SopaquinReumaquinDelagilQuinoscanAvlochlorNivaquineHelioparElestolAvloclorArthrochinBemasulph3377 RP opalateNivachineQuinagaminSanoquinReumachlorQuinachlorMalarexCapquinCocartritBemaphateAralenBenaquinArechinSolprinaPfizerquineTanakanBemacoAralen HClResoquineNeochinQuingamineQuinilonIroquineGontochinMalaquinLapaquinMesylithPlaquenilImagonMalarenTrochinTresochinQuinercylAmokinChemochinSiraganSilbesanRoquineDichinalexResochenNivaquine BChingaminCidanchinBipiquinQuinagamineChlorochinResoquinaResochinKlorokinArtrichin
The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses. [PubChem]
Indication
For the suppressive treatment and for acute attacks of malaria due to P. vivax, P.malariae, P. ovale, and susceptible strains of P. falciparum, Second-line agent in treatment of Rheumatoid Arthritis
Pharmacology
Chloroquine is the prototype anti malarial drug, most widely used to treat all types of malaria except for disease caused by chloroquine resistant Plasmodium falciparum. It is highly effective against erythrocytic forms of Plasmodium vivax, Plasmodium ovale and Plasmodium malariae, sensitive strains of Plasmodium falciparum and gametocytes of Plasmodium vivax. Being alkaline, the drug reaches high concentration within the food vacuoles of the parasite and raises its pH. It is found to induce rapid clumping of the pigment. Chloroquine inhibits the parasitic enzyme heme polymerase that converts the toxic heme into non-toxic hemazoin, thereby resulting in the accumulation of toxic heme within the parasite. It may also interfere with the biosynthesis of nucleic acids.
Affected Organisms
Plasmodium
Biotransformation
Hepatic (partially)
Absorption
Completely absorbed from gastrointestinal tract
Half Life
1-2 months
Protein Binding
~55% of the drug in the plasma is bound to nondiffusible plasma constituents
Elimination
Excretion of chloroquine is quite slow, but is increased by acidification of the urine.
Standard anti-malarial drug. Substrate for MRP in multidrug resistant cell line and inhibits photoaffinity labelling of MRP by quinoline-based photoactive drug IAAQ.
