Timolol-Solofarm, eye drops 0.5% 5 ml

A nonselective beta-adrenoblocker.

When used topically in ophthalmology it reduces both normal and elevated intraocular pressure by reducing intraocular fluid formation and improving its outflow, has no effect on accommodation and pupil size.

It has antianginal, hypotensive and antiarrhythmic effects, which appear with systemic use. It reduces automatism of sinus node, decreases heart rate, slows down AV conduction, reduces contractility and myocardial oxygen demand.

Indications

Elevated intraocular pressure (ophthalmohypertension), open-angle glaucoma, glaucoma in the aphthous eye and other secondary glaucoma, congenital glaucoma (when other agents are not effective), as an additional means for reducing intraocular pressure in closed-angle glaucoma (in combination with myotics).

Active ingredient

Composition

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

Excipients:

benzalkonium chloride – 0.1 mg,

sodium dihydrophosphate dihydrate – 6.1 mg,

sodium hydrophosphate dihydrate – 15.16 mg,

water d/i – up to 1 ml.

How to take, the 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 once daily in the morning. Doses greater than 1 drop of 0.5% solution of timolol twice daily do not result in additional decrease of intraocular pressure. If intraocular pressure levels cannot be achieved with timolol administration, additional hypotensive drugs should be considered. Simultaneous use of two beta-adrenoblockers 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 time to achieve intraocular pressure compensation. After discontinuation of treatment, the hypotensive effect of timolol may persist for several days, and the residual p-potensive effect may persist for 2 to 4 weeks if prior treatment is prolonged. When Ti-melolol therapy is given in only one eye, hypotensive effects may also be noted in the contralateral eye.

Control of the efficacy of the drug is recommended approximately 3 to 4 weeks after initiation of therapy (at the earliest after 1-2 weeks). There may be a weakening of the effect with prolonged use of ti- mtlol.

Transition from other hypotensive therapy:

When switching from therapy with one beta-adrenoblocker to therapy with another drug from the beta-adrenoblocker group, it is recommended that you complete a full day of therapy with the previously p mented hypotensive agent and begin instillations of timolol 0.25% in each affected eye 1 drop 2 times daily the next day.

If therapy does not respond adequately, the dose may be increased to one drop of 0.5% timolol solution in each affected eye twice daily.

If therapy with a hypotensive drug other than a beta-adrenoblocker is switched to therapy, continue instillation of the previously-directed drug with the addition of instillations of one drop of 0.25% timololol solution in each affected eye twice daily. The next day, the previous treatment is withdrawn and timolol therapy is continued.

Paediatric use

Limolol may be recommended to decrease intraocular pressure in infantile and juvenile congenital glaucoma in the preoperative period or if surgical treatment has failed. Before using the drug, the risks and benefits of timolol in the pediatric population should be carefully evaluated through a thorough history of systemic abnormalities.

If the benefits outweigh the risks, the use of timolol at the lowest concentration available, 1 drop once daily, is recommended. If intraocular pressure control is insufficient, change to twice daily use of

1 drop with an interval of 12 hours between instillations. Ocular and systemic adverse events should be monitored for 1-2 hours after the first instillation, especially in infants and children under 3 years of age, due to the possibility of apnea and Cheyne-Stokes-type breathing. Parents of children treated with Timolol should be advised that the drug should be discontinued if the child develops respiratory side effects, particularly coughing and sneezing.

Timolol treatment is usually prolonged. Interruption of treatment or changes in the dosage of the drug are made only on the prescription of the treating physician.

Interaction

The co-administration 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 may increase with the simultaneous use of eye drops containing epinephrine and pilocarpine.

Two different runaway adrenoblockers should not be injected into the same eye. Arterial hypotension and bradycardia may worsen if the drug is used concomitantly with potassium antagonists, reserpine and systemic beta- and crenoblockers.

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

Simultaneous use with insulin or oral antidiabetic agents may lead to hypoglycemia.

Timolol increases the effects of muscle relaxants, therefore it is necessary to cancel the drug 48 hours before the planned surgery under general anesthesia.

This information may also apply to medications used shortly before.

Special Instructions

In the postoperative period of antiglaucomatous surgeries and when using drugs that reduce intraocular fluid secretion, an ocular vascular detachment may develop.

The use of timolol in patients with a history of atopy or severe pathological reactions to various allergens may provoke more severe reactions in response to accidental, diagnostic or therapeutic allergen management. Such patients may respond poorly to the administration of normal doses of epinephrine to control anaphylactic reactions.

Beta-adrenoblockers can mask a number of clinical symptoms of hyperthyroidism (particularly tachycardia). Caution is required when using beta-arenoblockers in patients with the possibility of thyrotoxicosis.

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

The main pathogenetic aspect of treating closed angle glaucoma is the need to open the anterior chamber angle, which is achieved by constricting the pupil with myotics. Due to the lack of influence of timolol on pupil diameter, the drug may be used only in combination with myotics in the therapy of angle-closure glaucoma. Due to the possible effect of beta-adrenoreceptor blockers on blood pressure and heart rate, these drugs should be used with caution in patients with cerebral circulatory insufficiency. If signs or symptoms of decreased cerebral circulation develop after initiation of timolol therapy, the need for therapy with local beta-adrenoblockers should be reconsidered.

The use of timolol may exacerbate muscle weakness in myasthenia gravis (e.g., cause increased diplopia, ptosis, and general weakness). Some patients with myasthenia gravis and other myasthenic diseases have shown increased muscle weakness when using timolol.

If used concomitantly with other drugs, an interval of at least 15 minutes between instillations should be observed.

