Information for Healthcare Professionals

Revised: 17 June 2015

Data Sheet


Pilocarpine hydrochloride


PILOPT EYE DROPS 0.5% contain 5mg/ml of the active ingredient pilocarpine hydrochloride.

PILOPT EYE DROPS 1% contain 10mg/ml of the active ingredient pilocarpine hydrochloride.

PILOPT EYE DROPS 2% contain 20mg/ml of the active ingredient pilocarpine hydrochloride.

PILOPT EYE DROPS 3% contain 30mg/ml of the active ingredient pilocarpine hydrochloride.

PILOPT EYE DROPS 4% contain 40mg/ml of the active ingredient pilocarpine hydrochloride.

PILOPT EYE DROPS 6% contain 60mg/ml of the active ingredient pilocarpine hydrochloride.

All PILOPT EYE DROP strengths are a clear to slightly hazy, colourless, odourless, sterile, slightly viscous liquid, containing the inactive ingredients disodium edetate, hypromellose, sodium phosphate, sodium acid phosphate, sodium chloride, water - purified, and benzalkonium chloride as a preservative.



Pilocarpine hydrochloride directly stimulates cholinergic receptors. It produces contraction of the iris sphincter muscle, resulting in pupillary constriction (miosis); constriction of the ciliary muscle, resulting in increased accommodation; and reduction in intraocular pressure associated with an increase in the outflow and a decrease in the inflow of aqueous humour.

In chronic open angle glaucoma, the exact mechanism by which miotics lower intraocular pressure is not precisely known; however, contraction of the ciliary muscle apparently opens the intertrabecular spaces and facilitates aqueous humour outflow. There is also a decrease in the rate of inflow of aqueous humour.

In angle-closure glaucoma, constriction of the pupil apparently pulls the iris away from the trabeculum, thereby relieving blockage of the trabecular meshwork.


Miosis (pupillary constriction) occurs within 10 to 30 minutes and lasts 4 to 8 hours. Intraocular pressure is decreased within 75 minutes depending on the strength used and persists for 4 to 14 hours.

Following systemic absorption pilocarpine undergoes biotransformation which is thought to occur at the neural synapses and in the plasma. Elimination is not fully understood; in the urine, as unchanged pilocarpine and its minimally active or inactive degradation products, such as pilocarpic acid.


The management of increased intraocular pressure in chronic open angle glaucoma.

Dosage and Administration

Usually 1 or 2 drops of the selected strength product two to four times a day. To minimise systemic absorption of the active ingredient of these eye drops pressure should be applied for one minute on the tear duct after application. The hands should be washed immediately after use of the drops to remove traces of the medication from the fingers.

The drops should be discarded no later than 4 weeks after first opening the container.


Warnings and Precautions

If blurred vision or changes in near or far sight occur, especially at night, patients should exercise caution when involved in night driving or hazardous work in poor light.

It is recommended that intraocular pressure measurements be performed regularly during therapy.

For patients who suffer from bronchial asthma, the risk/benefit should be weighed before prescribing.

To avoid excessive systemic absorption, patient should press finger to the lacrimal sac during and for 1 or 2 minutes following instillation.

Use in Pregnancy

Safe use during pregnancy has not been established.

Use in Lactation

Problems in humans have not been documented. However, ophthalmic pilocarpine is systemically absorbed.

Use in Children

Appropriate studies on the effects of paediatric dosage have not been performed. However, no paediatric-specific problems have been documented to date.

Carcinogenicity, Mutagenicity, Impairment of Fertility

No definitive long term animal studies have evaluated the carcinogenic potential of pilocarpine hydrochloride.

Adverse Effects


Adverse reactions associated with systemic absorption include:



Belladonna alkaloids or cyclopentolate used ophthalmically may interfere with the miotic effects of pilocarpine and may have their own mydriatic effects dampened. This latter may be used to therapeutic advantage.


Dilution with water and other fluids is the usual response to accidental or deliberate overdose.

Pharmaceutical Precautions

Medicine Classification

Prescription Medicine.

Package Quantities

PILOPT EYE DROPS are presented in a plastic dropper bottle with tamper seal. Six different strengths are available. They are 0.5%, 1%, 2%, 3%, 4%, 6%.

Further Information

PILOPT EYE DROPS contain pilocarpine hydrochloride. Pilocarpine hydrochloride is a sterile ophthalmic solution, which is odourless, colourless, hygroscopic crystals or a white or almost white powder. It is soluble 1 in 0.3 of water, 1 in 3 of alcohol; 1 in 360 of chloroform, practically insoluble in ether. A 0.5% solution in carbon dioxide-free water has a pH of 3.5 to 4.5.

Molecular formula of pilocarpine hydrochloride is C11H16N2O2,HCl. Relative molecular mass is 244.7.

Name and Address

Pharmacy Retailing (NZ) Limited
Trading as Healthcare Logistics
58 Richard Pearce Drive
Airport Oaks
Ph (09) 918 5100
Fax (09) 901 5101

Date of Preparation

3 August 2006