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ARICEPT
Overview
What is ARICEPT?
What does ARICEPT look like?
What are the available doses of ARICEPT?
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What should I talk to my health care provider before I take ARICEPT?
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How should I use ARICEPT?
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What interacts with ARICEPT?
ARICEPT® is contraindicated in patients with known hypersensitivity to donepezil hydrochloride or to piperidine derivatives.
What are the warnings of ARICEPT?
Anesthesia
ARICEPT®, as a cholinesterase inhibitor, is likely to exaggerate succinylcholine-type muscle relaxation during anesthesia.
Cardiovascular Conditions
Because of their pharmacological action, cholinesterase inhibitors may have vagotonic effects on the sinoatrial and atrioventricular nodes. This effect may manifest as bradycardia or heart block in patients both with and without known underlying cardiac conduction abnormalities. Syncopal episodes have been reported in association with the use of ARICEPT®.
Gastrointestinal Conditions
Through their primary action, cholinesterase inhibitors may be expected to increase gastric acid secretion due to increased cholinergic activity. Therefore, patients should be monitored closely for symptoms of active or occult gastrointestinal bleeding, especially those at increased risk for developing ulcers, e.g., those with a history of ulcer disease or those receiving concurrent nonsteroidal anti-inflammatory drugs (NSAIDS). Clinical studies of ARICEPT® have shown no increase, relative to placebo, in the incidence of either peptic ulcer disease or gastrointestinal bleeding.
ARICEPT®, as a predictable consequence of its pharmacological properties, has been shown to produce diarrhea, nausea and vomiting. These effects, when they occur, appear more frequently with the 10 mg/day dose than with the 5 mg/day dose. In most cases, these effects have been mild and transient, sometimes lasting one to three weeks, and have resolved during continued use of ARICEPT®.
Genitourinary
Although not observed in clinical trials of ARICEPT®, cholinomimetics may cause bladder outflow obstruction.
Neurological Conditions
Seizures: Cholinomimetics are believed to have some potential to cause generalized convulsions. However, seizure activity also may be a manifestation of Alzheimer's Disease.
Pulmonary Conditions
Because of their cholinomimetic actions, cholinesterase inhibitors should be prescribed with care to patients with a history of asthma or obstructive pulmonary disease.
Sulfites
ARICEPT® Oral Solution contains sodium metabisulfite, a sulfite that may cause allergic-type reactions including anaphylactic symptoms and life-threatening or less severe asthmatic episodes in certain susceptible people. The overall prevalence of sulfite sensitivity in the general population is unknown and probably low. Sulfite sensitivity is seen more frequently in asthmatic than nonasthmatic people.
What are the precautions of ARICEPT?
Drug-Drug Interactions
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No clinical trials have investigated the effect of ARICEPT® on the clearance of drugs metabolized by CYP 3A4 (e.g. cisapride, terfenadine) or by CYP 2D6 (e.g. imipramine). However, studies show a low rate of binding to these enzymes (mean Ki about 50-130 μM), that, given the therapeutic plasma concentrations of donepezil (164 nM), indicates little likelihood of interference.
Whether ARICEPT® has any potential for enzyme induction is not known.
Formal pharmacokinetic studies evaluated the potential of ARICEPT® for interaction with theophylline, cimetidine, warfarin and digoxin. No significant effects on the pharmacokinetics of these drugs were observed..
Ketoconazole and quinidine, inhibitors of CYP450, 3A4 and 2D6, respectively, inhibit donepezil metabolism . Whether there is a clinical effect of these inhibitors is not known. In a 7-day crossover study in 18 healthy volunteers, ketoconazole (200mg q.d.) increased mean donepezil (5mg q.d.) concentrations (AUC and C) by 36%. The clinical relevance of this increase in concentration is unknown.
Inducers of CYP 2D6 and CYP 3A4 (e.g., phenytoin, carbamazepine, dexamethasone, rifampin, and phenobarbital) could increase the rate of elimination of ARICEPT®.
Formal pharmacokinetic studies demonstrated that the metabolism of ARICEPT® is not significantly affected by concurrent administration of digoxin or cimetidine.
Use with Anticholinergics
Because of their mechanism of action, cholinesterase inhibitors have the potential to interfere with the activity of anticholinergic medications.
