Artesunate

Artesunate is metabolized to the active 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 a calcium adenosine triphosphatase and EXP1, a glutathione S-transferase.

It is to be given by oral route. The oral dose of Artesunate tablet can be defined as follows:

For Artesunate 50 mg tablet:
Adults:

• Two Artesunate 50 tablets twice on the first day, then
• one Artesunate 50 tablet twice daily for the next four days (4, 2, 2, 2, 2)

Children:

• 1-3 years: 3 Artesunate 50 tablets for 5 days (1, 1⁄2, 1⁄2, 1⁄2, 1⁄2)
• 4-5 years: 6 Artesunate 50 tablets for 5 days (2, 1, 1, 1, 1)
• 6-12 years: 8 Artesunate 50 tablets for 5 days (3, 2, 1, 1, 1)

For Artesunate 100 mg tablet:
Adults: One Artesunate 100 tablet twice on the first day, then half Artesunate 100 tablet twice daily for the next four days (2, 1, 1, 1, 1)

Children:

• 4-5 years: 3 Artesunate 100 tablets for 5 days (1, 1⁄2, 1⁄2, 1⁄2, 1⁄2)
• 6-12 years: 4 Artesunate 100 tablets for 5 days (11⁄2,1,1⁄2,1⁄2,1⁄2)
• Patients aged more than 12 years: should be given same as adult dose.

Dosage for the prevention of malaria: Two Artesunate 50 tablets (or one Artesunate 100 tablet) as a single dose once a week, from one week before entering a malaria-affected area to four weeks after leaving the area.

Artesunate may have interaction with other artemisinin drugs i.e. artemether, arteether which have the same effect in prolonging the PQ and QT interval. It has interaction when it is given with other antimalarial drugs (eg. Quinine, quinidine, mafloquine and halofantrine) which have cardiac action. It also has interaction with other drugs which prolong QT interval (such as erythromycin, terfenadine, astemizole, probucol, procainamide, disopyramide, amiodarone, bretylium, bepridil, sotalol, tricyclic antidepressants and neuroleptics).

Artesunate is contraindicated for patients with known hypersensitivity to Artemisinin and its derivatives or its inactive ingredients.

Artesunate tablet is well tolerated. No adverse effects have been reported from the treatment of artesunate at recommended dose.

A WHO report assessing the safety of artemisinin derivatives in pregnancy concluded that these drugs should continue to be available for the treatment of malaria in pregnancy, irrespective of the trimester. WHO also stressed that further study was needed. Therefore Artesunate tablet should be given to pregnant women especially, in first trimester if recommended by Registered Physician. Like many other drugs there is possibility for presence of artesunate in breast milk. Because of potential of adverse effect of artesunate in nursing baby, breast-feeding should be stopped during the treatment of malaria by Artesunate tablet.

• This tablet should be used with caution in patients vomiting severely.
• For emergency treatment of patients suffering from severe malaria, intravenous or intramuscular injection is preferred.
• Do not use the drug without the advice of a Registered Physician.
• Do not exceed the recommended dose.

Anti-malarial drugs

Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.