Artesunate

Artesunate is an antiparasitic medication derived from artemisinin, used in the treatment of severe and complicated malaria caused by Plasmodium falciparum, uncomplicated malaria in multidrug-resistant areas, and malaria caused by P. vivax.

Artesunate is metabolized to the active metabolite dihydroartemisinin (DHA). The endoperoxide bridge of DHA reacts with heme, generating free radicals which inhibit protein and nucleic acid synthesis of Plasmodium parasites during all erythrocytic stages.

Common side effects include headache, dizziness, weakness, and loss of appetite.

• Severe and complicated malaria caused by Plasmodium falciparum
• Uncomplicated malaria in multidrug-resistant P. falciparum areas
• Malaria caused by Plasmodium vivax
• Pernicious malaria (salvage therapy)

Artesunate is an artemisinin derivative that is metabolized to the active metabolite dihydroartemisinin (DHA). The endoperoxide bridge of DHA reacts with heme, generating free radicals which inhibit protein and nucleic acid synthesis of the Plasmodium parasites during all erythrocytic stages.

Reactions with these free radicals can also lead to alkylation of parasitic proteins such as calcium adenosine triphosphatase and EXP1, a glutathione S-transferase.

Artesunate is converted to its active metabolite DHA, which reacts with heme in the parasite to generate free radicals. These free radicals inhibit protein and nucleic acid synthesis, leading to parasite death.

Artesunate 50 mg Tablet:

• Adults: Day 1: 2 tablets twice; Days 2-5: 1 tablet twice daily (4, 2, 2, 2, 2)
• Children (1-3 years): 3 tablets over 5 days (1, ½, ½, ½, ½)
• Children (4-5 years): 6 tablets over 5 days (2, 1, 1, 1, 1)
• Children (6-12 years): 8 tablets over 5 days (3, 2, 1, 1, 1)

Artesunate 100 mg Tablet:

• Adults: Day 1: 1 tablet twice; Days 2-5: half tablet twice daily (2, 1, 1, 1, 1)
• Children (4-5 years): 3 tablets over 5 days (1, ½, ½, ½, ½)
• Children (6-12 years): 4 tablets over 5 days (1½, 1, ½, ½, ½)

Malaria Prophylaxis: 2 tablets (50 mg) or 1 tablet (100 mg) once weekly, from 1 week before entering a malaria area to 4 weeks after leaving.

Your doctor or nurse will give you this medicine. Do not self-administer. For emergency treatment of severe malaria, IV or IM injection is preferred.

If you miss a dose, please consult your doctor.

No significant side effects reported at recommended dose. Rare cases may include:

• Headache
• Dizziness
• Weakness
• Loss of appetite

Serious Precautions:

• Use only under the advice of a Registered Physician
• Do not exceed the recommended dose
• Use with caution in patients with severe vomiting
• Use in first trimester of pregnancy only if recommended by a Registered Physician
• Breastfeeding should be stopped during treatment
• May cause dizziness - use caution while driving or operating machinery
• Regular blood tests may be required to monitor parasite clearance

• Hypersensitivity to Artemisinin and its derivatives
• Hypersensitivity to inactive ingredients

• Other artemisinin derivatives (artemether, arteether): Combined effect on prolonging PQ and QT interval
• Other antimalarials (quinine, quinidine, mefloquine, halofantrine): Cardiac effects
• Drugs that prolong QT interval (erythromycin, terfenadine, astemizole, probucol, procainamide, disopyramide, amiodarone, bretylium, bepridil, sotalol, tricyclic antidepressants, neuroleptics)

Alcohol consumption should be avoided.

[CONSULT YOUR DOCTOR] According to WHO, artesunate should be available for malaria treatment in pregnancy irrespective of trimester. Use in first trimester only if recommended by a Registered Physician.

[CONSULT YOUR DOCTOR] Artesunate may be present in breast milk. Breastfeeding should be stopped during malaria treatment with Artesunate due to potential adverse effects on the nursing infant.

Pediatric dosing table available for 1-3 years, 4-5 years, and 6-12 years.

Patients aged more than 12 years should be given adult dose.

Limited information available on use in kidney disease. Consult your doctor.

Limited information available on use in liver disease. Consult your doctor.

In case of overdose, provide symptomatic and supportive treatment.

Store below 30°C, away from light and moisture. Keep out of reach of children.

Artesunate (C₁₉H₂₈O₈)