Betac (Tablets) Instructions for Use

Marketing Authorization Holder

Medochemie, Ltd. (Cyprus)

Contact Information

MEDOCHEMIE Ltd. (Cyprus)

ATC Code

C07AB05 (Betaxolol)

Active Substance

Betaxolol (Rec.INN registered by WHO)

Dosage Form

Betac

Film-coated tablets, 20 mg: 30 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets white or almost white, round, biconvex, with a score on one side; the core on the fracture is white or almost white.

Excipients: lactose monohydrate, microcrystalline cellulose, sodium starch glycolate, colloidal anhydrous silica, magnesium stearate, hypromellose, titanium dioxide, polyethylene glycol 400.

10 pcs. – blister packs (3) – cardboard packs.

Clinical-Pharmacological Group

Beta₁-adrenoblocker

Pharmacotherapeutic Group

Selective beta1-adrenergic blocker

Pharmacological Action

Cardioselective beta₁-adrenergic blocker without intrinsic sympathomimetic activity. It has weak membrane-stabilizing activity.

It exerts an antihypertensive effect due to a reduction in cardiac output and a decrease in sympathetic stimulation of peripheral vessels.

When used in therapeutic doses, the drug does not have a pronounced cardiodepressant effect, does not affect glucose metabolism, does not reduce the bronchodilator effect of beta-adrenergic agonists, and does not cause sodium and water retention in the body.

The onset of action of the drug occurs within 1-2 hours, and the duration of action is 24 hours.

The antihypertensive effect occurs after 2-5 days, with the maximum effect developing after 1-2 months.

Pharmacokinetics

Absorption

After oral administration, it is completely absorbed from the gastrointestinal tract (100%). Bioavailability is up to 90%. C_max is reached after 2-4 hours.

Distribution

It binds to blood proteins by 55%. V_d – from 4.9 to 9.8 L/kg.

It penetrates the blood-brain barrier and placental barrier insignificantly and is excreted in breast milk to a small extent.

Elimination

T_1/2 is 14-22 hours. It is excreted in the urine (15% unchanged). Clearance is 4.7 ml/min and increases with age.

Indications

• Arterial hypertension;
• Coronary artery disease: stable and unstable angina pectoris, myocardial infarction (as part of combination therapy);
• Hypertrophic cardiomyopathy;
• Cardiac arrhythmias (sinus tachycardia, supraventricular and ventricular tachyarrhythmia and extrasystole, arrhythmias against the background of mitral valve prolapse, thyrotoxicosis).

ICD codes

Dosage Regimen

Take Betac once daily, with water, without regard to meals.

For arterial hypertension, initiate therapy at 5-10 mg once daily. After 1-2 weeks, if the therapeutic response is inadequate, increase the dose to a maximum of 20 mg once daily.

For stable angina pectoris, the usual maintenance dose is 20 mg once daily. Initiate treatment at a lower dose and titrate upward based on clinical response.

For cardiac arrhythmias (supraventricular and ventricular tachyarrhythmias, extrasystole), the dosage is 10-20 mg once daily. Adjust the dose based on heart rate control and tolerability.

In patients with hypertrophic cardiomyopathy, the recommended dose is 20 mg once daily.

For elderly patients, initiate treatment at the lower end of the dosage range ( 5 mg). Monitor closely and titrate cautiously due to potential for age-related changes in pharmacokinetics.

Do not crush or chew the tablets; they can be divided at the score line for dose adjustment.

Monitor heart rate and blood pressure regularly during therapy. Reduce the dose or discontinue if significant bradycardia occurs.

When discontinuing long-term therapy, gradually reduce the dose over 1-2 weeks (e.g., decrease by 5 mg every 3-4 days) to avoid acute withdrawal syndrome.

Adverse Reactions

From the cardiovascular system: bradycardia, AV block, heart failure, orthostatic hypotension, worsening of peripheral circulation (cold extremities, paresthesia, Raynaud’s syndrome).

From the respiratory system: bronchospasm.

Allergic reactions: skin rash, urticaria.

From the central nervous system: asthenia, depression, increased fatigue, drowsiness, confusion, hallucinations, dizziness, headache.

