Betaxolol-Solofarm eye drops 0.5%, 5ml

Composition

1 ml of betaxolol hydrochloride 5.6 mg, which corresponds to the content of betaxolol 5 mg

Auxiliary substances:

benzalkonium chloride-0.1 mg,

sodium chloride-5.49 mg,

disodium phosphate dihydrate-3.579 mg,

disodium edetate (trilon B) – 0.5 mg,

sodium dihydrogen phosphate dihydrate-3.165 mg,

water d / i-up to 1 ml

Pharmacological action

Anti – glaucoma agent-beta-blocker

Indications

Reduction of elevated intraocular pressure in patients with ophthalmic hypertension and primary open-angle glaucoma as monotherapy or in combination with other medications.

Contraindications

– Hypersensitivity to betaxolol and other components of the drug;

– bradycardia;

– atrioventricular block II and III degree, uncontrolled artificial pacemaker;

syndrome of weakness of the sinus node;

– sinoatrial block;

– cardiogenic shock;

– decompensated chronic heart failure;

reactive airway disease, including severe asthma (including in the anamnesis);

– severe chronic obstructive pulmonary disease.

With caution:

Treatment of patients using beta-1-blocker agents and betaxolol (eye drops) should be carried out under regular medical supervision due to the risk of a total potential effect on intraocular pressure and the appearance of undesirable systemic effects.

Despite the weakly expressed general effect of betaxolol (in the form of eye drops) on the body, caution should be exercised when prescribing it to patients with thyrotoxicosis and diabetes mellitus (especially unstable), since the drug can mask the manifestations of hypoglycemia.

Before surgery using general anesthesia, the drug should be gradually discontinued, as the drug may change the patient’s response to the use of general anesthetics.

Side effects

Like other medications in the form of eye drops, betaxolol can enter the systemic circulation, which leads to the development of systemic side effects.

Adverse reactions are presented according to the following gradation of their frequency: very common (≥ 10%); common (≥ 1, < 10%); infrequent (≥ 0.1, < 1%); rare (≥ 0.01, < 0.1%); very rare (

Visual disturbances

Very common: eye discomfort.

Often: blurred vision, increased lacrimation.

Infrequently: pinpoint keratitis, keratitis, conjunctivitis, blepharitis, visual disturbances, photophobia, eye pain, dry eye syndrome, asthenopia, blepharospasm, itching in the eye, eye discharge, crusting on the edges of the eyelids, eye irritation, conjunctival disorders, conjunctival edema, eye hyperemia.

Rare: cataracts, decreased corneal sensitivity, redness of the eyelids.

Nervous system disorders

Often: headache.

Rare: fainting.

Frequency unknown: dizziness.

Cardiac disorders

Infrequently: bradycardia, tachycardia.

Frequency unknown: arrhythmia.

Vascular disorders

Rarely: hypotension.

Respiratory, thoracic and mediastinal disorders

Infrequently: bronchospasm, shortness of breath, rhinitis.

Rare: cough, rhinorrhea.

Disorders of the gastrointestinal tract

Infrequently: nausea.

Rare: dysgeusia.

Skin and subcutaneous tissue disorders

Rare: dermatitis, rash, alopecia.

Disorders of the reproductive system and breast

Rarely: decreased libido.

Mental disorders

Rare: anxiety, insomnia, depression.

General disorders and reactions at the injection

site Frequency unknown: asthenia.

Immune system disorders

With unknown frequency: hypersensitivity.

There were other adverse reactions that may develop with the use of local beta-blockers (there is no information on the frequency of development). :

Immune system disorders: systemic allergic reactions, including angioedema, urticaria, local and generalized rash, pruritus, anaphylactic reactions.

Metabolic and nutritional disorders:  hypoglycemia.

Mental disorders: nightmares, memory loss, hallucinations, psychosis, confusion.

Nervous system disorders: cerebrovascular disorders, cerebral ischemia, worsening of signs and symptoms of myasthenia gravis, paresthesia.

Visual disturbances:  detachment of the choroid of the eye after fistulizing anti-glaucoma operations, corneal erosion, ptosis, diplopia.

