Dosing & Uses
Dosage Forms & Strengths
capsule
- 1.5mg
- 3mg
- 4.5mg
- 6mg
transdermal patch
- 4.6mg/24hr
- 9.5mg/24hr
- 13.3mg/24hr
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
Dosage Modifications
Interruption of treatment (Oral)
- If adverse effects (e.g., nausea, vomiting, abdominal pain, loss of appetite) cause intolerance during treatment, patient should be instructed to discontinue treatment for several doses ; if dosing is interrupted for ≤3, restart treatment with same or lower dose; if dosing is interrupted for >3 days, restart treatment with 1.5 mg twice a day and titrate as described above
Interruption of treatment (Patch)
- If dosing is interrupted for ≤3 days, restart treatment with same or lower strength patch; if dosing is interrupted for >3 days, restart treatment with 4.6 mg/24 hours patch and titrate as described above
Renal impairment
- Oral: Patients with moderate and severe renal impairment may be able to only tolerate lower doses
- Transdermal: Not studied; dosage adjustment may not be required
Hepatic impairment
- Mild-to-moderate hepatic impairment (Child-Pugh class A and B): 1.5 mg qDay with slow titration recommended for oral administration; transdernal patch, not to exceed 4.6 mg q24hr
- Severe hepatic impairment: Not studied
Low body weight (<50 kg)
- Carefully titrate and monitor patients for toxicities (eg, excessive nausea, vomiting), and consider reducing maintenance dose if toxicities develop while taking orally; reduce to 4.6 mg q24hr if toxicities develop with transdermal patch
Administration
Take with food
Oral solution may be swallowed directly from provided syringe or mixed with small glass of fluid
Switching from oral to transdermal
- If PO dose <6 mg/day, switch to 4.6 mg/24 hr patch
- If PO dose is 6-12 mg/day, switch to 9.5 mg/24 hr patch
- Apply patch on day following last oral dose
Not applicable
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Adverse Effects
>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%)
Postmarketing Reports
Cardiac Disorders: Tachycardia
Hepatobiliary Disorders: Abnormal liver function tests, hepatitis
Nervous System Disorders: Seizure
Psychiatric Disorders: Aggression, nightmares
Skin and Subcutaneous Tissue Disorders: Allergic dermatitis, application site hypersensitivity (patch), blister, disseminated allergic dermatitis, Stevens-Johnson syndrome, urticarial
Warnings
Contraindications
Hypersensitivity to rivastigmine or carbamates
History of application site reaction with transdermal patch
Active GI bleeding
Cautions
Anorexia
Sick sinus syndrome
History of peptic ulcer
History of asthma/COPD
May induce/exacerbate extrapyramidal symptoms
Concomitant NSAID
Gastrointestinal adverse reactions may include significant nausea, vomiting, diarrhea, anorexia/decreased appetite, and weight loss, and may necessitate treatment interruption; dehydration may result from prolonged vomiting or diarrhea and can be associated with serious outcomes
Medication errors with transdermal patches have resulted in serious adverse events; some cases have required hospitalization, and in rare instances, medication errors have led to death; most of the errors have involved not removing the old patch when putting on a new one and the use of multiple patches at the same time
Skin application site reactions may occur with transdermal application and are usually mild or moderate in intensity; these reactions are not in themselves an indication of sensitization; however, use of rivastigmine patch may lead to allergic contact dermatitis
Isolated postmarketing reports of disseminated hypersensitivity reactions of the skin irrespective of the administration route (oral or transdermal); treatment should be discontinued if disseminated hypersensitivity reaction of the skin occurs
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
Pregnancy Categories
A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA:Information not available.
Pharmacology
Mechanism of Action
Reversible acetylcholinesterase inhibitor that causes an increase in concentrations of acetylcholine, which in turn enhances cholinergic neurotransmission
Absorption
Bioavailability: 36% (PO)
Duration: 10 hr (PO); 24 hr (patch)
Peak plasma time: 1 hr (PO); 8 hr (patch)
Distribution
Protein bound: 40%
Vd: 1.8-2.7 L/kg
Metabolism
Metabolized by cholinesterase
Elimination
Half-life: 1.5 hr (PO), 3 hr (patch)
Total body clearance: 1.2-2.4 L/min
Excretion: Urine (97%)
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Patient Handout
Formulary
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