Betac

Betac

betaxolol

Manufacturer:

Medochemie

Distributor:

Medochemie
Full Prescribing Info
Contents
Betaxolol hydrochloride
Description
Each "Betac" 20 mg tablet contains 20 mg betaxolol as betaxolol hydrochloride.
Excipients/Inactive Ingredients: "Betac" 20 mg tablets also contain: lactose, microcrystalline cellulose, sodium starch glycolate, colloidal anhydrous silica, magnesium stearate, polyvinyl alcohol, titanium oxide (E 171), talc, lecithin and xanthan gum.
Action
Betaxolol is a cardioselective beta-adrenoceptor blocking agent. The drug is characterized by a long duration of action, no intrinsic sympathomimetic activity, weak membrane stabilizing activity.
Indications/Uses
For the management of hypertension.
Dosage/Direction for Use
Betaxolol is administered once a day.
Therapy should be initiated with 10 mg betaxolol HCI daily (half a tablet). If necessary the dose may be increased up to 20 mg daily (one tablet) after 7 to 14 days of treatment. Doses more than 20 mg daily have been shown to produce no significant additional effect, although they are well tolerated.
Withdrawal of therapy must be performed gradually over a period of about 2 weeks. Patients should be carefully observed during that period.
Renal failure: Renal dysfunction results in a decrease in betaxolol clearance. Dose titration should begin at 5 mg once daily for those with severe renal impairment (creatinine clearance less than 20 ml/min). In the case of chronic haemodialysis (blood or peritoneal), the initial recommended dose is 5 mg/day. If necessary, dosage may be increased in increments of 5mg daily, no more frequently than at 2-week intervals, up to a maximum of 20mg daily.
For a creatinine clearance over 20ml per minute, it is necessary to change the dosage. However, clinical monitoring is recommended at the start of the treatment until the equilibration of blood levels is reached (4 days on average).
Hepatic failure: No dose adjustment is necessary, but clinical supervision is recommended at therapy initiation.
Elderly patients: Geriatric patients are more susceptible to bradycardia, one of the adverse reactions of betaxolol, which appears to be dose related. Elderly patients should initiate betaxolol therapy at lower doses; the usual starting dose is 5 mg once daily.
Children: Safety and efficacy of the drug in children has not been established. Betaxolol is not recommended for pediatric use.
Overdosage
In case of overdose the most common effects expected are bradycardia, hypotension, congestive heart failure, bronchospasm and hypoglycaemia.
There is no specific antidote. Treatment must be symptomatic and supportive.
For the management of hypotension the administration of dopamine, dobutamine or norepinephrine is recommended. Atropine should be administered for the management of bradycardia. In case of cute cardiac failure, conventional therapy including digitalis, diuretics and oxygen must be initiated immediately. Bronchospasm may be related with a β2 agonist. Additional therapy with aminophylline may be considered.
Contraindications
The administration of drug is contraindicated in patients with known hypersensitivity to betaxolol or any other components of the tablet.
Betaxolol is also contraindicated when patients have: Uncompensated congestive heart failure.
Cardiogenic shock.
Second and third degree AV block.
Association with MAOI or verapamil.
Bradycardia (<45-50 beats per minute).
Severe forms of asthma and chronic obstructive pulmonary disease.
Cardiac insufficiency not controlled with treatment.
Prinzmetal's angina (as a monotherapy in its isolated/typical form).
Sinus node dysfunction (including sinoatrial block).
Severe forms of Raynaud's phenomenon and peripheral arterial disorders.
Untreated pheochromocytoma.
Hypotension.
Previous history of anaphylactic reaction.
In combination with floctafene and sultopride.
Special Precautions
Asthma and chronic obstructive pulmonary disease: Beta-blockers may only be administered in mild forms of these conditions, using a beta-1 selective blocker at an initially low dose. It is recommended to have pulmonary function tests performed before beginning treatment. In case of an attack while undergoing treatment, beta-mimetic bronchodilators may be used.
Cardiac Insufficiency: In patients with cardiac insufficiency which is controlled with treatment, when necessary betaxolol should be administered at very low doses and then progressively increased under strict medical monitoring. Bradycardia: If the heart rate decreases to less than 50-55 beats per minute at rest and the patient exhibits bradycardia-related symptoms, the dosage should be reduced.
First-degree atrioventricular block: Given the negative dromotropic effect of beta-blockers, betaxolol should only be administered with caution to patients with first-degree atrioventricular block.
Prinzmetal's angina: Beta-blockers can increase the number and duration of anginal episodes in patients with Prinzmetal's angina. The use of beta-1 cardioselective beta-blocker is possible in mild and related forms, provided that it is administered concomitantly with a vasodilator.
Peripheral arterial disorders: In patients with peripheral arterial disorders (Raynaud's disease or phenomenon, arteritis or chronic obliterating arteriopathies of lower limbs), the use of beta-blockers can worsen these conditions. In these situations, it is advisable to use a cardio-selective beta-blocker with partial agonist potential, which shall be administered with caution.
