The fastest acting schizonticidal drug among the following is:

Correct Answer: Artemether
Description: Artemether-lumefantrine ​ Lumefantrine is an orally active, high efficacy, long-acting erythrocytic schizontocide, related chemically and in mechanism of action to halofantrine and MQ. Like the other schizontocides, vivax hypnozoites are not affected. Lumefantrine is highly lipophilic; absorption starts after 2 hours of ingestion and peaks at 6-8 hours. Antimalarial action is slower than CQ. Plasma protein binding is 99%, and it is metabolized predominantly by CYP3A4. Terminal t½  is  2- 3 days, which is prolonged to 4 -6 days in malaria patients. ​ Lumefantrine is used only in combination with artemether, as FDC tablets. The two components protect each other from plasmodial resistance. ​ As  such, no clinically relevant resistance has developed so far. Clinical efficacy is high achieving 95- 99% cure rate. Artemether-lumefantrine is  active even in multidrug resistant Plasmodium falciparum areas, including  MQ-resistant.​ Key Concept:​ Artemisinin derivatives like dihydroartemisinin, arteether and artemether, etc., are fastest acting  antimalarial drugs.​ Reference: Essentials of Medical Pharmacology Eighth Edition KD TRIPATHI page no 889​ ​
Category: Pharmacology
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