Ajmaline

(BANM)
Ajmaline Chemical formula
Synonyms: Aimaliini; Ajmalin; Ajmalina; Ajmalinum; Rauwolfine. (17R,21R)Ajmalan-17,21-diol.
Cyrillic synonym: Аймалин.

💊 Chemical information

Chemical formula: C20H26N2O2 = 326.4.
CAS — 4360-12-7.
ATC — C01BA05.
ATC Vet — QC01B A05.

Pharmacopoeias.

In Jpn.

💊 Adverse Effects

Ajmaline depresses the conductivity of the heart, and at high doses can cause heart block. At very high doses it may produce a negative inotropic effect. High doses may cause cardiac arrhythmias, coma, and death. Arrhythmias have also been reported after usual intravenous doses (see below). Adverse neurological effects have been reported including eye twitching, convulsions, and respiratory depression. Hepatotoxicity and agranulocytosis may occasionally occur.

Effects on the heart.

Electrophysiologic study1 in 1955 patients revealed that ajmaline 1 mg/kg given intravenously could induce arrhythmias; 63 developed a supraventricular arrhythmia and 7 an atrioventricular re-entrant tachycardia. Ventricular tachycardia2,3 and torsade de pointes4 have been reported during diagnostic use.
1. Brembilla-Perrot B, Terrier de la Chaise A. Provocation of supraventricular tachycardias by an intravenous class I antiarrhythmic drug. Int J Cardiol 1992; 34: 189–98
2. Rolf S, et al. The ajmaline challenge in Brugada syndrome: diagnostic impact, safety, and recommended protocol. Eur Heart J 2003; 24: 1104–12
3. Pinar Bermúdez E, et al. Spontaneous sustained monomorphic ventricular tachycardia after administration of ajmaline in a patient with Brugada syndrome. Pacing Clin Electrophysiol 2000; 23: 407–9
4. Haverkamp W, et al. Torsade de pointes induced by ajmaline. Z Kardiol 2001; 90: 586–90.

💊 Precautions

As for Quinidine.

💊 Interactions

Antiarrhythmics.

Oral use of quinidine with ajmaline increased plasma concentrations of ajmaline considerably in 4 healthy subjects; the elimination half-life of ajmaline was increased about twofold.1 The pharmacokinetics of quinidine did not seem to be affected by ajmaline.
1. Hori R, et al. Quinidine-induced rise in ajmaline plasma concentration. J Pharm Pharmacol 1984; 36: 202–4.

💊 Uses and Administration

Ajmaline is an alkaloid obtained from the root of Rauwolfia serpentina (Apocynaceae). It is a class Ia antiarrhythmic used in the treatment of supraventricular and ventricular arrhythmias and for differential diagnosis of Wolff-ParkinsonWhite syndrome. Ajmaline is given by intravenous injection in a usual dose of 50 mg over at least 5 minutes. It may also be given by intravenous infusion, and has been given orally and by intramuscular injection. Ajmaline has also been used as the hydrochloride, monoethanolate, and phenobarbital salts.

Brugada syndrome.

Brugada syndrome is a congenital disorder affecting myocardial sodium channels and may be associated with sudden cardiac death. Class 1a antiarrhythmics such as ajmaline block the sodium channel and may have a role in the diagnosis of Brugada syndrome, although they are not suitable for treatment.
1. Rolf S, et al.The ajmaline challenge in Brugada syndrome: diagnostic impact, safety, and recommended protocol. Eur Heart J 2003; 24: 1104–12.

💊 Preparations

Proprietary Preparations

Austria: Gilurytmal; Cz.: Gilurytmal†; Ger.: Gilurytmal.
Published October 29, 2018.