Drugs List

Therapeutic Indications

Uses

Chronic open-angle glaucoma
Acute closed-angle glaucoma alone or in conjunction with other agents to decrease intra-ocular pressure prior to surgical treatment
Miosis - to counteract the effects of cycloplegic or mydriatic drops

Administration

For ocular use.

Contraindications

Acute iritis
Anterior uveitis
Inflammatory glaucoma
Soft contact lenses

Precautions and Warnings

Systemic reactions must be considered in the treatment of acute closed-angle glaucoma because of the higher doses given. Caution is particularly advised in patients with acute heart failure, bronchial asthma, peptic ulceration, hypertension, hypotension, urinary tract obstruction, epilepsy, hyperthyroidism and Parkinson's disease.

Caution should also be taken in patients with conjunctival or corneal damage.

Retinal detachment has been associated with the use of miotics in susceptible individuals and those with pre-existing retinal disease, therefore fundus examination is advised in all patients prior to the initiation of therapy.

Patients with chronic open-angle glaucoma receiving long-term pilocarpine therapy should have regular monitoring of intraocular pressure and visual fields.

Systemic absorption may be reduced by compressing the lacrimal sac at the medial canthus during and for one minute following instillation of the drops.

Pregnancy - see 'Pregnancy' section.

Breastfeeding - see 'Lactation' section.

Caution is necessary when night driving and when hazardous tasks are undertaken in poor illumination as this medication causes difficulty with dark adaptation. Pilocarpine impairs accommodation by paralysis or spasm and patients should not drive or operate machinery if they experience blurred vision.

Some formulations contain benzalkonium chloride; soft contact lenses should not be worn during treatment.

Pregnancy and Lactation

Pregnancy

Pilocarpine is used topically in the eye for glaucoma. No reports of developmental toxicity attributable to the drug have been located. However, animal reproduction studies have observed toxicity with oral doses less than or equal to 10 times the human dose.

A single report of the topical use during pregnancy has been located. A woman with glaucoma was treated throughout gestation with topical pilocarpine (two drops twice daily), timolol (two drops each eye), and oral acetazolamide (2). Within 48 hours of delivery at 36 weeks' gestation, the infant presented with hyperbilirubinemia, hypocalcaemia, hypomagnesaemia and metabolic acidosis. The toxic effects, attributed to the carbonic anhydrase inhibitor acetazolamide resolved quickly on treatment. Milk hypertonicity requiring physiotherapy was observed at examinations at 1, 3 and 8 months of age.

The manufacturer notes that pilocarpine eye drops should only be used if essential during pregnancy and that systemic absorption may occur and mothers using the drops may give birth to infants with signs mimicking neonatal meningitis such as restlessness, convulsions, diaphoresis and hypothermia.

The use of all medication in pregnancy should be avoided whenever possible; particularly in the first trimester. Non-drug treatments should also be considered. When essential, a medication with the best safety record over time should be chosen, employing the lowest effective dose for the shortest possible time. Polypharmacy should be avoided. Teratogens taken in the pre-embryonic period, often quoted as lasting until 14-17 days post-conception, are believed to have an all-or-nothing effect. Where drugs have a short half-life, and when the date of conception is certain, this may allow women to be reassured where drug exposure has occurred within this time frame. Further advice may be available from the UK National Teratology Information Service (NTIS) and through ToxBase, available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).

Lactation

Pilocarpine is a direct acting cholinergic agent used primarily in the eyes for treatment of open-angle glaucoma. The ophthalmic dose is approximately 1mg or less per day. It is not know if pilocarpine enters milk, but it probably does in low levels due to its minimal plasma level. It is not likely that an infant would receive a clinical dose via milk, but this is presently unknown. Side effects would largely include diarrhoea, gastric upset, excessive salivation, and other typical cholinergic symptoms.

The manufacturer notes that this medication should only be used whilst breastfeeding when clearly indicated.

