Exelon

What Is Exelon?

Exelon (rivastigmine tartrate) is a reversible cholinesterase inhibitor used to treat mild to moderate dementia caused by Alzheimer's or Parkinson's disease.

What Are Side Effects of Exelon?

Common side effects of Exelon include:

• nausea,
• vomiting,
• upset stomach,
• loss of appetite,
• weight loss,
• diarrhea,
• weakness,
• dizziness,
• swelling in your hands or feet,
• joint pain,
• cough,
• runny or stuffy nose,
• increased sweating,
• drowsiness,
• sleep problems (insomnia),
• headache, and
• shakiness (tremors).

Tell your doctor if you have serious side effects of Exelon including:

• slow or irregular heartbeat,
• fainting,
• black stools,
• vomit that looks like coffee grounds,
• severe stomach or abdominal pain,
• seizures, or
• trouble urinating.

Dosage for Exelon

The dosage of Exelon to treat Alzheimer's Disease is 6-12 mg/day, given twice-a-day. The dose to treat Parkinson's Disease is 3-12 mg/day, given twice-a-day.

What Drugs, Substances, or Supplements Interact with Exelon?

Exelon may interact with atropine, belladonna, clidinium, dicyclomine, glycopyrrolate, hyoscyamine, mepenzolate, methantheline, methscopolamine, propantheline, or scopolamine. Tell your doctor all medications you are taking.

Exelon During Pregnancy and Breastfeeding

During pregnancy, this medication should be used only when prescribed by a doctor. It is unknown if this medication passes into breast milk. Consult your doctor before breastfeeding.

Additional Information

Our Exelon (rivastigmine tartrate) Side Effects Drug Center provides a comprehensive view of available drug information on the potential side effects when taking this medication.

 

Exelon Consumer Information

Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have:

• severe or ongoing vomiting or diarrhea, loss of appetite, weight loss;
• bloody or tarry stools, cough with bloody mucus or vomit that looks like coffee grounds;
• a light-headed feeling, like you might pass out;
• tremors (uncontrolled shaking), restless muscle movements in your eyes, tongue, jaw, or neck;
• seizure (convulsions);
• painful or difficult urination;
• severe skin redness, itching, or irritation; or
• dehydration symptoms--feeling very thirsty or hot, being unable to urinate, heavy sweating, or hot and dry skin.

Common side effects may include:

• upset stomach, nausea, vomiting;
• loss of appetite; or
• weakness.

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

Read the entire detailed patient monograph for Exelon (Rivastigmine Tartrate)

 

Exelon Professional Information

SIDE EFFECTS

The following adverse reactions are described below and elsewhere in the labeling:

• Gastrointestinal Adverse Reactions [see WARNINGS AND PRECAUTIONS]
• Allergic Dermatitis [see WARNINGS AND PRECAUTIONS]
• Other Adverse Reactions from Increased Cholinergic Activity [see WARNINGS AND PRECAUTIONS]

Clinical Trials Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

EXELON has been administered to over 5,297 individuals during clinical trials worldwide. Of these, 4,326 patients have been treated for at least 3 months, 3,407 patients have been treated for at least 6 months, 2,150 patients have been treated for 1 year, 1,250 patients have been treated for 2 years, and 168 patients have been treated for over 3 years. With regard to exposure to the highest dose, 2,809 patients were exposed to doses of 10 mg to 12 mg, 2,615 patients treated for 3 months, 2,328 patients treated for 6 months, 1,378 patients treated for 1 year, 917 patients treated for 2 years, and 129 patients treated for over 3 years.

Mild-To-Moderate Alzheimer’s Disease

Most Common Adverse Reactions

The most common adverse reactions, defined as those occurring at a frequency of at least 5% and twice the placebo rate, are largely predicted by EXELON's cholinergic effects. These include nausea, vomiting, anorexia, dyspepsia, and asthenia.

Gastrointestinal Adverse Reactions

EXELON use is associated with significant nausea, vomiting, and weight loss [see WARNINGS AND PRECAUTIONS].

