Betaksolol

General characteristics. Structure:

Active ingredient: 5 mg of a betaksolol (in the form of a hydrochloride) in 1 ml of solution.

Excipients: sodium chloride, dinatrium of an edetat a dihydrate (disodium salt of ethylene diamine tetraacetic acid a dihydrate), a benzetoniya chloride, Acidum hydrochloricum of 1 M or sodium hydroxide of 1 M to pH 6,0-7,8, the water purified.

Pharmacological properties:

Pharmacodynamics. Protivoglaukomny drug. The selection beta1-adrenoblocker without internal sympathomimetic activity. Does not possess membrane stabilizing (mestnoanesteziruyushchy) action.

At topical administration бетаксолол reduces intraocular pressure due to reduction of products of intraocular liquid. Betaksolol (in comparison with other beta adrenoblockers) does not cause decrease in a blood-groove in an optic nerve. (Miosis) and a tsiliarny muscle (an accommodation spasm), a hemeralopia, effect of "veil" before eyes does not cause reduction of a circular muscle.

Approach of hypotensive action is observed in 30 min. after an instillation, the maximum effect develops in 2 h. After single instillation influence on intraocular tension remains during 12 h.

Pharmacokinetics. At topical administration of drug system absorption of a betaksolol of a hydrochloride is possible. Resorptive action is expressed slightly. Communication with proteins of plasma - 50%. An elimination half-life (T1/2) - 14-22 h. It is removed by kidneys (15% in an invariable look). Permeability through a blood-brain barrier - low; secretion with breast milk - insignificant.

Indications to use:

Drug is used for decrease in intraocular pressure as monotherapy or in combination with other drugs at an open angle glaucoma and eye hypertensia.

Route of administration and doses:

Locally. Dig in in a conjunctival sac on 1 drop 2 times a day; within the first month treatment is carried out under control of intraocular pressure.

Features of use:

Pregnancy and lactation. Betaksolol at pregnancy and in the period of a lactation is not present sufficient experience of use of drug. Use of drug at pregnancy and in the period of a lactation (breastfeeding) is possible only in that case when the estimated advantage for mother exceeds potential risk for a fruit or the child.

Does not influence pupil size; at closed-angle glaucoma to apply only in combination with miotika.

At transfer of the patient on Betaksolol after treatment by several protivoglaukomny medicines, the last are cancelled gradually.

With care appoint drug to patients with a diabetes mellitus because beta adrenoblockers can mask symptoms of an acute hypoglycemia.

With care appoint drug to patients with a thyrotoxicosis because beta adrenoblockers can mask thyrotoxicosis symptoms (for example, tachycardia). At patients with suspicion of a thyrotoxicosis it is not necessary to cancel sharply beta adrenoblockers, it can cause strengthening of symptomatology.

It is necessary to consider that beta adrenoblockers can cause the symptoms similar to symptoms at a myasthenia (a diplopia, a ptosis, the general weakness).

Betaksolol exerts the minimum impact on arterial pressure and heart rate. However patients should be careful at purpose of drug with an atrioventricular block or heart failure. Treatment by Betaksolol should be stopped immediately at emergence of the first symptoms of a decompensation from cardiovascular system.

Before planned surgery it is necessary to cancel gradually beta adrenoblockers for 48 h to the general anesthesia because during the general anesthesia they can reduce sensitivity of a myocardium to sympathetic stimulation.

It is necessary to be careful at combined use of Betaksolol and adrenergic psychotropic drugs.

Eye drops Betaksolol contain preservatives which can be besieged in soft contact lenses and have the damaging effect on eye tissues. Therefore the patients carrying contact lenses should remove them before use of drops and to establish back not earlier than in 20 min. after an instillation.

Influence on ability to manage vehicles and mekhaizm. If after Betaksolol's use for patients sight clearness temporarily decreases, before its recovery it is not recommended to drive the car and to be engaged in the types of activity requiring special attention and reaction.

Side effects:

From sense bodys: often - short-term discomfort in eyes after an instillation, dacryagogue. In rare instances - decrease in sensitivity of a cornea, reddening, an eye, a dot keratitis, a photophobia, an anisocoria, photophobia, an itch, feeling of "dryness" of eyes, allergic reactions.

System side effects are noted seldom:

From the central nervous system: dizziness, nausea, drowsiness, sleeplessness, headache, depression, strengthening of symptoms of a myasthenia.

From respiratory system: asthma, bronchospasm, respiratory insufficiency.

From cardiovascular system: bradycardia, disturbance of cordial conductivity, heart failure.

If the side effects specified in the instruction are aggravated, or you noticed any other side effects which are not specified in the instruction, report about it to the doctor.

Interaction with other medicines:

At simultaneous use of Betaksolol with beta adrenoblockers for intake the risk of development of the additive effect (manifestation of local and system side effects) increases. The patients receiving this combination of drugs have to be under medical observation.

At Betaksolol's use in combination with the drugs oppressing deposition of catecholamines (Reserpinum) hypotension and bradycardia can be observed.

At co-administration of muscle relaxants and hypoglycemic means strengthening of their action can be observed.

At combined use with sympathomimetics - strengthening of their vasoconstrictive effect.

It is necessary to be careful at combined use of Betaksolol and adrenergic psychotropic drugs owing to possible strengthening of their action.

Contraindications:

Hypersensitivity to drug components, a sinus bradycardia (less than 45-50 beats/min), a syndrome of weakness of a sinus node, an atrioventricular block of II and III degrees, heavy chronic heart failure, cardiogenic shock, a myasthenia, heavy obstructive respiratory insufficiency, arterial hypotension, bronchial asthma, age up to 18 years.

With care. A chronic obstructive pulmonary disease, unstable stenocardia, tendency to bradycardia, an atrioventricular block of the I degree, disturbance of peripheric circulation, a diabetes mellitus in a decompensation stage, a hypoglycemia, Reynaud's syndrome, a pheochromocytoma, abnormal liver functions and kidneys, a thyrotoxicosis, a myasthenia, advanced age.

Overdose:

At hit in eyes of excess amount of drug it is necessary to wash out eyes warm water.

Storage conditions:

In the place protected from light at a temperature not above 15 °C (for drug in a tube droppers, a bottle droppers); in the place protected from light at a temperature not above 25 °C (for drug in bottles). To protect from freezing. To store in the places unavailable to children. A period of validity - 2 years in a tube droppers, a bottle droppers. 3 years in bottles. A drug period of validity after opening - 1 month. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Drops are eye, 0,5%. Packaging: 1,5 ml, 2 ml or 5 ml in a tube dropper polymeric. 1, 2, 4, 5 or 10 tube droppers with the application instruction of drug and the application instruction a tube dropper is placed in a pack from a cardboard with partitions or without partitions. 5 ml or 10 ml in a bottle dropper polymeric. The 1 or 2 bottle of a dropper with the application instruction of drug and the application instruction a bottle dropper is placed in a pack from a cardboard. 5 ml in bottles glass. 1 bottle in a set with a sterile cover dropper and the application instruction of drug is placed in a pack from a cardboard.