Prostigmin Bromide

Prostigmin Bromide Uses, Dosage, Side Effects, Food Interaction and all others data.

Prostigmin Bromide is a parasympathomimetic, specifically, a reversible cholinesterase inhibitor. By interfering with the breakdown of acetylcholine, Prostigmin Bromide indirectly stimulates both nicotinic and muscarinic receptors. It does cross the blood-brain barrier but only poorly. Prostigmin Bromide binds to the anionic site of cholinesterase. The drug blocks the active site of acetylcholinesterase; so the enzyme can no longer break down the acetylcholine molecules before they reach the postsynaptic membrane receptors. This allows for the threshold to be reached so a new impulse can be triggered in the next neuron. In myasthenia gravis there are too few acetylcholine receptors. So with the acetylcholinesterase blocked, acetylcholine can bind to the few receptors and trigger a muscular contraction.

Prostigmin Bromide is a cholinesterase inhibitor used in the treatment of myasthenia gravis and to reverse the effects of muscle relaxants such as gallamine and tubocurarine. Prostigmin Bromide, unlike physostigmine, does not cross the blood-brain barrier. By inhibiting acetylcholinesterase, more acetylcholine is available in the synapse, therefore, more of it can bind to the fewer receptors present in myasthenia gravis and can better trigger muscular contraction.

Prostigmin Bromide
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Prostigmin Bromide
Availability	Prescription only
Generic	Neostigmine
Neostigmine Other Names	Eustigmin, Eustigmine, Neostigmina
Related Drugs	pyridostigmine, bethanechol, Mestinon, Soliris, Vyvgart, Ultomiris, sugammadex, Urecholine, eculizumab, Bridion
Weight	1mg/ml, 0.5mg/ml,
Type	Injectable Solution, Intravenous Solution, Oral
Formula	C₁₂H₁₉N₂O₂
Weight	Average: 223.2915 Monoisotopic: 223.144652862
Protein binding	Protein binding to human serum albumin ranges from 15 to 25 percent.
Groups	Approved, Vet approved
Therapeutic Class	Anti-cholinesterases, Drugs used in Myasthenia Gravis
Manufacturer
Available Country	United States
Last Updated:	September 19, 2023 at 7:00 am

Uses

Prostigmin Bromide Methyl Sulphate is used for-

Reversal of nondepolarising neuromuscular blockade for surgical anesthetic procedures
The prevention and treatment of post-operative abdominal distention and urinary retention after mechanical obstruction has been excluded.
Treatment of the systemic control of Myasthenia Gravis when oral therapy is impractical.

Prostigmin Bromide is also used to associated treatment for these conditions: Curarization therapy, Myasthenia Gravis, Neuromuscular Blockade, Ogilvie's syndrome, Postoperative Urinary Retention, Post-operative intestinal atony

How Prostigmin Bromide works

Prostigmin Bromide is a parasympathomimetic, specifically, a reversible cholinesterase inhibitor. The drug inhibits acetylcholinesterase which is responsible for the degredation of acetylcholine. So, with acetylcholinesterase inhibited, more acetylcholine is present By interfering with the breakdown of acetylcholine, neostigmine indirectly stimulates both nicotinic and muscarinic receptors which are involved in muscle contraction.. It does not cross the blood-brain barrier.

Dosage

Prostigmin Bromide dosage

Reversal of the effects of Non-depolarizing Neurormuscular Blocking Agents: The usual dose is 0.5 to 2 mg given by slow intravenous injection over 60 seconds; repeated as required. Total dose should not exceed 5 mg (in exceptional cases). When Prostigmin Bromide is administered intravenously, it is recommended that Atropine Sulphate (0.6-1.2 mg) also be given intravenously using separate syringe.

Prevention of post-operative abdominal distention and urinary retention: 0.25 mg intramuscularly or subcutaneously as soon as possible after operation; repeat every 4 6 hours for 2-3 days.

Treatment of post-operative abdominal distention: 0.5 mg intramuscularly or subcutaneously or as required.

Treatment of urinary retention: 0.5 mg intramuscularly or subcutaneously. If urination does not occur within an hour, the patient should be catheterized. After the patient has voided, or the bladder has been emptied, continue the 0.5 mg injection every 3 hours, for at least 5 injections.

Symptomatic control of Myasthenia Gravis: 0.5 mg intramuscularly or subcutaneously. Subsequent dose should be based on the individual patient's response.

Neonates: 50-250 micrograms (0.1 to 0.5 ml) every 4 hours.

Children: 200-500 micrograms (0.4 ml to 1 ml) as recommended.

Side Effects

Nausea, vomiting, increased salivation, diarrhoea and abdominal cramps (more marked with high doses). Signs of overdose are increased gastrointestinal discomfort, bronchial secretions and sweating, involuntary defecation and micturition, miosis, nystagmus, bradycardia, hypotension, agitation, excessive dreaming and weakness eventually leading to fasciculation and paralysis.

Toxicity

Overdosage of Prostigmin Bromide can cause cholinergic crisis, which is characterized by increasing muscle weakness, and through involvement of the muscles of respiration, may result in death. The LD 50 of neostigmine methylsulfate in mice is 0.3 ± 0.02 mg/kg intravenously, 0.54 ± 0.03 mg/kg subcutaneously, and 0.395 ± 0.025 mg/kg intramuscularly; in rats the LD 50 is 0.315 ± 0.019 mg/kg intravenously, 0.445 ± 0.032 mg/kg subcutaneously, and 0.423 ± 0.032 mg/kg intramuscularly.

Precaution

Asthma, bradycardia, recent myocardial infarction, epilepsy, hypotension, parkinsonism, vagotonia, peptic ulceration. Atropine or other antidote to muscarinic effccts may be necessary (particularly when Prostigmin Bromide is given by injection), but it should not be given routinely as it may mask signs of overdose.

Interaction

Anti-arrhythmic Procainamide, Quinidine and possibly Propafenone antagonise effect of Prostigmin Bromide. Antibacterials, Aminoglycosides, Clindamycin, Lincomycin and Polymyxins antagonise effect of Prostigmin Bromide.

Food Interaction

No interactions found.

Prostigmin Bromide Drug Interaction

Moderate: pyridostigmineUnknown: aspirin, epinephrine, RHO Immunoglobulin , calcium / vitamin d, Allergy , glucose, heparin, ipratropium, acetaminophen, procaine penicillin, phenytoin, valproic acid, multivitamin, thiamine, cyanocobalamin, pyridoxine, ascorbic acid, phytonadione, phytonadione

Prostigmin Bromide Disease Interaction

Major: bradycardia, bronchospasm, coronary artery disease, parkinsonism, PUD, seizuresModerate: hyperthyroidism

Elimination Route

Prostigmin Bromide bromide is poorly absorbed from the gastrointestinal tract following oral administration

Half Life

The half-life ranged from 42 to 60 minutes with a mean half-life of 52 minutes.

Pregnancy & Breastfeeding use

Pregnancy Category C. There are no adequate or well-controlled studies of Prostigmin Bromide in either laboratory animals or in pregnantwomen. It is not known whether Prostigmin Bromide can cause fetal harm when administered to a pregnant woman or can affect reproductive capacity. Prostigmin Bromide 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 intravenously to pregnant women near term.

Nursing Mothers: It is not known whether Prostigmin Bromide is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions from Prostigmin Bromide 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.

Contraindication

Prostigmin Bromide is contraindicated in patients with known hypersensitivity to the drug. It is also contraindicated in patients with peritonitis or mechanical obstruction of the intestinal or urinary tract.