Galantamine 4mg/ml Oral Solution
It is used to treat dementia in people with Alzheimer's disease.
Drug Class
Cholinesterase inhibitor
Pharmacologic Class
Acetylcholinesterase inhibitor; Allosteric potentiator of nicotinic acetylcholine receptors
Pregnancy Category
Category C
FDA Approved
Sep 2001
DEA Schedule
Not Controlled
Overview
What is this medicine?
Galantamine is a medication used to treat mild to moderate Alzheimer's disease. It works by increasing the levels 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 perform daily activities.
How to Use This Medicine
Taking Your Medication Correctly
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. Take your medication at the same time every day to establish a routine. Continue taking your medication as directed by your doctor or healthcare provider, even if you start to feel better.
It's recommended to take your medication with food to help your body absorb it properly. Drink plenty of non-caffeinated liquids, unless your doctor advises you to limit your fluid intake. When taking a liquid dose, measure it accurately using the measuring device provided with your medication. Mix the dose with 3 to 4 ounces (about 100 mL) of a non-alcoholic liquid, stir well, and consume it immediately. Do not store the mixture for later use.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, away from the bathroom. Do not freeze your medication. 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 drug take-back programs available in your area.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember, with food. If it's close to the time for your next dose, skip the missed dose and resume your regular schedule. Do not take two doses at the same time or take extra doses. If you miss taking your medication for more than 3 days in a row, contact your doctor before restarting 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. Take your medication at the same time every day to establish a routine. Continue taking your medication as directed by your doctor or healthcare provider, even if you start to feel better.
It's recommended to take your medication with food to help your body absorb it properly. Drink plenty of non-caffeinated liquids, unless your doctor advises you to limit your fluid intake. When taking a liquid dose, measure it accurately using the measuring device provided with your medication. Mix the dose with 3 to 4 ounces (about 100 mL) of a non-alcoholic liquid, stir well, and consume it immediately. Do not store the mixture for later use.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, away from the bathroom. Do not freeze your medication. 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 drug take-back programs available in your area.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember, with food. If it's close to the time for your next dose, skip the missed dose and resume your regular schedule. Do not take two doses at the same time or take extra doses. If you miss taking your medication for more than 3 days in a row, contact your doctor before restarting your medication.
Lifestyle & Tips
- Take galantamine exactly as prescribed by your doctor. Do not stop taking it without consulting your doctor.
- Take the oral solution with food (preferably breakfast and dinner) to help reduce stomach upset, nausea, and vomiting.
- Measure the dose carefully using the provided measuring device (e.g., oral syringe).
- If you miss a dose, take it as soon as you remember, unless it's almost time for your next dose. Do not double dose.
- If you miss several doses, contact your doctor before restarting the medication, as you may need to restart at a lower dose and re-titrate.
- Stay hydrated, especially if experiencing diarrhea or vomiting.
- Be aware of potential dizziness or lightheadedness, especially when standing up quickly. Avoid driving or operating machinery until you know how the medication affects you.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Initial: 4 mg (1 mL) orally twice daily (8 mg/day). Titrate to 8 mg (2 mL) orally twice daily (16 mg/day) after 4 weeks. If tolerated, may increase to 12 mg (3 mL) orally twice daily (24 mg/day) after an additional 4 weeks. Administer with morning and evening meals.
Dose Range:
8 - 24 mg
Condition-Specific Dosing:
mild_moderate_alzheimers_dementia:
Initial: 4 mg (1 mL) orally twice daily (8 mg/day). Titrate to 8 mg (2 mL) orally twice daily (16 mg/day) after 4 weeks. If tolerated, may increase to 12 mg (3 mL) orally twice daily (24 mg/day) after an additional 4 weeks. Administer with morning and evening meals.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No dosage adjustment needed (CrCl 60-89 mL/min).
Moderate:
Maximum dose 16 mg/day (CrCl 30-59 mL/min).
Severe:
Not recommended (CrCl <9 mL/min).
Dialysis:
Not recommended; galantamine and its metabolites are not significantly removed by dialysis.
Hepatic Impairment:
Mild:
No dosage adjustment needed (Child-Pugh A).
Moderate:
Maximum dose 16 mg/day (Child-Pugh B).
Severe:
Not recommended (Child-Pugh C).
Pharmacology
Mechanism of Action
Galantamine is a reversible, competitive acetylcholinesterase inhibitor. It increases the concentration of acetylcholine in the synaptic cleft by slowing its breakdown. Additionally, galantamine allosterically potentiates the action of acetylcholine at nicotinic acetylcholine receptors, which may lead to increased acetylcholine release.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 90%
Tmax:
Approximately 1 hour
FoodEffect:
Food delays Tmax by about 1.5 hours but does not affect AUC (extent of absorption).
