Coartem 20-120mg Tablets
It is used to treat malaria.
Drug Class
Antimalarial
Pharmacologic Class
Artemisinin derivative (Artemether); Arylaminoalcohol (Lumefantrine)
Pregnancy Category
Category C
FDA Approved
Apr 2009
DEA Schedule
Not Controlled
Overview
What is this medicine?
Coartem is a medicine used to treat malaria, a serious disease caused by parasites spread by mosquitoes. It contains two different drugs, artemether and lumefantrine, that work together to kill the malaria parasites in your blood. It's very important to take this medicine exactly as prescribed, especially with food, to make sure it works properly.
How to Use This Medicine
Taking Your Medication
To take this medication correctly, follow your doctor's instructions and read all the information provided. Take this medication with food as directed by your healthcare provider. Continue taking the medication as prescribed, even if you start to feel better.
If you need to, you can crush the tablet and mix it with 1 or 2 teaspoons (5 or 10 mL) of water. If you mix the medication with water, swallow it immediately and do not store it for later use. Rinse the cup with more water and drink it to ensure you get the full dose.
If you vomit within 2 hours of taking the medication, you may need to take an additional dose. Contact your doctor right away for guidance. If you vomit again after taking the second dose, call your doctor for further instructions.
If you are unable to eat when taking this medication, consult with your doctor for advice.
Storing and Disposing of Your Medication
Store the tablets in their original container at room temperature, keeping the cap tightly closed. Keep the container in a dry place, away from the bathroom. Ensure that all medications are kept in a safe location, out of the reach of children and pets.
Missing a Dose
If you miss a dose, take it as soon as you remember. However, if it is 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 take this medication correctly, follow your doctor's instructions and read all the information provided. Take this medication with food as directed by your healthcare provider. Continue taking the medication as prescribed, even if you start to feel better.
If you need to, you can crush the tablet and mix it with 1 or 2 teaspoons (5 or 10 mL) of water. If you mix the medication with water, swallow it immediately and do not store it for later use. Rinse the cup with more water and drink it to ensure you get the full dose.
If you vomit within 2 hours of taking the medication, you may need to take an additional dose. Contact your doctor right away for guidance. If you vomit again after taking the second dose, call your doctor for further instructions.
If you are unable to eat when taking this medication, consult with your doctor for advice.
Storing and Disposing of Your Medication
Store the tablets in their original container at room temperature, keeping the cap tightly closed. Keep the container in a dry place, away from the bathroom. Ensure that all medications are kept in a safe location, out of the reach of children and pets.
Missing a Dose
If you miss a dose, take it as soon as you remember. However, if it is 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.
Lifestyle & Tips
- Always take Coartem with food or milk. Fatty foods (e.g., peanut butter, whole milk, cheese) are best to help your body absorb the medicine. If you cannot eat, take it with water.
- Complete the entire 3-day course of treatment, even if you start feeling better. Stopping early can lead to the malaria coming back or becoming resistant to the medicine.
- If you vomit within 1-2 hours after taking a dose, take another full dose as soon as possible.
- Avoid grapefruit juice during treatment as it may affect how the medicine works.
- Use reliable birth control methods if you are taking hormonal contraceptives, as Coartem may make them less effective.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
4 tablets (80 mg artemether/480 mg lumefantrine) orally as an initial dose, then 4 tablets again after 8 hours, and then 4 tablets twice daily for the next 2 days (total 6 doses over 3 days).
Condition-Specific Dosing:
uncomplicated_P_falciparum_malaria:
Administer with food or milk. If vomiting occurs within 1-2 hours of a dose, a repeat dose should be taken.
Pediatric Dosing
Neonatal:
Not established (limited data for infants <5 kg or <3 months old).
Infant:
Weight-based dosing for infants âĨ5 kg.
Child:
Weight-based dosing for children.
Adolescent:
Weight-based dosing for adolescents, typically same as adult for âĨ35 kg.
Weight_based_dosing:
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment recommended.
Moderate:
No dose adjustment recommended.
Severe:
Use with caution; not studied in severe renal impairment. Monitor for adverse effects.
Dialysis:
Not available; use with caution.
Hepatic Impairment:
Mild:
No dose adjustment recommended.
Moderate:
No dose adjustment recommended.
Severe:
Use with caution; not studied in severe hepatic impairment. Monitor for adverse effects.
