Betalmic ES (Drops) Instructions for Use

Marketing Authorization Holder

Unimed Pharma, s.r.o. (Slovakia)

ATC Code

S01ED02 (Betaxolol)

Active Substance

Betaxolol (Rec.INN registered by WHO)

Dosage Form

Betalmic ES

Eye drops 0.5%: dropper bottle 5 ml or 10 ml

Dosage Form, Packaging, and Composition

Excipients: benzalkonium chloride, disodium edetate, sodium hydroxide, sodium chloride, water.

5 ml – polyethylene dropper bottles (1) – cardboard packs.
10 ml – polyethylene dropper bottles (1) – cardboard packs.

Clinical-Pharmacological Group

Antiglaucoma drug – beta-adrenoblocker

Pharmacotherapeutic Group

Antiglaucoma agent – beta-adrenergic blocking agent

Pharmacological Action

An 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.

Maintain a consistent dosing schedule, approximately every 12 hours.

Stabilization of intraocular pressure in some patients may occur over several weeks.

Monitor intraocular pressure during the first month of treatment to assess therapeutic response.

If using other topical ophthalmic medications, administer them at least 10 minutes apart.

To minimize systemic absorption, apply gentle pressure to the lacrimal sac at the inner corner of the eye for 1-2 minutes after instillation.

Avoid allowing the dropper tip to contact the eye, eyelids, or any other surface.

Replace the bottle cap immediately after use.

Do not exceed the prescribed dosage.

Adverse Reactions

Eye disorders very common – eye discomfort; common – blurred vision, increased lacrimation; uncommon – punctate keratitis, keratitis, conjunctivitis, blepharitis, vision disorders, 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.

Nervous system disorders common – headache; rare – syncope; frequency unknown – dizziness.

Cardiac disorders: uncommon – bradycardia, tachycardia; rare – arterial hypotension; frequency unknown – arrhythmia.

Respiratory, thoracic and mediastinal disorders uncommon: bronchospasm, dyspnea, rhinitis; rare – cough, rhinorrhea.

Gastrointestinal disorders uncommon – nausea; rare – dysgeusia.

Skin and subcutaneous tissue disorders rare – dermatitis, rash, alopecia.

Reproductive system and breast disorders rare – decreased libido.

Psychiatric disorders rare – anxiety, insomnia, depression.

Immune system disorders frequency unknown – hypersensitivity.

General disorders and administration site conditions frequency unknown – asthenia.

Contraindications

Hypersensitivity to betaxolol, sinus bradycardia; sinoatrial block; second- and third-degree AV block 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-blockers, Raynaud’s syndrome, pheochromocytoma, bronchial asthma, chronic obstructive bronchitis, first-degree AV block, 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 minimum available concentration in the minimum effective dose.

Geriatric Use

Used in elderly patients as indicated.

Special Precautions

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

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

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

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

Caution should be exercised when prescribing beta-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 cannot be ruled out.

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

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

Betoptic has minimal effect on blood pressure and heart rate. However, caution should be exercised when prescribing it to patients with first-degree AV block or heart failure. Treatment should be discontinued at the first signs of cardiovascular system decompensation.

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 minimum available concentration in the minimum effective dose. Monitoring for ocular and systemic side effects within 1-2 hours after the first instillation is necessary.

Effect on ability to drive vehicles and operate machinery

Patients in whom the instillation of the medicinal product temporarily reduces visual clarity are not recommended to engage in activities requiring increased attention and reaction 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 stores (such as reserpine), an increase in effects such as decreased blood pressure and bradycardia may be observed.

With simultaneous use of betaxolol and oral beta-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.