Rivastigmine

Indications

Rivastigmine is used for: Severe dementia in Alzheimer's disease, Parkinson Dementia

Adult Dose

Alzheimer Dementia Oral Indicated for mild-to-moderate dementia of the Alzheimer's type Initial: 1.5 mg PO q12hr Increase by 1.5 mg/dose q2Weeks; not to exceed 6 mg PO q12hr Maintenance: 3-6 mg PO q12hr (higher end may be more beneficial) Transdermal Indicated for mild, moderate, and severe dementia of the Alzheimer's type Initial: Apply 4.6 mg q24hr Dose titration: May increase dose to 9.5 mg q24hr after a minimum 4 weeks if well tolerated; after an additional 4 weeks, may further increase to 13.3 mg patch if needed Mild-to-moderate Alzheimer disease: Effective dosage range is 9.5-13.3 mg/24 hr Moderate-to-severe Alzheimer disease: Effective dose is 13.3 mg/24 hr Replace with new patch q24hr Parkinson Dementia Oral Initial: 1.5 mg PO q12hr Increase by 1.5 mg/dose q4Weeks; not to exceed 6 mg PO q12hr Maintenance: 1.5-6 mg PO q12hr Transdermal Initial: Apply 4.6 mg q24hr May increase dose to 9.5 mg q24hr after a minimum 4 weeks if well tolerated; after an additional 4 weeks, may further increase to 13.3 mg patch if needed Transdermal Mild-to-moderate hepatic impairment: Not to exceed 4.6 mg q24hr

Child Dose

Renal Dose

Transdermal Renal impairment: No dosage adjustment required

Administration

Should be taken with food.

Contra Indications

Hypersensitivity to other carbamate derivatives. Severe hepatic impairment.

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. Lactation: Unknown if excreted in milk; not recommended

Pregnancy-Lactation

Pregnancy There are no adequate data on developmental risks associated with use of drug in pregnant women Animal data In animals, no adverse effects on embryo-fetal development were observed at oral doses 2-4 times maximum recommended human dose (MRHD) Lactation There are no data on presence of drug in human milk, effects on breastfed infant, or on milk production; the drug and its metabolites are excreted in rat milk following oral administration of rivastigmine; levels of rivastigmine plus metabolites in rat milk are approximately 2 times that in maternal plasma; developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed infant from drug or underlying maternal condition

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.

Adverse Effects

Side effects of Rivastigmine : >10% Nausea (PO 47%; patch 21%), Vomiting (PO 31%; patch 6-19%), Dizziness (PO 21%; patch 2-7%), Diarrhea (PO 19%; patch 6-10%), Headache (PO 17%; patch 3-4%), Anorexia (PO 17%; patch 3-9%), Abdominal pain (PO 13%; patch 2-4%) 1-10% Decreased weight (3-8%), Insomnia (PO 9%; patch 1-4%), Anxiety (PO 5%; patch 3%), Asthenia (PO 6%; patch 2-3%), Vertigo (2%), Fatigue (2%) Potentially Fatal: Serious GI reactions such as anorexia, vomiting and weight loss.

Mechanism of Action

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.