pharm Antiparasitics by drugs only

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pharm Antiparasitics by drugs only
2012-05-05 20:33:13
antiparasitics drugs

antiparasitic drugs
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  1. Metronidazole
    • Use: E. histolytica, T. vaginalis, G. lamblia, and anaerobic bacteria
    • Mechanism: prevents terminal electron transport system from re-oxidizing NADH and NADPH
    • Pharmacology: good GI absorption; eliminated by kidneys; disulfiram like effects when taken with alcohol; do not use in pregnancy
  2. Iodoquinol
    • Uses: E. histolytica (only intestinal amebiasis)
    • Mechanism: liberated iodine, an amebicide
    • Pharmacology: not absorbed in GI tract; high dose can cause loss of visual acuity, optical atrophy, and blindness
  3. Paromomycin
    • Use: intestinal amebiasis and some intestinal cestode infections
    • Mechanism: aminoglycoside antibiotic - inhibits protein synthesis
    • Pharmacology: poorly absorbed in the intestine; can mess with gut flora and cause superinfection
  4. Nitazoxanide
    • Uses: giardiasis, cryptosporidiosis, and possibly amebiasis, I. belli, and some helminths
    • Mechanism: inhibits parasite pyruvate-ferredoxin (but different than metronidazole)
    • Pharmacology: Absorbed in GI tract; prodrug (active species is tizoxanide); mild side effects; no known drug interactions; safety in pregnancy not shown
  5. TMP/SMX
    • Uses: Cyclospora, Isospora belli, Pneumocystis jiroveci, toxoplasmosis prophylaxis
    • Mechanism: sequential blockade of folate synthesis
    • Pharmacology: Good tissue distribution (including CNS and prostate); not safe in pregnancy; patients with AIDS have a higher incidence of adverse effects
  6. Pyrimethamine + sulfadiazine
    • Uses: toxoplasmosis
    • Mechanism: folate antagonist
    • Pharmacology: must administer with folinic acid suplements; not safe in pregnancy
  7. Pentamidine
    • Uses: Trypanosomiasis gambiense, Leishmania donovani (kala azar), Pneumocystis jiroveci
    • Mechanism: selective breaks in the kinetoplast DNA
    • Pharmacology: not well absorbed from GI (give IM or IV); does not penetrate CNS; many toxic side effects including direct toxicity to beta islet cells
  8. Eflornithine
    • Uses: late stage trypanosomiasis
    • Mechanism: suicide inhibitor of ornithine decarboxylase (required for DNA synthesis)
    • Pharmacology: generally well tolerated and effective
  9. Mebendazole
    • Uses: whipworm, ascariasis, capillariasis, hookworm, visceral larval migrans, mixed infections of whipworm with Ascaris and/or pinworm
    • Mechanism: inhibition of microtubule polymerization by binding to beta-tubulin
    • Pharmacology: broad spectrum; virtually atoxic; can kill nematode eggs; poor GI absorption; contraindicated in pregnancy
  10. Albendazole
    • Uses: broad spectrum against intestinal helminths and neurocysticercosis
    • Mechanism: inhibition of microtubule polymerization by binding to beta-tubulin
    • Pharmacology: contraindicated in cirrhosis, pregnancy, and infants
  11. Pyrantel pamoate
    • Uses: pinworm and hookworm
    • Mechanism: depolarizing muscular blocker - leads to paralysis of worm and subsequent expulsion
    • Pharmacology: poorly absorbed form GI tract
  12. Diethylcarbamazine
    • Uses: both forms of W. bancrofti and Loa loa, but only the microfilariae of O. volvulus
    • Mechanism: unknown
    • Pharmacology: readily absorbed from GI tract; side effects from worm destruction; pre-treat with anti-histamines
  13. Ivermectin
    • Uses: O. volvulus, W. bancrofti, B. malayi, Strongyloides, Ascaris, Enterobius, and Trichuris
    • Mechanism: hyperpolarization via chloride ion influx resulting in muscle paralysis
    • Pharmacology: milder symptoms than DEC; side effects due to worm destruction; CNS toxicity at high doses
  14. Praziquantel
    • Uses: Broad spectrum anti-schistosomal as well as some anti-trematode and anti-cestode activity
    • Mechanism: increases worm's permeability to calcium ions leading to vacuolization, contraction, and paralysis
    • Pharmacology: mild and transient side effects