Betaxolol

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Betaxolol: instructions for use and reviews

1. Release form and composition
2. Pharmacological properties
3. Indications for use
4. Contraindications
5. Method of application and dosage
6. Side effects
7. Overdose
8. Special instructions
9. Application during pregnancy and lactation
10. Use in childhood
11. In case of impaired renal function
12. For violations of liver function
13. Use in the elderly
14. Drug interactions
15. Analogs
16. Terms and conditions of storage
17. Terms of dispensing from pharmacies
18. Reviews
19. Price in pharmacies

Latin name: Betaxolol

ATX code: S01ED02, C07AB05

Active ingredient: betaxolol (betaxolol)

Manufacturer: Moscow Endocrine Plant (Russia)

Description and photo update: 2019-19-08

Prices in pharmacies: from 85 rubles.

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Betaxolol is a beta-blocker used to treat hypertension (oral administration) and as an antiglaucoma agent to lower intraocular pressure (topical application).

Release form and composition

Dosage forms of Betaxolol release:

film-coated tablets: almost white or white, round, biconvex, scored; the core in the cut is almost white or white (10 pcs. in blisters, 1-3, 5 or 10 packs in a cardboard box);
eye drops: transparent, colorless or slightly yellowish (1.5, 2 or 5 ml each in polymer tube-droppers, 1, 2, 4, 5 or 10 tube-droppers in a cardboard box; 5 or 10 ml each in polymer bottles -droppers, 1 or 2 dropper bottles in a cardboard box; 5 or 10 ml in bottles, 1 bottle in a cardboard box).

Composition of 1 tablet:

active substance: betaxolol hydrochloride - 20 mg;
auxiliary components: aerosil (colloidal silicon dioxide) - 1.2 mg; lactose monohydrate (milk sugar) - 128.1 mg; sodium carboxymethyl starch (primogel) - 7.4 mg; microcrystalline cellulose - 85.8 mg; magnesium stearate - 2.5 mg;
shell: Opadry II white 85F18422 (titanium dioxide - 1.25 mg; polyethylene glycol - 1.01 mg; polyvinyl alcohol - 2 mg; talc - 0.74 mg).

Composition of 1 ml drops:

active substance: betaxolol - 5 mg (in the form of betaxolol hydrochloride - 5.6 mg);
auxiliary components: sodium chloride - 8 mg; disodium edetate dihydrate (ethylenediaminetetraacetic acid disodium salt dihydrate) - 0.1 mg; benzethonium chloride - 0.1 mg; 1 M hydrochloric acid or 1 M sodium hydroxide - up to pH 6.0–7.8; purified water - up to 1 ml.

Pharmacological properties

Pharmacodynamics

When taken orally, betaxolol has a cardioselective β-adrenergic blocking effect on the body. In higher therapeutic doses, a weak membrane stabilizing effect is observed (similar to local anesthetics or quinidine). Betaxolol is characterized by the absence of partial agonist activity (that is, it does not exhibit its own sympathomimetic action).

The selective effect of the drug on β ₁ -adrenergic receptors is not considered absolute, since when taking betaxolol in high concentrations, it is possible to affect β ₂ -adrenergic receptors, mainly located in the smooth muscles of blood vessels and bronchi (such an effect is significantly weaker in comparison with the effect of non-selective β-adrenergic blockers on β ₂ -adrenergic receptors).

The activity of betaxolol, which blocks β ₁ -adrenergic receptors, is manifested by a number of the following pharmacodynamic effects:

a decrease in the number of heart contractions during exercise and at rest (provided by the blockade of β-adrenergic receptors in the sinus node and the lack of internal sympathomimetic activity of betaxolol, which together slows down the automatism of the sinus node);
decrease in cardiac output during exercise and at rest (provided by competitive antagonism with catecholamines in peripheral adrenergic nerve endings);
lowering diastolic and systolic blood pressure during exercise and at rest (the mechanism of hypotensive action is described below);
decreased orthostatic tachycardia reflex.

