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Propraderel

Al-Tinez Pharmaceuticals Limited
9, Olowogbowo Str off Obokun Str by Coker Rd, Ilupeju, Lagos
Tel: 01-4826452; 0802-307-7320, 0803-305-7978

Brand Name

Propraderel

Manufacturer

ALPA LABORATORIES LTD. 33/2, A.B. Road, Pigdamber-453446.

Therapeutic Class

Beta-blockers

Dosage Form, Composition & NAFDAC Registration Number (NRN)

Tablet(NRN: A4-4809): Each uncoated tablet contains Propanolol Hydrochloride BP 40 mg.

Pack size: 14 Tablets in a strip.

Pharmacology

Indications

1). Management of angina pectoris.

2). Control of hypertension.

3). Long-term prophylaxis against reinfarction after recovery from acute myocardial infarction.

4). Management of hypertrophic obstructive cardiomyopathy.

5). Management of essential tremor.

6). Relief of situation anxiety and generalised anxiety symptoms, particularly those of somatic type

7). Control of most forms of cardiac arrhythmia.

8). Adjunctive management of thyrotoxicosis and thyrotoxic crisis

9). Management of phaeochromocytoma peri-operatively (with an alpha-blocker).

10). Prophylaxis of migraine.

11). Prophylaxis of upper gastrointestinal bleeding in patients with renal hypertension and oesophageal varices.

Contra-indications

Propranolol is contraindicated in cardiogenic shock; sinus bradycardia and greater than first degree block; bronchial asthma: and in patients with known hypersensitivity to propranolol hydrochloride.

Precautions/Warnings

Interactions

Adrenaline (epinephrine):
Care should be taken in the parenteral administration of preparations containing adrenaline (epinephrine) to patients taking beta-adrenoceptor blocking drugs and in rare cases, vasoconstriction, hypertension and bradycardia may result.

Anaesthetics:
Care should be taken when using anaesthetic agents with propranolol. The anaesthetist should be informed and the choice of anaesthetic should be the agent with as little negative inotropic activity as possible

Anti-arrhythmic:
Caution must be exercised in co-prescribing beta-adrenoceptor blockers with Class I anti-arrhythmic agents such as disopyramide, quinidine, flecainide and amiodarone as they may have potentiating effects on arterial conduction time and induce the negative inotropic effect. Administration of propranolol during infusion of lidocaine may increase the plasma concentration of lidocaine by approximately 30%. Patients already receiving propranolol tend to have higher lidocaine levels than controls. The combination should be avoided.

A combined use of beta-adrenoceptor blocking drugs and calcium channel blockers with negative inotropic effects eg verapamil, diltiazem can lead to prolongation of SA and AV conduction particularly in patients with impaired ventricular function or conduction abnormalities. This may result in severe hypotension, bradycardia and cardiac failure. Neither the beta-adrenoceptor blocking drug nor the calcium channel blocker should be administered intravenously within 48 hours of discontinuing the other. Digitalis glycosides used in association with beta-adrenoceptor blockers may increase AV conduction time.

Anticoagulants:
Propranolol may cause a reduction in clearance and an increase in plasma concentrations of warfarin.

Antidiabetic drugs:
Propranolol modifies the tachycardia of hypoglycaemia; caution should, therefore, be exercised in the concomitant use of propranolol and hypoglycaemic therapy in diabetic patients. Propranolol may prolong the hypoglycaemic response to insulin.

Antihypertensives:
Beta-adrenoceptor blocking agents may exacerbate the rebound hypertension which can follow the withdrawal of clonidine. If the drugs are co-administered, the beta-adrenoceptor blocking drug should be withdrawn several days before discontinuing clonidine. If replacing clonidine with beta-adrenoceptor therapy the introduction of the beta-adrenoceptor blocking drug should be delayed for several days after clonidine administration has stopped.

Concomitant use of moxonidine and beta blockers may result in an enhanced hypotensive effect. The steps for moxonidine withdrawal/introduction should be the same as for clonidine. A hypotensive effect may be enhanced when propranolol is taken with diuretics, methyldopa or levodopa.
Prazosin or other alpha-adrenoreceptor blockers may potentiate postural hypotension, tachycardia and palpitations.

