Timolol-solofarm drops hl. 0.5% 5ml fl cap. 1 PC
Adverse reactions that occur after oral administration of timolol and other beta-blockers can be regarded as potential adverse reactions for timolol preparations in the dosage form of eye drops. Adverse reactions, information about which was obtained during clinical trials and during post-marketing surveillance of timolol medicinal products in the dosage form of eye drops
The frequency of side effects identified both during studies and during post-marketing surveillance was assessed as follows: very common (>1/10); often (>1/100 to 1/1000 to 1/10000 to
General reactions
With unknown frequency: headache, asthenia/fatigue, chest pain.
From the side of the organ of vision
Common: blurred vision, eye pain, burning and itching of the eyes, eye discomfort, conjunctival injection.
Uncommon: blepharitis, punctate keratitis, keratitis, conjunctivitis, iritis, diplopia, corneal erosion, corneal ulcer, lacrimation or decreased lacrimation, photophobia, feeling of “sand” in the eyes, eyelid edema, conjunctival edema, ptosis.
Rarely: uveitis, double vision, corneal pigmentation, eyelid erythema.
Very rare: development of corneal calcification with significant damage due to the presence of phosphates in the drops.
With unknown frequency: decreased sensitivity of the cornea, detachment of the choroid in the postoperative period of antiglaucomatous surgery.
From the cardiovascular system
Uncommon: 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.
From the digestive system
Uncommon: dysgeusia.
Rarely: dyspepsia, dry oral mucosa, abdominal pain.
With unknown frequency: nausea, vomiting, diarrhea.
From the immune system
With unknown frequency: systemic lupus erythematosus.
Mental disorders
Rarely: depression.
With unknown frequency: insomnia, memory loss, nightmares.
From the nervous system
Uncommon: headache.
Rarely: cerebral ischemia, dizziness, migraine.
With unknown frequency: cerebrovascular accident, fainting, paresthesia, dizziness, worsening myasthenia gravis.
From the skin and subcutaneous tissues
Rarely: facial swelling, erythema.
Not known: psoriasis or worsening of psoriasis, localized rash, alopecia.
From the connective tissue side
Not known: arthropathy, muscle pain.
Allergic reactions
With unknown frequency: systemic allergic reactions, including anaphylaxis, angioedema, urticaria, local or generalized rash, itching.
From the respiratory system and mediastinal organs
Uncommon: respiratory failure, shortness of breath, bronchitis.
Rarely: bronchospasm (mainly in patients with existing bronchospastic conditions), cough, nasal congestion, upper respiratory tract infections.
From the endocrine system
With unknown frequency: subclinical hypoglycemia in patients with diabetes mellitus (see section "Special Instructions").
From the genitourinary system
Not known: retroperitoneal fibrosis, sexual dysfunction (including impotence), decreased libido, Peyronie's disease.
From the ENT organs
With unknown frequency: ringing in the ears.
Adverse reactions that occurred after taking timolol or other beta-blockers orally
Allergic reactions: erythematous rash, fever accompanied by sore throat, laryngospasm accompanied by distress syndrome.
General reactions and reactions at the injection site: pain in the extremities, decreased exercise tolerance, weight loss.
From the cardiovascular system: worsening arterial insufficiency, vasodilation.
From the digestive system: gastrointestinal pain, hepatomegaly, vomiting, thrombosis of mesenteric arteries, ischemic colitis.
From the blood and lymphatic system: non-thrombocytopenic purpura, thrombocytopenic purpura, agranulocytosis.
From the endocrine system: hyperglycemia, hypoglycemia.
From the skin and subcutaneous tissues: itching, skin irritation, increased pigmentation, sweating.
From the musculoskeletal system: arthralgia.
Nervous system/mental disorders: vertigo, decreased concentration, reversible depression of mental functions progressing to catatonia, acute reversible syndrome characterized by impaired orientation in time and space, emotional lability, some difficulty perceiving and reduced ability to perform neuropsychological tests.
From the respiratory system: wheezing, bronchial obstruction.
From the genitourinary system: difficulty urinating.
Timolol-pos 0.25% 10ml eye drops without preservatives
pharmachologic effect
Antiglaucoma.
Composition and release form Timolol-pos 0.25% 10ml eye drops without preservatives
Drops - 1 ml:
- Active substance: Timolol maleate 3.42/6.84 mg (corresponding to 2.5/5 mg timolol);
- Excipients: sodium dihydrogen phosphate dihydrate; sodium hydrogen phosphate dodecahydrate; water for injections.
Eye drops (without preservative), 0.5%. 10 ml in a multi-dose plastic dropper bottle. The bottle is placed in a cardboard box.
Description of the dosage form
Transparent, colorless solution.
Directions for use and doses
Conjunctivally.
For newborns and children under 10 years of age: instill 1 drop of a 0.25% solution 2 times a day.
Adults and children over 10 years of age: instill 1 drop of a 0.25% solution into the conjunctival sac 2 times a day; if the effectiveness is insufficient, 1 drop of a 0.5% solution 2 times a day. If necessary, the dose can be reduced to 1-2 drops 1 time per day.
