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Santen Brand: Santen

Pharmacological properties

Fotil and fotil forte are a combination of pilocarpine and timolol, drugs that reduce intraocular pressure.
Chemical name of pilocarpine: 3 - ethyl-4 - [(1-methylimidazol-5-yl) methyl] tetrahydrofuran-2-one. Used in the form of hydrochloride. Chemical name of timolol maleate: (S) -1- [1,1-dimethylethyl) amino] -3 [[4- (4-morpholinyl) -1,2,5-thiadiazol-3-yl] -oxy] -2- propanol. (Z) -butenedioate (1: 1) salt. The structure of the compound contains an asymmetric carbon atom, and the levorotatory isomer of the compound is included in the Fotil eye drops.
Pilocarpine is a parasympathomimetic, a stimulant of M-cholinergic receptors. When instilled in the eyes, it reduces intraocular pressure, causes miosis and spasm of accommodation. A decrease in intraocular pressure is achieved by contraction of the ciliary and circular muscles of the iris, which is accompanied by an increase in the angle of the anterior chamber of the eye and changes the organization of the trabecular tissue, thus facilitating the outflow of aqueous humor. When instilling a solution of pilocarpine into the eye, the drug penetrates well into the cornea. Its maximum concentration in aqueous humor is reached after 30 minutes. It spreads in the tissues of the eye, the half-life of them is 1.5–2.5 hours. The spasm of accommodation and constriction of the pupil are observed 10 minutes after instillation and persist for 1–2 hours. The decrease in intraocular pressure persists for several hours. Pilocarpine is not metabolized in aqueous humor, but is eliminated with its outflow. The simultaneous use of timolol, which reduces the production of aqueous humor, reduces the rate of elimination of pilocarpine. Resorbed pilocarpine in the blood and liver tissue is hydrolyzed to inactive metabolites. The half-life of blood plasma is 30 minutes.
Timolol is a β-adrenergic receptor blocker that effectively inhibits the interaction of sympathomimetic neurotransmitters with β1- and β2-adrenergic receptors. Reduces intraocular pressure by reducing the production of aqueous humor. Acts on β2-adrenergic receptors of the ciliary body.
It does not possess ICA, local anesthetic (membrane stabilizing) effect, does not affect blood circulation in the retina. When the eyes are instilled, a certain amount of timolol is resorbed and enters the systemic circulation, through the nasolacrimal canal it enters the digestive tract, which can lead to the development of undesirable systemic effects, primarily from the cardiovascular and respiratory systems.
When administered orally, timolol is well absorbed; undergoes active first-pass metabolism. It is excreted mainly by the kidneys in the form of inactive metabolites, the half-life is about 4 hours. It penetrates well through the cornea. A decrease in intraocular pressure with topical application of the drug usually develops after 2 hours. The maximum effect is observed after 3-4 hours, the duration of action is 10-20 hours.
When pilocarpine and timolol are combined in one preparation, an additive effect is observed in relation to a decrease in intraocular pressure, since the mechanisms of action of timolol and pilocarpine are different. When applied topically, Fotil reduces both high and normal intraocular pressure. After Fotil's instillation, intraocular pressure usually begins to decrease after 30 minutes. The maximum effect is noted after 2 hours, and a significant decrease in intraocular pressure with a single administration can persist for 20 hours.


Open-angle and closed-angle glaucoma, glaucoma associated with aphakia; newly-onset secondary glaucoma; as an additional agent in the treatment of glaucoma with other drugs; with an increase in intraocular pressure, including in the postoperative period.


Usually 1 drop of Fotila is prescribed in the affected eye / s 2-3 times a day. Fotil forte is prescribed 1 drop 2 times a day. Since some patients need several weeks to stabilize the drug-induced decrease in intraocular pressure, the effectiveness of the action of Fotil should be evaluated approximately 4 weeks after the start of treatment. if the intraocular pressure is maintained at a satisfactory level, then the dose of the drug can be reduced to 1 drop once a day into the affected eye.
Increasing the dose of Fotila Forte (more than 1 drop 2 times a day) does not lead to a further decrease in intraocular pressure. If intraocular pressure is still high at such a dose, dipivephrine therapy and / or systemic use of carbonic anhydrase inhibitors (for example, acetazolamide) should be prescribed.