Antimigraine drugs:
Caution is necessary if ergotamine, dihydroergotamine or related compounds are given in combination with propranolol since vasopastic reactions have been reported in a few patients. Propranolol inhibits the metabolism of rizatriptan which can significantly increase plasma concentration levels. A dose reduction to 5 mg is recommended. Administration should be separated by 2 hours.

Barbiturates:
The metabolism of propranolol may be increased by potent liver enzyme inducer barbiturates.

Chlorpromazine:
Concomitant administration of propranolol and chlorpromazine may result in an increase in plasma levels of both drugs. This may lead to an enhanced antipsychotic effect for chlorpromazine and an increased antihypertensive effect for propranolol.

Cimetidine:
Concomitant use of cimetidine will increase, whereas alcohol will decrease the plasma levels of propranolol

Hydralazine:
Concomitant use of hydralazine with increase, whereas alcohol, will decrease the plasma levels of propranolol

Imipramine:
Propranolol may cause plasma concentrations of imipramine to increase.

Monoamine-oxidase inhibitors:
The hypotensive effects of beta-blockers may be enhanced by MAOls.

Non-steroidal anti-inflammatory drugs:
NSAIDs notably indometacin, may cause an increase in blood pressure. This may be particularly significant in patients with poorly controlled hypertension.

Rifampicin:
The metabolism of propranolol may be increased by potent liver enzyme inducer rifampicin.

Selective Serotonin Re-uptake Inhibitors:
Fluvoxamine inhibits oxidative metabolism and increases plasma concentrations of propranolol. This may result in severe bradycardia

Theophylline:
Propranolol reduces the clearance and consequentially increases the plasma concentration of theophylline

Tobacco:
Smoking tobacco may oppose the effects of beta-blockers in the treatment of angina or hypotension. Patients should be encouraged to stop smoking, apart from its other toxic effects, it aggravates myocardial ischaemia, increases heart rate and can impair blood pressure control if patient continues to smoke, dosage of the beta blocker may need to be increased or a cardio-selective beta blocker may be more appropriate

Laboratory tests:
Interference with laboratory tests - Propranolol has been reported to interfere with the estimation of serum bilirubin by the diazo method and with the determination of catecholamines by methods using fluorescence.

Adverse Effects

Very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1,000 to <1/100); rare (≥1/10,000 to <1/1,000); very rare (<1/10,000); Frequency not known (cannot be estimated from the available data).

The following undesired events, listed by body system, have been reported:

Blood and lymphatic system disorders
Rare: Thrombocytopenia,
Frequency not known: agranulocytosis

Endocrine disorders
Frequency not known: masking signs of thyrotoxicosis.

Metabolic and nutritional disorders
Frequency not known: hypoglycaemia in neonates, infants, children, elderly patients, patients on haemodialysis, patients on concomitant antidiabetic therapy, patients with prolonged fasting and patients with chronic liver disease has been reported. Changes In lipid metabolism (changes in blood concentrations of triglycerides and cholesterol)

Psychiatric disorders
Common: Sleep disturbances, nightmares.
Frequency not known: depression, confusion

Nervous system disorders
Rare: Hallucinations, psychoses, mood changes, confusion, memory loss, dizziness, paraesthesia.
Very rare: Isolated reports of myasthenia gravis like syndrome or exacerbation of myasthenia gravis have been reported.
Frequency not known: headache, seizure linked to hypoglycaemia.

Eye disorders
Rare: visual disturbances, dry eyes
Frequency not known: conjunctivitis

Cardiac disorders
Common: bradycardia
Rare: Heart failure deterioration, precipitation of heart block, postural hypotension which may be associated with syncope.
Frequency not known: worsening of attacks of angina pectoris.

Vascular disorders
Common: cold extremities, Raynaud's syndrome.
Rare: exacerbaction of intermittent claudication.

Respiratory thoracic and mediastinal disorders.
Rare: Bronchospasm may occur in patients with bronchial asthma or a history of asthmatic complaints, sometimes with fatal outcome.
Frequency not known: dyspnoea.

Gastrointestinal disorders.
Uncommon: diarrhoea, nausea, vomiting.
Frequency not known: constipation, dry mouth.

Skin and subcutaneous tissue disorders.
Rare: alopecia, purpura, psoriasiform skin reactions, exacerbation of psoriasis, rash.

