antiparasitics Flashcards
metronidazole- MOA
•Pro-drug targets enzyme unique to the parasite. Active form is free radical that damages DNA and causes oxidative stress that kills parasite.
metronidazole uses
GET GAP: giardia, entamoeba, trichomonas, gardnerella vaginalis, anaerobes (bacteroides, C. diff), H. Pylori. It doesn’t reach lumen so better for systemic dz. Can use with lumenal amebicide (paromomycin/ diloxanide) for amebiasis.
Metronidazole adverse rxns/ contraindications
disulfiram like rxn with alcohol (flushing, tachycardia, hypotension), headache, metallic taste. Contraindicated in hepatic dz, renal dz, CNS abnormalities
Paromomycin- MOA, uses
aminoglycoside Abx (inhibits 30S).Concentrates in parasite in the gut. Little systemic absorption. Uses: asymptomatic lumenal amebiasis, cryptosporidiosis (AIDS), visceral and cutaneous Leishmanias.
Toxoplasmosis treatment
Pyrimethamine + sulfadiazine (or clindamycin if sulfa allergy). Pyrimethamine targets dihydrofolate reductase and sulfadiazine targets dihydropteroic synthase, blocking folic acid synthesis and thus nucleic acid and protein synthesis
Pneumocystis jirovecii treatment
TMP-SMX
Pentamide MOA
disrupts DNA structure/ function (inhibits SAM decarboxylase), inhibits protein synthesis (binds minor groove of DNA), inhibits DNA replication (type II topoisomerase)
Pentamide uses
PCP pneumonia alternative to TMP-SMX, West African Trypanosomiasis (T. brucei gambiense), Visceral Leishmanias
Pentamide adverse rxns
histamine release (dying orgnaisms), drop in BP, hypoglycemia, elevates LFTS, impaired renal function. Few side effects when inhaled for PCP
Benzimidazoles MOA
inhibit microtubule formation - selectively binds to parasite tubulin.
Benzimidazoles uses
Mebendazole: nematodes - enterobiasis (pinworm), ascariasis, trichuriasis (whipworm), hookworm. Albendazole: nematodes- ascariasis, enterobiasis, hookworm. Invasive cestodes- cystic hydatid dz, cysticercosis (pork tapeworm).
mebendazole vs albendazole
mebendazole: poor absorption, excreted in bile, uncomplicated nematode infections. Albendazole better absorption, excreted in urine, cysticercosis, used in kids >4yrs. Both are teratogens
Pyrantel Pamoate MOA
concentrates in parasite- Ach receptor agonists cuases complete spastic paralysis of worm.
Pyrantel Pamoate uses
ascariasis (roundworm), enterobiasis (pinworm) DOC, hookworms
Pyrantel Pamoate contraindications
liver dysfunction.
Praziquantel MOA
Ca2+ ionophore - induces paralysis, detachment, excretion. Induces tegmental damage - activates immune system