Donepezil 10mg 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
Anti-Alzheimer's agent
Pharmacologic Class
Central acetylcholinesterase inhibitor
Pregnancy 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. This can help improve memory, awareness, and the ability to function in people with Alzheimer's.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. Continue taking the medication as directed by your doctor or healthcare provider, even if you feel well. Take the medication at bedtime, with or without food. It is recommended to drink plenty of non-caffeinated liquids, unless your doctor advises you to limit your fluid intake.
Storing and Disposing of Your Medication
Store the medication at room temperature in a dry place, avoiding 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. If you have questions about disposing of your medication, consult your pharmacist. You may also want to check if there are drug take-back programs available in your area.
Missing a Dose
If you miss a dose, skip it and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses. If you miss seven consecutive days of medication, contact your doctor for guidance on how to proceed.
To use this medication correctly, follow your doctor's instructions and read all the information provided. Continue taking the medication as directed by your doctor or healthcare provider, even if you feel well. Take the medication at bedtime, with or without food. It is recommended to drink plenty of non-caffeinated liquids, unless your doctor advises you to limit your fluid intake.
Storing and Disposing of Your Medication
Store the medication at room temperature in a dry place, avoiding 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. If you have questions about disposing of your medication, consult your pharmacist. You may also want to check if there are drug take-back programs available in your area.
Missing a Dose
If you miss a dose, skip it and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses. If you miss seven consecutive days of medication, contact your doctor for guidance on how to proceed.
Lifestyle & Tips
- Take donepezil exactly as prescribed by your doctor, usually once daily in the evening, just before bedtime. Taking it at bedtime may help reduce stomach upset.
- Do not stop taking donepezil suddenly without talking to your doctor, as this can worsen symptoms.
- Report any new or worsening side effects to your doctor, especially severe nausea, vomiting, diarrhea, dizziness, or fainting spells.
- Maintain regular follow-up appointments with your doctor to monitor your condition and the effectiveness of the medication.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
10 mg orally once daily (maintenance dose)
Dose Range:
5 - 23 mg
Condition-Specific Dosing:
initial_dose:
5 mg orally once daily for 4-6 weeks
maintenance_dose:
10 mg orally once daily after 4-6 weeks on 5 mg
severe_alzheimers:
23 mg orally once daily after at least 3 months on 10 mg
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment needed
Moderate:
No dose adjustment needed
Severe:
Use with caution; monitor for adverse effects
Dialysis:
Not significantly removed by dialysis; no specific recommendations, monitor closely
Hepatic Impairment:
Mild:
No dose adjustment needed
Moderate:
No dose adjustment needed
Severe:
Use with caution; monitor for adverse effects
Pharmacology
Mechanism of Action
Donepezil is a reversible inhibitor of acetylcholinesterase, the enzyme responsible for the hydrolysis of acetylcholine. By inhibiting acetylcholinesterase, donepezil increases the concentration of acetylcholine at cholinergic synapses in the central nervous system, which is thought to compensate for the cholinergic deficit in Alzheimer's disease.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 100%
Tmax:
3-4 hours
FoodEffect:
Food does not affect the rate or extent of absorption.
Distribution:
Vd:
Approximately 12 L/kg
ProteinBinding:
Approximately 95-97% (primarily to albumin and alpha1-acid glycoprotein)
CnssPenetration:
Yes
Elimination:
HalfLife:
Approximately 70 hours
Clearance:
Not available (systemic clearance approximately 0.13 L/hr/kg)
ExcretionRoute:
Urine (57%), Feces (14.5%)
Unchanged:
Approximately 17% (in urine)
Pharmacodynamics
OnsetOfAction:
Clinical effects typically observed after several weeks of treatment (steady-state reached in about 3 weeks)
PeakEffect:
Steady-state plasma concentrations reached in approximately 3 weeks
DurationOfAction:
Long half-life supports once-daily dosing
Safety & Warnings
Side Effects
Serious Side Effects: Seek Medical Help 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 attention 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, contact your doctor if they bother you or do not go away:
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. Your doctor can provide medical advice about side effects.
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 attention 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, contact your doctor if they bother you or do not go away:
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. Your doctor can provide medical advice about side effects.
Seek Immediate Medical Attention If You Experience:
- Severe or persistent nausea, vomiting, or diarrhea
- Severe stomach pain or black/tarry stools (signs of GI bleeding)
- Slow heart rate (bradycardia)
- Fainting spells (syncope)
- Dizziness or lightheadedness
- New or worsening seizures
- Difficulty urinating
- Muscle weakness or cramps
- Unusual dreams or nightmares
- Hallucinations
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 information will help your doctor assess 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 crucial to verify that this medication can be taken with all your current medications and health conditions. Never start, stop, or adjust the dose of any medication without first consulting your doctor. By sharing this information, you can help your doctor make informed decisions about your treatment and minimize potential risks.
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 information will help your doctor assess 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 crucial to verify that this medication can be taken with all your current medications and health conditions. Never start, stop, or adjust the dose of any medication without first consulting your doctor. By sharing this information, you can help your doctor make informed decisions about your treatment and minimize potential risks.
