Betaxolol is a selective Beta-1 receptor blocker that is used to treat patients with hypertension (Beta-blockers are used as alternative agents for the treatment of hypertension). It is also used as off-label in the treatment of the following conditions:

• Acute Myocardial infarction
• For rate control in Atrial fibrillation
• Chronic stable angina
• For the prevention of Postoperative atrial fibrillation associated with cardiac surgery.

Betaxolol Dose in Adults

Betaxolol dosage as off label use in the treatment of Atrial fibrillation for rate control:

• 20 mg once a day.
• It may be used in combination with digoxin.

Betaxolol dose as Off label use in the treatment of chronic stable angina:

• 20 mg once a day.

Betaxolol dose as an alternative agent in Hypertension:

• 5 to 10 mg once a day.
• The dose is titrated every one to two weeks if required based on the patients' response.
• The maximum dose is 20 mg once a day.

Betaxolol dose as Off label use in the prevention of postoperative atrial fibrillation associated with cardiac surgery:

• 20 mg once a day.

Dose in children:

It is not recommended for use in children.

Betaxolol Pregnancy Risk Factor C

• Betaxolol crosses over the placental barriers and can be detected in neonatal blood or urine.
• Betaxolol can cause lasting effects in the neonate for up to seven days after delivery.
• Neonatals may experience hypoglycemia and bradycardia. Monitor neonates for three to five days
• Uncontrolled hypertension can also be associated with maternal preeclampsia and neonatal adverse effects.
• Beta-blockers can be used when indicated to treat hypertension during pregnancy. However, it is best to use other preferred agents as first-line.

Use during breastfeeding:

• Breastfeeding mothers should use betaxolol with caution, as it is excreted through breastmilk and can have beta-blocking effect on the baby.

Dose in patients with renal impairment:

• Severe impairment:

  • 5 mg once a day initially.
  • The dosage may be increased every 2 weeks up to a maximum of 20 mg once a day.

• Hemodialysis:

  • 5 mg once a day.
  • The dose may be increased every 2 weeks up to a maximum of 20 mg once a day.

Dose in patients with liver disease:

Adjustment in the dose is not required.

Side Effects of Betaxolol:

• Cardiovascular:

  • Bradycardia
  • Chest Pain
  • Cold Extremities
  • Palpitations
  • Edema

• Central Nervous System:

  • Fatigue
  • Insomnia
  • Lethargy
  • Paresthesia

• Gastrointestinal:

  • Nausea
  • Dyspepsia
  • Diarrhea

• Hematologic & Oncologic:

  • Positive ANA Titer

• Neuromuscular & Skeletal:

  • Arthralgia

• Respiratory:

  • Dyspnea
  • Pharyngitis

Contraindication to Betaxolol include:

• Allergy reactions to betaxolol and any component of the formulation
• Sinus bradycardia
• Heart block of second or third degree
• Cardiogenic shock
• Cardiac failure

Warnings and precautions

• Anaphylactic reactions
  • Patients who have had anaphylaxis in the past should be cautious.
  • Patients using beta-blockers may be less sensitive to the effects of epinephrine if anaphylaxis develops.

• Bronchospastic Disease:

  • In severe bronchospasm, beta-blockers should be avoided.
  • Betaxolol, a selective Beta-1-blocker, can be used in low doses (between 5 and 10 mg) for mild bronchospasm. It is also available in divided doses.

• Cerebrovascular Insufficiency

  • Cerebrovascular Insufficiency patients should be cautious when taking the drug. Hypotension and bradycardia can further decrease cerebral blood flow.

• Conductive abnormality

  • Consider pre-existing conditions that have reduced heart rate or contractility, such as sick sinus syndrome, before you start the treatment.

• Diabetes:

  • Patients with diabetes should not take beta-blockers as they can mask hypoglycemia symptoms.

• Heart failure:

  • In patients with symptomatic heart disease, beta-blockers should not be used.
  • It should not be used in compensated heart failure. Instead, you should use other beta-blockers like bisoprolol or carvedilol.

• Myasthenia gravis:

  • Beta-blockers can be used to increase myasthenia-related muscle weakness, including diplopia or ptosis.
  • Patients with myasthenia Gravis should use it with caution.

• Raynaud and peripheral vascular disease (PVD).

  • Patients suffering from Raynaud’s disease or peripheral arterial disease should be cautious when taking the drug.
  • It is important to monitor the clinical signs and progression of peripheral arterial disease.

• Pheochromocytoma:

  • Patients with pheochromocytoma need to have adequate alpha-blockade before they can use a beta-blocker.

• Angina Prinzmetal version:

  • Patients suffering from prinzmetal angina should not use Beta-blockers that do not block alpha1-adrenergic receptor activity.
  • The presence of unopposed alpha1 receptors can cause coronary vasoconstriction, which can lead to worsening of anginal symptoms.

• Psoriasis:

  • Use of beta-blockers may make psoriasis worse.

• Renal impairment

  • Patients with impaired renal function should be cautious and adjust the dosage.

• Thyroid disease:

  • Hyperthyroidism may be disguised by beta-blockers.
  • Avoid abrupt withdrawal from beta-blockers as it can cause a thyroid storm.

Betaxolol (systemic): Drug Interaction

Note: Drug Interaction Categories:

• Risk Factor C: Monitor When Using Combination
• Risk Factor D: Consider Treatment Modification
• Risk Factor X: Avoid Concomitant Use

Monitoring parameters while using Betaxolol:

• Montor Blood pressure, pulse, and renal functions

Target Blood pressure:

• Target blood pressure of less than 130/80 mmHg in patients with hypertension and known cardiovascular disease or the 10-year ASCVD risk is greater than 10%.

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• The target blood pressure of less than 130/80 mmHg may be reasonable in patients with ASCVD risk.

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• Target blood pressure of less than 140/90 mmHg in patients aged 18 – 65 years with Diabetes and hypertension without cardiovascular disease and the 10-year ASCVD risk is less than 15%.

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• Target blood pressure of less than 130/80 mmHg in patients aged 18 – 65 years with Diabetes, hypertension, cardiovascular disease, or the 10-year ASCVD risk is greater than 15%.

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• Target blood pressure of less than 140/90 mmHg in patients aged more than 65 years and without major comorbid conditions.

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• Target blood pressure of less than 150/90 mmHg in patients aged more than 65 years and poor health or comorbid conditions.

How to take Betaxolol?

It may be taken with or without meals as its absorption is not affected by food.

Mechanism of action of Betaxolol:

• It blocks beta-1 receptors in a competitive manner, but has minimal or no effect on beta-2.
•  It takes approximately 1 to 1.5 hours for it to take effect.
• The drug can be taken orally and almost all of it (100%) is eliminated. 

It is 50% protein-bound and metabolized by your liver to multiple metabolites.

It has a bioavailability rate of 89% and a half life elimination time of 14 to 22 hours. 

Patients with renal and liver disease have a longer half-life.

It takes approximately 1.5 to 6 hours to reach peak serum concentration. 

The drug excreted in this form is more than 80%.

Betaxolol Brand Names (International):

• Beof
• Bertocil
• Betac
• Betakor
• Betarun
• Betasel S
• Betaxen
• Betaxol
• Betoptima
• Betoquin
• Bexolo
• Daberol
• Kerlon
• Kerlone
• Lokren
• Optibet
• Optipres
• Presmin
• Vistagan

Betaxolol Brand Names in Pakistan: