Pilocarpine pharmacological characteristics. Pilocarpine - description of the drug, instructions for use, reviews. Contraindications for use
Formula: C11H16N2O2, chemical name: (3S-cis)-3-Ethyldihydro-4-[(1-methyl-1H-imidazol-5-yl)methyl]-2(3H)-furanone (and as hydrochloride or nitrate).
Pharmacological group: vegetotropic agents / cholinomimetics / m-cholinomimetics.
Pharmachologic effect: antiglaucoma.
Pharmacological properties
Pilocarpine has a stimulating effect on muscarinic receptors of smooth muscles, including bronchial, digestive, external secretion (sweat, salivary and other) glands, and the iris. Pilocarpine causes contraction of the ciliary (accommodation spasm) and circular (miosis) muscles. After oral administration, pilocarpine is rapidly absorbed, the maximum concentration is reached after about 1 hour. Pilocarpine is metabolized in plasma and synapses. The elimination half-life is 0.76 hours and increases in proportion to the dose. Excreted mainly by the kidneys, pilocarpine is found in the urine as metabolites and unchanged. In the conjunctival sac, pilocarpine is almost not absorbed and has no general effect. Systems with prolonged release of the active ingredient (eg, eye film) when wetted with lacrimal fluid, swell and remain in the lower conjunctival fornix. Liberation of pilocarpine occurs directly upon contact of the film with the conjunctiva. In angle-closure glaucoma, pilocarpine causes pupillary constriction, displaces the iris from the angle of the anterior chamber, and promotes the opening of fountain spaces and Schlemm's canal. In patients with open-angle glaucoma, pilocarpine opens the trabecular fissures and Schlemm's canal and increases the tone of the ciliary muscle. With ocular hypertension or primary open-angle glaucoma, instillation of a 1% solution once causes a 25–26% decrease in intraocular pressure. The action begins in 30-40 minutes, becomes maximum after 1.5-2 hours and lasts 4-8 hours. Within 24 hours, control of intraocular pressure of the system with prolonged release of pilocarpine is provided, while induced myopia, which develops during the first hours, quickly decreases and does not usually exceed 0.5 diopters.
Indications
Glaucoma (including acute attack); violation of the trophism of the eye in acute obstruction of the arteries of the retina or thrombosis of its central vein, hemorrhage into the vitreous body, atrophy of the optic nerve; to eliminate the mydriatic action of homatropine, atropine, scopolamine.
Route of administration of pilocarpine and dosage
In ophthalmic practice, I usually use a 1 or 2% solution of pilocarpine 2-4 times a day, less often 5 or 6% solutions are prescribed. Before going to bed for the eyelids, you can lay 1 or 2% pilocarpine ointment. Systems with prolonged release of pilocarpine (eye films) 40 or 20 mcg are used in cases where 3-4 instillations per day are not enough to normalize intraocular pressure; the film is laid 1–2 times a day behind the lower eyelid using eye tweezers (immediately after laying the film, it is necessary to hold the eye motionless for 30–60 seconds so that the film is wetted and becomes soft).
During therapy with pilocarpine, intraocular pressure should be regularly monitored. To reduce absorption after instillation of pilocarpine, it is recommended to pinch the lacrimal canal for 1-2 minutes - press at the inner corner of the eye with a finger. The physician should educate the patient on their own use of sustained release systems and warn them of the development of tolerance with prolonged use. Pilocarpine is used with caution in persons who are engaged in driving vehicles and other potentially hazardous activities that require clear vision, high reaction speed and increased attention.
Contraindications for use
Hypersensitivity, iridocyclitis, iritis, conditions in which constriction of the pupil is not recommended (for example, after ophthalmic operations, except when the pupil must be constricted immediately after the operation so that synechia does not form); high myopia with a risk of retinal detachment, a history of retinal detachment.
Application restrictions
No data.
Use during pregnancy and lactation
The use of pilocarpine during pregnancy is possible if the expected effects of the treatment of the mother outweigh the possible risk to the fetus (strictly controlled and adequate safety studies of the use of pilocarpine in pregnant women have not been conducted). During therapy with pilocarpine, breastfeeding should be discontinued.
Side effects of pilocarpine
Headache (in the periorbital or temporal areas), myopia, eye pain, spasm of accommodation, impaired twilight vision, blurred vision, lacrimation, superficial keratitis, rhinorrhea, with prolonged use - eyelid contact dermatitis, follicular conjunctivitis.
