Universal reference book for medicines

Active substance: betaxolol

Type: anti-glaucoma preparation - beta-blocker

Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..

Cardioselective beta- 1- adrenoblocker 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 glucose metabolism, 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.
After ingestion, more than 95% of the dose of betaxolol is rapidly absorbed from the digestive tract.
C max of the active substance in the blood plasma is achieved 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.
T 1/2 Betaxolol is 15-20 hours. It is excreted by the kidneys mainly in the form of metabolites, 10-15% in unchanged form.

For systemic use: as a monotherapy and as part of a combination therapy - arterial hypertension, prevention of angina pectoris attacks.

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

For systemic use when ingestion - 20 mg 1 time / day.
For patients who are on permanent hemodialysis or peritoneal dialysis, the initial dose is 10 mg / day; The time of taking betaxolol is set regardless of the mode of dialysis sessions.
For topical application in ophthalmology - 1 drop 2 times / 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.
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 central nervous system and peripheral nervous system: at the beginning of treatment - asthenia, paresthesia of 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.
Cardiogenic shock;
acute heart failure, chronic heart failure in the stage of decompensation, not compensated as a result of treatment with diuretics, inotropic drugs, ACE inhibitors, other vasodilators; AV-blockade II and III degree (without the installed artificial pacemaker); angina prinzmetal (contraindicated monotherapy); SSSU, sinoatrial blockade; pronounced bradycardia (heart rate less than 45-50 beats per minute); severe peripheral circulatory disorders, severe forms of bronchial asthma and COPD; severe forms of Raynaud's disease and obliterating diseases of peripheral arteries; pheochromocytoma without simultaneous administration of alpha-blockers;arterial hypotension (systolic blood pressure <100 mm Hg); anaphylactic reactions in the anamnesis; metabolic acidosis; cardiomegaly (no signs of heart failure);simultaneous application with sultopride and floktaphenin; simultaneous administration of MAO inhibitors; children and adolescents under 18; increased sensitivity to betaxolol.
During pregnancy and during lactation (breastfeeding), the use of betaxolol is possible only in cases where the intended benefit to the mother exceeds the possible risk to the fetus or child.

When used internally with renal failure (CC less than 20 ml / min), there is no need to adjust the dosage regimen, however, regular clinical observation is recommended during the first few days of treatment.

When administered internally with liver failure, there is no need to adjust the dosage regimen, however, regular clinical observation is recommended during the first few days of treatment.

Betaxolol in children is not recommended.

With caution should be used for bronchial asthma and COPD of a moderate course (start treatment with small doses and preferably under the control of indicators of the function of external respiration, thanks to the beta 1- selectivity of betaxolol in the event of an attack of bronchial asthma on the background of its admission, it is possible to stop the attack with beta 2 -adrenomimetics);
with chronic heart failure in the compensation stage (treatment with betaxolol is possible only under strict medical supervision, treatment should be started from very small doses with a gradual increase); with AV-blockade I degree (requires close monitoring, including ECG monitoring); with obliterating diseases of peripheral arteries, Reynaud's syndrome (with the exception of severe form) (peripheral circulatory disorders may be increased); with Prinzmetal angina (there may be an increase in angina attacks, the use of a selective beta 1 -adrenoconvertor is possible only with the simultaneous use of vasodilators); with a treated pheochromocytoma (careful monitoring of BP indications is required); in elderly patients (treatment with small doses should be started and under careful medical supervision); with renal insufficiency (with QC more than 20 ml / min - careful monitoring of the patient during the first few days of treatment, with a CC less than 20 ml / min and / or hemodialysis requires a correction of the dosing regimen); with liver failure (requires more thorough clinical observation at the beginning of treatment); in patients with diabetes mellitus (regular monitoring of blood glucose concentration, including active self-control by the patient, at the beginning of treatment, it is possible to reduce the severity of precursors of hypoglycemia such as tachycardia, palpitations and increased sweating); at a psoriasis (beta-adrenoblockers can worsen a course of a psoriasis); with desensitizing therapy.
The abolition of betaxolol should be carried out gradually, especially in patients with IHD, angina.

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 gradually phased out, at least 1 week into the 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, incl.
betaxolol, should be discarded.
When topical application of betaxolol should not wear contact lenses.

Betaxolol in children is not recommended.

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.

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 NSAIDs, GCS 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), blood pressure decreases, 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 with 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.

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