- Before each instillation, you need to remove the protective cap;
- Before using the drug for the first time, turn the bottle over with the dropper vertically down and press on its base (bottom) several times until the first drop appears at the tip of the dropper. After this, the bottle is ready for further use;
- When instilling the drug, hold the bottle with the dropper down, quickly and vigorously pressing on its base (bottom). Thus, the dropper mechanism is activated and only one drop of the drug is extracted. The special design of the dropper valve system always ensures the same size of the extracted drop and the same speed of its extraction, even with very strong pressure on the base of the bottle;
- tilt your head back a little, slightly move your lower eyelid with your finger and drop 1 drop into the conjunctival sac as described above. Slowly close your eyes. When instilling, avoid contact of the tip of the dropper with the surface of the eye and skin;
- after completing the procedure, immediately put a protective cap on the dropper;
Pharmacodynamics
Non-selective beta-adrenergic receptor blocker without sympathomimetic activity. When applied topically, it lowers IOP by reducing the formation of aqueous humor and slightly increasing its outflow. The effect appears 20 minutes after instillation, the maximum effect occurs after 1-2 hours; duration of action - 24 hours.
Pharmacokinetics
Timolol maleate quickly penetrates the cornea into the eye tissue. In small quantities it enters the systemic circulation by absorption through the conjunctiva, nasal mucosa and lacrimal tract. Excretion of metabolites by the kidneys. In newborns and young children, the concentration of the active substance in plasma significantly exceeds its Cmax in the plasma of adults.
Indications for use Timolol-pos 0.25% 10ml eye drops without preservatives
- Primary open-angle glaucoma;
- secondary glaucoma (uveal, aphakic, post-traumatic);
- congenital glaucoma (if other therapeutic measures are ineffective);
- acute increase in ophthalmotonus;
- primary angle-closure glaucoma (in combination with miotics).
Contraindications
- Hypersensitivity to the components of the drug;
- severe chronic obstructive pulmonary disease, incl. bronchial asthma;
- sinus bradycardia (slow heartbeat);
- atrioventricular block, II and III degree block;
- acute and chronic heart failure of II and III degrees;
- cardiogenic shock;
- dystrophic diseases of the cornea;
- severe vasomotor rhinitis.
Use of Timolol-pos 0.25% 10ml eye drops without preservatives during pregnancy and breastfeeding
During pregnancy, the drug is used if the expected benefit to the mother outweighs the potential risk to the fetus. Breastfeeding should be stopped while using the drug.
special instructions
Monitoring of effectiveness should be carried out approximately 3-4 weeks after the start of therapy. During the treatment period, tear function, corneal integrity, and visual fields should be monitored at least once every 6 months.
Contact lenses should be removed before instillation and put on no earlier than 15 minutes after it.
With long-term use of the drug Timolol-POS, the effect may weaken.
Before an upcoming surgical intervention using general anesthesia, the drug should be discontinued 48 hours before.
The original design of the dropper bottle, operating on the principle of an airless pump, does not allow outside air to penetrate into the bottle and thereby ensures the sterility of eye drops in the absence of a preservative.
The use of the drug Timolol-POS allows you to avoid unwanted effects of the preservative on the external tissues of the eye, conjunctiva and cornea, and also eliminates the risk of developing allergic reactions to the preservative.
After opening the bottle and instilling the drug Timolol-POS for the first time, it can be used for 12 weeks. To do this, it is necessary to mark the date of first use of the drug on the bottle and/or on the cardboard box. On the label of the bottle and on the cardboard box there is a special column for the patient to fill out - “Date of first use”.
After using the contents of the bottle, you should purchase a new bottle of the drug; the used bottle is not intended for reuse and must be disposed of (the used bottle must be thrown into the trash).
Impact on the ability to drive vehicles and operate machinery. During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions and good vision (within 0.5 hours after instillation into the eye).
Overdose
When applied topically at the recommended dose, no overdose symptoms were observed.
Symptoms (if accidentally ingested): nausea, vomiting, dizziness, headache, decreased blood pressure, bronchospasm, bradycardia.
Treatment: symptomatic. Isoprenaline can be administered intravenously to eliminate severe bradycardia or bronchospasm, and dobutamine can be administered to treat arterial hypotension.
Side effects Timolol-pos 0.25% 10ml eye drops without preservatives
Local reactions:
Eye irritation, manifested in the form of conjunctivitis, blepharitis, keratitis (hyperemia of the eyelid skin, burning and itching in the eyes, conjunctival hyperemia, lacrimation or decreased lacrimation, photophobia, swelling of the corneal epithelium, short-term impairment of visual acuity; with long-term use, the development of superficial punctate keratopathy is possible ( decreased corneal transparency and decreased corneal sensitivity), ptosis, diplopia.
Systemic reactions:
From the cardiovascular system: decreased blood pressure, bradycardia, bradyarrhythmia, AV block, heart failure, cardiac arrest, decreased myocardial contractility, chest pain, transient cerebrovascular accident, collapse.
From the respiratory system: shortness of breath, bronchospasm, pulmonary failure.
