pharmacopeia
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/api/v1/drug/neostigmine

Mechanism of action

Sourced from openFDA

Neostigmine methylsulfate is a competitive cholinesterase inhibitor. By reducing the breakdown of acetylcholine, neostigmine methylsulfate induces an increase in acetylcholine in the synaptic cleft which competes for the same binding site as non-depolarizing neuromuscular blocking agents, and reverses the neuromuscular blockade.

Cholinesterase

Indications

Sourced from openFDA
  • Neostigmine methylsulfate injection is a cholinesterase inhibitor indicated for the reversal of the effects of non-depolarizing neuromuscular blocking agents after surgery. Neostigmine methylsulfate injection, a cholinesterase inhibitor, is indicated for the reversal of the effects of non-depolarizing neuromuscular blocking agents (NMBAs) after surgery (1) .

Contraindications

Sourced from openFDA
  • Neostigmine methylsulfate injection is contraindicated in patients with: • known hypersensitivity to neostigmine methylsulfate (known hypersensitivity reactions have included urticaria, angioedema, erythema multiforme, generalized rash, facial swelling, peripheral edema, pyrexia, flushing, hypotension, bronchospasm, bradycardia and anaphylaxis). • peritonitis or mechanical obstruction of the intestinal or urinary tract.contraindicated

Dosage & administration

Sourced from openFDA

• Should be administered by trained healthcare providers ( 2.1) • Peripheral nerve stimulator and monitoring for twitch responses should be used to determine when neostigmine methylsulfate injection should be initiated and if additional doses are needed ( 2.2 ) • For reversal of NMBAs with shorter half-lives, when first twitch response is substantially greater than 10% of baseline, or when a second twitch is present: 0.03 mg/kg by intravenous route ( 2.2 ) • For reversal of NMBAs with longer half-lives or when first twitch response is close to 10% of baseline: 0.07 mg/kg by intravenous route ( 2.2 ) • Maximum total dosage is 0.07 mg/kg or up to a total of 5 mg (whichever is less) ( 2.2 ) • An anticholinergic agent, e.g., atropine sulfate or glycopyrrolate, should be administered prior to or concomitantly with neostigmine methylsulfate injection ( 2.4 ) 2.1. Important Dosage Information Neostigmine methylsulfate injection should be administered by trained healthcare providers familiar with the use, actions, characteristics, and complications of neuromuscular blocking agents (NMBA) and neuromuscular block reversal agents. Doses of neostigmine methylsulfate injection should be individualized, and a peripheral nerve stimulator should be used to determine the time of initiation of neostigmine methylsulfate injection and should be used to determine the need for additional doses. Neostigmine methylsulfate injection is for intravenous use only and should be injected slowly over a period of at least 1 minute.

Warnings & precautions

Sourced from openFDA

• Bradycardia: Atropine or glycopyrrolate should be administered prior to neostigmine methylsulfate injection to lessen risk of bradycardia. ( 5.1 ) • Serious Reactions with Coexisting Conditions: Use with caution in patients with, coronary artery disease, cardiac arrhythmias, recent acute coronary syndrome or myasthenia gravis. ( 5.2 ) • Neuromuscular Dysfunction: Can occur if large doses of neostigmine methylsulfate injection are administered when neuromuscular blockade is minimal; reduce dose if recovery from neuromuscular blockade is nearly complete. ( 5.4 ) 5.1. Bradycardia Neostigmine has been associated with bradycardia. Atropine sulfate or glycopyrrolate should be administered prior to neostigmine methylsulfate injection to lessen the risk of bradycardia [see Dosage and Administration ( 2.4) ]. 5.2. Serious Adverse Reactions in Patients with Certain Coexisting Conditions Neostigmine methylsulfate injection should be used with caution in patients with coronary artery disease, cardiac arrhythmias, recent acute coronary syndrome or myasthenia gravis. Because of the known pharmacology of neostigmine methylsulfate as an acetylcholinesterase inhibitor, cardiovascular effects such as bradycardia, hypotension or dysrhythmia would be anticipated. In patients with certain cardiovascular conditions such as coronary artery disease, cardiac arrhythmias or recent acute coronary syndrome, the risk of blood pressure and heart rate complications may be increased. Risk of these complications may also be increased in patients with myasthenia gravis.

Adverse reactions

Sourced from openFDA

Most common adverse reactions during treatment: bradycardia, nausea and vomiting ( 6) To report SUSPECTED ADVERSE REACTIONS, contact Dr. Reddy's Laboratories Inc., at 1-888-375-3784 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1. Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Adverse reactions to neostigmine methylsulfate are most often attributable to exaggerated pharmacological effects, in particular, at muscarinic receptor sites. The use of an anticholinergic agent, e.g., atropine sulfate e or glycopyrrolate, may prevent or mitigate these reactions. Quantitative adverse event data are available from trials of neostigmine methylsulfate in which 200 adult patients were exposed to the product. The following table lists the adverse reactions that occurred with an overall frequency of 1% or greater.

