Timolol-Solopharm eye drops 0.5% in dropper bottle, 5ml

Composition

1 ml of timolol maleate 6.84 mg, which corresponds to the content of timolol 5 mg

Auxiliary substances:

benzalkonium chloride-0.1 mg,

sodium dihydrogen phosphate dihydrate-6.1 mg,

sodium hydrophosphate dihydrate-15.16 mg,

d/i water-up to 1 ml

Pharmacological action

Non-selective beta-blocker.

When applied topically in ophthalmology, it reduces both normal and elevated intraocular pressure by reducing the formation of intraocular fluid and improving its outflow, and does not affect accommodation and pupil size.

It has antianginal, antihypertensive and antiarrhythmic effects that occur with systemic use. Reduces the automatism of the sinus node, reduces heart rate, slows down AV conduction, reduces contractility and the need for oxygen in the myocardium.

Indications

Increased intraocular pressure (oftazmogypertension), open-angle glaucoma, glaucoma in the afactic eye and other types of secondary glaucoma, congenital glaucoma (if other means are not effective), as an additional means to reduce intraocular pressure in closed-angle glaucoma (in combination with myotics).

Contraindications

Bronchial asthma, sinus bradycardia, grade II and III atrioventricular block without pacemaker, decompensated chronic heart failure, cardiogenic shock, severe chronic obstructive pulmonary disease, sinus node weakness syndrome. hypersensitivity to the components of the drug.

With caution:

Cerebrovascular insufficiency, arterial hypotension, diabetes mellitus, hypoglycemia, pulmonary insufficiency, thyrotoxicosis, myasthenia gravis, sinoatrial blockade, peripheral circulatory disorders (including Rspo syndrome), pregnancy, simultaneous use of other beta-blockers.

Side effects

Adverse reactions that occur after oral use of timolol and other beta-blockers may also be considered potential side effects for timolol preparations in the dosage form of eye drops.

Adverse reactions, details of which were obtained during clinical trials and post-marketing surveillance of drugs Timo – l )La in the pharmaceutical form eye drops,

the Frequency of side effects identified during studies and ostmarka – t Sholom observation, was estimated as follows: very often (>1/10); often (>1/100 to <1/10), sometimes (>1/1000 to <1/100); rare (>1/10000 to <1/1000); very rare (<1/10000), frequency unknown (existing data can not be estimated).

General reactions

With unknown frequency: headache, asthenia/fatigue, chest pain.

From the side of the organ of vision

Often: blurred vision, pain in the eyes, burning and itching in the eyes, discomfort in the eye, conjunctival injection.

Infrequently: blepharitis, punctate keratitis, keratitis, conjunctivitis, iritis, diplopia, corneal erosion, corneal ulcer, lacrimation or reduced lacrimation, photophobia, a feeling of “sand” in the eyes, eyelid edema, conjunctival edema, ptosis.

Rare: uveitis, double vision, corneal pigmentation, erythema of the eyelids.

Very rare: development of corneal calcification with significant damage due to the presence of phosphates in the drops.

With unknown frequency: decreased corneal sensitivity, vascular wall detachment in the postoperative period of anti-glaucomatous surgery.

From the cardiovascular system Infrequently: bradycardia, hypotension.

Rare: myocardial infarction, low or high blood pressure, intermittent claudication.

With unknown frequency: cardiac arrest, atrioventricular block, arrhythmia, rapid heartbeat, congestive heart failure, Raynaud’s phenomenon.

From the digestive system Infrequently: dysgeusia.

Rarely: dyspepsia, dryness of the oral mucosa, abdominal pain.

With unknown frequency: nausea, vomiting, diarrhea.

Immune system disorders With unknown frequency: systemic lupus erythematosus.

Psychiatric disorders are Rare: depression.

With unknown frequency: insomnia, memory loss, nightmares.

From the nervous system Infrequently: headache.

Rare: cerebral ischemia, dizziness, migraine.

With unknown frequency: cerebrovascular accident, syncope, paresthesia, dizziness, worsening of myasthenia gravis.

From the side of the rut and subcutaneous tissues of the Psc: facial edema, erythema.

With unknown frequency: psoriasis or worsening of psoriasis, localized rash, alopecia.

Connective tissue disorders With unknown frequency: arthropathy. muscle pain.

Allergic reactions

With unknown frequency: systemic allergic reactions, including anaphylaxis, angioedema, urticaria, local or generalized rash, pruritus.

From the respiratory system and mediastinal organs Infrequently: respiratory failure, shortness of breath, bronchitis.