Interaction of pilocarpine with other substances
The effects of pilocarpine are terminated (weakened) with the use of drugs of the atropine group. Phenylephrine and timolol maleate potentiate a decrease in intraocular pressure by reducing the formation of intraocular fluid. Pilocarpine enhances the side effects of beta-blockers (impaired intracardiac conduction, severe bradycardia). In a combination of pilocarpine with adrenomimetics, mutual antagonism is manifested in the size of the pupil. M-cholinomimetic activity of pilocarpine is enhanced by anticholinesterase agents, reduced by phenothiazine derivatives, tricyclic antidepressants, clozapine, chlorprothixene. Hypotension and bradycardia may occur during halothane anesthesia in patients who use pilocarpine hydrochloride eye drops.
Overdose
An overdose of pilocarpine is manifested by a pronounced increase in m-cholinomimetic effects, including the development of bronchoconstriction and severe cardiovascular insufficiency. It is necessary: monitoring of respiratory function, blood pressure, pulse rate, administration of epinephrine (0.3-1.0 intramuscularly or subcutaneously), atropine (0.5-1.0 mg intravenously or subcutaneously), sufficient fluid.
Gross formula
C 11 H 16 N 2 O 2Pharmacological group of the substance Pilocarpine
Nosological classification (ICD-10)
CAS code
92-13-7Characteristics of the substance Pilocarpine
plant alkaloid Pilocarpus pinnatifolius Jaborandi. Colorless crystals or odorless white crystalline powder, with a bitter taste; hygroscopic, very easily soluble in water, easily in alcohol, insoluble in most non-polar solvents; aqueous solutions have a pH of 5-5.5.
Pharmacology
pharmachologic effect- antiglaucoma.Stimulates muscarinic receptors of smooth muscles, incl. the iris of the eye and the glands of the digestive, bronchial, external secretion (salivary, sweat, etc.). It causes contraction of the circular (miosis) and ciliary (accommodation spasm) muscles.
When taken orally, it is rapidly absorbed, the time to reach C max is about 60 minutes. Metabolized in synapses and plasma. T 1/2 is 0.76 h and increases in proportion to the dose. It is excreted mainly by the kidneys, in the urine it is found unchanged and in the form of metabolites. In the conjunctival sac, it is practically not absorbed and has no general effect. Systems with a prolonged release of the active ingredient (eye film), being wetted by the lacrimal fluid, swell and are retained in the lower conjunctival fornix. The release of pilocarpine begins immediately after contact of the film with the conjunctiva.
In angle-closure glaucoma, it constricts the pupil, causes displacement of the iris from the angle of the anterior chamber, and contributes to the opening of the Schlemm's canal and fountain spaces. In patients with open-angle glaucoma, it also opens the Schlemm canal and trabecular fissures and increases the tone of the ciliary muscle. In primary open-angle glaucoma or ocular hypertension, a single instillation of a 1% solution causes a decrease in intraocular pressure by 25-26%. The action begins after 30-40 minutes, reaches a maximum after 1.5-2 hours and lasts 4-8 hours. Systems with a long release of pilocarpine provide control of intraocular pressure for 1 day, while the induced myopia that develops during the first hours quickly decreases and usually does not exceed 0.5 diopters.
Application of the substance Pilocarpine
Glaucoma, incl. acute attack, violation of the trophism of the eye with thrombosis of the central vein of the retina or acute obstruction of its arteries, atrophy of the optic nerve, hemorrhage into the vitreous body; elimination of the mydriatic action of atropine, homatropine, scopolamine.
Contraindications
Hypersensitivity, iritis, iridocyclitis and other conditions in which pupil constriction is not recommended (for example, after ophthalmic operations, except when it is necessary to narrow the pupil immediately after surgery to prevent the formation of synechia); anamnestic indications of retinal detachment, high myopia with a risk of retinal detachment.
Use during pregnancy and lactation
For the period of treatment, it is desirable to refuse breastfeeding.
Side effects of Pilocarpine
Headache (in the temporal or periorbital areas), eye pain, myopia, spasm of accommodation, blurred vision, impaired twilight vision, lacrimation, rhinorrhea, superficial keratitis; with prolonged use - follicular conjunctivitis, contact dermatitis of the eyelids.
