Aricept 5mg Tablets
It is used to treat dementia in people with Alzheimer's disease.It may be given to you for other reasons. Talk with the doctor.
Drug Class
Cholinesterase Inhibitor
Pharmacologic Class
Central Acetylcholinesterase Inhibitor
Pregnancy Category
Category C
FDA Approved
Nov 1996
DEA Schedule
Not Controlled
Overview
What is this medicine?
Donepezil is a medication used to treat Alzheimer's disease. It works by increasing the amount of a natural substance in the brain called acetylcholine, which is important for memory and thinking. It can help improve memory, awareness, and the ability to function in daily life, but it is not a cure for Alzheimer's disease.
How to Use This Medicine
Taking Your Medication
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely. Continue taking your medication as directed by your doctor or healthcare provider, even if you start to feel better.
Take your medication at bedtime, with or without food. Drink plenty of non-caffeinated liquids, unless your doctor advises you to limit your fluid intake.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, away from the bathroom. Keep all medications in a safe location, out of the reach of children and pets. Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so by your doctor or pharmacist. If you have questions about disposing of your medication, consult with your pharmacist. You may also want to check if there are any drug take-back programs in your area.
Missing a Dose
If you miss a dose, skip it and take your next dose at the usual time. Do not take two doses at once or take extra doses. If you miss seven days of your medication, contact your doctor for guidance on what to do next.
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely. Continue taking your medication as directed by your doctor or healthcare provider, even if you start to feel better.
Take your medication at bedtime, with or without food. Drink plenty of non-caffeinated liquids, unless your doctor advises you to limit your fluid intake.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, away from the bathroom. Keep all medications in a safe location, out of the reach of children and pets. Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so by your doctor or pharmacist. If you have questions about disposing of your medication, consult with your pharmacist. You may also want to check if there are any drug take-back programs in your area.
Missing a Dose
If you miss a dose, skip it and take your next dose at the usual time. Do not take two doses at once or take extra doses. If you miss seven days of your medication, contact your doctor for guidance on what to do next.
Lifestyle & Tips
- Take donepezil exactly as prescribed by your doctor, usually once daily at bedtime.
- Taking it at bedtime may help reduce side effects like nausea and vomiting.
- Do not stop taking donepezil suddenly without consulting your doctor, as this can worsen symptoms.
- Report any new or worsening side effects to your doctor promptly.
- Maintain regular follow-up appointments with your doctor to monitor your condition and medication effectiveness.
- Inform all healthcare providers that you are taking donepezil, especially before any surgery or dental procedures, due to potential interactions with anesthesia.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
5 mg orally once daily at bedtime
Dose Range:
5 - 23 mg
Condition-Specific Dosing:
Alzheimer's Disease (Mild to Moderate):
Initial: 5 mg orally once daily at bedtime. After 4-6 weeks, may increase to 10 mg orally once daily at bedtime.
Alzheimer's Disease (Moderate to Severe):
Initial: 5 mg orally once daily at bedtime. After 4-6 weeks, may increase to 10 mg orally once daily at bedtime. For patients stable on 10 mg for at least 3 months, may consider increasing to 23 mg orally once daily.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment generally required.
Moderate:
No dose adjustment generally required.
Severe:
Use with caution; monitor for adverse effects.
Dialysis:
Donepezil is not dialyzable. No specific dose adjustment recommendations, but monitor for adverse effects.
Hepatic Impairment:
Mild:
No dose adjustment generally required.
Moderate:
No dose adjustment generally required.
Severe:
Use with caution; monitor for adverse effects. Consider slower titration.
Pharmacology
Mechanism of Action
Donepezil is a reversible inhibitor of acetylcholinesterase (AChE), the enzyme responsible for the hydrolysis of acetylcholine. By inhibiting AChE, donepezil increases the concentration of acetylcholine in the synaptic cleft, particularly in the cerebral cortex, thereby enhancing cholinergic neurotransmission. This action is thought to compensate for the cholinergic deficit observed in Alzheimer's disease.
Pharmacokinetics
Absorption:
Bioavailability:
100%
Tmax:
3-4 hours
FoodEffect:
Food does not affect the rate or extent of absorption.
