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Microbio > Anti fungal/viral > Flashcards

Anti fungal/viral Flashcards

1
Q

Amphotericin B

A

1) Serious systemic mycoses, Cryptococcus (w or w/o Flucytosine for cryptococcal meningitis), Blastomyces, Coccidioides, Histoplasma, Candida, Mucor. Intrathecally for fungal meningitis.
2) Antifungal; Binds ERGOSTEROL (unique to fungi), forms membrane pores that allow leakage of electrolytes (AmphoTERicin “TEARs” holes in fungal membrane)
3) Fever/chills (“shake & bake”), Hypotension, NEPHROTOXICITY (–> Hypo-/kalemia/magnesiema), Arrhythmias, Anemia, IV phlebitis (“AMPHOTERRIble); Hydration reduces nephrotoxicity (see line #4); Liposomal Amphotericin reduced toxicity
4) Supplement K & Mg b/c of altered renal tubule permeability

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2
Q

Nystatin

A

1) “Swish & swallow” for oral candidiasis (thrush); Topical for diaper rash or vaginal candidiasis
2) Antifungal; Same MOA as Amphotericin B [Binds ergosterol (unique to fungi), forms membrane pores that allow leakage of electrolytes (AmphoTERicin “TEARs” holes in fungal membrane)].

Topical form b/c too toxic for systemic use

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3
Q

Fluconazole

A

1) Local & Less serious systemic mycoses; Floconazole specific=Chronic suppression of cryptoccal meningitis in AIDs pts & candida infection of all types
2) Antifungal-Azole; Inhib fungal sterol (ergosterol) synth by inhib P-450 enzyme that converts lanostrerol –> ergosterol
3) Testosterone synth inhib (GYNECOMASTIA, esp w Ketoconazole) Liver dysfnx (inhib cytochrome P-450)

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4
Q

Ketoconazole

A

1) Local & Less serious systemic mycoses
2) Antifungal-Azole; Inhib fungal sterol (ergosterol) synth by inhib P-450 enzyme that converts lanostrerol –> ergosterol
3) Testosterone synth inhib (GYNECOMASTIA, esp w Ketoconazole) Liver dysfnx (inhib cytochrome P-450**)

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5
Q

Clotrimazole

A

1) Topical fungal infxns**
2) Antifungal-Azole; Inhib fungal sterol (ergosterol) synth by inhib P-450 enzyme that converts lanostrerol –> ergosterol
3) Testosterone synth inhib (GYNECOMASTIA, esp w Ketoconazole) Liver dysfnx (inhib cytochrome P-450)

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6
Q

Miconazole

A

1) Topical fungal infxns
2) Antifungal-Azole; Inhib fungal sterol (ergosterol) synth by inhib P-450 enzyme that converts lanostrerol –> ergosterol

3) Testosterone synth inhib (GYNECOMASTIA, esp w Ketoconazole) Liver dysfnx (inhib cytochrome P-450)

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7
Q

Itraconazole

A

1) Local & Less serious systemic mycoses; Itraconazole specific=Tx for Bastomyces, Coccidiodes, & Histoplasma
2) Antifungal-Azole; Inhib fungal sterol (ergosterol) synth by inhib P-450 enzyme that converts lanostrerol to ergosterol
3) Testosterone synth inhib (gynecomastia) Liver dysfnx (inhib cytochrome P-450)

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8
Q

Voriconazole

A

1) Local & Less serious systemic mycoses
2) Antifungal-Azole; Inhib fungal sterol (ergosterol) synth by inhib P-450 enzyme that converts lanostrerol to ergosterol
3) Testosterone synth inhib (gynecomastia) Liver dysfnx (inhib cytochrome P-450)

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9
Q

Flucytosine

A

1) Tx of systemic fungal infections (esp. meningitis caused by Cryptococcus) in combo w/ Amphotericin B
2) Antifungal; Inhib DNA & RNA biosynth by conversion to 5-fluorouracil by cytosine deaminase
3) BM suppression

