Neostigmine Methylsulfate (neostigmine methylsulfate)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Neostigmine methylsulfate is an anticholinesterase agent.
Neostigmine is an anticholinesterase agent; the drug inhibits the enzyme acetylcholinesterase, reducing the degradation of acetylcholine. By competing with acetylcholine for binding to acetylcholinesterase, neostigmine slows the rate of hydrolysis of acetylcholine. As a consequence, acetylcholine accumulates in the synaptic cleft, and competes with and reverses the effects of nondepolarizing neuromuscular blocking agents.
Neostigmine stimulates both muscarinic and nicotinic receptors, producing generalized cholinergic effects including miosis, increased tonus of intestinal and skeletal musculature, constriction of bronchi and ureters, bradycardia, and stimulation of secretion by salivary and sweat glands. In addition, neostigmine has a direct cholinomimetic effect on skeletal muscle.
Neostigmine does not cross the blood-brain barrier to produce CNS effects. Extremely high doses, however, produce CNS stimulation followed by CNS depression, in addition to a depolarizing neuromuscular blockade, and may result in respiratory depression, paralysis, and death.
Neostigmine is 15-25% bound to serum albumin. Following administration of a single IV dose of neostigmine, the reported elimination half-life of the drug ranged from 24-113 minutes. In a pharmacokinetic study in pediatric patients, the half-life of neostigmine (administered as an IV infusion over 2 minutes) was approximately 39, 48, or 67 minutes in infants 2-10 months of age, children 1-6 years of age, or adults 29-48 years of age, respectively.
Neostigmine is metabolized by microsomal enzymes in the liver. Approximately 80% of the drug is excreted in urine within 24 hours (50% as unchanged drug).
Generic name: neostigmine methylsulfate
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Neostigmine Methylsulfate
Indications
The following indications are listed for Neostigmine Methylsulfate:
- Reversal Of Neuromuscular Blockade
Also known as: Reversal Of Muscle Blockade.
Dosing
No dosing information is available for this tab.
Neostigmine methylsulfate is administered by slow IV injection (over a period of at least 1 minute). The drug also has been administered by IM or subcutaneous injection+, but the manufacturer of the currently available injectable preparation labeled for reversal of neuromuscular blocking agents states that the injection is for IV use only.
Neostigmine methylsulfate injection should be stored at controlled room temperature (20-25degreesC) but may be exposed to temperatures ranging from 15-30degreesC; the injection should be stored in the original carton until time of use and protected from light.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
Drug interaction studies have not been conducted to date with neostigmine methylsulfate. Clinically important drug interactions are not likely to occur if neuromuscular monitoring is employed and both relaxants and reversal agents are titrated to effect.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Known hypersensitivity to neostigmine.
*Mechanical obstruction of the intestinal or urinary tract.
*Peritonitis.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
The most common adverse effects of neostigmine include bradycardia, nausea, and vomiting. Adverse effects of neostigmine methylsulfate generally are due to exaggerated pharmacologic effects of the drug, particularly at muscarinic-cholinergic receptors.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
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Neostigmine may be used in pediatric patients of all ages to reverse the effects of nondepolarizing neuromuscular blocking agents after surgery. The available data indicate that efficacy and pharmacokinetics of neostigmine are similar across all pediatric age groups and also similar to those in adults when the same dosing guidelines are applied.
Based on limited data, neostigmine dosing requirements for reversal of neuromuscular blockade may be lower in infants and neonates than in older pediatric patients and adults; however, pediatric patients have a greater risk of incomplete reversal of neuromuscular blockade because of their decreased respiratory reserve. Therefore, the risks of administering higher doses of neostigmine (up to maximum recommended dosage) should not outweigh the risks associated with incomplete reversal in this age group.
Because pediatric patients, particularly neonates and infants, may be more sensitive to changes in heart rate, the effects of anticholinergic agents should be observed prior to administration of neostigmine to lessen the probability of bradycardia and hypotension.
It is not known whether neostigmine can cause fetal harm when administered to pregnant women or affect reproductive capacity; the drug should be used during pregnancy only when clearly indicated as no adequate or well-controlled studies of the drug have been conducted in pregnant women. Administration of anticholinesterase drugs such as neostigmine to pregnant women near term may cause uterine irritability and induce premature labor.
There are limited data from animal reproduction studies; in such studies, no teratogenic or other adverse effects were identified; however, drug exposure was well below the predicted exposures in humans.
It is not known whether neostigmine is distributed into human milk. Caution should be exercised when the drug is used in nursing women.
Although dosage adjustments are not required in geriatric patients undergoing reversal of neuromuscular blockade, a longer period of monitoring is recommended in such patients to ensure that additional doses of neostigmine are not necessary to adequately reverse neuromuscular blockade.
Because geriatric patients may have decreased renal function, neostigmine should be used with caution and increased monitoring in this age group. The duration of action of neostigmine is prolonged in geriatric patients; however, such patients also experience slower spontaneous recovery from neuromuscular blocking agents. Geriatric patients should be monitored for longer periods of time to ensure that additional doses of neostigmine are not necessary to adequately reverse neuromuscular blockade.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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