Fotil^® (Drops) Instructions for Use

ATC Code

S01EB51 (Pilocarpine in combination with other drugs)

Active Substances

Pilocarpine (BAN)

Timolol (Rec.INN)

Clinical-Pharmacological Group

Antiglaucoma drug

Pharmacotherapeutic Group

Combined antiglaucoma agent (M-cholinomimetic + beta-adrenergic blocker)

Pharmacological Action

Combined antiglaucoma drug.

Pilocarpine is an M-cholinomimetic.

When instilled into the eye, pilocarpine causes miosis, spasm of accommodation, and reduces intraocular pressure.

The reduction in intraocular pressure is due to the contraction of the ciliary muscle and the iris muscle, which leads to the widening of the anterior chamber angle and changes the physical structure of the trabecular meshwork, facilitating the outflow of aqueous humor.

This effect lasts from 4 hours to 14 hours.

Timolol, being a beta-adrenergic blocker, prevents the binding of sympathomimetic neurotransmitters to β₁– and β₂-adrenergic receptors in the ciliary body.

It reduces intraocular pressure by decreasing the production of aqueous humor.

The hypotensive effect occurs 20 minutes after instillation, reaches its maximum after 2 hours, and lasts about 24 hours.

Pharmacokinetics

Pilocarpine

Absorption

It penetrates the cornea well.

The concentration in the aqueous humor reaches its maximum after 30 minutes.

Pilocarpine binds to many eye tissues.

Metabolism and Excretion

T_1/2 from the eye media is 1.5-2.5 hours.

Pilocarpine is excreted unchanged in the intraocular fluid.

Its combination with timolol, which reduces the formation of aqueous humor, slows down the rate of pilocarpine excretion.

Pilocarpine is rapidly hydrolyzed into inactive forms in the blood plasma and liver.

T_1/2 is less than 0.5 hours.

Timolol

Absorption

It rapidly penetrates the cornea into the aqueous humor of the anterior chamber of the eye.

About 80% of topically applied timolol enters the systemic circulation.

C_max in blood plasma is determined approximately 1 hour after instillation of the eye drops.

Metabolism and Excretion

It is metabolized mainly in the liver.

T_1/2 is 2-5 hours.

It is excreted primarily through the kidneys.

Indications

Glaucoma or elevated intraocular pressure when a combination of timolol and pilocarpine is necessary

• Open-angle glaucoma;
• Angle-closure glaucoma;
• Secondary glaucoma;
• Elevated intraocular pressure after ophthalmic surgeries.

ICD codes

Dosage Regimen

Drops

The drug is prescribed as 1 drop into the affected eye 2 times/day.

In some patients, a stable reduction in intraocular pressure caused by the use of Fotil^® is achieved only after several weeks of therapy.

Therefore, when evaluating treatment results, intraocular pressure should be measured approximately 4 weeks after the start of treatment.

If the expected reduction in intraocular pressure does not occur during treatment with Fotil^® eye drops, it is recommended to continue treatment with Fotil^® forte eye drops, 1 drop 2 times/day.

Adverse Reactions

Local reactions blurred vision, eye irritation, transient burning sensation and eye pain, increased lacrimation, dry eye syndrome, eyelid dermatitis, conjunctival redness, ciliary muscle spasm and induced myopia, decreased visual acuity in low light (due to miosis), decreased corneal sensitivity, punctate keratitis, allergic blepharoconjunctivitis; very rarely – diplopia, ptosis.

Several cases of retinal detachment, iris rigidity, or cyst formation in the iris have been noted in connection with the use of miotic agents.

Reversible lens opacity was observed with prolonged use of pilocarpine.

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

Timolol penetrates the BBB and affects the CNS.

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

Very rarely, nasal congestion was noted.

Contraindications

• Anterior uveitis;
• Sinus bradycardia;
• Second- and third-degree AV block;
• Decompensated heart failure;
• Cardiogenic shock;
• Bronchial asthma;
• COPD;
• Children and adolescents under 18 years of age (due to the lack of data on the efficacy and safety of the drug use in children and adolescents);
• The condition immediately after ophthalmic surgeries and other eye diseases in which pupil constriction is undesirable;
• Hypersensitivity to the drug components.

With caution, the drug should be prescribed for heart failure, cerebrovascular disorders, diabetes mellitus, hypoglycemia, thyrotoxicosis, retinal detachment, myopia, before surgical operations under general anesthesia.

Use in Pregnancy and Lactation

The use of Fotil^® forte during pregnancy and breastfeeding is possible only if the intended benefit to the mother outweighs the potential risk to the fetus and child.

Pediatric Use

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

Special Precautions

Fotil^® forte eye drops should not be used simultaneously with other eye drops containing beta-adrenergic blockers.

The use of other eye drops should be discontinued before starting therapy with Fotil^® forte.

The previous antiglaucoma drug should be discontinued, and therapy with Fotil^® forte eye drops should be started the next day.

The evaluation of the drug’s efficacy 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.

Fotil^® forte eye drops contain benzalkonium chloride as a preservative and are not recommended for use when wearing contact lenses.

Before using the drug, contact lenses should be removed and reinserted no earlier than 15 minutes after instillation of the drug.

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 upcoming surgery under general anesthesia, Fotil^® forte should be discontinued 48 hours before surgery, because the drug enhances the effect of muscle relaxants and general anesthetics.

Effect on the ability to drive vehicles and operate machinery

The miotic effect can cause transient visual impairment (a feeling of myopia), so during the treatment period, caution should be exercised when driving a car or operating any complex equipment requiring increased concentration and speed of psychomotor reactions.

Overdose

Symptoms bradycardia, decreased BP, bronchospasm, acute heart failure.

Treatment symptomatic therapy is carried out.

Atropine can be used as an antidote for pilocarpine.

The administration of isoprenaline IV is indicated for severe bradycardia, bronchospasm; dobutamine – for arterial hypotension.

Drug Interactions

With simultaneous use with drugs that promote the release of catecholamines (for example, with reserpine), in isolated cases, arterial hypotension (including orthostatic), bradycardia, and dizziness were observed.

Simultaneous use of beta-adrenergic blockers and systemic slow calcium channel blockers leads to an enhancement of their pharmacological effect and increases the risk of cardiac conduction disorders and arterial hypotension.

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

Storage Conditions

The drug should be stored out of the reach of children at a temperature from 2°C (35.6°F) to 8°C (46.4°F).

Shelf Life

Shelf life – 3 years.

After opening the package, the drug can be stored at a temperature not exceeding 25°C (77°F).

The shelf life after opening the bottle is 1 month.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.