Cholinergic drugs (pilocarpine) are contraindicated in acute iritis, as well as in corneal lesions. blockers of β-adrenergic receptors (timolol) are contraindicated in patients with BA or with a history of it, as well as with hoblas, sinus bradycardia, av-blockade of II – III degrees, severe heart failure, cardiogenic shock and hypersensitivity to any of the components of the drug.

Side effects

When using eye drops containing pilocarpine, the following local side reactions are possible: quickly passing burning and acute pain, spasm of the ciliary muscle, hyperemia of the conjunctival vessels, headache in the temporal and supraorbital regions, induced myopia. such reactions are observed, as a rule, in young people who have recently started treatment with pilocarpine. the decrease in visual acuity in poor lighting is caused by miosis. with the use of miotics, rare cases of retinal detachment, rigidity of the iris of the eye, the formation of cysts of the iris were noted. with prolonged use of pilocarpine, cases of reversible lens opacity have been observed. with local application of β-adrenergic receptor blockers, the following local adverse reactions were observed: corneal anesthesia, punctate keratitis, dry eye syndrome, allergic blepharoconjunctivitis. with prolonged use of the drug in patients with glaucoma, resistance to pilocarpine and timolol may develop.
From systemic reactions, nausea, diarrhea, increased sweating, salivation, decreased blood pressure, asthma attacks, congestive heart failure, arrhythmia, arterial hypotension, hallucinations, confusion, headache, asthenia, hyperemia of the nasal mucosa, rarely - depression, paresthesia and pain in the limbs, increased fatigue, anxiety, anorexia, retroperitoneal fibrosis, impotence, abdominal pain, purpura.

Special instructions

The safety and efficacy of the drug in children have not been established.
The appointment of Fotila during pregnancy is allowed only if the expected benefit to the expectant mother outweighs the potential risk to the fetus. In view of the possible serious effects of timolol on a baby, the question of whether to continue or stop breastfeeding should be decided based on the need for this drug to treat the mother.
Miosis usually causes difficulty in adapting to darkness. Patients taking Fotil should be careful when driving at night. With oral administration of β-adrenergic receptor blockers simultaneously with Fotil, an additive effect may be observed in relation to the action on intraocular pressure or the systemic action of β-adrenergic receptor blockers. Also, you should not prescribe Fotil simultaneously with other β-adrenergic receptor blockers used in ophthalmic practice.
Fotil and Fotil Forte should be used with caution in patients with impaired cerebral circulation. In the event of symptoms of cerebrovascular accident, another type of therapy should be considered. There are isolated reports that β-adrenergic receptor blockade can lead to muscle weakness due to certain myasthenic symptoms (eg, diplopia, ptosis, general weakness). With prolonged (over several years) use of Fotila and Fotila Forte, as well as with the use of other antiglaucoma drugs, tolerance to them may develop.
The drug is capable of exerting a systemic effect after resorption up to bronchospasm in patients with asthma and heart failure. The use of Fotila should be discontinued when the first symptoms of heart failure appear. Fotil should not be prescribed for patients with COPD. However, if necessary, the drug should be used with extreme caution.
Fotil and Fotil Forte should also be used with caution when performing selective surgical interventions using anesthetics. It is recommended to gradually stop taking β-adrenergic receptor blockers before surgery; this reduces the risk of developing arterial hypotension and asystole during anesthesia.
Remove contact lenses before using the drug; they can be reinstalled no earlier than 15 minutes after instillation of the drug.


Care should be taken with the simultaneous use of photil and calcium ion antagonists, both when taken orally and when administered intravenously due to possible violations of av-conduction, left ventricular failure, arterial hypotension. patients with cardiac dysfunction should not be prescribed these drugs at the same time.


In case of an overdose of parasympathomimetic agents and systemic β-adrenergic receptor blockers, bradycardia, arterial hypotension, bronchospasm and acute heart failure may occur.
Treatment is symptomatic. Atropine is used as an antidote to pilocarpine. With severe bradycardia or bronchospasm, isoprenaline is administered intravenously, with severe hypotension - dobutamine, oxygen therapy is prescribed.

Storage conditions

In the dark place at a temperature of 2-8 ° C; an open bottle can be stored at room temperature, the drug should be used within 1 month.


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