Interaction
The effect is weakened (stopped) by cholinomimetics of the atropine group. Timolol maleate and phenylephrine (reduce the production of intraocular fluid) potentiate a decrease in intraocular pressure. It is possible to increase the side effects of beta-blockers (severe bradycardia, intracardiac conduction disturbances). In combination with adrenomimetics, mutual antagonism is manifested (by the size of the pupil). m-cholinomimetic activity is reduced by tricyclic antidepressants, phenothiazine derivatives, chlorprothixene, clozapine, and enhanced by anticholinesterase agents. Perhaps the development of bradycardia and hypotension during halothane anesthesia in patients using pilocarpine hydrochloride in eye drops.
Overdose
It is manifested by a significant increase in m-cholinomimetic effects, incl. with the development of severe cardiovascular insufficiency and bronchoconstriction.
Treatment: monitoring of heart rate, blood pressure, respiratory function, the introduction of atropine (0.5-1.0 mg s / c or / in), epinephrine (0.3-1.0 s / c or / m), as well as a sufficient amount liquids.
Routes of administration
locally.
Precautions Substance Pilocarpine
Regular monitoring of intraocular pressure is necessary. To reduce absorption after instillation, it is recommended to pinch the lacrimal canal for 1-2 minutes by pressing with a finger at the inner corner of the eye. The patient should be educated in the use of sustained release systems and warned that tolerance may develop with prolonged use. Be wary appoint persons engaged in driving vehicles and other potentially hazardous activities that require clear vision, increased attention and high reaction speed.
Interactions with other active substances
Trade names
| Name | The value of the Wyshkovsky Index ® |
INSTRUCTIONS
on the medical use of a medicinal product
Registration number:
Tradename:
Pilocarpine
INN or grouping name:
Pilocarpine (Pilocarpinum)
chemical name: (3S-cis)-3-Ethyldihydro-4-[(1-methyl-1H-imidazol-5-yl)methyl]-2(3H)-furanone (as hydrochloride)
Dosage form:
eye drops
Composition per 1 ml:
Active substance:
Pilocarpine hydrochloride - 10 mg
Excipients:
boric acid - 12.5 mg
sodium hydroxide 1 M to pH 3.5-5.0
water for injection up to 1 ml
Description: Clear colorless liquid
Pharmacotherapeutic group:
antiglaucoma agent - m-cholinomimetic
ATX code:
Pharmacological properties
M-cholinomimetic, has a miotic and antiglaucoma effect. It increases the secretion of the digestive, bronchial and sweat glands, the tone of the smooth muscles of the bronchi, intestines, gall and bladder, uterus.
Pharmacodynamics
It causes contraction of the ciliary muscle (accommodation spasm) and the muscle that narrows the pupil (miosis). Contraction of the muscle that constricts the pupil (miosis) leads to a displacement of the basal part of the iris from the angle of the anterior chamber of the eye, which contributes to the opening of the Schlemm's canal and fountain spaces in angle-closure glaucoma. Contraction of the ciliary muscle (accommodative spasm) leads to the opening of the Schlemm's canal and trabecular fissures in open-angle glaucoma. Due to these processes, the outflow of aqueous humor from the anterior chamber of the eye increases with a further decrease in intraocular pressure. The hypotensive effect of pilocarpine begins after 10-30 minutes. The duration of the hypotensive effect with a single instillation of a solution of pilocarpine varies individually and averages 4-6 hours. Intraocular pressure decreases by 4-8 mm Hg. (17-20% of the original level).
In primary open-angle glaucoma, instillation of a 1% solution causes a decrease in intraocular pressure by 25-26%. The onset of the effect is after 30-40 minutes, reaches a maximum after 1.5-2 hours and lasts for 4-14 hours.
Pharmacokinetics
Pilocarpine penetrates well through the cornea and is well absorbed through the conjunctiva. It is practically not absorbed in the conjunctival sac. When applied topically, its concentration in the aqueous humor of the eye reaches a maximum (Tcmax) 30 minutes after installation. It lingers in the tissues of the eye, which increases its half-life from the tissues of the eye (T1 / 2), which is 1.5-2.5 hours.
Pilocarpine is not metabolized in the tissues of the eye and is excreted unchanged in the intraocular fluid. Pilocarpine is converted to its inactive form by hydrolysis in the blood serum and liver. The plasma half-life is about 30 minutes.
Indications for use
- acute attack of angle-closure glaucoma;
- secondary glaucoma (vascular, post-traumatic (burns));
- primary open-angle glaucoma (in combination with β-blockers or other drugs that reduce intraocular pressure);
- the need for pupil constriction after the installation of mydriatics.
