Formulary
Pilocarpine: Indications, Dosing, Side Effects and Interactions
When used by eye: Pilocarpine acts by opening the inefficient drainage channels in the trabecular meshwork.
MedNext Academy | 4 min read
Pilocarpine: Indications, Dosing, Side Effects and Interactions
When used by eye: Pilocarpine acts by opening the inefficient drainage channels in the trabecular meshwork.
Drug action
When used by eye: Pilocarpine acts by opening the inefficient drainage channels in the trabecular meshwork.
Indications and dose
**Primary angle-closure glaucoma,Some secondary glaucomas**
- **Adult** (To The Eye): Apply up to 4 times a day.
**Xerostomia following irradiation**
- **Adult** (By Mouth): for head and neck cancer 5 mg 3 times a day for 4 weeks, then increased if tolerated to up to 30 mg daily in divided doses if required, dose to be taken with or immediately after meals (last dose always with evening meal), maximum therapeutic effect normally within 4-8 weeks; discontinue if no improvement after 2-3 months.
**Dry mouth and dry eyes in Sjgren's syndrome**
- **Adult** (By Mouth): 5 mg 4 times a day; increased if tolerated to up to 30 mg daily in divided doses if required, dose to be taken with meals and at bedtime, discontinue if no improvement after 2-3 months.
**Raised intra-ocular pressure for pilocarpine**
- **Child 1 month-1 year** (To the eye): Apply 1 drop 3 times a day, doses are for 0.5% or 1% solution.
- **Child 2-17 years** (To the eye): Apply 1 drop 4 times a day.
**Pre- and postoperatively in goniotomy and trabeculotomy for pilocarpine**
- **Child** (To the eye): Apply once daily, 1% or 2% solution to be applied.
Cautions
When used by eye A darkly pigmented iris may require a higher concentration of the miotic or more frequent administration and care should be taken to avoid overdosage; asthma; cardiac disease; care in conjunctival damage; care in corneal damage; epilepsy; gastro-intestinal spasm; hypertension; hyperthyroidism; hypotension; marked vasomotor instability; Parkinson's disease; peptic ulceration; retinal detachment has occurred in susceptible individuals and those with retinal disease; urinary-tract obstruction With oral use Asthma (avoid if uncontrolled); biliary-tract disease; cardiovascular disease (avoid if uncontrolled); cholelithiasis; chronic obstructive pulmonary disease (avoid if uncontrolled); cognitive disturbances; maintain adequate fluid intake to avoid dehydration associated with excessive sweating; peptic ulceration; psychiatric disturbances; risk of increased renal colic; risk of increased urethral smooth muscle tone; susceptibility to angle-closure glaucoma
Contraindications
When used by eye Acute iritis; anterior uveitis; conditions where pupillary constriction is undesirable; some forms of secondary glaucoma (where pupillary constriction is undesirable) With oral use Acute iritis; uncontrolled asthma (increased bronchial secretions and increased airways resistance); uncontrolled cardiorenal disease; uncontrolled chronic obstructive pulmonary disease (increased bronchial secretions and increased airways resistance)
Side effects
General side-effects: Common or very common Diarrhoea; headache; hyperhidrosis; hypersalivation; nausea; skin reactions; vision disorders; vomiting Frequency not known Hypotension Specific side-effects: Common or very common With oral use Asthenia; conjunctivitis; constipation; dizziness; excessive tearing; eye pain; flushing; gastrointestinal discomfort; hypersensitivity; hypertension; increased risk of infection; palpitations; urinary disorders Uncommon With oral use Gastrointestinal disorders Frequency not known When used by eye (topical) Bradycardia; bronchospasm; conjunctival vascular congestion; eye disorder (long term use); eye disorders; lens changes (long term use); pain; paraesthesia; pulmonary oedema; sensitisation; vitreous haemorrhage With oral use Affective disorder; agitation; arrhythmias; atrioventricular block; chills; confusion; hallucination; memory loss; psychiatric disorder; respiratory distress; shock; tremor
Interactions
**Other interactions (7):**
- Cyclopentolate may interfere with the ocular anti-hypertensive action of carbachol, pilocarpine, or ophthalmic cholinesterase inhibitors.
- Pharmacodynamic interactions Because of its mechanism of action, galantamine should not be given concomitantly with other cholinomimetics (such as ambenonium, donepezil, neostigmine, pyridostigmine,...
- Treatment with fingolimod should not be initiated in patients receiving beta blockers, or other substances which may decrease heart rate, such as class Ia and III antiarrhythmics, calcium channel...
- If systemic absorption occurs, pilocarpine may enhance the effects of alcohol and anticholinesterases and diminish the effects of anticholinergics.
- The effects of pilocarpine may be enhanced by anticholinesterases, MAOI's, phenothiazines, antihistamines and tricyclic antidepressants.
- Adrenergic blockers may decrease the effects of pilocarpine.
Pregnancy
When used by eye: Avoid unless the potential benefit outweighs risk-limited information available. With oral use: Avoid-smooth muscle stimulant; toxicity in animal studies.
Breast feeding
When used by eye: Avoid unless the potential benefit outweighs risk-no information available. With oral use: Manufacturer advises avoid-present in milk in animal studies.
Hepatic impairment
With oral use: Manufacturer advises caution in moderate to severe cirrhosis. Dose adjustments With oral use: Manufacturer advises initial dose reduction in moderate to severe cirrhosis.
Renal impairment
With oral use: Manufacturer advises caution with tablets.
Medicinal forms
Solution,Tablet,Drops
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
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