Classes
DEA Class; Rx
Common Brand Names; Prostigmin, Bloxiverz
- Acetylcholinesterase Inhibitors, Central
Description
Oral, SC, IM, and IV cholinesterase inhibitor
Used for symptomatic tx of myasthenia gravis (PO, SC, IM), reversal of non-depolarizing neuromuscular blocking agents (IV), and for prevention/tx of post-op distention and urinary retention (SC, IM)
Similar to, but shorter-acting than, pyridostigmine
Indications
For the symptomatic treatment of myasthenia gravis.
For non-depolarizing neuromuscular blockade reversal.
For the treatment or prevention of post-operative, non-obstructive urinary retention.
For the treatment of post-operative, non-obstructive abdominal distention (adynamic ileus).
For the treatment of acute colonic pseudo-obstruction (Ogilvie’s syndrome)
Contraindications
Hypersensitivity, previous history of reaction to bromides
Peritonitis or mechanical GI or urinary tract obstruction
Adverse Effects
Allergic: Allergic reactions and anaphylaxis
Neurologic: Dizziness, convulsions, loss of consciousness, drowsiness, headache, dysarthria, miosis and visual changes
Cardiovascular: Cardiac arrhythmias (including bradycardia, tachycardia, A-V block and nodal rhythm) and nonspecific EKG changes have been reported, as well as cardiac arrest, syncope and hypotension (predominantly with parenteral dosage form)
Respiratory: Increased oral, pharyngeal and bronchial secretions, and dyspnea; respiratory depression, respiratory arrest and bronchospasm have been reported following the use of the injectable form
Dermatologic: Rash and urticaria
Gastrointestinal: Nausea, emesis, flatulence, and increased peristalsis and salivation
Genitourinary: Urinary frequency
Musculoskeletal: Muscle cramps and spasms, arthralgia
Miscellaneous: Diaphoresis, flushing and weakness
Warnings
To lessen risk of bradycardia, administer glycopyrrolate or atropine sulfate prior to therapy
Caution in epilepsy, bronchial asthma, bradycardia, recent coronary occlusion, vagotonia, hyperthyroidism, cardiac arrhythmias, peptic ulcer
In patients with certain cardiovascular conditions such as coronary artery disease, cardiac arrhythmias or recent acute coronary syndrome, 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 (eg, atropine) is generally successful to mitigate risk of cardiovascular complications
Neonates; because of self-limiting nature of myasthenia gravis, reduce daily dosage gradually released until drug can be withdrawn
Avoid large doses in situations where there might be an increased absorption rate from the intestinal tract; caution when coadministered with anticholinergic drugs because of decreased GI motility
Pregnancy and Lactation
There are no adequate or well-controlled studies in pregnant women; not known whether neostigmine can cause fetal harm or affect reproductive capacity; should administer only if clearly needed
Anticholinesterase drugs, including neostigmine, may cause uterine irritability and induce premature labor when administered to pregnant women near term
The drug has not been studied in lactating women; not known whether neostigmine methylsulfate is present in human milk, or has effects on milk production or breastfed child; the developmental and health benefits of breastfeeding should be considered along with mother’s need for therapy and any potential adverse effects on breastfed child from drug or from underlying maternal condition
Maximum Dosage
375 mg/day PO; 0.5 mg/dose IM or SC; 0.07 mg/kg or 5 mg total dose (whichever is less) IV.
375 mg/day PO; 0.5 mg/dose IM or SC; 0.07 mg/kg or 5 mg total dose (whichever is less) IV.
0.07 mg/kg or 5 mg total dose (whichever is less) IV; safety and efficacy of the PO, SC, and IM formulations have not been established.
0.07 mg/kg or 5 mg total dose (whichever is less) IV; safety and efficacy of the PO, SC, and IM formulations have not been established.
0.07 mg/kg IV; safety and efficacy of the PO, SC, and IM formulations have not been established.
0.07 mg/kg total dose IV; safety and efficacy of the PO, SC, and IM formulations have not been established.