ANTI-PARASITIC DRUGS

name anti-malarials primaquine (PO, IV) chloroquine (PO, IV) mech tissue schizonticide: kills liver schizonts of P. vivax, P. ovale blood schizonticide: kills RBC forms of plasmodia use liver stage of P. vivax, P. ovale use with chloroquine treatment, prophylaxis of P. falciparum, P. malariae use with primaquine for P. vivax, P. ovale amebic liver abscesses chloroquine-res P. falciparum adverse effects hemolytic anemia w/G6PD-def X pregnancy visual: color vision changes, central vision loss, potentially permanent visual damage pruritis hemolytic anemia w/G6PD-def X pregnancy cinchonism (tinnitus, vertigo, visual disturbance, N/V/d, h/a, fever) hemolytic anemia w/G6PD-def arrhythmias blackwater fever (rare): massive lysis of RBCs, dark urine

quinine (PO, IV, IM)

kills RBC, gametocyte forms

mefloquine (PO) pyrimethamine/sulfadoxine

kills RBC forms inhibits TH4 synthesis (like TMP, dapsone, MTX): block purine, DNA synthesis inhibits 30s ribosomal subunit

chloroquine-resistant P. falciparum prophylaxis for chloroquine-resistant regions chloroquine-resistant P. falciparum

doxycycline

prophylaxis

phototoxicity, nausea stains teeth, inhibits bone growth in children < 8 yrs X children, pregnancy

anti-protozoal metronidazole

forms toxic metabolites

trimethoprim/sulfamethoxazo le pentamidine (IV, aerosol)

inhibit THF synthesis

amebiasis Giardia lamblia Entamoeba histolytica Trichomonas vaginalis anaerobic bacteria: bacteroides, clostridia gardnerella, H. pylori pneumocystis carinii: prophylaxis, treatment; 1st line cyclospora, isospora pneumocystis: 2nd line, prophylaxis alternative to suramin for African sleeping sickness toxoplasma gondii leishmania: cutaneous, mucocutaneous, visceral (Kala-Azar) leishmania African sleeping sickness (Trypanosome brucei) WITHOUT neurologic involvement African sleeping sickness WITH neurologic involvement Chagas: American Trypanosome cruzi

metallic taste disulfram-like effect with EtOH

macrocytic anemia: Rx with folate

pyrimethamine + sulfadiazine stilbogluconate antimony suramin (IV) melarsoprol nifurtimox

inhibit THF synthesis arsenic ? does not enter CNS arsenic, binds sulfhydryl groups enters CNS generates oxygen radicals

pancreatic -cell dysfunction with hypoglycemia nephrotoxicity hypotension BMS: Rx with folinic acid

allergy, GI, CNS

quinacrine

block phospholipase A2, ACh receptors

giardia lamblia