Drug Index

Neostigmine

Mechanism :

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. It also has a direct cholinomimetic effect on skeletal muscle and possibly on autonomic ganglion cells and neurons of the central nervous system.


Indication :

  • Myasthenia gravis
  • Muscle relaxant - reversal of non-depolarising muscle relaxant

Contraindications :

Contraindicated in patients with known hypersensitivity to the drug. Because of the presence of the bromide ion, it should not be used in patients with a previous history of reaction to bromides. It is contraindicated in patients with peritonitis or mechanical obstruction of the intestinal or urinary tract.


Dosing :

Myasthenia gravis:
Diagnosis:
0.025-0.04 mg/kg IM once with atropine.
Treatment:
0.01-0.04 mg/kg IV/IM/SC every 2-3 hours and as and when needed.
Reversal of non-depolarising neuromuscular blockade:
0.03-0.07 mg/kg I. Max: 0.07 mg/kg IV or a total of 5 mg, whichever is lesser.

Adverse Effect :

Cardiac arrhythmias, cardiac arrest, syncope, hypotension, increased oral, pharyngeal and bronchial secretions, and dyspnea. Following injectables: respiratory depression, respiratory arrest and bronchospasm may occur.

Other: allergic reactions (rash, urticaria) and anaphylaxis, dizziness, loss of consciousness, drowsiness, convulsions, headache, dysarthria, miosis, visual changes, nausea, emesis, flatulence and increased peristalsis, increased salivation, muscle cramps, spasms, arthralgia.


Interaction :

Aminoglycosides, Chlorpromazine, Clindamycin, Colistin, Imipenem/Cilastatin, Lithium, Procainamide and Quinidine: Effects of neostigmine are antagonized.
Acetazolamide, Ampicillin, Aspirin, Chloroquine, Dipyridamole, Erythromycin, Hydroxychloroquine, Ketoprofen and Penicillamine: May worsen myasthenia and thus diminish the effect of neostigmine.
Beta-Blockers: Can worsen bradycardia.
Atracurium, Tubocurarine, Pancuronium and Vecuronium: Antagonised.



Renal Dose :

Dose in Renal Impairment GFR (mL/min)
20-5050–100% of normal dose
10-2050–100% of normal dose
<1050–100% of normal dose

Dose in Patients undergoing Renal Replacement Therapies
CAPDUnknown dialysability. Dose as in GFR<10 mL/min
HDUnknown dialysability. Dose as in GFR<10 mL/min
HDF/High fluxUnknown dialysability. Dose as in GFR<10 mL/min
CAV/VVHDUnknown dialysability. Dose as in GFR=10–20 mL/min

Hepatic Dose :

No dose adjustments are recommended.
08/09/2024 22:44:49 Neostigmine
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