Contraindications
Iritis, iridocyclitis and other conditions in which pupil constriction is not recommended (for example, after eye surgery, unless it is necessary to constrict the pupil immediately after surgery to prevent the formation of synechia), hypersensitivity to pilocarpine, children under 18 years of age , retinal detachment (including history), as well as conditions predisposing to retinal detachment.
Carefully
In young patients with high myopia.
If you have one of the listed diseases, be sure to consult your doctor before taking the drug.
Use during pregnancy and during breastfeeding
Perhaps the use of pilocarpine for the treatment of pregnant and lactating mothers as prescribed by the attending physician, if the expected benefit to the mother outweighs the potential risk to the fetus and child.
Dosage and administration
Buried in the conjunctival sac 1-2 drops. The number of installations may vary depending on the indications and the individual sensitivity of the patient.
Acute attack of closed glaucoma: during the first hour, a solution of pilocarpine is instilled every 15 minutes, 2-3 hours - every 30 minutes, 4-6 hours - every 60 minutes and then 3-6 times a day, until the attack stops.
Secondary glaucoma (vascular, post-traumatic (burns)): 1-2 drops 2-4 times a day;
Primary open glaucoma: 1-2 drops 2-4 times a day in combination with β-blockers or other drugs that reduce intraocular pressure;
To narrow the pupil after the installation of mydriatics: 1-2 drops once.
Side effect
Headache (in the temporal and periorbital areas), short-term pain in the eye area; myopia; decreased vision, especially at dusk, due to the development of persistent miosis and spasm of accommodation; lacrimation, rhinorrhea, superficial keratitis; allergic reactions.
With prolonged use, the development of follicular conjunctivitis, contact dermatitis of the eyelids and reversible clouding of the lens is possible.
Systemic side effects are rare. Pilocarpine, as an m-cholinomimetic, can cause bronchospasm, slow heart rate, increase salivation, and rhinorrhea.
If any of the side effects indicated in the instructions are aggravated, or you notice any other side effects not listed in the instructions, tell your doctor.
Overdose
In case of an overdose, increased salivation, sweating, bradycardia, the development of bronchospasm, and a decrease in blood pressure are possible.
When ingested, poisoning is possible, manifested by a significant increase in m-cholinomimetic effects, incl. with the development of severe heart failure and bronchoconstriction.
Treatment: gastric lavage; monitoring of heart rate (HR), blood pressure (BP), respiratory function; the introduction of atropine (0.5-1.0 mg subcutaneously or intravenously), epinephrine (0.3-1.0 mg subcutaneously or intravenously).
Interaction with other drugs
Pilocarpine antagonists are atropine and other m-anticholinergics.
With simultaneous use with adrenomimetics, antagonism of action (on the diameter of the pupil) can be observed.
Timolol and phenylephrine increase the decrease in intraocular pressure, reducing the production of intraocular fluid.
Perhaps the use of pilocarpine in combination with sympathomimetics, β-blockers, carbonic anhydrase inhibitors.
M-cholinomimetic activity of pilocarpine is reduced by tricyclic antidepressants, phenothiazine derivatives, chlorprothixene, clozapine; enhanced by cholinesterase inhibitors.
Perhaps the development of bradycardia and a decrease in blood pressure during general anesthesia with the use of halothane (in patients using pilocarpine in eye drops).
special instructions
Treatment should be carried out with regular monitoring of intraocular pressure.
To reduce suction, it is recommended to pinch the eye canal for 1-2 minutes after installation, pressing with a finger at the inner corner of the eye.
Due to the development of persistent miosis, as well as the myopic effect associated with a change in accommodation, a decrease in visual acuity is possible, therefore, the use of the drug is not recommended for drivers of vehicles at dusk and at night, care must be taken when engaging in potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.
The use of pilocarpine is not recommended when wearing soft contact lenses.
Release form.
Eye drops 1%.
1.5 ml, 2 ml or 5 ml in a polymer dropper tube. 1, 2, 4, 5 or 10 dropper tubes with instructions for using the drug are placed in a cardboard pack.
The text of the instructions for use of the dropper tube is printed on the pack.
5 ml or 10 ml in a polymer dropper bottle. 1 or 2 dropper bottles with instructions for using the drug are placed in a cardboard box.
The text of the instructions for use of the dropper bottle is printed on the pack.
