Administer dose of 0.5 to 2.5 mg subcutaneously/intramuscularly/ intravenously every day
Take a maintenance dose of 15 to 375 mg daily orally divided every 6 to 8 hours
Administer injectable containing 0.6 to 1.2 mg of atropine intravenously to counteract the muscarinic effects
Dose of 0.03 to 0.07 mg/kg intravenous will typically result in a train-of-four twitch ratio of 90% within 10 to 20 minutes of administration
Dose not more than 0.07 mg/kg or a cumulative total of 5 mg whichever dose is smaller from these is to be injected by slow intravenous for minimum 1 minute
For Prevention:
Administer dose of 0.25 mg intramuscularly once surgery completed
Repeat this every 4 to 6 hours for next 2 to 3 days
For Treatment:
Administer dose of 0.5 to 1 mg intramuscularly and up to every 3 hours as needed Administration
Intravenous train-of-four monitoring for Neuromuscular Blockade reversal:
Peripheral nerve stimulation devices capable of producing a train-of-four stimulus are required to effectively and safely regulate intravenous dose
Use this with atropine drug
Administer dose of 0.01 to 0.04 mg/kg subcutaneously/intramuscularly/ intravenously every 2 to 3 hours as needed
Take a dose of 2 mg/kg daily orally divided every 4 hour and maximum dose up to 375 mg in a day
Dose of 0.03 to 0.07 mg/kg intravenous will typically result in a train-of-four twitch ratio of 90% within 10 to 20 minutes of administration
Dose not more than 0.07 mg/kg or a cumulative total of 5 mg whichever dose is smaller from these is to be injected by slow intravenous for minimum 1 minute Administration
Intravenous train-of-four monitoring for Neuromuscular Blockade reversal:
Peripheral nerve stimulation devices capable of producing a train-of-four stimulus are required to effectively and safely regulate intravenous dose
Refer to adult dosing
Frequency not defined
Drowsiness, headache
Dysarthria
Allergic reactions and anaphylaxis
Dizziness
Loss of consciousness
Convulsions
Miosis and visual changes
Cardiac arrhythmias
Increased oral
Respiratory depression
Rash and urticaria
Pharyngeal and bronchial secretions
Arthralgia
Diaphoresis
Dyspnea
Increased peristalsis and salivation
Urinary frequency
Nausea
Emesis
Flatulence
Muscle cramps and spasms
Flushing and weakness
Black Box Warning
None
Contraindication/Caution:
Contraindication:
neostigmine is contraindicated in individuals who have a known hypersensitivity or allergy to neostigmine or any of its components.
Caution:
Caution is advised when administering the drug to individuals with a history of asthma.
Patients with peptic ulcer disease should be used with caution in these individuals.
neostigmine should be used cautiously in elderly patients and those with impaired liver or kidney function.
Pregnancy consideration:
Pregnancy category: N/A
Lactation: Excretion into human milk is unknown
Pregnancy Categories:
Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.
Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.
Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.
Category N: There is no data available for the drug under this category.
Pharmacology
neostigmine works by inhibiting the activity of acetylcholinesterase (AChE), an enzyme responsible for breaking down acetylcholine.
AChE rapidly breaks it down to terminate the signal and prevent continuous muscle contraction.
Pharmacodynamics
Limited information available
Pharmacokinetics
Absorption
The bioavailability of orally administered neostigmine is low due to significant first-pass metabolism in the liver.
Distribution
neostigmine has a relatively small volume of distribution.
Metabolism
neostigmine undergoes metabolism in the liver.
Elimination and excretion
neostigmine and its metabolites occur mainly via the kidneys through renal excretion.
Administration
neostigmine can be administered through various routes such as intravenously, subcutaneous and intramuscular Injection.
neostigmine also administered orally in the form of tablets.
Patient information leaflet
Generic Name:neostigmine
Why do we use neostigmine?
neostigmine is used for managing myasthenia gravis, an autoimmune neuromuscular disorder.
neostigmine is used to reverse the effects of non-depolarizing neuromuscular-blocking agents that are used during surgery to induce muscle relaxation.
neostigmine can be used to stimulate the bladder muscles and facilitate urination in postoperative urinary retention.
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Administer dose of 0.5 to 2.5 mg subcutaneously/intramuscularly/ intravenously every day
Take a maintenance dose of 15 to 375 mg daily orally divided every 6 to 8 hours
Administer injectable containing 0.6 to 1.2 mg of atropine intravenously to counteract the muscarinic effects
Dose of 0.03 to 0.07 mg/kg intravenous will typically result in a train-of-four twitch ratio of 90% within 10 to 20 minutes of administration
Dose not more than 0.07 mg/kg or a cumulative total of 5 mg whichever dose is smaller from these is to be injected by slow intravenous for minimum 1 minute
For Prevention:
Administer dose of 0.25 mg intramuscularly once surgery completed
Repeat this every 4 to 6 hours for next 2 to 3 days
For Treatment:
Administer dose of 0.5 to 1 mg intramuscularly and up to every 3 hours as needed Administration
Intravenous train-of-four monitoring for Neuromuscular Blockade reversal:
Peripheral nerve stimulation devices capable of producing a train-of-four stimulus are required to effectively and safely regulate intravenous dose
Use this with atropine drug
Administer dose of 0.01 to 0.04 mg/kg subcutaneously/intramuscularly/ intravenously every 2 to 3 hours as needed
Take a dose of 2 mg/kg daily orally divided every 4 hour and maximum dose up to 375 mg in a day
Dose of 0.03 to 0.07 mg/kg intravenous will typically result in a train-of-four twitch ratio of 90% within 10 to 20 minutes of administration
Dose not more than 0.07 mg/kg or a cumulative total of 5 mg whichever dose is smaller from these is to be injected by slow intravenous for minimum 1 minute Administration
Intravenous train-of-four monitoring for Neuromuscular Blockade reversal:
Peripheral nerve stimulation devices capable of producing a train-of-four stimulus are required to effectively and safely regulate intravenous dose