From the side of the central nervous system: dizziness, headache, drowsiness, hallucinations, slowdown in the speed of psychomotor reactions.
Other side effects: allergic reactions (including urticaria), rhinitis, nasal congestion, nosebleeds, nausea, vomiting, diarrhea, paresthesia, muscle weakness, sexual dysfunction, depression.
Drug interactions
Epinephrine, pilocarpine, systemic beta-blockers enhance the effect.
When used with reserpine, severe bradycardia or hypotension may develop (this combination requires careful medical supervision).
When combined with CCBs or cardiac glycosides, AV conduction disturbance, acute left ventricular failure or arterial hypotension are possible.
Enhances the effect of muscle relaxants - Timolol-POS should be discontinued 48 hours before the intended general anesthesia with the use of peripheral muscle relaxants.
Cannot be used simultaneously with antipsychotic drugs (neuroleptics) and anxiolytic drugs (tranquilizers).
During treatment, it is not recommended to take ethanol (a sharp decrease in blood pressure is possible).
Prescribe with caution simultaneously with antihypertensive drugs, other beta-blockers, insulin or oral hypoglycemic drugs, corticosteroids, and psychoactive drugs.
Timolol maleate
Like other ophthalmic drugs, timolol undergoes systemic absorption.
When beta-blockers are used topically, the same adverse reactions may occur as when they are used systemically. For example, severe respiratory reactions and cardiac events have been reported with both systemic and topical use of timolol, including death due to bronchospasm in patients with bronchial asthma and, less commonly, death due to heart failure (see section "Contraindications"). .
Heart failure
To maintain blood circulation in persons with impaired myocardial contractility, sympathetic stimulation is necessary. The use of beta-blockers may aggravate the course of heart failure.
In patients without a history of heart failure, long-term myocardial suppression with beta-blockers may in some cases lead to the development of heart failure. When the first signs of heart failure occur, timolol should be discontinued.
Chronic obstructive pulmonary disease
Patients with COPD (for example, chronic bronchitis, emphysema) of mild to moderate severity, bronchospastic diseases, including a history (other than bronchial asthma (including a history), in which the use of timolol is contraindicated), the use of beta-blockers, in including timolol, is generally not recommended.
Extensive surgical interventions
The need and desirability of discontinuing beta-blockers before undergoing major surgery has not been definitively established. Beta-adrenergic receptor blockade impairs the heart's ability to respond to beta-adrenergic receptor-mediated reflex stimuli, which may increase the risk of complications of general anesthesia.
In some patients who continued the use of beta-blockers during general anesthesia, a prolonged severe decrease in blood pressure occurred. The difficulty of resuming and maintaining heart contractions was also noted. In this regard, patients referred for elective operations are advised to gradually discontinue the use of beta-blockers. During surgery, if necessary, the effects of beta-blockers are stopped by high doses of adrenergic agonists.
Diabetes
Patients with spontaneous hypoglycemia or diabetes mellitus (especially those with an unstable course) using insulin or oral hypoglycemic agents should use beta-blockers with caution. Beta blockers may mask the signs and symptoms of acute hypoglycemia.
Thyrotoxicosis
Beta blockers can mask certain clinical symptoms of hyperthyroidism (for example, tachycardia). The use of beta-blockers in patients who may develop thyrotoxicosis should be used with caution, avoiding abrupt withdrawal, in order to prevent the development of thyrotoxic crisis.
General recommendations
Due to the potential effect on blood pressure and heart rate, beta blockers should be used with caution in patients with cerebrovascular insufficiency. If symptoms of cerebrovascular accident develop after initiation of timolol therapy, alternative therapies should be considered.
Cases of bacterial keratitis associated with the use of multi-dose containers for ophthalmic drugs have been described. These containers were unintentionally contaminated by patients who, in most cases, had concomitant corneal diseases or disruption of the integrity of the epithelial surface of the eyeball.
In patients taking medications that reduce the formation of intraocular fluid (for example, timolol), cases of choroidal detachment after filtration surgery have been reported.
Angle-closure glaucoma
The main goal of treatment for patients with angle-closure glaucoma is to open the angle of the eye, which requires contraction of the pupil. Timolol does not affect the pupil, therefore the use of timolol in monotherapy for the treatment of angle-closure glaucoma is not allowed.
Anaphylaxis
The use of beta-blockers in patients with atopy or a history of severe anaphylactic reactions to various allergens may provoke more severe reactions in response to accidental, diagnostic or therapeutic administration of allergens. Such patients may respond poorly to normal doses of epinephrine to relieve anaphylactic reactions.
Muscle weakness
The use of beta-blockers increases muscle weakness in myasthenia gravis (for example, increased diplopia, ptosis and general weakness). Some patients with myasthenia gravis and other myasthenic diseases have experienced an increase in muscle weakness when taking timolol.
Excipients
Timolol maleate contains benzalkonium chloride, which can cause eye irritation, be absorbed by soft contact lenses, causing discoloration, and have adverse effects on eye tissue. Before using the drug, contact lenses should be removed and reinserted if necessary, no earlier than 15 minutes after instillation.