When using it, visceral function, the condition of the cornea should be monitored and the visual fields should be assessed at least once every 6 months.

The product contains the preservative benzalkonium chloride which may irritate the eyes, be absorbed by soft contact lenses causing discoloration and have an adverse effect on ocular tissue. Contact lenses should be removed prior to application and reapplied, if necessary, no earlier than 15 minutes after instillation.

The preservative benzalkonium chloride may have a toxic effect on the corneal epithelium during long-term use (development of pitting keratopathy and/or toxic ulcerative keratopathy).

Cases of bacterial keratitis have been reported in patients who have used timolol in multi-dose ophthalmic drug containers. These containers were inadvertently contaminated by patients with concomitant corneal disease.

Patients transferring to timolol treatment may need to correct refractive changes caused by previously used myotics.

The drug, like other beta-adrenoblockers, may mask possible symptoms of hypoglycemia in diabetic patients.

If surgery is to be performed under general anesthesia, the drug should be discontinued 48 hours prior to surgery, since it potentiates the effects of muscle relaxants and general anesthetics.

The effect on the ability to operate vehicles and mech:

At the time of treatment, caution should be exercised when driving and engaging in other potentially hazardous activities requiring increased concentration and quick psychomotor reactions due to the profile of adverse events (particularly those involving the visual and nervous system).

Contraindications

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

With caution:

Cerebrovascular insufficiency, arterial hypotension, diabetes mellitus, hypoglycemia, pulmonary insufficiency, thyrotoxicosis, myasthenia gravis, sinoatrial blockade, peripheral circulation disorders (including Psypo syndrome), pregnancy, simultaneous administration of other beta-adrenoblocarb.

Side effects

Indesirable reactions after oral administration of timolol and other beta-adrenoblockers may be considered as potential adverse reactions also for timolol prefat in the dosage form of eye drops.

Unwanted reactions reported in clinical studies and in post-marketing follow-up of timolol dosage form eye drops

The frequency of adverse reactions reported in both studies and post-marketing follow-up were evaluated as follows: very often (>1/10); often (>1/100 to <1/10); sometimes (>1/1000 to <1/100); rarely (>1/10000 to <1/1000); very rarely (<1/10000), frequency unknown (available data cannot be estimated).

General reactions

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

Visual side

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

Infrequent: blepharitis, pitting keratitis, keratitis, conjunctivitis, iritis, diplopia, corneal erosion, corneal ulceration, lacrimation or decreased lacrimation, photophobia, sensation of “sand” in eyes, edema, conjunctival edema, ptosis.

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

very rarely: development of corneal calcification if the cornea is significantly damaged due to the presence of phosphates in the drops.

With unknown frequency: decreased corneal sensitivity, detachment of the vascular rim in the postoperative period of antiglaucomatous surgery.

Cardiovascular system disorders Infrequent: bradycardia, hypotension.

Rarely: myocardial infarction, decreased or increased blood pressure, intermittent claudication.

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

Digestive system disorders Infrequent: dysgeusia.

Rarely: dyspepsia, dry mouth, abdominal pain.

With unknown frequency: nausea, vomiting, diarrhea.

Immune system disorders With unknown frequency: systemic lupus erythematosus.

Mental disorders Rarely: depression.

With unknown frequency: insomnia, memory loss, nightmares.

Nervous system disorders Infrequent: headache.

Rarely: cerebral ischemia, dizziness, migraine.

With unknown frequency: impaired cerebral circulation, fainting, paresthesia, dizziness, aggravation of the course of myasthenia gravis.

Particular rash and subcutaneous tissues: facial edema, erythema.

With unknown frequency: psoriasis or worsening of the course of psoriasis, localized rash, and 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. itching.

Respiratory system and mediastinal organs Infrequent: respiratory failure, shortness of breath, bronchitis.

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

Endocrine system disorders

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

Urogenital system disorders

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

ENT Organs With unknown frequency: tinnitus.

Unwanted reactions that have occurred after taking timolol or other oral beta- a )reblockers

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

General reactions and reactions at the site of administration: pain in the extremities, decreased tolerance to physical activity, decreased body weight.

Cardiovascular system: aggravation of arterial insufficiency, in dilatation.

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

In the blood and lymphatic system: nonthrombocytopenic purpura, thrombocytopenic purpura, agranulocytosis.

Endocrine system disorders: hyperglycemia, hypoglycemia.

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

Skeletal and muscular system disorders: arthralgia.

Nervous system disorders/psychiatric disorders: vertigo, decreased concentration of charge, reversible suppression of mental functions progressing to catatonia, acute reversible syndrome characterized by impaired orientation in time and space, emotional lability, some difficulty in perception and decreased ability to perform neuropsychological tests.

Respiratory system: wheezing, bronchial obstruction.

He urinary system: difficulty in urination.

Overdose

The following systemic effects characteristic of beta-adrenoblockers may develop: 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 administration of activated charcoal are necessary. It has been shown that the drug cannot be removed from the body by hemodialysis.

In case of bradycardia and bradyarrhythmia (in degree II and III atrioventricular block), intravenous administration of atropine sulfate at a dose of 0.25 to 2 mg is recommended; and isoprenaline is indicated to relieve bradycardia partially. If bradycardia is difficult to relieve, a pacemaker should be considered. In hypotension, administration of simiatomimetics, such as dopamine, dobutamine, neradrenaline is recommended. If there is no effect, administration of glucagon.

In the development of acute heart failure, use of foxglove drugs and diuretics is recommended, as well as oxygen therapy; if ineffective, intravenous aminophylline administration is recommended.

Similarities