Confidence:
Medium
Pharmacology
Mechanism of Action
Artemether and lumefantrine are blood schizonticides. Artemether, an artemisinin derivative, is rapidly metabolized to dihydroartemisinin (DHA), which is thought to produce reactive oxygen species and inhibit parasite protein synthesis, leading to rapid parasite clearance. Lumefantrine, an arylaminoalcohol, is thought to interfere with the detoxification of heme, a byproduct of hemoglobin digestion by the parasite, by inhibiting the formation of hemozoin. This leads to accumulation of toxic heme, causing parasite death. The combination provides synergistic activity, rapid parasite clearance, and reduces the risk of resistance development.
Pharmacokinetics
Absorption:
Bioavailability:
Artemether: Low (variable, increased by food). Lumefantrine: Low (variable, significantly increased by food).
Tmax:
Artemether: ~2 hours. Lumefantrine: ~6-8 hours.
FoodEffect:
Crucial for lumefantrine absorption; bioavailability increases significantly (up to 16-fold) when taken with fatty food or milk. Artemether absorption also increased by food.
Distribution:
Vd:
Artemether: ~1-2 L/kg. Lumefantrine: ~5-10 L/kg (extensive tissue distribution).
ProteinBinding:
Artemether: >95%. Lumefantrine: >99%.
CnssPenetration:
Limited
Elimination:
HalfLife:
Artemether: ~2-3 hours. Dihydroartemisinin (DHA): ~2-4 hours. Lumefantrine: ~3-6 days (90-120 hours).
Clearance:
Not available (complex due to metabolism and distribution).
ExcretionRoute:
Fecal (primary for lumefantrine); Renal (minor for both).
Unchanged:
Artemether: <1%. Lumefantrine: <1%.
Pharmacodynamics
OnsetOfAction:
Rapid (due to artemether component, within hours)
PeakEffect:
Not precisely defined for antimalarial effect, but parasite clearance typically begins within 24-48 hours.
DurationOfAction:
Prolonged (due to long half-life of lumefantrine, providing sustained antimalarial activity and preventing recrudescence).
Confidence:
High
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
Abnormal heartbeat (prolonged QT interval), which may cause:
+ Fast heartbeat
+ Irregular heartbeat
+ Fainting (passing out)
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 unusual symptoms, contact your doctor or seek medical help:
Headache
Dizziness, tiredness, or weakness
Fever or chills
Upset stomach or vomiting
Stomach pain or diarrhea
Decreased appetite
Muscle or joint pain
Trouble sleeping
* Cough
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, contact your doctor for medical advice. 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 heartbeat (prolonged QT interval), which may cause:
+ Fast heartbeat
+ Irregular heartbeat
+ Fainting (passing out)
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 unusual symptoms, contact your doctor or seek medical help:
Headache
Dizziness, tiredness, or weakness
Fever or chills
Upset stomach or vomiting
Stomach pain or diarrhea
Decreased appetite
Muscle or joint pain
Trouble sleeping
* Cough
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, contact your doctor for medical advice. 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 severe allergic reaction (e.g., rash, itching, swelling of face/tongue/throat, severe dizziness, trouble breathing).
- New or worsening heart problems (e.g., fast/irregular heartbeat, severe dizziness, fainting).
- Signs of liver problems (e.g., yellowing of skin/eyes, dark urine, severe stomach pain, persistent nausea/vomiting).
- Persistent or worsening malaria symptoms after 3 days of treatment (e.g., fever, chills, headache, body aches).
- Severe or persistent nausea, vomiting, or diarrhea.
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. Describe the allergic reaction you experienced, including the symptoms that occurred.
Certain health conditions, including:
+ Low levels of potassium or magnesium in your blood.
+ A history of abnormal heart rhythms, such as a prolonged QT interval on an electrocardiogram (ECG).
+ A family history of sudden, unexplained death or a prolonged QT interval on an ECG.
+ Heart problems, including a recent heart attack.
Medications you are currently taking, including:
+ Amitriptyline, carbamazepine, clomipramine, flecainide, imipramine, phenytoin, rifampin, or St. John's wort.
+ Any medications that can cause abnormal heart rhythms (prolonged QT interval). There are many medications that can have this effect, so be sure to ask your doctor or pharmacist if you are unsure.
+ Halofantrine, if you have taken it within the past month.
All your medications, including prescription and over-the-counter drugs, natural products, and vitamins. This is not an exhaustive list, and it is crucial to discuss all your medications and health conditions with your doctor to ensure safe use.