Use in specific populations

Sourced from openFDA

• Pregnancy: No human data and limited animal data exist. Use only if clearly needed. 8.1 Pregnancy Risk Summary There are no adequate or well-controlled studies of neostigmine methylsulfate injection in pregnant women. It is not known whether neostigmine methylsulfate injection can cause fetal harm when administered to a pregnant woman or can affect reproductive capacity. The incidence of malformations in human pregnancies has not been established for neostigmine as the data are limited. All pregnancies, regardless of drug exposure, have a background risk of 2 to 4% for major birth defects, and 15 to 20% for pregnancy loss. No adverse effects were noted in rats or rabbits treated with human equivalent doses of neostigmine methylsulfate doses up to 8.1 and 13 mcg/kg/day, respectively, during organogenesis (0.1 to 0.2-times the maximum recommended human dose of 5 mg/60 kg person/day based on body surface area comparisons). Anticholinesterase drugs, including neostigmine may cause uterine irritability and induce premature labor when administered to pregnant women near term. Neostigmine methylsulfate injection should be given to a pregnant woman only if clearly needed.

Pharmacokinetics

Sourced from openFDA
Metabolism
Distribution: Following intravenous injection, the observed neostigmine methylsulfate volume of distribution is reported between 0.12 and 1.4 L/kg. Protein binding of neostigmine methylsulfate to human serum albumin ranges from 15 to 25%.

Overdosage

Sourced from openFDA

Muscarinic symptoms (nausea, vomiting, diarrhea, sweating, increased bronchial and salivary secretions, and bradycardia) may appear with overdosage of neostigmine methylsulfate injection (cholinergic crisis), but may be managed by the use of additional atropine or glycopyrrolate. The possibility of iatrogenic overdose can be lessened by carefully monitoring the muscle twitch response to peripheral nerve stimulation. Should overdosage occur, ventilation should be supported by artificial means until the adequacy of spontaneous respiration is assured, and cardiac function should be monitored. Overdosage of neostigmine methylsulfate injection can cause cholinergic crisis, which is characterized by increasing muscle weakness, and through involvement of the muscles of respiration, may result in death. Myasthenic crisis, due to an increase in the severity of the disease, is also accompanied by extreme muscle weakness and may be difficult to distinguish from cholinergic crisis on a symptomatic basis.

Approval history

Sourced from openFDA
  • May 31, 2013NDANDA204078Exela Pharma
  • Jan 8, 2015NDANDA203629Fresenius Kabi Usa
  • Dec 28, 2015ANDAANDA207042Hikma
  • Apr 26, 2017ANDAANDA208405Ph Health
  • Sep 25, 2017ANDAANDA209933Amphastar Pharms Inc
  • Jun 15, 2018ANDAANDA210051Amneal
  • Jul 10, 2018ANDAANDA209135Dr Reddys
  • Feb 23, 2023NDANDA216903Azurity

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
1,552 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Drug Ineffective1056.8%
  2. 2Drug Interaction1026.6%
  3. 3Hypotension1016.5%
  4. 4Cardiac Arrest936.0%
  5. 5Bradycardia865.5%
  6. 6Serotonin Syndrome825.3%
  7. 7Nausea684.4%
  8. 8Tachycardia684.4%
  9. 9Pyrexia654.2%
  10. 10Respiratory Failure513.3%
  11. 11Abdominal Distension503.2%
  12. 12Off Label Use503.2%
  13. 13Pulmonary Oedema503.2%
  14. 14Dyspnoea493.2%
  15. 15Abdominal Pain463.0%

Literature

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Recent PubMed references pinned to Neostigmine as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 279 ClinicalTrials.gov registrations naming Neostigmine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Neostigmine work?
Neostigmine methylsulfate is a competitive cholinesterase inhibitor. By reducing the breakdown of acetylcholine, neostigmine methylsulfate induces an increase in acetylcholine in the synaptic cleft which competes for the same binding site as non-depolarizing neuromuscular blocking agents, and reverses the neuromuscular blockade.
What is Neostigmine used for?
According to FDA labeling, Neostigmine carries indications including: Neostigmine methylsulfate injection is a cholinesterase inhibitor indicated for the reversal of the effects of non-depolarizing neuromuscular blocking agents after surgery. Neostigmine methylsulfate injection, a cholinesterase inhibitor, is indicated for the reversal of the effects of non-depolarizing neuromuscular blocking agents (NMBAs) after surgery (1) .. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Neostigmine?
Neostigmine is classified as Anticholinesterases, Parasympathomimetics, Cholinesterase Inhibitor, Cholinesterase Inhibitors, Genitourinary Arterial Vasoconstriction, Increased Acetylcholine Activity, Increased GI Smooth Muscle Tone, Increased Striated Muscle Contraction, Pupillary Constriction, Salivation Stimulation.
What are the brand names for Neostigmine?
Neostigmine is marketed under brand names including Bloxiverz, Prevduo.
What are the contraindications for Neostigmine?
Neostigmine labeling lists contraindications including: Neostigmine methylsulfate injection is contraindicated in patients with: • known hypersensitivity to neostigmine methylsulfate (known hypersensitivity reactions have included urticaria, angioedema, erythema multiforme, generalized rash, facial swelling, peripheral edema, pyrexia, flushing, hypotension, bronchospasm, bradycardia and anaphylaxis). • peritonitis or mechanical obstruction of the intestinal or urinary tract.. Always consult the full prescribing information and a clinician.
Note. Data for neostigmine is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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