Megestrol 625mg/5ml Suspension
It is used to help raise feelings of hunger.It is used to treat endometrial or breast cancer.It may be given to you for other reasons. Talk with the doctor.
Drug Class
Antineoplastic Agent; Appetite Stimulant
Pharmacologic Class
Progestin
Pregnancy Category
Category X
FDA Approved
Jan 1970
DEA Schedule
Not Controlled
Overview
What is this medicine?
Megestrol is a man-made hormone similar to progesterone. It is used to help people with certain medical conditions, like AIDS, gain weight and improve their appetite. It can also be used in some cancers.
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. Continue taking your medication as directed by your doctor or healthcare provider, even if you start to feel better.
Before using your medication, shake the bottle well. If you are taking a liquid dose, measure it carefully using the measuring device that comes with the medication. If no device is provided, ask your pharmacist for a suitable measuring tool. It's essential to ensure you have the correct strength of the liquid medication, as there may be multiple strengths available.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, away from heat. Avoid storing it in a bathroom. By following these storage instructions, you can help maintain the effectiveness of your medication.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for a missed dose.
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.
Before using your medication, shake the bottle well. If you are taking a liquid dose, measure it carefully using the measuring device that comes with the medication. If no device is provided, ask your pharmacist for a suitable measuring tool. It's essential to ensure you have the correct strength of the liquid medication, as there may be multiple strengths available.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, away from heat. Avoid storing it in a bathroom. By following these storage instructions, you can help maintain the effectiveness of your medication.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for a missed dose.
Lifestyle & Tips
- Take exactly as prescribed, usually once a day.
- Shake the oral suspension well before each use.
- Can be taken with or without food, but taking it with food may help with absorption.
- Do not stop taking this medication suddenly without talking to your doctor, especially if you have been on it for a long time, as it can affect your body's natural hormones.
- Monitor your weight regularly as advised by your doctor.
- If you have diabetes, monitor your blood sugar closely as this medication can increase blood sugar levels.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
625 mg (5 mL) once daily
Dose Range:
625 - 625 mg
Condition-Specific Dosing:
anorexia_cachexia_aids:
625 mg (5 mL) once daily
advanced_breast_carcinoma:
40 mg four times daily (tablet formulation, not this suspension)
advanced_endometrial_carcinoma:
40-320 mg/day in divided doses (tablet formulation, not this suspension)
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment recommended, use with caution.
Moderate:
No specific dose adjustment recommended, use with caution.
Severe:
Use with caution; monitor for adverse effects due to potential accumulation. Data limited.
Dialysis:
Not available; caution advised due to potential for accumulation.
Hepatic Impairment:
Mild:
No specific dose adjustment recommended, use with caution.
Moderate:
No specific dose adjustment recommended, use with caution.
Severe:
Use with caution; monitor for adverse effects due to potential accumulation. Data limited.
Pharmacology
Mechanism of Action
Megestrol acetate is a synthetic progestin. Its exact mechanism of action in producing weight gain and appetite stimulation in cachexia is not fully understood but is thought to involve modulation of cytokine production (e.g., TNF-alpha, IL-1, IL-6) and/or direct effects on appetite centers in the hypothalamus. In cancer, it exerts antineoplastic effects through anti-estrogenic and anti-luteinizing hormone activity, possibly by altering hormone receptor status or directly inhibiting tumor growth.
Pharmacokinetics
Absorption:
Bioavailability:
Increased with food; the micronized suspension (625mg/5ml) has enhanced bioavailability compared to conventional tablets.
Tmax:
2-5 hours
FoodEffect:
Food increases the extent of absorption.
Distribution:
Vd:
Approximately 20 L
ProteinBinding:
Approximately 90% (primarily to albumin)
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 20-50 hours (highly variable)
Clearance:
Not precisely quantified, primarily renal excretion.
ExcretionRoute:
Urine (57-78%), Feces (8-30%)
Unchanged:
Approximately 5-8% (renal)
Pharmacodynamics
OnsetOfAction:
Appetite stimulation may be observed within a few weeks.
PeakEffect:
Weight gain typically peaks after several weeks to months of therapy.