Remember to consult your doctor before starting, stopping, or changing the dose of any medication. Your doctor and pharmacist need to know about all your medications and health conditions to determine if it is safe for you to take 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. Describe the allergic reaction you experienced, including the symptoms that occurred.
Certain health conditions, including:
+ Low levels of potassium or magnesium in your blood.
+ A history of abnormal heart rhythms, such as a prolonged QT interval on an electrocardiogram (ECG).
+ A family history of sudden, unexplained death or a prolonged QT interval on an ECG.
+ Heart problems, including a recent heart attack.
Medications you are currently taking, including:
+ Amitriptyline, carbamazepine, clomipramine, flecainide, imipramine, phenytoin, rifampin, or St. John's wort.
+ Any medications that can cause abnormal heart rhythms (prolonged QT interval). There are many medications that can have this effect, so be sure to ask your doctor or pharmacist if you are unsure.
+ Halofantrine, if you have taken it within the past month.
All your medications, including prescription and over-the-counter drugs, natural products, and vitamins. This is not an exhaustive list, and it is crucial to discuss all your medications and health conditions with your doctor to ensure safe use.
Remember to consult your doctor before starting, stopping, or changing the dose of any medication. Your doctor and pharmacist need to know about all your medications and health conditions to determine if it is safe for you to take 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. Before starting and during treatment with this drug, your doctor may require you to undergo an electrocardiogram (ECG) to monitor your heart activity.
To avoid potential interactions, do not consume grapefruit or grapefruit juice while taking this medication. Additionally, if you are using birth control pills or other hormone-based birth control methods, be aware that this drug may reduce their effectiveness in preventing pregnancy. As a precaution, consider using a supplementary form of birth control, such as condoms, to minimize the risk of unplanned pregnancy.
If you are pregnant, planning to become pregnant, or are breast-feeding, it is crucial to discuss the potential benefits and risks of this medication with your doctor. This will help you make an informed decision about your treatment and ensure the best possible outcome for both you and your baby.
To avoid potential interactions, do not consume grapefruit or grapefruit juice while taking this medication. Additionally, if you are using birth control pills or other hormone-based birth control methods, be aware that this drug may reduce their effectiveness in preventing pregnancy. As a precaution, consider using a supplementary form of birth control, such as condoms, to minimize the risk of unplanned pregnancy.
If you are pregnant, planning to become pregnant, or are breast-feeding, it is crucial to discuss the potential benefits and risks of this medication with your doctor. This will help you make an informed decision about your treatment and ensure the best possible outcome for both you and your baby.
Overdose Information
Overdose Symptoms:
- QT interval prolongation (may lead to irregular heartbeats, fainting)
- Gastrointestinal disturbances (nausea, vomiting, diarrhea)
- Dizziness
- Headache
- Fatigue
What to Do:
Seek immediate medical attention. There is no specific antidote. Treatment is symptomatic and supportive, including ECG monitoring and correction of electrolyte imbalances. Call 1-800-222-1222 (Poison Control Center) for advice.
Drug Interactions
Contraindicated Interactions
- Strong CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin, St. John's Wort) - may significantly decrease lumefantrine concentrations, leading to loss of efficacy.
- Drugs known to prolong the QT interval (e.g., Class IA and III antiarrhythmics, some antipsychotics, tricyclic antidepressants, macrolide antibiotics, fluoroquinolone antibiotics) - additive QT prolongation risk.
- Concurrent use with other artemisinin derivatives (unless part of a fixed-dose combination).
Major Interactions
- Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, ritonavir, clarithromycin) - may increase artemether and lumefantrine concentrations, increasing risk of adverse effects including QT prolongation.
- Mefloquine - administer Coartem after mefloquine (at least 12 hours later) to avoid potential for additive cardiotoxicity.
- HIV protease inhibitors (e.g., ritonavir, saquinavir) and non-nucleoside reverse transcriptase inhibitors (NNRTIs) (e.g., efavirenz, nevirapine) - complex interactions due to CYP3A4 induction/inhibition; requires careful monitoring.
- Drugs that lower potassium or magnesium levels (e.g., loop diuretics) - increased risk of QT prolongation.
Moderate Interactions
- Oral contraceptives - lumefantrine may reduce efficacy of hormonal contraceptives; advise alternative contraception.
- Grapefruit juice - may inhibit CYP3A4, potentially increasing drug levels.