5 ml in glass vials.
1 vial complete with a sterile cap-dropper and instructions for use of the drug is placed in a pack of cardboard.
5 bottles in a blister pack.
1 blister pack complete with 5 sterile dropper caps and instructions for using the drug is placed in a pack.
Storage conditions
In a place protected from light, at a temperature not exceeding 15 ° C for the drug in a dropper tube and dropper bottles, in a place protected from light at a temperature not exceeding 25 ° C for the drug in glass vials. Keep out of the reach of children.
Best before date
3 years for the drug in vials; 2 years for the drug in a dropper tube, dropper bottle.
After opening the dropper tube, dropper bottle and bottle - 1 month.
Do not use after the expiry date stated on the packaging.
Holiday conditions
Released by prescription.
Marketing Authorization Holder/Complaint Receiving Organization
109052 Moscow, st. Novokhokhlovskaya, 25.
Manufacturer:
Federal State Unitary Enterprise "Moscow Endocrine Plant"
109052, Moscow, st. Novokhokhlovskaya, 25, building 1, building 2
Pilocarpine- antiglaucoma, miotic drops.
Pilocarpine hydrochloride belongs to the M-cholinomimetic drugs. The mechanism of action is due to the excitation of peripheral M-cholinergic receptors, which causes a contraction of the circular muscle of the iris and ciliary muscle, accompanied by a narrowing of the pupil and the opening of the angle of the anterior chamber of the eye, an improvement in the outflow of intraocular fluid, which generally causes a decrease in intraocular pressure and improves trophic processes in the tissues of the eye. The decrease in ophthalmotonus reaches 3-4 mm Hg. Art. Pharmacokinetics
.
When instilled on the conjunctiva, pilocarpine hydrochloride penetrates the cornea and is maximally concentrated in the aqueous humor of the eye after 30-40 minutes. The half-life of the eye is 1.5-2 hours, however, the effect of the drug on the level of intraocular pressure lasts for 4-8 hours. Pilocarpine hydrochloride is not metabolized in the tissues of the eye, but is excreted along with the intraocular fluid, inactivated by hydrolysis in the blood serum and liver. The plasma half-life is 30 minutes.
Indications for use
Indications for the use of drops Pilocarpine are:- Primary and chronic open-angle glaucoma.
- Acute attack of angle-closure glaucoma.
- Chronic angle-closure glaucoma (before surgery).
- Secondary glaucoma (as a result of thrombosis of the central retinal vein, acute obstruction of the retinal artery, optic nerve atrophy, pigmentary retinal degeneration, vitreous hemorrhage).
- The need for constriction of the pupil in case of an overdose of mydriatics, for diagnostic purposes and during surgical interventions (except for persons with high myopia).
Mode of application
Pilocarpine instilled in each eye 1-2 drops 2-4 times a day. The daily dose and duration of the course of treatment is determined by the doctor depending on the level of intraocular pressure. If necessary, the drug can be combined with β-adrenergic blockers.In an acute attack of angle-closure glaucoma, Pilocarpine is prescribed: during the first hour - every 15 minutes, 1 drop; for 2-3 hours - every 30 minutes, 1 drop; for 4-6 hours - every 60 minutes, 1 drop; further - 3-6 times a day until the attack stops.
Side effects
During application Pilocarpine may develop:- local side effects: miosis, short-term pain in the eye, redness, spasm of accommodation as a consequence of persistent miosis (at night), decreased visual acuity, headache in the temples and paraorbital areas, increased lacrimation, allergic conjunctivitis and eyelid skin dermatitis, superficial keratitis, itching in the eye area, myopia, photophobia, conjunctival hyperemia, corneal edema and erosion, spasm of the ciliary muscle; occasionally - retinal detachment;
- systemic side effects develop very rarely: bronchospasm, headache, dizziness, hypersalivation, rhinorrhea, pulmonary edema, increased blood pressure, bradycardia, vascular disorders, arterial hypotension, increased sweating, nausea, vomiting, diarrhea;
- long-term treatment can lead to follicular conjunctivitis, contact dermatitis of the eyelids, keratopathy, cataracts, reversible lens opacity, changes in the conjunctival tissue.
Contraindications
:Iritis, iridocyclitis, iridocyclic crisis, uveitis, cyclitis, keratitis and other eye diseases in which pupil constriction is not desirable (after surgical interventions on the eye to prevent posterior synechia). Paradoxical reaction to the drug in congestive glaucoma.
