Artesunate 110mg/1vial Inj (2vials)
It is used to treat malaria.
Drug Class
Antimalarial
Pharmacologic Class
Artemisinin derivative
Pregnancy Category
Not available
FDA Approved
May 2020
DEA Schedule
Not Controlled
Overview
What is this medicine?
Artesunate is a powerful medicine given by injection directly into your vein to treat severe forms of malaria. Malaria is a serious disease caused by parasites spread by mosquito bites. Artesunate works very quickly to kill these parasites in your blood, helping you recover faster and preventing life-threatening complications.
How to Use This Medicine
To use this medication correctly, follow your doctor's instructions and carefully read all accompanying information. Take this medication exactly as directed, and adhere to all guidelines provided. This drug is administered via intravenous injection.
For storage and disposal, consult with your doctor, nurse, or pharmacist to determine the best approach if you need to keep this medication at home.
If you miss a dose, contact your doctor promptly to receive guidance on the appropriate course of action.
For storage and disposal, consult with your doctor, nurse, or pharmacist to determine the best approach if you need to keep this medication at home.
If you miss a dose, contact your doctor promptly to receive guidance on the appropriate course of action.
Lifestyle & Tips
- It is crucial to complete the entire course of treatment as prescribed, even if you start feeling better.
- After the initial injections, you will likely switch to an oral malaria medication to complete your treatment. Take this exactly as directed.
- Follow your doctor's instructions for follow-up blood tests to ensure the malaria parasites are completely gone and to monitor for any side effects.
- To prevent future malaria infections, take precautions against mosquito bites, such as using insect repellent, wearing protective clothing, and sleeping under mosquito nets, especially if you are in a malaria-endemic area.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
2.4 mg/kg IV at 0, 12, and 24 hours, then once daily until the patient can tolerate oral therapy and a full course of an oral artemisinin-based combination therapy (ACT) can be completed.
Condition-Specific Dosing:
severeMalaria:
2.4 mg/kg IV at 0, 12, and 24 hours, then once daily.
Pediatric Dosing
Neonatal:
2.4 mg/kg IV at 0, 12, and 24 hours, then once daily.
Infant:
2.4 mg/kg IV at 0, 12, and 24 hours, then once daily.
Child:
2.4 mg/kg IV at 0, 12, and 24 hours, then once daily.
Adolescent:
2.4 mg/kg IV at 0, 12, and 24 hours, then once daily.
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment needed.
Moderate:
No specific dose adjustment needed.
Severe:
No specific dose adjustment needed.
Dialysis:
No specific dose adjustment needed; Artesunate is rapidly metabolized and not significantly cleared by dialysis.
Hepatic Impairment:
Mild:
No specific dose adjustment needed.
Moderate:
No specific dose adjustment needed, but monitor clinical response and adverse effects.
Severe:
No specific dose adjustment needed, but monitor clinical response and adverse effects closely due to potential for altered pharmacokinetics.
Pharmacology
Mechanism of Action
Artesunate is a water-soluble prodrug that is rapidly hydrolyzed to its active metabolite, dihydroartemisinin (DHA). DHA is thought to exert its antimalarial effect by interacting with heme iron within the malaria parasite, leading to the generation of reactive oxygen species and alkylation of parasitic proteins. This causes oxidative stress, damage to parasite membranes, and inhibition of essential parasitic enzymes and protein synthesis, ultimately leading to parasite death.
Pharmacokinetics
Absorption:
Bioavailability:
100% (IV)
Tmax:
Rapid (within minutes for DHA)
FoodEffect:
Not applicable for IV administration
Distribution:
Vd:
Relatively large (e.g., DHA Vd: 0.5-1.5 L/kg)
ProteinBinding:
DHA: 47-90%
CnssPenetration:
Yes (important for cerebral malaria)
Elimination:
HalfLife:
Artesunate: <10 minutes; DHA: 0.5-3 hours
Clearance:
High
ExcretionRoute:
Primarily renal (urine) and fecal (bile) as metabolites
Unchanged:
<1% (Artesunate); <1% (DHA)
Pharmacodynamics
OnsetOfAction:
Rapid (within hours, leading to rapid parasite clearance)
PeakEffect:
Within hours
DurationOfAction:
Short (requires multiple doses and follow-on oral therapy)
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Attention Immediately
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 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
Signs of hemolytic anemia, including:
+ Dark urine or lips
+ Dizziness or fainting
+ Confusion
+ Feeling extremely tired or weak
+ Pale skin
+ Shortness of breath
+ Yellow skin or eyes
Signs of kidney problems, such as:
+ Inability to urinate
+ Changes in urine output
+ Blood in the urine
+ Sudden weight gain
Fever, chills, or sore throat
Unexplained bruising or bleeding
Feeling extremely tired or weak
Severe dizziness or fainting
Shortness of breath
Ringing in the ears
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 that bother you or persist, contact your doctor for guidance:
Stomach pain
Vomiting
Changes in taste
Dizziness or headache
Cough
This list is not exhaustive, and you may experience other side effects not mentioned here. If you have questions or concerns about side effects, 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 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
