Relationship between plasma propranolol concentration and dose in young, healthy volunteers

Abstract

The relationship between dose and bioavailability of propranolol was determined in 12 healthy male subjects. The doses employed were 10, 40, 80 or 160 mg of propranolol HCl given three times daily for 4 days. Daily minimum plasma levels showed that there was no accumulation of the drug. In all subjects, non-linear relationships were observed between peak plasma level, or area under the plasma concentration-time curve, and dose. The between subject variation of these parameters was not dose related.

Anti-tumor activity of the beta-adrenergic receptor antagonist propranolol in neuroblastoma

“…Interestingly, the IC50 for hemangioma-derived cells in vitro (100μM) is similar to those for NB cells in vitro [53]. Pharmacokinetic data suggests that in patients treated with propranolol the peak serum concentrations range from 200-400 ng/ml, which is equivalent to 0.77-1.5µM [54]. There are many possible explanations for this significant discrepancy between in vitro and in vivo effects.…”

Pharmacokinetic and pharmacodynamic comparison of two doses of long acting propranolol (80 and 160 mg) in healthy subjects.

“…The bioavailability of the long acting propranolol has been estimated to be 50-80% (McAinsh et al, 1978), 50% (Serlin et al, 1983) and 68% (Leahey et al, 1980), that of the conventional tablet. The lack of a relationship between the propranolol dose and its blood (or plasma) concentrations and consequently its lack of a relation between the dose and the bioavailability has been observed in many studies (Walle etal., 1978;Dey et al, 1986;Kopitar et al, 1986). These studies used doses ranging from 10 to 160 mg following single or repeated administration of conventional propranolol.…”

Propranolol’s effects on the consolidation and reconsolidation of long-term emotional memory in healthy participants: a meta-analysis

“…Propranolol (or placebo) is typically administered 60-90 minutes before viewing the slides so that when memory consolidation begins (i.e., immediately after viewing the slides), propranolol is at its peak plasma concentration. 31 Memory for the viewed material is tested in a surprise forced-choice quiz after a washout period of 1-7 days.…”

“…Reactivation of the fear memory is achieved by a single presentation of the CS, (i.e., the reactivation cue) and memory is tested after a drug washout period of 1-7 days. It should be noted that pre-rather than postretrieval propranolol represents a slight departure from the typical reconsolidation protocol; however, in humans this time is required for pharmaco logical reconsolidation blockers ingested orally to reach their peak bioavailability 31 (for a discussion, see Schiller and Phelps 32 and Brunet and colleagues 33 ). A second method of manipulating memory reconsolidation involves script-driven imagery tasks.…”