It has indirect parasympathomimetic action. It inhibits the enzyme acetylcholinesterase, responsible for the destruction of acetylcholine . Stimulates peristalsis, tone and motility of the intestinal and bladder muscles.
Mechanism of action
- Cholinergic (cholinesterase inhibitor): Inhibits the degradation of acetylcholine by acetylcholinesterase, facilitates the transmission of impulses at the myoneural junction. The cholinergic responses that occur are: myosis, bradycardia , increased tone of the intestinal and skeletal muscles, constriction of the bronchi and ureters, stimulation of the secretion of the salivary and sweat glands. It acts on the cells of the autonomic ganglia and neurons of the CNS . Prevents or alleviates postoperative distension, stimulates gastric motility and gastric tone. Prevents or alleviates urinary retention and increases the tone of the bladder detrusor muscle urinary.
- Antimiasthenic: muscle strength and response to repetitive nerve stimulation increase as a consequence of the potentiation of the maximum effect and the longer duration of acetylcholine in the motor end plate produced by the drug.
International non-proprietary name
Neostigmine bromide.
Composition
Each tablet contains 15 mg of neostigmine bromide.
Pharmacokinetics
It is poorly absorbed from the gastrointestinal tract. Widely distributed to organs innervated by the autonomic nervous system. It is metabolized in the liver . Protein binding: low (to albumin). Elimination: plasma; hepatic. Half-life: 42-60 min. Start of action: 45-75 min. Peristaltic activity begins 2–4 hours after oral ingestion. Time to plasma concentration: 1-2 h. Duration of action: 2-4 h. Elimination (% excreted maximum): renal, it is eliminated in the urine as water-soluble metabolites, around 40%.
Indications
- Myasthenia gravis .
- In anesthesia, reversal of the neuromuscular blockade of non-depolarizing agents, associated with or after the administration of atropine.
- Paralytic ileus.
Contraindications
Hypersensitivity to the drug . Uninary or gastrointestinal tract obstruction and peritonitis .
Precautions
- LM: compatible, monitor infant.
- Children and the elderly: insufficient safety studies.
- RD: moderate, dose adjustment.
- Bronchial asthma .
- Recent gastrointestinal or urinary surgery.
- Bradycardia .
- Arrhythmias
- Recent myocardial infarction.
- Epilepsy .
- Hypotension .
- Parkinsonism.
- Vagotonia.
- Peptic ulcer.
- Hyperthyroidism .
- The atropine or other muscarinic action antidotes may be necessary, but not routine because they usually mask the signs of overdose.
Adverse reactions
Occasional
- Nausea , vomiting , increased salivation, abdominal cramps, and diarrhea . Overdose often causes bronchoconstriction, increased bronchial secretions, lacrimation, excessive sweating, loss of sphincter control, miosis, nystagmus , bradycardia , heart block, arrhythmias, hypotension , agitation, and weakness that can lead to paralysis.
- Transient muscle weakness has occurred in the newborn; it usually causes uterine irritability and induces premature labor.
Interactions
They antagonize its effect procainamide, propafenone, quinidine, propranolol, aminoglycosides, clindamycin, polymyxins and lithium. Chloroquine: its effect decreases by increasing the symptoms of myasthenia gravis.
Posology
- Myasthenia gravis : adults, 15-30 mg orally distributed in individualized intervals and adjusted according to the response, total oral daily dose 75-300 mg.
- Children: newborn 1-5 mg PO every 4 h, 30 min before meals; up to 6 years start with 7.5 mg orally, from 6 to 12 years start with 15 mg orally, total oral daily dose 15-90 mg. The maximum dose that most patients tolerate is 180 mg / day. Paralytic ileus: 15-30 mg PO.
Treatment of acute overdose and serious adverse effects
Atropine sulfate 1-2 mg IV or IM, repeat until control of muscarinic effects. Do not pass 4 mg.
Basic information to the patient
Nothing to point out.
Distribution level
Throughout the pharmacy network
Regulation to prescription
By control card.
VEN classification
Essential drug
Producer laboratory
Pharmaceutical Laboratory Company “Reinaldo Gutiérrez”
ATC code
N07A
Defined daily dose
0.06 g