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PLAQUENIL (HYDROXYCHLOROQUINE SULFATE) TABLETS: CLINICAL PHARMACOLOGY

Microbiology

Malaria

Mechanism of action

The precise mechanism by which hydroxychloroquine exhibits activity against Plasmodium is not known. Hydroxychloroquine, like chloroquine, is a weak base and may exert its effect by concentrating in the acid vesicles of the parasite and by inhibiting polymerization of heme. It can also inhibit certain enzymes by its interaction with DNA.

Activity in vitro and in clinical infections

Hydroxychloroquine is active against the erythrocytic forms of chloroquine sensitive strains of Plasmodium falciparum, Plasmodium malariae, Plasmodium ovale, and Plasmodium vivax. Hydroxychloroquine is not active against the gametocytes and exoerythrocytic forms including the hypnozoite stage (P. vivax and P. ovale) of the Plasmodium parasites.

Drug resistance

P. falciparum strains exhibiting reduced susceptibility to chloroquine also show reduced susceptibility to hydroxychloroquine.

Resistance of Plasmodium parasites to chloroquine is widespread.

Patients in whom chloroquine or hydroxychloroquine have failed to prevent or cure clinical malaria or parasitemia, or patients who acquired malaria in a geographic area where chloroquine resistance is known to occur should be treated with another form of antimalarial therapy.

Rheumatoid Arthritis and Systemic Lupus Erythematosus

Mechanism of action

The mechanisms underlying the anti-inflammatory and immunomodulatory effects of Plaquenil (Hydroxychloroquine) are unknown.

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