Neostigmine Neostigmine

Neostigmine Neostigmine

Martindel Classification: Parasympathomimetics
Therapeutic Classification: Autonomic Drugs> Parasympathetic Immunoassays

Indications for neostigmine

Neostigmine is used to treat muscle weakness due to myasthenia gravis, non-obstructive urinary retention after surgery, and as an antidote to tobocurarin and other non-depolarizing neuromuscular blocking drugs.

Mechanism of action of neostigmine
*
Facilitate the transmission of nerve impulses at the junction of muscle nerves (by competitively inhibiting the enzyme acetylcholinesterase and preventing the breakdown of acetylcholine)
Elimination of neuromuscular block (by competing with non-polarizing neuromuscular blocking agents at the synapse site)
Direct quasi-cholinergic effects on skeletal muscle, central nervous system neurons and autonomic ganglion cells

Pharmacokinetics of neostigmine
*
Absorption: 2-1% (15 mg oral neostigmine equivalent to 0.5 mg injection)
Bioavailability: 15 mg oral neostigmine equivalent to 0.5 mg injection
Start of effect:
Oral 4-2 hours
Inject 30-10 minutes
Effect length:
Muscular 4-2.5 hours
Intravenous 2-1 hours
Plasma peak:
Oral 2-1 hours
Muscular 30 minutes
Protein binding: 25-15% to albumin
Metabolism: Liver enzymes and cholinesterase enzymes
half life:
Adult food 60-42 minutes
Adult muscle 90-51 minutes
Intravenous infants (10-2 months) 5 ± 39 minutes
Intravenous children (6-1 years) 16 ± 48 minutes
Adult venous (48-29 years) 8.67 minutes
Intravenous patients without kidneys 181 54 54 minutes
Intravenous kidney transplantation 64 ± 104.7 minutes
Excretion: Urine (50% as unchanged drug, the rest as metabolite)
Side effects of neostigmine
*
Other complications (unspecified percentage):
Cardiovascular: ventricular atrial block, cardiac arrhythmia (especially bradycardia), electrocardiogram changes (nonspecific), flushing, hypotension, nodular arrhythmia, syncope, tachycardia, thrombophlebitis
Central nervous system: dizziness, drowsiness, dysarthria (paralytic speech), headache, loss of consciousness, seizures, voice disorder
Skin: Increased sweating, skin rash, urticaria
Gastrointestinal: diarrhea, dysphagia, bloating, increased peristaltic bowel movements, nausea, salivation, stomach cramps, vomiting
Genitourinary: Urine urgency
Hypersensitivity: Anaphylaxis, hypersensitivity reaction
Nervous, musculoskeletal: joint pain, fasciculation (muscle jump), laryngeal spasm, muscle cramp, muscle spasm, weakness
Eye: tears, pupil stenosis
Respiratory: bronchospasm, shortness of breath, exacerbation of asthma, increased bronchial secretions, respiratory depression, respiratory paralysis
Neostigmine drug interactions
* General specifications of interactions:
Exacerbation of bradycardia
Intensification of cholinergic effects
– Seizure threshold reduction

Category X Interactions (Avoidance):
No significant interference has been identified.

Reducing the effects of drugs with neostigmine:
Anticholinergic agents, neuromuscular blocking drugs (non-depolarizing)

Reducing the effects of neostigmine by drugs:
Anticholinergic agents, dipyridamole

Increased effects of drugs by neostigmine:
Amifampridine, Benoxinate, Beta-blockers, Cholinergic agonists, Succinylcholine

Increased effects of neostigmine by drugs:
Amifampridine, corticosteroids (systemic)

Food interference:
has not been stated.