Use with Cholinomimetics and Other Cholinesterase Inhibitors
A synergistic effect may be expected when cholinesterase inhibitors are given concurrently with succinylcholine, similar neuromuscular blocking agents or cholinergic agonists such as bethanechol.
Carcinogenesis, Mutagenesis, Impairment of Fertility
No evidence of a carcinogenic potential was obtained in an 88-week carcinogenicity study of donepezil hydrochloride conducted in CD-1 mice at doses up to 180 mg/kg/day (approximately 90 times the maximum recommended human dose on a mg/m basis), or in a 104-week carcinogenicity study in Sprague-Dawley rats at doses up to 30mg/kg/day (approximately 30 times the maximum recommended human dose on a mg/m basis).
Donepezil was not mutagenic in the Ames reverse mutation assay in bacteria, or in a mouse lymphoma forward mutation assay . In the chromosome aberration test in cultures of Chinese hamster lung (CHL) cells, some clastogenic effects were observed. Donepezil was not clastogenic in the mouse micronucleus test and was not genotoxic in an unscheduled DNA synthesis assay in rats.
Donepezil had no effect on fertility in rats at doses up to 10 mg/kg/day (approximately 8 times the maximum recommended human dose on a mg/m basis).
Pregnancy
Teratology studies conducted in pregnant rats at doses up to 16 mg/kg/day (approximately 13 times the maximum recommended human dose on a mg/m basis) and in pregnant rabbits at doses up to 10 mg/kg/day (approximately 16 times the maximum recommended human dose on a mg/m basis) did not disclose any evidence for a teratogenic potential of donepezil. However, in a study in which pregnant rats were given up to 10 mg/kg/day (approximately 8 times the maximum recommended human dose on a mg/m basis) from day 17 of gestation through day 20 postpartum, there was a slight increase in still births and a slight decrease in pup survival through day 4 postpartum at this dose; the next lower dose tested was 3 mg/kg/day. There are no adequate or well-controlled studies in pregnant women. ARICEPT® should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
It is not known whether donepezil is excreted in human breast milk. ARICEPT® has no indication for use in nursing mothers.
Pediatric Use
There are no adequate and well-controlled trials to document the safety and efficacy of ARICEPT® in any illness occurring in children.
Geriatric Use
Alzheimer's disease is a disorder occurring primarily in individuals over 55 years of age. The mean age of patients enrolled in the clinical studies with ARICEPT® was 73 years; 80% of these patients were between 65 and 84 years old and 49% of patients were at or above the age of 75. The efficacy and safety data presented in the clinical trials section were obtained from these patients. There were no clinically significant differences in most adverse events reported by patient groups ≥ 65 years old and < 65 years old.
What are the side effects of ARICEPT?
Mild to Moderate Alzheimer's Disease Trials
The rates of discontinuation from controlled clinical trials of ARICEPT® due to adverse events for the ARICEPT® 5 mg/day treatment groups were comparable to those of placebo-treatment groups at approximately 5%. The rate of discontinuation of patients who received 7-day escalations from 5 mg/day to 10 mg/day, was higher at 13%.
The most common adverse events 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.
| Dose Group | Placebo | 5 mg/day ARICEPT® | 10 mg/day ARICEPT® |
|---|---|---|---|
| Patients Randomized | 355 | 350 | 315 | Event/%Discontinuing |
| Nausea | 1% | 1% | 3% |
| Diarrhea | 0% | <1% | 3% |
| Vomiting | <1% | <1% | 2% |
The most common adverse events, defined as those occurring at a frequency of at least 5% in patients receiving 10 mg/day and twice the placebo rate, are largely predicted by ARICEPT®'s cholinomimetic effects. These include nausea, diarrhea, insomnia, vomiting, muscle cramp, fatigue and anorexia. These adverse events were often of mild intensity and transient, resolving during continued ARICEPT® treatment without the need for dose modification.
There is evidence to suggest that the frequency of these common adverse events may be affected by the rate of titration. An open-label study was conducted with 269 patients who received placebo in the 15 and 30-week studies. These patients were titrated to a dose of 10 mg/day over a 6-week period. The rates of common adverse events were lower than those seen in patients titrated to 10 mg/day over one week in the controlled clinical trials and were comparable to those seen in patients on 5 mg/day.