The result of these effects is a reduction in the stress on the heart during exercise and at rest. The mechanism of hypotensive action is not fully understood. Presumably, β-blockers act on the body as follows:

reduce cardiac output;
eliminate spasm of peripheral arteries (as a result of central action, providing a decrease in sympathetic impulses to the periphery, and inhibition of renin activity).

With prolonged use of betaxolol, its hypotensive effect does not decrease. In the case of a single dose of betaxolol at a dose of 5–40 mg per day, the hypotensive effect is the same 3-4 hours after application (the time to reach the maximum concentration in the blood) and 1 day later (before taking the next dose).

In the case of taking betaxolol at doses of 5 and 10 mg, the hypotensive effect of the drug, respectively, is 50% and 80% of the hypotensive effect provided when using betaxolol at a dose of 20 mg. In the dose range from 5 to 20 mg, the hypotensive effect is dose-dependent, and with an increase in the dose from 10 mg to 20 mg, the increase in the hypotensive effect is insignificant. With an increase in the dose of betaxolol from 20 to 40 mg, the hypotensive effect changes slightly. For each dose of betaxolol, the maximum hypotensive effect is achieved after 1–2 weeks.

The effect of reducing the number of heart contractions, in contrast to the hypotensive effect of betaxolol, does not increase with increasing doses (from 10 to 40 mg).

Along with this, taking betaxolol can slow down the conduction of the atrioventricular node.

When applied topically in the form of eye drops, betaxolol lowers intraocular pressure by reducing the production of intraocular fluid. Unlike the use of other β-blockers, taking the drug does not lead to a decrease in blood flow in the optic nerve. Betaxolol does not cause contraction of the ciliary muscle (spasm of accommodation) and circular muscle (miosis), hemeralopia, the effect of the appearance of a "veil" before the eyes.

The hypotensive effect is manifested 30 minutes after instillation, and the maximum effect - after 2 hours. The effect of the drug on ophthalmotonus persists for 12 hours after a single instillation.

Pharmacokinetics

After oral administration, betaxolol is completely (100%) and rapidly absorbed from the gastrointestinal tract. Bioavailability is about 85%. The time to reach maximum plasma concentrations is 2–4 hours. The connection with blood plasma proteins is about 50%.

The drug is characterized by low permeability through the placental and blood-brain barriers and insignificant excretion in breast milk.

It is metabolized in the liver to inactive metabolites. The volume of distribution is approximately 6 l / kg. Moderate fat solubility is characteristic.

More than 80% is excreted as metabolites by the kidneys. From 10 to 15% of the drug is excreted unchanged. The half-life of betaxolol is 15–20 hours. With impaired liver function, the half-life is extended by 33% with a constant clearance. In case of impaired renal function, the half-life is doubled (dose reduction is required).

It is not removed during hemodialysis.

When applied topically, there is a possibility of systemic absorption of betaxolol. The resorptive effect is negligible. Approximately 50% binds to plasma proteins. The half-life is from 14 to 22 hours. It is excreted by the kidneys (unchanged - 15%).

Indications for use

Pills

arterial hypertension;
attacks of exertional angina (prevention).

Eye drops

Betaxolol is prescribed to reduce intraocular pressure in the treatment of the following diseases (monotherapy or as part of a combination treatment):

open-angle glaucoma;
ocular hypertension.

Contraindications

Pills

Absolute:

cardiogenic shock;
atrioventricular block II and III degree (without connecting an artificial pacemaker);
burdened history of anaphylactic reactions;
sick sinus syndrome (including sinoatrial blockade);
pheochromocytoma (without combined use with α-blockers);
arterial hypotension (with systolic blood pressure less than 90 mm Hg. Art.);
severe bradycardia (less than 50 beats / min);
acute heart failure, chronic heart failure in the stage of decompensation, in which inotropic therapy is required;
metabolic acidosis;
Prinzmetal's angina;
severe peripheral circulatory disorders;
congenital galactosemia, galactose / glucose malabsorption syndrome or lactase deficiency (Betaxolol contains lactose);
cardiomegaly (no signs of heart failure);
bronchial asthma and chronic obstructive pulmonary disease, occurring in severe forms;
combined use with floktaphenin, sultopride, monoamine oxidase inhibitors;
simultaneous intravenous administration of slow calcium channel blockers such as diltiazem and verapamil and other antiarrhythmic drugs (for example, disopyramide, amiodarone, etc.);
age up to 18 years (the safety profile for this group of patients has not been studied);
lactation period (the safety profile for this group of patients has not been studied);
hypersensitivity to the components of the drug, as well as other beta-blockers.

