Betaksolol

General characteristics. Structure:

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

Excipients: a benzalkoniya chloride, dinatrium эдетат, sodium chloride, sodium hydroxide – to рН 6,0-7,8, water for injections.

Pharmacological properties:

Pharmacodynamics. At topical administration бетаксолол reduces intraocular pressure due to reduction of products of intraocular liquid.

Betaksolol can improve eye blood circulation (perfusion). Does not cause a hemeralopia (unlike miotik). Approach of hypotensive effect is observed in 30 min. after an instillation, time of approach of the maximum effect – the 2nd hour. After single instillation influence on intraocular tension remains during the 12th hour.

Pharmacokinetics. Betaksolol is characterized by high degree of lipophilicity therefore it is quickly absorbed by a cornea epithelium, and in intraocular liquid its high concentration is created.

Indications to use:

Betaksolol, drops eye 0,5% are applied to decrease in intraocular pressure as monotherapy or in combination with other drugs:
• at eye hypertensia;
• at an open angle glaucoma.

Route of administration and doses:

Locally. The adult (including to elderly patients) in a conjunctival sac on 1 drop 2 times a day; within the first month treatment is carried out under control of intraocular pressure.

For reduction of system side effects after an instillation it is careful to close eyes, not to blink. Not to open an eye for two minutes for the best absorption of drug.

Treatment duration ― to the discretion of the attending physician.

Features of use:

Use at pregnancy and a lactation. There is no sufficient experiment on use of drug during pregnancy, feeding by a breast. Use of drug during pregnancy and a lactation is possible only in that case when the potential advantage for mother exceeds possible risk for a fruit and the child. At oral administration of β-adrenoblockers during pregnancy there is a risk of a delay of pre-natal fetation and development of signs of blockade of β-adrenoceptors.......... If nevertheless drug was used before childbirth, newborn first days of life have to be under careful observation.

In a small amount бетаксолол gets into breast milk, however development of clinical symptoms of blockade of β-adrenoceptors at use of drug in therapeutic doses is improbable.

System side effects at use of drug in the form of instillations are noted less than side effects at system use.

Extra care at treatment of the patients having disturbance of atrioventricular conductivity or heart failure in the anamnesis is required. Treatment should be stopped at emergence of the first symptoms of a decompensation of cardiovascular system.

Thyrotoxicosis. At patients with suspicion of a thyrotoxicosis it is not necessary to cancel sharply beta adrenoblockers (for the purpose of prevention of strengthening of symptomatology).

Myasthenia. 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).

Surgery. Before planned operation beta adrenoblockers have to be gradually cancelled (not in one step!) in 48 hours prior to the general anesthesia as during the general anesthesia they can reduce sensitivity of a myocardium to the sympathetic stimulation necessary for cardiac performance.

Risk of development of anaphylactic reaction. Patients at whom beta adrenoblockers are applied can have an atopy or anaphylactic reactions in the anamnesis. In case of development of repeated hypersensitivity reactions such patients can be not sensitive to usual doses of Epinephrinum (adrenaline) necessary for stopping of an anaphylaxis.

Use at closed-angle glaucoma. Betaksolol does not influence pupil size, at closed-angle glaucoma to apply to decrease in the increased intraocular pressure only in combination with miotika.

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

Drug the benzalkoniya contains chloride which can be absorbed by contact lenses. The patients carrying contact lenses should remove them before use of drug and to establish back not earlier than in 20 min. after an instillation. When using drug it is necessary to avoid contact of a tip of a stopper dropper with any surface or objects in order to avoid microbic pollution.

Influence on control of motor transport and mechanisms. Patients at whom after drug instillation sight clearness temporarily decreases before its recovery are not recommended to be engaged in the types of activity requiring special attention and reaction.

Side effects:

At assessment of frequency of occurrence of various side reactions the following gradation are used: often ― 1-10%; not often ― 0,1-1%; seldom ― 0,01-0,1%; frequency is unknown (according to the available data it is impossible to establish emergence frequency).

Local reactions. Disturbances from an organ of sight. Often: discomfort in eyes after an instillation, irritation, reddening of eyes. Not often: an itch and unpleasant feelings after an instillation, the obscured sight, a photophobia, dacryagogue. Seldom: decrease in sensitivity of a cornea, erythema, conjunctiva itch, pointed coloring of a cornea, keratitis, anisocoria (different diameter of pupils), photophobia. Frequency is unknown: irritation of eyes (reddening, burning sensation, prickings), a blepharitis, the obscured sight, a xerophthalmus, a cornea erosion, a ptosis, a diplopia, choroid amotio after the filtrational procedures.

System reactions. From immune system. Frequency is unknown: system allergic reactions, including Quincke's disease, small tortoiseshell, local and generalized rash, itch, anaphylactic reaction.

