Source: Medicines & Healthcare Products Regulatory Agency (GB) Revision Year: 2019 Publisher: Accord-UK Ltd (Trading style: Accord), Whiddon Valley, Barnstaple, Devon, EX32 8NS
Pharmacotherapeutic group: beta blocking agents, non-selective
ATC code: C07AA05
Propranolol hydrochloride is a beta-adrenoceptor blocking agent.
Propranolol is a competitive antagonist at both beta, and beta2-adrenoceptor, but has membrane stabilising activity at concentrations exceeding 1-3mg/litre, though such concentrations are rarely achieved during oral therapy. Competitive beta-blockade has been demonstrated in man by a parallel shift to the right in the dose-heart rate response curve to beta-agonists such as isoprenaline.
Propranolol as with other beta-blockers, has negative inotropic effects, and is therefore contraindicated in uncontrolled heart failure.
Propranolol is a racemic mixture and the active form is the S (-) isomer of propranolol. With the exception of inhibition of the conversion of thyroxine to triiodothyronine, it is unlikely that any additional ancillary properties possessed by R (+) propranolol, in comparison with the racemic mixture, will give rise to different therapeutic effects.
Propranolol is effective and well tolerated in most ethnic populations, although the response may be less in black patients.
Propranolol is almost completely absorbed from the gastrointestinal tract, but it is subject to considerable first-pass metabolism.
Peak plasma concentrations occur about 1 to 2 hours after dosing in fasting patients. Propranolol is widely and rapidly distributed throughout the body with highest levels occurring in the lungs, liver, kidney, brain and heart. Propranolol is highly protein bound (80 to 95%).
It is metabolised in the liver, the metabolites being excreted in the urine together with only small amounts of unchanged Propranolol; at least one of its metabolites is considered to be biologically active.
The biological half-life of Propranolol is longer than would be anticipated from its plasma half-life of about 3-6 hours.
There are no pre-clinical data of relevance to the prescriber which are additional to that already included in other sections of the SPC.
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