Pilotimol® (Pilotymol)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substancePilocarpine + TimololPilocarpine + Timolol
Dosage form: & nbspEye Drops

Composition:1 ml of the solution contains:
Active substances: timolol maleate (in terms of timolol) - 5 mg; pilocarpine hydrochloride - 20 mg.
Excipients: sodium citrate for injection - 5.79 mg, lemon
acid - 1.12 mg, hypromellose (hydroxypropylmethylcellulose) 0.1 mg,
Benzalkonium chloride 0.1 mg, water for injection up to 1 ml.

Description:Transparent or slightly opalescent colorless or slightly colored liquid.

Pharmacotherapeutic group:An antiglaucoma agent (m-cholinomimetic + beta-adrenoblocker)
ATX: & nbsp

S.01.E.B.51   Pilocarpine in combination with other drugs

Pharmacodynamics:Eye drops Pilotimol® contains two active substances. Pilocarpine is a cholinergic agent that stimulates m-cholinergic receptors. When instilled in the eye pilocarpine causes miosis and spasm of accommodation, reduces intraocular pressure. Reduction of intraocular pressure is caused by contraction of the ciliary muscle and the muscle of the iris,which leads to an expansion of the angle of the anterior chamber of the eye and changes the physical structure of the trabecular tissue, thereby facilitating the outflow of aqueous humor. This effect lasts from 4 to 14 hours.
Timolol is a beta-adrenoblocker, which prevents the binding of sympathomimetic neurotransmitters to beta-1 and beta-2 adrenergic receptors. Reduces intraocular pressure, reducing the production of watery moisture. Localization of the action of timolol - beta-2 adrenoreceptors in the ciliary body.

Pharmacokinetics:Pilocarpine well penetrates the cornea. Concentration in aqueous humor reaches its maximum after 30 minutes. Pilocarpine binds in many eye tissues. This prolongs the half-life of the eye, which lasts from 1.5 to 2.5 hours. However, the effect of decreasing intraocular pressure continues for several hours.
Pilocarpine is not metabolized in aqueous humor, but is released together with it. The concomitant administration of timolol, which reduces the formation of intraocular fluid, is a decrease in the rate of elimination of pilocarpine.
Timolol maleate quickly penetrates through the cornea into the tissues of the eye.In an insignificant amount enters the systemic bloodstream by absorption through the conjunctiva, the mucous membranes of the nose and the lacrimal tract. Excretion of metabolites by the kidneys. In newborns and young children, the concentration of the active substance is significantly higher than its C max in adult plasma.

Indications:Primary open-angle glaucoma, secondary glaucoma (uveal, aphakic, posttraumatic), closed-angle glaucoma (in combination with miotics), increased intraocular pressure after ophthalmic surgery.

Contraindications:Bronchial asthma, sinus bradycardia (50 or less beats per minute), AV blockade II-III, decompensated heart failure, cardiogenic shock, pronounced corneal dystrophy, iritis, iridocyclitis, rhinitis, hypersensitivity to one of the components of the drug, chronic obstructive disease light, children's age.

Carefully:Retinal detachment, cerebrovascular disorders, diabetes mellitus, thyrotoxicosis, before operations under general anesthesia, hypoglycemia, oral administration of beta-blockers.

Pregnancy and lactation:In pregnancy, the drug is used if the expected benefit to the mother exceeds the potential risk to the fetus. During the use of the drug, breastfeeding should be discontinued.

Dosing and Administration:The drug is buried in the affected eye 1 drop - 2 times a day. Evaluation of therapy should include measurement of intraocular pressure approximately 4 weeks after initiation of treatment.

Side effects:Local reactions: hyperemia of the skin of the eyelids, burning and itching in the eyes, eye pain, ciliary muscle spasm, induced myopia, conjunctival hyperemia, lacrimation or tearing, photophobia, reduced visual acuity in case of insufficient illumination, corneal epithelial edema, short-term visual acuity; blepharitis, conjunctivitis, with prolonged use, it is possible to develop a surface point keratopathy (decrease the transparency of the cornea) and decrease the sensitivity of the cornea, it is possible ptosis, rarely - diplopia.
With prolonged use - clouding of the lens, dry eye syndrome, increased sweating, asthenia, confusion.
Systemic reactions: stiffness of the iris, cyst of the iris, retinal detachment, paresthesia, rhinitis, nasal congestion, epistaxis, lowering of blood pressure, bradycardia, bradyarrhythmia, AV blockade, heart failure, cardiac arrest; dizziness, headache, drowsiness, hallucinations, muscle weakness, impaired sexual function, decreased potency, transient cerebral circulation, collapse, depression; shortness of breath, bronchospasm, pulmonary insufficiency; nausea, vomiting, diarrhea, allergic reactions (including urticaria).

Overdose:The most common symptoms caused by an overdose of beta-blockers are a-cardiac, a decrease in blood pressure, bronchospasm and acute heart failure.
Treatment of an overdose is mostly symptomatic. Atropine can be used as an antidote for pilocarpine. Isoprenaline can be administered intravenously to eliminate severe bradycardia or bronchospasm; dobutamine - for the treatment of arterial hypotension.

Interaction:

When interacting with calcium channel blockers or cardiac glycosides, it is possible to disrupt AV conduction,acute left ventricular failure or arterial hypotension.
Drugs that disrupt the deposition of catecholamines (reserpine) promotes the development of arterial hypotension (including orthostatic), bradycardia and dizziness.
Simultaneous application of beta-adrenoblockers of systemic action leads to an increase in their pharmacological effect.

Special instructions:Before the start of treatment Pilotimol® the day before, other antiglaucoma medicines are being canceled. Measurement of intraocular pressure is carried out at different times of the day. With prolonged administration, resistance may develop.
Eye drops Pilotimol® contain benzalkonium chloride as a preservative and are not recommended for use with contact lenses. Before using the drug, contact lenses should be removed and reinstalled no earlier than 15 minutes.

Effect on the ability to drive transp. cf. and fur:Care should be taken when driving in the dark or when working in poor lighting conditions.

Form release / dosage:Eye drops.
5 ml in polymer bottles with plugs-droppers and screw-on caps (bottle-dropper polymer).

Packaging:Each vial with instructions for use in a pack of cardboard.

Storage conditions:In the dark place at a temperature of + 2 to +15 ° C.
Keep out of the reach of children.

Shelf life:3 years.
Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription
Registration number:LSR-002555/07
Date of registration:04.09.2007
The owner of the registration certificate:SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products Russia
Manufacturer: & nbsp
Representation: & nbspSYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products SYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products Russia
Information update date: & nbsp16.12.2014
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