PILOTIMOL
Active material: Pilokarpin, Timolol
When ATH: S01ED51
CCF: Antiglaucoma drug
ICD-10 codes (testimony): H40.0, H40.1, H40.2, H40.3, H40.4, H40.5
When CSF: 26.01.01.09
Manufacturer: SYNTHESIS JSC (Russia)
Pharmaceutical form, composition and packaging
Eye drops a transparent or slightly opalescent, colorless or slightly colored liquid.
| 1 ml | |
| timolol (in the form of maleate) | 5 mg |
| pilocarpine hydrochloride | 20 mg |
Excipients: benzalkonium chloride, sodium citrate d/and, lemon acid, hydroxypropyl (gipromelloza), water d / and.
5 ml – flakonah- polymer (1) – packs cardboard.
Pilotimol® MINI
Eye drops a transparent or slightly opalescent, colorless or slightly colored liquid.
| 1 ml | |
| timolol (in the form of maleate) | 5 mg |
| pilocarpine hydrochloride | 10 mg |
Excipients: benzalkonium chloride, sodium citrate, lemon acid, hydroxypropyl (gipromelloza), sodium chloride, water d / and.
5 ml – flakonah- polymer (1) – packs cardboard.
Pharmacological action
Antiglaucoma drug, It contains 2 active substances.
Pilokarpin – cholinergic agent, stimulating m-cholinergic receptors. When instilled into the eye, pilocarpine causes miosis and accommodation spasm., reduces intraocular pressure. The decrease in intraocular pressure is caused by the contraction of the ciliary muscle and the muscle of the iris., which leads to the expansion of the angle of the anterior chamber of the eye and changes the physical structure of the trabecular tissue, thus facilitating the outflow of aqueous humor. The action of pilocarpine begins after 30-40 m, reaches through 1.5-2 hours and lasts from 4 to 14 no.
Timolol – selective beta, preventing the binding of sympathomimetic neurotransmitters to β1– и b2-adrenoreceptor. Reduces intraocular pressure, reducing the production of aqueous humor. Localization of the action of timolol – b2-adrenergic receptors in the ciliary body. Penetrating into the systemic circulation by absorption through the mucous membrane of the eye, nose and lacrimal tract, may cause systemic effects, typical for beta-blockers. The action of timolol is manifested through 20 min after instillation, reaches through 1-2 hours and continues until 24 no.
When combined in one drug, pilocarpine and timolol mutually reinforce each other's action.
Pharmacokinetics
Absorption
Pilocarpine penetrates well into the cornea. FROMmax pilocarpine in aqueous humor reaches its maximum through 30 m.
Timolol maleate quickly penetrates through the cornea into the tissues of the eye. FROMmax timolol in aqueous humor is achieved through 1-2 no.
Distribution
Pilocarpine binds in many ocular tissues, which prolongs T1/2 out of the eye. When instilled into the conjunctival sac, it does not enter the systemic circulation.
Timolol enters the systemic circulation in small amounts by absorption through the conjunctiva, mucous membranes of the nose and lacrimal tract.
Metabolism
Pilocarpine is not metabolized in aqueous humor, but stands out with her. Timolol is extensively metabolized in the liver.
Deduction
T1/2 pilocarpine from the eye is 1.5-2.5 no. However, the effect of decreasing intraocular pressure continues for several hours..
Timolol is excreted in the urine unchanged and in the form of inactive metabolites. T1/2 timolol is 4 no.
Reducing the formation of intraocular fluid, timolol reduces the rate of elimination of pilocarpine from the eye.
Pharmacokinetics in special clinical situations
In newborns and young children, the concentration of timolol is significantly higher than its Cmax in plasma of adults.
Testimony
- primary open-angle glaucoma;
- secondary glaucoma (incl. uveal, aphakic, posttraumatic);
- Zakrыtougolynaya glaucoma (in combination with miotics);
- increased intraocular pressure after ophthalmic surgery.
Dosage regimen
The drug is instilled into the affected eye by 1 drop 2 times / day.
Evaluation of therapy should include the measurement of intraocular pressure approximately 4 weeks after initiation of treatment.
Side effect
On the part of the organ of vision: Local reactions – hyperemia of the skin of the eyelids, burning and itchy eyes, sore eyes, ciliary muscle spasm, induced myopia, conjunctival hyperemia, watery eyes or decreased tearing, photophobia, decreased visual acuity in low light, edema of the corneal epithelium, short-term visual impairment; .Aloe, conjunctivitis; with prolonged use, the development of superficial punctate keratopathy is possible (decrease in the transparency of the cornea), reduced corneal sensitivity, ptosis, cataract, dry eye syndrome; rarely – diplopia, rigidity of radishes, iris cyst, retinal disinsertion.
From the central and peripheral nervous system: paresthesia, dizziness, headache, drowsiness, depression; hallucinations, confusion.
Cardio-vascular system: decrease in blood pressure, bradycardia, ʙradiaritmija, AV блокада, heart failure, cardiac arrest, transient ischemic attack, collapse.
The respiratory system: rhinitis, nasal congestion, nose bleed, breathlessness, bronchospasm, pulmonary insufficiency.
From the digestive system: nausea, vomiting, diarrhea.
Reproductive system: sexual dysfunction, reduced potency.
Allergic reactions: hives.
Other: muscular weakness; prolonged use – increased perspiration, asthenia.
Contraindications
- Bronchial asthma;
— sinusova aetiology (Heart Rate <50 u. / min);
— AV-blockade II and III degrees;
- Decompensated heart failure;
- Cardiogenic shock;
- severe corneal dystrophy;
- irit;
- iridocyclitis;
- rhinitis;
- COPD;
- Children's age;
- Hypersensitivity to the drug.
FROM caution the drug should be used for retinal detachment, cerebrovascular disorders, diabetes, thyrotoxicosis, gipoglikemii, oral intake of beta-blockers, as well as before operations under general anesthesia.
Pregnancy and lactation
Application of the drug Pilotimol® Pregnancy may only, when the intended benefits to the mother outweighs the potential risk to the fetus.
If necessary, use during lactation should decide the issue of termination of breastfeeding.
Cautions
Before starting treatment with Pilotimol® and Pilotimol® MINI cancels other antiglaucoma drugs. Measurement of intraocular pressure is carried out at different times of the day.. Long-term administration may lead to the development of drug resistance.
Pilotimol eye drops® and Pilotimol® MINI contain benzalkonium chloride as a preservative, therefore they are not recommended for use when wearing contact lenses. Before using the drug, contact lenses should be removed and reinstalled at the earliest., than 15 minutes.
Effects on ability to drive vehicles and management mechanisms
Care should be taken when driving in the dark or when working in poor lighting.
Overdose
Symptoms: bradycardia, decrease in blood pressure, bronchospasm, acute heart failure.
Treatment: mostly symptomatic. Atropine can be used as an antidote to pilocarpine. Isoprenaline can be administered IV to eliminate severe bradycardia or bronchospasm; doʙutamin – for the treatment of arterial hypotension.
Drug Interactions
With the simultaneous use of Pilotimol® and Pilotimol® MINI with calcium channel blockers or cardiac glycosides – possible violation of AV conduction, acute left ventricular failure or arterial hypotension.
Combined use of Pilotimol® with drugs, violating the deposition of catecholamines (reserpine) promotes the development of arterial hypotension (incl. orthostatic), bradycardia and dizziness.
Simultaneous use of Pilotimol® with beta-blockers of systemic action leads to an increase in their pharmacological effect.
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
List B. The drug should be stored out of reach of children, protected from light at a temperature of 2 ° to 15 ° С. Shelf life – 2 year.
