Antihelmenthic Drugs - Chapter 53 review

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Antihelmenthic Drugs - Chapter 53 review
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2013-02-24 19:07:02
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Antihelmenthic Pharmacology
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Antihelmenthic Drugs - Chapter 53 review
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  1. ALBENDAZOLE - MOA
    inhibits microtubule synthesis in nematodes, thus irreversibly impairing glucose uptake.
  2. ALBENDAZOLE - Indication
    approved for the treatment of hydatid disease and cysticercosis.

    also used for pinworms, Ascariasis, trichuriasis, strongyloidiasis, and hookworms.

    **Broad spectrum antihelmenthic
  3. ALBENDAZOLE - Contraindications
    Relatively contraindicated in pregnancy
  4. ALBENDAZOLE - Adverse effects
    - When used for 2-3 days it is nearly free of adverse effects

    • Long-term treatment is associated with:
    • liver toxicity
    • agranulocytosis
    • and pancytopenia
  5. ALBENDAZOLE - Drug interactions
    Dexamethasone, cimetidine, and praziquantel will increase the serum concentration of the active metabolite of Albendazole.
  6. DIETHYLCARBAMAZINE CITRATE - MOA
    Mechanisms of action

    immobilizes microfilariae and alters their surface structure displacing them from tissues and making them more susceptible to destruction by host defenses.
  7. DIETHYLCARBAMAZINE CITRATE - Indications
    DOC for filariasis, loiasis, and tropical eosinophilia
  8. DIETHYLCARBAMAZINE CITRATE

    Adverse Reactions / Toxicity
    • Toxicity
    • –headache, dizziness, nausea, and vomiting.

    • –Adverse reactions also occur as a result of the release of proteins from dying microfilariae or adult worms.
    • (fever, malaise, headache, joint pain)
  9. DIETHYLCARBAMAZINE CITRATE

    Contraindications?
    –use with caution in patients with hypertension or renal disease
  10. IVERMECTIN - MOA
    It intensifies GABA-mediated neurotransmission in nematodes and causes immobilization.
  11. IVERMECTIN - Indications / DOC
    DOC for strongyloidiasis (threadworm) and onchocerciasis (river blindness)

     - alternative treatment for filariasis.

    • Can also be used to control scabies,
    • lice, cutaneous larva migrans, and ascariasis.
  12. IVERMECTIN - Toxicity?
    • Selective toxicity results because in humans, GABA is a neurotransmitter only in the CNS
    • and ivermectin does not cross the blood-brain barrier.
  13. IVERMECTIN - Adverse Reactions / Toxicity
    In onchocerciasis treatment, the Mazzotti reaction occurs which is due to the killing of microfilariae

    Mazzotti reaction - fatigue, dizziness, nausea, and vomiting,  abdominal pain, and rashes.
  14. What drug causes a reaction known as Mazzotti reaction?
    IVERMECTIN
  15. IVERMECTIN - Contraindications
    The drug should not be given to patients with an impaired blood-brain barrier (meningitis and African sleeping sickness).
  16. IVERMECTIN - Drug interactions
    Avoid using with other drugs that enhance GABA transmission such as benzodiazepines, barbiturates, and valproic acid.
  17. MEBENDAZOLE (VERMOX) - MOA
    Inhibits microtubule synthesis in nematodes, thereby irreversibly inhibiting glucose uptake.
  18. MEBENDAZOLE (VERMOX) - Indications
    approved for the treatment of Ascariasis, trichuriasis, hookworm, and pinworms
  19. MEBENDAZOLE (VERMOX) - Contraindication
    –Pregnancy
  20. MEBENDAZOLE (VERMOX) - Toxicity?
    neutropenia and hepatitis when taken for a long period of time
  21. MEBENDAZOLE (VERMOX) - Interactions
    Cimetidine will increase mebendazole levels

