QRS complex prolongation, ventricular tachycardia, first to third degree AV block, ventricular fibrillation or asystole may also occur. Patients should be informed of the signs of overdose and advised to seek urgent medical assistance if an overdose of propranolol has been taken.Ĭlinical features: Cardiac: Bradycardia, hypotension, and cardiogenic shock may develop. Propranolol is known to cause severe toxicity when used in overdose. Migraine: Under the age of 12: 20 mg two or three times daily. With regard to the elderly, the optimum dose should be individually determined according to clinical response.Ĭhildren: Dosage should be individually determined and the following is only a guide: Arrhythmias, phaeochromocytoma, thyrotoxicosis: 0.25 - 0.5 mg/kg three or four times daily as required. Non-operable malignant cases: 30 mg daily (see table).Įlderly: Evidence concerning the relation between blood level and age is conflicting. Preoperative: 60 mg daily for three days is recommended. Phaeochromocytoma: (Inderal is to be used only in the presence of effective alpha-blockade). In order to improve compliance the total daily dosage may thereafter be given as 80 mg twice a day (see table). Post-myocardial infarction: Treatment should start between days 5 and 21 after myocardial infarction, with an initial dose of 40 mg four times a day for 2 or 3 days. A maximum daily dose of 240 mg for arrhythmias must not be exceeded. A maximum daily dose of 240 mg for migraine and 480 mg for angina must not be exceeded (see table).Īrrhythmias, anxiety tachycardia, hypertrophic obstructive cardiomyopathy and thyrotoxicosis: A dosage range of 10-40 mg three or four times a day usually achieves the required response. An adequate response in anxiety, migraine and essential tremor is usually seen in the range.Ĩ0-160 mg/day, and in angina in the range 120-240 mg/day. With concurrent diuretic or other antihypertensive drugs a further reduction of blood pressure is obtained.Īngina, anxiety, migraine and essential tremor: A starting dose of 40 mg two or three times daily may be increased by the same amount at weekly intervals according to patient response. The usual dose range is 160-320 mg per day and the maximum daily dose must not exceed 640 mg per day (see table). Since the half-life may be increased in patients with significant hepatic or renal impairment, caution must be exercised when starting treatment and selecting the initial dose.Īdults: Hypertension: A starting dose of 80 mg twice a day may be increased at weekly intervals according to response. Propranolol is highly protein bound (80-95%). Propranolol is widely and rapidly distributed throughout the body with highest levels occurring in the lungs, liver, kidney, brain and heart. The liver removes up to 90% of an oral dose with an elimination half-life of 3 to 6 hours.
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Pharmacokinetics: Propranolol is completely absorbed after oral administration and peak plasma concentrations occur 1-2 hours after dosing in fasting patients.
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Propranolol is effective and well-tolerated in most ethnic populations, although the response may be less in black patients.
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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 a racemic mixture and the active form is the S(-) isomer, of propranolol. Propranolol, as with other beta-blockers, has negative inotropic effects, and is therefore contraindicated in uncontrolled heart failure (see Precautions). Competitive beta-adrenoceptor 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. It has no agonist activity at the beta-adrenoceptor, but has membrane stabilising activity at concentrations exceeding 1-3 mg/litre, though such concentrations are rarely achieved during oral therapy. Pharmacology: Pharmacodynamics: Propranolol is a competitive antagonist at both the beta-1 and beta-2 adrenoceptors.