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32 Cards in this Set

  • Front
  • Back
Amphotericin B
Binds ergosterol= membrane pores

Systemic mycoses; does not cross blood-brain barrier, need intrathecal admin

Tox: caused by binding to cholesterol in host cells
Fever, chills, hypotension, nephrotox, arrhythmias, anemia, IV phlebitits
Nystatin
Binds ergosterol= membrane pores
Too toxic for systemic use

"Swish and swallow" for oral candiasis
Topical for diaper rash or vaginal candiasis
-Azoles
Inhibit Ergosterol synthesis
Inhibits 14α-demethylase= ↑lanosterol

Systemic mycoses

Tox: hormone synthesis inhibition, gynecomastia, liver dysfunction, inhibits P450's, fever, chills
Fluconazole
Inhibit Ergosterol synthesis

Cryptococcal meningitis in AIDS pts b/c it crosses blood-brain barrier
All Candidal infections
Ketoconazole
Inhibit Ergosterol synthesis

Blastomyces, Coccidioides, Histoplasma, Candida, hypercortisolism
Flucytosine
Converts to 5-fluorouracil= Inhibits DNA Synthesis

Systemic mycoses in combo with Amphotericin B

Tox: BONE MARROW SUPPRESSION, nausea, vomitting, diarrhea
Caspofungin
Inhibits cell wall synthesis by inhibiting synthesis of β-glucan

Aspergillosis

Tox: GI upset, flushing
Terbinafine
Inhibits Squalene Epoxidase= ↑squalene and ↓lanosterol= inhibits ergosterol synthesis

Dermatophytoses (especially onychomycosis)
Griseofulvin
Disrupts microtubule function= disrupts mitosis
Deposits in keratin-containing tissue

Superficial infections, Dermatophytes

Tox: teratogenic, carcinogenic, confusion, headaches, ↑P450 & warfarin metabolism
Amantadine
Blocks viral penetration/uncoating (M2 protein);
Causes release of dopamine

Influenza A, rubellA, Parkinson's Dx

Tox: cerebellA problems

Resistance: Mutated M2 protein (90% of Influenza A now)

A man to dine takes of his coat
Rimantidine
Blocks viral penetration/uncoating (M2 protein)

Less CNS side effects than Amantidine
Zanamivir
Inhibits influenza neuraminidase= ↓release of progeny virus

Influenza A & B
Oseltamivir
Inhibits influenza neuraminidase= ↓release of progeny virus

Influenza A & B
Ribavirin
Inhibits IMP dehydrogenase= ↓guanine nucleotides

RSV, chronic Hep C

Tox: severe teratogen, Hemolytic Anemia
Acyclovir
Guanosine analog; monophosphorylated by HSV thymidine kinase; triphosphorylated by cellular kinases
Inhibits VIRAL DNA Polymerase by chain termination

Herpes Simplex, Varicella, EBV
NO effect on latent forms- use Famciclovir

Resistance: lack of thymidine kinase
Ganciclovir
Guanosine analog;
5'-monophosphate by thymidine kinase or viral kinase; triphosphorylated by cellular kinases
Inhibits VIRAL DNA Polymerase by chain termination

CMV

Tox: PANCYTOPENIA, renal toxicity
More toxic to host enzymes than Acyclovir

Resistance: mutated CMV DNA poly or lack of viral kinase
Foscarnet
pyroFOSphate analog: inhibits viral DNA polymerase at pyrophostate binding site
Does NOT require activation by viral kinase

CMV retinitis when Ganciclovir fails
Acyclovir-resistant HSV
Interferon-α
Block various stages viral penetration and synthesis
Induce ribonuclease that degrade viral mRNA

Chronic Hep B & C
Kaposi's Sarcoma (HHV-8)

Tox: Neutropenia
Interferon-β
Block various stages viral penetration and synthesis
Induce ribonuclease that degrade viral mRNA

Multiple Sclerosis

Tox: Neutropenia
Interferon-γ
Block various stages viral penetration and synthesis
Induce ribonuclease that degrade viral mRNA

NADPH oxidase deficiency

Tox: Neutropenia
-Navir
Saquinavir
Ritonavir
Indinavir
Nelfinavir
Amprenavir
HIV Protease Inhibitor: Inhibit maturation of NEW virus
NAVIR (never) tease a proTEASE

HAART therapy

Tox: GI intolerance, HYPERGLYCEMIA, lipodystrophy, thrombocytopenia (indinavir)
Zidovudine (ZDV)
Nucleoside HIV Reverse Transcriptase Inhibitors
need cellular thymidine kinase to activate

HAART Therapy
PROPHYLAXIS & during PREGNACY

Tox:
bone marrow suppression (neutropenia, anemia)- use GM-CSF and EPO
peripheral neuropathy, lactic acidosis
Megaloblastic Anemia
Didanosine (ddI)
Nucleoside HIV Reverse Transcriptase Inhibitors

HAART Therapy

Tox:
bone marrow suppression (neutropenia, anemia)- use GM-CSF and EPO
peripheral neuropathy, lactic acidosis
Zalcitabine (ddC)
Nucleoside HIV Reverse Transcriptase Inhibitors

HAART Therapy

Tox:
bone marrow suppression (neutropenia, anemia)- use GM-CSF and EPO
peripheral neuropathy, lactic acidosis
Stavudine (d4T)
Nucleoside HIV Reverse Transcriptase Inhibitors

HAART Therapy

Tox:
bone marrow suppression (neutropenia, anemia)- use GM-CSF and EPO
peripheral neuropathy, lactic acidosis
Lamivudine (3TC)
Nucleoside HIV Reverse Transcriptase Inhibitors

HAART Therapy

Tox:
bone marrow suppression (neutropenia, anemia)- use GM-CSF and EPO
peripheral neuropathy, lactic acidosis
Abacavir
Nucleoside HIV Reverse Transcriptase Inhibitors

HAART Therapy

Tox:
bone marrow suppression (neutropenia, anemia)- use GM-CSF and EPO
peripheral neuropathy, lactic acidosis
Highly active antiretroviral therapy (HAART)
HIV Combo Therapy:
Protease inhibitors + Reverse Transcriptase inhibitors

Initiate @ high viral load or low CD4 counts (<500 cells/mm3)
Nevirapine
Non-nucleoside HIV Reverse Transcriptase Inhibitors

HAART Therapy

Tox:
bone marrow suppression (neutropenia, anemia)- use GM-CSF and EPO
peripheral neuropathy, rash
Efavirenz
Non-nucleoside HIV Reverse Transcriptase Inhibitors

HAART Therapy

Tox:
bone marrow suppression (neutropenia, anemia)- use GM-CSF and EPO
peripheral neuropathy, rash
Delaviridine
Non-nucleoside HIV Reverse Transcriptase Inhibitors

HAART Therapy

Tox:
bone marrow suppression (neutropenia, anemia)- use GM-CSF and EPO
peripheral neuropathy, rash
Enfuvirtide
HIV Fusion Inhibitor:
Binds viral gp41 subunit= inhibition of conformation change= block entry

Use for persistent viral replication in spite of antiretrovrial therapy

Tox: Hypersensitivity, bacterial PNEUMONIA