Relative (Betaxolol tablets are prescribed with caution in the presence of the following diseases / conditions):

burdened history of allergic reactions;
diabetes;
psoriasis;
obliterating diseases of peripheral vessels (intermittent claudication, Raynaud's syndrome);
liver failure;
thyrotoxicosis;
impaired renal function;
myasthenia gravis;
hemodialysis;
atrioventricular block I degree;
chronic heart failure;
emphysema of the lungs;
chronic obstructive pulmonary disease (bronchial asthma);
depression (current / history);
desensitizing therapy;
elderly age;
pregnancy (the appointment of Betaxolol is possible after assessing the ratio of benefits to risks).

Eye drops

Absolute:

myasthenia gravis;
cardiogenic shock;
bronchial asthma;
arterial hypotension;
severe obstructive respiratory failure;
sinus bradycardia (less than 45-50 beats / min);
atrioventricular block II – III degree;
sick sinus syndrome;
chronic heart failure in severe course;
age up to 18 years;
hypersensitivity to drug components.

Relative (Betaxolol eye drops are prescribed with caution in the presence of the following diseases / conditions):

hypoglycemia;
pheochromocytoma;
Raynaud's syndrome;
unstable angina;
chronic obstructive pulmonary disease;
tendency to develop bradycardia;
atrioventricular block I degree;
diabetes mellitus in the stage of decompensation;
violation of peripheral circulation;
functional disorders of the kidneys / liver;
myasthenia gravis;
thyrotoxicosis;
elderly age;
pregnancy and lactation period (the appointment of Betaxolol is possible after assessing the ratio of benefits to risks).

Instructions for the use of Betaxolol: method and dosage

Pills

Betaxolol tablets are taken orally with a sufficient amount of liquid, the tablets should not be chewed.

Daily dose: initial - 10 mg, maintenance - 20 mg.

In case of liver failure, Betaxolol is prescribed in a standard initial dose, however, at the beginning of the course, regular medical supervision is required.

Features of use for renal failure (depending on the severity of the course):

mild / moderate: adjustment of the initial dose is not required, at the beginning of therapy, regular medical monitoring should be carried out;
severe (with creatinine clearance less than 20 ml / min): the initial dose is not higher than 10 mg, the maximum per day is 20 mg.

Eye drops

Betaxolol eye drops are applied topically (in the conjunctival sac).

Dosage regimen: 2 times a day, 1 drop.

The first month of therapy should be carried out under the control of intraocular pressure.

Side effects

Pills

Possible violations (> 10% - very often;> 1% and 0.1% and 0.01% and <0.1% - rarely; <0.01%, taking into account individual reports - very rare):

endocrine system: very rarely - hypothyroid state, hyperglycemia in patients with type 2 diabetes mellitus, hypoglycemia in patients receiving insulin;
central nervous system: often - weakness, increased fatigue, nightmares, dizziness, insomnia or drowsiness, headache; rarely, depression; very rarely - muscle weakness, short-term memory loss or confusion, anxiety, hallucinations, asthenic syndrome, paresthesia in the limbs (with intermittent claudication, Raynaud's syndrome), tremor;
digestive system: often - abdominal pain, nausea, vomiting, diarrhea or constipation; rarely - dryness of the oral mucosa, changes in taste, functional disorders of the liver (dark urine, yellowness of the skin or sclera, cholestasis);
cardiovascular system: often - a feeling of palpitations, sinus bradycardia, orthostatic hypotension, myocardial conduction disturbance, atrioventricular block (up to cardiac arrest), weakening of myocardial contractility, arrhythmias; rarely - a pronounced decrease in blood pressure, the development (or aggravation) of symptoms of heart failure (in the form of swelling of the feet, ankles, legs), chest pain, manifestation of angiospasm (in the form of a decrease in peripheral blood circulation, cooling of the lower extremities, Raynaud's syndrome);
respiratory system: rarely - nasal congestion, shortness of breath (develops when high doses are prescribed due to loss of selectivity or in the presence of a predisposition), broncho- and laryngospasm;
skin: rarely - exanthema, increased sweating, psoriasis-like skin reactions, skin flushing, exacerbation of the course of psoriasis;
organ of vision: rarely - soreness and dryness of the eyes, decreased secretion of the lacrimal glands, conjunctivitis; very rarely - visual impairment;
allergic reactions: rarely - itching, skin rash, urticaria;
laboratory indicators: in rare cases - an increase in the titer of antinuclear antibodies, which in exceptional cases may be accompanied by clinical manifestations such as systemic lupus erythematosus (is transient);
effect on the fetus: hypoglycemia, intrauterine growth retardation, bradycardia;
others: weakening of libido, back pain, decreased potency, arthralgia, withdrawal syndrome (in the form of increased angina attacks, increased blood pressure).