Cardiac disorders:  chest pain, palpitation, swelling, chronic heart failure, atrioventricular block, cardiac arrest, heart failure, slowing of atrioventricular conduction, or worsening of the degree of blockage.

Vascular disorders: Raynaud’s phenomenon, cold and cyanosis of the hands and feet, aggravation of the existing intermittent claudication.

Respiratory, thoracic and mediastinal disorders:  bronchospasm (mainly in patients with a history of bronchospastic diseases).

Disorders of the gastrointestinal tract:  dyspepsia, diarrhea, dry mouth, abdominal pain, vomiting.

Skin and subcutaneous tissue disorders:  psoriasis-like rash or exacerbation of psoriasis.

Musculoskeletal disorders:  myalgia.

Genital and breast disorders:  sexual dysfunction, impotence.

General disorders and reactions at the injection site:  fatigue.

Interaction

Special studies of the interaction of betaxolol with other drugs have not been conducted.

In patients receiving betaxolol and simultaneously taking other beta-blockers orally, the risk of adverse reactions (both systemic and local) may be higher due to the possible additive effect. Such patients should be under close medical supervision.

Concomitant use of beta-blockers for topical ophthalmic use with oral forms of slow calcium channel blockers, beta-blockers, antiarrhythmic drugs (including amiodarone), cardiac glycosides, parasympathomimetics, guanethidine, and catecholamine depletion drugs such as reserpine may result in increased effects such as lowering blood pressure and severe bradycardia. There have been cases of mydriasis with concomitant use of beta-blockers and epinephrine.

When concomitant use of betaxolol with muscle relaxants and hypoglycemic agents may increase the effect of the latter.

Beta-blockers may reduce the effect of epinephrine, which is used to stop anaphylactic reactions. It should be used with extreme caution in patients with a history of atopy or anaphylaxis.

When used together with sympathomimetics, their vasoconstrictor effect is enhanced.

Caution should be exercised when concomitantly using betaxolol and adrenergic psychotropic drugs due to the possible increase in their effect.

If necessary, it can be used in combination with other topical ophthalmic medications, in which case the interval between their use should be at least 10 minutes.

How to take, course of use and dosage

Locally. 1-2 drops in the conjunctival sac 2 times a day.

In some patients, stabilization of intraocular pressure occurs within a few weeks, so it is recommended to monitor intraocular pressure during the first month of treatment.

The duration of use of the drug is determined by the attending physician, depending on the effectiveness of therapy.

If the clinical effectiveness of monotherapy is insufficient, additional therapy is prescribed.

The use of two beta-blockers for topical use is not recommended.

To reduce the systemic absorption of the drug, nasolacrimal occlusion is recommended – pressing the inner edges of the eyelids for 2-3 minutes after instillation of the drug.

Switching from another antihypertensive therapy

When switching from therapy with one beta-blocker to therapy with another drug from the group of beta-blockers, it is recommended to complete the full day of therapy with the previously used antihypertensive agent, and the next day start instillation of betaxolol 0.25% in each affected eye,1 drop 2 times a day.

In the absence of an adequate response to therapy, the dose can be increased to 1-2 drops of 0.5% betaxolol solution in each affected eye twice a day.

When switching from therapy with a hypotensive drug of another group, in addition to beta-blockers, instillations of the previously prescribed drug are continued with the addition of instillations of one drop of 0.25% betaxolol solution in each affected eye twice a day. The next day, the previously applied treatment is canceled and betaxolol therapy continues.

Use in the pediatric population

According to limited data, betaxolol can be recommended for reducing intraocular pressure in true congenital glaucoma, infantile and juvenile congenital glaucoma in the preoperative period or in the case of ineffectiveness of surgical treatment.Before using the drug, it is necessary to carefully assess the risks and benefits of using betaxolol in the pediatric population by carefully collecting anamnesis of systemic disorders.

