Microbiology Antiparasitic Drugs

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Melarsoprol

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Trivalent arsenic - inactivates sulhydryl groups of enzymes involved in carbohydrate metabolism.

Used for trypanosomiasis in CNS; can penetrate blood-brain barrier and is active against all stages of trypanosomiasis

Effects host neuronal, renal tubular, intestinal, & bone marrow stem cells

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Sodium stibogluconate, meglumine antimonate

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Antimonials - inactivates sulhydryl groups of enzymes involved in carbohydrate metabolism.
Used for LEISHMANIASIS
Toxicity similar to arenicals

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Chloroquine phosphate

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Antimalarial quinolines: accumulates in parasitized host cells (RBC) & blocks DNA synthesis, and kills the schizonts
For prophylaxis and Rx of all Plasmodium species.
P. falciparum resistance in Asia, Africa, South America.

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Primaquine

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Antimalarial quinolines: accumulates in parasitized host cells (RBC) & blocks DNA synthesis
Used to eradicate hepatic parasites.
May cause hemolytic anemia in patients with G6PDH deficiency; severe if Mediterranea/Far Eastern ancestry, mild in blacks

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Quinine

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Most toxic antimalarial quinolines: accumulates in parasitized host cells (RBC) & blocks DNA synthesis.
Used to Rx CHLOROINE-RESISTANT P. Falciparum & P. vivax; used with sulfonamide/tetracycline

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Mefloquine

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Antimalarial quinolines: accumulates in parasitized host cells (RBC) & blocks DNA synthesis
Used against chloroquine resistant strains
P. falciparum strains in SE Asia may also show some resistance

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Sulfonamide

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Folic acid antagonist - inhibits conversion of aminobenzoic acid to dihydropteroic acid.
Protozoa unable to absorb exogenous folate

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Trimethoprim

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Diaminopyrimidine - inhibits dihydrofolate reductase, blocking synthesis of THF that would form purine, pyrimidine, certain AA.
Used with sulfamethoxazole to treat toxoplasmosis

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Pyrimethamine

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Diaminopyrimidine - inhibits dihydrofolate reductase, blocking synthesis of THF that would form purine, pyrimidine, certain AA.
Used with sulfamethoxazole to treat malaria and toxoplasmosis

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Clindamycin

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Protein synthesis inhibitor. Active against Plasmodium species, Babesia species, amebas, and Toxoplasma species

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Tetracycline

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Protein synthesis inhibitors. Used for chemoprophylaxis and treatment of chloroquine-resistant P. falciparum malaria;
use in combo with quinine

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Paramomycin

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Protein synthesis inhibitor - aminoglycoside. Used to treat cryptosporidiosis

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Metronidazole

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Nitroimidazole - inhibits DNA synthesis; unclear mechanism.
Effective for treatment of disseminated amebiasis, giardiasis; drug of choice for trichomoniasis

Trichomonas Vaginalis - CAREFUL NOT TO USE DURING 1st TRIMESTER

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Thiabendazole

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Benzimidazole - broad-spectrum antihelminthic agents (inhibits fumarate reductase; distrupts microtubular function; inhibits glucose functions).
Active against larval & adult nematodes

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Mebendazole

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Benzimidazole - broad-spectrum antihelminthic agents (inhibits fumarate reductase; distrupts microtubular function; inhibits glucose functions).
Activate against several intestinal nematodes (E. vermicularis, T. trichuria, Ascaris, N. Americanis, Trichinella Spiralis,

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Albendazole

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Benzimidazole - broad-spectrum antihelminthic agents (inhibits fumarate reductase; distrupts microtubular function; inhibits glucose functions).
Activate aginst NEMATODES (all); also certain protozoa

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Ivermectin

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Avermectins - Causes neruomuscular paralysis of nematode parasites, by influencing nematode neurotransmitter

(S. Stercoalis)

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Praziquantel

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Calcium agonist - causes helminths to undergo tetanic conraction; distrupts parasite surface & tegument) - activate against broad spectrum of trematodes & cestodes;
drug of choices for Rx of schistosomiasis & neurocysticercosis (Taenia Solium)