rivastigmine

Absorption: Well absorbed following oral administration. Transdermal patch is slowly absorbed over 8 hr.

Distribution: Widely distributed to tissues.

Metabolism/Excretion: Rapidly and extensively metabolized by the liver; metabolites are excreted by the kidneys.

Half-Life: PO: 1.5 hr; Transdermal: 24 hr.

Time/Action Profile ⬆ ⬇

(improvement in dementia)

ROUTE	ONSET	PEAK	DURATION
PO	within 2 wk	up to 12 wk	unknown
Transdermal	unknown	unknown	unknown

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity to rivastigmine or other carbamates;
History of application site reactions with transdermal product suggestive of allergic contact dermatitis.

Use Cautiously in:

History of asthma or obstructive pulmonary disease;
History of GI bleeding;
Sick sinus syndrome or other supraventricular cardiac conduction abnormalities;
Moderate or severe renal impairment (dose ↓ may be needed);
Mild or moderate hepatic impairment (dose ↓ may be needed);
Patients weighing <50 kg (dose ↓ may be needed);
OB: Safety not established in pregnancy;
Lactation: Use during breastfeeding only if potential maternal benefit justifies potential risk to infant;
Pedi: Safety and effectiveness not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

CV: edema, HF, hypotension

Derm: allergic dermatitis

GI: anorexia, diarrhea, nausea, vomiting, ↓weight, abdominal pain, dyspepsia, flatulence

Local: application reactions (transdermal patch)

Neuro: weakness, dizziness, drowsiness, headache, tremor

Misc: fever

Interactions ⬆ ⬇

Drug-drug:

Nicotine may ↓ levels and effectiveness.

Route/Dosage ⬆ ⬇

PO (Adults ): 1.5 mg twice daily initially; after ≥2 wk, may ↑ to 3 mg twice daily. Further increments may be made at 2-wk intervals up to 6 mg twice daily.
Transdermal (Adults ): Initial Dose: 4.6 mg/24-hr transdermal patch initially; ↑ to 9.5 mg/24-hr transdermal patch after ≥4 wk; may ↑ to 13.3 mg/24-hr transdermal patch if needed (is recommended effective dose for patients with severe Alzheimer disease).

Hepatic Impairment

Transdermal (Adults ): Mild to moderate hepatic impairment: Do not exceed dose of 4.6 mg/24 hr.

Availability ⬆ ⬇

(Generic available)

Capsules: 1.5 mg; 3 mg; 4.5 mg; 6 mg
Transdermal patch: 4.6 mg/24 hr; 9.5 mg/24 hr; 13.3 mg/24 hr

Assessment ⬆ ⬇

Assess cognitive function (memory, attention, reasoning, language, ability to perform simple tasks) periodically throughout therapy.
Monitor for nausea, vomiting, anorexia, and weight loss.
Monitor for hypersensitivity skin reactions; may occur after oral or transdermal administration. If allergic contact dermatitis is suspected after transdermal use, may switch to oral rivastigmine after negative allergy testing. If disseminated hypersensitivity reaction of the skin occurs, discontinue rivastigmine.

Implementation ⬆ ⬇

Patients switching from oral doses of <6 mg to transdermal doses should use 4.6 mg/24-hr patch. Patients taking oral doses of 6–12 mg may be converted directly to 9.5 mg/24-hr patch. Apply patch on the day following the last oral dose.
PO: Administer in the morning and evening with food.
Apply patch to clean, dry, hairless area that will not be rubbed by tight clothing. Upper or lower back is recommended; may also use upper arm or chest. Do not apply to red, irritated, or cut skin. Rotate sites to prevent irritation; do not use same site within 14 days. Remove adhesive liner and apply by pressing patch firmly until edges stick well. May be worn during bathing and hot weather. Every 24 hr, remove old patch and discard by folding in half and apply new patch to a new area.

Patient/Family Teaching ⬆ ⬇

PO: Explain the purpose and side effects of rivastigmine. Emphasize the importance of taking at regular intervals as directed. If a dose is missed for several days in a row, advise patient to contact health care provider, as drug may need to be restarted at a lower dose. Advise patient to read Patient Information before starting and with each Rx refill in case of changes.
Instruct patient and caregiver on the correct application, rotation, and discarding of patch. Patch should be folded in half and discarded out of reach of children and pets; medication remains in discarded patch. Replace missed doses immediately and apply next patch at usual time. Advise patient and caregiver to avoid contact with eyes and to wash hands after applying patch. Avoid exposure to heat sources (excessive sunlight, saunas, heating pads) for long periods.
- Advise patient and caregiver to notify health care provider if skin reactions occur.
- Advise patient referred for MRI test to discuss patch with referring health care provider and MRI facility to determine if removal of patch is necessary prior to test and for directions for replacing patch.
Caution patient and caregiver that rivastigmine may cause dizziness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
Advise patient and caregiver to notify health care provider if nausea, vomiting, anorexia, or weight loss occur. If adverse effects become intolerable during treatment with transdermal patch, instruct patient to discontinue patches for several days and then restart at same or next lower dose level. If treatment is interrupted for more than several days, lowest dose level should be used when restarting and titrate according to Route and Dosage section.
Advise patient and caregiver to notify health care provider of medication regimen prior to treatment or surgery.
Inform patient and caregiver that improvement in cognitive functioning may take weeks to months and that the degenerative process is not reversed.
Advise patient to notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care provider before taking other medications.
Rep: Advise women of reproductive potential to notify health care provider if pregnancy is planned or suspected or if breastfeeding.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