Rivastigmine

Indications
 Oral
Mild to moderately severe dementia in Alzheimer's disease
Adult: Initially, 1.5 mg bid, increased according to response by 1.5 mg bid at intervals of at least 2 wk. If treatment is interrupted for >a few days, restart at 1.5 mg bid and increase dose accordingly, if required. Max: 6 mg bid.
Contraindications
 Hypersensitivity to other carbamate derivatives. Severe hepatic impairment.
Warnings / Precautions
 Patients with sick sinus syndrome or conduction defects, resp diseases. Cholinergic stimulation may increase gastric acid secretion. May exacerbate urinary obstruction and seizures. Pregnancy. Renal impairment, mild to moderate hepatic impairment. Monitor body wt. Asthma or obstructive pulmonary disease. May worsen extrapyramidal symptoms. Lactation.
Adverse Reactions
 Accidental trauma, fatigue, asthenia, dizziness, headache, somnolence, agitation, insomnia, confusion, depression, nausea, vomiting, diarrhoea, abdominal pain, loss of appetite, dyspepsia, upper respiratory tract infection, urinary tract infection. Rarely, angina pectoris, gastric and duodenal ulcers, GI haemorrhage; bradycardia, seizures, rashes and syncope.
Potentially Fatal: Serious GI reactions such as anorexia, vomiting and weight loss.
Overdose Reactions
 May result in cholinergic crisis. General supportive measures should be used.
Drug Interactions
 Not to be used with other cholinomimetic drugs that might interfere with the activity of anticholinergic medications. May exaggerate the effects of succinylcholine-type muscle relaxants during anaesthesia. Tobacco smoking may increase its clearance.
See Below for More rivastigmine Drug Interactions
Food Interactions
 Food delays absorption.
Mechanism of Actions
 Rivastigmine reversibly inhibits hydrolysis of acetylcholine by cholinesterases thus increasing acetylcholine present in the CNS. It is selective for the CNS and is used for the symptomatic treatment of dementia in Alzheimer's disease and idiopathic Parkinson's disease.
Absorption: Readily absorbed from the GI tract (oral); peak plasma concentrations after 1 hr.
Distribution: Crosses the blood-brain barrier. Protein-binding: 40%.
Metabolism: Rapid and extensive; hydrolysis by cholinesterase.
Excretion: Via urine (90%), via faeces (<1%); 1 hr (elimination half-life).
Administration
 Should be taken with food.
Storage Conditions
 Oral: Store below 25°C.
ATC Classification
 N06DA03 - rivastigmine ; Belongs to the class of anticholinesterases. Used in the management of dementia.
Storage
 Oral: Store below 25°C.
Available As
  • Rivastigmine 1.5 mg
  • Rivastigmine 3 mg
  • Rivastigmine 4.5 mg
  • Rivastigmine 6 mg

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