Neostig 0.5 mg/ml (Injection)

Title

• Neostigmine Methylsulfate Injection

Categories

• Medicine
• Pharmaceutical

Description

• Neostigmine Methylsulfate is indicated for the symptomatic control of myasthenia gravis when oral therapy is impractical, the prevention and treatment of postoperative distention and urinary retention after mechanical obstruction has been excluded, and the reversal of effects of nondepolarizing neuromuscular blocking agents after surgery. It is a sterile, nonpyrogenic solution intended for intramuscular, intravenous, or subcutaneous administration, and is a parasympathomimetic, specifically, a reversible cholinesterase inhibitor. The drug inhibits acetylcholinesterase and indirectly stimulates both nicotinic and muscarinic receptors involved in muscle contraction.

Dosage & Administration

• Antagonist to Nondepolarising Neuromuscular Blockade:
  • Adults: A single dose of Neostigmine Methylsulfate injection 2 to 3 mg with atropine sulphate 0.6-1.2 mg by slow IV injection over 1 minute. The recommended ratio of atropine to Neostigmine Methylsulfate injection is 1:2 to 1:3. The maximum recommended dose of Neostigmine Methylsulfate injection in adults is 5 mg.
  • Children: The suggested dose in children is 0.05 mg/kg/dose and atropine sulphate 0.02 mg/kg/dose by slow IV injection. Maximum recommended dose of Neostigmine Methylsulfate injection in children is 2.5 mg.
• Myasthenia Gravis:
  • Adults: 1 mg to 2.5 mg given IM or SC at intervals throughout the day with a total daily dose of 5 to 20 mg. Duration of action of a single dose is 2 to 4 hours. Neonates: 0.05-0.25 mg IM every 2-4 hours, half an hour before feeding. Treatment is not usually required beyond 8 weeks of age. Because the condition is usually self-limiting, the daily dosage should gradually be reduced until the medicine can be withdrawn.
• Urinary Retention:
  • Prophylaxis: 0.25 mg SC or IM before or immediately after the operation, repeated every 4 to 6 hours for 2-3 days. Treatment: 0.5 mg SC or IM and apply warmth to lower abdomen. After the patient has voided, continue 0.5 mg SC or IM every 3 hours for at least 5 injections. If there has been no urinary response within one hour of the first dose, the patient should be catheterized.

Interaction

• Neostig Methylsulfate injection does not antagonize, and may in fact prolong, the Phase I block of depolarizing muscle relaxants such as succinylcholine or decamethonium. Certain antibiotics, especially neomycin, streptomycin, and kanamycin, have a mild but definite nondepolarizing blocking action which may accentuate neuromuscular block. Local and some general anesthetics, antiarrhythmic agents, and other drugs that interfere with neuromuscular transmission should be used cautiously, if at all, in patients with myasthenia gravis; the dose of Neostig Methylsulfate may have to be increased accordingly.

Contraindications

• Neostigmine Methylsulfate injection is contraindicated in patients with known hypersensitivity to the drug and in patients with peritonitis or mechanical obstruction of the intestinal or urinary tract.

Side Effects

• Adverse reactions generally associated with Neostig overdosage are cardiovascular: cardiac arrhythmias (especially bradycardia), hypotension, cardiac arrest, syncope; central nervous system: headache, dizziness, convulsions, loss of consciousness, coma, drowsiness, restlessness, ataxia, slurred speech, agitation, and fear; gastrointestinal: nausea, vomiting, diarrhea, flatulence, abdominal cramps, increased peristalsis, and involuntary defecation; genitourinary: involuntary urination or desire to urinate; musculoskeletal: muscle cramps, fasciculation, general weakness and paralysis.

Pregnancy & Lactation

• Pregnancy: Category C. There are no adequate or well-controlled studies of Neostigmine Methylsulfate in either laboratory animals or in pregnant women. It is not known whether Neostigmine Methylsulfate can cause fetal harm when administered to a pregnant woman or can affect reproductive capacity. Neostigmine Methylsulfate should be given to a pregnant woman only if clearly needed.
• Nonteratogenic Effects: Anticholinesterase drugs may cause uterine irritability and induce premature labor when given IV to pregnant women near term.
• Use in Lactation: It is not known whether Neostigmine Methylsulfate is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions from Neostigmine Methylsulfate in nursing infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Precautions & Warnings

Neostig Methylsulfate should be used with caution in patients with epilepsy, bronchial asthma, bradycardia, recent coronary occlusion, vagotonia, hyperthyroidism, cardiac arrhythmias, or peptic ulcer. When large doses of Neostig Methylsulfate are administered, the prior or simultaneous injection of atropine sulfate may be advisable. Separate syringes should be used for the Neostig Methylsulfate and atropine. Because of the possibility of hypersensitivity in an occasional patient, atropine and antishock medication should always be readily available.

Overdose Effects

Overdosage with Neostig Methylsulfate can cause cholinergic crisis, which is characterized by increasing muscle weakness. Myasthenic crisis is due to an increase in severity of the disease and may be difficult to distinguish from cholinergic crisis on a symptomatic basis. Cholinergic crisis can lead to respiratory paralysis, which may result in death, while myasthenic crisis is extreme muscle weakness. The differentiation between the two crises is extremely important as treatment is different for each.

Therapeutic Class

• Anti-cholinesterases
• Drugs used in Myasthenia Gravis

Storage Conditions

Store at controlled room temperature protected from light. Any portion of the contents remaining should be discarded.

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