Other protozoal drugs

Question 1

Metronidazole

Answer 1

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Prodrug actives nitro group to radical which then binds DNA
——
-Trichomoniasis
-amebiasis
-giardiasis
——–
-Rare neurotoxicity (ataxia)
-teratogenic

Question 2

Tinidazole

Answer 2

Same MOA as metronidazole but can be used in pregnancy

Question 3

Iodoquinol

Answer 3

/
-MOA unknown but does bind metals
——–
-E. Histolytica
——-
-optic atrophy leading to permanent loss of vision

Question 4

Paromomycin

Answer 4

amino glycoside
-irreversibly binds 30S subunit trapping AUG
——–
-cyptosporidiosis, giardiasis, trichomoniasis
——-
-Nephrotoxicity
-ototoxicity

Question 5

Nitazoxanide

Answer 5

Prodrug for tizoxanide
-inhibits PFOR preventing energy metabolism
——
-giardiasis
-cryptosporidiosis
—–
-headache
-GI upset

Question 6

Sulfamethoxazole/trimethoprim

Answer 6

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folic acid inhibitors
——-
-toxoplasmosis
-pneumocystis pneumonia

Question 7

Suramin

Answer 7

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Binds plans proteins and enters parasite to inhibit enzymes
——-
-Early stage ASS
——–
-Renal toxicity
-Leukopenia if also has AIDS

Question 8

Pentamidine

Answer 8

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enters via ATPase then inhibits transcription and translation
——
-Early stage ASS
——
-hypoglycemia

Question 9

Melarsoprol

Answer 9

/
arsenic like prodrug of melarsen oxide which binds to sulfhydryl groups inhibiting enzymes
——–
-late stage ASS
———
-highly toxic
-encephalopathy
-imediate fatality

Question 10

Eflornithine

Answer 10

/
inhibits ODC irreversibly to inhibit polyamides for replication
——-
-late stage ASS
——-
-abdominal pain
-seizures

Question 11

Nifutimox

Answer 11

/
Nitrofuran analog activated by nitro reductases in mito increasing radicals to kill
——-
-Chagas disease
——–
-GI upset

Question 12

Benznidazole

Answer 12

/
Nitroimidazole analog activated by nitro reductases in mito increasing radicals to kill
——
-Chagas disease
——
-GI upset