Eye drops

During the use of Betaxolol, the following sensory disturbances may develop: often - short-term discomfort in the eyes after instillation, lacrimation; rarely - photophobia, decreased sensitivity of the cornea, allergic reactions, anisocoria, photophobia, redness of the eyes, punctate keratitis, itching, feeling of dry eyes.

In rare cases, during therapy, the development of systemic side effects may occur:

respiratory system: shortness of breath, respiratory failure, bronchospasm;
central nervous system: depression, insomnia, dizziness, drowsiness, nausea, headache, increased symptoms of myasthenia gravis;
cardiovascular system: cardiac conduction disorders, bradycardia, heart failure.

Overdose

Symptoms: dizziness, severe bradycardia, atrioventricular block, severe lowering of blood pressure, ventricular premature beats, arrhythmias, heart failure, fainting, shortness of breath, bronchospasm, convulsions, cyanosis of the palms and fingernails.

Treatment: gastric lavage, intake of adsorbing agents. With the development of bradycardia, the following measures are recommended: intravenous atropine at a dose of 1–2 mg, and then (if necessary) the appointment of a slow infusion of isoprenaline at a dose of 0.025 mg or dobutamine infusion at a dose of 0.0025–0.01 mg / kg / min.

In some cases, with bradycardia, an artificial pacemaker is temporarily placed.

In the case of a pronounced decrease in blood pressure, intravenous administration of vasopressor drugs and plasma-substituting solutions is indicated.

In bronchospasm, it is recommended to prescribe bronchodilators, including aminophylline and / or β ₂ -adrenomimetics.

In case of heart failure in newborns (provided that the mother takes beta-blockers during pregnancy), hospitalization is carried out in the intensive care unit, and long-term use of isoprenaline and dobutamine in high doses is recommended under the supervision of a specialist.

When applied topically, if an excessive amount of the drug gets into the eyes, they should be rinsed with warm water.

special instructions

Pills

When treating patients with angina pectoris, Betaxolol cannot be abruptly canceled, since this can lead to the development of severe cardiac arrhythmias, myocardial infarction or sudden death (dose reduction should be carried out for 1-2 weeks, in order to avoid disease progression, simultaneous replacement therapy is possible).

Monitoring the patient's condition should include monitoring blood pressure, heart rate, in diabetes mellitus - the concentration of glucose in the blood, in elderly patients - renal function.

The patient should be familiar with the method of counting the number of heartbeats, if this figure is less than 50 beats / min, you should consult your doctor.

Before conducting studies of the content in urine and blood of catecholamines, vanillin mandelic acid, normetanephrine, as well as titers of antinuclear antibodies, Betaxolol must be canceled.

Ethanol should not be taken during therapy.

The active substance of the drug can give a positive reaction during doping control tests, which must be taken into account when prescribing Betaxolol to athletes.

The effectiveness of Betaxolol in smoking is reduced.

In newborns whose mothers used the drug, its effect persists for several days after birth. This residual effect may not have clinical consequences, but in some cases a heart defect may develop, requiring intensive neonatal care.