DurationOfAction:
Effects persist as long as therapy is continued.
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction: rash, hives, itching, red, swollen, blistered, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, difficulty breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
Signs of high blood sugar: confusion, drowsiness, unusual thirst or hunger, frequent urination, flushing, rapid breathing, or fruity-smelling breath.
Signs of Cushing's syndrome: weight gain in the upper back or abdomen, moon face, severe headache, or slow wound healing.
Signs of adrenal insufficiency: severe nausea or vomiting, severe dizziness or fainting, muscle weakness, extreme fatigue, mood changes, decreased appetite, or weight loss.
Signs of high blood pressure: severe headache or dizziness, fainting, or changes in vision.
Shortness of breath, significant weight gain, or swelling in the arms or legs.
Abnormal vaginal bleeding.
Mood changes.
Decreased libido.
Erectile dysfunction.
Fever.
Pain or numbness in the hands or wrists.
Tumor flare reaction: increased pain or tenderness at the tumor site, hot flashes, or other symptoms. Notify your doctor immediately if you experience any of these symptoms.
Blood clots: although rare, blood clots can be life-threatening. Seek medical help right away if you experience chest, arm, back, neck, or jaw pain or pressure; coughing up blood; numbness or weakness on one side of the body; difficulty speaking or thinking; changes in balance or vision; shortness of breath; or swelling, warmth, or pain in the leg or arm.
Other Possible Side Effects
As with any medication, you may experience side effects. While many people have no side effects or only mild ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects, contact your doctor or seek medical help if they bother you or persist:
Nausea or vomiting.
Headache.
Increased appetite.
Weight gain.
Insomnia.
Gas.
Fatigue or weakness.
Hair loss.
Hot flashes.
Excessive sweating.
* Diarrhea.
This is not an exhaustive list of possible side effects. If you have questions or concerns, consult 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, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction: rash, hives, itching, red, swollen, blistered, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, difficulty breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
Signs of high blood sugar: confusion, drowsiness, unusual thirst or hunger, frequent urination, flushing, rapid breathing, or fruity-smelling breath.
Signs of Cushing's syndrome: weight gain in the upper back or abdomen, moon face, severe headache, or slow wound healing.
Signs of adrenal insufficiency: severe nausea or vomiting, severe dizziness or fainting, muscle weakness, extreme fatigue, mood changes, decreased appetite, or weight loss.
Signs of high blood pressure: severe headache or dizziness, fainting, or changes in vision.
Shortness of breath, significant weight gain, or swelling in the arms or legs.
Abnormal vaginal bleeding.
Mood changes.
Decreased libido.
Erectile dysfunction.
Fever.
Pain or numbness in the hands or wrists.
Tumor flare reaction: increased pain or tenderness at the tumor site, hot flashes, or other symptoms. Notify your doctor immediately if you experience any of these symptoms.
Blood clots: although rare, blood clots can be life-threatening. Seek medical help right away if you experience chest, arm, back, neck, or jaw pain or pressure; coughing up blood; numbness or weakness on one side of the body; difficulty speaking or thinking; changes in balance or vision; shortness of breath; or swelling, warmth, or pain in the leg or arm.
Other Possible Side Effects
As with any medication, you may experience side effects. While many people have no side effects or only mild ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects, contact your doctor or seek medical help if they bother you or persist:
Nausea or vomiting.
Headache.
Increased appetite.
Weight gain.
Insomnia.
Gas.
Fatigue or weakness.
Hair loss.
Hot flashes.
Excessive sweating.
* Diarrhea.
This is not an exhaustive list of possible side effects. If you have questions or concerns, consult 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:
- Signs of a blood clot: sudden severe headache, sudden vision changes, sudden numbness or weakness on one side of the body, chest pain, shortness of breath, pain or swelling in an arm or leg.
- Signs of high blood sugar: increased thirst, increased urination, confusion, fruity breath odor.
- Signs of adrenal problems: severe tiredness, weakness, dizziness, nausea, vomiting, loss of appetite.
- Unusual vaginal bleeding (in females).
- Any new or worsening side effects.
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:
If you have a known allergy to megestrol acetate or any component of this medication. Describe the allergic reaction and its symptoms.