Rarely: bronchospasm (mainly in patients with pre – existing bronchospastic conditions), cough, nasal congestion, upper respiratory tract infections.

From the endocrine system

With unknown frequency: subclinical course of hypoglycemia in patients with diabetes mellitus (see section “Special instructions”).

From the genitourinary system

With unknown frequency: retroperitoneal fibrosis, sexual dysfunction (including impotence), decreased libido, Peyronie’s disease.

ENT disorders With unknown frequency: tinnitus.

Adverse reactions that occurred after taking timolol or other beta – a )blockers inside

Allergic reactions: erythematous rash, fever accompanied by sore throat, laryngosiasm accompanied by distress syndrome.

General reactions and reactions at the injection site: pain in the extremities, decreased exercise tolerance, weight loss.

From the side of the cardiovascular system: aggravation of arterial insufficiency, in po dilation.

From the digestive system: gastrointestinal ool. hepatomegaly. vomiting. mesenteric artery thrombosis, ischemic colitis.

From the blood and lymphatic system: non-thrombocytopenic purpura, thrombocytopenic purpura, agranulocytosis.

Endocrine system disorders: hyperglycemia, hypoglycemia.

From the skin and subcutaneous tissues: itching, skin irritation, increased pigmentation, sweating.

Musculoskeletal system disorders: arthralgia.

Nervous system disorders / psychiatric disorders: vertigo, decreased concentration of cognition, reversible depression of mental functions that progresses to catatonia, acute reversible syndrome characterized by disorientation in time and space, emotional lability, some difficulty in perception and reduced ability to perform neuropsychic tests.

Respiratory system disorders: wheezing, bronchial obstruction.

From the genitourinary system: difficulty urinating.

Interaction

Concomitant use of the drug with eye drops containing epinephrine may cause dilation of the pupil.

The specific effect of the drug is a decrease in intraocular pressure, which can increase with the simultaneous use of eye drops containing epinephrine and pilocarpine.

Two different adrenoblockers should not be placed in the same eye. Hypotension and bradycardia may worsen with concomitant use of the drug with cationic antagonists, reserpine and systemic beta-adrenoblockers.

CYP2D6 inhibitors, such as quinidine and cimetidip, may increase the plasma concentration of timolol.

Concomitant use with insulin or oral antidiabetic agents may result in hypoglycemia.

Timolol enhances the effect of muscle relaxants, so it is necessary to cancel the drug 48 hours before the planned surgical intervention under general anesthesia.

These data may also apply to medications that were used shortly before.

How to take, course of use and dosage

At the beginning of treatment,1-2 drops in the affected eye 2 times a day.

If intraocular pressure normalizes with regular use, the dose should be reduced to 1 drop 1 time a day in the morning. Doses exceeding 1 drop of 0.5% solution of ti-molol 2 times a day do not lead to an additional decrease in intraocular pressure. If the use of timolol does not achieve the required level of intraocular pressure, it is necessary to consider the use of additional antihypertensive drugs. Simultaneous use of two beta-blockers for topical use is not possible. Patients with a significantly pigmented iris may experience a less pronounced decrease in intraocular pressure. as well as a longer period of achieving intraocular pressure compensation. After discontinuation of treatment, the antihypertensive effect of timolol may persist

for several days, and in the case of prolonged previous treatment, the residual pensive effect may persist from 2 to 4 weeks. Antihypertensive effects may also occur in the contralateral eye during t-malol therapy only in one eye

.

Cantrol of the effectiveness of the drug is recommended to be carried out approximately 3-4 weeks after the start of therapy (not earlier than 1-2 weeks). With prolonged use of ti-m tlol, the effect may weaken.

Switching from another antihypertensive therapy:

When switching from therapy with one beta-adrenoblocker 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 timolol 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 one drop of 0.5% timolol solution in each affected eye twice a day.

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

Use in the pediatric population

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

If the benefits outweigh the risks, it is recommended to use timolol in the lowest possible available concentration,1 drop 1 time a day. If there is insufficient control of intraocular pressure, it is necessary to switch to the use of 2 times a day for

1 drop with an interval between instillations of 12 hours. Ocular and systemic side effects should be monitored for 1-2 hours after the first instillation, especially in newborns and children under 3 years of age, due to the possibility of developing apnea and breathing of the Cheyne-Stokes type. Parents of a child receiving timolol treatment should be warned that the drug should be discontinued if the child develops side effects from the respiratory system, in particular coughing and sneezing.

Treatment with Timolol is usually carried out for a long time. A break in treatment or a change in the dosage of the drug is carried out only on the instructions of the attending physician.

