Drugs for Amebiasis - Chapter 52 review part2

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Drugs for Amebiasis - Chapter 52 review part2
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2013-02-24 19:33:46
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Antiprotozoal Amebiasis amebicides pharmacology
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Antiprotozoal Part2 (Drugs for Amebiasis) - Chapter 52
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  1. What are Tissue amebicides?
    Drugs that act on organisms in the bowel wall and the liver.
  2. What are Luminal amebicides?
    Drugs that act only in the lumen of the bowel.
  3. Name the 3 Tissue amebicides.
    • chloroquine,
    • emetines,
    • metronidazole
  4. Name the 3 Luminal amebicides
    • diloxanide,
    • iodoquinol,
    • paromomycin
  5. What is the brand name for METRONIDAZOLE?
    FLAGYL
  6. METRONIDAZOLE - MOA
    Mechanism of Action

    –Undergoes reductive bio-activation of its nitro group by ferredoxin to form reactive cytotoxic products that interfere with nucleic acid synthesis
  7. METRONIDAZOLE - Indications
    • Pseudomembranous colitis,
    • amebiasis,
    • trichomoniasis,
    • Non-specific vaginitis
  8. METRONIDAZOLE - Adverse effects
    • GI irritation,
    • headache,
    • disulfiram reaction with EtOH,
    • metallic taste in mouth
  9. METRONIDAZOLE - Interactions
    potentiates Warfarin
  10. CHLOROQUINE - Indications
    • Reaches high liver concentrations and may
    • be used for amebic abscesses that fail to respond to metronidazole
  11. EMETINES - MOA
    Mechanism of action

    • Emetine and dehydroemetine
    • inhibit protein synthesis by blocking ribosomal movement along messenger RNA
  12. EMETINES - Indications
    is limited to unusual circumstances of severe amebiasis in which metronidazole cannot be used
  13. EMETINES - Contra
    • Hypersensitivity,
    • cardiac,
    • renal dz
  14. EMETINES - Adverse Effects
    • GI distress,
    • diarrhea,
    • muscle weakness,
    • heart failure and hypo-tension.
  15. EMETINES - Drug interactions
    Additive cardiac depressant effects with beta blockers
  16. DILOXANIDE FUROATE - Indication
    Intestinal amebiasis
  17. DILOXANIDE FUROATE - Contraindications
    –Pregnancy
  18. DILOXANIDE FUROATE - Adverse effects
    • Flatulence,
    • nausea,
    • abdominal cramps
  19. IODOQUINOL - Indication
    –intestinal amebiasis
  20. IODOQUINOL - Contraindications
    –use with caution in patients with optic neuropathy, thyroid or renal disease
  21. IODOQUINOL - Adverse effects
    NVD
  22. IODOQUINOL - •Drug interactions
    –increases protein-bound iodine which causes a decrease in measured 131 I uptake

    –Would interfere with thyroid scan
  23. PAROMOMYCIN - MOA
    • aminoglycoside antibiotic,
    • inhibits protein synthesis
  24. PAROMOMYCIN - Indications
    –Intestinal amebiasis
  25. PAROMOMYCIN - Contraindications
    –renal insufficiency
  26. PAROMOMYCIN - Adverse effects
    –diarrhea
  27. NITAZOXANIDE - MOA
    Mechanism of action

    interferes with the pyruvate-ferredoxin oxidoreductase enzyme dependent electron transfer which is essential for anaerobic energy metabolism
  28. NITAZOXANIDE - Indications
    • Giardia lamblia,
    • Cryptosporidium parvum
  29. NITAZOXANIDE - Adverse effects
    • headache,
    • bright yellow urine,
    • abdominal pain,
    • yellow sclerae
  30. Name 3 drugs for treatment of
    PNEUMOCYSTOSIS AND TOXOPLASMOSIS.
    • Pentamidine,
    • TMP-SMX (Bactrim),
    • Pyrimethamine/Sulfadiazine
  31. PENTAMIDINE - MOA
    Mechanism of action

    –interference with nucleic acid metabolism
  32. PENTAMIDINE - Indications
    –Treatment and prevention of pneumonia caused by Pneumocystis jiroveci in patients who fail to respond to TMP-SMX. 

    –Treatment of African trypanosomiasis. 

