Alprenolol, or alfeprol, alpheprol, and alprenololum (Gubernal, Regletin, Yobir, Apllobal, Aptine, Aptol Duriles), is a non-selective beta blocker as well as a 5-HT1A and 5-HT1B receptor antagonist,[1] used in the treatment of angina pectoris.[2] It is no longer marketed by AstraZeneca, but may still be available from other pharmaceutical companies or generically.

Pharmacology

Pharmacokinetics

The brain-to-blood ratio of alprenolol in humans has been found to be 16:1.[3] For comparison, the brain-to-blood ratio of the highly lipophilic propranolol was 15:1 to 26:1 and of the hydrophilic atenolol was 0.2:1.[3]

References

  1. Langlois M, Brémont B, Rousselle D, Gaudy F (1993). "Structural analysis by the comparative molecular field analysis method of the affinity of beta-adrenoreceptor blocking agents for 5-HT1A and 5-HT1B receptors". Eur. J. Pharmacol. 244 (1): 77–87. doi:10.1016/0922-4106(93)90061-d. PMID 8093601.
  2. Hickie JB (1970). "Alprenolol ("aptin") in angina pectoris. A double-blind multicentre trial". Med. J. Aust. 2 (6): 268–72. doi:10.5694/j.1326-5377.1970.tb49984.x. PMID 4393977. S2CID 6879318.
  3. 1 2 Drayer DE (1987). "Lipophilicity, hydrophilicity, and the central nervous system side effects of beta blockers". Pharmacotherapy. 7 (4): 87–91. doi:10.1002/j.1875-9114.1987.tb04029.x. PMID 2891122.