Overdose

It is possible to develop systemic effects characteristic of beta-blockers: dizziness, headache, arrhythmia, bradycardia, bronchospasm, nausea and vomiting, loss of consciousness, hypotension, shortness of breath, generalized convulsions, cardiogenic shock, heart failure and cardiac arrest.

In case of accidental ingestion of timolol, gastric lavage and use of activated charcoal are necessary. It is shown that the drug cannot be removed from the body by hemodialysis.

With the development of bradycardia and bradiarrhythmia (with atrioventricular block II and III degrees), intravenous use of atropine sulfate at a dose of 0.25 to 2 mg is recommended; and after partial relief of bradycardia, isoprenaline is indicated. If bradycardia is difficult to control, consider installing a pacemaker. For hypotension, it is recommended to take simiatomimetics, such as dopamine, dobutamine, and neradrenaline. In the absence of an effect-the introduction of glucagon.

With the development of acute heart failure, the use of digitalis preparations and diuretics, as well as oxygen therapy, is recommended; if ineffective, intravenous use of aminophylline is recommended.

Special instructions

In the postoperative period of anti-glaucomatous operations and with the use of drugs that reduce the secretion of intraocular fluid, detachment of the choroid of the eye may develop.

The use of timolol in patients with atopic or severe pathological reactions to various allergens in the anamnesis may provoke more severe reactions in response to accidental, diagnostic or therapeutic management of allergens. Such patients may not respond well to the use of conventional doses of epinephrine to stop anaphylactic reactions.

Beta-blockers can mask a number of clinical symptoms of hyperthyroidism (and in particular tachycardia). Caution is required when using beta-aarenoblockers in patients with the possibility of developing thyrotoxicosis.

In patients without a history of heart failure, prolonged myocardial depression can sometimes lead to the development of heart failure. If the first signs of heart failure occur, timolol should be discontinued. Caution should be exercised when prescribing timolol to patients with grade I atrioventricular block, Prinzmetal angina, and peripheral circulatory disorders (Raynaud’s phenomenon).

The main pathogenetic aspect of the treatment of closed-angle glaucoma is the need to open the angle of the anterior chamber, which is achieved by narrowing the pupil with the help of myotics. Due to the absence of the effect of timolol on the pupil diameter in the treatment of open-angle glaucoma, the drug can only be used in combination with myotics. Due to the possible effect of beta-blockers on blood pressure and heart rate, these drugs should be used with caution in patients with cerebral circulation insufficiency. If signs or symptoms of decreased cerebral circulation develop after starting timolol therapy, the need for local beta-blockers should be reviewed.

The use of timolol may increase muscle weakness in myasthenia gravis (eg. cause increased diplopia, ptosis, and general weakness). In some patients with myasthenia gravis and other myasthenic diseases, increased muscle weakness was observed with the use of timolol.

When used concomitantly with other medications, it is necessary to observe the interval between instillations of at least 15 minutes.

When applying the drug, it is necessary to monitor the function of the eye socket, the condition of the cornea, and evaluate the size of the visual fields at least once every 6 months.

The preparation contains the preservative benzalkonium chloride, which can cause eye irritation, be absorbed by soft contact lenses, causing discoloration and have an adverse effect on the eye tissue. Contact lenses should be removed before applying the drug and, if necessary, put them back on no earlier than 15 minutes after instillation.

With prolonged use of the drug, the toxic effect of the preservative benzalkonium chloride on the corneal epithelium (development of pinpoint keratopathy and/or toxic ulcerative keratopathy) is possible.

There were cases of bacterial keratitis in patients who used timolol in containers for multiple dosing of ophthalmic drugs. These containers were inadvertently contaminated by patients with concomitant corneal diseases.

When transferring patients to timolol treatment, it may be necessary to correct refractive changes caused by previously used myotics.

The drug, like other beta-blockers, can hide the possible symptoms of hypoglycemia in the blood of diabetic patients.

In case of an upcoming surgical intervention under general anesthesia, it is necessary to cancel the drug 48 hours before the operation, since it increases the effect of muscle relaxants and general anesthetics.

Influence on the ability to drive vehicles and mechanisms:

During treatment, 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 due to the profile of side effects (in particular, from the visual organ and nervous system).

Form of production

Eye drops 0.5% colorless, transparent or with a slightly brownish tinge.

Active ingredient

Timolol

Conditions of release from pharmacies

By prescription

Dosage form

eye drops

Purpose

For adults as directed by your doctor

Indications

Glaucoma