Distribution:
Vd:
Approximately 175 L
ProteinBinding:
18%
CnssPenetration:
Yes
Elimination:
HalfLife:
Approximately 7 hours
Clearance:
Approximately 6.6 L/hour
ExcretionRoute:
Renal (major), fecal (minor)
Unchanged:
Approximately 20-30% (renal excretion)
Pharmacodynamics
OnsetOfAction:
Within hours (pharmacological effect)
PeakEffect:
Not precisely defined for clinical effect, but steady-state plasma concentrations are reached within 7 days.
DurationOfAction:
Approximately 12 hours (due to twice-daily dosing)
Confidence:
Medium
Safety & Warnings
Side Effects
Urgent 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
Abnormal heart rhythms, including:
+ Slow heartbeat
+ Irregular heartbeat
Gastrointestinal bleeding, characterized by:
+ Black, tarry, or bloody stools
+ Vomiting blood or coffee ground-like material
Urinary retention or difficulty passing urine
Seizures
New or worsening trouble controlling body movements
Severe skin reactions, including:
+ Stevens-Johnson syndrome (SJS)
+ Toxic epidermal necrolysis (TEN)
+ Other severe skin reactions, such as:
- Red, swollen, blistered, or peeling skin
- Skin irritation (with or without fever)
- Red or irritated eyes
- Sores in the mouth, throat, nose, or eyes
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 if they bother you or persist, contact your doctor:
Dizziness or headache
Diarrhea, upset stomach, or vomiting
Decreased appetite
* Weight loss
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 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
Abnormal heart rhythms, including:
+ Slow heartbeat
+ Irregular heartbeat
Gastrointestinal bleeding, characterized by:
+ Black, tarry, or bloody stools
+ Vomiting blood or coffee ground-like material
Urinary retention or difficulty passing urine
Seizures
New or worsening trouble controlling body movements
Severe skin reactions, including:
+ Stevens-Johnson syndrome (SJS)
+ Toxic epidermal necrolysis (TEN)
+ Other severe skin reactions, such as:
- Red, swollen, blistered, or peeling skin
- Skin irritation (with or without fever)
- Red or irritated eyes
- Sores in the mouth, throat, nose, or eyes
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 if they bother you or persist, contact your doctor:
Dizziness or headache
Diarrhea, upset stomach, or vomiting
Decreased appetite
* Weight loss
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 or persistent nausea, vomiting, or diarrhea
- Significant weight loss
- Slow heartbeat (bradycardia)
- Fainting or feeling lightheaded (syncope)
- New or worsening stomach pain or heartburn
- Difficulty urinating
- Muscle weakness or cramps
- Seizures
- Signs of liver problems (e.g., yellowing of skin/eyes, dark urine, persistent nausea/vomiting)
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.
If you have a history of kidney disease or liver disease.
This list is not exhaustive, and it is crucial to discuss all your medications (including prescription, over-the-counter, natural products, and vitamins) and health conditions with your doctor and pharmacist. They will help determine if it is safe to take this medication in conjunction with your other treatments and health issues.
Remember, do not start, stop, or adjust the dosage of any medication without first consulting your doctor to ensure your safety.
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.
If you have a history of kidney disease or liver disease.
This list is not exhaustive, and it is crucial to discuss all your medications (including prescription, over-the-counter, natural products, and vitamins) and health conditions with your doctor and pharmacist. They will help determine if it is safe to take this medication in conjunction with your other treatments and health issues.
Remember, do not start, stop, or adjust the dosage of any medication without first consulting your doctor to ensure your safety.
Precautions & Cautions
It is essential to inform all of your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
While taking this drug, you may experience weight loss, and regular weight checks will be necessary to monitor this potential side effect. Be sure to discuss any concerns or questions you have about weight loss with your doctor.
If you are pregnant, planning to become pregnant, or are currently breast-feeding, it is crucial to notify your doctor. Your doctor will need to discuss the potential benefits and risks of this medication to both you and your baby, allowing you to make an informed decision about treatment.
While taking this drug, you may experience weight loss, and regular weight checks will be necessary to monitor this potential side effect. Be sure to discuss any concerns or questions you have about weight loss with your doctor.
If you are pregnant, planning to become pregnant, or are currently breast-feeding, it is crucial to notify your doctor. Your doctor will need to discuss the potential benefits and risks of this medication to both you and your baby, allowing you to make an informed decision about treatment.
Overdose Information
Overdose Symptoms:
- Severe nausea, vomiting, and diarrhea
- Excessive sweating
- Salivation (drooling)
- Bradycardia (slow heart rate)
- Hypotension (low blood pressure)
- Collapse
- Muscle weakness or fasciculations (twitching)
- Seizures
- Severe muscle cramps
- Respiratory depression (slow, shallow breathing)
- Miosis (pinpoint pupils)
What to Do:
Seek immediate medical attention. Call 911 or Poison Control (1-800-222-1222). Treatment is supportive and may include atropine for severe cholinergic symptoms.
Drug Interactions
Major Interactions
- Strong CYP2D6 inhibitors (e.g., paroxetine, fluoxetine, quinidine): May increase galantamine exposure, increasing risk of cholinergic side effects. Consider dose reduction of galantamine.