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10
Q

Caspofungin

A

1) Invasive aspergilliosis, Candida
2) Antifungal; Inhib cell wall synth by inhibiting synth of Beta-glucan
3) GI upset, flushing (by histasmine release)

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11
Q

Micafungin

A

1) Invasive aspergilliosis, Candida
2) Antifungal; Inhib cell wall synth by inhibiting synth of Beta-glucan
3) GI upset, flushing (by histasmine release)

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12
Q

Terbinafine

A

1) Tx dermatophytoses (esp onchomycosis=fungal infection of finger or toe nails)
2) Antifungal; Inhib fungal enzyme SQUALENE EPOXIDASE which is needed to make ergosterol
3) Abn LFTs, Visual disturbances

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13
Q

Griseofulvin

A

1) PO tx of superficial infections; Inhib growth of dermatophytes (tinea, ringworm)
2) Antifungal; Interferes w/ microtubule fxn; Disrupts mitosis. Deposits in keratin-containing tissues (e.g. nails)
3) Teratogenic (CI in pregnancy), Carinogenic, Confusion, HAs, Increase P-450**** & warfarin metabolism

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14
Q

Pyrimethamine

A

1) Tx Toxoplasmosis
2) Antiprotozoan; Inhibits parasitic Dihydrofolate Reductase (like Trimethoprim and Methotrexate)

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15
Q

Suramin and Melarsoprol

A

1) Tx Trypanosoma brucei (african sleeping ds)
2) Antiprotozoan

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16
Q

Nifurtimox

A

1) Tx Trypansoma cruzi (chagas)
2) Antiprotozoan

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17
Q

Sodium stibogluconate

A

1) Tx Leishmaniasis
2) Antiprotozoan

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18
Q

Chloroquine

A

1) Tx of plasmodial species other than P. falciparium ( d/t high resistance; see line #4)
2) Blocks detoxification of heme into hemozoin. Heme accumulates and is toxic to plasmodia
3) Retinopathy
4) P. falciparum mechanism of resistance: Membrane pump that decreases intracellular concentration of Chloroquine; Tx P. falciparum w/ Artemether/Lumifantrine OR Atovaquone/Proguanil; Tx life-threatening malaria w/ Quinidine in US (quinine elsewere) or Artisunate

19
Q

Txs for P. falciparum

A

-Artemether/Lumifantrine OR Atovaquone/Proguanil -NOT Chloroquine (d/t resistance)

20
Q

Txs for life-threatening malaria

A

-Quinidine in US (quinine elsewere) or Artisunate

21
Q

Zanamivir

A

1) Tx and prevention of: Influenza A & B
2) Antiviral therapy; Inhib influenza neuraminidase, Decreasing the release of progeny virus

22
Q

Oseltmavir = Tamiflu

A

1) Tx and prevention of: Influenza A & B
2) Antiviral therapy; Inhib influenza neuraminidase, Decreasing the release of pogeny virus

23
Q

Ribavirin

A

1) RSV** (bronchiolitis in babies), Chronic hepatitis C
2) Antiviral therapy; Inhib synth of G nucleotides by competitively inhibiting IMP dehydrogenase
3) Hemolytic anemia, Severe teratogen

24
Q

Acyclovir

A

1) HSV & ZVZ; Weak activity against EBV. No activity against CMV. Used for HSZ-induced mucocutaneous & genital lesions as well as encephalitis. Prophylaxis in immunocompromised pts. No effect on latent forms of HSZ & ZVZ.
2) Antiviral therapy; Monophosphorylated by HSV/VZV thymidine kinase. Guanosine analog. Triphosphate formed by cellular enzymes. Preferentially inihib viral DNA polymerase by chain termination*
4) Mechanism of resistance: Mutated viral thymidine kinase

