Neostigmine Methylsulfate - Neostigmine Methylsulfate injection

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. The neostigmine methylsulfate injection dosage is weight-based



Prior to neostigmine methylsulfate injection administration and until complete recovery of normal ventilation, the patient should be well ventilated and a patent airway maintained. Satisfactory recovery should be judged by adequacy of skeletal muscle tone and respiratory measurements in addition to the response to peripheral nerve stimulation. An anticholinergic agent, e.g., atropine sulfate or glycopyrrolate, should be administered prior to or concomitantly with neostigmine methylsulfate injection .



a. Peripheral nerve stimulation devices capable of delivering a train-of-four (TOF) stimulus are essential to effectively using neostigmine methylsulfate injection.



b. There must be a twitch response to the first stimulus in the TOF of at least 10% of its baseline level, i.e., the response prior to NMBA administration, prior to the administration of neostigmine methylsulfate injection.



c. Prior to administration, visually inspect neostigmine methylsulfate injection for particulate matter and discoloration.



d. Neostigmine methylsulfate injection should be injected slowly by intravenous route over a period of at least 1 minute.



e. A 0.03 mg/kg to 0.07 mg/kg dose of neostigmine methylsulfate will generally achieve a TOF twitch ratio of 90% (TOF_0.9) within 10 to 20 minutes of administration. Dose selection should be based on the extent of spontaneous recovery that has occurred at the time of administration, the half-life of the NMBA being reversed, and whether there is a need to rapidly reverse the NMBA.



• The 0.03 mg/kg dose is recommended for:

    • Reversal of NMBAs with shorter half-lives, e.g., rocuronium, or

    • 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

    • NMBAs with longer half-lives, e.g., vecuronium and pancuronium, or

    • When the first twitch response is relatively weak, i.e., not substantially greater than 10% of baseline or

    • There is need for more rapid recovery.



f. TOF monitoring should continue to be used to evaluate the extent of recovery of neuromuscular function and the possible need for an additional dose of neostigmine methylsulfate injection.



g. TOF monitoring alone should not be relied upon to determine the adequacy of reversal of neuromuscular blockade as related to a patient’s ability to adequately ventilate and maintain a patent airway following tracheal extubation.



h. Patients should continue to be monitored for adequacy of reversal from NMBAs for a period of time that would assure full recovery based on the patient’s medical condition and the pharmacokinetics of neostigmine and the NMBA used.

i. The recommended maximum total dose is 0.07 mg/kg or up to a total of 5 mg, whichever is less.

Adult guidelines should be followed when neostigmine methylsulfate injection is administered to pediatric patients. Pediatric patients require neostigmine Methylsulfate doses similar to those for adult patients.







An anticholinergic agent, e.g., atropine sulfate or glycopyrrolate, should be administered prior to or concomitantly with neostigmine methylsulfate injection. The anticholinergic agent should be administered intravenously using a separate syringe. In the presence of bradycardia, it is recommended that the anticholinergic agent be administered prior to neostigmine methylsulfate injection. 

 Neostigmine has been associated with bradycardia. Atropine sulfate or glycopyrrolate should be administered prior to neostigmine methylsulfate to lessen the risk of bradycardia .

 

 Neostigmine methylsulfate 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. Standard antagonism with anticholinergics (e.g., atropine) is generally successful to mitigate the risk of cardiovascular complications.

 

 Because of the possibility of hypersensitivity, atropine and medications to treat anaphylaxis should be readily available.

 

 Large doses of neostigmine methylsulfate administered when neuromuscular blockade is minimal can produce neuromuscular dysfunction. The dose of neostigmine methylsulfate should be reduced if recovery from neuromuscular blockade is nearly complete.

 

 It is important to differentiate between myasthenic crisis and cholinergic crisis caused by overdosage of neostigmine methylsulfate. Both conditions result in extreme muscle weakness but require radically different treatment .