Precautions & Cautions
It is essential to inform all of your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. This drug does not cure Alzheimer's disease, and you should continue to receive regular care from your doctor. If you are pregnant, planning to become pregnant, or are breast-feeding, be sure to discuss this with your doctor, as you will need to carefully weigh the 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 (slow, shallow breathing)
- Collapse
- Convulsions
- Increased muscle weakness (potentially leading to death if respiratory muscles are involved)
What to Do:
In case of overdose, seek immediate medical attention or call a poison control center (1-800-222-1222). Atropine is the antidote for cholinergic crisis.
Drug Interactions
Major Interactions
- Anticholinergic agents (e.g., atropine, scopolamine, tricyclic antidepressants, antipsychotics): May antagonize the effects of donepezil.
- Succinylcholine, other neuromuscular blocking agents: May prolong neuromuscular blockade due to enhanced cholinergic activity.
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.
- CYP3A4/2D6 inducers (e.g., rifampin, phenytoin, carbamazepine, phenobarbital): May decrease donepezil plasma concentrations.
- Beta-blockers (e.g., metoprolol, propranolol): Increased risk of bradycardia and syncope.
- NSAIDs (e.g., ibuprofen, naproxen): Increased risk of gastrointestinal bleeding (due to increased gastric acid secretion from cholinergic stimulation).
Monitoring
Baseline Monitoring
Cognitive function assessment (e.g., MMSE, ADAS-Cog)
Rationale: To establish baseline cognitive status and track disease progression/response to treatment.
Timing: Prior to initiation of therapy
Heart rate and ECG (if cardiac history)
Rationale: Donepezil can cause bradycardia and QT prolongation.
Timing: Prior to initiation of therapy
Liver function tests (ALT, AST, bilirubin)
Rationale: Donepezil is metabolized by the liver; to assess baseline hepatic function.
Timing: Prior to initiation of therapy
Renal function (SCr, eGFR)
Rationale: To assess baseline renal function, though dose adjustments are generally not needed for mild-moderate impairment.
Timing: Prior to initiation of therapy
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 treatment or dose.
Heart rate and blood pressure
Frequency: Periodically, especially during dose titration or if symptoms of bradycardia/syncope occur
Target: Normal sinus rhythm, stable blood pressure
Action Threshold: Bradycardia (<50 bpm), symptomatic hypotension, or syncope should prompt evaluation and potential dose reduction/discontinuation.
Gastrointestinal symptoms (nausea, vomiting, diarrhea)
Frequency: Regularly, especially during initial therapy and dose titration
Target: Absence or mild, tolerable symptoms
Action Threshold: Persistent or severe GI symptoms may require dose reduction or discontinuation.
Weight
Frequency: Periodically
Target: Stable weight
Action Threshold: Significant unexplained weight loss may indicate underlying issues or severe GI side effects.
Symptom Monitoring
- Nausea
- Vomiting
- Diarrhea
- Anorexia
- Dizziness
- Insomnia
- Fatigue
- Muscle cramps
- Bradycardia (slow heart rate)
- Syncope (fainting)
- Urinary incontinence
- Seizures (rare)
Special Patient Groups
Pregnancy
Donepezil is Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
Potential risk based on animal studies, but human data are lacking.
Second Trimester:
Potential risk based on animal studies, but human data are lacking.
Third Trimester:
Potential risk based on animal studies, but human data are lacking.
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. Generally not recommended.
Infant Risk:
Potential for cholinergic effects (e.g., bradycardia, increased secretions, GI upset) in the infant. Risk level is L3/L4 (Moderately Safe to Potentially Hazardous) due to lack of data and potential for harm.
Pediatric Use
Safety and effectiveness in pediatric patients have not been established. Donepezil is not indicated for use in children.
Geriatric Use
Donepezil is primarily used in the geriatric population. 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
- Administer donepezil in the evening, just prior to bedtime, to minimize the incidence of gastrointestinal side effects (nausea, vomiting) and sleep disturbances.
- Titrate the dose slowly (e.g., 5 mg for 4-6 weeks before increasing to 10 mg) to improve tolerability.
- Monitor patients for signs of bradycardia, syncope, and falls, especially during dose escalation and in patients with pre-existing cardiac conditions.
- Be aware of the potential for increased gastric acid secretion and increased risk of GI bleeding, particularly in patients taking NSAIDs concurrently.
- Donepezil's long half-life (approximately 70 hours) means that steady-state concentrations are reached slowly (around 3 weeks), and effects may persist for some time after discontinuation.
Alternative Therapies
- Rivastigmine (Exelon) - another acetylcholinesterase inhibitor (oral, patch)
- Galantamine (Razadyne) - another acetylcholinesterase inhibitor (oral)
- Memantine (Namenda) - an NMDA receptor antagonist (often used in moderate to severe AD, sometimes in combination with donepezil)
Cost & Coverage
Average Cost:
Varies widely, typically $10-$50 per 30 tablets (10mg)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (Generic)
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, 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 medical attention. When reporting the incident, be prepared to provide details about the medication taken, the amount, and the time it occurred.