INDICATIONS     CONTRA-INDICATIONS     DOSAGE     SIDE-EFFECTS     PREGNANCY     OVERDOSE     IDENTIFICATION     PATIENT INFORMATION
PUR-BLOKA® 10 TABLETS
PUR-BLOKA® 40 TABLETS

SCHEDULING STATUS:
S3

PROPRIETARY NAME
(and dosage form):

PUR-BLOKA^® 10 TABLETS
PUR-BLOKA^® 40 TABLETS

COMPOSITION:
Tablets containing 10 mg and 40 mg propranolol hydrochloride.

PHARMACOLOGICAL CLASSIFICATION:
A 5.2 Adrenolytics (Sympathicolytics).

PHARMACOLOGICAL ACTION:
Propranolol ß-adrenergic blocking agent, reduces cardiac activity by diminishing or preventing ß-adrenergic stimulation. It reduces the rate and force of contraction of the heart and prolongs A-V conduction time. In response to the inhibition of the ß-receptors, the oxygen requirement diminishes which proves beneficial in cases of angina pectoris. The blood pressure in hypertensive patients is also reduced because of this effect.
Its principal effect is to reduce the response of the heart to stress and exercise and it reduces blood pressure in patients with hypertension.
Peak plasma concentrations occur about 1 to 2 hours after an oral dose. Propranolol is more than 90% bound to plasma proteins. It is metabolised in the liver, the metabolites being excreted in the urine together with only small amounts of unchanged propranolol. The plasma half-life of propranolol is about 3 to 6 hours, the biological half-life being longer than plasma half-life.
Propranolol crosses the blood-brain barrier and the placenta and is distributed into breast milk.

INDICATIONS:

1.	Cardiac arrhythmias, especially supraventricular arrhythmias.
2.	To improve the tolerance to exercise in patients with angina of effort.
3.	Treatment of hypertension - usually in conjunction with a thiazide diuretic.
4.	Thyrotoxicosis - it may be given to reduce the heart-rate and control nervousness and perspiration.
5.	Phaeochromocytoma in conjunction with ß-adrenergic blocking agents.
6.	For the prophylaxis of migraine.
7.	Control of essential tremor.

CONTRA-INDICATIONS:
Hypersensitivity to any of the ingredients.
Avoid in patients with reactive airways disease such as bronchial asthma, bronchitis, bronchospasm or obstructive airways disease, congestive heart failure, sinoatrial or atrioventricular nodal abnormalities, metabolic acidosis, atrioventricular block, sinus bradycardia, heart failure refractory to digitalis, partial heart block, peripheral vascular disease, Raynaud's phenomena, ureamia, lactation and hypoglycaemia.
Pur-bloka should not be used in patients with cardiogenic shock.
Patients with phaeochromocytoma should not receive propranolol without concomitant alpha-adrenoceptor blocking therapy.
Safely in pregnancy has not been established and as propranolol is distributed in breast milk it is best avoided while the patient is breastfeeding.
In the pre-operative period, it is generally unwise to reduce the dosage to that which the patient is
accustomed, as there may be danger of aggravation of angina pectoris or of hypertension. A patient’s normal tachycardiac response to hypovolaemia or blood loss may be obscured during or after surgery. Particular caution should be taken in this regard. Pur-bloka should not be used after prolonged fasting.

WARNINGS:
Beta blockers may mask the symptoms of hyperthyroidism and of hypoglycaemia and may also unmask myasthenia gravis. Psoriasis may be aggravated.
In elderly patients or those with renal or hepatic dysfunction the dose may have to be reduced.
Abrupt withdrawal of (ß-blockers may result in angina, myocardial infarction, ventricular arrhythmias and death especially in patients with underlying cardiac disorders. Discontinuation of therapy should be gradual and patients should be advised to limit the extent of their physical activity during the period that the medicine is being discontinued.
Should not be given to patients with congestive heart failure unless their heart failure is controlled, and great care is still then necessary.
Administration to pregnant women shortly before giving birth or during labour may result in the newborn infants being born hypotonic, collapsed and hypoglycaemic.
While taking Pur-bloka, patients with a history of anaphylactic reaction to a variety of allergens may have a more serious reaction on repeated challenge. Such patients may be unresponsive to the usual dose of adrenaline used to treat the allergic reactions.