  22. Metrifonate - MOA
    • Organophosphate compound,
    • Inhibits acetylcholinesterase,
    • Paralyzes adult worms
  23. Metrifonate - Indication
    Used to treat Schistosoma haematobium
  24. Metrifonate - Side effects
    Cholinergic side effects:

    intestinal cramping, blurred vision, slow heart beat, muscle weakness, muscle cramps, and muscle pain, convulsions, weak breathing, inability to breath, increased stomach acid and saliva, nausea and vomiting, dizziness, drowsiness, and headache
  25. Metrifonate - Contraindications
    • Should not be used in pregnancy or after
    • exposure to insecticides
  26. Niclosamide - MOA
    Mech of action

    – inhibition of oxidative phosphorylation or stimulation of ATPase
  27. Niclosamide - Indications
    Second line treatment for tapeworm infections
  28. Niclosamide - Side effects
    – NVD and abdominal discomfort
  29. Oxamniquine - Indications
    Alternative to praziquantel for Schistosoma mansoni infections
  30. Oxamniquine - Adverse effects
    – dizziness, headache, drowsiness, NVD, abdominal cramps,
  31. Oxamniquine - Contraindication
    pregnancy and HX of seizures
  32. PIPERAZINE - MOA
    Mechanisms of action

    causes paralysis of ascaris by blocking acetylcholine at the myoneural junction
  33. PIPERAZINE - Indications
    Ascariasis

    –Not used for other helminth infections
  34. PIPERAZINE - Contraindications
    • pregnancy,
    • patients with impaired renal or hepatic function
  35. PIPERAZINE - Adverse effects
    • NVD,
    • dizziness,
    • headache
  36. PIPERAZINE - Drug interactions
    Antagonistic with pyrantel pamoate
  37. PRAZIQUANTEL - MOA
    Mechanisms of action

    –Increases the cell permeability to calcium in schistosomes; causes strong contractions and paralysis of worm musculature leading to detachment of suckers from the blood vessel walls and to dislodgement
  38. PRAZIQUANTEL - Indications
    • Schistosomiasis,
    • cysticercosis,
    • intestinal trematodes,
    • and tapeworms

    –FLUKES of ALL kinds
  39. What medicine can cause ocular cysticercosis?
    Praziquantel
  40. What is ocular cysticercosis?
    Ocular cysticercosis result from a worm larvae developing in the eye.
  41. What are the treatment considerations concerning ocular cysticercosis?
    If medication (Praziquantel) is taken for a worm in the eye the inflammatory response to the dead worm is worse than leaving the worm alive.
  42. PRAZIQUANTEL - Contraindications
    • hypersensitivity to the drug,
    • ocular cysticercosis,
    • spinal cysticercosis
  43. PRAZIQUANTEL - Toxicity
    • dizziness,
    • drowsiness,
    • headache,
    • fever.
  44. PRAZIQUANTEL - Interactions
    • Alcohol increases CNS depression,
    • cimetidine increases praziquantel levels
  45. PYRANTEL PAMOATE - MOA
    • Stimulates nicotinic receptors present at
    • neuromuscular junctions of nematodes

    • Contraction of muscles occurs followed by
    • a depolarization-induced paralysis.
  46. PYRANTEL PAMOATE - Indications
    • broad-spectrum anthelminthic for treating pinworms,
    • Ascariasis,
    • and Trichostrongylus orientalis.
  47. PYRANTEL PAMOATE - Toxicity / Adverse effects
    • headache,
    • GI distress,
    • and weakness
  48. PYRANTEL PAMOATE - Contraindications
    relatively contraindicated in pregnancy and liver disease
  49. PYRANTEL PAMOATE - Drug Interactions
    piperazine antagonizes the effect of pyrantel pamoate.
  50. THIABENDAZOLE - Indications
    • strongyloidiasis, cutaneous larva migrans,
    • visceral larva migrans, dracunculosis,
    • trichinosis, and mixed helminthic infections
  51. THIABENDAZOLE - Contraindications
    –pregnancy
  52. THIABENDAZOLE - MOA
    Mechanisms of action

    –inhibits helminth-specific mitochondrial fumarate reductase
  53. THIABENDAZOLE - Toxicity / Adverse effects
    • dizziness,
    • anorexia,
    • abdominal pain,
    • liver failure,
    • and Stevens-Johnson syndrome
  54. THIABENDAZOLE - Interactions
    Increases serum theophylline concentrations

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