Musculoskeletal system and connective tissue disorders.
Frequency not known: arthralgia

Renal and urinary disorders
Frequency not known: reduced renal blood flow and GFR.

Reproductive system and breast disorders.
Frequency not known: sexual dysfunction

General disorders and administration site conditions.
Common: fatigue and/or lassitude (often transient)

Investigations

Very rare: An increase in ANA (antinuclear antibodies) has been observed with many beta blockers, however the clinical relevance of this is not clear.

Discontinuation of the drug should be considered if, according to clinical judgement, the well being of the patient is adversely affected by any of the above reactions. Cessation of therapy with a beta-blocker should be gradual in the rare event of intolerance manifested as bradycardia and hypotension, the drug should be withdrawn and, if necessary, treatment for overdosage instituted.

Dosage & Administration

The tablets should preferably be administered before meals.

Adults and children over 12 years:

Angina, migraine and essential tremor: initially 40 mg two or three times daily, increasing by the same amount at weekly intervals according to response. An adequate response in migraine and essential tremor is usually seen in the range 80 – 160 mg daily and in angina 120 – 240 mg daily.

Hypertension: Initially 80 mg twice daily, which may be increased at weakly intervals according to response. The usual dose range is 160-320 mg/daily. With concurrent diuretic or other antihypertensive drugs a further reduction of blood pressure is obtained.

Arrhythmias, anxiety tachycardia, hypertrophic obstructive cardiomyopethy and thyrotoxicosis: Most patients respond within the dosage range of 10-40 mg three or four times daily.

Situational and generalised anxiety: A dose of 40 mg daily may provide short term relief of acute situational anxiety. Generalised anxiety, requiring longer term therapy, usually responds adequately to 40 mg twice daily which, in individual cases, may be increased to 40 mg three times daily. Treatment should be continued according to response. Patients should be reviewed after six to twelve months' treatment.

Post myocardial infarction: Treatment should be initiated between days 5 - 21 after myocardial infarction with an initial dose of 40 mg four times daily for two or three days. In order to improve compliance, the total daily dosage may thereafter be given as 80 mg twice a day.
Phaeochromocytoma (used only in conjunction with an alpha-receptor blocking drug) Pre-operatively; 60 mg daily for three days is recommended. Non-operable malignant cases, 30 mg daily.

Portal Hypertension: Dosage should be titrated to achieve approximately 25% reduction in resting heart rate Dosing should begin with 40 mg twice daily, increasing to 80 mg twice daily depending on heart rate response. If necessary, the dose may be increased incrementally to a maximum of 160 mg twice daily.

Children and Adolecent:
Arrhythmias. Dosage should be determined according to the cardiac status of the patient and the circumstances necessitating treatment. The doses given are intended only as a guide; 0.25 - 0.5 mg/kg bodyweight three or four times daily as required.

Elderly: Evidence concerning the relationship between blood level and age is conflicting. The optimum dose should be individually determined according to clinical response.

Hepatic impairment
The bioavailability of propranolol may be increased in patients with hepatic impairment and dose adjustments may be required. In patients with severe liver disease (e.g. cirrhosis) a low initial dose is recommended (not exceeding 20 mg three times a day) with close monitoring of the response to treatment (such as the effect on heart rate).

Renal Impairment
Concentrations of propranolol may increase in patients with significant renal impairment and haemodialysis.
Caution should be exercised when starting treatment and selecting the initial dose.

For oral use.

PREGNANCY AND LACTATION

Pregnancy
As with all other drugs, propranolol should not be given in pregnancy or lactation unless its use is essential. There is no evidence of teratogenicity with propranolol. However beta-adrenoceptor blocking drugs reduce placental perfusion, which may result in intra-uterine foetal death, immature and premature deliveries. In addition, adverse effects (especially hypoglycaemia and bradycardia in the neonate and bradycardia in the foetus) may occur. There is an increased risk of cardiac and pulmonary complications in the neonate in the post-natal period

Lactation
Most beta-adrenoceptor blocking drugs, particularly lipophilic compounds, will pass into breast milk although to a variable extent. Breast feeding is therefore not recommended following administration of these compounds.

Storage/Handling Recommendations

Store in a cool and dry place.

KEEP MEDICINES OUT OF REACH OF CHILDREN.

Review Date

2017-11-25 02:50:27