Betaxolol-Solofarm, eye drops 0.5% 5 ml

Glaucoma, Elevated Intraocular Pressure

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

Active ingredient

Composition

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

Excipients:

benzalkonium chloride – 0.1 mg,

sodium chloride – 5.49 mg,

dinatrium phosphate dihydrate – 3.579 mg,

dinatrium edetate (trilon B) – 0.5 mg,

sodium dihydrophosphate dihydrate – 3.165 mg,

d/i water – up to 1 ml.

How to take, the dosage

Topically. 1-2 drops into the conjunctival sac 2 times a day.

In some patients it takes several weeks for intraocular pressure to stabilize, so it is recommended that intraocular pressure be monitored during the first month of treatment.

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

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

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

In order to reduce systemic absorption of the drug, nasolacrimal occlusion – pressing the inner edges of the eyelids for 2-3 minutes after injecting the drug – is recommended.

Transitioning from another hypotensive therapy

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

If there is no adequate response to therapy, the dose may be increased to 1-2 drops of betaxolol 0.5% solution in each affected eye twice daily.

If therapy with a hypotensive drug other than beta-adrenoblockers is switched from the previous drug group, instillations of the previously prescribed drug are continued with the addition of instillations of one drop of 0.25% betaxololol solution in each affected eye twice a day. The next day, the earlier treatment is withdrawn and therapy with betaxolol continues.

Paediatric Use

Limited data suggest that betaxololol may be recommended for reducing intraocular pressure in true congenital glaucoma, infantile and juvenile congenital glaucoma before surgery or if surgical treatment has failed. Before using the drug, the risks and benefits of betaxolol in the pediatric population should be carefully evaluated through a thorough history of systemic abnormalities.

If the benefits outweigh the risks, it is recommended that betaxolol at the lowest available concentration of 1 drop once daily. If the hypotensive effect is insufficient, it is necessary to switch to use 2 times a day with an interval between instillations of 12 hours. Ocular and systemic side effects should be monitored for 1-2 hours after the first instillation.

Interaction

Special studies of interactions of betaxolol with other medicinal products have not been conducted.

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

. When concomitant administration of beta-adrenoblockers for topical ophthalmic use with oral forms of “slow” calcium channel blockers, beta-adrenoblockers, antiarrhythmic drugs (including amiodarone) cardiac glycosides, parasympathomimetics, guanethidine, and catecholamine depleting drugs such as reserpine, increased effects such as decreased blood pressure and marked bradycardia may be observed. There have been cases of mydriasis when concomitant use of beta-adrenoblockers and epinephrine.

In concomitant administration of betaxololol with myorexants and hypoglycemic agents there may be an increase in the effect of the latter.

Beta-adrenoblockers may decrease the effect of adrenaline used to stop anaphylactic reactions. Special caution should be used in patients with a history of atopy or anaphylaxis.

When used together with sympathomimetics, an increase in their vasoconstrictor effect.

Caution should be exercised when co-administering betaxolol and adrenergic psychotropic drugs due to possible enhancement of their effects.

It can be used in combination with other topical ophthalmic drugs if necessary, in which case the interval between applications should be at least 10 minutes.

Special Instructions

Beta-adrenoblockers should be used with caution in patients with a tendency to spontaneous hypoglycemia and in patients with labile diabetes, because these drugs may mask the signs and symptoms of acute hypoglycemia.

Thyrotoxicosis

Beta-adrenoblockers can mask some symptoms of hyperthyroidism (e.g., tachycardia). In patients with suspected thyrotoxicosis, beta-adrenoblockers should not be abruptly withdrawn, as this may cause worsening of symptoms.

Myasthenia gravis

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

Surgery

The anesthesiologist should be advised that the patient is taking betaxolol. Prior to elective surgery, beta-adrenoblockers must be gradually (not overnight!) withdrawn 48 hours before general anesthesia because during general anesthesia they can decrease myocardial sensitivity to sympathetic stimulation necessary for heart function (for example, they can block adrenaline).

Pulmonology

There have been reports of respiratory reactions, including death, due to bronchospasm in patients with bronchial asthma when certain beta-adrenoblockers are used in ophthalmology.

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

Anaphylactic reactions

Betaxololol administration to patients with a history of atopy or severe anaphylactic reactions to various allergens may show a more pronounced reaction to repeated administration of these allergens and insensitivity to standard doses of epinephrine in controlling anaphylactic reactions.

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

When administered topically, beta-adrenoblockers may enter the systemic bloodstream and cause adverse reactions in the cardiovascular, pulmonary and other systems.

Severe respiratory and cardiovascular events have been described, including death from bronchospasm in patients with bronchial asthma and death from heart failure when using betaxololol.

