Chloroquine classification and pharmacokinetics

Chloroquine is a 4-aminoquinoline derivative. The drug is rapidly absorbed when given orally, is widely distributed to tissues, and has an extremely large volume of distribution. Antacids may decrease oral absorption of the drug. Chloroquine is excreted largely unchanged in the urine. Chloroquine is rapidly and completely absorbed following oral administration. Usually, 4 days of therapy suffice to cure the disease. The drug has a very large volume of distribution and concentrates in erythrocytes, liver, spleen, kidney, lung, melanin-containing tissues, and leukocytes. It persists in erythrocytes The drug also penetrates the central nervous system (CNS) and traverses the placenta. Chloroquine is dealkylated by the hepatic mixed-function oxidase system, but some metabolic products retain antimalarial activity. Both parent drug and metabolites are excreted predominantly in urine.The excretion rate is enhanced with acidified urine.