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

The combination drug contains two active ingredients. Pilocarpine in the form of eye drops causes constriction of the pupil and accommodation spasm, and also reduces intraocular pressure by contracting the ciliary muscle and iris muscle, which facilitates outflow of aqueous humor from the anterior chamber of the eye. The effect of pilocarpine occurs within 30 minutes and lasts 4-14 hours, the elimination half-life is 1.5 to 2.5 hours. The substance is not metabolized, it is excreted with aqueous humor.

Timolol is a beta-adrenoblocker that reduces intraocular pressure and reduces the production of aqueous humor by the visual organ. It acts mainly on the ciliary body. It slows down excretion of pilocarpine with aqueous humor. Its half-life is less than 30 minutes. Reduces intraocular pressure 2 hours after injection into the eye. Maximum effect should be expected after 4 hours, the effect lasts from 10 to 20 hours.

Pharmacokinetics

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

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

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

Timolol quickly penetrates through the cornea into the aqueous humor of the anterior chamber of the eye. About 80% of timolol applied topically penetrates into the systemic bloodstream. Cmax in plasma is determined approximately 1 h after installation of eye drops.

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

Indications

Elevated intraocular pressure, Glaucoma

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

Active ingredient

Pilocarpine, Timolol

Composition

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

5 mg pilocarpine,

hydrochloride 40 mg

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.

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How to take, the dosage

Prescribe 1 drop of Fotil (Fotil Eye Drops, 5 ml Cor. 1 by Santen AO) into the affected eye 2 times a day.

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

Interaction

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

The simultaneous use with beta-adrenoblockers of systemic action increases their pharmacological effect, therefore the combination is not recommended.

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

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Special Instructions

Do not use Fotil Forte at the same time as other eye drops containing beta-adrenoblockers.

The use of other eye drops should be discontinued before starting Photil. If antiglaucoma medications have been used, they should be discontinued, and Fotil drops should be started the next day.

The efficacy of the drug should be evaluated 4 weeks after the start of treatment with regular monitoring of intraocular pressure.

Continued treatment should also be performed with regular intraocular pressure monitoring.

The drug is injected with contact lenses removed because Fotil forte eye drops contain benzalkonium chloride as a preservative. They can be placed in the eye 15 minutes after using the eye drops.

The Timolol in the drug may mask the symptoms of hypoglycemia in patients with diabetes or symptoms of thyroid hyperfunction.

In case of upcoming surgery under general anesthesia, Motil Forte must be discontinued 48 hours prior to surgery, as the drug potentiates the effects of muscle relaxants and general anesthetics.

Impact on driving and operating machinery

Myotic effect may cause transient visual impairment (myopia sensation); therefore, during treatment, caution should be exercised when driving motor vehicles or operating any complex equipment requiring increased concentration and rapid psychomotor reactions.

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Contraindications

• anterior uveitis;
• sinus bradycardia;
• AV-blockade of degree II and III;
• cardiac failuredecompensated heart failure;
• cardiogenic shock;
• bronchial asthma;
• COPD;
• children and adolescents under 18 years of age (due to lack of data about the efficacy and safety of the drug in children and adolescents);
• condition immediately after ophthalmic surgeries and other eye diseases in which pupil contraction is undesirable;
• high sensitivity to the drug components.

With caution, use in hypoglycemia, cerebrovascular disorders, heart failure, diabetes, thyrotoxicosis, cerebrovascular disorders, and before surgical procedures in which general anesthesia is planned.

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Side effects

Local reactions: Blurred vision, eye irritation, rapidly disappearing burning sensation and pain in the eye, increased lacrimation, dry eye syndrome, eyelid dermatitis, conjunctival redness, ciliary muscle spasm and induced myopia, reduced visual acuity in low light (due to myosis), reduced corneal sensitivity, pitting keratitis, allergic blepharonjunctivitis; very rarely, diplopia, ptosis.

A few cases of retinal detachment, iris stiffness or iris cyst formation have been reported in connection with the use of myotics. Reversible lens opacity has been 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 through the HEB and has an effect on the CNS.

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

Nasal congestion has very rarely been noted.

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Overdose

In case of overdose of Fotil eye drops a slowed heart rate, decreased blood pressure, acute heart failure, bronchospasm develop.

The overdose is treated symptomatically. Atropine may be used as an antidote to pilocarpine. Administration of isoprenaline by IV is indicated for marked bradycardia, bronchospasm; dobutamine – for arterial hypotension.

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Pregnancy use

Till now there have not been enough adequate and strictly controlled studies in pregnant women.

The use of Fotilol in pregnancy and lactation is possible only when the estimated benefit to the mother exceeds the potential risk to the fetus.

There have been no negative effects of timolol on fertility in experimental studies.

There is currently no evidence that pilocarpine has teratogenic effects in the therapy of glaucoma in humans.

Preventive use in children

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

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Similarities

Fotil