DA DRUGS

Question 1

What is the MoA of metronidazole and tinidazole?

Answer 1

Broken down to free radicals –> breakup DNA strands

Question 2

What is the distribution of metronidazole and tinidazole?

Answer 2

Tissue anti-parasitic
Low concentration in the intestine
High bioavailability

Question 3

What do metronidazole and tinidazole treat?

Answer 3

Giardiasis, amebic dysentery, and anaerobic GI bacteria

NOT cyrptosporidium

Question 4

What are the potential toxic effects of metronidazole and tinidazole?

Answer 4

Disulfiram reaction
Nausea, diarrhea, metallic taste
Disturb normal GI flora

Question 5

What is the MoA of iodoquinol?

Answer 5

Unknown…and not just by me…

Question 6

What is the distribution of iodoquinol?

Answer 6

Not well absorbed…works well locally on protozoa including cysts in the GI tract

Luminal anti-parasitic

Question 7

What is iodoquinol used to treat?

Answer 7

Amebic dysentery

Question 8

What are the potential toxicities of iodoquinol?

Answer 8

Loss of visual acuity

Possible thyroid effects

Question 9

What is the MoA of paromomycin?

Answer 9

Inhibits 30S subunit of ribosome…it is an aminoglycoside

Question 10

What is the distribution of paromomycin?

Answer 10

Minimal absorption after oral administration

Luminal anti-parasitic

Question 11

What does paromomycin treat?

Answer 11

Intestinal protozoa

Only partially against cryptoporidium

Question 12

What are some possible toxicities of paromomycin?

Answer 12

Diarrhea

Other GI effects…including issues with intestinal flora

Question 13

What is the MoA of TMP-SMX?

Answer 13

Inhibits folate formation

Question 14

What does TMP-SMX treat?

Answer 14

Many bacteria (broad spectrum)
Protozoans (Toxoplasma, Cystoisospora, Cyclospora)

Question 15

What are the potential toxicities of TMP-SMX?

Answer 15

Crosses BBB
Potentially interferes with intestinal flora
Harms developing fetus…DON’T give to PREGO

Question 16

What is the MoA of nitazoxanide?

Answer 16

Interferes with pyruvate::ferredoxin oxidoreductase enzyme dependent electron transfer

Essential to anaerobic energy metabolism protein

Question 17

What is the distribution of nitazoxanide?

Answer 17

Metabolized to tizoxanide

No parent compound in plasma

Question 18

What is nitazoxanide used to treat?

Answer 18

Giardiasis and cryptosporidiosis (kinda)

Also give anti-perstaltic agent (loperamide) and oral rehydration is important

Question 19

Why isn’t nitazoxanide really used to treat cryptosporidiosis?

Answer 19

cryptosporidiosis isn’t usually treated in immunocompetent people…and nitazoxanide does not really work in immunosuppressed people

Question 20

What are some possible toxicities of nitazoxanide?

Answer 20

Abdominal pain
Diarrhea
Headaches

Question 21

What is the MoA of albendazole and mebendazole?

Answer 21

Bind to beta-tubulin…no microtubule formation

May take multiple doses/couple of days

Question 22

What is the distribution of albendazole and mebendazole?

Answer 22

Limited oral absorption

Albendazole is better if trying to kill tissue-migrating larvae

Question 23

What are albendazole and mebendazole used to treat?

Answer 23

Roundworms

Tapeworms

Question 24

What is the MoA of pyrantel and lavamisole?

Answer 24

Activate ACh receptors…cause spastic contractions causing parasite to lose grip and get swept away

Question 25

What is the distribution of pyrantel and lavamisole?

Answer 25

Luminal...poorly absorbed

Question 26

What are pyrantel and lavamisole used to treat?

Answer 26

Roundworms Pyrantel does NOT work against whipworm

Question 27

What is the MoA of ivermectin?

Answer 27

Activates glutamate gated chloride channels

Question 28

What is the distribution of ivermectin?

Answer 28

Doesn't cross BBB...which is good because we have those same channels in our CNS

Question 29

What can lead to resistance to ivermectin?

Answer 29

Efflux transporters

Question 30

What is ivermectin used to treat?

Answer 30

Nematodes (ascaris, strongloides**, and onchocerca)

Question 31

What are the possible toxicities of ivermectin?

Answer 31

``` Generally well tolerated, but: Possible itching Swollen lymph glands Rarely dizziness Inflammation (d/t rxn to death of adult worms) ```

Question 32

What is the MoA of praziquantel?

Answer 32

Increased permeability to divalent cations (calcium??) leading to contraction of the worm's musculature

Question 33

What is praziquantel used to treat?

Answer 33

Cestodes | Trematodes** (Schistosoma)

Question 34

What are some possible toxicities to praziquantel?

Answer 34

Generally well tolerated, but: Possible dizziness Possible nausea