RIVASTIGMINE

It inhibits both AChE and BuChE enzymes equally well. It inhibits the G1 form of enzyme greater than G4 form. Because of this, it has selectivity for AChE in the hippocampus and cortex, which are most affected by Alzheimer’s disease.

Indications

Treatment of patients with mild to moderately severe dementia of the Alzheimer type.

Dosage

1.5mg twice a day. If this dose is well tolerated after a minimum of two weeks of treatment, the dose may be increased to 3mg twice a day. Subsequent increases to 4.5mg and then 6mg twice a day. Maintenance dose : 1.5 to 6mg twice a day. Maximum daily dose : 6mg twice a day. If adverse effects or weight decrease are observed during treatment, these may respond to omitting one or more doses. If adverse effects persist, the daily dose should be reduced to the previous well-tolerated dose.

Contra-Indications

Hypersensitivity to rivastigmine or other carbamate derivatives, severe liver impairment.

Special Precautions

Care must be taken when in patients with sick sinus syndrome or conduction defects, respiratory disease. Cholinergic stimulation may cause increased gastric acid secretion and may exacerbate urinary obstruction and seizures.

Side Effects

Accidental trauma, fatigue, asthenia, dizziness, headache, somnolence, abdominal pain, loss of appetite, dyspepsia, agitation, insomnia, confusion, depression, upper respiratory tract infection, urinary tract infection. Rare : angina pectoris, gastric and duodenal ulcers, gastrointestinal haemorrhage, bradycardia, seizures, rashes, and syncope, nausea, vomiting, diarrhoea.

Drug Interactions

It should not be given concomitantly with other cholinomimetic drugs and might interfere with the activity of anticholinergic medications. It may exaggerate the effects of succinylcholine-type muscle relaxants during anaesthesia