How Do Aminoquinoline Antimalarials Work?

Reviewed on 9/30/2021

HOW DO AMINOQUINOLINE ANTIMALARIALS WORK?

Aminoquinoline antimalarials are drugs used to treat and prevent malaria. They act against all malarial parasites, especially Plasmodium malariae, Plasmodium vivax, and all strains of Plasmodium falciparum.

Aminoquinoline antimalarials include:

Chloroquine: Inhibits the activity of an enzyme heme polymerase in malarial trophozoites; this prevents the conversion of heme to hemozoin. This leads to the accumulation of poisonous heme, eventually killing the parasite. Chloroquine accumulates in the organelles such as lysosomes and endosomes, increases the pH of the parasite, and alters the process of protein degeneration which changes their functionality and thus cannot enter into the host cells.

Hydroxychloroquine sulfate, whose exact mechanism of action is unknown, increases pH in the parasite and interferes with an enzyme that prevents normal growth and replication of the parasite. Hydroxychloroquine sulfate also increases the concentrations of toxic heme.

Primaquine may bind with and alter the properties of parasite DNA

Tafenoquine is active against most forms of Plasmodium in the body. Tafenoquine has good activity against hypnozoite, the pre-erythrocytic stage, which grows in the liver. The prevention of hypnozoite can prevent relapse of Plasmodium vivax malaria.

HOW ARE AMINOQUINOLINE ANTIMALARIALS USED?

Aminoquinoline antimalarials are indicated for:

  • Treatment of uncomplicated malaria due to Plasmodium falciparum, Plasmodium malariae, Plasmodium ovale, and Plasmodium vivax
  • Prophylaxis of malaria in geographic areas where chloroquine resistance is not reported

Other uses of aminoquinoline antimalarials include:

Off-label use includes:

WHAT ARE SIDE EFFECTS OF AMINOQUINOLINE ANTIMALARIALS? 

Side effects associated with aminoquinoline antimalarials include:

 

The information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with your doctor or pharmacist to make sure these drugs do not cause any harm when you take them along with other medicines. Never stop taking your medication and never change your dose or frequency without consulting your doctor.

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WHAT ARE NAMES OF AMINOQUINOLINE ANTIMALARIALS?

Generic and brand names of aminoquinoline antimalarials include:

References
https://reference.medscape.com/drugs/antimalarials-aminoquinoline

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6097041/

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