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

Excipients: benzalkonium chloride 0.1 mg, disodium edetate 0.1 mg, sodium chloride 8 mg, sodium hydroxide to pH 6.0-7.8, water for injection up to 1 ml.

Description:

A clear, colorless liquid.

Pharmacotherapeutic group:Anti-glaucoma - beta-blocker

ATX: & nbsp

S.01.E.D.02 Betaxolol

Pharmacodynamics:

Selective beta₁-adrenoceptor without internal sympathomimetic activity. Practically does not have membrane stabilizing (local anesthetic action).

With topical application betaxolol reduces intraocular pressure due to decreased production of intraocular fluid.

Betaxolol can improve the ocular circulation (perfusion). Does not cause hematology (in contrast to myotics).

The onset of the hypotensive effect is observed 30 minutes after instillation, the time of the maximum effect is 2 hours. After a single instillation, the effect on the ophthalmotonus persists for 12 hours.

Pharmacokinetics:

Betaxolol is characterized by a high degree of lipophilicity, as a result of which it is rapidly absorbed by the corneal epithelium, and high concentration is created in the intraocular fluid.

With topical application of the drug, systemic absorption is possible. Resorptive effect is not significant. Connection with plasma proteins - 50%. Half-life (T_1/2) - 16-22 hours. It is excreted mainly by the kidneys in the form of two carboxylic acids and in unchanged form (about 16% of the applied dose in unchanged form).Permeability through the blood-brain barrier (BBB) and the placental barrier is low, secretion with breast milk is insignificant.

Indications:

It is used to reduce intraocular pressure as a monotherapy or in combination with other drugs:

- with ocular hypertension;

- with open-angle glaucoma.

Contraindications:

Hypersensitivity to the components of the drug, sinus bradycardia, syndrome of weakness of the sinus node, atrioventricular block II-III degree, cardiogenic shock, severe heart failure, severe forms of chronic obstructive pulmonary disease, severe forms of bronchial asthma (including history), children under 18 years of age.

Carefully:

- In patients using other beta-blockers (especially systemic action) due to the risk of a total potential impact on intraocular pressure and the appearance of unwanted systemic effects;

- in patients with unstable angina, cardiac arrest of the 1st degree, hypotension (propensity to bradycardia), coronary heart disease, heart failure;

- in patients with a serious impairment of peripheral circulation (severe forms of Raynaud's disease or Raynaud's syndrome);

- in patients with mild / moderate forms of bronchial asthma (including history), patients with mild / moderate forms of chronic obstructive pulmonary disease;

- in patients with diabetes, especially unstable (beta-adrenoblockers can mask the symptoms of acute hypoglycemia);

- in patients with thyrotoxicosis (beta-adrenoblockers can mask the symptoms of hyperthyroidism);

- in patients with dry eye syndrome, corneal diseases or tear film disorders;

- in patients with closed-angle glaucoma (only in combination with miotics);

- patients who have a history of atopy or anaphylactic reactions;

- in patients with myasthenia gravis (beta-blockers may increase symptoms);

- in patients with pheochromocytoma;

- in patients after filtration procedures (in connection with the probability of detachment of the choroid).

Pregnancy and lactation:

Sufficient experience in the use of the drug during pregnancy, breast-feeding is not.

The use of the drug during pregnancy and lactation is possible only if the potential benefit to the mother exceeds the possible risk to the fetus and the baby.When oral beta-blockers are taken orally during pregnancy, there is a risk of delay in intrauterine fetal development and development of signs of blockade of β-adrenergic receptors. If, however, the drug was used before delivery, the newborns should be closely monitored during the first days of life.

In a small amount betaxolol penetrates into breast milk, but it is unlikely that clinical symptoms of β-adrenoreceptor blockade will develop when the drug is used in therapeutic doses.

Dosing and Administration:

Locally. Adults (including elderly patients) in the conjunctival sac 1 drop 2 times a day; During the first month, treatment is carried out under the control of intraocular pressure.

To reduce systemic side effects after instillation, gently close your eyes, do not blink. Do not open your eyes for two minutes for better absorption of the drug.

The duration of treatment is at the discretion of the attending physician.

Side effects:

When assessing the frequency of occurrence of various adverse reactions, the following grades are used: often 1-10%; infrequently, 0.1-1%; rarely - 0,01-0,1%; the frequency is unknown (it is not possible to determine the frequency of occurrence from the available data).

Local Reactions

Disturbances on the part of the organ of sight

Often: discomfort of the eyes after instillation, irritation, redness of the eyes.

Infrequently: itching and discomfort after instillation, blurred vision, photophobia, lacrimation.

Rarely: decreased sensitivity of the cornea, erythema, conjunctival itching, spotting of the cornea, keratitis, anisocoria (different pupil diameter), photophobia.

Frequency unknown: eye irritation (redness, burning sensation, tingling sensations), blepharitis, blurred vision, dry eyes, corneal erosion, ptosis, diplopia, detachment of the choroid after filtration procedures.

Systemic reactions

From the immune system

Frequency unknown: systemic allergic reactions, including angioedema, hives, local and generalized rash, itching anaphylactic reaction.

Metabolic disorders

Frequency unknown: hypoglycemia.

