Betaxolol - instructions for use, dose, side effects, contraindications

The drug is a cardioselective beta₁-adrenoceptor without internal sympathomimetic activity. Has a weak membrane-stabilizing activity. Has hypotensive effect, associated with a decrease in the minute volume of the heart and a decrease in sympathetic stimulation of peripheral vessels. When used in therapeutic doses, it does not have cardiodepressive action,does not affect the exchange of glucose, does not reduce the bronchodilating action of beta-adrenomimetics, does not cause a delay in the body of sodium ions. It lasts a long time.

When topical application in the form of eye drops reduces the increased intraocular pressure. Resorptive effect is not significant.

Pharmacokinetics:

After ingestion, more than 95% of the dose of betaxolol is rapidly absorbed from the digestive tract. C_max the active substance in the blood plasma is reached in 1-2 hours. It is exposed to the effect of "first passage" through the liver. The binding to plasma proteins is about 50%. V_d - about 6 l / kg.

The half-life of betaxolol is 15-20 hours. It is excreted by the kidneys mainly in the form of metabolites, 10-15% in unchanged form.

Indications:

For systemic use: arterial hypertension.

For topical application in ophthalmology: chronic open-angle glaucoma, increased intraocular pressure, condition after laser trabeculoplasty.

ICD-10

VII.H40-H42.H40.0 Suspicion of glaucoma

VII.H40-H42.H40.1 Primary open angle glaucoma

IX.I10-I15.I10 Essential [primary] hypertension

Contraindications:

Cardiogenic shock, severe forms of chronic heart failure, AV blockade II and III degree, syndrome of weakness of the sinus node, sinoatrial blockade, sinus bradycardia, severe peripheral circulatory disturbances, hypersensitivity to betaxolol.

Carefully:

Impact on the ability to drive vehicles and manage mechanisms

They are used with caution in patients whose activity requires increased attention and rapid psychomotor reactions.

Pregnancy and lactation:

Category by FDA - FROM.

The drug is contraindicated for use in pregnancy and lactation.

Dosing and Administration:

For systemic administration for ingestion - 20 mg once a day. For patients who are on permanent hemodialysis or peritoneal dialysis, the initial dose is 10 mg per day; The time of taking betaxolol is set regardless of the mode of dialysis sessions.

For topical application in ophthalmology - 1 drop 2 times a day in the affected eye. During the first month, therapy is carried out under the control of the level of intraocular pressure, in the future the frequency of measurement of intraocular pressure is determined individually. In the case of using betaxolol after previous treatment with another similar preparation, the dosing regimen is set individually.

Side effects:

From the cardiovascular system: at the beginning of treatment - AV-blockade, sinus bradycardia, arterial hypotension, heart failure, Raynaud's syndrome.

From the digestive system: rarely - pain in the abdomen, nausea, vomiting.

From the side of the central nervous system and the peripheral nervous system: at the beginning of treatment - asthenia, paresthesia of the limbs, sleep disorders, depression, drowsiness, dizziness.

From the respiratory system: rarely - bronchospasm.

Allergic reactions: rarely - psoriasis-like skin manifestations.

Local reactions: when applied in the form of eye drops immediately after instillation, short-term discomfort in the eyes, sometimes tearing, is possible; rarely - a decrease in the sensitivity of the cornea, erythema, pruritus, spotted corneal stain, keratitis, anisocoria, photophobia.

Overdose:

Treatment is symptomatic. No cases of drug overdose have been recorded.

Interaction:

With simultaneous use with adrenomimetics, xanthine derivatives decreases the effectiveness of betaxolol.

When used simultaneously with antacids and antidiarrhoeic agents, it is possible to reduce the absorption of beta-blockers.

With simultaneous use with antihypertensive drugs, antihypertensive effect is enhanced.

With the simultaneous use of halogen containing agents for inhalation anesthesia, an increase in the negative inotropic effect is possible.

With the simultaneous use of nondepolarizing muscle relaxants, it is possible to increase their duration of action.

With the simultaneous use of non-steroidal anti-inflammatory drugs, glucocorticosteroids decreases the antihypertensive effect of betaxolol.

With the simultaneous use of cardiac glycosides, bradycardia may be strengthened.

With the simultaneous use of tricyclic antidepressants (imipramine), lowers blood pressure, there is a risk of developing orthostatic hypotension.

With the simultaneous use of amiodarone, verapamil, diltiazem, beta-adrenoblokatorov for topical application in glaucoma may increase the negative inotropic action and conduction disorders.

With the simultaneous use of lidocaine, the concentration of lidocaine in the blood plasma increases.

When used simultaneously with drugs that deplete the stores of catecholamines (including reserpine), it is possible to intensify the hypotensive effect and bradycardia.

With simultaneous use with sulfasalazine increases the concentration of betaxolol in the blood plasma.

Special instructions:

It is not recommended for bronchial asthma, chronic bronchitis with bronchial obstructive syndrome. They are used with caution in diabetes mellitus, suspected thyrotoxicosis, with a history of bronchial hyperreactivity, in patients with type I AV blockade, Reynaud's syndrome, and pheochromocytoma. When administered internally with liver failure, as well as with renal failure (creatinine clearance less than 20 ml per minute), there is no need to adjust the dosage regimen, however, regular clinical observation is recommended for the first few days of treatment. In the first days of treatment, the possibility of symptoms of heart failure in predisposing patients should be considered. The abolition of betaxolol should be carried out gradually, especially in patients suffering from coronary heart disease, angina pectoris.

Betaxolol does not affect the size of the pupil, so with closed-angle glaucoma, the drug should be used only in combination with miotics. When transferring the patient to betaxolol after treatment with several antiglaucoma drugs, the latter is canceled gradually, in a period of not less than 1 week per drug.

With the simultaneous use of betaxolol in the form of eye drops and beta-adrenoblockers inside, it is possible to develop additive effects on both the intraocular pressure side and the manifestations of the systemic action of beta-blockers.

Before the planned operation, beta-blockers, including betaxolol, should be canceled.

When topical application of betaxolol should not wear contact lenses.

It is not recommended to apply betaxolol in children.

Instructions

Betaxolol (Betaxololum)