Discontinuation Rates

The rate of discontinuation due to adverse events in controlled clinical trials of EXELON (rivastigmine tartrate) was 15% for patients receiving 6 mg to 12 mg per day compared to 5% for patients on placebo during forced weekly dose titration. While on a maintenance dose, the rates were 6% for patients on EXELON compared to 4% for those on placebo.

The most common adverse reactions leading to discontinuation, defined as those occurring in at least 2% of patients and at twice the incidence seen in placebo patients, are shown in Table 1.

Table 1: Most Frequent Adverse Reactions Leading to Withdrawal from Clinical Trials During Titration and Maintenance in Patients Receiving 6 mg to 12 mg per day EXELON Using a Forced-Dose Titration

Study Phase	Titration		Maintenance		Overall
	EXELON ≥ 6 to 12 mg/day	Placebo	EXELON ≥ 6 to 12 mg/day	Placebo	EXELON ≥ 6 to 12 mg/day	Placebo
	(n = 1,189)	(n = 868)	(n = 987)	(n = 788)	(n = 1,189)	(n = 868)
Event/% Discontinuing
Nausea	8	< 1	1	< 1	8	1
Vomiting	4	< 1	1	< 1	5	< 1
Anorexia	2	0	1	< 1	3	< 1
Dizziness	2	< 1	1	< 1	2	< 1

Adverse Reactions Observed at an Incidence of at Least 2%

Table 2 lists adverse reactions that occurred in at least 2% of patients in placebo-controlled trials, and for which the rate of occurrence was greater for patients treated with EXELON doses of 6 mg to 12 mg per day than for those treated with placebo.

In general, adverse reactions were less frequent later in the course of treatment.

No systematic effect of race or age could be determined from the incidence of adverse reactions in the controlled studies. Nausea, vomiting and weight loss were more frequent in women than men.

Table 2: Proportion of Adverse Reactions Observed with a Frequency of Greater Than or Equal to 2% and at a Rate Greater than Placebo in Clinical Trials

Body System/Adverse Reaction	EXELON	Placebo
	(6–12 mg/day) (n = 1,189)	(n = 868)
Percent of Patients with any Adverse Event	92	79
Increased Sweating	4	1
Syncope	3	2
Body as a Whole
Fatigue	9	5
Asthenia	6	2
Malaise	5	2
Decreased Weight**	3	< 1
Cardiovascular Disorders, General
Hypertension	3	2
Central and Peripheral Nervous System
Dizziness	21	11
Headache	17	12
Somnolence	5	3
Tremor	4	1
Gastrointestinal System
Nausea*	47	12
Vomiting*	31	6
Diarrhea	19	11
Anorexia***	17	3
Abdominal Pain	13	6
Dyspepsia	9	4
Psychiatric Disorders
Insomnia	9	7
Confusion	8	7
Depression	6	4
Anxiety	5	3
Hallucination	4	3
Aggressive Reaction	3	2
Resistance Mechanism Disorders
Urinary Tract Infection	7	6
*Nausea and Vomiting: In the controlled clinical trials, 47% of the patients treated with an EXELON dose in the therapeutic range of 6 mg to 12 mg per day (n = 1189) developed nausea (compared with 12% in placebo). A total of 31% of EXELON-treated patients developed at least 1 episode of vomiting (compared with 6% for placebo). The rate of vomiting was higher during the titration phase (24% versus 3% for placebo) than in the maintenance phase (14% versus 3% for placebo). The rates were higher in women than men. Five percent of patients discontinued for vomiting, compared to less than 1% for patients on placebo. Vomiting was severe in 2% of EXELON-treated patients and was rated as mild or moderate each in 14% of patients. The rate of nausea was higher during the titration phase (43% versus 9% for placebo) than in the maintenance phase (17% versus 4% for placebo). **Weight Decreased: In the controlled trials, approximately 26% of women on high doses of EXELON (greater than 9 mg per day) had weight loss equa l to or greater than 7% of their baseline weight compared to 6% in the placebo-treated patients. About 18% of the males in the high-dose group experienced a similar degree of weight loss compared to 4% in placebo-treated patients. It is not clear how much of the weight loss was associated with anorexia, nausea, vomiting, and the diarrhea associated with the drug. ***Anorexia: In the controlled clinical trials, of the patients treated with an EXELON dose of 6 mg to 12 mg per day, 17% deve loped anorexia compared to 3% of the placebo patients. Neither the time course nor the severity of the anorexia is known.

