Detail of "53267-01-9"

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The efficacy of cibenzoline in preventing PES induction of ventricular tachycardia in the dog

The efficacy of cibenzoline in preventing PES induction of ventricular tachycardia in the dog. Keren, Gad; Tepper, David; Butler, Brenda; Miura, Dennis; Aogaichi, Keiko; Somberg, John (Dep. Med. Pharmacol., Albert Einstein Coll. Med., Bronx, NY 10461, USA). J. Clin. Pharmacol., 24(10), 466-72 (English) 1984. CODEN: JCPCBR. ISSN: 0091-2700. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The electrophysiol. effects of cibenzoline (I) [53267-01-9] were studied using programmed elec. stimulation (PES) techniques and were compared to those of quinidine [56-54-2]. Cibenzoline, like the conventional class 1 agent quinidine, was effective in preventing arrhythmia induction. Twelve dogs were given 0.02 mg/kg digoxin i.v. for seven days to achieve a steady-state digoxin level. On the eighth day, cibenzoline was administered in incremental doses (0.5 to 10.5 mg/kg) and PES was performed at 30-min intervals. A mean dose of 2.6 mg/kg cibenzoline prevented ventricular tachycardia induction. At this dose, cibenzoline had no significant effect on mean arterial blood pressure, but PR interval increased by 17%, QRS duration by 27% and the ventricular refractory period (ERP) for the first extra stimulus increased by 35%. A gradual decrease in heart rate and an increase in PR interval and QRS duration was caused by incremental doses of cibenzoline. In 6 addnl. animals, quinidine was administered in incremental doses (1 to 30 mg/kg) and PES performed at 30-min intervals. A mean of 15 mg/kg prevented induction of ventricular tachycardia in 5 animals. No significant change in heart rate, PR interval, QRS duration, and ERP was found at the ED.

Quantitation of cibenzoline in human plasma by gas chromatography-negative-ion chemical-ionization mass spectrometry

Quantitation of cibenzoline in human plasma by gas chromatography-negative-ion chemical-ionization mass spectrometry. Min, Bo H.; Garland, William A. (Dep. Pharmacokinet., Biopharm. Drug. Metab., Hoffmann-La Roche Inc., Nutley, NJ 07110, USA). J. Chromatogr., 336(2), 403-9 (English) 1984. CODEN: JOCRAM. ISSN: 0021-9673. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Cibenzoline (I) [53267-01-9] and the internal std. (a 15N2-stable isotope analog of I) were extd. from the human plasma samples with C18 bonded-phase disposable columns eluted with MeOH and the MeOH was evapd. The residues were reconstituted in EtOAc and I and the internal std. were derivatized with pentafluoropropionic acid to their pentafluoropropionyl acid to their pentafluoropropionyl (PFP) derivs. The PFP derivs. were analyzed on a gas chromatograph with a glass column with 3% SP-2250 on 80-100 mesh Supelcoport at 265° with CH4 as the carrier gas. Detection was by neg.-ion chem.-ionization mass spectrometry with selected-ion monitoring at m/z 368 and m/z 370. The calibration curves were linear for I concns. of 1-50 ng/mL. Mean intra- and interassay precisions were 2.1 and 8.1%, resp. The assay was used to det. I levels in plasma from humans given a 50 mg oral dose of I.