DOSAGE AND DIRECTIONS FOR USE:
Tablets should preferably be taken before meals.
Dosage is largely determined by response of the patient. In most conditions, treatment should begin with a small dose which should be gradually increased.

ADULTS:
HYPERTENSION:
40 to 80 mg twice a day increased to 160 to 320 mg daily.
Propranolol is not suitable for the emergency treatment of hypertension.
ANGINA:
40 mg given 2 or 3 times daily, increased at weekly intervals as required to 120 to 240 mg daily.
MANAGEMENT OF CARDIAC ARRYTHMIAS:
30 to 160 mg daily in divided doses for long term management.
TEMPORARY SUPPRESSION OF THYROTOXICOSIS AND IN THYROTOXIC CRISIS:
Usually 10 to 40 mg three or four times daily.
PHAEOCHROMOCYTOMA:
60 mg daily should be given on 3 pre-operative days always in association with alpha-blockade. If the tumor is inoperable, prolonged treatment may be given with a daily dose of 30 mg.
ANXIETY:
40 mg daily which can be increased to 40 mg two or three times daily.
MIGRAINE PROPHYLAXIS:
40 mg two or three times daily increased at weekly intervals up to 160 mg daily.
A dose of 240 mg daily may be needed by some patients.
ESSENTIAL TREMOR:
40 mg two or three times daily, increased at weekly intervals up to 160 mg daily.
A dose of 320 mg daily may be needed by some patients.
If symptoms of weakness or faintness occur, treatment should be withdrawn temporarily and started again at a lower dose which may be increased very slowly.

SIDE-EFFECTS AND SPECIAL PRECAUTIONS:
Side-effects may be minimised by starting treatment with a small dose and gradually increasing, although serious reactions have been reported after small doses.
Among the most serious side-effects are heart failure, heart block and bronchospasm.
Subjective side-effects include fatigue and coldness of extremeties.
The side-effects of propranolol include nausea, vomiting, diarrhoea, constipation, abdominal cramping, fatigue and dizziness.
Central nervous system effects include depression, malaise, hallucinations, sleep disturbances and confusion.
Bronchospasm may be precipitated in susceptible patients especially those suffering from asthma, bronchitis and other pulmonary diseases. Pneumonitis, pulmonary fibrosis and pleurisy may occur.
Other side-effects include skin rash, pruritis reversible alopecia, dry mouth, a lupus-like syndrome, male impotence, sclerosing perotinitis and retroperitoneal fibrosis.
Ocular symptoms include decreased tear production, blurred vision and soreness of the eyes.
Cardiovascular effects include bradycardia, congestive heart failure, hypotension, heart block, parenthesia, peripheral neuropathy and myopathies. Abrupt withdrawal of ß-blockers may exacerbate angina and lead to sudden death.
Exacerbation of peripheral vascular disease or the development of Raynaud's phenomenon (due to unopposed arteriolar alpha-sympathetic activation) may occur. Severe peripheral vascular disease and even peripheral gangerene may be precipitated.
Haematological reactions include nonthrombocytopenic purpura, thrombocytopenia and rarely agranulocytosis. Transient eosinophilia can occur.
Metabolic changes that may occur can affect glucose control and cholesterol concentrations.
In congestive heart failure propranolol should only be administered when the patient is fully digitalised and then only with great caution.
In diabetes mellitus propranolol may reduce blood sugar levels and may enhance the effects of hypoglycaemic agents.
Great care should be exercised in giving propranolol to patients undergoing anaesthesia, and myocardial depressants such as chloroform or ether must be avoided.

