pilocarpine (Pilocar, Isopto Carpine, Salagen, Ocusert Pilo)
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Introduction
Tradename: Pilocar, Isopto Carpine. (pilocarpine HCl).
Indications
- glaucoma
- counteract effects of cycloplegics
- management of post-radiation xerostomia
- presbyopia (Vuity)
Contraindications
(oral)
- uncontrolled asthma
Dosage
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
- dose-related increase in salivary flow
- onset of action is 20 minutes
- duration of action is 3-5 hours
- absorption is decreased when taken with a fatty meal
- metabolized by neuronal synapses & plasma
- 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
- common (> 10%)
- less common (1-10%)
- headache, stinging, burning, lacrimation, ciliary spasm, retinal detachment, browache, photophobia, acute iritis, conjunctival & ciliary congestion early in therapy, hypersensitivity
- uncommon (< 1%)
- 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
- beta-blockers in combination can worsen cardiac conduction disturbances
- anticholinergic agents & diphenhydramine antagonize effects of pilocarpine
- separate from latanoprost by at least 1 hour (CVS)
- drug interaction(s) of cholinesterase inhibitors with NSAIDs
- drug interaction(s) of parasympatholytic with parasympathomimetic
Mechanism of action
- cholinergic agent
- stimulates parasympathetic system
- increased secretion of sweat glands, salivary glands, lacrimal glands, gastric glands, pancreatic glands & intestinal glands
- stimulates gastric motility
- increases gastric tone
- restores impaired rhythmic peristalsis
- 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]
- pilocarpine may also decrease aqueous formation with long term administration[4]
More general terms
Component of
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ 2.0 2.1 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
- ↑ 4.0 4.1 4.2 4.3 Pilocarpine Eye Drops BP 2.0% w/v https://www.medicines.org.uk/emc/product/3399/smpc