Pilocarpine Prolong (Pilocarpine prolong)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Dosage form: & nbspeye drops
Composition:

Per 1 ml:

active substances: pilocarpine hydrochloride - 10.0 mg, hypromellose - 4.3 mg;

Excipients: disodium edetate (disodium ethylenediamine salt N, N, N ', N'-tetraacetic acid 2-aqueous (Trilon B) 0.1 mg, benzalkonium chloride 0,1 mg, sodium chloride - 2.0 mg, boric acid - 10.0 mg, water for injection - up to 1 ml.

Description:

Transparent or slightly opalescent colorless or slightly colored viscous liquid.

Pharmacotherapeutic group:antiglaucoma means - m-cholinomimetic
ATX: & nbsp
  • Pilocarpine in combination with other drugs
    • Pharmacodynamics:

    The composition of the drug includes two active substances: pilocarpine hydrochloride + hypromellose.

    Pilocarpine - m-holinomimeticheskoe means, has a miotic effect.

    Causes the contraction of the circular and ciliary muscles, which is accompanied by the narrowing of the pupil (miosis) and the widening of the angle of the anterior chamber of the eye (the iris root is drawn back), the increase in the tone of the iris and the ciliary body, as a result of which the trabecula is stretched and the blocked sections of the helmet canal are opened. Due to the opening of the anterior chamber angle and the increase of the permeability of the trabecular diaphragm, the outflow of aqueous humor improves and the intraocular pressure decreases.With primary open-angle glaucoma, instillation of 1% solution causes a decrease in intraocular pressure by 17-20% of the initial value.

    The beginning of the drug - after 10-30 minutes, the maximum effect - after 1,5-2 hours and its effect persists for 4-14 hours.

    Hypromellose - the protector of the epithelium of the cornea, has a lubricating and softening effect on the eye tissue, it reduces the locally irritating effect of pilocarpine. Having a high viscosity, hypromellose increases the duration of contact between the pilocarpine solution and the cornea. The refractive index of hypophyseal is similar to the natural tear. Helps restore and stabilize the optical characteristics of tear film. Has a protective effect against the cornea with a decrease in the secretion of tear fluid.

    Frequency of instillation during the day of eye drops Pilocarpine prolongus is usually an average of one instillation less than the eye drops of pilocarpine that do not contain hypromellose.

    Pharmacokinetics:

    Pilocarpine hydrochloride - a cholinergic parasympathomimetic substance that acts through direct stimulation of muscarinic receptors of smooth muscles and secretory glands.

    Pilocarpine penetrates well through the cornea into the watery moisture of the anterior chamber of the eye, it is well absorbed through the conjunctiva. Time to reach the maximum concentration (TCmOh) in the aqueous humor of the anterior chamber of the eye - 30 min. It is retained in the tissues of the eye, which prolongs its half-life (T1/2) from the eyes, which is 1,5-2,5 hours. However, the action of pilocarpine on intraocular pressure lasts for several hours (from 4 to 14 hours).

    It is excreted with intraocular fluid and is partially metabolized in blood plasma. In the intraocular fluid, it is not metabolized and is excreted unchanged. Pilocarpine is partially metabolized in the blood serum and in the liver, becoming an inactive form by hydrolysis. T1/2 from the blood plasma is about 30 min.

    Indications:

    - Acute attack of angle-closure glaucoma;

    - secondary glaucoma (vascular, post-traumatic (burns));

    - primary open-angle glaucoma (as a monotherapy and in combination with beta-blockers or other drugs that reduce intraocular pressure);

    - chronic closed angle glaucoma;

    - if necessary, narrowing the pupil after instillation midriatikov (except for people with myopia of high degree).

    Contraindications:

    Hypersensitivity to pilocarpine, irit, cyclit, iridocyclitis, keratitis, condition after ophthalmic operations and other eye diseases, in which the narrowing of the pupil is undesirable, age is 18 years.

    Carefully:

    In patients with retinal detachment in history and in young patients with high degree of myopia.

    Pregnancy and lactation:

    Use during pregnancy is contraindicated.

    If necessary, the appointment of lactation, breastfeeding should be discontinued for the duration of treatment.

    Dosing and Administration:

    Bury in the conjunctival sac 1 drop 1-3 times a day. The number of instillations can vary depending on the indications and individual sensitivity of the patient.

    To treat an acute attack of angle-closure glaucoma, during the first hour Pilocarpine solution is instilled in 1 drop every 15 minutes, for 2-3 hours every 30 minutes, for 4-6 hours every 60 minutes and further 3-6 times a day, until cupping of an attack.

    It is possible to use a combination with adrenomimetics, beta-adrenoblockers, inhibitors of carbonic anhydrase.

    Side effects:

    From the side of the organ of vision: local reactions - pain in the eye area; myopia; decreased vision, especially in the dark (due to the development of persistent miosis and spasm of accommodation); lacrimation, superficial keratitis.

    With prolonged use, it is possible to develop follicular conjunctivitis, contact eyelid dermatitis. Rarely - nuclear cataract, edema of the corneal endothelium, keratopathy, retinal detachment.

    System: headache (in temporal or periorbital regions), rhinorrhea, bronchospasm, hypersalivation, vomiting, diarrhea, increase or decrease in blood pressure, allergic reactions.

    Overdose:

    In case of accidental ingestion, it manifests itself as a significant enhancement of m-cholinomimetic effects, incl. with the development of severe cardiovascular insufficiency and bronchoconstriction.

    Treatment includes gastric lavage, administration of atropine (0.5-1.0 mg PO / IV or IV), epinephrine (0.3-1.0 mg, SC or IM), as well as a sufficient amount of fluid.

    Interaction:

    Pilocarpine antagonists are atropine and other m-anticholinergic agents.

    With simultaneous use with adrenomimetics - antagonism of action (effect on the diameter of the pupil).

    Simultaneous use with adrenomimetics (including phenylephrine), beta-adrenoblockers (including timolol), inhibitors of carbonic anhydrase increases the decrease in intraocular pressure.

    M-cholinomimetic activity of pilocarpine decreases with combination with tricyclic antidepressants, phenothiazine derivatives, chlorprotixen, clozapine; is enhanced by cholinesterase inhibitors by drugs.

    Possible development of bradycardia and lowering blood pressure during general anesthesia with halothane.

    Special instructions:

    Treatment should be performed with regular monitoring of intraocular pressure.

    To reduce absorption to the systemic blood stream, it is recommended to squeeze the lacrimal canaliculi for 1-2 minutes after instillation, pressing the finger at the inner corner of the eye in the area of ​​the projection of the lacrimal sac.

    Effect on the ability to drive transp. cf. and fur:

    In the presence of an initial cataract, the myotonic effect can cause a transient visual impairment (sensation of nearsightedness), therefore, during the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities,requiring increased concentration of attention and speed of psychomotor reactions.

    Form release / dosage:Eye drops, 1% + 0,43%.
    Packaging:

    To 5 ml in polymeric matt bottles with stoppers-droppers and screw-on caps (bottles-dropper polymer).

    Each vial with instructions for use is placed in a pack of cardboard.

    Storage conditions:

    In the dark place at a temperature of 15 to 25 ° C. Do not freeze.

    Keep out of the reach of children.

    Shelf life:

    2 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:PL-000939
    Date of registration:18.10.2011
    Date of cancellation:2016-10-18
    The owner of the registration certificate:SYNTHESIS, OJSC SYNTHESIS, OJSC 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: & nbsp16.03.2016
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