INTERACTIONS:
It can be dangerous to administer this medicine concomitantly with the following medicine: hypoglycaemic agents, phenothiazines and Class 1 antiarrhythmic agents such as disopyramide. Such interactions can have life-threatening consequences.
The effects of other myocardial depressant agents such as quinidine, procainamide or lignocaine may also be enhanced by propranolol. The effects of propranolol are dimished by ß-adrenergic stimulating agents; the hypotensive effects of propranolol may be dangerously reversed and the peripheral vasoconstrictor effects enhanced by alpha-adrenergic stimulating agents such as nor-adrenaline, or those with mixed alpha-and (ß-adrenergic stimulating properties such as adrenaline. Propranolol can impair the clearance of lidocaine. The effects of propranolol may be enhanced by adrenergic neurone blocking agents such as guanethidine, bethanidine, or reserpine, and the hypotensive effects by diuretics.
Propranolol may enhance some of he cardiac effects of digitalis and diminish others. Digitalisation of patients receiving long term ß-blocker therapy may be necessary if congestive heart failure is likely to develop. This combination can be considered despite the potentiation of chronotropic effect of the two medicines. Careful control of dosages and of the individual patients response (and notably pulse-rate) is essential in this situation.
Aluminium salts, cholestyramine and colestipol may decrease absorption of ß-blockers.
Phenytoin, rifampicin, phenobarbital and smoking induced hepatic biotransformation enzymes may decrease plasma concentrations of propranolol.
Cimetidine and hydrallazine may increase the bio-availability of propranolol by affecting hepatic blood flow.
Propranolol and cardiodepressant calcium-channel blockers such as verapamil and diltiazem have additive effects on the cardiac conducting system.
Concurrent use of amiodarone and propranolol can result in bradycardia, cardiac arrest and ventricular fibrillation.
Alcohol may increase the plasma clearance rate of propranolol.
The use of chlorpromazine with propranolol results in an increase in plasma-propranolol concentrations and bio-availability and reduced metabolism.
Bio-availability of propranolol is increased when used with dextropropoxyphene.
If a ß-blocker and clonidine are given concurrently, the clonidine should not be discontinued until several days after the withdrawal of the ß-blocker, as severe rebound hypertension may occur.
Caution should be exercised when transferring a patient from clonidine. The withdrawal from clonidine may result in the release of large amounts of catecholamines which may give rise to a hypertensive crisis.
If ß-blockers are administered in these circumstances, the unopposed alpha-receptor stimulation may potentiate this effect.

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT:
Overdosage may produce bradycardia and severe hypotension. Bronchospasm and heart failure may be produced in certain individuals. Cases of mild overdose should be observed for at least 4 hours, as apnoea and cardiovascular collapse may appear suddenly. Gastric lavage should be performed if within 4 hours of suspected overdose. Repeated activated charcoal is necessary in severe overdoses. Atropine may be used to treat bradycardia. If the response is inadequate, glucagon may be given intravenously. Alternatively dobutamine or isoprenaline may be used for the management of hypotension. Large doses of isoprenaline may be required to counteract the beta-blockade. Transvenous cardiac pacing may be required for severe bradycardia. Bronchospasm should be treated with IV aminophylline or inhaled or IV beta-agonist, eg. salbutamol.

IDENTIFICATION:

10 mg Tablets:	A plummish-pink flat, bevelled edged tablet, one side bisected and the other side engraved with a Lennon logo.
40 mg Tablets:	A plummish-pink, round shallow convex tablet with one side bisected and the other side engraved with a Lennon logo.

PRESENTATION:

10 and 40 mg:	Blister packs containing 50 tablets.
	Securitainers containing 250 and 1000 tablets.

STORAGE INSTRUCTIONS:
Store under 25°C and protect from light and moisture. KEEP OUT OF REACH OF CHILDREN.

REGISTRATION NUMBER:

10 mg	–L/5.2/192.
40 mg	– L/5.2/193.

NAME AND BUSINESS ADDRESS OF APPLICANT:
Pharmacare Limited
7 Fairclough Road
PORT ELIZABETH
6001

DATE OF PUBLICATION OF THIS PACKAGE INSERT:
5 December 1978

                        G682B
                KOHLER C&P P.E.

Updated on this site: December 1998
Current: December 2004
Source: Community Pharmacy
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