Neonates, infants born prematurely, those with low birth weight, those with an unstable gastrointestinal function or who have serious illnesses may require special consideration. For any infant, if a drug is prescribed to the nursing mother, it should be at the lowest practical dose and for the shortest time. When drug administration is unavoidable and breastfeeding is to continue, minimisation of exposure of the infant to the drug may sometimes be achieved by timing the maternal doses to just after a feeding episode. Infants exposed to drugs via breast milk should be monitored for unusual signs or symptoms. Interactions between the drug received by the infant from the mother's milk and medication prescribed for the infant should also be considered, for example, when the drug given to the infant may prevent metabolism of the drug received via breast milk.
Specialist advice is available from the UK Drugs in Lactation Advisory Service at https://www.midlandsmedicines.nhs.uk/content.asp?section=6&subsection=17&pageIdx=1

Side Effects

Burning sensation (local)
Itching sensation (local)
Smarting
Blurred vision
Ciliary spasm
Conjunctival vascular congestion
Myopia (transient)
Sensitisation of eyelids
Sensitisation of conjunctiva
Reduced visual acuity in poor light
Lens changes (chronic use)
Increased pupillary block
Vitreous haemorrhage
Brow ache
Headache
Blood pressure changes
Bronchospasm
Pulmonary oedema
Salivation
Sweating
Nausea
Vomiting
Diarrhoea
Lacrimation
Retinal detachment
Tremor
Bradycardia

Presentation

Eye drops containing:-

Pilocarpine hydrochloride 0.5%
Pilocarpine hydrochloride 1%
Pilocarpine hydrochloride 2%
Pilocarpine hydrochloride 3%
Pilocarpine hydrochloride 4%

Drugs List

Therapeutic Indications

Uses

Chronic open-angle glaucoma
Acute closed-angle glaucoma alone or in conjunction with other agents to decrease intra-ocular pressure prior to surgical treatment
Miosis - to counteract the effects of cycloplegic or mydriatic drops

Dosage

Adults

Children

Administration

For ocular use.

Contraindications

Acute iritis
Anterior uveitis
Inflammatory glaucoma
Soft contact lenses

Precautions and Warnings

Systemic reactions must be considered in the treatment of acute closed-angle glaucoma because of the higher doses given. Caution is particularly advised in patients with acute heart failure, bronchial asthma, peptic ulceration, hypertension, hypotension, urinary tract obstruction, epilepsy, hyperthyroidism and Parkinson's disease.

Caution should also be taken in patients with conjunctival or corneal damage.

Retinal detachment has been associated with the use of miotics in susceptible individuals and those with pre-existing retinal disease, therefore fundus examination is advised in all patients prior to the initiation of therapy.

Patients with chronic open-angle glaucoma receiving long-term pilocarpine therapy should have regular monitoring of intraocular pressure and visual fields.

Systemic absorption may be reduced by compressing the lacrimal sac at the medial canthus during and for one minute following instillation of the drops.

Pregnancy - see 'Pregnancy' section.

Breastfeeding - see 'Lactation' section.

Caution is necessary when night driving and when hazardous tasks are undertaken in poor illumination as this medication causes difficulty with dark adaptation. Pilocarpine impairs accommodation by paralysis or spasm and patients should not drive or operate machinery if they experience blurred vision.

Some formulations contain benzalkonium chloride; soft contact lenses should not be worn during treatment.

Pregnancy and Lactation

Pregnancy

Pilocarpine is used topically in the eye for glaucoma. No reports of developmental toxicity attributable to the drug have been located. However, animal reproduction studies have observed toxicity with oral doses less than or equal to 10 times the human dose.

A single report of the topical use during pregnancy has been located. A woman with glaucoma was treated throughout gestation with topical pilocarpine (two drops twice daily), timolol (two drops each eye), and oral acetazolamide (2). Within 48 hours of delivery at 36 weeks' gestation, the infant presented with hyperbilirubinemia, hypocalcaemia, hypomagnesaemia and metabolic acidosis. The toxic effects, attributed to the carbonic anhydrase inhibitor acetazolamide resolved quickly on treatment. Milk hypertonicity requiring physiotherapy was observed at examinations at 1, 3 and 8 months of age.

The manufacturer notes that pilocarpine eye drops should only be used if essential during pregnancy and that systemic absorption may occur and mothers using the drops may give birth to infants with signs mimicking neonatal meningitis such as restlessness, convulsions, diaphoresis and hypothermia.

The use of all medication in pregnancy should be avoided whenever possible; particularly in the first trimester. Non-drug treatments should also be considered. When essential, a medication with the best safety record over time should be chosen, employing the lowest effective dose for the shortest possible time. Polypharmacy should be avoided. Teratogens taken in the pre-embryonic period, often quoted as lasting until 14-17 days post-conception, are believed to have an all-or-nothing effect. Where drugs have a short half-life, and when the date of conception is certain, this may allow women to be reassured where drug exposure has occurred within this time frame. Further advice may be available from the UK National Teratology Information Service (NTIS) and through ToxBase, available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).

