NEOSTIGMINE BROMIDE 
(nee-oh-stig'meen)
Prostigmin
NEOSTIGMINE METHYLSULFATE
Prostigmin
Classifications: autonomic nervous system agent; cholinergic (parasympathomimetic) agent; cholinesterase inhibitor
Pregnancy Category: C
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15 mg tablets; 1:1000, 1:2000, 1:4000 injection
Produces reversible cholinesterase inhibition or inactivation. Has direct stimulant action on voluntary muscle fibers and
possibly on autonomic ganglia and CNS neurons.
Allows intensified and prolonged effect of acetylcholine at cholinergic synapses (basis for use in myasthenia gravis). Also
produces generalized cholinergic response including miosis, increased tonus of intestinal and skeletal muscles, constriction
of bronchi and ureters, slower pulse rate, and stimulation of salivary and sweat glands.
To prevent and treat postoperative abdominal distension and urinary retention; for symptomatic control of and sometimes for
differential diagnosis of myasthenia gravis; and to reverse the effects of nondepolarizing muscle relaxants (e.g., tubocurarine).
Hypersensitivity to neostigmine, cholinergics, or bromides; bradycardia, hypotension; mechanical obstruction of intestinal
or urinary tract; peritonitis; administration with other cholinergic drugs; pregnancy (category C), lactation.
Recent ileorectal anastomoses; epilepsy; bronchial asthma; bradycardia, recent coronary occlusion; vagotonia; hyperthyroidism;
cardiac arrhythmias; peptic ulcer.
Diagnosis of Myasthenia Gravis
Adult: IM 0.022 mg/kg, may increase to 0.031 mg/kg if first test is inconclusive
Child: IM 0.025–0.04 mg/kg
Treatment of Myasthenia Gravis
Adult: PO 15–375 mg/d in 3–6 divided doses IM/IV/SC 0.5–2.5 mg q1–3h
Child: PO 7.5–15 mg t.i.d. or q.i.d. or 0.333 mg/kg or 10 mg/m2 6 times/d IM/IV/SC 0.01–0.04 mg/kg q2–4h
Neonate: PO 1–4 mg q2–3h IM 0.03 mg/kg q2–4h
Reversal of Nondepolarizing Neuromuscular Blockade
Adult: IV 0.5–2.5 mg slowly
Child: IV 0.025–0.08 mg/kg
Infant: IV 0.025–0.1 mg/kg
Postoperative Distention and Urinary Retention
Adult: IM/SC 0.25 mg q4–6h for 2–3 d
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Note: Size of oral dose is considerably larger than that of parenteral dose because drug is poorly absorbed when taken orally (15
mg of oral drug is approximately equivalent to 0.5 mg of parenteral form).
Oral
- Give with food or milk to reduce GI distress.
Intramuscular/Subcutaneous
- Note: 1 mg = 1 mL of the 1:1000 solution; 0.5 mg = 1 mL of the 1:2000 solution; 0.25 mg = 1 mL of the 1:4000 solution.
- Give undiluted.
| Intravenous PREPARE: Direct: Give undiluted.
ADMINISTER: Direct: Give at a rate of 0.5 mg or a fraction thereof over 1 min.
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Body as a Whole: Muscle cramps, fasciculations, twitching, pallor, fatigability, generalized weakness, paralysis, agitation, fear, death. CV: Tightness in chest, bradycardia, hypotension, elevated BP. GI: Nausea, vomiting, eructation, epigastric discomfort, abdominal cramps, diarrhea, involuntary or difficult defecation. CNS: CNS stimulation. Respiratory: Increased salivation and bronchial secretions, sneezing, cough, dyspnea, diaphoresis, respiratory depression. Special Senses: Lacrimation, miosis, blurred vision. Urogenital: Difficult micturition.
Drug: Succinylcholine decamethonium may prolong phase I block or reverse phase II block; neostigmine antagonizes effects of tubocurarine; atracurium, vecuronium, pancuronium; procainamide, quinidine, atropine antagonize effects of neostigmine.
Absorption: Poorly absorbed from GI tract (1–2%). Onset: 10–30 min IM or IV; 2–4 h PO. Peak: 20–30 min IM or IV; 1–2 h PO. Distribution: Not reported to cross placenta or appear in breast milk. Metabolism: Hydrolyzed by cholinesterases; also metabolized in liver. Elimination: 80% of drug and metabolites excreted in urine within 24 h. Half-Life: 50–90 min.
Assessment & Drug Effects
- Check pulse before giving drug to bradycardic patients. If below 60/min or other established parameter, consult physician.
Atropine will be ordered to restore heart rate.
- Monitor pulse, respiration, and BP during period of dosage adjustment in treatment of myasthenia gravis.
- Report promptly and record accurately the onset of myasthenic symptoms and drug adverse effects in relation to last dose in
order to assist physician in determining lowest effective dosage schedule.
- Reduce possible GI (muscarinic) side effects, which occur especially during early therapy, by giving drug with milk or food.
Physician may prescribe atropine or other anticholinergic agent to suppress side effects (note: these drugs may mask toxic symptoms of neostigmine).
- Note time of muscular weakness onset carefully in myasthenic patients. It may indicate whether patient is in cholinergic or
myasthenic crisis: Weakness that appears approximately 1 h after drug administration suggests cholinergic crisis (overdose)
and is treated by prompt withdrawal of neostigmine and immediate administration of atropine. Weakness that occurs 3 h or more
after drug administration is more likely due to myasthenic crisis (underdose or drug resistance) and is treated by more intensive
anticholinesterase therapy.
- Record drug effect and duration of action. S&S of myasthenia gravis relieved by neostigmine include lid ptosis; diplopia;
drooping facies; difficulty in chewing, swallowing, breathing, or coughing; and weakness of neck, limbs, and trunk muscles.
- Manifestations of neostigmine overdosage often appear first in muscles of neck and those involved in chewing and swallowing,
with muscles of shoulder girdle and upper extremities affected next.
- Monitor respiration, maintain airway or assisted ventilation, and give oxygen as indicated, when used as antidote for tubocurarine
or other nondepolarizing neuromuscular blocking agents (usually preceded by atropine). Respiratory assistance is continued
until recovery of respiration and neuromuscular transmission is assured.
- Report to physician if patient does not urinate within 1 h after first dose when used to relieve urinary retention.
Patient & Family Education
- Be aware that regulation of dosage interval is extremely difficult; dosage must be adjusted for each patient to deal with
unpredictable exacerbations and remissions.
- Be aware that drug therapy is often required both day and night. Larger portions of total dose are given at times of greater
fatigue; late afternoon and at mealtimes.
- Keep a diary of "peaks and valleys" of muscle strength.
- Keep an accurate record for physician of your response to drug. Learn how to recognize adverse effects, how to modify dosage
regimen according to your changing needs, or how to administer atropine if necessary.
- Be aware that certain factors may require an increase in size or frequency of dose (e.g., physical or emotional stress, infection,
menstruation, surgery), whereas remission requires a decrease in dosage.
- Some patients become refractory to neostigmine after prolonged use and require change in dosage or medication.
- Do not breast feed while taking this drug.
1%)
Canadian drug name;