If the benefit outweighs the risk, it is recommended to use betaxolol in the minimum available concentration of 1 drop 1 time a day. If the hypotensive effect is insufficient, it is necessary to switch to the use of 2 times a day with an interval between instillations of 12 hours. It is necessary to monitor ocular and systemic side effects within 1-2 hours after the first instillation.

Overdose

If the contents of the bottle are accidentally swallowed, beta-block symptoms may develop, including bradycardia, hypotension, acute heart failure, and bronchospasm.

Treatment of overdose symptoms should be symptomatic and supportive.

If an excessive amount of the drug is applied topically, it is necessary to rinse the eyes with warm water.

Special instructions

Diabetes mellitus

Beta-blockers should be used with caution in patients with a tendency to spontaneous hypoglycemia and patients with labile diabetes mellitus, since these drugs can mask the signs and symptoms of acute hypoglycemia.

Thyrotoxicosis

Beta-blockers can mask some of the symptoms of hyperthyroidism (for example, tachycardia). In patients with suspected thyrotoxicosis, beta-blockers should not be abruptly discontinued, as this may cause increased symptoms.

Myasthenia

gravis Beta-blockers can cause symptoms and signs similar to those of myasthenia gravis (e. g., diplopia, ptosis, general weakness).

Surgery

The anesthesiologist should be informed that the patient is taking betaxolol. Before elective surgery, beta-blockers should be taken gradually (not simultaneously!) they are canceled 48 hours before general anesthesia, because during general anesthesia they can reduce the sensitivity of the myocardium to sympathetic stimulation necessary for the heart to work (for example, they can block the action of epinephrine).

Pulmonology

There have been reports of respiratory reactions, including death, due to bronchospasm in patients with asthma when using certain beta-blockers in ophthalmology.

Betaxolol should be used with caution in patients with moderate to moderate asthma (including a history of asthma), and in patients with mild to moderate chronic obstructive pulmonary disease.

Anaphylactic reactions

When using betaxolol in patients with atopic or severe anaphylactic reactions to various allergens in the anamnesis, there may be a more pronounced reaction to repeated use of these allergens and immunity to standard doses of epinephrine when stopping anaphylactic reactions.

Betaxolol should be used with caution in patients with severe peripheral circulatory disorders (i. e., in patients with severe Raynaud’s disease or Raynaud’s syndrome, as well as with pheochromocytoma).

When administered topically, beta-blockers can enter the systemic circulation and cause undesirable reactions from the cardiovascular, pulmonary and other systems.

Cases of severe respiratory and cardiovascular disorders, including death from bronchospasm in patients with bronchial asthma and death from heart failure with the use of betaxolol, have been described.

Cardiac disorders

In patients with cardiovascular diseases (e. g., ischemic heart disease, Prinzmetal angina, heart failure) and arterial hypotension, beta-blocker therapy should be critically evaluated with consideration of the possibility of treatment with drugs of other groups. It is necessary to carefully monitor the development of signs of exacerbation of the disease and adverse reactions in patients suffering from cardiovascular diseases.

Corneal diseases

Beta-blockers can cause dry eyes. In patients with corneal diseases, the drug should be used with caution.

The main pathogenetic aspect of the treatment of angle-closure glaucoma is the need to open the angle of the anterior chamber, which is achieved by narrowing the pupil with the help of myotics. Betaxolol does not affect the pupil diameter, so for open-angle glaucoma, the drug should only be used in combination with mystics.

Vasculature detachment

Cases of detachment of the choroid of the eye are described when using drugs that reduce the production of intraocular fluid (for example, timolol, acetazolamide) after fistulizing anti-glaucomatous operations.

The product contains the preservative benzalkonium chloride, which can cause eye irritation and discoloration of soft contact lenses. Direct contact of the drug with soft contact lenses should be avoided. Patients using contact lenses should remove the lenses before using the drug and put them back no earlier than 15 minutes after instillation.

Influence on the ability to drive vehicles and mechanisms:

During the treatment period, care should be taken when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Form of production

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

Active ingredient

Betaxolol

Conditions of release from pharmacies

By prescription

Dosage form

eye drops

Purpose

For adults as directed by your doctor

Indications

Glaucoma