Usage
- Alpha-Beta Arteether is prescribed for the treatment of uncomplicated and severe Plasmodium falciparum malaria, particularly in regions where resistance to other antimalarials like chloroquine is prevalent. It is also used for cerebral malaria. It is not used for prophylaxis (prevention) of malaria or for other species of Plasmodium.
- Pharmacological Classification: Antimalarial, Antiparasitic
- Mechanism of Action: Alpha-Beta Arteether, a semi-synthetic derivative of artemisinin, acts as a blood schizonticide. It generates reactive oxygen species within the parasite, leading to damage of parasitic proteins and ultimately parasite death.
Alternate Names
- Artemotil (beta-arteether)
- Alpha/Beta Arteether
How It Works
- Pharmacodynamics: Alpha-Beta Arteether acts rapidly against the asexual blood stages of P. falciparum, reducing parasitemia and alleviating symptoms like fever. It has limited action against liver stages or gametocytes.
- Pharmacokinetics: Alpha-Beta Arteether is administered intramuscularly. It is rapidly absorbed and metabolized by the liver. Elimination occurs mainly via hepatic metabolism, with a small portion excreted in the urine. The primary metabolic pathway involves cytochrome P450 enzymes, specifically CYP3A4.
- Mode of Action: The endoperoxide bridge of Alpha-Beta Arteether interacts with heme iron within the parasite-infected red blood cells. This interaction generates free radicals, leading to oxidative stress and damage to parasitic proteins and membranes.
- Elimination Pathways: Primarily hepatic metabolism via CYP3A4, with minor renal excretion.
Dosage
Standard Dosage
Adults:
- 150 mg intramuscularly once daily for 3 consecutive days. The total cumulative dose is 450 mg, regardless of body weight.
Children:
- 3 mg/kg body weight intramuscularly once daily for 3 consecutive days.
Special Cases:
- Elderly Patients: Dosage adjustments are not usually required but close monitoring is recommended due to potential age-related decline in organ function.
- Patients with Renal Impairment: Use with caution. Dose adjustments may be necessary. Close monitoring of renal function is recommended.
- Patients with Hepatic Dysfunction: Use with caution. Close monitoring of liver function is recommended. Dosage adjustments may be required.
- Patients with Comorbid Conditions: Use with caution in patients with cardiac conditions, especially those prone to arrhythmias, due to the potential for QT prolongation.
Clinical Use Cases
- Alpha-Beta Arteether is used for treating severe and complicated P. falciparum malaria. Specific clinical use cases include cerebral malaria and cases where other antimalarials are ineffective due to resistance. It is generally administered in a hospital setting under close medical supervision.
Dosage Adjustments
- Dosage adjustments may be necessary for patients with renal or hepatic impairment.
Side Effects
Common Side Effects
- Pain or discomfort at the injection site
- Nausea
- Vomiting
- Headache
- Dizziness
- Diarrhoea
- Abdominal Pain
Rare but Serious Side Effects
- Allergic reactions (rash, itching, swelling, difficulty breathing)
- Neurotoxicity (rare)
- Cardiac arrhythmias (rare)
Long-Term Effects
Limited data available.
Adverse Drug Reactions (ADR)
- Severe allergic reactions
- QT interval prolongation (rare)
Contraindications
- Hypersensitivity to artemisinin derivatives
- First trimester of pregnancy (unless absolutely necessary)
- Severe liver or kidney disease
Drug Interactions
- CYP3A4 inducers (e.g., rifampicin, carbamazepine) may decrease Alpha-Beta Arteether levels.
- CYP3A4 inhibitors (e.g., ketoconazole, erythromycin) may increase Alpha-Beta Arteether levels.
- QT-prolonging drugs (e.g., quinine, halofantrine, amiodarone, sotalol) may increase the risk of cardiac arrhythmias.
- Mefloquine should be avoided in combination with Arteether
- Antacids may interfere with drug absorption.
Pregnancy and Breastfeeding
- Pregnancy Safety Category: Not established. Arteether should generally be avoided during the first trimester of pregnancy. In later trimesters, it should only be used if the potential benefits outweigh the risks to the fetus.
- Breastfeeding: Arteether is excreted in breast milk. Use with caution. Consider the risk to the infant.
Drug Profile Summary
- Mechanism of Action: Blood schizonticide, generates reactive oxygen species within the parasite.
- Side Effects: Injection site pain, nausea, vomiting, headache, dizziness. Rarely: allergic reactions, neurotoxicity, cardiac arrhythmias.
- Contraindications: Hypersensitivity to artemisinin, first trimester of pregnancy, severe liver/kidney disease.
- Drug Interactions: CYP3A4 inducers/inhibitors, QT-prolonging drugs, mefloquine, antacids.
- Pregnancy & Breastfeeding: Avoid in first trimester, caution in later trimesters and during breastfeeding.
- Dosage: 150 mg IM daily for 3 days (adults); 3 mg/kg IM daily for 3 days (children).
- Monitoring Parameters: Liver function tests, renal function tests, ECG (in patients with cardiac history), parasite counts.
Popular Combinations
Alpha-Beta Arteether is sometimes used in combination with other antimalarials, such as Lumefantrine, to enhance efficacy and prevent resistance development.
Precautions
- General Precautions: Evaluate liver and kidney function, cardiac history. Monitor for allergic reactions.
- Specific Populations: Avoid in the first trimester of pregnancy; use with caution during breastfeeding. Pediatric use under medical supervision.
- Lifestyle Considerations: Avoid alcohol during treatment.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Alpha-Beta Arteether?
A: Adults: 150 mg intramuscularly once daily for 3 days. Children: 3 mg/kg intramuscularly once daily for 3 days.
Q2: What are the common side effects of Alpha-Beta Arteether?
A: Common side effects include pain at the injection site, nausea, vomiting, headache, and dizziness.
Q3: Is Alpha-Beta Arteether safe in pregnancy?
A: It should be avoided in the first trimester unless absolutely necessary. In later trimesters, it should only be used if the benefits outweigh the risks.
Q4: Can Alpha-Beta Arteether be used in patients with liver or kidney disease?
A: Use with caution in patients with liver or kidney disease. Close monitoring and dosage adjustments may be necessary.
Q5: What are the drug interactions of Alpha-Beta Arteether?
A: It interacts with CYP3A4 inducers/inhibitors, QT prolonging agents, mefloquine, and antacids.
Q6: What is the mechanism of action of Alpha-Beta Arteether?
A: It generates reactive oxygen species that damage parasitic proteins, leading to parasite death.
Q7: What type of malaria does Alpha-Beta Arteether treat?
A: It is used to treat uncomplicated and severe Plasmodium falciparum malaria.
Q8: Can Alpha-Beta Arteether be self-administered?
A: No, it must be administered intramuscularly by a healthcare professional.
Q9: How long does the treatment with Alpha-Beta Arteether last?
A: The standard treatment course is 3 consecutive days.
Q10: What should I monitor in a patient receiving Alpha-Beta Arteether?
A: Monitor for allergic reactions, liver and kidney function, and cardiac rhythm (especially in patients with pre-existing cardiac conditions), and parasite counts.
