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Pilocarpine

Cholinergic (muscarinic) agonist · Miotics, Sialagogues, Glaucoma agents

Also known as Pilocarpine Hydrochloride, Pilocarpine Nitrate, Salagen, Isopto Carpine, Pilocar

START
Ophthalmic 1–2% 1 drop up to QID; oral xerostomia 5 mg PO 3–4×/day
TYPICAL MAX
Oral ~30 mg/day; ophthalmic per regimen
STOP IF
Bronchospasm, severe bradycardia/hypotension, cholinergic crisis, retinal detachment
WATCH
Respiratory (asthma/COPD), heart rate, sweating/cholinergic symptoms, vision/retina in at-risk eyes
CDSCO approvedSchedule HATC S01EB01
Dose laddermg/d
5start20common oral/day30oral max/day
Renal dose adjustmenteGFR mL/min/1.73m²
FULLNo specific dose adjustment at any eGFR90

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours
20minONSET1hPEAK1h4hDURATION
ONSET
20min · effect onset
PEAK
1h · peak effect
1h · plasma t½
DURATION
4h · effect duration
EXCRETION
Esterase inactivation; renal
route + CYP
INTERACTIONS
2 major
SEVERE in our sources
PREGNANCY
Use only if clearly needed — limited data
FDA category + note
Top interactionssee all 5
  • Beta BlockersSevereDatabaseKimi deep-research + Cla
  • SiponimodSevereDatabaseDDInter
Available in India

15 branded formulations and 2 fixed-dose combinations. Look up specific brands in the Drugs workspace.

Mechanism

Directly stimulates muscarinic receptors — ocular: ciliary muscle contraction (accommodation) and pupillary sphincter contraction (miosis) opening the trabecular meshwork (lowers IOP); systemic (oral): stimulates exocrine glands (saliva).

Indications

Open-angle glaucoma; acute angle-closure glaucoma (emergency miosis)Reversal of mydriasis; presbyopia (low-dose ophthalmic)Xerostomia (Sjögren syndrome, post head-and-neck radiation — oral)

Dosing

Adult
Ophthalmic 1–2% : 1 drop up to 4×/day (acute angle-closure more frequent initially). Oral xerostomia: 5 mg PO 3–4×/day (radiation); Sjögren 5 mg QID; presbyopia drop once daily.
Pediatric
Ophthalmic per specialist.
Renal adjustment
No specific adjustment.
Hepatic adjustment
Moderate hepatic impairment: reduce oral dose (e.g. 5 mg BID).
Geriatric
Cautious; cardiac/respiratory comorbidity.
Max dose
Oral ~30 mg/day (xerostomia); ophthalmic per regimen

Pharmacokinetics

Onset
Ocular miosis 10–30 min; salivary effect ~20 min (oral)
Peak effect
Ocular IOP ~75 min; oral ~1 h
Duration
Ocular 4–8 h; oral ~3–5 h
Half-life
Oral ~0.8–1.3 h (dose-dependent)
Bioavailability
Oral well absorbed; ocular topical
Protein binding
Low
Metabolism
Inactivation at neuronal synapses/plasma (esterase); hepatic
Excretion
Renal

Contraindications

  • Acute iritis/anterior uveitis (ocular)
  • Uncontrolled asthma/COPD (bronchospasm)
  • Acute heart failure / significant bradyarrhythmia
  • Narrow-angle where pupillary block would worsen (specific scenarios)
  • Hypersensitivity to pilocarpine

Side effects

Common
Sweating (oral — prominent)Ocular: brow ache, blurred/dim vision, miosisIncreased salivation, nauseaRhinitis, urinary frequency
Serious
  • Bronchospasm/pulmonary oedema (asthma/COPD)
  • Severe bradycardia/AV block, hypotension
  • Retinal detachment (predisposed eyes, ocular)
  • Cholinergic crisis (overdose)

Pregnancy & lactation

Pregnancy

Use only if clearly needed — limited data

Lactation

Unknown excretion; caution (oral); ophthalmic minimal systemic

Drug interactions

Beta Blockers
Severe
Database

Additive bradycardia/conduction effects

Monitor heart rate; caution

Source: Kimi deep-research + Cla

Siponimod
Severe
Database

Clinical effect not specified

Source: DDInter

Anticholinergics
Moderate
Database

Mutual antagonism — reduced efficacy of both

Avoid concurrent; counsel

Source: Kimi deep-research + Cla

Drugs Causing Bronchospasm
Moderate
Database

Additive airway effects

Avoid in uncontrolled asthma/COPD

Source: Kimi deep-research + Cla

Other Cholinergics
Moderate
Database

Additive cholinergic toxicity

Avoid combination; monitor

Source: Kimi deep-research + Cla

7 additional low-confidence interactions hidden — those rows lack a documented mechanism or management plan in our sources.

Related guidelines

Ask House about Pilocarpine

Continue into a citation-backed clinical answer with the drug context already attached.

Sources: KD Tripathi 7e, Goodman & Gilman 14e, Katzung, BNF·Verified: 2026-05-19 · House clinical team·Cockpit curated: 2026-05-19