Mild-To-Moderate Parkinson’s Disease Dementia

EXELON has been administered to 779 individuals during clinical trials worldwide. Of these, 663 patients have been treated for at least 3 months, 476 patients have been treated for at least 6 months, and 313 patients have been treated for 1 year.

Most Common Adverse Reactions

The most common adverse reactions, defined as those occurring at a frequency of at least 5% and twice the placebo rate, are largely predicted by EXELON's cholinergic effects. These include nausea, vomiting, tremor, anorexia, and dizziness.

Discontinuation Rates

The rate of discontinuation due to adverse events in the single placebo-controlled trial of EXELON was 18% for patients receiving 3 mg to 12 mg per day compared to 11% for patients on placebo during the 24-week study.

The most frequent adverse reactions that led to discontinuation from this study, defined as those occurring in at least 1% of patients receiving EXELON and more frequent than those receiving placebo, were nausea (3.6% EXELON versus 0.6% placebo), vomiting (1.9% EXELON versus 0.6% placebo), and tremor (1.7% EXELON versus 0.0% placebo).

Adverse Reactions Observed at an Incidence of at Least 2%

Table 3 lists adverse reactions that occurred in at least 2% of patients in a single placebo-controlled trial and during the first 24 weeks of a 76-week open-label active-controlled trial for which the rate of occurrence was greater for patients treated with EXELON doses of 3 mg to 12 mg per day than for those treated with placebo in the placebo-controlled trial.

In general, adverse reactions were less frequent later in the course of treatment.

Table 3: Proportion of Adverse Reactions Observed at a Frequency Greater Than or Equal to 2% and Occurring at Rate Greater than Placebo in Clinical Trials

Body System/Adverse Reaction	Active-Controlled Study	Placebo-Controlled Study
	EXELON (3 to 12 mg/day)	EXELON (3 to 12 mg/day)	Placebo
	(n = 294)	(n = 362)	(n = 179)
Percent of Patients with any Adverse Event	88	84	71
Gastrointestinal Disorders
Nausea	38	29	11
Vomiting	13	17	2
Diarrhea	8	7	4
Upper Abdominal Pain	4	4	1
Salivary hypersecretion	2	1	0
General Disorders and Administrative Site Conditions
Fall	10	6	6
Fatigue	5	4	3
Asthenia	4	2	1
Metabolism and Nutritional Disorders
Anorexia	-	6	3
Decreased Appetite	5	8	5
Dehydration	1	2	1
Nervous System Disorders
Tremor	23	10	4
Dizziness	8	6	1
Headache	4	4	3
Somnolence	6	4	3
Parkinson’s Disease (worsening)	-*	3	1
Bradykinesia	3	3	2
Dyskinesia	3	1	1
Cogwheel rigidity	3	1	0
Hypokinesia	2	1	0
Parkinsonism	-	2	1
Psychiatric Disorders
Anxiety	4	4	1
Insomnia	2	3	2
Restlessness	1	3	2
Skin and Subcutaneous Tissue Disorders
Increased Sweating	2	2	1
*Parkinson’s disease (worsening) in the active-controlled study was assessed by reported pre-identified adverse events (tremor, cogwheel rigidity, fall), each of them listed with corresponding frequencies.

Postmarketing Experience

The following adverse reactions have been identified during post approval use of EXELON Capsules, EXELON Oral Solution, or EXELON Patch. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

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, urticaria

Read the entire FDA prescribing information for Exelon (Rivastigmine Tartrate)