Each mL contains: Neostigmine methylsulfate 500 mcg.
Pharmacology: Pharmacokinetics: After absorption or IV administration, 80% of a single neostigmine dose is excreted by the kidney in the unchanged (50%) and metabolized (30%) forms in 24 hours. The elimination half-life is approximately 51 to 91 minutes. Protein binding in human serum albumin is reported to range from 15 to 25%.
Myasthenia gravis, antagonist to non-depolarising neuromuscular blockade, paralytic ileus, post-op distension, urinary retention, paroxysmal supraventricular tachycardia.
Intestinal atony, postoperative: Prophylaxis: 250 mcg as for intestinal atony.
Treatment: 500 mcg SC, IM (or possibly slow IV) repeated at intervals of 4 to 5 hours.
Urinary retention: Prophylaxis: 250 mcg as for intestinal atony.
Treatment: 500 mcg SC or IM and apply heat to the lower abdomen. If urination does not occur within one hour, the patient should be catheterized. After the patient has voided, continue the 0.5 mg injections at 3 hour intervals for at least 5 additional injections.
Myasthenia gravis: Occasionally parenteral therapy is needed in seriously ill patients and up to 1 mg IM every hour may be necessary in myasthenic crises. Curare antagonist (to neutralize the effect of curare in surgical anesthesia and shock therapy); 0.5 to 2 mg slow IV Atropine sulfate 0.6 to 1.2 mg IV should be given.
Neostigmine should be used with caution in patients with epilepsy, bronchial asthma, bradycardia, recent coronary occlusion, vagotonia, hyperthyroidism, cardiac arrhythmias or peptic ulcer.
Neostigmine should not be administered to patients with peritonitis, mechanical obstruction of the intestinal or urinary tracts or doubtful bowel viability. Patients with a known sensitivity to neostigmine should not be treated with the drug.
When large doses are given, simultaneous administration of atropine sulfate may be advisable. Because of the possibility of hypersensitivity in an occasional patient, atropine should always be at hand, together with antishock medications. Hypotension and bradycardia may occur if the effect of gallamine of curare is antagonized by neostigmine.
The untoward effects of neostigmine are most commonly related to overdosage and generally are of two varieties: muscarinic and nicotinic. Among the former group are nausea, vomiting, diarrhea, abdominal cramps, increased salivation, increased bronchial secretions, miosis and diaphoresis. Muscarinic untoward effects can usually be counteracted by atropine. Nicotinic adverse effects are chiefly muscle cramps, fasciculation and weakness, which can be difficult to distinguish from exacerbation of underlying myasthenia gravis.
Neostigmine should not be used in conjunction with depolarizing muscle relaxants such as suxamethonium. It should not be used during cyclopropane or halothane anesthesia, although it may be used after withdrawal of these agents. Prolonged bradycardia has occurred in patients receiving beta-adrenoceptor blocking agents following administration of neostigmine. The action of neostigmine may be antagonized by agents such as the aminoglycoside antibiotics, that possess non-depolarising blocking actions. Neostigmine's action may also be antagonized by other agents that interfere with neuromuscular transmission including some anti arrhythmic agents such as quinidine.
Protect from light. Store at temperatures not exceeding 25°C.
N07AA01 - neostigmine ; Belongs to the class of anticholinesterase. Used as parasympathomimetics.
Soln for inj (vial) 500 mcg/mL x 10 mL x 10's.