Concentrates in parasite food vacuoles, preventing the biocrystallization of the hemoglobin breakdown product, heme, into hemozoin, and thus eliciting parasite toxicity due to the buildup of free heme.

Pruritis, vision blurring, anorexia, malaise, hemolysis, ototoxicity, confusion, psychosis, seizures, agranulocytosis, alopecia

Drug of choice for treatment & chemoprophylaxis of nonfaciparum and sensitive falciparum malaria.

Unknown

Effective blood shizonticide against 4 human malaria parasites; gametocidal against P vivax and P ovale but not P falciparum

Cinchonism (tinnitus, flushing, visual disturbances, etc.), visual/auditory, hypersensitivity (angioedema,  bronchospasm), hemolytic anemia, leukopenia, agranulocytosis, hrombocytopenia

Parenteral treatment of severe falciparum malaria, oral treatment of falciparum malaria, babesiosis

Unknown

Strong blood shizonticidal activity against P falciparum and P vivax, but not hepatic stages or gametocytes

Sleep/behavioral disturbances, leukocytosis, thrombocytopenia

Chemoprophylaxis and treatment of P falciparum

Selectively inhibit plasmodial dihydrofolate reductase, a key enzyme in the pathway for synthesis of folate.

Act slowly against erythrocytic forms of susceptible strains of all 4 human species

Mouth ulcers, alopecia

Steven-Johnson syndrome

Chemoprophylaxis, intermittent preventive therapy, treatment of chloroquine-resistant falciparum malaria, toxopasmosis, pneumocystosis

Selectively inhibit plasmodial dihydrofolate reductase, a key enzyme in the pathway for synthesis of folate.

Act slowly against erythrocytic forms of susceptible strains of all 4 human species

Mouth ulcers, alopecia

Steven-Johnson syndrome

Chemoprophylaxis, intermittent preventive therapy, treatment of chloroquine-resistant falciparum malaria, toxopasmosis, pneumocystosis

Unknown

Effective against erythrocytic (but no other) stages of all 4 human species

Cardiac toxicity, abdominal pain, teratogenic

Treatment of P falciparum infections (not chemoprophylaxis)

Rapidly acting blood schizonticides against all human malaria species.  Antimalarial activity may result from the production of free radicals that follows the iron-catalyzed cleavage of the artemisinin endoperoxide bridge in the parasite food vacuole or form inhibition of a parasite calcium ATPase.

Neutropenia, anemia, hemolysis

Treatment of P falciparum infection, oral combination therapies for uncomplicated disease; IV for severe disease

Unknown

Active against hepatic stages of all human malaria parasites.  Only agent active against dormant hypnozoite stages of P vivax and P ovale.  Also gametocidal against 4 human species.

Leukopenia, agranulocytosis, leukocytosis, arrhythmias,  hemolytic anemia, methemoglobinemia

Therapy (radical cure) of acute vivax and ovale malaria, terminal prophylaxis of vivax and ovale malaria, chemoprophylaxis of malaria, gametocidal action (disrupt transmission), pneumocystis jiroveci

Acts against plasmodia by disrupting mitochondrial electron transport.  Active against tissue and erythrocytic shizonts

Fever, rash, insomnia

Treatment and chemophylaxis of malaria; P jiroveci pneumonia

The nitro group is chemically reduced in anaerobic bacteria & sensitive protozoans.

Reactive reduction products are responsible for antimicrobial activity.

Metallic taste in mouth, dark urine, vertigo, neutropenia

Altered taste

Inhibits ethanol metabolism

Rx: extra-luminal amebiasis, giardiasis, trichomoniasis

The nitro group is chemically reduced in anaerobic bacteria & sensitive protozoans.

Reactive reduction products are responsible for antimicrobial activity.

Metallic taste in mouth, dark urine, vertigo, neutropenia

Altered taste

Inhibits ethanol metabolism

Rx: extra-luminal amebiasis, giardiasis, trichomoniasis

Unknown

Luminal amebicide

Optic neuritis, iodine toxicity (dermatitis, urticarial, pruritus)

Active against trophozoites in bowel lumen

Unknown

Luminal amebicide

flatulence

Asymptomatic luminal infections

Aminoglycoside antibiotic

Aminiglycosides → ototoxicity, renal damage/renal failure

Luminal amebicide, Leishmaniasis

Inhibit protein synthesis by blocking ribosome movement along mRNA

Cardiac toxicity, muscle weakness, arrhythmias, heart failure, hypotension

Rx: severe amebiasis

CI: cardiac/renal disease, kids, pregnancy

Unknown

Significant toxicity: hypotension, tachycardia, dyspnea, dizziness,  pancreatic toxicity, hallucinations,  arrhythmias

Pneumocystosis by P jiroveci, early hemolymphatic stage of Trypanosomiasis (Sleeping Sickness), Leishmaniasis

Unknown

GI symptoms, arrhythmias

1^st line agents for cutaneous and visceral leishmaniasis

Inhibits the pyruvate-ferredoxin

oxidoreductase pathway

Giardiasis, cryptosporidiosis, H.

pylori, tapeworms, etc.

Unknown

Early: fatigue, seizures, shock, rarely death

Late: neuropathies, chronic diarrhea, agranulocytosis, hemolytic anemia

Early hemolymphatic trypanosomiasis (Sleeping Sickness) – but does not enter CNS

Unknown

Binds essential thiol groups, preventing trophozite multiplication (?)

Extremely toxic: Reactive encephalopathy --> (cerebral edema, seizures, coma, death)

Renal & cardiac disease

Advanced CNS trypanosomiasis

Inhibitor of ornithine decarboxylase

Depilatory, anemia, seizures thrombocytopenia, leukopenia,

Advanced West afrcian trypanosomiasis, but not effective for East african disease

Metabolized to reactive oxygen

Species (?)

Seizures, neuropathies, insomnia,

restlessness

American trypanosomiasis (Chagas’ disease)