Neostigmine

Registered South African indications:

• Atony of smooth muscle
• Myasthenia gravis
• Reversal of competitive neuromuscular blocking agents

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Mechanical gastrointestinal obstruction
• Urinary obstruction
• Peritonitis
• Doubtful bowel viability
• Coadministration with depolarising muscle relaxants such as suxamethonium

Cautions

• Pregnancy
• Breastfeeding
• Renal impairment
• Asthma
• Bradycardia
• Cardiac arrhythmia  
• Recent coronary occlusion
• Epilepsy
• Vagotonia
• Hyperthyroidism
• Peptic ulceration
• Parkinsonism
• Intestinal anastomoses
• Sodium controlled diet

Forms avail. in SA and covered in this monograph: inj

Atony of smooth muscles
Paralytic ileus
Post-operative urinary retention

• IM/SC: 0.5-1mg

Atropine should always be available to counteract any excessive reactions

Myasthenia gravis

• IM/SC: 1-2.5mg, given at intervals to provide maximum relief; Titrate according to patient response: Usual dose: 5-20mg/24hrs

Given at intervals to provide maximum relief: give at times when maximum strength is needed

The usual duration of action of a dose is 2-4hrs

Atropine should always be available to counteract any excessive reactions

Reversal of competitive neuromuscular blocking agents (with atropine)

• IV: 0.05-0.07mg/kg given over 1min; Max dose: 5mg

Atropine and Neostigmine may be given simultaneously, but in patients with bradycardia, the pulse rate should be increased to 80 per minute with atropine before giving neostigmine

Paed. forms avail. in SA and covered in this monograph: inj

Myasthenia gravis

• IM/SC: 0.01-0.04mg/kg, given at intervals to provide maximum relief (2-6hrly)

Given at intervals to provide maximum relief

Atropine should always be available to counteract any excessive reactions

Reversal of competitive neuromuscular blocking agents (additional agent required)

• IV: 40μg/kg given over 1min; Max dose: 2.5mg

Atropine and Neostigmine may be given simultaneously

Pregnancy

• Caution
• The use of neostigmine during pregnancy has not been established. Although the possible hazards to mother and child must be weighed against the potential benefits in every case. Experience with myasthenia gravis has revealed no untoward effect of the drug on the course of pregnancy. As the severity of myasthenia gravis often fluctuates considerably, particular care is required to avoid cholinergic crisis due to overdosage of neostigmine

Breastfeeding 

• Caution
• The use of neostigmine during breastfeeding has not been established. Only negligible amounts of neostigmine are excreted in breast milk. Nevertheless, attention should be paid to possible effects on the breastfeeding infant

Renal Impairment 

• Caution; dose adjustment recommended

Hepatic Impairment 

• No dose adjustment recommended

Elderly

• Caution; No dose adjustment recommended

Porphyria Information

• Probably not porphyrinogenic (PNP)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Cholinergic syndrome

Cardiovascular Disorders

• Bradycardia
• Decreased cardiac conduction
• Heart block
• Cardiac arrest
• Hypotension

Respiratory Disorders

• Increased bronchial secretion
• Bronchospasm

Gastrointestinal Disorders 

• Nausea and vomiting
• Diarrhoea
• Abdominal cramps
• Salivary hypersecretion
• Increased intestinal motility  
• Involuntary defecation

Genitourinary Disorders

• Urinary incontinence

Musculoskeletal Disorders

• Muscle spasms

Skin and Subcutaneous Tissue Disorders

• Hyperhidrosis

Sensory Disorders

• Miosis
• Increased lacrimation

Immune, Blood and Lymphatic System Disorders

• Hypersensitivity
• Angioedema
• Anaphylactic reaction

• Neuromuscular blocking agents
• Atropine
• Aminoglycosides
• Agents that interfere with neuromuscular transmission  
• Suxamethonium
• Cycloproprane or halothane anaesthesia

None routine 

Neostigmine is a reversible cholinesterase inhibitor. It prolongs and intensifies the muscarinic and nicotinic effects of acetylcholine. It is used mainly for its action on skeletal muscle and less frequently to increase the activity of smooth muscle.

Injection (per ml) 0.5mg

• Neostigmine methyl-fresenius (Fresenius)

Injection (per ml) 2.5mg

• Micro-Neostigmine (Micro) 
• Neostigmine methyl-fresenius (Fresenius)