Drug reference

Neostigmine

Reversible acetylcholinesterase inhibitor (quaternary) · Antimyasthenic; Reversal of Neuromuscular Blockade

Also known as Neostigmine Methylsulfate, Prostigmin

START

Reversal 0.04–0.07 mg/kg IV WITH atropine/glycopyrrolate (after some spontaneous recovery); myasthenia 15–30 mg PO q3–4h

TYPICAL MAX

Reversal ≤~5 mg total IV

STOP IF

Severe bradycardia/bronchospasm, cholinergic crisis

WATCH

Co-administer antimuscarinic for reversal, neuromuscular monitoring (avoid recurarisation), HR/secretions; distinguish myasthenic vs cholinergic crisis

CDSCO approvedSchedule HJan AushadhiATC N07AA01

Dose laddermg/d

Renal dose adjustmenteGFR mL/min/1.73m²

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours

ONSET: 3min · IV onset (~3 min)
PEAK: 9min · IV peak (~9 min)
t½: 1h · plasma t½
DURATION: 1.5h · IV reversal duration

EXCRETION

Cholinesterase hydrolysis; ~50% renal unchanged

route + CYP

INTERACTIONS

7 major

SEVERE in our sources

PREGNANCY

Use if needed (myasthenia/reversal) — limited data; transient neonatal weakness possible near term

FDA category + note

Top interactionssee all 12 →

BupropionSevereDatabaseDDInter
IohexolSevereDatabaseDDInter
IopamidolSevereDatabaseDDInter
Depolarising BlockersSevereDatabaseKimi deep-research + Cla

Available in India

11 branded formulations and 5 fixed-dose combinations. Look up specific brands in the Drugs workspace.

Jan Aushadhi — generic available at GoI pharmacies

Mechanism

Reversibly inhibits acetylcholinesterase, increasing acetylcholine at nicotinic (neuromuscular junction) and muscarinic synapses → reversal of non-depolarising neuromuscular blockade, increased GI/bladder motility and improved myasthenic strength.

Indications

Reversal of non-depolarising neuromuscular blockade (with an antimuscarinic)Myasthenia gravis (symptomatic)Postoperative ileus / urinary retention (non-obstructive)

Dosing

Adult: Reversal: 0.04–0.07 mg/kg IV (max ~5 mg) WITH atropine/glycopyrrolate. Myasthenia: 15–30 mg PO every 3–4 h (individualised); 0.5 mg SC/IM. Ileus/retention: 0.5–2.5 mg SC/IM.
Pediatric: Reversal 0.04 mg/kg with antimuscarinic (specialist).
Renal adjustment: Renally cleared — reduce dose/extend interval in impairment (prolonged effect).
Hepatic adjustment: No specific adjustment.
Geriatric: Cautious dosing; cholinergic effects.
Max dose: Reversal generally ≤5 mg total IV

Pharmacokinetics

Onset

IV ~1–3 min; IM ~20–30 min; oral ~30–60 min

Peak effect

IV ~7–11 min

Duration

~1–2 h (IV); oral 2–4 h

Half-life

~0.5–1.5 h (prolonged in renal impairment)

Bioavailability

Oral poor (~1–2%) — quaternary

Protein binding

~15–25%

Metabolism

Plasma cholinesterase hydrolysis + hepatic

Excretion

Renal (~50% unchanged)

Contraindications

Mechanical GI or urinary obstruction
Peritonitis
Hypersensitivity to neostigmine/bromides
Caution: asthma, bradyarrhythmia, recent coronary occlusion

Side effects

Common

Muscarinic: bradycardia, salivation, sweating, nausea/abdominal cramps, miosisIncreased bronchial secretions

Serious

Severe bradycardia/asystole, hypotension
Bronchospasm/pulmonary oedema
Cholinergic crisis (overdose — weakness, fasciculation, respiratory failure)
Recurarisation (if block deeper than reversal capacity)

Pregnancy & lactation

Pregnancy

Use if needed (myasthenia/reversal) — limited data; transient neonatal weakness possible near term

Lactation

Limited data; low oral bioavailability — caution/monitor infant

Drug interactions

Bupropion

Severe

Database

Drug interaction classified as: synergy

Source: DDInter

Iohexol

Severe

Database

Clinical effect not specified

Source: DDInter

Iopamidol

Severe

Database

Clinical effect not specified

Source: DDInter

Depolarising Blockers

Severe

Database

Prolongs/potentiates phase I block (cholinesterase inhibition)

Avoid neostigmine soon after succinylcholine

Source: Kimi deep-research + Cla

Siponimod

Severe

Database

Clinical effect not specified

Source: DDInter

Succinylcholine

Severe

Database

Neostigmine is not effective against the skeletal muscle paralysis caused by succinylcholine; instead, it will enhance depolarization and the resultant blockade, potentially worsening paralysis.

Avoid combination or use with extreme caution. Neostigmine should not be used to reverse succinylcholine-induced paralysis.

Source: DDInter

Tramadol

Severe

Database

Clinical effect not specified

Source: DDInter

Competitive Neuromuscular Blockers

Moderate

Textbook

Rapid reversal of muscle paralysis.

Administer neostigmine 0.5–2.0 mg (30–50 g/kg) i.v., preceded by atropine or glycopyrrolate 10 g/kg to block muscarinic effects.

Source: KDT 7e · p110

Glycopyrrolate

Moderate

Textbook

Serious cardiac arrhythmias have occasionally occurred (in context of neostigmine with antimuscarinics).

Glycopyrrolate is used to block the parasympathomimetic effects of neostigmine when reversing skeletal muscle relaxation after surgery.

Source: G&G 14e · p218

Tubocurarine

Moderate

Textbook

The competitive block caused by tubocurarine is antagonized and reversed by neostigmine.

Neostigmine is used for pharmacological reversal of tubocurarine's effects.

Source: KDT 7e · p348, Table 25.1

Atropine

Moderate

Database

Serious cardiac arrhythmias have occasionally occurred.

Atropine is used to block responses to vagal reflexes induced by surgical manipulation of visceral organs, and to block parasympathomimetic effects of neostigmine. Clinicians should be aware of the potential for cardiac arrhythmias.

Source: DDInter

Aminoglycosides

Moderate

Database

Aminoglycoside neuromuscular blockade antagonises reversal

Awareness; may need higher reversal/ventilation

Source: Kimi deep-research + Cla