Fotil forte eye drops 40mg/ml + 5mg/ml, 5ml

Composition

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

5 mg of pilocarpine,

40 mg hydrochloride

Auxiliary substances:

benzalkonium chloride – 0.1 mg,

citric acid-0.88 mg,

sodium citrate-6.13 mg,

hypromellose-5 mg,

d/i water-up to 1 ml

Pharmacological action

The combined preparation contains two active ingredients. Pilocarpine in the form of eye drops causes a narrowing of the pupil and a spasm of accommodation, and also lowers intraocular pressure by contracting the ciliary muscle and the iris muscle, which facilitates the outflow of watery moisture from the anterior chamber of the eye. The effect of pilocarpine occurs in 30 minutes and lasts 4-14 hours, with a half-life of 1.5 to 2.5 hours. The substance is not metabolized, it is excreted with watery moisture.

Timolol is a beta-blocker that reduces intraocular pressure and reduces the production of watery moisture by the visual organ. It acts mainly on the ciliary body. Slows down the process of removing pilocarpine with watery moisture. Its half-life is less than 30 minutes. Reduces intraocular pressure 2 hours after instillation in the eyes. The maximum effect should be expected in 4 hours, the action lasts from 10 to 20 hours.

Pharmacokinetics

Pilocarpine penetrates well through the cornea. The concentration in the aqueous humor reaches its maximum after 30 minutes. Pilocarpine binds to many eye tissues. T1 / 2 from the eye media is 1.5-2.5 h. Pilocarpine is excreted unchanged with intraocular fluid.

Its combination with timolol, which reduces the formation of watery moisture, slows down the rate of elimination of pilocarpine.

Pilocarpine is rapidly hydrolyzed to inactive forms in the blood plasma and liver. T1 / 2 is less than 0.5 h.

Timolol quickly penetrates through the cornea into the watery moisture of the anterior chamber of the eye. About 80% of topically applied timolol penetrates the systemic circulation. Cmax in blood plasma is determined approximately 1 h after the eye drops are inserted.

It is mainly metabolized in the liver. T1 / 2 is 2-5 hours. It is excreted mainly through the kidneys.

Indications

• Open-angle and closed-angle glaucoma.
• Glaucoma associated with aphakia.
• Secondary glaucoma.
• Increased intraocular pressure in the postoperative period.
• Glaucoma after cataract surgery.
• Marked increase in intraocular pressure with a risk of eye damage (including as part of combined anti-glaucoma therapy).

Use during pregnancy and lactation

To date, there have not been sufficiently adequate and strictly controlled studies in pregnant women.

The use of Fotil during pregnancy and lactation is possible only if the intended benefit to the mother exceeds the potential risk to the fetus.

In experimental studies, no negative effect of timolol on fertility was found.

Currently, there is no evidence that pilocarpine has a teratogenic effect in the treatment of glaucoma in humans.

 Use in children

 Contraindication: children under 18 years of age (due to the lack of data on the effectiveness and safety of the drug in children and adolescents).

Contraindications

• anterior uveitis;
• sinus bradycardia;
• AV-block II and III degree;
• decompensated heart failure;
• cardiogenic shock;
• bronchial asthma;
• COPD;
• childhood and adolescence to 18 years (due to a lack of data on efficacy and safety of the drug in children and adolescents);
• state immediately after eye surgery and other eye diseases in which the constriction of the pupil is undesirable;
• hypersensitivity to the components of the drug.

With caution, it is prescribed for hypoglycemia, cerebrovascular disorders, heart failure, diabetes mellitus, thyrotoxicosis, cerebrovascular disorders, as well as before surgery, in which general anesthesia is planned.

Side effect

Local reactions: blurred vision, eye irritation, momentary burning sensation and pain in the eye, increased tearing, dry eye syndrome, dermatitis of the eyelids, redness of the conjunctiva, a spasm of the ciliary muscle and induced myopia, reduced visual acuity in low light (due to miosis), decreased sensitivity of the cornea, point, keratitis, allergic blepharoconjunctivitis; very rare – diplopia, ptosis.

Several cases of retinal detachment, iris rigidity, or cyst formation in the iris have been reported in connection with the use of myotic agents. With prolonged use of pilocarpine, reversible opacity of the lens was observed.

Systemic reactions: nausea, diarrhea, increased sweating, increased salivation, decreased blood pressure, exacerbation of bronchial asthma, heart failure, bradycardia, arrhythmia, temporal and supraorbital headaches, skin rash.

Timolol penetrates the BBB and affects the central nervous system.

In all patients with heart failure, timolol may cause asthenic syndrome, nausea, dizziness, anxiety, hallucinations, headache, and depression.

Nasal congestion was very rare.

Interaction

The active components of the drug increase the likelihood of developing AV conduction disorders, and in combination with reserpine, they contribute to the development of arterial hypotension, a decrease in heart rate, and dizziness.

When taken concomitantly with systemic beta-blockers, their pharmacological effect increases, so the combination is not recommended.

Inhibitors of the CYP2D6 isoenzyme, such as quinidine and cimetidine, can increase the concentration of timolol in plasma.

How to take, course of use and dosage

Assign 1 drop of the drug Fotil (Fotil drops of ocular fl. – drops of 5 ml cor. 1 Centen AO) to the affected eye 2 times / day.

In some patients, a stable decrease in intraocular pressure is achieved only after a few weeks of therapy. Therefore, when evaluating the results of treatment, intraocular pressure should be measured approximately 4 weeks after the start of treatment. If the expected decrease in intraocular pressure does not occur, then Fotil forte should be prescribed 1 drop 2 times a day.

Overdose

An overdose of Fotil eye drops causes a slowing of the heart rate, a decrease in blood pressure, acute heart failure, and bronchospasm.

Overdose is treated symptomatically. Atropine can be used as an antidote to pilocarpine. Intravenous isoprenaline is indicated for severe bradycardia and bronchospasm; dobutamine is indicated for hypotension.

Special instructions

Do not use Fotil forte simultaneously with other eye drops containing beta-blockers.

You should stop using other eye drops before using Fotil. If anti-glaucoma agents were used, they are canceled, and Fotil drops are started from the next day.

Evaluation of the effectiveness of the drug should be carried out 4 weeks after the start of treatment with regular monitoring of intraocular pressure.

Further treatment should also be carried out with regular monitoring of intraocular pressure.

The drug is instilled by removing contact lenses, since Fotil forte eye drops contain benzalkonium chloride as a preservative. You can install them in your eyes 15 minutes after using eye drops.

Timolol, which is part of the drug, can mask the symptoms of hypoglycemia in patients with diabetes mellitus or symptoms of hyperthyroidism.

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

Influence on the ability to drive motor vehicles and manage mechanisms

The myotic effect can cause temporary visual impairment (a feeling of nearsightedness), so during treatment, care should be taken when driving vehicles or operating any complex equipment that requires increased concentration of attention and speed of psychomotor reactions.

Form of production

Eye drops in the form of a clear, colorless solution.

Storage conditions

The drug should be stored out of the reach of children at a temperature of 2° to 8°C. After opening the package – at a temperature not exceeding 25°C.

Shelf

life is 3 years. After opening the package – 1 month.

Active ingredient

Pilocarpine, Timolol

Conditions of release from pharmacies

By prescription

Dosage form

eye drops

Purpose

Nursing mothers as prescribed by a doctor, Adults as prescribed by a doctor, Pregnant Women as prescribed by a doctor

Indications

Glaucoma