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Current anti-malarial agents
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Drug name |
Drug class |
Anti-malarial activity |
Side effects |
Quinine |
arylaminoalcohol |
Accumulates in food vacuoles and forms toxic haem complexes |
hearing impairment, rashes, vertigo, vomiting and in some cases neurotoxicity |
quinidine |
arylaminoalcohol |
Acts similarly to quinine |
Headache, nausea, sweating vasodilatation and diarrhoea are common |
Mefloquine |
Amino alcohol |
Acts similarly to quinine |
Nausea, dizziness, diarrhoea, bradycardia and neurotoxicity |
Lumefantrine |
Amino alcohol |
Similar to quinine, mefloquine and halofantrine. Marketed in combination with artemether. |
headache, dizziness, vomiting |
Chloroquine |
4-Aminoquinoline |
Being dibasic it achieves high concentrations in the digestive vacuole and is believed to inhibit haem olymerization and thus disrupt parasite haemoglobin metabolism |
May cause psoriasis |
Amodiaquine |
4-Aminoquinoline |
Similar mechanism to chloroquine |
Vomiting, dizziness and in some cases hepatic disorders |
Quinacrine |
4-Aminoacridine |
Exact mechanism poorly understood. Evidence of and inhibition of haem polymerization in the digestive vacuole. No longer used clinically as an antimalarial. |
mild transient headache, dizziness, and GI disorders such as diarrhea, anorexia, nausea, |
Primaquine |
8-Aminoquinoline |
Believed to block oxidative metabolism in the parasite |
Anorexia, vomiting, cramps and anaemia |
Halofantrine |
Amino alcohol |
Acts similarly to quinine |
Nausea, diarrhoea, itching and high cardiotoxicity |
Sulfadoxine |
Anilinosulphonamide |
Targets dihydropteroate synthase (DHPS) competing with paraaminobenzoic acid (PABA) |
Skin reactions (rare) |
Dapsone |
Anilinosulphone |
acts similarly to sulfadoxine |
bluish lips or skin, chest pain, mood changes |
Sulfamethoxypyridazine |
sulfonamide antibacterial. |
Sulfonamides are structural analogues of para-aminobenzoic acid (PABA) and act as competitive inhibitors of dihydropteroate synthase |
GI disturbances (nausea, vomiting, anorexia) and allergic skin reactions |
Proguanil |
Biguanide |
Proguanil is metabolized in vivo to cycloguanil, a DHFR inhibitor, but is also known to have antimalarial activity in its right. |
Very few: hair loss and mouth ulcers |
Cycloguanil |
Diamino-dihydrotriazine |
In vivo metabolite from proguanil. Inhibitor of DHFR
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abdominal pain, nausea, headache, and fever. |
Chlorproguanil |
Biguanide |
Close analog of proguanil |
gastrointestinal distress, including diarrhea, cramps, nausea, vomiting, and increased flatulence |
Pyrimethamine |
Diaminopyrimidine |
Inhibits DHFR |
Occasional rashes |
Tetracycline |
Tetracyclic antibiotic/ antiparasitic |
Inhibits cell growth by inhibiting translation and results in a delayed death phenotype. Putative targets are 70S ribosomal subunit within the apicoplast and mitochondrian |
nausea, vomiting, diarrhea, upset stomach, swollen tongue |
Doxycycline |
Tetracyclic antibiotic/ antiparasitic |
Acts similarly to tetracycline |
Depression of bone growth and gastrointestinal disturbances |
Clindamycin |
Lincosamide antibiotic/ antiparasitic. |
Inhibits protein synthesis |
Nausea, vomiting and cramps |
Azithromycin |
Macrolides and analogues |
Displays similar phenotype to tetracyclines |
May cause angioedema and jaundice |
Artemisinin |
Endoperoxide |
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Nausea, anorexia, dizziness and neurotoxicity |
Artemether |
Endoperoxide |
Semi-synthetic artemisinin derivative with similar activity
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Joint pain, muscle pain |
Arteether |
Endoperoxide |
Semi-synthetic artemisinin derivative with similar activity
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Headache,.nausea or vomiting. persistent cough. dizziness. |
Dihydroartemisinin |
Endoperoxide |
Mixture of epimers. Metabolite of artemisinin and other artemisinin semi-synthetic derivatives with similar activity in its own right but less chemically stable. |
dizziness, headache, cough, nausea, vomiting, anorexia, asthenia |
Artesunate |
Endoperoxide |
Highly soluble semi-synthetic dihydroartemisinin analogue. Marketed with mefolquine, amodiaquine and pyronaridine |
slow heartbeat, allergic reaction,dizziness, and low white blood cell levels. |
Atovaquone |
Hydroxy-quinone |
The site of action appears to be the cytochrome bc1 complex (Complex III) and disruption of electron transport, resulting in inhibition of mitochondrial dehydrogenases. This inhibits pyrimidine biosynthesis and nucleic acid and ATP synthesis. Marketed in |
May cause rashes, diarrhoea and headache |
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