Pheochromocytoma: The use of beta-blockers in the treatment of hypertension due to treated pheochromocytoma requires close monitoring of the arterial blood pressure. Diabetic patients: Instruct the patient and reinforce the self-monitoring of blood glucose at the start of treatment. The warning signs of hypoglycaemia may be masked, particularly with tachycardia, palpitations and sweats.
Psoriasis: As exacerbations of the disorder have been reported with the use of beta-blockers, the indication of use should be carefully considered.
Allergic reactions: In patients with a risk of any severe anaphylactic reaction, particularly to floctafenine or in those receiving drug sensitization treatments, treatment with beta-blockers may lead to an exacerbation of the reaction and resistance to its treatment with adrenaline at the usual doses.
General anaesthesia: Beta-blockers result in a reduction of reflex tachycardia and an increased risk of hypotension. Continuation of treatment with beta-blockers reduces the risk of arrhythmias, myocardial ischaemia and hypertensive episodes. It is advisable to inform the anaesthetist that the patient is being treated with beta-blockers.
If the discontinuation of treatment is deemed necessary, a 48-hours interruption is considered sufficient to restore catecholamine sensitivity.
Beta-blocker treatment may not be interrupted in certain cases: In patients with coronary insufficiency, it is advisable to continue treatment until the intervention, given the risks involved with the sudden withdrawal of beta-blockers.
In case of emergency or the possibility of stopping treatment, the patient should be protected from a predominant vagal reaction by sufficient premedication with atropine, repeated as necessary. The anaesthetist should use products with as little myocardial depressant effects as possible and blood loss should be compensated for.
The anaphylactic risk should be taken into account.
Thyrotoxicosis: Beta-blockers may mask the cardiovascular signs.
Athletes: Athletes should take note of the fact that this product contains an active substance which may induce a positive reaction in tests performed during anti-doping controls.
Also it should be noted that systemic effects of oral and ophthalmic administered beta-blockers are additive.
Use in Pregnancy: Betaxolol crosses the placenta barrier. The drug was found to cause foetal abnormalities in animals when administered in doses up to 600 times the maximum recommended human dose. Since there are no well-controlled studies in pregnant women, betaxolol should no be administered during pregnancy unless the potential benefits outweigh the hazard to the foetus.
Use in Lactation: Betaxolol is excreted to milk. Since hypotension or bradycardia may appear to the nursing infant, discontinuation of breastfeeding is advisable.
Neonatal aspect: In neonates of treated mothers, the beta-blocking action persists for several days after birth. Though this residual effect may have no clinical consequence, it is nevertheless possible that cardiac failure may occur. This would require hospitalisation in intensive care, in which replacement fluids should be avoided (risk of acute pulmonary oedema). In addition, bradycardia, respiratory distress and hypoglycaemia have been reported, therefore careful monitoring of the neonate (cardiac rate and serum glucose during the first 3 to 5 days of life) is recommended in a specialised setting.
Use In Pregnancy & Lactation
Pregnancy: Betaxolol crosses the placenta barrier. The drug was found to cause foetal abnormalities in animals when administered in doses up to 600 times the maximum recommended human dose. Since there are no well-controlled studies in pregnant women, betaxolol should no be administered during pregnancy unless the potential benefits outweigh the hazard to the foetus.
Lactation: Betaxolol is excreted to milk. Since hypotension or bradycardia may appear to the nursing infant, discontinuation of breastfeeding is advisable.
Neonatal aspect: In neonates of treated mothers, the beta-blocking action persists for several days after birth. Though this residual effect may have no clinical consequence, it is nevertheless possible that cardiac failure may occur. This would require hospitalisation in intensive care, in which replacement fluids should be avoided (risk of acute pulmonary oedema). In addition, bradycardia, respiratory distress and hypoglycaemia have been reported, therefore careful monitoring of the neonate (cardiac rate and serum glucose during the first 3 to 5 days of life) is recommended in a specialised setting.
Adverse Reactions
The most commonly reported: Asthenia; cool extremities; bradycardia, possibly severe; digestive disorders (gastralgias, nausea, vomiting); impotence; insomnia.
Much more infrequent: Slowing of atrioventricular conduction or worsening of pre-existing atrioventricular block; cardiac insufficiency; drop in blood pressure; bronchospasm; hypoglycaemia; Raynaud's phenomenon; aggravation of pre-existing intermittent claudication; various cutaneous manifestation, including psoriasis-like rashes or psoriasis exacerbation; paresthesia; eye dryness; nightmares.
Drug Interactions