Pilocarpine should be used with caution in patients with a history of retinal detachment, young people with high myopia. Acute inflammatory diseases of the tissues of the eye. Allergic reactions to the components of the drug and a history of bronchial asthma.
Pregnancy
:Application Pilocarpine during pregnancy or lactation is possible only if, in the opinion of the doctor, the expected effect outweighs the risk of possible adverse reactions.
Interaction with other drugs
Atropine and other M-cholinolytic drugs are antagonists of Pilocarpine. With simultaneous use with adrenostimulants, antagonism of action (influence on pupil diameter) can be observed.Timolol and mezaton increase the decrease in intraocular pressure.
It is possible to use Pilocarpine in combination with β-blockers, carbonic anhydrase inhibitors.
M-cholinostimulating effect of Pilocarpine is reduced when combined with tricyclic antidepressants, phenothiazine derivatives, chlorprothixene, clozapine; enhanced by anticholinesterase drugs.
Perhaps the occurrence of bradycardia and a decrease in blood pressure during general anesthesia with the use of halothane (in patients who use Pilocarpine in eye drops).
Overdose
The first symptoms of an overdose are nausea, bradycardia, persistent miosis, eye pain, blurred vision, and headache may develop.With the onset of these symptoms, the drug Pilocarpine canceled.
Treatment of overdose is symptomatic. Atropine, tropicamide can be used as specific antidotes. With severe bradycardia due to an overdose of parasympathomimetics, 0.5-2 mg of atropine is administered parenterally.
Storage conditions
To store in the place protected from light at a temperature from 8 °C to 15 °C.Keep out of the reach of children.
Release form
Pilocarpine - eye drops.5 ml or 10 ml in a vial. 1 bottle in a pack.
Compound
1 ml drops Pilocarpine contains pilocarpine hydrochloride 10 mg.Excipients: boric acid, sodium tetraborate, water for injection.
Additionally
:Immediately before use, hold the vial with the drug in the palm of your hand to warm it to body temperature. The cap is unscrewed, removed and, slightly pressing on the body of the bottle, the solution is instilled into the eye. After instillation, the cap is screwed tightly.
Use with caution in patients with acute heart failure, recent myocardial infarction, severe bradycardia, arterial hypotension, arterial hypertension, hyperthyroidism, epilepsy, urinary tract obstruction, vasomotor instability, Parkinson's disease.
Miotic preparations are used in the absence of newly formed vessels in the iris.
Increasing the concentration and frequency of instillation (6 or more) is not advisable, because it does not lead to an increase in the hypotensive effect and causes general negative reactions of the body.
Pilocarpine has practically no effect on the level of ophthalmotonus in healthy people, but is effective in patients with glaucoma of various forms. It is advisable to replace Pilocarpine with other, non-myotic drugs for 1-3 months during the year. With prolonged instillation, miosis persists all the time, which is important for older people with phacosclerosis and cataracts of the initial stage.
The ability to influence the reaction rate when driving vehicles or working with other mechanisms.
When using the drug, it is not recommended to drive vehicles and engage in other potentially hazardous activities that require clarity of vision.
main parameters
| Name: | PILOCARPIN |
| ATX code: | S01EB01 - |
Excipients: boric acid - 19 mg, water for injection up to 1 ml.
Description: Transparent colorless liquid. Pharmacotherapeutic group:Antiglaucoma agent - m-cholinomimetic. ATX:S.01.E.B.01 Pilocarpine
Pharmacodynamics:refers to m-cholinomimetic agents. The mechanism of action is due to the excitation of peripheral m-cholinergic receptors, which causes contraction of the circular muscle of the iris and ciliary muscle, accompanied by pupil constriction and expansion of the angle of the anterior chamber of the eye, improving the outflow of intraocular fluid. In primary open-angle glaucoma, instillation of a 1% solution causes a decrease in intraocular pressure by 25-26%. The onset of the effect is after 30-40 minutes, reaches a maximum after 1.5-2 hours and lasts for 4-14 hours. Pharmacokinetics:penetrates well through the cornea. It is practically not absorbed in the conjunctival sac. The time to reach the maximum concentration (TCmax) in the intraocular fluid is 30 minutes. It lingers in the tissues of the eye, which increases its half-life from the tissues of the eye (T1 / 2), which is 1.5-2.5 hours. It is excreted unchanged with intraocular fluid. Partially penetrates into the blood plasma and is inactivated by hydrolysis in the blood serum and liver. Indications: Acute attack of closed-angle glaucoma, secondary glaucoma (vascular, post-traumatic (burns)), primary open-angle glaucoma (in combination with beta-blockers or other drugs that reduce intraocular pressure). The need for pupillary constriction after instillation of mydriatics. Contraindications:Hypersensitivity to the components of the drug. Iritis, iridocyclitis, iridocyclic crisis, uveitis, cyclitis, keratitis and other eye diseases in which pupil constriction is undesirable (after surgical interventions on the eye to prevent posterior synechia). Bronchial asthma.Pregnancy, lactation period, age up to 18 years.
