Project Description

Pilocarpine hydrochloride

(solution 1% (eye drops) Solutio Pilocarpini hydrochloridi 1% (guttae ophthalmicae)

international nonproprietary name

Pilocarpine.

Ref

BP-0107

Pharmacotherapeutic group

Antiglaucoma preparation, miotics. Parasympathomimetic agents.

Composition of the preparation

1 ml of sterile solution (eye drops) contains 10 mg of policarpine hydrochloride.

Pharmacological action

Pharmacodynamics

Pilocarpine stimulates flat muscle muscarine receptors, comprising the iris and glands — peptic, bronchial, external secretion (salivary, sweat, etc.). It induces contraction of circular (mios) and ciliary (spasm accommodation) muscle.

In case of angle-closure glaucoma it narrows the pupil, induces the iris displacement from the frontal chamber angle and provides opening of Schlemm canals and Fontana’s spaces.

In patients with angle-open glaucoma it also opens Schlemm canals and trabecular fissues and increases ciliary muscle tonus.

In case of primary angle-open glaucoma or eye hypertension, single instillation of 1% solution induces intraocular tension at 25—26%. The action starts after 30—40 minutes, and its maximum is achieved after 1,5—2 hour and lasts 4—8 hours.

Indications 

Glaucoma, comprising acute form; eye trophism disturbance on thrombosis of the retina central vein or acute artery impassability, on visual nerve atrophy, hemorrhage into vitreous body; elimination of atropine mydriatic action, homatropine, scopolamine.

special indication

The pilocardine may cause decrement in visual acuity therefore it shall be prescribed with care to drivers and persons carrying out potentially dangerous activities requiring visual acuity, high concentration and quick reaction.

special warning

Not established

Dosage and method of administration

The preparation shall be instilled into the conjunctival sac 1—2 drops 2—3—4 times a day.

overdosage

On overdosing and high sensitivity excessive salivation, sweating, bradycardia, blood pressure drop are possible. On oral administration poisoning is possible that induces m-cholinoceptive effects, among them – development of serious heart failure and bronchocontriction.

Treatment: stomach lavage, monitoring of heart rate, blood pressure, respiratory function, atropine administration (0,5—1,0 mg i/v or s/c), epinephrine (0,3—1,0 mg i/v or s/c), as well as drinking a lot of liquid.

safety measures

The treatment shall be carried out on a regular monitoring of intraocular pressure. To decrease the absorption after instillation it is recommended to pinch the lachrymal canal pressing the internal eye angle with finger.

Side effects

Headache in the temporal and periorbital zones, pain in the eye, myopia, spasm accommodation, blurring, decrement in twilight vision, watering, rhinorrhea, follicular conjunctivitis, superficial keratitis,contact eyelid dermatitis (rarely).

Contraindications

Antagonists of pilocarpine hydrochloride are antropin and other М-cholinolytic agents. Timolol maleate and mezaton reduces intraocular pressure. Side effects of beta-adrenoblockers are possible (marked bradycardia, intracardial conductivity). М-cholinoceptive activity is decreased by tricyclic antudepressants, phenothiazine derivatives, chlorprothixene, clozapin. It is increased by anticholinesterase preparations. Development of bradycardia and hypotension is possible on halothane hypnosis in patients using pilocarpine in eye drops.

Interactions with other medicinal preparations

Phytonsol increases the hypertensive effect of medicinal preparations. It may be prescribed simultaneously with immunostimulating preparations of plant origin, vitamins, honey. The phytonsol effect may enhance when it is taken simultaneously with preparations from the group of psychostimulators.

The form of release

1 ml of sterile solution (eye drops) contains 10 mg of policarpine in 1 ml. In 1 ml drop tube (2 or 10 drop tubes per package).