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Table 1 Pharmacology of selected candidates for IPTp

From: Intermittent preventive treatment for malaria in pregnancy in Africa: What's new, what's needed?

Drug

Mode of action

Elimination half life

Advantages/disadvantages

Artemether

Inhibits falciparum sarcoplasmic-endoplasmic reticulum calcium ATPase

3 – 7 h (converted to DHA)

Appears safe in the second and third trimester

Widely available in a cheap, fixed dose co-formulation with lumefantrine (Coartem©/Riamet©)

Artemisinin

Inhibits falciparum sarcoplasmic-endoplasmic reticulum calcium ATPase

2 – 3 h (converted to DHA)

Appears safe in the second and third trimester

Fixed dose co-formulations unavailable

Artesunate

Inhibits falciparum sarcoplasmic-endoplasmic reticulum calcium ATPase

2 – 5 mins (converted to DHA)

Appears safe in the second and third trimester

Fixed dose co-formulations unavailable

Atovaquone

Selective inhibitor of parasite mitochondrial metabolism

48 – 72 h

Appears safe in the third trimester

Available only in fixed dose co-formulation with proguanil (Malarone©), which is expensive outside specific donation programmes

Azithromycin

Exact mode of action unknown

68 h

Safe in all trimesters where has been used extensively in STI treatment

Expensive; fixed dose co-formulations unavailable

Chlorproguanil

Folic acid antagonist (inhibits dihydrofolate reductase)

32 h

Cheap; appears safe in the third trimester and likely to be safe earlier in pregnancy based on experience with proguanil

Available only in fixed dose co-formulation with dapsone (Lapdap©), which WHO have recommended be used with caution in areas of high G6PD deficiency

Dapsone

Folic acid antagonist (inhibits dihydropteroate synthase)

31 h

Cheap; appears safe in the third trimester

Available in fixed dose co-formulation with chlorproguanil (Lapdap©), which WHO have recommended be used with caution in areas of high G6PD deficiency

Dihydroartemisinin (DHA)

Inhibits falciparum sarcoplasmic-endoplasmic reticulum calcium ATPase

40 – 60 mins

Likely to be safe in the second and third trimester

Available in SE Asia, China in a cheap fixed dose co-formulation with piperaquine (Artekin©/Eurartekin©)

Lumefantrine

Inhibits metabolism of haem within parasite acid food vacuole

4 – 6 days

Safety in children and adults established but no data available in pregnancy

Widely available in a cheap [through WHO pricing agreement], fixed dose co-formulation with artemether (Coartem©/Riamet©)

Mefloquine

Exact mode of action unknown

2 – 4 weeks

Appears safe in the second and third trimester

Expensive; fixed dose co-formulations unavailable

Piperaquine

Inhibits detoxification of haem

3 – 4 weeks

Safety in children and adults established but no data available in pregnancy

Available in SE Asia, China in a cheap, fixed dose co-formulation with dihydroartemisinin (Artekin©/Eurartekin©)

Proguanil

Folic acid antagonist (inhibits dihydrofolate reductase)

12 – 21 h

Cheap; appears safe in all trimesters

Available alone or in fixed dose co-formulation with atovaquone (Malarone©), which is expensive outside specific donation programmes

Pyrimethamine

Folic acid antagonist (inhibits dihydrofolate reductase)

100 h

Cheap; widely available in fixed-dose combination with sulphadoxine

Increasing resistance particularly in East Africa

Sulphadoxine

Folic acid antagonist (inhibits dihydropteroate synthase)

200 h

Cheap; widely available in fixed-dose combination with pyrimethamine

Increasing resistance particularly in East Africa