If you are taking dofetilide.
If you are pregnant or think you might be pregnant. Note that this medication should not be used to stimulate appetite during pregnancy.
If you are breastfeeding. You should not breastfeed while taking this medication.
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 issues with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health conditions. Never start, stop, or adjust the dose of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
If you have a known allergy to megestrol acetate or any component of this medication. Describe the allergic reaction and its symptoms.
If you are taking dofetilide.
If you are pregnant or think you might be pregnant. Note that this medication should not be used to stimulate appetite during pregnancy.
If you are breastfeeding. You should not breastfeed while taking this medication.
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 issues with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health conditions. Never start, stop, or adjust the dose of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Regular blood tests will be necessary, as directed by your doctor, to monitor your condition. Be sure to discuss any concerns or questions with your doctor.
One potential side effect of this medication is the development of high blood sugar, which may lead to new-onset diabetes or worsen existing diabetes. To manage this risk, it is crucial to check your blood sugar levels as instructed by your doctor.
This medication may also affect your body's natural production of steroids. If you experience a severe infection, undergo surgery, or suffer an injury, notify your doctor promptly. Additionally, if you experience severe dizziness, fainting, persistent nausea and vomiting, or extreme fatigue and weakness, seek medical attention immediately, as you may require steroid replacement therapy. Consult with your doctor to discuss the best course of action.
Women of childbearing age should be aware that this medication may harm an unborn baby if taken during pregnancy. To confirm that you are not pregnant before starting treatment, your doctor may require a pregnancy test. It is vital to use a reliable form of birth control to prevent pregnancy while taking this medication. If you become pregnant or suspect you may be pregnant while taking this medication, contact your doctor immediately.
One potential side effect of this medication is the development of high blood sugar, which may lead to new-onset diabetes or worsen existing diabetes. To manage this risk, it is crucial to check your blood sugar levels as instructed by your doctor.
This medication may also affect your body's natural production of steroids. If you experience a severe infection, undergo surgery, or suffer an injury, notify your doctor promptly. Additionally, if you experience severe dizziness, fainting, persistent nausea and vomiting, or extreme fatigue and weakness, seek medical attention immediately, as you may require steroid replacement therapy. Consult with your doctor to discuss the best course of action.
Women of childbearing age should be aware that this medication may harm an unborn baby if taken during pregnancy. To confirm that you are not pregnant before starting treatment, your doctor may require a pregnancy test. It is vital to use a reliable form of birth control to prevent pregnancy while taking this medication. If you become pregnant or suspect you may be pregnant while taking this medication, contact your doctor immediately.
Overdose Information
Overdose Symptoms:
- Nausea
- Vomiting
- Diarrhea
- Shortness of breath
- Cough
- Heart palpitations
What to Do:
Seek immediate medical attention or call a poison control center (1-800-222-1222). Treatment is generally supportive.
Drug Interactions
Contraindicated Interactions
- Indinavir (decreases indinavir plasma concentrations, potentially leading to loss of virologic response and resistance)
Major Interactions
- Warfarin (may alter INR, requiring close monitoring and dose adjustment of warfarin)
- Other hormonal agents (e.g., corticosteroids, other progestins, estrogens - potential for additive effects or altered efficacy)
Moderate Interactions
- Drugs metabolized by CYP3A4 (theoretical interaction, but megestrol is not a strong inducer or inhibitor)
- Insulin and oral hypoglycemics (may increase blood glucose, requiring dose adjustment of antidiabetic agents)
Monitoring
Baseline Monitoring
Weight
Rationale: To establish baseline for monitoring efficacy.
Timing: Prior to initiation of therapy.
Blood Glucose
Rationale: Megestrol can cause hyperglycemia, especially in patients with diabetes or pre-diabetes.
Timing: Prior to initiation of therapy, particularly in diabetic patients.
Adrenal Function (e.g., morning cortisol)
Rationale: Prolonged use of megestrol, especially at high doses, can cause adrenal suppression.
Timing: Consider for patients on long-term therapy or with pre-existing adrenal insufficiency.
INR (if on warfarin)
Rationale: Megestrol can alter warfarin effects.
