What is the typical dosing for Neostigmine (acetylcholinesterase inhibitor)?

From the Guidelines

Neostigmine is typically dosed at 0.04 mg/kg intravenously for reversal of neuromuscular blockade after surgery, with a maximum dose of 2.5 mg, as recommended by the most recent guidelines 1. The dosing of Neostigmine can vary depending on the specific clinical scenario, such as the degree of neuromuscular blockade and the patient's response to the medication.

• For reversal of neuromuscular blockade, the dose of Neostigmine is typically in the range of 0.04 mg/kg, with a maximum dose of 2.5 mg 1.
• The medication should be administered with an anticholinergic agent, such as atropine or glycopyrrolate, to prevent cholinergic side effects such as bradycardia and increased secretions.
• The dose of Neostigmine should be titrated based on patient response and degree of blockade, with monitoring for potential side effects including nausea, vomiting, abdominal cramps, increased salivation, and bradycardia. Some studies have investigated the effects of different doses of Neostigmine on neuromuscular transmission, with results suggesting that high doses may impair neuromuscular transmission and induce TOF fade 1. However, the most recent and highest-quality study recommends a dose of 0.04 mg/kg for reversal of neuromuscular blockade after surgery 1. Key points to consider when administering Neostigmine include:
• Monitoring for potential side effects, including respiratory depression and cardiac arrhythmias
• Adjusting the dose based on patient response and degree of blockade
• Administering the medication with an anticholinergic agent to prevent cholinergic side effects.

From the FDA Drug Label

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. A 0.03 mg/kg to 0. 07 mg/kg dose of neostigmine methylsulfate injection will generally achieve a TOF twitch ratio of 90% (TOF0.9) within 10 to 20 minutes of administration. The 0. 03 mg/kg dose is recommended for: i. Reversal of NMBAs with shorter half-lives, e.g., rocuronium, or ii. When the first twitch response to the TOF stimulus is substantially greater than 10% of baseline or when a second twitch is present. The 0.07 mg/kg dose is recommended for: iii. NMBAs with longer half-lives, e.g., vecuronium and pancuronium, or iv. When the first twitch response is relatively weak, i.e., not substantially greater than 10% of baseline or v. There is need for more rapid recovery. The recommended maximum total dose is 0.07 mg/kg or up to a total of 5 mg, whichever is less.

The typical dosing for Neostigmine is 0.03 mg/kg to 0.07 mg/kg. The dose selection should be based on the extent of spontaneous recovery, the half-life of the NMBA being reversed, and whether there is a need to rapidly reverse the NMBA. The recommended maximum total dose is 0.07 mg/kg or up to a total of 5 mg, whichever is less 2.

From the Research

Neostigmine Dosing

• The typical dosing for Neostigmine, an acetylcholinesterase inhibitor, can vary depending on the patient and the specific use case.
• In patients with myasthenia gravis, Neostigmine (1-2 mg) intravenously was used as rescue medication 3.
• The efficacy of intranasally administered neostigmine was tested in 22 patients with generalized myasthenia gravis (MG), with topical therapy to the highly vascularized oropharynx proving to be quickly effective in 5-15 min both clinically and electrophysiologically 4.
• The oral bioavailability of Neostigmine is low, with a value even lower than that of pyridostigmine, which is approximately 10% 5.
• Neostigmine might interfere with the bioavailability of pyridostigmine when both drugs are concurrently administered orally 6.

Administration Routes

• Neostigmine can be administered intravenously, as seen in the study where 1-2 mg was used as rescue medication 3.
• Intranasal administration of Neostigmine has also been tested, proving to be quickly effective in 5-15 min both clinically and electrophysiologically 4.
• Oral administration of Neostigmine is also possible, but its bioavailability is low 5.

Dosing Considerations

• The dosing of Neostigmine may need to be adjusted in patients with severely impaired renal function, as this can prolong the elimination of the drug 5.
• The presence of repetitive compound muscle action potentials (R-CMAPs) after diagnostic neostigmine testing may be a good indicator of the risks of side effects and intolerance to acetylcholinesterase inhibitors, including Neostigmine 7.