Signs of hemolytic anemia, including:
+ Dark urine or lips
+ Dizziness or fainting
+ Confusion
+ Feeling extremely tired or weak
+ Pale skin
+ Shortness of breath
+ Yellow skin or eyes
Signs of kidney problems, such as:
+ Inability to urinate
+ Changes in urine output
+ Blood in the urine
+ Sudden weight gain
Fever, chills, or sore throat
Unexplained bruising or bleeding
Feeling extremely tired or weak
Severe dizziness or fainting
Shortness of breath
Ringing in the ears
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 that bother you or persist, contact your doctor for guidance:
Stomach pain
Vomiting
Changes in taste
Dizziness or headache
Cough
This list is not exhaustive, and you may experience other side effects not mentioned here. If you have questions or concerns about side effects, 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:
- Persistent or worsening fever, chills, or body aches
- Severe headache or confusion
- Yellowing of your skin or eyes (jaundice)
- Dark or reddish-brown urine (may indicate blood in urine)
- Unusual bleeding or bruising
- Severe abdominal pain, nausea, or vomiting
- Difficulty breathing or shortness of breath
- Any new or worsening neurological symptoms (e.g., seizures, weakness, difficulty speaking)
- Skin rash or severe itching
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 and pharmacist assess potential interactions between this medication and other substances.
* Any existing health problems, as this medication may interact with certain conditions.
To ensure your safety, it is crucial to verify that this medication can be taken safely with all your current medications and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting 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 and pharmacist assess potential interactions between this medication and other substances.
* Any existing health problems, as this medication may interact with certain conditions.
To ensure your safety, it is crucial to verify that this medication can be taken safely with all your current medications and health conditions. Never start, stop, or adjust the dosage 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. Discuss any concerns or questions you have with your doctor.
Kidney problems are a potential risk associated with this medication, and in severe cases, hospitalization or dialysis may be required. If you are pregnant, planning to become pregnant, or are breastfeeding, you must notify your doctor. You and your doctor will need to carefully weigh the benefits and risks of this medication to you and your baby to make an informed decision.
Kidney problems are a potential risk associated with this medication, and in severe cases, hospitalization or dialysis may be required. If you are pregnant, planning to become pregnant, or are breastfeeding, you must notify your doctor. You and your doctor will need to carefully weigh the benefits and risks of this medication to you and your baby to make an informed decision.
Overdose Information
Overdose Symptoms:
- Symptoms of overdose are not well-defined but may include severe gastrointestinal upset (nausea, vomiting, diarrhea), neurological disturbances (dizziness, confusion, seizures), or bone marrow suppression (leading to anemia, low white blood cells, or low platelets).
What to Do:
If you suspect an overdose, seek immediate emergency medical attention. Call 911 or your local emergency number. Contact a poison control center (1-800-222-1222 in the US). Treatment is supportive and symptomatic.
Drug Interactions
Major Interactions
- Strong CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin, St. John's Wort): May significantly decrease plasma concentrations of DHA, potentially leading to reduced efficacy. Use with caution and monitor closely.
- Strong CYP3A4 inhibitors (e.g., ketoconazole, ritonavir): May increase plasma concentrations of DHA. Monitor for increased adverse effects.
Moderate Interactions
- Other antimalarials: May have additive or synergistic effects. Monitor for increased toxicity or altered efficacy.
- Drugs that prolong QT interval: Theoretical concern, but Artesunate itself has minimal QT prolongation effect. Use with caution.
Monitoring
Baseline Monitoring
Complete Blood Count (CBC) with differential
Rationale: To assess baseline hematological status and identify pre-existing anemia or other blood dyscrasias, and to monitor for potential post-treatment hemolytic anemia.
Timing: Prior to initiation of therapy
Liver Function Tests (LFTs) including AST, ALT, bilirubin
Rationale: To assess baseline hepatic function and monitor for drug-induced liver injury.
Timing: Prior to initiation of therapy
Renal Function Tests (RFTs) including BUN, creatinine
Rationale: To assess baseline renal function.
Timing: Prior to initiation of therapy
Blood Glucose
Rationale: To assess baseline glucose levels, as severe malaria can cause hypoglycemia.
Timing: Prior to initiation of therapy
Routine Monitoring
Parasitemia (malaria parasite count)
Frequency: Daily until negative, then periodically as clinically indicated.
Target: Rapid decrease in parasite count, eventual clearance.
Action Threshold: Persistent or increasing parasitemia may indicate treatment failure or resistance.
Clinical status (e.g., fever, consciousness, vital signs)
Frequency: Continuously/frequently during acute phase, then daily.
