Betaxolol-Optic eye drops 0.5%, 5ml No. 1

• Chronic open-angle glaucoma

• increased intraocular pressure,

• condition after laser trabeculoplasty

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

Eye drops in the form of a transparent, colorless or light yellow liquid.

1 ml

betaxolol hydrochloride 5.6 mg,

which corresponds to the content of betaxolol 5 mg

Excipients: benzalkonium chloride - 0.1 mg, disodium edetate - 0.5 mg, sodium chloride - 8 mg, sodium hydroxide solution 1M / hydrochloric acid solution 1M - up to pH 4.0-8.0, purified water - up to 1 ml.

• Individual hypersensitivity to the components of the drug.

• Sinus bradycardia.

• AV block II and III degree.

• Cardiogenic shock.

• Severe heart failure.

• Children under the age of 18.

pharmachologic effect

Cardioselective beta1-blocker without intrinsic sympathomimetic activity. It has a weak membrane stabilizing activity. It has a hypotensive effect associated with a decrease in cardiac output and a decrease in sympathetic stimulation of peripheral vessels. When used in therapeutic doses, it does not have a cardiodepressant effect, does not affect glucose metabolism, does not reduce the bronchodilatory effect of beta-adrenergic agonists, does not cause a delay in the body of sodium ions. It has a long-term effect. When applied topically in the form of eye drops, it lowers increased intraocular pressure. The resorptive effect is insignificant.

Pharmacokinetics

After oral administration, more than 95% of the dose of betaxolol is rapidly absorbed from the gastrointestinal tract. Cmax of the active substance in blood plasma is reached after 1-2 hours. It is exposed to the effect of the 'first pass' through the liver. Plasma protein binding is about 50%. Vd - about 6 l / kg. T1 / 2 of betaxolol - 15-20 hours. It is excreted by the kidneys mainly in the form of metabolites, by 10-15% - unchanged.

Side effect

From the side of the cardiovascular system: at the beginning of treatment - AV blockade, sinus bradycardia, arterial hypotension, heart failure, Raynaud's syndrome. From the digestive system: rarely - abdominal pain, nausea, vomiting. From the side of the central nervous system and peripheral nervous system: at the beginning of treatment - asthenia, paresthesia of the extremities, sleep disturbances, 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 is possible, sometimes lacrimation; rarely - a decrease in the sensitivity of the cornea, erythema, itching, spotted coloration of the cornea, keratitis, anisocoria, photophobia.

Application during pregnancy and lactation

During pregnancy and lactation (breastfeeding), the use of betaxolol is possible only in cases where the intended benefit to the mother outweighs the possible risk to the fetus or child.

Application for violations of liver function

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

Application for impaired renal function

When administered orally 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.

Application in children

It is not recommended to use betaxolol in children.

special instructions

It should be used with caution in bronchial asthma and COPD of moderate course (start treatment with low doses and preferably under the control of respiratory function indicators; thanks to the beta1-selectivity of betaxolol in the event of an attack of bronchial asthma against the background of its administration, it is possible to arrest an attack with beta2-adrenomimetics); with chronic heart failure in the compensation stage (treatment with betaxolol is possible only under strict medical supervision; treatment should be started with very small doses with a gradual increase); with AV blockade of the I degree (careful observation is required, including ECG control); with obliterating diseases of peripheral arteries, Raynaud's syndrome (with the exception of a severe form) (possibly increased peripheral circulatory disorders);with Prinzmetal's angina pectoris (an increase in angina attacks is possible; the use of a selective beta1-blocker is possible only with the simultaneous use of vasodilators); with treated pheochromocytoma (careful monitoring of blood pressure is required); in elderly patients (treatment should be started with low doses and under close medical supervision); with renal failure (with CC more than 20 ml / min - careful monitoring of the patient during the first few days of treatment; with CC less than 20 ml / min and / or hemodialysis requires a correction of the dosage regimen); with hepatic failure (more careful clinical observation is required at the beginning of treatment); in patients with diabetes mellitus (regular monitoring of blood glucose concentration is necessary, including active self-monitoring by the patient, at the beginning of treatment;it is possible to reduce the severity of the precursors of the development of hypoglycemia, such as tachycardia, palpitations and increased sweating); with psoriasis (beta-blockers can worsen the course of psoriasis); when carrying out desensitizing therapy. Cancellation of betaxolol should be carried out gradually, especially in patients with coronary artery disease, angina pectoris. Betaxolol does not affect the size of the pupil, therefore, in case of angle-closure glaucoma, the drug should be used only in combination with miotics. When a patient is transferred to betaxolol after treatment with several antiglaucoma drugs, the latter are canceled gradually, within a period of at least 1 week per drug. With the simultaneous use of betaxolol in the form of eye drops and beta-blockers inside, it is possible to develop additive effects from both intraocular pressure,and manifestations of the systemic action of beta-blockers. Before the planned operation, beta-blockers, incl. betaxolol should be canceled. When using betaxolol topically, contact lenses should not be worn. It is not recommended to use betaxolol in children.

Influence on the ability to drive vehicles and use mechanisms

It is used with caution in patients whose activities require increased attention and quick psychomotor reactions.

Drug interactions

With simultaneous use with adrenergic agonists, xanthine derivatives, the effectiveness of betaxolol decreases. With simultaneous use with antacids and antidiarrheal agents, it is possible to reduce the absorption of beta-blockers. With simultaneous use with antihypertensive drugs, the 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 non-depolarizing 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, an increase in bradycardia is possible. 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-blockers for topical use in glaucoma, an increase in the negative inotropic effect and conduction disturbances are possible. With the simultaneous use of lidocaine, the concentration of lidocaine in the blood plasma increases. With simultaneous use with drugs that deplete the reserves of catecholamines (including with reserpine), an increase in the hypotensive effect and bradycardia is possible. With simultaneous use with sulfasalazine, the concentration of betaxolol in the blood plasma increases.With the simultaneous use of lidocaine, the concentration of lidocaine in the blood plasma increases. With simultaneous use with drugs that deplete the reserves of catecholamines (including with reserpine), an increase in the hypotensive effect and bradycardia is possible. With simultaneous use with sulfasalazine, the concentration of betaxolol in the blood plasma increases.With the simultaneous use of lidocaine, the concentration of lidocaine in the blood plasma increases. With simultaneous use with drugs that deplete the reserves of catecholamines (including with reserpine), an increase in the hypotensive effect and bradycardia is possible. With simultaneous use with sulfasalazine, the concentration of betaxolol in the blood plasma increases.