- Strong CYP3A4 inhibitors (e.g., ketoconazole, ritonavir, erythromycin): May increase galantamine exposure, increasing risk of cholinergic side effects. Consider dose reduction of galantamine.
- Other cholinesterase inhibitors (e.g., donepezil, rivastigmine): Additive cholinergic effects, increased risk of adverse events (e.g., bradycardia, syncope, GI upset). Avoid concomitant use.
- Succinylcholine and other neuromuscular blocking agents: Galantamine may exaggerate neuromuscular blockade.
Moderate Interactions
- Beta-blockers (especially those that cause bradycardia): Increased risk of bradycardia and syncope.
- Drugs that prolong the QT interval: Theoretical increased risk of QT prolongation, though not a primary effect of galantamine.
- Anticholinergic agents (e.g., atropine, benztropine, tricyclic antidepressants): Antagonistic effects, may reduce efficacy of both drugs.
Monitoring
Baseline Monitoring
Cognitive function assessment (e.g., MMSE, ADAS-Cog)
Rationale: To establish baseline cognitive status and monitor treatment efficacy.
Timing: Prior to initiation of therapy
Heart rate and blood pressure
Rationale: Galantamine can cause bradycardia and syncope.
Timing: Prior to initiation of therapy
Liver function tests (ALT, AST, bilirubin)
Rationale: To assess baseline hepatic function, especially in patients with suspected impairment.
Timing: Prior to initiation of therapy
Renal function (CrCl)
Rationale: To guide initial dosing and dose adjustments in patients with renal 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 may indicate need for 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: Within normal limits for the patient
Action Threshold: Bradycardia (<50 bpm), symptomatic hypotension, or syncope requires immediate evaluation and potential dose reduction/discontinuation.
Gastrointestinal symptoms (nausea, vomiting, diarrhea)
Frequency: Regularly, especially during dose titration
Target: Minimal to no symptoms
Action Threshold: Persistent or severe symptoms may require dose reduction or discontinuation.
Weight
Frequency: Periodically
Target: Stable
Action Threshold: Significant weight loss may indicate inadequate caloric intake due to GI side effects.
Symptom Monitoring
- Nausea
- Vomiting
- Diarrhea
- Anorexia
- Weight loss
- Bradycardia
- Syncope
- Dizziness
- Headache
- Insomnia
- Muscle cramps
- Urinary incontinence
Special Patient Groups
Pregnancy
Galantamine 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 adverse effects on fetal development, though human data are limited.
Second Trimester:
Potential for adverse effects on fetal development, though human data are limited.
Third Trimester:
Potential for adverse effects on fetal development, though human data are limited. Cholinesterase inhibitors may cause uterine irritability and premature labor.
Lactation
Galantamine is excreted in the milk of rats. It is unknown if galantamine 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:
L3 (Moderate risk) - Potential for cholinergic effects in the infant (e.g., bradycardia, GI upset).
Pediatric Use
Safety and effectiveness in pediatric patients have not been established. Galantamine is not indicated for use in children.
Geriatric Use
Galantamine is primarily used in the geriatric population for Alzheimer's disease. No specific dose adjustment is required based solely on age, but dose adjustments are necessary for renal and hepatic impairment, which are more common in the elderly. Elderly patients may be more susceptible to cholinergic side effects (e.g., bradycardia, syncope, GI upset).
Clinical Information
Clinical Pearls
- Galantamine should be taken with food to minimize gastrointestinal side effects, which are common, especially during dose titration.
- Titration is crucial to improve tolerability and reduce the incidence of adverse events. Do not rush dose increases.
- Monitor for signs of bradycardia and syncope, particularly in patients with pre-existing cardiac conditions or those taking other medications that slow heart rate.
- Patients should be advised to report any significant weight loss, as this can be a concern with cholinesterase inhibitors.
- If treatment is interrupted for several days or more, re-initiate at the lowest dose and re-titrate to the therapeutic dose to avoid severe adverse effects.
- Galantamine is available as an oral solution, immediate-release tablets, and extended-release capsules, offering flexibility in administration.
Alternative Therapies
- Donepezil (Aricept) - another acetylcholinesterase inhibitor
- Rivastigmine (Exelon) - another acetylcholinesterase inhibitor (oral and transdermal patch)
- Memantine (Namenda) - an NMDA receptor antagonist (often used in moderate to severe Alzheimer's, or in combination with cholinesterase inhibitors)
Cost & Coverage
Average Cost:
Varies widely, typically $100-$300 per 100 mL (4mg/mL)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or 2 (generic), Tier 3 or 4 (brand) for most commercial and Medicare Part D plans.
General Drug Facts
If your symptoms or health issues persist or worsen, it is 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 it's a good idea to check with your pharmacist. If you have any questions or concerns about this medication, don't hesitate to discuss them with 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 information about the medication taken, the amount, and the time it happened.