During the period of treatment, the amount of tear fluid may decrease, which should be taken into account by patients who use contact lenses.

During the period of use of Betaxolol, patients need to be careful when driving and performing other potentially dangerous work.

Eye drops

Betaxolol does not affect the size of the pupil; for angle-closure glaucoma, it should only be used in combination with miotics.

It should be borne in mind that the drug can cause symptoms similar to those in myasthenia gravis (ptosis, diplopia, general weakness).

Betaxolol has a minimal effect on heart rate and blood pressure, but care should be taken when prescribing the drug to patients with heart failure or atrioventricular block. In cases of the appearance of the first symptoms of decompensation from the cardiovascular system, the drug is canceled.

Due to the preservatives included in Betaxolol, which can be deposited in soft contact lenses, they should be removed before using the drops, they can be reinstalled no earlier than 20 minutes after the procedure.

With the development of a temporary decrease in vision clarity after instillation of Betaxolol until it is fully restored, it is not recommended to drive a car and engage in activities that require an increased response and attention.

Application during pregnancy and lactation

When conducting experiments on animals, the teratogenic effect of Betaxolol was not found. Teratogenic effects in humans have not yet been recorded, and congenital malformations have not been identified in controlled prospective studies.

Use during pregnancy is allowed only if the perceived risk to the child is lower than the potential benefit to the mother.

β-blockers are excreted in breast milk. The risk of developing bradycardia and hypoglycemia has not been investigated, therefore, breastfeeding should be discontinued during the treatment period.

Pediatric use

According to the instructions, Betaxolol is not allowed to be used to treat patients under the age of 18.

With impaired renal function

In case of impaired renal function, the drug should be used with caution.

For violations of liver function

In case of impaired liver function, the drug should be used with caution.

Use in the elderly

When treating elderly patients, Betaxolol should be used with caution.

Drug interactions

Pills

Contraindicated combinations:

floktaphenin: a decrease in compensatory cardiovascular reactions in shock or arterial hypotension caused by floktaphenin;
sultopride: development of severe bradycardia (additive effect).

Combinations not recommended:

reserpine, α-methyldopa, guanfacine, cardiac glycosides: development of severe bradycardia, impaired automatism;
fingolimod: an increase in the likelihood of increased bradycardia;
sympathomimetics: development of interaction;
amiodarone: development of violations of contractility, conduction and automatism;
adrenaline (epinephrine): weakening of its action;
antacids: decrease in absorption, and, as a consequence, the hypotensive effect of Betaxolol;
iodine-containing drugs: reduction of compensatory cardiovascular reactions (before performing X-ray studies using iodine-containing contrast agents, Betaxolol therapy is recommended to be canceled if possible).

Combinations requiring careful use:

drugs such as verapamil, mibefradil and diltiazem: an increase in the likelihood of developing cardiac automatism disorders (in the form of severe bradycardia, stopping the sinus node), atrioventricular conduction disorders, heart failure (the combination is possible only with careful electrocardiographic / clinical monitoring, especially in elderly patients);
drugs that can cause pirouette-type arrhythmias (with the exception of sultopride): an increase in the likelihood of developing ventricular arrhythmias (when the combination is prescribed, electrocardiographic / clinical monitoring must be performed);
inhalation halogen-containing anesthetics: reducing the hypotensive effect of Betaxolol;
baclofen: increased hypotensive effect (when prescribing a combination, it is necessary to monitor blood pressure with subsequent, if necessary, dose adjustment);
propafenone: violation of contractility, conductivity and automatism (when prescribing a combination, it is necessary to carry out electrocardiographic / clinical control);
cholinesterase inhibitors, including neostigmine, ambenomium, rivastigmine, donepezil, tacrine, galantamine, pyridostigmine: increased likelihood of increased bradycardia (additive action; regular clinical monitoring is necessary);
oral hypoglycemic agents and insulin: it is possible to mask some symptoms of hypoglycemia, for example, palpitations and tachycardia (the patient should exercise self-control over the concentration of glucose in the blood, especially at the beginning of the course);
lidocaine (as an antiarrhythmic agent, intravenous administration): an increase in its plasma concentration in the blood with a possible increase in undesirable neurological effects and symptoms from the cardiovascular system (it is recommended to conduct electrocardiographic / clinical observation and, possibly, to control the plasma concentration of lidocaine in the blood);
centrally acting antihypertensive drugs, including rilmenidine, clonidine, apraclonidine, moxonidine: a significant increase in blood pressure in case of abrupt withdrawal of these drugs (clinical monitoring is necessary; abrupt withdrawal should be avoided).