    –Treatment of visceral leishmaniasis
  33. PENTAMIDINE - Adverse effects
    • hypotension,
    • tachycardia,
    • nephrotoxicity
  34. PENTAMIDINE - Interactions
    • Use with aminoglycosides increases risk of nephrotoxicity,
    • use with didanosine increases risk of pancreatitis
  35. PENTAMIDINE - Alternative use?
    • Used as alternative to suramin for the early hemolymphatic stage of African trypanosomiasis,
    • Used as alternative to sodium stibogluconate for the treatment of visceral leishmaniasis
  36. What is another name for hemolymphatic
    East African Trypanosomiasis?
    – African sleeping sickness
  37. What drugs will treat African sleeping sickness?
    • Suramin,
    • Pentamidine (alternative to Suramin)
  38. TMP-SMX - MOA
    Mechanism of action

    –Sequential blockade of folate production
  39. TMP-SMX - DOC
    Drug of choice for treatment and prevention of    pneumocystis pneumonia
  40. TMP-SMX - Contraindications
    –sulfa allergy
  41. TMP-SMX - Adverse effects
    • GI distress,
    • rash,
    • fever,
    • neutropenia,
    • thrombocytopenia
  42. TMP-SMX - Drug interactions
    –TMP-SMX decreases the clearance of warfarin.
  43. Brand name for TMP-SMX.
    - Biaxin
  44. PYRIMETHAMINE/SULFADIAZINE - MOA
    Mechanism of action

    –Sequential blockade of folate synthesis
  45. PYRIMETHAMINE/SULFADIAZINE - •Indications
    • DOC for prophylaxis of Toxoplasmosis,
    • Alternative to TMP/SMX or pentamidine for
    • prophylaxis against pneumocystis pneumonia in AIDS patients,
    • Treatment of active toxoplasmosis.
  46. PYRIMETHAMINE/SULFADIAZINE,
    Adverse effects
    • Gastric irritation,
    • headache,
    • insomnia,
    • tremors,
    • megaloblastic anemia
  47. PYRIMETHAMINE/SULFADIAZINE - Contra
    Hypersensitivity
  48. SODIUM STIBOGLUCONATE - Indications
    First-line treatment of cutaneous and visceral leishmaniasis.
  49. SODIUM STIBOGLUCONATE - Contraindications
    –long QT syndrome
  50. SODIUM STIBOGLUCONATE - Toxicity
    • GI distress,
    • fever,
    • headache,
    • myalgia,
    • rash
  51. SODIUM STIBOGLUCONATE - Interactions
    Cisapride also prolongs QT interval
  52. Suramin - Adverse effects
    • fatigue,
    • nausea,
    • seizures,
    • shock,
  53. Suramin - Indications
    - treats early hemolymphatic East African Trypanosomiasis (aka African sleeping sickness)

    • *Does not enter the CNS so not used for
    • advanced disease
  54. Melarsoprol - MOA / Composition
    - Arsenical compound
  55. Melarsoprol - Indication
    • First line therapy for advanced CNS East African Trypanosomiasis,
    • Secondline therapy for advanced West African Trypanosomiasis
  56. Melarsoprol - Adverse effects
    • Immediate Adverse effects -
    • Fever, vomiting, abdominal pain, joint pain.

    • –Later…Reactive encephalopathy within
    • the first week of treatment.

    **Extremely toxic - arsenical
  57. Eflornithine - MOA
    Mech of action

    – inhibits ornithine decarboxylase
  58. Eflornithine - Indication
    First line therapy for advanced West African Trypanosomiasis
  59. Eflornithine - Adverse effects
    • diarrhea,
    • vomiting,
    • anemia,
    • thrombocytopenia,
    • leukopenia,
    • and seizures
  60. Nifurtimox - MOA
    Mech of action 

    interacts with parasitic nucleic acid, inhibits trypanothione reductase (a parasite specific antioxidant defense enzyme)
  61. Nifurtimox - Indication
    treatment of American trypanosomiasis (Chagas disease)
  62. Miltefosine - Indication
    First effective oral agent for visceral leishmaniasis
  63. Miltefosine - Adverse effects
    • vomiting,
    • diarrhea,
    • transient elevation of LTFs.
  64. Miltefosine - Contraindications
    Avoid in pregnancy

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