From the digestive system: nausea; rarely – vomiting, diarrhea or constipation, cholestasis.

From the organ of vision: dry eyes.

From the hematopoietic system: leukopenia, thrombocytopenia.

Other: exacerbation of psoriasis, impotence.

Contraindications

• Chronic heart failure stage II-III;
• Cardiogenic shock;
• AV block grade II or III;
• Sinoatrial block;
• Bradycardia;
• Prinzmetal’s angina;
• Cardiomegaly;
• Arterial hypotension (systolic BP less than 100 mm Hg);
• Diabetes mellitus;
• Myasthenia gravis;
• Psoriasis;
• Raynaud’s syndrome;
• Obliterating endarteritis;
• Severe renal impairment;
• Bronchial asthma;
• Pulmonary emphysema;
• Chronic obstructive bronchitis;
• Hypersensitivity to betaxolol and other components of the drug.

Use in Pregnancy and Lactation

The use of Betac during pregnancy and lactation (breastfeeding) is possible with caution and only if the potential benefit of its use to the mother outweighs the possible risk to the fetus.

Use in Renal Impairment

The drug is contraindicated in severe renal impairment.

Pediatric Use

The use of the drug in children is not recommended.

Special Precautions

The drug should be used with caution in pheochromocytoma.

If planned surgical treatment is necessary, the drug should be discontinued 48 hours before the start of general anesthesia.

The possibility of developing heart failure in the first days of treatment with Betac should be considered in patients with a corresponding predisposition.

Betaxolol may mask the symptoms of hypoglycemia (e.g., tachycardia), so when used in patients with diabetes mellitus, blood glucose levels should be monitored regularly.

Betac should be used under heart rate control. If bradycardia develops, the dose should be reduced or the drug discontinued.

When discontinuing therapy with Betac, a gradual dose reduction (by 5 mg every 3-4 days) over 1-2 weeks is recommended to avoid withdrawal syndrome.

It is not recommended to prescribe the drug concurrently with MAO inhibitors.

Use in pediatrics

The use of the drug in children is not recommended.

Effect on the ability to drive vehicles and operate machinery

The drug should be prescribed with caution to patients whose activities require increased attention and rapid psychomotor reactions.

Overdose

Symptoms: bradycardia, AV block, drop in blood pressure, fainting, heart failure, bronchospasm, convulsions.

Treatment: symptomatic. For AV block, intravenous administration of atropine, alupent or epinephrine (adrenaline), temporary pacemaker is indicated. For arterial hypotension, if there are no signs of pulmonary edema, intravenous drip infusion of plasma substitutes is recommended; if ineffective – epinephrine (adrenaline), dopamine, dobutamine. In case of bronchospasm – inhaled beta₂-adrenergic agonists; for convulsions – diazepam.

Drug Interactions

Concomitant use of Betac with amiodarone, calcium channel blockers (verapamil, diltiazem) and beta-blockers used as eye drops for glaucoma may enhance the inhibitory effect of betaxolol on myocardial contractility and cardiac conduction.

Concomitant use of Betac with cardiac glycosides increases the likelihood of AV block development.

Antihypertensive agents, when used concomitantly with Betac, enhance its hypotensive effect.

Concomitant use of Betac with drugs for inhalation anesthesia increases the risk of myocardial function depression and arterial hypotension development. The duration of action of non-depolarizing muscle relaxants may increase against the background of simultaneous Betac intake.

NSAIDs, when used concomitantly, weaken the hypotensive effect of Betac due to sodium and water retention and inhibition of prostaglandin synthesis in the kidneys. Estrogens also reduce the hypotensive effect of Betac (due to sodium retention).

Cocaine, when used concomitantly, may reduce the therapeutic effects of betaxolol.

With combined use of Betac and adrenomimetics or xanthines, their therapeutic effects are mutually weakened.

Concomitant use of phenothiazines with Betac leads to an increase in the plasma concentration of each of the drugs.

Betaxolol slows down the elimination of lidocaine and theophylline.

Sulfasalazine increases the serum level of betaxolol.

Storage Conditions

The drug should be stored in a dry, light-protected place, out of the reach of children, at a temperature not exceeding 25°C (77°F).

Shelf Life

The shelf life is 2 years.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.