Glucovis

Approved Indications:

A. Ophthalmic Use (Betaxolol 0.25% or 0.5% eye drops):

• Primary open-angle glaucoma
• Ocular hypertension

Used to lower intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension, either alone or in combination with other IOP-lowering medications (e.g., prostaglandin analogs, alpha-agonists, carbonic anhydrase inhibitors).

B. Oral Use (Betaxolol 10–20 mg tablets):

• Hypertension (mild to moderate)
• Angina pectoris (chronic stable angina)

Off-label / Clinically Accepted Uses:

• Migraine prophylaxis
• Hypertrophic cardiomyopathy (symptomatic relief)
• Arrhythmias (less preferred than other beta-blockers)
• Anxiety symptoms (adjunctive use) – rare and limited evidence
• Tremor – non-selective beta-blockers like propranolol preferred, but selective agents like betaxolol may be used in special cases

A. Ophthalmic (Eye Drops):

Adults (including elderly):

• Instill 1 drop of 0.25% or 0.5% solution in the affected eye(s) twice daily.
• May be used in combination with other ocular hypotensives.
• Wait at least 5 minutes between different ophthalmic agents.

Children (>2 years):

• Safety and efficacy not well established; use only if prescribed by a specialist.

Renal/Hepatic Impairment:

• Use with caution; systemic absorption may occur with ocular use, though minimal.

Administration Instructions:

• Avoid touching the dropper tip to any surface.
• Apply pressure to the nasolacrimal duct (punctal occlusion) for 1–2 minutes to reduce systemic absorption.

B. Oral (Tablets):

Adults:

• Initial dose: 10 mg orally once daily
• Maintenance: 10–20 mg once daily, adjusted based on clinical response.
• Max dose: 40 mg/day (in divided doses)

Elderly:

• Start at lower end of dosing range (e.g., 5–10 mg daily), monitor for bradycardia or hypotension.

Renal Impairment:

• CrCl < 20 mL/min: Consider dose reduction to 5 mg/day due to decreased clearance.

Hepatic Impairment:

• Use with caution; monitor closely, especially during dose titration.

Betaxolol hydrochloride is a selective beta-1 adrenergic receptor blocker. In the eye, it reduces intraocular pressure by decreasing aqueous humor production by the ciliary epithelium in the anterior chamber. Systemically, when administered orally, it reduces myocardial contractility, heart rate, and cardiac output, which leads to reduced blood pressure and oxygen demand. Unlike non-selective beta-blockers, betaxolol has minimal beta-2 activity, making it safer in patients with reactive airway disease.

Oral Formulation:

• Absorption: Well absorbed (≥ 90%) after oral administration
• Bioavailability: ~85%
• Time to Peak Concentration: 1–3 hours (oral); ~0.5–1 hour (ocular)
• Distribution: Widely distributed; crosses the blood-brain barrier; low plasma protein binding (~50%)
• Metabolism: Primarily hepatic (CYP450-independent pathways)
• Active Metabolites: None clinically significant
• Elimination: Renal (mainly unchanged); ~15% fecal excretion
• Half-life: ~14–22 hours (oral), allowing once-daily dosing
• Ophthalmic Absorption: Limited systemic absorption through conjunctiva and nasolacrimal ducts

• Pregnancy:
• Former FDA Category C
• Use only if clearly needed. Beta-blockers may cause fetal bradycardia, hypoglycemia, or growth restriction, especially during late pregnancy.
• Lactation:
• Excreted into breast milk in small amounts.
• May cause bradycardia, hypotension, or respiratory depression in infants.
• Caution is advised, especially with oral formulations. Ophthalmic forms are considered lower risk.

• Primary Class: Beta-Adrenergic Blocker
• Subclass: Cardioselective (Beta-1 Selective) Beta-Blocker
• Use Type: Antiglaucoma agent (ophthalmic), Antihypertensive/Antianginal agent (oral)

• Hypersensitivity to betaxolol or any formulation component
• Sinus bradycardia
• Second- or third-degree atrioventricular (AV) block (unless a functioning pacemaker is present)
• Cardiogenic shock
• Overt cardiac failure
• Severe peripheral arterial disease (oral)
• Sick sinus syndrome
• Concurrent use with IV calcium channel blockers (e.g., verapamil, diltiazem) without supervision

• Bronchospastic disease: Though beta-1 selective, may still cause bronchospasm in asthmatics—use cautiously.
• Diabetes: May mask symptoms of hypoglycemia (e.g., tachycardia); monitor closely.
• Thyrotoxicosis: May mask tachycardia—caution during withdrawal.
• Renal impairment: Dose reduction may be necessary (oral).
• Depression: May worsen existing symptoms.
• Discontinuation: Avoid abrupt withdrawal, especially in coronary artery disease—taper gradually over 1–2 weeks.
• Ophthalmic Use: May still cause systemic effects like bradycardia or hypotension in sensitive individuals.

A. Ophthalmic Use:

Common:

• Eye irritation
• Transient burning or stinging
• Blurred vision
• Dry eyes
• Tearing

Less Common:

• Bradycardia (rare systemic absorption)
• Fatigue
• Headache
• Conjunctivitis

Rare/Serious:

• Bronchospasm
• Hypotension
• Depression
• Heart block

B. Oral Use:

Cardiovascular:

• Bradycardia
• Hypotension
• AV block
• Worsening of heart failure

Central Nervous System:

• Dizziness
• Fatigue
• Depression
• Insomnia

Respiratory:

• Dyspnea (rare)
• Bronchospasm (mainly in predisposed individuals)

Gastrointestinal:

• Nausea
• Diarrhea

Timing: Most side effects occur within the first 1–2 weeks of treatment and may resolve or stabilize thereafter.

Major Interactions:

• Calcium Channel Blockers (Verapamil, Diltiazem): Additive effects on AV conduction, risk of bradycardia and heart block
• Clonidine: Enhanced rebound hypertension on withdrawal
• Antiarrhythmics (e.g., amiodarone, digoxin): Increased risk of bradyarrhythmia
• Insulin and oral antidiabetics: May mask hypoglycemia symptoms
• CYP450 Interactions: Minimal (not significantly metabolized by CYP enzymes)

Alcohol: May enhance hypotensive effects.

Food: No significant food interactions known; can be taken with or without meals.

• Glaucoma guidelines (e.g., AAO, NICE) continue to recommend beta-blockers like betaxolol as second-line agents after prostaglandin analogs for IOP reduction.
• American Heart Association (AHA) reaffirms use of selective beta-blockers like betaxolol in hypertensive patients with stable angina and airway sensitivity, though atenolol or bisoprolol are more commonly preferred.
• Recent labeling updates emphasize cautious use in patients with asthma or diabetes, even with cardioselective agents.

• Tablets:
• Store at 20°C to 25°C (68°F to 77°F)
• Protect from light and moisture
• Keep in a tightly closed container
• Eye Drops:
• Store at 2°C to 25°C (36°F to 77°F)
• Protect from light
• Do not freeze
• Discard 4 weeks after opening (unless otherwise stated)
• Shake gently before use if suspension