See Table 2 for a comparison of the most common adverse events following one and six week titration regimens.
| Nausea | 6% | 5% | 19% | 6% |
| Diarrhea | 5% | 8% | 15% | 9% |
| Insomnia | 6% | 6% | 14% | 6% |
| Fatigue | 3% | 4% | 8% | 3% |
| Vomiting | 3% | 3% | 8% | 5% |
| Muscle cramps | 2% | 6% | 8% | 3% |
| Anorexia | 2% | 3% | 7% | 3% |
The events cited reflect experience gained under closely monitored conditions of clinical trials in a highly selected patient population. In actual clinical practice or in other clinical trials, these frequency estimates may not apply, as the conditions of use, reporting behavior, and the kinds of patients treated may differ. Table 3 lists treatment emergent signs and symptoms that were reported in at least 2% of patients in placebo-controlled trials who received ARICEPT® and for which the rate of occurrence was greater for ARICEPT® assigned than placebo assigned patients. In general, adverse events occurred more frequently in female patients and with advancing age.
| Body System/Adverse Event | ||
|---|---|---|
| Percent of Patients with any Adverse Event | 72 | 74 | Body as a Whole |
| Headache | 9 | 10 |
| Pain, various locations | 8 | 9 |
| Accident | 6 | 7 |
| Fatigue | 3 | 5 | Cardiovascular System |
| Syncope | 1 | 2 | Digestive System |
| Nausea | 6 | 11 |
| Diarrhea | 5 | 10 |
| Vomiting | 3 | 5 |
| Anorexia | 2 | 4 | Hemic and Lymphatic System |
| Ecchymosis | 3 | 4 | Metabolic and Nutritional Systems |
| Weight Decrease | 1 | 3 | Musculoskeletal System |
| Muscle Cramps | 2 | 6 |
| Arthritis | 1 | 2 | Nervous System |
| Insomnia | 6 | 9 |
| Dizziness | 6 | 8 |
| Depression | <1 | 3 |
| Abnormal Dreams | 0 | 3 |
| Somnolence | <1 | 2 | Urogenital System |
| Frequent Urination | 1 | 2 |
ARICEPT® has been administered to over 1700 individuals during clinical trials worldwide. Approximately 1200 of these patients have been treated for at least 3 months and more than 1000 patients have been treated for at least 6 months. Controlled and uncontrolled trials in the United States included approximately 900 patients. In regards to the highest dose of 10 mg/day, this population includes 650 patients treated for 3 months, 475 patients treated for 6 months and 116 patients treated for over 1 year. The range of patient exposure is from 1 to 1214 days.
Treatment emergent signs and symptoms that occurred during 3 controlled clinical trials and two open-label trials in the United States were recorded as adverse events by the clinical investigators using terminology of their own choosing. To provide an overall estimate of the proportion of individuals having similar types of events, the events were grouped into a smaller number of standardized categories using a modified COSTART dictionary and event frequencies were calculated across all studies. These categories are used in the listing below. The frequencies represent the proportion of 900 patients from these trials who experienced that event while receiving ARICEPT®. All adverse events occurring at least twice are included, except for those already listed in Tables 2 or 3, COSTART terms too general to be informative, or events less likely to be drug caused. Events are classified by body system and listed using the following definitions: - those occurring in at least 1/100 patients; - those occurring in 1/100 to 1/1000 patients. These adverse events are not necessarily related to ARICEPT® treatment and in most cases were observed at a similar frequency in placebo-treated patients in the controlled studies. No important additional adverse events were seen in studies conducted outside the United States.
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Severe Alzheimer's Disease
Adverse Events Leading to Discontinuation
The rates of discontinuation from controlled clinical trials of ARICEPT® due to adverse events for the ARICEPT® patients were approximately 12% compared to 7% for placebo patients.
The most common adverse events leading to discontinuation, defined as those occurring in at least 2% of ARICEPT® patients and at twice the incidence seen in placebo patients, were anorexia (2% vs 1% placebo), nausea (2% vs <1% placebo), diarrhea (2% vs 0% placebo) and urinary tract infection (2% vs 1% placebo).