Target: Improvement in symptoms and vital signs.
Action Threshold: Worsening clinical condition, new neurological symptoms, or signs of organ dysfunction.
Complete Blood Count (CBC) with differential
Frequency: Daily during treatment, then weekly for 4 weeks post-treatment (especially for high parasite burden or prolonged treatment) to monitor for delayed hemolytic anemia.
Target: Stable or improving hemoglobin, platelet count.
Action Threshold: Significant drop in hemoglobin, new onset anemia, or thrombocytopenia.
Liver Function Tests (LFTs)
Frequency: Every 2-3 days during treatment, then weekly if abnormalities noted or prolonged treatment.
Target: Within normal limits or stable.
Action Threshold: Significant elevation of liver enzymes or bilirubin.
Symptom Monitoring
- Persistent or worsening fever
- Worsening headache or body aches
- Nausea, vomiting, or severe abdominal pain
- Yellowing of skin or eyes (jaundice)
- Dark urine (indicating hemolysis)
- Unusual bleeding or bruising
- Confusion, seizures, or altered mental status
- Skin rash or itching
- Signs of respiratory distress
Special Patient Groups
Pregnancy
Artesunate is the World Health Organization (WHO) recommended first-line treatment for severe malaria in all trimesters of pregnancy. The benefits of treating severe malaria, which is life-threatening for both mother and fetus, far outweigh any potential risks associated with Artesunate. Close monitoring of the mother and fetus is recommended.
Trimester-Specific Risks:
First Trimester:
Considered safe and recommended by WHO for severe malaria. While animal studies at very high doses have shown some embryotoxicity, human data and clinical experience support its use due to the high risk of untreated severe malaria.
Second Trimester:
Recommended by WHO for severe malaria.
Third Trimester:
Recommended by WHO for severe malaria.
Lactation
Artesunate and its active metabolite, dihydroartemisinin (DHA), are excreted into breast milk in small amounts. However, the amount transferred to the infant is generally considered too low to cause harm. The World Health Organization (WHO) recommends that breastfeeding can be continued during Artesunate treatment for severe malaria.
Infant Risk:
Low risk. Monitor the infant for any unusual symptoms like diarrhea or rash, though these are rare.
Pediatric Use
Artesunate is the drug of choice for severe malaria in children of all ages, including neonates and infants. Dosing is weight-based and similar to adults. Children with severe malaria require close monitoring for complications such as hypoglycemia, anemia, and neurological sequelae.
Geriatric Use
No specific dose adjustments are typically required based on age alone. However, geriatric patients may have age-related declines in renal or hepatic function, or multiple comorbidities, which could affect drug pharmacokinetics or increase susceptibility to adverse effects. Monitor clinical response and adverse effects closely.
Clinical Information
Clinical Pearls
- Artesunate IV is the first-line treatment for severe malaria globally, including in the United States, due to its superior efficacy and faster parasite clearance compared to quinine.
- Rapid conversion to dihydroartemisinin (DHA) is essential for its potent antimalarial activity.
- Patients treated with IV Artesunate for severe malaria must be transitioned to a full course of an oral artemisinin-based combination therapy (ACT) once they are clinically stable and can tolerate oral medications.
- Delayed hemolytic anemia (DHA-induced hemolytic anemia) can occur 2-4 weeks after treatment, particularly in patients with high parasite burdens. Close monitoring of hemoglobin levels for several weeks post-treatment is crucial.
- Artesunate is generally well-tolerated, with common side effects being mild and transient, such as nausea, vomiting, and dizziness.
Alternative Therapies
- Quinine (historically used for severe malaria, but less effective and associated with more adverse effects than artesunate)
- Artemether (another artemisinin derivative, available as an intramuscular injection, used in some regions for severe malaria when IV artesunate is not available)
Cost & Coverage
Average Cost:
Price range varies significantly by supplier, quantity, and country. Typically several hundred to over a thousand USD per course for the US market. per course
Generic Available:
Yes
Insurance Coverage:
Often covered under medical benefit for inpatient treatment of severe malaria. Outpatient coverage may vary and require prior authorization.
General Drug Facts
If your symptoms or health problems persist or worsen, it is essential to contact your doctor for further guidance. To ensure safe use, never share your medication with others, and do not take medication prescribed for someone else. Store all medications in a secure location, out of reach of children and pets, to prevent accidental ingestion. Dispose of unused or expired medications properly. Unless instructed otherwise, do not flush medications down the toilet or pour them down the drain. If you are unsure about the correct disposal method, consult your pharmacist, who can also inform you about potential drug take-back programs in your area. Some medications may come with an additional patient information leaflet, which your pharmacist can provide. If you have any questions or concerns about your medication, discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately contact your local poison control center or seek emergency medical attention. Be prepared to provide information about the medication taken, the amount, and the time it occurred.