Psychiatric Disorders

Rarely: insomnia, depression.

Frequency unknown: nightmares, memory loss, hallucinations, psychosis, confusion.

From the nervous system

Rarely: headache.

Frequency unknown: syncope, impaired cerebral circulation, ischemia of the brain,increased signs and symptoms of myasthenia gravis, dizziness, paresthesia.

From the function of the heart

Rarely: bradycardia.

Frequency unknown: pain in the chest, palpitations, arrhythmia, heart failure, suppression of atrioventricular conduction, the onset of atrioventricular blockade or its amplification, cardiac arrest.

Vascular disorders

Frequency unknown: Arterial hypotension, Raynaud phenomenon, cold, cyanotic palms and feet, increased intermittent claudication.

Disturbances from the respiratory system

Rarely: dyspnea (dyspnea), choking.

Frequency unknown: bronchospasm, respiratory failure, cough.

From the gastrointestinal tract

Frequency unknown: dysgeusia (perversion of taste), nausea, dyspepsia, diarrhea, xerostomia (dry mouth), abdominal pain, vomiting.

Disturbances from the skin

Rarely: alopecia.

Frequency unknown: psoriatic rash or exacerbation of psoriasis, skin rash.

Disorders from the musculoskeletal system and connective tissue

Frequency unknown: myalgia.

Disorders from the reproductive system

Frequency unknown: decreased libido, impotence.

Are common

Frequency unknown: asthenia (increased fatigue).

Other: an increase in the titer of antinuclear antibodies.

Overdose:

If eye contact is excessive, rinse eyes with warm running water.

With an overdose of beta-blockers, there may be a decrease in blood pressure, bradycardia, acute heart failure.

Treatment: the drug should be withdrawn and symptomatic therapy should be given.

Interaction:

There may be an increase in such effects as lowering blood pressure and bradycardia, while taking (orally) calcium channel blockers, beta-blockers, antiarrhythmics (including amidarone), digitalis glycosides, parasympathomimetics, guanethidine and preparations depleting catecholamine stores (such as reserpine).

Such patients should be under careful medical supervision.

When combined with sympathomimetics, they intensify their vasoconstrictive effect.

Care should be taken when combining betaxolol and adrenergic psychotropic drugs, as a result of the possible increase in their effect.

If necessary, it can be used in combination with other local ophthalmic preparations. In this case, the interval between their use should be at least 15 minutes.

With simultaneous use with epinephrine (adrenaline) betaxolol can cause a dilated pupil (mydriasis).

Special instructions:

Systemic side effects when using the drug in the form of instillations are noted less often than side effects in systemic application.

Special care is required in the treatment of patients with a history of atrioventricular conduction disorder or heart failure. Treatment should be discontinued when the first symptoms of decompensation of the cardiovascular system appear.

Thyrotoxicosis

In patients with suspected thyrotoxicosis, beta-blockers should not be abruptly abolished (in order to prevent symptoms from increasing).

Myasthenia gravis

It should be borne in mind that beta-adrenoblockers can cause symptoms similar to those in myasthenia gravis (diplopia, ptosis, general weakness).

Surgery

Before the planned operation, beta-blockers should be phased out (not instantaneously!) 48 hours before the general anesthesia,since during general anesthesia they can reduce the sensitivity of the myocardium to sympathetic stimulation necessary for the work of the heart.

The risk of developing an anaphylactic reaction

Patients who use beta-blockers may have a history of atopy or anaphylactic reactions. In the case of the development of repeated reactions of hypersensitivity, such patients may not be sensitive to the usual doses of epinephrine (adrenaline) necessary for arresting anaphylaxis.

Application with angle-closure glaucoma

Betaxolol does not affect pupil size, with closed-angle glaucoma to reduce increased intraocular pressure to be used only in combination with miotics.

When transferring the patient to betaxolol After treatment with several antiglaucoma drugs, the latter are gradually phased out.

The preparation contains benzalkonium chloride, which can be absorbed by contact lenses. For patients wearing contact lenses, they should be removed before using the drug and should not be set back until 20 minutes after instillation. When using the drug, avoid touching the tip of the dropper with anysurface or objects to avoid microbial contamination.

Effect on the ability to drive transp. cf. and fur:

Patients who, after instillation of the drug, temporarily lose their clear vision, are not recommended to engage in activities requiring increased attention and response before recovery.

Form release / dosage:Eye drops, 0,5%.

Packaging:

For 5 or 10 ml in polyethylene bottles, hermetically sealed with stoppers, droppers and caps screwed.

Each bottle, together with the instructions for use, is placed in a pack of cardboard.

50 bottles and 50 instructions for use are placed in a cardboard box (for hospitals).

Storage conditions:

At a temperature of 8 to 25 ° C, in a place protected from light.

Keep out of the reach of children.

Shelf life:

3 years, after opening - 28 days.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002470

Date of registration:21.05.2014 / 14.09.2015

Expiration Date:21.05.2019

The owner of the registration certificate:Firm VIPS-MED, LLC Firm VIPS-MED, LLC Russia

Manufacturer: & nbsp

Firm VIPS-MED, LLC Russia

Information update date: & nbsp24.01.2017

Illustrated instructions

Instructions

Betaxolol (Betaxolol)