Most Frequent Adverse Clinical Events Seen in Association with the Use of ARICEPT
The most common adverse events, defined as those occurring at a frequency of at least 5% in patients receiving ARICEPT® and twice the placebo rate, are largely predicted by ARICEPT®'s cholinomimetic effects. These include diarrhea, anorexia, vomiting, nausea, and ecchymosis. These adverse events were often of mild intensity and transient, resolving during continued ARICEPT® treatment without the need for dose modification.
Adverse Events Reported in Controlled Trials
Table 4 lists treatment emergent signs and symptoms that were reported in at least 2% of patients in placebo-controlled trials who received ARICEPT® and for which the rate of occurrence was greater for ARICEPT® assigned than placebo assigned patients.
Other Adverse Events Observed During Clinical Trials
ARICEPT® has been administered to over 600 patients with severe Alzheimer's Disease during clinical trials of at least 6 months duration, including 3 double blind placebo controlled trials, one of which had an open label extension. All adverse events occurring at least twice are included, except for those already listed in Table 4, COSTART terms too general to be informative, or events less likely to be drug caused. Events are classified by body system using the COSTART dictionary and listed using the following definitions: - those occurring in at least 1/100 patients; - those occurring in 1/100 to 1/1000 patients. These adverse events are not necessarily related to ARICEPT® treatment and in most cases were observed at a similar frequency in placebo-treated patients in the controlled studies.
Body as a Whole:
Frequent:
Infrequent:
Cardiovascular System:
Frequent:
Infrequent:
Digestive System:
Frequent:
Infrequent:
Endocrine System:
Infrequent:
Hemic and Lymphatic System:
Frequent:
Infrequent
Metabolic and Nutritional Disorders:
Frequent:
Infrequent
Musculoskeletal System:
Frequent:
Infrequent:
Nervous System:
Frequent:
Infrequent:
Respiratory System:
Frequent:
Infrequent:
Skin and Appendages:
Frequent:
Infrequent:
Special Senses:
Infrequent:
Urogenital System:
Frequent:
Infrequent:
| Body System/Adverse Event | ||
|---|---|---|
| Percent of Patients with any Adverse Event | 73 | 81 | Body as a Whole |
| Accident | 12 | 13 |
| Infection | 9 | 11 |
| Headache | 3 | 4 |
| Pain | 2 | 3 |
| Back Pain | 2 | 3 |
| Fever | 1 | 2 |
| Chest Pain | <1 | 2 | Cardiovascular System |
| Hypertension | 2 | 3 |
| Hemorrhage | 1 | 2 |
| Syncope | 1 | 2 | Digestive System |
| Diarrhea | 4 | 10 |
| Vomiting | 4 | 8 |
| Anorexia | 4 | 8 |
| Nausea | 2 | 6 | Hemic and Lymphatic System |
| Ecchymosis | 2 | 5 | Metabolic and Nutritional Systems |
| Creatine Phosphokinase Increased | 1 | 3 |
| Dehydration | 1 | 2 |
| Hyperlipemia | <1 | 2 | Nervous System |
| Insomnia | 4 | 5 |
| Hostility | 2 | 3 |
| Nervousness | 2 | 3 |
| Hallucinations | 1 | 3 |
| Somnolence | 1 | 2 |
| Dizziness | 1 | 2 |
| Depression | 1 | 2 |
| Confusion | 1 | 2 |
| Emotional Lability | 1 | 2 |
| Personality Disorder | 1 | 2 | Skin And Appendages |
| Eczema | 2 | 3 | Urogenital System |
| Urinary Incontinence | 1 | 2 |
Postintroduction Reports
Voluntary reports of adverse events temporally associated with ARICEPT® that have been received since market introduction that are not listed above, and that there is inadequate data to determine the causal relationship with the drug include the following: abdominal pain, agitation, cholecystitis, confusion, convulsions, hallucinations, heart block (all types), hemolytic anemia, hepatitis, hyponatremia, neuroleptic malignant syndrome, pancreatitis, and rash.
What should I look out for while using ARICEPT?
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What might happen if I take too much ARICEPT?
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How should I store and handle ARICEPT?
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Clinical Information
Chemical Structure
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Non-Clinical Toxicology
Reference
This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"
While we update our database periodically, we cannot guarantee it is always updated to the latest version.
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