The pharmacodynamics and metabolism of propranolol in man

A comparison of the pharmacokinetics of atenolol, metoprolol, oxprenolol and propranolol in elderly hypertensive and young healthy subjects.

“…Albumin concentrations were significantly lower in the Creatinine clearance (ml min 1) Figure 1 The relationship between atenolol renal clearance and creatinine clearance in young (v) and elderly (0) subjects. (Paterson et al, 1970;Reiss et al, 1970;Regardh et al, 1974). Atenolol is incompletely absorbed but a comparison of atenolol apparent oral clearance with atenolol renal clearance indicated that 31 + 3% and 41 + 6% of the dose was absorbed in the young and elderly groups respectively.…”

Direct measurement of propranolol bioavailability during accumulation to steady‐state.

“…According to theoretical arguments previously put forward (Wilkinson & Shand, 1975) the apparent oral clearance should equal intrinsic drug clearance (a measure of the activity of the drug metabolizing enzymes), provided the drug is completely absorbed and metabolized in the liver. Propranolol appears to satisfy both of these conditions, as the drug is fully absorbed and is not significantly eliminated by the kidneys (Paterson, Conolly, Dollery, Hayes & Cooper, 1970). Although some pulmonary extraction has been found in the dog (George, Orme, Buranapong, Macalene, Breckenridge & Dollery, 1976) it was not noted in the monkey (Nies, Evans & Shand, 1973) nor in man (Pessayre, Lebrec, Descatoire, Peigniux & Benhamou, 1977).…”

The assessment of beta‐adrenoceptor blocking drugs in man.

“…An explanation for this apparent discrepancy is provided by the work of Paterson et al (1970). They showed that an active metabolite of propranolol, 4-hydroxy propranolol, can be detected in the plasma only after oral administration.…”