Lactation

Pilocarpine is a direct acting cholinergic agent used primarily in the eyes for treatment of open-angle glaucoma. The ophthalmic dose is approximately 1mg or less per day. It is not know if pilocarpine enters milk, but it probably does in low levels due to its minimal plasma level. It is not likely that an infant would receive a clinical dose via milk, but this is presently unknown. Side effects would largely include diarrhoea, gastric upset, excessive salivation, and other typical cholinergic symptoms.

The manufacturer notes that this medication should only be used whilst breastfeeding when clearly indicated.

Neonates, infants born prematurely, those with low birth weight, those with an unstable gastrointestinal function or who have serious illnesses may require special consideration. For any infant, if a drug is prescribed to the nursing mother, it should be at the lowest practical dose and for the shortest time. When drug administration is unavoidable and breastfeeding is to continue, minimisation of exposure of the infant to the drug may sometimes be achieved by timing the maternal doses to just after a feeding episode. Infants exposed to drugs via breast milk should be monitored for unusual signs or symptoms. Interactions between the drug received by the infant from the mother's milk and medication prescribed for the infant should also be considered, for example, when the drug given to the infant may prevent metabolism of the drug received via breast milk.
Specialist advice is available from the UK Drugs in Lactation Advisory Service at https://www.midlandsmedicines.nhs.uk/content.asp?section=6&subsection=17&pageIdx=1

Effects on Ability to Drive and Operate Machinery

Caution is necessary when night driving and when hazardous tasks are undertaken in poor illumination as this medication causes difficulty with dark adaptation. Pilocarpine impairs accommodation by paralysis or spasm and patients should not drive or operate machinery if they experience blurred vision.

Counselling

Advise patient to wash their hands prior to use.

Advise patient to avoid contact of the container with eye or other surfaces as contamination leading to
ophthalmic infection may occur.

Advise patient to leave an interval of at least 5 minutes before instilling another ophthalmic medication.

Advise patient to compress the lacrimal sac during administration and for one minute afterwards, to reduce systemic absorption.

Advise patient that caution is necessary when night driving and when hazardous tasks are undertaken in poor illumination as this medication causes difficulty with dark adaptation. Pilocarpine impairs accommodation by paralysis or spasm and patients should not drive or operate machinery if they experience blurred vision.

Advise patient to discard 4 weeks after first opening.

Side Effects

Burning sensation (local)
Itching sensation (local)
Smarting
Blurred vision
Ciliary spasm
Conjunctival vascular congestion
Myopia (transient)
Sensitisation of eyelids
Sensitisation of conjunctiva
Reduced visual acuity in poor light
Lens changes (chronic use)
Increased pupillary block
Vitreous haemorrhage
Brow ache
Headache
Blood pressure changes
Bronchospasm
Pulmonary oedema
Salivation
Sweating
Nausea
Vomiting
Diarrhoea
Lacrimation
Retinal detachment
Tremor
Bradycardia

Overdosage

It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.

The following number will direct the caller to the relevant local centre (0844) 892 0111

Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet (https://www.toxbase.org/).

Shelf Life and Storage

Store upright, below 25 degrees C in a dry place.
Protect from light.

Further Information

Last Full Review Date: April 2012.

Reference Sources

Drugs in Pregnancy and Lactation: A Reference Guide to Fetal and Neonatal Risk, 9th edition (2011) ed. Briggs, G., Freeman, R. and Yaffe, S. Lippincott Williams & Wilkins, Philadelphia.

Medications and Mothers' Milk, 14th Edition (2010) Hale, T. Hale Publishing, Amarillo, Texas.

Summary of Product Characteristics: Pilocarpine eye drops 1%. Martindale Pharmaceuticals Ltd. Revised April 2016.

Summary of Product Characteristics: Pilocarpine eye drops 2%. Martindale Pharmaceuticals Ltd. Revised April 2016.

Summary of Product Characteristics: Pilocarpine eye drops 4%. Martindale Pharmaceuticals Ltd. Revised April 2016.

NICE Evidence Services Available at: www.nice.org.uk Last accessed: 31 August 2017