Neostigmine

ADMINISTRATION ROUTES:

IV

ALTERNATIVE NAMES:

Bloxiverz, Prostigmin

ICU INDICATIONS:

1. Reversal of neuromuscular blockade
2. Ileus

PRESENTATION AND ADMINISTRATION:

IV:

2.5 mg in 1 mL vial

For reversal of neuromuscular blockade administer with either atropine or glycopyrrolate.

For ileus, add 2.5 mg to 100 mL of compatible IV fluid and administer over 1 - 5 hours (use the longer duration for younger patients or those at risk of bradycardia)

Compatible with the following IV fluids: 0.9% saline, 5% dextrose

Store at room temperature

DOSAGE:

IV:

For reversal of neuromuscular blockade:

2.5 mg neostigmine with 0.6 - 1.2 mg of atropine

For treatment of ileus:

2.5 mg neostigmine over 1-5 hours by infusion

DOSAGE IN RENAL FAILURE AND RENAL REPLACEMENT THERAPY:

Dose as in normal renal function

DOSAGE IN PAEDIATRICS:

IV:

For reversal of neuromuscular blockade:

Add 1.25 mg (0.5 mL) of neostigmine to 0.3 mg (0.5 mL) of atropine to 0.5 mL of 0.9% saline

Give 0.1 mL/kg IV

Note: do NOT use as a treatment for ileus in children due to high risk of symptomatic bradycardia or asystole

CLINICAL PHARMACOLOGY:

Neostigmine inhibits the hydrolysis of acetylcholine by competing with acetylcholine for attachment to acetylcholinesterase at sites of cholinergic transmission. It enhances cholinergic action by facilitating the transmission of impulses across neuromuscular junctions.

CONTRAINDICATIONS:

1. Hypersensitivity to neostigmine
2. Mechanical obstruction of the gastrointestinal tract

WARNINGS:

Neostigmine can cause severe bradycardia or asystole. It should never be administered as bolus without an anticholinergic (such as atropine)

PRECAUTIONS:

General:

Neostigmine methylsulfate should be used with caution in patients with epilepsy, bronchial asthma, bradycardia, recent coronary occlusion, vagotonia, hyperthyroidism, cardiac arrhythmias or peptic ulcer

Laboratory Tests:

No tests in addition to usual ICU tests are indicated

Drug/Laboratory Test Interactions:

None of note

IMPORTANT DRUG INTERACTIONS IN ICU:

Neostigmine methylsulfate does not antagonize, and may in fact prolong, the Phase I block of depolarising muscle relaxants such as succinylcholine

ADVERSE REACTIONS:

Body as a Whole:

Anaphylaxis

Neurologic:

Dizziness, convulsions, loss of consciousness, drowsiness, headache, dysarthria, miosis and visual changes

Cardiovascular:

Cardiac arrhythmias (including bradycardia, tachycardia, A-V block and nodal rhythm), cardiac arrest, syncope and hypotension

Respiratory:

Increased oral, pharyngeal and bronchial secretions, dyspnoea, respiratory depression, respiratory arrest and bronchospasm

Dermatologic:

Rash and urticaria

Gastrointestinal:

Nausea, salivation, cramp, emesis, diarrhoea, flatulence and increased peristalsis

Genitourinary:

Urinary frequency

Musculoskeletal:

Muscle cramps and spasms, arthralgia

Miscellaneous:

Diaphoresis, flushing and weakness