[Pharmacodynamics and pharmacokinetics of the new specific bradycardic preparation bradizole].
The new drug Bradizol (SM-345), a 2-mercaptobenzimidazole derivative producing a specific bradycardic effect, is quite rapidly eliminated upon intravenous bolus in anaesthetiezed cats. After a combined injection (bolus followed by a 60-min infusion), a constant bradizol concentration in the blood plasma is observed over a time period of 90 min. The bradizol-induced bradycardic effect and the drug concentration in the blood plasma are tightly correlated. Upon per os administration of bradizol to the experimental animals, neither the drug is detected in the blood plasma, nor the bradycardic effect is observed. It is suggested that bradizol, possessing antiarrhythmic, antifibrillator, and antiischemic properties, can be used (by intravenous injections) for the therapy of patients with diverse tachyarrhythmia geneses, including those with the ischemic heart disease.
Chichkanov
G G
GG
Laboratory of Circulation System Pharmacology, Russian Academy of Medical Sciences, Moscow, Russia.
Zherdev
V P
VP
Tsorin
I B
IB
Sariev
A K
AK
Litvin
A A
AA
Kolyvanov
G B
GB
Kirsanova
G Iu
GIu
D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics / Q000494:pharmacology*; D001562:Benzimidazoles / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics / Q000494:pharmacology*; D002415:Cats; D003864:Depression, Chemical; D006339:Heart Rate / Q000187:drug effects*; D007262:Infusions, Intravenous; D007275:Injections, Intravenous; D013438:Sulfhydryl Compounds / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics / Q000494:pharmacology*
C111159:2-(2-(diethylamino)ethyl)thio-5-ethoxybenzimidazole; D000889:Anti-Arrhythmia Agents; D001562:Benzimidazoles; D013438:Sulfhydryl Compounds