Distribution:
Vd:
12 L/kg
ProteinBinding:
Approximately 96% (primarily to albumin and alpha1-acid glycoprotein)
CnssPenetration:
Yes
Elimination:
HalfLife:
Approximately 70 hours
Clearance:
0.13 L/hr/kg
ExcretionRoute:
Renal (urine) and fecal
Unchanged:
Approximately 17% (urine)
Pharmacodynamics
OnsetOfAction:
Clinical effects may be observed within 3 weeks, but optimal benefit may take longer with dose titration.
PeakEffect:
Plasma concentrations peak at 3-4 hours. Steady-state plasma concentrations are achieved within 15 days.
DurationOfAction:
Due to its long half-life, once-daily dosing maintains therapeutic concentrations.
Safety & Warnings
Side Effects
Serious Side Effects: Seek Medical Attention Immediately
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical help right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Severe dizziness or fainting
Slow heartbeat
Abnormal heartbeat
Difficulty urinating
Seizures
Heartburn
Severe stomach pain
Vomiting blood or coffee ground-like material
Black, tarry, or bloody stools
New or worsening trouble breathing
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor:
Dizziness, fatigue, or weakness
Diarrhea, upset stomach, or vomiting
Trouble sleeping
Muscle cramps
Decreased appetite
Weight loss
Headache
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical help right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Severe dizziness or fainting
Slow heartbeat
Abnormal heartbeat
Difficulty urinating
Seizures
Heartburn
Severe stomach pain
Vomiting blood or coffee ground-like material
Black, tarry, or bloody stools
New or worsening trouble breathing
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor:
Dizziness, fatigue, or weakness
Diarrhea, upset stomach, or vomiting
Trouble sleeping
Muscle cramps
Decreased appetite
Weight loss
Headache
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Severe nausea, vomiting, or diarrhea
- Black, tarry stools or vomit that looks like coffee grounds (signs of stomach bleeding)
- Slow heartbeat, dizziness, or fainting spells (syncope)
- New or worsening muscle cramps or weakness
- Difficulty breathing or worsening of asthma/COPD symptoms
- Seizures
- Severe abdominal pain
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced as a result of the allergy.
All medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. This is crucial to avoid potential interactions between this medication and other substances.
Any existing health problems, as they may affect the safety and efficacy of this medication.
To ensure your safety, it is vital to:
Discuss all your medications and health problems with your doctor and pharmacist to verify that it is safe to take this medication in conjunction with your other treatments.
* Avoid starting, stopping, or changing the dosage of any medication without first consulting your doctor. This will help prevent potential interactions and ensure the safe use of this medication.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced as a result of the allergy.
All medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. This is crucial to avoid potential interactions between this medication and other substances.
Any existing health problems, as they may affect the safety and efficacy of this medication.
To ensure your safety, it is vital to:
Discuss all your medications and health problems with your doctor and pharmacist to verify that it is safe to take this medication in conjunction with your other treatments.
* Avoid starting, stopping, or changing the dosage of any medication without first consulting your doctor. This will help prevent potential interactions and ensure the safe use of this medication.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. While this drug can help manage symptoms, it is not a cure for Alzheimer's disease, and you should continue to receive regular care from your doctor. If you are pregnant, planning to become pregnant, or are breastfeeding, be sure to discuss this with your doctor, as you will need to carefully weigh the potential benefits and risks of this medication to both you and your baby.
Overdose Information
Overdose Symptoms:
- Severe nausea
- Vomiting
- Salivation
- Sweating
- Bradycardia (slow heart rate)
- Hypotension (low blood pressure)
- Respiratory depression
- Collapse
- Convulsions
- Increased muscle weakness (potentially leading to death if respiratory muscles are involved)
What to Do:
Seek immediate medical attention. Call 911 or your local poison control center (1-800-222-1222 in the US). Atropine is a commonly used antidote for cholinergic crisis.
Drug Interactions
Major Interactions
- Anticholinergic agents (e.g., atropine, scopolamine, benztropine): May antagonize the effects of donepezil.
- Succinylcholine, other neuromuscular blocking agents: May prolong neuromuscular blockade.
Moderate Interactions
- CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, erythromycin, clarithromycin, ritonavir): May increase donepezil plasma concentrations.
- CYP2D6 inhibitors (e.g., quinidine, fluoxetine, paroxetine): May increase donepezil plasma concentrations.
- CYP3A4 inducers (e.g., phenytoin, carbamazepine, rifampin, dexamethasone, phenobarbital): May decrease donepezil plasma concentrations.
