[Absence of an anti-ischemic effect of the peripheral benzodiazepine receptor antagonist PK 11195. Study by atrial stimulation in man].

Abstract

We investigated the anti-ischemic effects of PK 11195 (RP 52028), a selective ligand for peripheral type benzodiazepine binding sites in man. In a first series of patients, we did not find any hemodynamic effect of 10 mg (8 patients) or 20 mg (8 patients) of the intravenously administered drug. The anti-ischemic effect was evaluated on 16 patients with coronary heart disease and a positive stress test in a double blind study of 20 mg of intra-venous PK 11195 (8 patients) versus placebo (8 patients). Ischemia was induced by pacing, and assessed by ST segment depression and lactates extraction before and 15 minutes after administration of the drug. No statistical differences could be found on these ischemia indices between the placebo and PK 11195 treated groups. Although experimental studies have shown interaction of the drug with the calcium channels, our study did not demonstrate any anti-ischemic effect with the dosage used.

• Authors: G Drobinski, P Lechat, L Eugène, Y Grosgogeat
• Journal: Therapie (Therapie) 1989 Jul-Aug Vol. 44 Issue 4 Pg. 263-7 ISSN: 0040-5957 [Print] France
• Vernacular Title: Absence d'effet anti-ischémique d'un antagoniste des récepteurs périphériques aux benzodiazépines PK 11195. Etude par stimulation atriale chez l'homme.
• PMID: 2595644 (Publication Type: Clinical Trial, Journal Article, Randomized Controlled Trial)

Chemical References

• Isoquinolines
• PK 11195

Topics

• Adult
• Aged
• Coronary Disease (drug therapy)
• Double-Blind Method
• Drug Evaluation
• Electric Stimulation
• Female
• Heart
• Hemodynamics (drug effects)
• Humans
• Injections, Intravenous
• Isoquinolines (pharmacology)
• Male
• Middle Aged