Universal reference book for medicines

Active substance: pilocarpine, timolol

Type: Antiglaucoma preparation

Manufacturer: SYNTHESIS (Russia)
Composition, form of production and packaging
Eye drops
in the form of a transparent or slightly opalescent, colorless or slightly colored liquid.

1 ml

pilocarpine hydrochloride 20 mg

timolol (in the form of maleate) 5 mg

Excipients: benzalkonium chloride 0.1 mg, sodium citrate d / and 5.79 mg, citric acid 1.12 mg, hypromellose hydroxypropyl methylcellulose 0.1 mg, water d / and up to 1 ml.

5 ml - a bottle-droppers polymer (1) - packs cardboard.

PilotimolВ® MINI

Eye drops in the form of a transparent or slightly opalescent, colorless or slightly colored liquid.

1 ml

pilocarpine hydrochloride 10 mg

timolol (in the form of maleate) 5 mg

Excipients: benzalkonium chloride 0.1 mg, sodium citrate 5.79 mg, citric acid 1.12 mg, hypromellose hydroxypropyl methylcellulose 0.1 mg, sodium chloride 4 mg, water d / and up to 1 ml.

5 ml - a bottle-droppers polymer (1) - packs cardboard.


Description of the drug approved by the manufacturer for the printed edition of 2013.


The antiglaucoma preparation 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. The action of pilocarpine lasts from 4 to 14 hours.
Timolol - beta-adrenoblocker, prevents the binding of sympathomimetic neurotransmitters with?
1 - and? 2- adrenoreceptors. Reduces intraocular pressure, reducing the production of watery moisture. Localization of the action of timolol -? 2- adrenoreceptors in the ciliary body. Penetrating into the systemic bloodstream by absorption through the mucous membrane of the eye, nose and lacrimal tract, can cause systemic effects characteristic of beta-blockers.
The hypotensive effect of timolol begins 20 minutes after instillation, reaches a maximum after 2 hours and lasts about 24 hours.

When combined in one preparation, pilocarpine and timolol mutually reinforce each other's action (synergism).



Pilocarpine penetrates well into the cornea.
C max pilocarpine in aqueous humor is achieved after 30 min. C max timolol in watery moisture is achieved in 1-2 hours.
Timolol maleate quickly penetrates through the cornea into the tissues of the eye.


Pilocarpine binds in many eye tissues, which prolongs T 1/2 from the eye.
When instillation in the conjunctival sac, pilocarpine does not enter the systemic bloodstream.
Timolol in an insignificant amount enters the systemic bloodstream through absorption through the conjunctiva, the nasal mucosa and the lacrimal tract.


Pilocarpine is not metabolized in aqueous humor, but is released together with it.

Timolol is extensively metabolized in the liver.


T 1/2 pilocarpine from the eye is 1.5-2.5 hours. However, the effect of decreasing intraocular pressure lasts several hours.

Timolol is excreted in the urine in unchanged form and in the form of metabolites.
T 1/2 timolol is 4 hours.
Reducing the formation of intraocular fluid, timolol reduces the rate of excretion of pilocarpine from the eye.

Pharmacokinetics in special clinical cases

In newborns and small children, the concentration of timolol significantly exceeds its C max in adult plasma.


- primary open-angle glaucoma;

- secondary glaucoma (uveal, aphakic, post traumatic);

- Closed-angle glaucoma (in combination with miotics);

- increased intraocular pressure after ophthalmic surgery.


The drug is buried in the affected eye 1 drop 2 times / day.

Evaluation of therapy should include measurement of intraocular pressure approximately 4 weeks after initiation of treatment.


Local reactions: eyelid hyperemia, burning and itching in the eyes, eye pain, ciliary muscle spasm, induced myopia, conjunctival hyperemia, lacrimation or decreased 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 superficial point keratopathy (decrease the transparency of the cornea) and decrease the sensitivity of the cornea, ptosis is possible, rarely - diplopia, reversible lens opacity, dry eye syndrome, increased sweating, asthenia, confusion.
Systemic reactions: Iris stiffness, iris cyst, 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).

- pronounced corneal dystrophy;

- irit;

- Iridocyclitis;

- bronchial asthma;

- sinus bradycardia (heart rate <50 bpm);

- AV blockade II and III degree;

Decompensated heart failure;

- cardiogenic shock;

- rhinitis;


- childhood;

- Hypersensitivity to the components of the drug.

With caution should apply the drug for detachment of the retina, cerebrovascular disorders, diabetes, thyrotoxicosis, hypoglycemia, oral administration of beta-blockers, as well as before operations under general anesthesia.


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.

The drug is contraindicated for use in childhood.


Before the start of treatment with Pilotimol or Pilotimol, MINI abolishes other antiglaucoma drugs.

Measurement of intraocular pressure is carried out at different times of the day.

With prolonged administration, resistance to the drug may develop.

Eye drops Pilotimol В® and Pilotimol В® MINI contain benzalkonium chloride as a preservative, so they are not recommended for use with contact lenses.
Before using the drug, contact lenses should be removed and reinstalled no earlier than 15 minutes.
Impact on the ability to drive vehicles and manage mechanisms

Care should be taken when driving in the dark or when working in poor lighting conditions.


Symptoms: the most common symptoms caused by an overdose of beta-blockers are bradycardia, a decrease in blood pressure, bronchospasm and acute heart failure.

Treatment: mainly symptomatic.
Atropine can be used as an antidote for pilocarpine. Isoprenaline can be administered IV to eliminate severe bradycardia or bronchospasm; dobutamine - for the treatment of arterial hypotension.

When used simultaneously with calcium channel blockers or cardiac glycosides, AV-conduction, development of acute left ventricular failure or arterial hypotension may occur.

Combined application of Pilotimol with drugs that disrupt the deposition of catecholamines (reserpine), promotes the development of arterial hypotension (including orthostatic), bradycardia and dizziness.

Simultaneous application with beta-blockers of systemic action leads to an increase in their pharmacological effect.
Pilotimol В® and Pilotimol В® MINI should not be used concomitantly with other eye drops containing a beta-blocker.

The drug is released by prescription.


List B. The drug should be stored out of reach of children, protected from light at a temperature of 2 В° to 15 В° C.
Shelf life - 2 years.
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