Timing: Prior to initiation of therapy.
Routine Monitoring
Weight
Frequency: Weekly to bi-weekly initially, then monthly.
Target: Desired weight gain.
Action Threshold: Lack of weight gain or excessive weight gain may require re-evaluation.
Blood Glucose
Frequency: Periodically, more frequently in diabetic patients (e.g., weekly to monthly).
Target: Individualized glycemic targets.
Action Threshold: Persistent hyperglycemia requiring adjustment of antidiabetic medications.
Signs/Symptoms of Thromboembolism
Frequency: Regularly throughout therapy.
Target: Absence of symptoms.
Action Threshold: Development of DVT/PE symptoms (e.g., leg pain/swelling, chest pain, shortness of breath) requires immediate medical attention.
Adrenal Function
Frequency: Consider periodically for long-term high-dose therapy (e.g., every 3-6 months).
Target: Normal cortisol levels.
Action Threshold: Evidence of adrenal suppression may require dose tapering or corticosteroid replacement.
INR (if on warfarin)
Frequency: More frequently (e.g., 2-3 times per week) after initiation or dose change, then as clinically indicated.
Target: Therapeutic INR range.
Action Threshold: INR outside target range requires warfarin dose adjustment.
Symptom Monitoring
- Appetite changes
- Fluid retention (edema)
- Nausea/vomiting
- Diarrhea
- Rash
- Hot flashes
- Vaginal bleeding (in females)
- Impotence (in males)
- Signs of deep vein thrombosis (DVT) or pulmonary embolism (PE) - e.g., leg pain/swelling, chest pain, shortness of breath
- Signs of hyperglycemia - e.g., increased thirst, increased urination, fatigue
Special Patient Groups
Pregnancy
Contraindicated in pregnancy (Category X). Megestrol acetate may cause fetal harm when administered to a pregnant woman. There is evidence of teratogenicity in animals.
Trimester-Specific Risks:
First Trimester:
High risk of fetal abnormalities.
Second Trimester:
High risk of fetal abnormalities and adverse effects on fetal development.
Third Trimester:
High risk of fetal abnormalities and adverse effects on fetal development.
Lactation
Not recommended during breastfeeding. Megestrol acetate is excreted in human milk. Due to the potential for serious adverse reactions in the nursing infant, 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:
L4 (Possibly Hazardous) - Potential for adverse effects on infant, including hormonal disruption.
Pediatric Use
Safety and effectiveness have not been established in pediatric patients. Use is generally not recommended.
Geriatric Use
Use with caution in elderly patients, as they may be more susceptible to adverse effects, particularly thromboembolic events, hyperglycemia, and fluid retention. Start at the lower end of the dosing range and monitor closely.
Clinical Information
Clinical Pearls
- Megestrol acetate often causes significant weight gain, but this is primarily fat mass, not lean body mass.
- Patients should be monitored for signs and symptoms of thromboembolic events (e.g., DVT, PE), especially those with a history of such events or other risk factors.
- Adrenal suppression can occur with prolonged high-dose use; consider tapering the dose if discontinuing after long-term therapy.
- Monitor blood glucose levels, particularly in diabetic patients, as megestrol can exacerbate hyperglycemia.
- The 625mg/5ml suspension is a high-concentration formulation specifically designed for enhanced absorption and is typically used for anorexia/cachexia, not for cancer indications where lower dose tablets are used.
Alternative Therapies
- Dronabinol (for appetite stimulation in AIDS-related anorexia)
- Corticosteroids (e.g., dexamethasone, prednisone - short-term use for appetite stimulation, but with significant side effects)
- Mirtazapine (antidepressant with appetite-stimulating side effect)
- Ghrelin receptor agonists (e.g., anamorelin - for cancer cachexia, not yet widely available/approved in all regions)
Cost & Coverage
Average Cost:
Varies widely, typically $500 - $1500+ per 240 mL bottle (625 mg/5 mL)
Generic Available:
Yes
Insurance Coverage:
Tier 2 or 3 (for generic), Tier 3 or 4 (for brand)
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 your 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 seeking help, be prepared to provide details about the medication taken, the amount, and the time it occurred.