nM to 706 microM, 0.5 nM to 75 microM and 860 nM to 115 microM, respectively. A good correlation between the relative intensity of drug-induced catalepsy and the Ki values for the dopamine D1 and D2 receptors was obtained (r =.911 and r =.896, respectively; P <.05). The partial tertiary structure of the tested drugs was well superimposed on that of haloperidol. In conclusion, these drug-induced catalepsies were due to the blockade of the D1 and D2 receptors, which was related to the analogous tertiary structures (diethylaminoethyl side chain).

Amiodarone↗
PubMed1975

[Clinical observations of the new anti-arrhythmic drug aprindine from long-term trend analyses(author's transl)].

The therapeutic effectiveness of aprindine (Amidonal) was evaluated by trend analyses in 25 patients with predominantly severe forms of ventricular extrasystoles. The arrhythmia was stopped or improved in most instances. Severe side-effects for which the drug had to be discontinued occurred in three patients. The drug has a long half-life (about 20-30 hours). As a result, there can be cumulative dose-dependent side-effects, largely of a CNS type, disappearing after the dose has been reduced. Thirteen patients continued to be treated on an ambulatory basis, the oral maintenance dose averaging 100 mg/d, the mean follow-up period 11 1/2 months. There was no evidence of side-effects on liver, electrolytes, renal function or blood.

Adolescent↗
PubMed1993

The metabolism of aprindine in relation to the sparteine/debrisoquine polymorphism.

1. Incubation of the class I antiarrhythmic drug aprindine (AP) with human liver microsomes resulted in the formation of two hydroxylated metabolites (HA1 and HA2) and desethylaprindine which were identified by GC-mass spectrometry. In liver microsomes isolated from a poor metaboliser (PM) of sparteine no hydroxylated metabolites of AP were detected whereas AP N-dealkylation was unimpaired. Thus hydroxylation of AP is mediated by cytochrome P450 2D6 (CYP2D6). 2. AP was found to be a competitive inhibitor of CYP2D6 as indicated by its ability to impair the formation of (2S)-hydroxysparteine, 5,6-didehydrosparteine and 5-hydroxypropafenone by human liver microsomes. 3. These in vitro findings are consistent with a major role of CYP2D6 in the clearance of AP in vivo, with its ability to impair the metabolism of other CYP2D6 substrates in vivo, and an ability to cause phenocopying (conversion of extensive metaboliser phenotypes for sparteine/debrisoquine to apparent 'poor metabolisers).

Aprindine↗
PubMed1998

Isolation of a major metabolite (i-OHAP) of aprindine and its identification as N-[3-(N,N-diethylamino)propyl]-N-phenyl-2-aminoindan-5-ol.

i-OHAP, a major metabolite of aprindine (AP), was isolated by TLC from rat feces and identified as N-13-(N,N-diethylamino)propyl]-N-phenyl-2-aminoindan-5-ol, based on 1H-NMR, the H-H correlation spectroscopy (COSY) spectrum, MS and LC-MS. Its structure was also confirmed by comparison with the synthesized compound. The hydroxy group of i-OHAP was located at the 5-position of the indan ring. AP is a prochiral compound, and the metabolism of AP to i-OHAP was stereoselective. The ratio of (+)/(-)-i-OHAP in rat feces and in human urine was about 5 and 15, respectively.

Adult↗
PubMed1999

Profiles of aprindine, cibenzoline, pilsicainide and pirmenol in the framework of the Sicilian Gambit. The Guideline Committee for Clinical Use of Antiarrhythmic Drugs in Japan (Working Group of Arrhythmias of the Japanese Society of Electrocardiology).

The Vaughan Williams classification has been used widely by clinicians, cardiologists and researchers engaged in antiarrhythmic drug development and testing in many countries throughout the world since its initial proposal in the early 1970s. However, a major criticism of the Vaughan Williams system arose from the extent to which the categorization of drugs into classes I-IV led to oversimplified views of both shared and divergent actions. The Sicilian Gambit proposed a two-dimensional tabular framework for display of drug actions to solve these problems. From April to December 1996, members of the Guideline Committee met to discuss pharmacologic profiles of 4 antiarrhythmic drugs (aprindine, cibenzoline, pilsicainide, and pirmenol) that were not included in the original spreadsheet but are used widely in clinical practice in Japan. The discussion aimed to fit the drug profiles into the Gambit framework based on all the important literature published to date regarding the actions of the 4 drugs. This report is a summary of that deliberation.

Animals↗
PubMed2002

Nonlinear pharmacokinetics of aprindine in guinea pigs.

After intravenous bolus administration of aprindine (AP) to conscious guinea pigs, the semilogarithmic plasma concentration versus time curve was linear at a dose of 2 mg/kg, but convex at doses of 5 and 10 mg/kg. AP concentrations immediately after administration (C(p0)) were almost identical, irrespective of the dose received. The areas under the plasma concentration-time curves (AUCs) were proportional to the AP doses. At 2 mg/kg, the plasma total clearance (CL(tot)) of AP was high (279+/-80 mL/h), and its volume of distribution (Vd(ss)) was large (245+/-99 mL). Total blood clearance and time-averaged blood clearance (CL(ave)) values for AP were similar to those for R(+) propranolol (PL) after intravenous coadministration of R(+) PL (0.25 mg/kg) and AP (2 or 10 mg/kg). An in vitro serum protein binding study showed that the unbound fraction of AP was concentration-dependent. In guinea pigs pretreated with turpentine oil (2 mL/kg/day), the elimination of AP after intravenous doses of 2 and 5 mg/kg closely followed first-order kinetics, while C(p0) and AUC increased in proportion to the AP doses. The bound fraction of AP in the serum was larger after turpentine oil pretreatment than in normal guinea pig serum in vitro. From these observations, the nonlinear pharmacokinetics of AP observed in guinea pigs can be attributed to nonlinear serum protein binding.

Journal Article↗
PubMed1978

Characterization of products derived from aprindine hydrochloride photolysis.

An investigation of the products resulting from the photolysis of apridine hydrochloride is described. The compounds were characterized by GLC spiking experiments and combined GLC--mass spectrometry. In some cases, Rf values derived from TLC and/or preparative TLC and subsequent high-resolution mass spectral measurements also were employed for identification.

Aprindine↗