Rivastigmine

Rivastigmine is a reversible cholinesterase inhibitor used to treat mild to moderate dementia caused by Alzheimer's or Parkinson's disease.

Rivastigmine is available under the following different brand names: Exelon, and Exelon Patch.

Adult Dosage Forms and Strengths

Capsule

• 1.5 mg
• 3 mg
• 4.5 mg
• 6 mg

Transdermal patch

• 4.6 mg/24 hours
• 9.5 mg/24 hours
• 13.3 mg/24 hours

Dosage Considerations – Should be Given as Follows:

Alzheimer's Dementia

Oral

• Indicated for mild-to-moderate dementia of the Alzheimer's type
• Initial: 1.5 mg orally every 12 hours
• Increase by 1.5 mg/dose every 2 weeks; not to exceed 6 mg orally every 12 hours
• Maintenance: 3-6 mg orally every 12 hours (higher end may be more beneficial)

Transdermal

• Indicated for mild, moderate, and severe dementia of the Alzheimer's type
• Initial: Apply 4.6 mg every 24 hours
• Dose titration: May increase dose to 9.5 mg every 24 hours 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 hours
• Moderate-to-severe Alzheimer disease: Effective dose is 13.3 mg/24 hours
• Replace with new patch every 24 hours

Parkinson Dementia

Oral

• Initial: 1.5 mg orally every 12 hours
• Increase by 1.5 mg/dose every 4 weeks; not to exceed 6 mg orally every 12 hours
• Maintenance: 1.5-6 mg orally every 12 hours

Transdermal

• Initial: Apply 4.6 mg every 24 hours
• May increase dose to 9.5 mg every 24 hours 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

Transdermal

• Renal impairment: No dosage adjustment required
• Mild-to-moderate hepatic impairment: Not to exceed 4.6 mg every 24 hours
• Low body weight (less than 50 kg): Carefully titrate and monitor patients with low body weight for toxicities (e.g., excessive nausea, vomiting), and consider reducing maintenance dose to 4.6 mg every 24 hours if toxicity develops

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 oral dose less than 6 mg/day, switch to 4.6 mg/24 hour patch
• If oral dose is 6-12 mg/day, switch to 9.5 mg/24 hour patch

Common side effects of Rivastigmine include:

• Nausea
• Vomiting
• Dizziness
• Diarrhea
• Headache
• Loss of appetite
• Abdominal pain
• Weight loss
• Insomnia
• Anxiety
• Weakness/lack of energy
• Spinning sensation (vertigo)
• Fatigue
• Upset stomach
• Swelling in your hands or feet
• Joint pain
• Cough
• Runny or stuffy nose
• Increased sweating
• Drowsiness
• Sleep problems (insomnia)
• Shakiness (tremors)

Serious side effects of rivastigmine include:

• Slow or irregular heartbeat
• Fainting
• Black stools
• Vomit that looks like coffee grounds
• Severe stomach or abdominal pain
• Seizures
• Trouble urinating

Postmarketing side effects of rivastigmine reported include:

• Fast heart rate
• Abnormal liver function tests, hepatitis
• Seizures
• Aggression, nightmares
• Allergic dermatitis, application site hypersensitivity (patch), blister, disseminated allergic dermatitis, Stevens-Johnson syndrome, hives

This is not a complete list of side effects and other serious side effects may occur. Call your doctor for information and medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

If your doctor has directed you to use this medication, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider or pharmacist first.

Rivastigmine has no known severe interactions with other drugs.

Serious interactions of rivastigmine include:

• atenolol
• betaxolol
• bisoprolol
• esmolol
• levobunolol
• metoclopramide
• metoprolol
• nadolol
• nebivolol
• propranolol
• sotalol
• timolol

Rivastigmine has moderate with at least 58 different drugs.

Mild interactions of rabies vaccine include:

• aspirin rectal
• aspirin/citric acid/sodium bicarbonate
• choline magnesium trisalicylate
• desipramine
• ketorolac intranasal
• trazodone

This document does not contain all possible interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist. Check with your physician if you have health questions or concerns.

Warnings

This medication contains rivastigmine. Do not take Exelon or Exelon Patch if you are allergic to rivastigmine or any ingredients contained in this drug.

Keep out of reach of children. In case of overdose, get medical help or contact a Poison Control Center immediately.

Contraindications

• Hypersensitivity to rivastigmine or carbamates
• History of application site reaction with transdermal patch
• Active gastrointestinal (GI) bleeding

Effects of Drug Abuse

• No information available

Short-Term Effects

• See "What Are Side Effects Associated with Using Rivastigmine?"

Long-Term Effects

• See "What Are Side Effects Associated with Using Rivastigmine?"

Cautions

• Anorexia.
• Sick sinus syndrome.
• History of peptic ulcer.
• History of asthma/chronic obstructive pulmonary disease (COPD).
• May induce/exacerbate extrapyramidal symptoms.
• Concomitant nonsteroidal anti-inflammatory drug (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 and Lactation

• Rivastigmine may be acceptable for use during pregnancy. Either animal studies show no risk but human studies are not available or animal studies showed minor risks and human studies were done and showed no risk.
• It is unknown if rivastigmine is excreted in milk. It is not recommended for use while breastfeeding.