25
Q

Ganciclovir

A

1) CMV**, esp in immunocompromised pts.
2) Antiviral therapy; 5’-monophosphate formed CMV viral kinase Guanosine analog. Triphosphate formed by cellular kinases. Preferentially inhib viral DNA polymerase*
3) Leukopenia, Neutropenia, Thrombocytopenia, Renal toxicity; More toxic to host enzymes vs Acyclovir
4) Mechanism of resistance: Mutated CMV DNA polymerase or lack of viral kinase

26
Q

Foscarnet

A

1) CMV retinitis in immunocompromised pts when Ganciclovir fails; Acyclovir-resistant HSV
2) Antiviral therapy; A pyrophosphate analog (Foscarnet=pyroFOSphate analog). Viral DNA polymerase inhib that binds to pyrophosphate-binding site of the enzyme. Does not req activation by viral kinase**
3) Nephrotoxicity
4) Mechanism of resistance: Mutated DNA polymerase

27
Q

Cidofovir

A

1) CMV retinitis in immunocompromised pts; Acyclovir-resistant HSV
2) Antiviral therapy; Preferentially inhib viral DNA polymerase. Does not req phosphorylation by viral kinase**. Long t-1/2.
3) Nephrotoxicity (co-admin w/ Probenecid & IV saline to reduce toxicity)

28
Q

Lopinavir; Atazanavir; darunavir; Forsamprenavir; Saquinavir; Ritonavir; Indinavir

A

1) HIV therapy
2) Protease inhib; Prevents maturation of new viruses by cleaving HIV-1 protease (Assembly of virions depends on HIV-1 protease, which cleaves polypeptide products of HIV mRNA into their functional parts)
3) Hyperglycemia, GI intolerance (N/D), Lipodystrophy, Nephropathy. Inhibit P450*
4) All protease inhibitors end in -navir [Navir (never) tease a protease]

29
Q

Tenofovir (TDF)

A

1) HIV therapy
2) Nucleoside reverse transcriptase inhib (NRTI); Completely inhib nucleotide binding to reverse transcriptase & terminate te DNA chain (lack a 3’ OH group)
3) BM suppression (can be reversed w/ G-CSF & EPO), Peripheral neuropathy, Lactic Acidosis
4) Is a nucleotide analog, so does not have to be activated (vs other NRTIs, which are nucleoside analogs & therefore, req activation)

30
Q

Nevirapine

A

1) HIV therapy
2) Non-nucleoside reverse transcriptase inhib (NNRTI); Bind to reverse transcriptase at site different from NRTIs (Nucleoside RTIs). Do not req phosphorylation to be active or compete w/ nucleotides
3) BM suppression (can be reversed w/ G-CSF & EPO), Peripheral neuropathy; Rash

31
Q

Raltegravir

A

1) HIV therapy
2) Integrase inhib; Inhibits HIV genome integration into host cell chromosome by reversibly inhibiting HIV integrase
3) Hypercholesterolemia

32
Q

IFN-Alpha

A

1) Chronic hepatitis B & C; Kaposi’s sarcoma
2) Interferon; Glycoproteins synth by virus-infected cells; Blocks replication of both RNA & DNA viruses
3) Neutropenia, Myopathy

33
Q

IFN-Beta

A

1) MS
2) Interferon; Glycoproteins synth by virus-infected cells; Blocks replication of both RNA & DNA viruses
3) Neutropenia, Myopathy

34
Q

IFN-Gamma

A

1) NADPH oxidase deficiency (Chronic Granulomatous Disease)
2) Interferon; Glycoproteins synth by virus-infected cells; Blocks replication of both RNA & DNA viruses
3) Neutropenia, Myopathy

35
Q

Abx to avoid in pregnancy

A

Contraindicated in Pregnancy –> Adverse Effect:

  • Sulfonamides –> Kernicterus
  • Aminoglycosides –> Ototoxicity
  • Fluoroquinolones –> Cartolage damage
  • Clarithromycin –> Embryotoxic
  • Tetracyclines –> Discolored teeth, Inhib of bone growth
  • Ribavirin (antiviral) –> Teratogenic
  • Griseofulvin (antifungal) –> Teratogenic
  • Chloramphenicol –> “Gray baby”

