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pilocarpine (Pilocar, Isopto Carpine, Salagen, Ocusert Pilo)
Tradename: Pilocar, Isopto Carpine. (pilocarpine HCl).
Indications:
1) glaucoma
a) open-angle glaucoma
b) acute narrow-angle glaucoma
c) some secondary glaucomas
2) counteract effects of cycloplegics
3) management of post-radiation xerostomia
4) presbyopia (Vuity)
Contraindications: (oral)
- uncontrolled asthma
Dosage:
1) 1 drop OU 4-6 times per day
2) 5-10 mg PO TID, titrate to effect (lowest possible dose)
Ophthalmic: gel 4% (5 g)
Ophthalmic: solution
- 0.25%, 0.5%, 1%, 2%, 3%, 4%, 5%, 6%, 8%, 10% (15 mL).
- 2%, 10 mL, 15 mL
- 1.3% Vuity for presbyopia
Tabs: 5 mg.
Therapeutic systems: Ocusert-Pilo-40:
- releases 40 ug/hour for 1 week (8)
Storage: ophthalmic 15-25 C
Pharmacokinetics:
1) dose-related increase in salivary flow
2) onset of action is 20 minutes
3) duration of action is 3-5 hours
4) absorption is decreased when taken with a fatty meal
5) metabolized by neuronal synapses & plasma
6) eliminated in urine
* ophthalmic administration
- onset of miosis a occurs within 10-30 minutes, with maximal effect within 30 minutes
- miosis usually persists for 4-8 hours, rarely, up to 20 hours
- reduction of intra-ocular pressure is evident within 60 minutes, peaks within 75 minutes & persists for 4-14 hours
- spasms of accommodation commence in about 15 minutes & persist for 2-3 hours
Adverse effects:
1) common (> 10%)
- blurred vision, miosis
2) less common (1-10%)
- headache, stinging, burning, lacrimation, ciliary spasm, retinal detachment, browache, photophobia, acute iritis, conjunctival & ciliary congestion early in therapy, hypersensitivity
3) uncommon (< 1%)
- hypertension, tachycardia, nausea/vomiting, diarrhea, sweating, salivation
4) other [2]
- abdominal cramps
- flushing
- bronchial constriction
- runny nose
- sore throat
- urinary frequency
- difficulty with dark adaptation
- due to its activity at the muscarinic receptor sites of the ciliary muscles & iris sphincter, pilocarpine causes varying degrees of accommodation spasm & pupillary constriction [4]
Drug interactions:
1) beta-blockers in combination can worsen cardiac conduction disturbances
2) anticholinergic agents & diphenhydramine antagonize effects of pilocarpine
3) separate from latanoprost by at least 1 hour (CVS)
Mechanism of action:
1) cholinergic agent
2) stimulates parasympathetic system
a) increased secretion of sweat glands, salivary glands, lacrimal glands, gastric glands, pancreatic glands & intestinal glands
b) stimulates gastric motility
c) increases gastric tone
d) restores impaired rhythmic peristalsis
e) believed to directly stimulate longitudinal muscle of the ciliary body, which in turn affects the scleral spur, widening the trabecular spaces & allowing for increased aqueous flow [4]
f) pilocarpine may also decrease aqueous formation with long term administration [4]
Interactions
drug interactions
drug adverse effects of cholinesterase inhibitors
General
alkaloid
cholinesterase inhibitor
miotic agent
Properties
MISC-INFO: pregnancy-category C
safety in lactation ?
Database Correlations
PUBCHEM correlations
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998
- Kaiser Permanente Northern California Regional Drug
Formulary, 1998
- Pilocarpine Eye Drops BP 2.0% w/v
https://www.medicines.org.uk/emc/product/3399/smpc
Component-of
betaxolol/pilocarpine
epinephrine/pilocarpine (E-Pilo-x PxEx)