- Beta-blockers (e.g., metoprolol, carvedilol): Increased risk of bradycardia and syncope.
- NSAIDs (e.g., ibuprofen, naproxen): Increased risk of gastrointestinal bleeding, especially in patients with a history of ulcers.
Monitoring
Baseline Monitoring
Cognitive function assessment (e.g., MMSE, ADAS-Cog)
Rationale: To establish baseline cognitive status and track disease progression/response to therapy.
Timing: Prior to initiation of therapy.
Heart rate and rhythm
Rationale: Donepezil can cause bradycardia and syncope due to its cholinergic effects.
Timing: Prior to initiation, especially in patients with pre-existing cardiac conditions.
Gastrointestinal symptoms assessment
Rationale: To assess for baseline GI issues that may be exacerbated by donepezil.
Timing: Prior to initiation.
Routine Monitoring
Cognitive function assessment
Frequency: Every 6-12 months, or as clinically indicated.
Target: Improvement or stabilization of cognitive scores.
Action Threshold: Significant decline in cognitive function may warrant re-evaluation of therapy.
Heart rate and blood pressure
Frequency: Periodically, or if symptoms of bradycardia/syncope occur.
Target: Normal sinus rhythm, heart rate >50 bpm.
Action Threshold: Symptomatic bradycardia, syncope, or significant hypotension may require dose reduction or discontinuation.
Gastrointestinal symptoms (nausea, vomiting, diarrhea, dyspepsia)
Frequency: Regularly, especially during dose titration.
Target: Minimal or tolerable GI upset.
Action Threshold: Severe or persistent GI symptoms may require dose reduction or discontinuation.
Weight
Frequency: Periodically
Target: Stable weight
Action Threshold: Significant weight loss may indicate persistent GI side effects or other issues.
Symptom Monitoring
- Nausea
- Vomiting
- Diarrhea
- Dyspepsia
- Anorexia
- Insomnia
- Muscle cramps
- Fatigue
- Dizziness
- Headache
- Bradycardia
- Syncope
- Urinary incontinence
- Seizures (rare)
- Signs of GI bleeding (e.g., black, tarry stools; coffee-ground emesis)
Special Patient Groups
Pregnancy
Donepezil is Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
Potential for fetal harm cannot be ruled out.
Second Trimester:
Potential for fetal harm cannot be ruled out.
Third Trimester:
Potential for fetal harm cannot be ruled out. Cholinergic effects could theoretically affect uterine tone or fetal heart rate.
Lactation
It is not known whether donepezil is excreted in human milk. Due to the potential for serious adverse reactions in breastfed infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Infant Risk:
Risk unknown; potential for cholinergic effects in the infant.
Pediatric Use
Safety and effectiveness in pediatric patients have not been established. Donepezil is not indicated for use in children.
Geriatric Use
No specific dose adjustment is required based on age alone. However, elderly patients may be more susceptible to cholinergic side effects (e.g., bradycardia, syncope, GI upset), and should be monitored closely.
Clinical Information
Clinical Pearls
- Donepezil is typically taken at bedtime to help mitigate common gastrointestinal side effects like nausea and vomiting.
- Titrate the dose slowly (e.g., 5 mg for 4-6 weeks before increasing to 10 mg) to improve tolerability.
- It is not a cure for Alzheimer's disease but can help slow the progression of cognitive and functional decline in some patients.
- Patients and caregivers should be educated on potential side effects, especially cardiac (bradycardia, syncope) and GI (nausea, vomiting, diarrhea, GI bleeding risk with NSAIDs).
- Regular re-evaluation of the patient's response and tolerability is crucial to determine continued benefit.
Alternative Therapies
- Rivastigmine (Exelon, Exelon Patch) - another cholinesterase inhibitor
- Galantamine (Razadyne) - another cholinesterase inhibitor
- Memantine (Namenda) - an NMDA receptor antagonist, often used for moderate to severe AD, or in combination with cholinesterase inhibitors.
Cost & Coverage
Average Cost:
Varies widely (e.g., $10-$30 for generic 5mg, $200-$400+ for brand 5mg) per 30 tablets
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 for generic; Tier 3 or higher for brand.
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor promptly. To ensure safe and effective treatment, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about this medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide details about the medication, including the amount taken and the time it happened, to facilitate prompt and appropriate care.