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pyridostigmine

Reversible acetylcholinesterase inhibitor (quaternary) · Anticholinesterase; Treatment for Myasthenia Gravis; Prophylaxis for Nerve Agent Poisoning

START
60 mg PO every 4–6 h, individualise
TYPICAL MAX
~1500 mg/day (rarely; cholinergic-crisis risk)
STOP IF
Cholinergic crisis (worsening weakness + muscarinic excess)
WATCH
Strength vs cholinergic signs, HR, secretions; distinguish crises
CDSCO approvedATC N07AA02
Dose laddermg/d
60per dose360usual/day1.5kmax/day
Renal dose adjustmenteGFR mL/min/1.73m²
FULLUsual dosing50REDUCEReduce dose (prolonged effect)10REDUCEMarked red…90

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours
24minONSET1.5hPEAK3.5h5hDURATION
ONSET
24min · absorption
PEAK
1.5h · peak effect
3.5h ·
DURATION
5h · per dose
EXCRETION
Renal — substantial unchanged
route + CYP
INTERACTIONS
1 major
SEVERE in our sources
PREGNANCY
Used in pregnancy for myasthenia gravis when needed (benefit usually outweighs risk).
FDA category + note
Top interactionssee all 6
  • SiponimodSevereDatabaseDDInter

Mechanism

Reversibly inhibits acetylcholinesterase, increasing acetylcholine at neuromuscular junctions; quaternary amine with limited CNS penetration — improves muscle strength in myasthenia gravis.

Indications

Myasthenia gravis (symptomatic)Reversal of non-depolarising neuromuscular blockade (with atropine)Pre-treatment against Soman nerve-agent poisoning (military)

Dosing

Adult
MG: 60 mg PO every 4–6 h (range 30–120 mg/dose), individualised; sustained-release 180 mg once–twice daily. Max ~1500 mg/day rarely.
Pediatric
7 mg/kg/day in 5–6 divided doses.
Renal adjustment
Renally excreted — reduce dose in impairment (prolonged effect).
Hepatic adjustment
No specific adjustment.
Geriatric
Lower doses; monitor for cholinergic effects.
Max dose
~1500 mg/day (rarely needed; cholinergic crisis risk)

Pharmacokinetics

Onset
~15–30 min (oral)
Peak effect
~1–2 h
Duration
~3–6 h (sustained-release longer)
Half-life
~3–4 h (longer in renal impairment)
Bioavailability
Low (~10–20%, quaternary)
Protein binding
Low
Metabolism
Hepatic + plasma cholinesterase hydrolysis
Excretion
Renal (substantial unchanged)

Contraindications

  • Mechanical GI or urinary obstruction
  • Hypersensitivity to pyridostigmine/bromides
  • Caution: asthma, bradyarrhythmia, peptic ulcer

Side effects

Common
Abdominal cramps/diarrhoeaIncreased salivation/secretionsNauseaSweatingMuscle fasciculationsMiosis
Serious
  • Cholinergic crisis (excess dosing — weakness mimicking myasthenic crisis)
  • Bradycardia/AV block
  • Bronchospasm
  • Respiratory failure

Pregnancy & lactation

Pregnancy

Used in pregnancy for myasthenia gravis when needed (benefit usually outweighs risk).

Lactation

Compatible (minimal milk levels; monitor infant).

Drug interactions

Siponimod
Severe
Database

Clinical effect not specified

Source: DDInter

Aminoglycosides
Moderate
Database

Neuromuscular blockade worsens MG

Avoid; choose alternative antibiotic

Source: Kimi deep-research + Cla

Anticholinergics
Moderate
Database

Antagonism of muscarinic effects

Use intentionally to limit muscarinic AEs; monitor

Source: Kimi deep-research + Cla

Beta Blockers
Moderate
Database

Additive bradycardia

Monitor HR

Source: Kimi deep-research + Cla

Non Depolarising Neuromuscular Blockers
Moderate
Database

Antagonism (intended for reversal)

Use deliberately for reversal; caution in MG anaesthesia

Source: Kimi deep-research + Cla

Succinylcholine
Moderate
Database

Reduced pseudocholinesterase → prolonged block

Anticipate prolonged succinylcholine effect

Source: Kimi deep-research + Cla

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

Related guidelines

Other Reversible acetylcholinesterase inhibitor (quaternary) drugs

Ask House about pyridostigmine

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Sources: KD Tripathi 7e, Goodman & Gilman 14e·Verified: 2026-05-20 · House clinical team·Cockpit curated: 2026-05-20