Carefully:Use with caution in patients with a history of retinal detachment and in young patients with high myopia. Pregnancy and lactation:The drug is contraindicated for use during pregnancy. If necessary, the appointment of the drug during lactation, breastfeeding should be discontinued. Dosage and administration:In case of primary glaucoma, instill 1-2 drops into each eye - 2-4 times a day, the daily dose, as well as the duration of the course of treatment, are determined by the doctor depending on the level of intraocular pressure. If necessary, the drug can be combined with β-blockers. In an acute attack of angle-closure glaucoma, the following is prescribed: during the first hour - every 15 minutes, 1 drop; for 2-3 hours - every 30 minutes, 1 drop; for 4-6 hours - every 60 minutes, 1 drop; further 3-6 times a day until the attack stops. Side effects:During the use of Pilocarpine may develop:Local side effects: miosis, short-term pain in the eye, its redness, decreased visual acuity as a consequence of persistent miosis (at night), spasm of accommodation, headache in the temples and paraorbital areas, superficial keratitis, increased lacrimation, allergic conjunctivitis.
With prolonged use, it is possible to develop follicular conjunctivitis, contact dermatitis of the eyelids, retinal detachment, nuclear cataract, edema of the endothelium of the optic discs, corneal keratopathy, reversible clouding of the lens.
Systemic side effects are possible: bronchospasm, headache, hypersalivation, pulmonary edema, increased blood pressure, nausea, vomiting, diarrhea.
Overdose: In case of overdose, the following symptoms are observed: nausea, bradycardia, persistent miosis, eye pain, blurred vision, headache. In case of accidental ingestion, bronchospasm, cardiovascular insufficiency may develop.Treatment: symptomatic. Cancel the drug, with severe bradycardia, enter 0.5-2 mg of atropine parenterally.
Interaction: and other M-anticholinergics are pilocarpine antagonists. With simultaneous use with adrenomimetics, antagonism of action (effect on pupil diameter) can be observed.Timolol and increase the decrease in intraocular pressure.
Perhaps the use of pilocarpine in combination with β-blockers, carbonic anhydrase inhibitors.
M-cholinomimetic effect of pilocarpine is reduced when combined with tricyclic antidepressants, phenothiazine derivatives, chlorprothixene, clozapine; enhanced by cholinesterase inhibitors.
Possible occurrence of bradycardia and a decrease in blood pressure during general anesthesia with the use of halothane (in patients who are used in eye drops).
Special instructions:Immediately before use, hold the vial with the drug in the palm of your hand to warm it to body temperature. The cap is unscrewed, removed and, slightly pressing on the body of the bottle, the solution is instilled into the eye. After instillation, the cap is screwed tightly.Treatment should be carried out with regular monitoring of intraocular pressure.
To reduce absorption into the systemic circulation, it is recommended to pinch the lacrimal ducts for 1-2 minutes after instillation, pressing with a finger at the inner corner of the eye in the area of the projection of the lacrimal sac.
In the presence of an initial cataract, the miotic effect can cause a transient deterioration in vision (a feeling of myopia), therefore, during the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Influence on the ability to drive transport. cf. and fur.:Care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions. Release form / dosage: Eye drops 1%. Package: 5 ml or 10 ml in polyethylene bottles, sealed with caps.Each bottle, together with instructions for medical use, is placed in a cardboard box.
Storage conditions:To store in the place protected from light at a temperature from 8 °C to 15 °C.Keep out of the reach of children.
Best before date: 3 years. After opening the vial, the drug is valid for 28 days.Do not use after the expiry date stated on the package.
Conditions for dispensing from pharmacies: On prescription Registration number: P N015742/01 Date of registration: 21.05.2009 Registration certificate holder: PHARMAK, PJSC