Anti-Protozoal Drugs Flashcards
Metronidazole
Anti-protozoal
DOC for E. histolytica, G. lamblia, T. vaginalis
- Can also be used for Bacteriodes fragilis, and Clostridum difficle, and non-specific BV or vaginitis
MOA:
- In anaerobic- converted to active metabolite that binds to protein and disrupts cellular processes
- Can interact directly with the parasite DNA
* NOT effective against luminal parasites - must be used with luminal amebicide
PK
- oral, topical
- metabolized by the liver (drug interaction) (caution in liver disease)
- effective for intestinal and extra-intestinal parasites
Toxicities
- Alcohol- disulfuram like effects
- GI effects
- reddish colour of urine
- Teratogenic
Tinidazole
Anti-protozoal
indicated for E. histolytica, G. lamblia, T. vaginalis
MOA: same as metronidazole but better toleratured
* NOT effective against luminal parasites - must be used with luminal amebicide
Iodoquinal
Anti-protozoal
Luminal Amebicide-
- effective against trophozites and cysts of E. histolytica
- used in combo with Metronidazole to tx amebic infections
- used is asymptomatic amebiasis
PK: Poorly absorbed from GI tract - most of drug excreted in feces
SE:
- rare and due to iodine content
- iodine content- thyroid enlargement
- blindness via optic neuritis, optic atrophy
- skin reactions, HA/D
Paromomycin
Anti-protozoal Tx amebiasis, giradiasis, T. vaginalis effective against luminal trophozoites Use in asymptomatic amebiais PK: Oral and cream aminoglycoside antibiotic SE: - GI upset
Diloxanide Furoate
Anti-protozoal Effective against luminal trophozites but not tissue trophozites Used in combo with metronidazole MOA: UNKNOWN SE: flatulence, N/V/, urticaria, rash
Emetine and Dehydroemetine
Anti-protozoal
Alternative to Metronidazole for severe intesting or systemic E. histolytica infections
PK:
parenterally
SE:
-pain, tenderness, weakness at injection site
- serious cardiotoxicity (prolong all intervals)
- GI toxicity
- Teratogenic
Tetracycline
Anti-protozoal
Kill the bacterial which G. lamblia and E. histolytica require for life
Used as alternative for tx for amebiasis and girardia
Pyrimethamine with Sulfadiazine and Folinic Acid
Anti-protozoal
DOC for toxoplasmosis
Trimethoprim with Sulfamethoxazole (Bactrim)
Anti-protozoal DOC for pneumocytosis Alternative for toxoplasmosis Prophylaxsis for P. carinii in AIDs pts SE: - rash, prurities, cytopenias, and AST/ALT elevations
Pentamidine
Anti-protozoal Effective against P. carinii- alternative to TMP/SMX (pts who cant tolerate TMP/SMX) Used to tx active infection Nebulizer for prophylaxis MOA: inhibit DNA replication PK: IM injection or neublizer SE: - hypotension - arrhythmia - hypoglycemia
Pyrantel Pamoate
Round worm - Broad spectrum agent effective against a variety of nematodes - alternative to mebendazole - oral MOA: cholinesterase inhibitor - produces depolarizing NM blockade in worm - SE: - very little because not absorbed - dizziness, HA, and drowziness
Ivermectin
Round worm drug
DOC for filaria infestation
Effective against a variety of nematodes as well as insects and acraine parasites, also for threadworms, roundworm, and cutaneous larva migrans
MOA: paralzyes the parasite, intensifies GABA- mediated transmission of signals in peripheral nerves
PK: rapidly absorbed, wide tissue distribution, fecal excretion
SE: minimal, pruritis, tender LN and fever
Praziquantel
Tapeworms and Flukes
DOC for all sp. of shistosomes
Effective against Cestodes, trematodes
Effective in tx of nyerocyscticercosis
Well absorbed in GI - can be used for systemic infections
MOA: inc. the worms permeability to Ca2+, resulting in contraction and then paralysis of the worms muscles
SE:
- few SE, N/V and ab discomfort from release of dead worms proteins
Bithionol
Tapeworms and flukes
Active against flukes- liver and lung flukes
MOA: uncouples Oxidative phosphorylation
PK: oral, absorbed from the GI tract
SE: mild N/V/HA/D dizziness, urticaria, and rash