Cardiac disorders

In patients with cardiovascular disease (e.g., coronary heart disease, Prinzmetal angina, heart failure) and arterial hypotension, therapy with beta-adrenoblockers should be critically evaluated with consideration of treatment with drugs from other groups. Careful monitoring of the development of signs of exacerbation and adverse reactions in patients with cardiovascular disease is necessary.

Corneal disease

Beta-adrenoblockers can cause dry eyes. The drug should be used with caution in patients with corneal diseases.

The main pathogenetic aspect of treating closed angle glaucoma is the need to open the angle of the anterior chamber, which is achieved by constricting the pupil with myotics. Betaxolol has no effect on pupil diameter, so in open angle glaucoma the drug should only be used in combination with miotics.

Vascular detachment

There have been cases of vascular detachment when using drugs that reduce intraocular fluid production (e.g., timolol, acetazolamide) after fistulizing anti-glaucomatous surgery.

The drug contains the preservative benzalkonium chloride which may irritate the eyes and cause discoloration of soft contact lenses. Direct contact of the product with soft contact lenses should be avoided. Patients who wear contact lenses shall remove the lenses and put them back on not earlier than 15 minutes after instillation of the drug.

Impact on ability to operate vehicles and machinery:

During treatment, caution should be exercised when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and rapid psychomotor reactions.

Contraindications

– Hypersensitivity to betaxolol and other drug components;

– bradycardia;

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

– sinus node weakness syndrome;

– sinoatrial block;

– cardiogenic shock;

– decompensated chronic heart failure;

– Reactive respiratory disease, including severe bronchial asthma (including a history);

– Severe chronic obstructive pulmonary disease.

With caution:

The treatment of patients using β1-adrenoblocker agents and betaxolol (eye drops) should be under regular medical supervision due to the risk of cumulative potential effects on intraocular pressure and the occurrence of adverse systemic effects.

While the overall effect of betaxolol (in the form of eye drops) on the body is mild, care should be taken when prescribing it to patients with thyrotoxicosis and diabetes mellitus (especially unstable) because the drug may mask the effects of hypoglycemia.

Before surgical intervention using general anesthesia the drug should be gradually discontinued because the drug may change the patient’s reaction to the use of general anesthetics.

Side effects

In common with other medications in the form of eye drops, betaxolol may enter the systemic bloodstream, leading to the development of systemic adverse events.

The undesired reactions are presented according to the following frequency gradation: very common (≥ 10%); common (≥ 1, < 10%); infrequent (≥ 0.1, < 1%); rare (≥ 0.01, < 0.1%); very rare (< 0.01%); frequency unknown (the frequency cannot be determined from available data).

Visual disturbances

Very common: eye discomfort.

Often: blurred vision, increased tear production.

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

Rarely: cataract, decreased corneal sensitivity, reddened eyelids.

Nervous system disorders

Often: headache.

Rarely: fainting.

Frequent unknown: dizziness.

Cardiac disorders

Infrequent: bradycardia, tachycardia.

Prevalence unknown: arrhythmia.

Vascular disorders

Rarely: hypotension.

Respiratory system, chest and mediastinum disorders

Infrequently: bronchospasm, dyspnea, rhinitis.

Rarely: cough, rhinorrhea.

Gastrointestinal disorders

Infrequent: nausea.

Rarely: dysgeusia.

Skin and subcutaneous tissue disorders

Rarely: dermatitis, rash, alopecia.

Reproductive system and breast disorders

Rare: decreased libido.

Mental disorders

Rarely: anxiety, insomnia, depression.

General disorders and reactions at the site of administration

Infrequent unknown: asthenia.

Immune system disorders

With unknown frequency: hypersensitivity.

There have been other adverse reactions that may also develop with topical beta-adrenoblockers (no information on the frequency of development):

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

Metabolic and nutritional disorders: hypoglycemia.

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

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

Visual organ disorders: detachment of the vasculature of the eye after fistulizing anti-occlusive surgeries, corneal erosion, ptosis, diplopia.

Chronic disorders: chest pain, palpitations, edema, chronic heart failure, atrioventricular block, cardiac arrest, heart failure, delayed atrioventricular conduction or worsening degree of blockade.

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

Respiratory system, chest and mediastinum disorders: bronchospasm (mainly in patients with a history of bronchospastic disorders).

Gastrointestinal disorders: dyspepsia, diarrhea, dry mouth, abdominal pain, vomiting.

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

Muscular system disorders: myalgia.

Gender and mammary gland disorders: sexual dysfunction, impotence.

General disorders and reactions at the site of administration: fatigue.

Overdose

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

The treatment of overdose symptoms should be symptomatic and supportive.

In case of topical application of excessive amounts of the drug, the eyes should be flushed with warm water.

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