Adult Dosing

Myasthenia gravis

• 0.5 mg IM/SC

Postoperative distention

• 0.5 mg IM/SC PRN

Urinary retention

• 0.5 mg IM/SC
• Catheterize patient if urination does not occur within an hour. Continue 0.5 mg IM/SC q3 hrs x 5 after the bladder has been emptied

Nondepolarizing neuromuscular blockade reversal

• 0.5-2 mg IV PRN
• Max: 5 mg IV
• Give slow IV; use with atropine or glycopyrrolate

Pediatric Dosing

• Safety and effectiveness in pediatric patients have not been established

[Outline]

• Adult Dosing
• Pediatric Dosing

• Symptomatic control of myasthenia gravis when oral therapy is impractical
• Prevention and treatment of postoperative distention and urinary retention after mechanical obstruction has been excluded
• Reversal of effects of non-depolarizing neuromuscular blocking agents after surgery

• Hypersensitivity to any of the ingredients of the product
• Hypersensitivity to bromides
• GI obstruction
• GU tract obstruction
• Peritonitis

• N/A

Renal Dose Adjustment (Based on CrCl)

• 10-25 mL/min: Decrease dose to 50%
• <10 mL/min: Decrease dose to 25%

Hepatic Dose Adjustment

• Hepatic impairment: Dose adjustments not defined

• Overdosage of therapy may result in cholinergic crisis which is characterized by increasing muscle weakness and which may lead to death
• Observe patients closely for cholinergic reactions; differentiation from myasthenic crisis is important because increasing the dose of neostigmine may have grave consequences in patients in cholinergic crisis
• Use smaller dosage in patients with renal disease as neostigmine is mainly excreted unchanged by the kidney

Cautions: Use cautiously in

• Renal impairment
• Hx of asthma
• COPD
• Peptic ulcer disease
• GERD
• CV disease
• Bradycardia
• Arrhythmias
• Cardiac conduction defects
• Hx of epilepsy
• Hyperthyroidism

Pregnancy Category:C

Breastfeeding: Probably safe. Limited data indicate that use of neostigmine to treat myasthenia gravis may be acceptable during breastfeeding. This information is based upon LactMed database (available at http://toxnet.nlm.nih.gov/cgi-bin/sis/htmlgen?LACT last accessed 18 March 2011). Due to the potential for serious adverse reactions in nursing infants, manufacturer recommends discontinuation of nursing or discontinuation of drug, taking into account the importance of the drug to the mother.

• CNS: Cholinergic crisis, seizures, dizziness, weakness, syncope, paralysis, headache, paresthesias, fatigue/malaise
• EENT: Lacrimation, miosis, rhinorrhea, blurred vision
• RESP: Bronchospasm, excessive secretions, respiratory depression, respiratory arrest, respiratory paralysis, pulmonary edema
• CV: Bradycardia, severe hypotension, AV block, arrhythmias, hypertension, cardiac arrest
• GI: Abdominal cramps, diarrhea, excessive salivation, nausea, vomiting, flatulence, dyspepsia
• DERM: Rashes, diaphoresis
• GU: Urinary frequency or urgency
• MUSC: Fasciculations, muscle weakness or cramps
• HYPERSENSITIVITY: Anaphylaxis, hypersensitivity reactions

• Cholinergic; inhibits the breakdown of acetylcholine and prolongs its effects
• Metabolized by liver; plasma (cholinesterases)
• Renally excreted (50% unchanged)
• Half-life: 51-90 mins (IM/SC); 47-60 mins (IV)

US Trade Name(s)

• Bloxiverz

US Availability

neostigmine (generic)

• SOLN for INJ: 0.5 mg/mL (10 mL vial)
• SOLN for INJ: 1 mg/mL (10 mL vial)

Bloxiverz

• SOLN for INJ: 0.5 mg/mL (10 mL vial)
• SOLN for INJ: 1 mg/mL (10 mL vial)

Canadian Trade Name(s)

• Only generic available

Canadian Availability

neostigmine (generic)

• SOLN for INJ: 0.5 mg/mL
• SOLN for INJ: 1 mg/mL
• SOLN for INJ: 2.5 mg/mL (10 mL vial)

UK Trade Name(s)

• Only generic available

UK Availability

neostigmine (generic)

• SOLN for INJ: 2.5 mg/mL (1 mL amp)

Australian Trade Name(s)

• Only generic available

Australian Availability

neostigmine (generic)

• SOLN for INJ: 0.5 mg/mL (1 mL amp)
• SOLN for INJ: 2.5 mg/mL (1 mL amp)

[Outline]

Neurologic

Muscle Stimulant

Anticholinesterase