Numerous medicines can induce bradycardia. These include beta-blockers, class Ia antiarrhythmics (quinidine, disopyramide), amiodarone and sotalol in the class III antiarrhythmis, diltiazem and verapamil in the class IV antiarrhythmics, and digitalis glycosides, clonidine, guafancine, mefloquine and anticholinesterase agents indicated in the treatment of Alzheimer's disease.
Contraindicated combinations: Floctafenine: In case of shock or hypotension due to floctafenine, there is a reduction of the compensatory cardiovascular reactions by beta-blockers.
Sultopride: Automatism disorders (excessive bradycardia) due to additive bradycardiac effects.
Inadvisable combinations: Calcium antagonists (bepridil, diltiazem and verapamil): Automatism disorders (excessive bradycardia, sinus arrest), sinoatrial and atrioventricular conduction disturbances and cardiac failure (synergistic effects). Such a combination should only be carried out under close clinical and electrocardiographic monitoring, particularly in elderly patients or at the start of treatment.
Amiodarone: Contractility, automatism and conduction disorders (suppression of the compensatory sympathetic mechanisms).
Combinations requiring precautions for use: Volatile halogenated anaesthetics: Reduction of compensatory cardiovascular reactions by beta-blockers (the beta-adrenergic inhibition may be alleviated during the intervention with beta-stimulants). As a general rule, do not discontinue beta-blocker treatment, and in any case, do not withdraw it abruptly. Inform the anaesthetist of this treatment.
Medicines which may cause torsades de pointes (apart from sultopride): Class Ia (quinidine, hydroquinidine, disopyramide) and class III (amiodarone, dofetilide, sotalol) antiarrhythmics, some phenothiazine neuroleptics (chlorpromazine, cyamemazine, levopromazine, thioridazine), benzamides (amisulpride, sulpride, tiapride), butyrophenone (droperidol, haloperidol), other neuroliptics (pimozide), and other medicines (cisapride, diphemanil, erythromycin IV, halofantrine, mizolastine, moxifloxacin, pentamidine, spiramycin IV, vincamine IV).
Increased risk of ventricular rhythm disturbances, particularly torsades de pointes (hypokalemia is a contributing factor).
Clinical and electrocardiographic monitoring.
Propafenone: Contractility, automatism and conduction disorders (suppression of compensatory sympathetic mechanisms).
Clinical and electrocardiographic monitoring.
Baclofen: Increased antihypertensive effect.
Blood pressure monitoring and dosage adjustment of the antihypertensive agent, if necessary.
Insulin, sulfonylurea hypoglycaemic agents: All beta-blockers may mask certain symptoms of hypoglycaemia, particularly palpitations and tachycardia.
Instruct the patient and reinforce self-monitoring of blood glucose, especially at the start of treatment.
Anticholinesterase agents (ambenomium, donepezil, galantamine, neostigmine, pyridostigmine, rivastigmine, tacrine): Risk of excessive bradycardia (additive bradycardia effects).
Regular clinical monitoring is needed.
Centrally-acting antihypertensive agents (clonidine, apraclonidine, alphamethyldopa, guanfancine, moxonidine, rilmenidine): Significant blood pressure increase in case of sudden withdrawal of the centrally-acting antihypertensive treatment.
Avoid sudden withdrawal of the central antihypertensive treatment.
Clinical monitoring is needed.
Lidocaine by IV route: Increased plasma levels of lidocaine with possible increase of adverse neurological and cardiac effects (reduced hepatic clearance of lidocaine).
Clinical and electrocardiographic monitoring of lidocaine plasma concentrations while receiving the combination and after discontinuation of the beta-blocker.
Adjustment, if necessary of the lidocaine dosage.
Iodine contrast media: In case of shock or hypotension due to iodine contrast media, beta-blockers induce a reduction of the cardiovascular compensatory reactions.
The beta-blocker therapy must be discontinued whenever possible prior to radiological investigation. If continuation of the treatment is essential, the physician must have appropriate resuscitation methods at his/her disposal.
Combinations to be taken into account: NSAIDS (systemic route), including selective COX-2 inhibitors: Reductions of the antihypertensive effect (inhibition of vasodilating prostaglandins by the NSAIDS and sodium and water retention with the pyrazole NSAIDS).
Calcium antagonists (dihydropyridine): Hypotension, cardiac deficiency in patients with latent or uncontrolled cardiac insufficiency. The beta-blocker may also minimise the reflex sympathetic response which occurs in case of excessive hemodynamic alterations.
Imipramine antidepressants, neuroliptics: Increase in antihypertensive effect and risk of orthostatic hypotension (additive effect).
Corticosteroids, tetracosactide: Diminished antihypertensive effect (water and sodium retention of corticosteroids).
Mefloquine: Risk of bradycardia (additive bradycardia effects).
Dipyridamole (IV route): Increased antihypertensive effect.
Alpha-blockers, for urological use (alfuzocin, doxazosin, prazosin, tamsulosin, terazosin): Increased antihypertensive effect.
Storage
Store in a dry place at room temperature (15 to 25°C) protected from light.
Shelf Life: 36 months after the production date.
MIMS Class
ATC Classification
C07AB05 - betaxolol ; Belongs to the class of selective beta-blocking agents. Used in the treatment of cardiovascular diseases.
Presentation/Packing
Tab 20 mg x 3 x 10's.
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