Betaxolol

Betaxololum

For medical students2 min readUpdated 2026-10-10

Betaxolol is a long-acting lipophilic agent used both systemically in cardiology and topically in ophthalmology. A distinctive feature of the substance is its high bioavailability and complete absence of the first-pass hepatic effect.

Half-life14–22 hours

Bioavailability80–90%

Eye dropsTrade name «Betoptic»

Metabolism85% is biotransformed in the liver into inactive metabolites

Pharmacokinetic Features in Systemic Administration

Being a pronounced lipophilic compound, Betaxololum is almost completely absorbed in the gastrointestinal tract. Importantly, concomitant food intake does not alter its absorption parameters, making the therapy regimen more convenient for the patient.

A key pharmacokinetic feature of the drug is the absence of the first-pass effect through the liver. Due to this, its bioavailability reaches high values of 80–90%. Elimination occurs primarily via hepatic metabolism (about 85% of the substance is converted into inactive metabolites), after which these metabolites are excreted by the kidneys.

The drug is classified as a long-acting agent: the clinical effect lasts up to 36 hours, and the half-life ($t_{1/2}$) ranges from 14 to 22 hours. However, in patients with concomitant hepatic or renal impairment, this period naturally lengthens, necessitating mandatory adjustment of the therapeutic dose.

Application in Cardiology

Systemic administration of betaxolol (orally) is indicated for several cardiovascular pathologies. In clinical practice, it is used to treat:

Essential hypertension (to achieve stable control of blood pressure levels);
Angina pectoris;
Tachyarrhythmias.

Due to its long half-life, the drug is prescribed in a convenient once-daily regimen, which improves patient adherence to treatment.

Betaxolol in Ophthalmology

In addition to cardiology, the drug has found wide application in the treatment of eye diseases. For these purposes, a special dosage form is produced: eye drops (known under the trade name «Betoptic»).

getMain indication for topical use is open-angle glaucoma. Instillation of the solution into the conjunctival sac effectively reduces intraocular pressure. The pharmacodynamic effect after a single instillation persists for 12 hours.

Adverse Reactions and Risks

Using eye drops may cause several side effects, which are generally divided into local and systemic.

Local reactions include:

Burning sensation and eye pain;
Itching and conjunctival hyperemia;
Development of allergic conjunctivitis.

Resorptive (systemic) effects occur if the drug is absorbed from the mucous membrane of the eye into the systemic circulation. In this case, classic beta-blocker effects can be observed: bradycardia and arterial hypotension.

Special attention should be paid to patients with a history of allergies and pulmonary disorders: in the presence of bronchial asthma, the resorptive action of betaxolol carries a high risk of triggering life-threatening bronchospasm.

Mnemonic

To remember the pharmacokinetics, recall the rule of the three Ps: Complete absorption, Peak (near 100%) bioavailability, and Pass-through of the liver (no first-pass effect).

Frequently asked questions

To which pharmacological group does betaxolol belong?

Betaxolol belongs to the pharmacological group of cardioselective $\beta_1$-blockers. In generational classifications, it is categorized as a second-generation drug.

Cardioselective — selective blockers of $\beta_1$-receptors.

Additionally, the drug is characterized as lipophilic, possesses weak membrane-stabilizing activity, and is a long-acting agent. The cardioselectivity ratio is 25/1.

What is the mechanism of intraocular pressure reduction with betaxolol?

The mechanism of intraocular pressure reduction with betaxolol involves decreasing the production of aqueous humor. This effect is achieved through the drug's action on the ciliary epithelium, which leads to reduced fluid secretion. This property allows the drug to be used as eye drops for the treatment of open-angle glaucoma.

How does betaxolol differ from non-selective beta-blockers in ophthalmology?

Betaxolol differs in ophthalmology by being a cardioselective $\beta_1$-blocker and is listed among the drugs of choice for glaucoma. Non-selective propranolol blocks both $\beta_1$- and $\beta_2$-receptors and is not used in glaucoma because it exhibits pronounced local anesthetic activity and carries a risk of corneal damage.

Characteristic	Betaxolol	Propranolol
Selectivity	Cardioselective $\beta_1$-blocker	Non-selective $\beta_1, \beta_2$-blocker
Glaucoma use	Drug of choice	Not used
Reason for restriction	Not specified in sources	Pronounced local anesthetic activity, risk of corneal damage

Does food intake affect the absorption of betaxolol?

No, the lipophilic structure of the drug allows it to be almost completely absorbed in the GI tract regardless of food intake.

How often should betaxolol tablets be taken?

Due to its prolonged action (effect lasting up to 36 hours), the drug is taken orally once daily.

Why can blood pressure drop when using eye drops?

This is due to the resorptive effect: when the drug is absorbed from the conjunctival sac into the bloodstream, its systemic actions (hypotension, bradycardia) manifest.

Go deeper

Mechanism of intraocular pressure reduction in open-angle glaucoma
Principles of dose adjustment in renal and hepatic impairment
Pathogenesis of bronchospasm development due to resorptive effects of eye drops
Differences between betaxolol and other drugs used for tachyarrhythmias