Betaxolol (Drops) Instructions for Use

ATC Code

S01ED02 (Betaxolol)

Active Substance

Betaxolol (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Antiglaucoma drug – beta-adrenoblocker

Pharmacotherapeutic Group

Drugs used in ophthalmology; antiglaucoma drugs and miotic agents; beta-adrenergic blockers

Pharmacological Action

Antiglaucoma agent, a selective beta₁-adrenergic blocker without intrinsic sympathomimetic activity. It does not possess membrane-stabilizing (local anesthetic) action.

When applied topically, Betaxolol reduces both elevated and normal intraocular pressure, due to a decrease in the production of intraocular fluid. The onset of the hypotensive effect is usually observed 30 minutes after topical application, and the maximum reduction in ophthalmotonus occurs approximately 2 hours later. After a single instillation, the effect on ophthalmotonus persists for 12 hours.

Betaxolol does not cause miosis, accommodation spasm, or hemeralopia (unlike miotics).

Pharmacokinetics

Betaxolol is highly lipophilic, resulting in good penetration through the cornea into the anterior chamber of the eye; C_max in the anterior chamber is determined 20 minutes after instillation. With topical application, systemic absorption is low, plasma concentration is below the detection threshold (2 ng/ml). Plasma protein binding is 50%. T_1/2 is 14-22 hours. It is excreted by the kidneys (15% unchanged). Permeability through the blood-brain barrier and placental barrier is low; secretion into breast milk is insignificant.

Indications

Ocular hypertension; chronic open-angle glaucoma; angle-closure glaucoma (in combination with miotics).

ICD codes

Dosage Regimen

Instill one drop into the conjunctival sac of the affected eye(s) twice daily, approximately every 12 hours.

Do not exceed the recommended dosage. If using other topical ophthalmic agents, administer them at least 10 minutes apart to prevent dilution and ensure adequate absorption.

Stabilization of intraocular pressure may require several weeks of therapy. Monitor intraocular pressure during the first month of treatment to assess therapeutic response.

Prior to administration, remove contact lenses if worn. You may reinsert lenses 15 minutes after instillation.

To administer, tilt your head back, pull down the lower eyelid, and apply the drop without allowing the dropper tip to contact the eye or any other surface. Close your eye gently for 1-2 minutes and apply light pressure to the nasolacrimal duct (inner corner of the eye) to minimize systemic absorption.

If a dose is missed, apply it as soon as possible. However, if it is almost time for the next dose, skip the missed dose and continue with the regular schedule. Do not double the dose.

Adverse Reactions

From the organ of vision Very common – eye discomfort; Common – blurred vision, increased lacrimation; Uncommon – punctate keratitis, keratitis, conjunctivitis, blepharitis, visual disturbances, photophobia, eye pain, dry eye syndrome, asthenopia, blepharospasm, eye itching, eye discharge, crusting on eyelid edges, eye irritation, conjunctival disorders, conjunctival edema, eye hyperemia; Rare – cataract, decreased corneal sensitivity, eyelid redness.

From the nervous system Common – headache; Rare – syncope; Frequency unknown – dizziness.

From the cardiovascular system : Uncommon – bradycardia, tachycardia; Rare – arterial hypotension; Frequency unknown – arrhythmia.

From the respiratory system Uncommon: bronchospasm, dyspnea, rhinitis; Rare – cough, rhinorrhea.

From the digestive system Uncommon – nausea; Rare – dysgeusia.

From the skin and subcutaneous tissues Rare – dermatitis, rash, alopecia.

From the reproductive system Rare – decreased libido.

Mental disorders Rare – anxiety, insomnia, depression.

From the immune system Frequency unknown – hypersensitivity.

General reactions Frequency unknown – asthenia.

Contraindications

Hypersensitivity to betaxolol, sinus bradycardia; sinoatrial block; AV block II and III degree without a pacemaker; sick sinus syndrome; cardiogenic shock; decompensated chronic heart failure; severe forms of COPD; severe forms of bronchial asthma (including history).