- Warfarin - potential for altered INR; monitor closely.
Minor Interactions
- Not available
Monitoring
Baseline Monitoring
Electrocardiogram (ECG) with QTc interval
Rationale: To assess baseline cardiac conduction and identify patients at higher risk for QT prolongation.
Timing: Prior to initiation, especially in patients with pre-existing cardiac conditions or on other QT-prolonging drugs.
Serum electrolytes (Potassium, Magnesium)
Rationale: Hypokalemia or hypomagnesemia can increase the risk of QT prolongation.
Timing: Prior to initiation, especially in patients at risk for electrolyte imbalances.
Routine Monitoring
Clinical response (fever, parasitemia)
Frequency: Daily during treatment, then follow-up for 28-42 days post-treatment.
Target: Resolution of fever, negative blood smear for parasites.
Action Threshold: Persistent fever or parasitemia after 3 days of treatment may indicate treatment failure or resistance; consider alternative therapy.
Adverse effects (e.g., GI upset, headache, dizziness, rash)
Frequency: Daily during treatment and at follow-up visits.
Target: Absence or mild, tolerable symptoms.
Action Threshold: Severe or persistent adverse effects warrant evaluation and potential discontinuation.
Symptom Monitoring
- Fever
- Chills
- Headache
- Muscle aches
- Nausea
- Vomiting
- Diarrhea
- Dizziness
- Fatigue
- Rash
- Signs of allergic reaction (e.g., swelling, difficulty breathing)
- Signs of cardiac issues (e.g., palpitations, chest pain, fainting)
Special Patient Groups
Pregnancy
Coartem is generally recommended by WHO as a preferred treatment for uncomplicated P. falciparum malaria in the second and third trimesters of pregnancy. Use in the first trimester is generally reserved for situations where other effective treatments are not available or are not tolerated, due to limited data and theoretical risks, though recent data suggest it may be safer than previously thought.
Trimester-Specific Risks:
First Trimester:
Limited data; theoretical risk of embryotoxicity. Use only if potential benefit justifies potential risk.
Second Trimester:
Generally considered safe and effective; preferred treatment.
Third Trimester:
Generally considered safe and effective; preferred treatment.
Lactation
Lumefantrine is excreted into breast milk. While the amount transferred to the infant is generally low, monitor breastfed infants for potential adverse effects (e.g., diarrhea, vomiting, rash). The benefits of breastfeeding should be weighed against the potential risks to the infant and the mother's clinical need for the drug. WHO generally considers it compatible with breastfeeding.
Infant Risk:
Low to Moderate (due to lumefantrine excretion and long half-life, but generally well-tolerated by infants).
Pediatric Use
Coartem is approved for use in pediatric patients weighing 5 kg and above. Dosing is weight-based. Ensure accurate weight measurement for correct dosing. Administer with food or milk. If vomiting occurs, repeat the dose.
Geriatric Use
No specific dose adjustments are recommended for elderly patients. However, elderly patients may have reduced hepatic or renal function or concomitant diseases/medications, which could increase the risk of adverse effects or drug interactions. Monitor closely for adverse reactions and drug interactions.
Clinical Information
Clinical Pearls
- The most critical instruction for patients is to take Coartem with food or milk, especially fatty food, to ensure adequate absorption of lumefantrine. Without food, absorption is significantly reduced, leading to treatment failure.
- Emphasize completing the full 3-day, 6-dose course, even if symptoms improve quickly, to prevent recrudescence and development of drug resistance.
- Coartem is effective against uncomplicated P. falciparum malaria, including multi-drug resistant strains, but resistance is an emerging concern in some regions.
- Monitor for QT prolongation, especially in patients with pre-existing cardiac conditions, electrolyte imbalances, or those on other QT-prolonging medications.
- Advise patients on hormonal contraception to use an alternative method during and for at least one cycle after Coartem treatment due to potential reduced efficacy.
Alternative Therapies
- Quinine (with doxycycline or clindamycin)
- Atovaquone-proguanil (Malarone)
- Mefloquine
- Chloroquine (where susceptible)
Cost & Coverage
Average Cost:
Varies, typically $100-$200 per 24 tablets (one full course)
Generic Available:
Yes
Insurance Coverage:
Tier 2 or 3 (preferred brand or non-preferred brand)
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 medical attention. Be prepared to provide detailed information about the overdose, including the medication taken, the amount, and the time it occurred.