neostigmine

Therapeutic Classification: antimyasthenics

Pharmacologic Classification: cholinergics

Indications ⬆ ⬇

REMS

Reversal of nondepolarizing neuromuscular blockers after surgery.

Action ⬆ ⬇

Inhibits the breakdown of acetylcholine so that it accumulates and has a prolonged effect.
Effects include miosis, increased intestinal and skeletal muscle tone, bronchial and ureteral constriction, bradycardia, increased salivation, lacrimation, and sweating.

Therapeutic effects:

Reversal of nondepolarizing neuromuscular blockers.

Pharmacokinetics ⬆ ⬇

Absorption: IV administration results in complete bioavailability.

Distribution: Probably does not cross the placenta or enter breast milk.

Metabolism/Excretion: Metabolized by plasma cholinesterases and the liver.

Half-Life: 24–113 min.

Time/Action Profile ⬆ ⬇

(cholinergic effects, ↑ muscle tone)

ROUTE	ONSET	PEAK	DURATION
IV	10–30 min	20–30 min	2–4 hr

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Mechanical obstruction of the GI or GU tract.

Use Cautiously in:

History of asthma;
Ulcer disease;
Cardiovascular disease;
Seizure disorder;
Hyperthyroidism;
OB: May cause uterine irritability and induce preterm labor when administered near term; use during pregnancy only if potential maternal benefit justifies potential fetal risk;
Lactation: Safety not established in breastfeeding;
Geri: Prolonged duration of effect in older adults due to ↓ in renal function.

Adv. Reactions/Side Effects ⬆ ⬇

CV: bradycardia, hypotension

Derm: sweating, rash

EENT: lacrimation, miosis

GI: abdominal cramps, diarrhea, excess salivation, nausea, vomiting

Neuro: dizziness, SEIZURES, weakness

Resp: bronchospasm, excess secretions

Interactions ⬆ ⬇

Drug-drug:

Action may be antagonized by drugs possessing anticholinergic properties, including antihistamines, antidepressants, atropine, haloperidol, phenothiazines, quinidine, and disopyramide.
Prolongs action of depolarizing muscle-relaxing agents (succinylcholine).

Route/Dosage ⬆ ⬇

IV (Adults and Children ): 0.03 mg/kg for neuromuscular blockers with short half-life (e.g. rocuronium); 0.07 mg/kg for neuromuscular blockers with longer half-life (e.g. vecuronium); dose may be repeated to a total dose of 0.07 mg/kg or 5 mg, whichever is less; pretreat with atropine IV (0.6–1.2 mg for adults; 20 mcg/kg for children).

Availability ⬆ ⬇

(Generic available)

Solution for injection: 0.5 mg/mL (vials); 1 mg/mL (vials and prefilled syringes)
In combination with: glycopyrrolate (Prevduo). See Appendix [not included in this PDA edition].

Assessment ⬆ ⬇

Assess pulse, respiratory rate, and BP prior to administration. Report significant changes in heart rate.
Reversal of Nondepolarizing Neuromuscular Blocking Agents: Monitor reversal of effects of neuromuscular blocking agents with a peripheral nerve stimulator. Recovery usually occurs consecutively in the following muscles: diaphragm, intercostal muscles, muscles of the glottis, abdominal muscles, limb muscles, muscles of mastication, and levator muscles of the eyelids. Closely observe the patient for residual muscle weakness and respiratory distress throughout the recovery period. Maintain airway patency and ventilation until recovery of normal respiration occurs.

Toxicity and Overdose:

If overdose occurs, atropine is the antidote.

Implementation ⬆ ⬇

Atropine or glycopyrrolate should be used prior to or concurrently with neostigmine to prevent or treat bradycardia.

IV Administration:

IV Push: Administer doses undiluted. May be given through Y-site of an IV of D5W, 0.9% NaCl, Ringer’s solution, or LR. Concentration: 0.5–1 mg/mL.
Rate: Administer each 0.5 mg over at least 1 min.
Y-Site Compatibility:
- heparin
- hydrocortisone sodium succinate
- palonosetron
- potassium chloride
- vitamin B complex with C

Patient/Family Teaching ⬆ ⬇

Explain purpose of neostigmine to patient.
Rep: Advise female patient to notify health care professional if pregnancy is planned or suspected or if breastfeeding. May cause uterine irritability and induce premature labor when administered to pregnant women near term.

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Pronunciation ⬇

Classifications ⬆ ⬇