Combinations to be taken into account:

antipsychotics, tricyclic antidepressants (such as imipramine), α-blockers, including tamsulosin, prazosin, alfuzosin, doxazosin, terazosin: increased antihypertensive effect and increased likelihood of orthostatic hypotension (additive effect);
non-steroidal anti-inflammatory drugs (with systemic use, including selective inhibitors of cyclooxygenase): lowering the hypotensive effect;
dipyridamole (intravenous administration), amifostine: increased hypotensive effect;
mefloquine: increased likelihood of developing the risk of bradycardia (additive effect).

Other possible interactions:

xanthines (except diphylline): a decrease in their clearance and an increase in their plasma concentration in the blood, especially with an initially increased clearance of theophylline (for example, due to smoking);
phenytoin (intravenous administration): an increase in the severity of the cardiodepressant effect and the likelihood of a decrease in blood pressure;
nifedipine: a significant decrease in blood pressure;
estrogens: weakening of the hypotensive effect (due to sodium retention);
non-depolarizing muscle relaxants: prolonging their action;
sympatholytics, diuretics, hydralazine and other antihypertensive drugs: excessive lowering of blood pressure;
ethanol, drugs with sedative and hypnotic effects: increased depression of the central nervous system;
coumarins: prolongation of the anticoagulant effect;
non-hydrogenated ergot alkaloids: increased likelihood of peripheral circulatory disorders;
monoamine oxidase inhibitors: a significant increase in the hypotensive effect (the combination is not recommended, the interval between taking monoamine oxidase inhibitors and Betaxolol should be at least 14 days).

Eye drops

With the combined use of Betaxolol with certain drugs / substances, the following effects may develop:

drugs that inhibit the deposition of catecholamines (reserpine): the development of hypotension and bradycardia;
oral beta-blockers: an increase in the likelihood of developing an additive effect with the manifestation of systemic / local side effects (when prescribing a combination, careful medical supervision is required);
sympathomimetics: enhancing their vasoconstrictor effect;
muscle relaxants, hypoglycemic agents: enhancing their action;
adrenergic psychotropic drugs: enhancing their action (the combination requires caution).

Analogs

Betaxolol analogues are: Betalmik EC, Betak, Betoftan, Betoptik, Lokren, Xonef, Optibetol.

Terms and conditions of storage

Pills

Store in a dark, dry place at temperatures up to 25 ° C. Keep out of the reach of children.

The shelf life is 3 years.

Eye drops

Store in a dark place at temperatures up to 15 ° C (in dropper vials and tube droppers) or up to 25 ° C (in vials). Do not freeze. Keep out of the reach of children.

Expiration date (depending on packaging):

dropper tube, dropper bottles - 2 years;
bottles - 3 years.

After opening the package, Betaxolol can be used for 30 days.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Betaxolol

Reviews of Betaxolol in tablet form are predominantly positive: the drug reduces stress on the heart and allows you to effectively control blood pressure. Some users report the possibility of developing allergic responses in the first days of therapy (in predisposed patients), or dyspeptic reactions.

Reviews of eye drops are also positive: the drug is well tolerated and practically does not cause side effects.

The price of Betaxolol in pharmacies

The approximate price for Betaxolol is: 30 tablets of 20 mg each - 380 rubles, eye drops 0.5% 5 ml - 150 rubles.

Betaxolol: prices in online pharmacies

Drug name

Price

Pharmacy

Betaxolol 0.5% eye drops 5 ml 1 pc.

RUB 85

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Betaxolol cap. eye 0.5% fl. 5 ml

91 rbl.

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Maria Kulkes Medical journalist About the author

Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!