(SAFe Children Take Really Good Care)

36
Q

Emtricitabine (FTC)

A

1) HIV therapy
2) Nucleoside reverse transcriptase inhib (NRTI); Completely inhib nucleotide binding to reverse transcriptase & terminate te DNA chain (lack a 3’ OH group)
3) BM suppression (can be reversed w/ G-CSF & EPO), Peripheral neuropathy; Lactic acidosis
4) Must be phosphorylated to be activated (True of all NRTIs, except Tenofovir b/c it is a nucleotide vs nucleoside analog)

37
Q

Abacavir (ABC)

A

1) HIV therapy
2) Nucleoside reverse transcriptase inhib (NRTI); Completely inhib nucleotide binding to reverse transcriptase & terminate te DNA chain (lack a 3’ OH group)
3) BM suppression (can be reversed w/ G-CSF & EPO), Peripheral neuropathy; Lactic acidosis
4) Must be phosphorylated to be activated (True of all NRTIs, except Tenofovir b/c it is a nucleotide vs nucleoside analog)

38
Q

Lamivudine (3TC)

A

1) HIV therapy
2) Nucleoside reverse transcriptase inhib (NRTI); Completely inhib nucleotide binding to reverse transcriptase & terminate te DNA chain (lack a 3’ OH group)
3) BM suppression (can be reversed w/ G-CSF & EPO), Peripheral neuropathy; Lactic acidosis
4) Must be phosphorylated to be activated (True of all NRTIs, except Tenofovir b/c it is a nucleotide vs nucleoside analog)

39
Q

Zidovudine (ZDV, formerly AZT)

A

1) HIV therapy
2) Nucleoside reverse transcriptase inhib (NRTI); Completely inhib nucleotide binding to reverse transcriptase & terminate te DNA chain (lack a 3’ OH group)
3) BM suppression (can be reversed w/ G-CSF & EPO), Peripheral neuropathy; Lactic acidosis; ZDZ specific ADE=Anemia
4) Used for general prophylaxis & during pregnancy to reduce risk of fetal transmission; Must be phosphorylated to be activated (the second statement is true of all NRTIs, except Tenofovir b/c it is a nucleotide vs nucleoside analog)

40
Q

Didanosine (ddl)

A

1) HIV therapy
2) Nucleoside reverse transcriptase inhib (NRTI); Completely inhib nucleotide binding to reverse transcriptase & terminate te DNA chain (lack a 3’ OH group)
3) BM suppression (can be reversed w/ G-CSF & EPO), Peripheral neuropathy; Lactic acidosis
4) Must be phosphorylated to be activated (True of all NRTIs, except Tenofovir b/c it is a nucleotide vs nucleoside analog)

41
Q

Stavudine (d4T)

A

1) HIV therapy
2) Nucleoside reverse transcriptase inhib (NRTI); Completely inhib nucleotide binding to reverse transcriptase & terminate te DNA chain (lack a 3’ OH group)
3) BM suppression (can be reversed w/ G-CSF & EPO), Peripheral neuropathy; Lactic acidosis
4) Must be phosphorylated to be activated (True of all NRTIs, except Tenofovir b/c it is a nucleotide vs nucleoside analog)

42
Q

Efazirenz

A

1) HIV therapy
2) Non-nucleoside reverse transcriptase inhib (NNRTI); Bind to reverse transcriptase at site different from NRTIs (Nucleoside RTIs). Do not req phosphorylation to be active or compete w/ nucleotides
3) BM suppression (can be reversed w/ G-CSF & EPO), Peripheral neuropathy; Rash

43
Q

Delavirdine

A

1) HIV therapy
2) Non-nucleoside reverse transcriptase inhib (NNRTI); Bind to reverse transcriptase at site different from NRTIs (Nucleoside RTIs). Do not req phosphorylation to be active or compete w/ nucleotides
3) BM suppression (can be reversed w/ G-CSF & EPO), Peripheral neuropathy; Rash

Microbio (13 decks)

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