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Exelon

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Exelon




Side Effects
Interactions

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 ≥ 6–12 mg/day
(n=1,189)
Placebo
(n=868)
EXELON ≥ 6–12 mg/day
(n=987)
Placebo
(n=788)
EXELON ≥ 6–12 mg/day
(n=1,189)
Placebo
(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 ≥ 2% and at a Rate Greater than Placebo in Clinical Trials

Body System/Adverse Reaction EXELON (6-12 mg/day)
(n=1,189)
Placebo
(n=868)
Percent of Patients with any Adverse Event 92 79
Autonomic Nervous System
  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 equal 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% developed 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 ≥ 2% and Occurring at Rate Greater than Placebo in Clinical Trials

Body System/Adverse Reaction Active-Controlled Study Placebo-Controlled Study
EXELON (3-l2 mg/day)
(n=294)
EXELON (3-12 mg/day)
(n=362)
Placebo
(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. 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.

Hepatobiliary Disorders: Hepatitis.

Psychiatric Disorders: Aggression.

Skin and Appendages: Stevens-Johnson syndrome, disseminated allergic dermatitis.

Read the Exelon (rivastigmine tartrate) Side Effects Center for a complete guide to possible side effects

DRUG INTERACTIONS

Metoclopramide

Due to the risk of additive extrapyramidal adverse reactions, the concomitant use of metoclopramide and EXELON is not recommendedd.

Cholinomimetic And Anticholinergic Medications

EXELON may increase the cholinergic effects of other cholinomimetic medications and may also interfere with the activity of anticholinergic medications (e.g., oxybutynin, tolterodine). Concomitant use of EXELON with medications having these pharmacologic effects is not recommended unless deemed clinically necessary [see WARNINGS AND PRECAUTIONS].

Beta-blockers

Additive bradycardic effects resulting in syncope may occur when EXELON is used concomitantly with beta-blockers, especially cardioselective beta-blockers (including atenolol). Concomitant use of EXELON with beta-blockers is not recommended.

Last reviewed on RxList: 2/13/2015
This monograph has been modified to include the generic and brand name in many instances.

Side Effects
Interactions
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Exelon - User Reviews

Exelon User Reviews

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You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088.


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