Neostigmine

Neostigmine (Methylsulphate) is a potent reversible inhibitor of acetylcholinesterase and its use is inthe treatment of mysthania gravis. Neostigmine bromide and neostigmine methylsulphate are quaternary ammonium compound. The pharmacologic properties of neostigmine mimic those of acetylcholine. Neostigmine (Methylsulphate) is more polar and does not enter in the CNS. its effects on skeletal muscle is greater than that of physostigmine.Neostigmine bromide and neostigmine methylsulphate are available for oral, opthalmic and parentral administration.


Adult Dose
Dose: 0.02 mg/ kg
Single Dose: 0.02 (0.02)
Frequency: As recommended.
Route: IM
Instructions: For diagnosis of myasthenia gravis
Neonatal
Dose: 50 ug/kg
Single Dose: 50 (50)
Frequency: As recommended.
Route: Intravenous
Instructions: As required
Paedriatic
Dose: 50 to 0 ug/kg
Single Dose: 25 (25)
Frequency: As recommended.
Route: Intra Venous
Instructions: To severe neuromuscular blockade.
Characteristics
Neostigmine also known as Neost gmine. Neostigmine (Methylsulphate), Neostigmine (Methylsulphate) are the derivatives of Neostigmine. It is of Synthetic origin and belongs to Quaternary Ammonium. It belongs to Cholinestrase inhibitor pharmacological group on the basis of mechanism of action and also classified in Antidotes and Cholinergic Agonist pharmacological group.The Molecular Weight of Neostigmine is 223.30. It is weakly acidic drug, 4.98% solution of the drug is isotonic and Its pKa is 12.0.
Contraindications
Neostigmine is contraindicated in conditions like Intestinal obstruction,Urinary obstruction.
Effects
The severe or irreversible adverse effects of Neostigmine, which give rise to further complications include Hallucinations, Hallucinations, Anxiety, Epilepsy, Disorientation, Loss of consciousness.Neostigmine produces potentially life-threatening effects which include Cholinergic crises, Depolarizing block. which are responsible for the discontinuation of Neostigmine therapy.The signs and symptoms that are produced after the acute overdosage of Neostigmine include Bradycardia, Hypotension, Nausea, Vomiting, Diarrhea, Sweating, Miosis, Abdominal cramps, Increased peristalsis, Fasciculation of skeletal muscles, General weakness, Increased bronchial secretion, Mucular cramps, Slivation.The symptomatic adverse reactions produced by Neostigmine are more or less tolerable and if they become severe, they can be treated symptomatically, these include Nausea, Vomiting, Diarrhea, Abdominal pain, Sweating, Salivation.
Indications
Neostigmine is primarily indicated in conditions like Adynamic ileus, Myasthenia gravis, Myasthenia gravis diagnosis, Neuromuscular blockade reversal, Reversal of non-depolarizing neuromuscular blockade, and can also be given in adjunctive therapy as an alternative drug of choice in Paralytic ileus, Urinary retention, Urinary retention.
Interactions
Neostigmine is known to interact with other drugs, the details of drug interactions is as follows:DrugDetailsSeverityOnsetManagementBethanechol (Cl)ChloroquineColistin (Sulphate & Sulphomethate Na)HydrocortisoneHydroxychloroquine (Sulphate)LithiumMethylcelluloseOxytetracycline (Dihydrate)Pantothenic AcidPantothenic Acid may increase the effects of Neostigmine.PenicillaminePolymyxin B (Sulphate)Procainamide (HCl)Trimeprazine (Tartrate)Verapamil (HCl) These interactions are sometimes beneficial and sometimes may pose threats to life. Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Interfrence
None well documented
Risks
Drug should not be given to Paediatrics, and Pregnant Mothers.If prescribing authority justifies the benefits of the drug against the possible damages he/she should reevaluate them and consult the reference material and previous studies.
Storage
Inj Store Below 40°C. Do not Freeze. Protect from Sunlight. Tab Store in a well closed container, Below 40°C.
Warnings
Neostigmine should be used with caution in patients with asthma, seizure disorder, epilepsy, heart disease such as hypertension, bradycardia, recent myocardial infraction, thyroid disorders, intestinal disorders, ulcers, urinary problems or if have any allergy especially to bromides. Large dose by mouth should be avoided in condition where there may be increased absorption from the gastrointestinal tract. It is classified as pregnancy category C and should be used only if clearly needed during pregnancy.
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