With caution

Diabetes mellitus, thyrotoxicosis, concurrent use of oral beta-adrenergic blockers, Raynaud’s syndrome, pheochromocytoma, bronchial asthma, chronic obstructive bronchitis, AV block I degree, heart failure.

Use in Pregnancy and Lactation

Use during pregnancy and lactation (breastfeeding) is possible only if the intended benefit to the mother outweighs the potential risk to the fetus or child.

Pediatric Use

According to limited data, Betaxolol may be recommended for reducing intraocular pressure in true congenital glaucoma, infantile and juvenile congenital glaucoma in the preoperative period or in case of ineffective surgical treatment. Before using betaxolol, the risks and benefits of using betaxolol in the pediatric population should be carefully assessed by taking a thorough history regarding systemic disorders. If the benefit outweighs the risk, it is recommended to use Betaxolol at the lowest available concentration in the minimum effective dose.

Geriatric Use

Used in elderly patients as indicated.

Special Precautions

Beta-adrenergic blockers should be prescribed with caution to patients prone to hypoglycemia, as these drugs may mask the symptoms of acute hypoglycemia.

Beta-adrenergic blockers may mask some symptoms of hyperthyroidism (e.g., tachycardia). In patients suspected of having thyrotoxicosis, beta-adrenergic blockers should not be abruptly discontinued, as this may exacerbate symptoms.

Beta-adrenergic blockers may cause symptoms similar to those of myasthenia (e.g., diplopia, ptosis, general weakness).

Before planned surgery, beta-adrenergic blockers should be gradually (not abruptly) discontinued 48 hours before general anesthesia, because during general anesthesia they may reduce myocardial sensitivity to sympathetic stimulation necessary for heart function.

Caution should be exercised when prescribing beta-adrenergic blockers to patients with significantly reduced respiratory function. Although clinical studies have shown no effect of betaxolol on external respiratory function, the possibility of increased sensitivity to this agent should not be excluded.

Patients taking beta-adrenergic blockers may have a history of atopy or anaphylactic reactions. In case of repeated reactions, such patients may not be sensitive to the usual doses of adrenaline necessary to stop anaphylaxis.

When instilled, Betaxolol can enter the systemic circulation. Thus, the same side effects as with IV and parenteral use of beta-adrenergic blockers may be observed.

Betoptima has minimal effect on BP and HR. However, caution should be exercised when prescribing it to patients with AV block I degree or heart failure. Treatment should be discontinued at the first signs of decompensation of the cardiovascular system.

According to limited data, Betaxolol may be recommended for reducing intraocular pressure in true congenital glaucoma, infantile and juvenile congenital glaucoma in the preoperative period or in case of ineffective surgical treatment. Before using betaxolol, the risks and benefits of using betaxolol in the pediatric population should be carefully assessed by taking a thorough history regarding systemic disorders. If the benefit outweighs the risk, it is recommended to use Betaxolol at the lowest available concentration in the minimum effective dose. Monitoring for ocular and systemic side effects within 1-2 hours after the first instillation is necessary.

Influence on the ability to drive vehicles and operate machinery

Patients in whom the clarity of vision is temporarily reduced after instillation of the drug are not recommended to engage in activities requiring increased attention and rapid reactions until it is restored.

Drug Interactions

With simultaneous use of betaxolol and adrenaline solution for ophthalmic application, mydriasis may develop in some cases.

When using betaxolol in combination with drugs that deplete catecholamine reserves (such as reserpine), an increase in effects such as decreased BP and bradycardia may be observed.

With simultaneous use of betaxolol and oral beta-adrenergic blockers, the risk of adverse effects (both local and systemic) increases due to an additive effect.

Caution should be exercised when using betaxolol in ophthalmology concomitantly with adrenergic psychotropic agents due to a possible enhancement of their action.

With simultaneous administration of muscle relaxants and hypoglycemic agents, an enhancement of their action may be observed.

When used concomitantly with sympathomimetics, an enhancement of their vasoconstrictive effect is noted.

If necessary, ophthalmic preparations containing Betaxolol can be used in combination with other topical ophthalmic preparations. In this case, the interval between their applications should be at least 10 minutes.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

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.