DA DRUGS Flashcards
What is the MoA of metronidazole and tinidazole?
Broken down to free radicals –> breakup DNA strands
What is the distribution of metronidazole and tinidazole?
Tissue anti-parasitic
Low concentration in the intestine
High bioavailability
What do metronidazole and tinidazole treat?
Giardiasis, amebic dysentery, and anaerobic GI bacteria
NOT cyrptosporidium
What are the potential toxic effects of metronidazole and tinidazole?
Disulfiram reaction
Nausea, diarrhea, metallic taste
Disturb normal GI flora
What is the MoA of iodoquinol?
Unknown…and not just by me…
What is the distribution of iodoquinol?
Not well absorbed…works well locally on protozoa including cysts in the GI tract
Luminal anti-parasitic
What is iodoquinol used to treat?
Amebic dysentery
What are the potential toxicities of iodoquinol?
Loss of visual acuity
Possible thyroid effects
What is the MoA of paromomycin?
Inhibits 30S subunit of ribosome…it is an aminoglycoside
What is the distribution of paromomycin?
Minimal absorption after oral administration
Luminal anti-parasitic
What does paromomycin treat?
Intestinal protozoa
Only partially against cryptoporidium
What are some possible toxicities of paromomycin?
Diarrhea
Other GI effects…including issues with intestinal flora
What is the MoA of TMP-SMX?
Inhibits folate formation
What does TMP-SMX treat?
Many bacteria (broad spectrum) Protozoans (Toxoplasma, Cystoisospora, Cyclospora)
What are the potential toxicities of TMP-SMX?
Crosses BBB
Potentially interferes with intestinal flora
Harms developing fetus…DON’T give to PREGO
What is the MoA of nitazoxanide?
Interferes with pyruvate::ferredoxin oxidoreductase enzyme dependent electron transfer
Essential to anaerobic energy metabolism protein
What is the distribution of nitazoxanide?
Metabolized to tizoxanide
No parent compound in plasma
What is nitazoxanide used to treat?
Giardiasis and cryptosporidiosis (kinda)
Also give anti-perstaltic agent (loperamide) and oral rehydration is important
Why isn’t nitazoxanide really used to treat cryptosporidiosis?
cryptosporidiosis isn’t usually treated in immunocompetent people…and nitazoxanide does not really work in immunosuppressed people
What are some possible toxicities of nitazoxanide?
Abdominal pain
Diarrhea
Headaches
What is the MoA of albendazole and mebendazole?
Bind to beta-tubulin…no microtubule formation
May take multiple doses/couple of days
What is the distribution of albendazole and mebendazole?
Limited oral absorption
Albendazole is better if trying to kill tissue-migrating larvae
What are albendazole and mebendazole used to treat?
Roundworms
Tapeworms
What is the MoA of pyrantel and lavamisole?
Activate ACh receptors…cause spastic contractions causing parasite to lose grip and get swept away
What is the distribution of pyrantel and lavamisole?
Luminal…poorly absorbed
What are pyrantel and lavamisole used to treat?
Roundworms
Pyrantel does NOT work against whipworm
What is the MoA of ivermectin?
Activates glutamate gated chloride channels
What is the distribution of ivermectin?
Doesn’t cross BBB…which is good because we have those same channels in our CNS
What can lead to resistance to ivermectin?
Efflux transporters
What is ivermectin used to treat?
Nematodes (ascaris, strongloides**, and onchocerca)
What are the possible toxicities of ivermectin?
Generally well tolerated, but: Possible itching Swollen lymph glands Rarely dizziness Inflammation (d/t rxn to death of adult worms)
What is the MoA of praziquantel?
Increased permeability to divalent cations (calcium??) leading to contraction of the worm’s musculature
What is praziquantel used to treat?
Cestodes
Trematodes** (Schistosoma)
What are some possible toxicities to praziquantel?
Generally well tolerated, but:
Possible dizziness
Possible nausea
