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Flashcards in Anti fungal/viral Deck (43):
1

Amphotericin B

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

2

Nystatin

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

3

Fluconazole

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)

4

Ketoconazole

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**)

5

Clotrimazole

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)

6

Miconazole

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)

7

Itraconazole

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)

8

Voriconazole

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)

9

Flucytosine

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

10

Caspofungin

1) Invasive aspergilliosis, Candida

2) Antifungal; Inhib cell wall synth by inhibiting synth of Beta-glucan

3) GI upset, flushing (by histasmine release)

11

Micafungin

1) Invasive aspergilliosis, Candida

2) Antifungal; Inhib cell wall synth by inhibiting synth of Beta-glucan

3) GI upset, flushing (by histasmine release)

12

Terbinafine

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

13

Griseofulvin

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

14

Pyrimethamine

1) Tx Toxoplasmosis

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

15

Suramin and Melarsoprol

1) Tx Trypanosoma brucei (african sleeping ds)

2) Antiprotozoan

16

Nifurtimox

1) Tx Trypansoma cruzi (chagas)

2) Antiprotozoan

17

Sodium stibogluconate

1) Tx Leishmaniasis

2) Antiprotozoan

18

Chloroquine

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

Txs for P. falciparum

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

20

Txs for life-threatening malaria

-Quinidine in US (quinine elsewere) or Artisunate

21

Zanamivir

1) Tx and prevention of: Influenza A & B

2) Antiviral therapy; Inhib influenza neuraminidase, Decreasing the release of progeny virus

22

Oseltmavir = Tamiflu

1) Tx and prevention of: Influenza A & B

2) Antiviral therapy; Inhib influenza neuraminidase, Decreasing the release of pogeny virus

23

Ribavirin

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

Acyclovir

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

Ganciclovir

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

Foscarnet

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

Cidofovir

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

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

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

Tenofovir (TDF)

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

Nevirapine

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

Raltegravir

1) HIV therapy

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

3) Hypercholesterolemia

32

IFN-Alpha

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

IFN-Beta

1) MS

2) Interferon; Glycoproteins synth by virus-infected cells; Blocks replication of both RNA & DNA viruses

3) Neutropenia, Myopathy

34

IFN-Gamma

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

Abx to avoid in pregnancy

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

Emtricitabine (FTC)

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

Abacavir (ABC)

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

Lamivudine (3TC)

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

Zidovudine (ZDV, formerly AZT)

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

Didanosine (ddl)

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

Stavudine (d4T)

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

Efazirenz

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

Delavirdine

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