Metabolism disturbances. Frequency is unknown: hypoglycemia.

Psychiatric frustration. Seldom: sleeplessness, depression. Frequency is unknown: nightmares, loss of memory, hallucination, psychosis, confusion of consciousness.

From a nervous system. Seldom: headache. Frequency is unknown: syncope, disturbance of cerebral circulation, brain ischemia, strengthening of signs and symptoms of a myasthenia, dizziness, paresthesias.

From function of heart. Seldom: bradycardia. Frequency is unknown: stethalgia, heart consciousness, arrhythmia, heart failure, oppression of atrioventricular conductivity, emergence of an atrioventricular block or its strengthening, cardiac standstill.

Vascular frustration. Frequency is unknown: arterial hypotension, Reynaud's phenomenon, cold, cyanotic palms and a foot, strengthening of the alternating lameness.

Disturbances from respiratory system. Seldom: диспноэ (short wind), suffocation.
Frequency is unknown: bronchospasm, respiratory insufficiency, cough.

From digestive tract. Frequency is unknown: a dysgeusia (food faddism), nausea, dyspepsia, diarrhea, a xerostomia (dryness in a mouth), an abdominal pain, vomiting.

Disturbances from integuments. Seldom: alopecia. Frequency is unknown: psoriasis rash or exacerbation of psoriasis, skin rash.

Frustration from skeletal and muscular system and connecting fabric. Frequency is unknown: mialgiya.

Disturbances from reproductive system. Frequency is unknown: decrease in a libido, impotence.

The general. Frequency is unknown: adynamy (increased fatigue).

Others: increase in a caption of antinuclear antibodies.

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

Interaction with other medicines:

Strengthening of such effects as lowering of arterial pressure and bradycardia can be observed, at a concomitant use (orally) of blockers of calcium channels, beta adrenoblockers, antiarrhytmic means (including амидарон), glycosides of a foxglove, parasympathomimetics, a guanetidin and the drugs exhausting stocks of catecholamines (such as Reserpinum).

Such patients have to be under careful medical control. At combined use with sympathomimetics ― strengthening of their vasoconstrictive effect.

It is necessary to be careful at combined use of a betaksolol and adrenergic psychotropic drugs owing to possible strengthening of their action. If necessary it can be applied in a combination with other local ophthalmologic drugs. In this case the interval between their use has to make not less than 15 minutes.

At simultaneous use with Epinephrinum (adrenaline) бетаксолол can cause a mydriasis (mydriasis).

Contraindications:

Hypersensitivity to drug components, a sinus bradycardia, a sick sinus syndrome, an atrioventricular block of the II-III degree, cardiogenic shock, the expressed heart failure, severe forms of a chronic obstructive pulmonary disease, severe forms of bronchial asthma (including in the anamnesis), children's age up to 18 years.

With care:

• At the patients applying other beta adrenoblockers (especially systemic action) in connection with risk of total potential impact on intraocular pressure and emergence of undesirable system effects.
• At patients with unstable stenocardia, a heart block of the I degree, hypotension (tendency to bradycardia), coronary heart disease, heart failure.
• At patients with serious violation of peripheric circulation (severe forms of a Raynaud's disease or Reynaud's syndrome).
• At patients with easy/moderate forms of bronchial asthma (including in the anamnesis), patients with easy/moderate forms of a chronic obstructive pulmonary disease.
• At patients with a diabetes mellitus, especially unstable (beta adrenoblockers can mask symptoms of an acute hypoglycemia).
• At patients with a thyrotoxicosis (beta adrenoblockers can mask hyperthyroidism symptoms).
• At patients with a syndrome of a dry eye, diseases corneas or disturbances of formation of the lacrimal film are.
• At patients with closed-angle glaucoma (only in combination with miotika).
• At the patients having an atopy or anaphylactic reactions in the anamnesis.
• At patients with a myasthenia (beta adrenoblockers can strengthen symptoms).
• At patients with a pheochromocytoma.
• At patients after the filtrational procedures (in connection with probability of amotio of a choroid).

Overdose:

At hit in eyes of excess amount of drug to wash out eyes warm flowing water.

At overdose of beta adrenoblockers the lowering of arterial pressure, bradycardia, an acute heart failure can be observed.

Treatment: drug it is necessary to cancel and carry out symptomatic therapy.

Storage conditions:

At a temperature from 8 to 25 °C in the place protected from light. To store in the place, unavailable to children. A period of validity - 3 years, after opening – 28 days. Not to apply after a period of validity.

Issue conditions:

According to the recipe

Packaging:

Drops eye 0,5%. On 5 or 10 ml in the polyethylene bottles which are hermetically closed by the traffic jams droppers and covers which are screwing on. Each bottle together with the application instruction is placed in a pack from a cardboard. 50 bottles and 50 application instructions place in a box from a cardboard (for hospitals).