Block V, Antimicrobials, Antifungals, Antivirals

Front 1

Name four classes of Beta-Lactam antibiotics

Back 1

1. Natural Penicillins
2. Aminopenicillins
3. antistaphylococcal penicillins
4. antipseudomonal penicillins

Front 2

what is an aminopenicillin?

Back 2

a penicillinase resistant penicillin

Front 3

List two natural penicillins

Back 3

1. Penicillin G
2. Penicillin V

Front 4

list two aminopenicillins

Back 4

1. ampicillin
2. amoxicillin

Front 5

list an antistaphylococcal penicillin

Back 5

Nafcillin

Front 6

list an antipseudomonal penicillin

Back 6

Piperacillin (Pipracil)

Front 7

How many generations of cephalosporin antibiotics are there?

Back 7

4

Front 8

list a parenteral first generation cephalosporin

Back 8

Cefazolin
(Ancef, Kefzol)

Front 9

list an oral first generation cephalosporin

Back 9

Cephalexin
(Keflex)

Front 10

list three parenteral second generation cephalosporins

Back 10

1. Cefoxitin (Mefoxin)
2. Cefuroxime (Zinacef)
3. Cefotetan (Cefotan)

Front 11

oral second generation cephalosporin antibiotics (2)

Back 11

1. Cefuroxime (Claforan)
2. Cefprozil (Cefzil)

Front 12

parenteral third generation cephalosporin antibiotics (3)

Back 12

1. Cefotaxime (Claforan)
2. Ceftriaxone (Rocephin)
3. Ceftazidime (Fortaz, Tazidime, Tazicef)

Front 13

parenteral fourth generation cephalosporin antibiotic (1)

Back 13

Cefepime (Maxipime)

Front 14

oral third/fourth generation cephalosporin (1)

Back 14

Cefdinir
(Omnicef)

Front 15

carpepenem antibiotics (2)

Back 15

1. Imipenem/Cilastin (Primaxin)
2. Ertapenem (Invanz)

Front 16

monobactam antibiotic (1)

Back 16

Aztreonam
(Azactam)

Front 17

combinations with Beta-Lactimase inhibitors (3)

Back 17

1. Clavulanic Acid/Amoxicillin (Augmentin)
2. Sulbactam/Ampicillin (Unasyn)
3. Tazobactam/Piperacillin (Zosyn)

Front 18

what is the prototype of a glycopeptide antibiotic?

Back 18

Vancomycin

Front 19

aminoglycosides (2)

Back 19

1. Gentamycin
2. Tobramycin

Front 20

macrolides (3)

Back 20

1. Erythromycin
2. Azithromycin
3. Clarithromycin

Front 21

Ketolides (1)

Back 21

Telithromycin (Ketek)

Front 22

Tetracyclins (2)

Back 22

1. Tetracycline
2. Doxycyclin

Front 23

Lincosamides (2)

Back 23

1. Clindamycin
2. Chloramphenicol

Front 24

Streptogramins (2)

Back 24

Quinupristin
Dalfopristin
(both Synercid)

Front 25

Oxazolidinones (1)

Back 25

Linezold (Zyvox)

Front 26

Sulfonamides (1)

Back 26

Trimethoprim/Sulfamethoxazole

Front 27

Fluoroquinolones (4)

Back 27

1. Ciprofloxacin (Cipro)
2. Levofloxacin (Levaquin)
3. Gatifloxacin (Tequin)
4. Moxifloxacin (Avelox)

Front 28

antiviral for Respiratory Syncytial Virus (RSV)

Back 28

Ribavarin (Virazole)

Front 29

agents for herpes and varicella viruses (4)

Back 29

1. Acyclovir (Zovirax)
2. Valcyclovir (Valtrex)
3. Famciclovir (Famvir)
4. Penciclovir (Denavir)

Front 30

Agents for CMV (4)

Back 30

1. Cidofovir (Vistide)
2. Foscarnet (Foscavir)
3. Ganciclovir (Cytovene)
4. Valganciclovir (Valcyte)

Front 31

What are these agents used to treat?
1. INF-alpha (PEG_Intron, Pegasys)
2. Ribavarin (Copegus, Rebetol)
3. Lamivudine (#TC, Epivir HBV)
4. Adefovir (Hepsera)

Back 31

Agents used to treat HepB and C

Front 32

Classes of HIV treatment agents (3)

Back 32

1. Antiretrovirals
2. Protease Inhibitors (PIs)
3. Fusion Inhibitors

Front 33

Three types of antiretrovirals

Back 33

1. Nucleoside reverse transcriptase inhibitors (NRTI)
2. Nucleotide analog reverse transcriptase inhibitors
3. Non-nucleoside reverse transcriptase inhibitors (NNRTI)

Front 34

What class of drug?
Used to treat?
1. Abacavir (Ziagen)
2. Didanosine (ddI) (Videx)
3. Lamivudine (3TC, Epivir)
4. Stavudine (d4T, Zerit)
5. Zalcitabine (ddC, Hivid)
6. Emtricitabine (Emtriva)

Back 34

Nucleoside reverse transcriptase inhibitors (NRTI)

Used to treat HIV/AIDS

Front 35

Tenofovir (Viread)

Back 35

Nucleotide analog reverse transcriptase inhibitor

Front 36

1. Delaviridine (Rescriptor)
2. Efavirenz (Sustiva)
3. Nevirapine (Viramune)

Back 36

Non-nucleoside reverse transcriptase inhibitors (NNRTI)

Front 37

1. Indinavir (Crixivan)
2. Nelfinavir (Viracept)
3. Ritonavir (RTV) (Norvir)
4. Saquinavir (SQV) (Invirase, Fortovase)
5. Amprenavir (Agenerase)
6. Atazanavir (Reyataz)

Back 37

Protease inhibitors (PIs)

Front 38

Fusion Inhibitor (1)

Back 38

Enfuvirtide (Fuzeon)

Front 39

Azoles (Antifungals) (4)

Back 39

1. Ketoconazole (Nizoral)
2. Itraconazole (Sporanox)
3. Fluconazole (Diflucan)
4. Miconazole (Monistat)

Front 40

Antimycobacterial agents (5)

Back 40

1. Isoniazid (INH)
2. Ethambutol (ETB)
3. Rifampin (RIF)
4. Rifabutin (Mycobutin)
5. Pyrazinamide (PZA)

Front 41

Antiparasitics (4)
(1,2,3-antimalarials)
(4-antiprotozoal & antihelminthic)

Back 41

1. Chloroquine
2. Primaquine
3. Doxycycline
4. Metronidazole

Front 42

what is the primary prevention approach to viral disease?

Back 42

vaccination

Front 43

what are the two general mechanisms used to treat viral disease?

Back 43

1. antivirals
2. stimulation of host defense mechanisms

Front 44

what must first happen to an antiviral drug before it is active?

Back 44

phosphorylation inside the cell

Front 45

why do antivirals have no effect on latent viruses?

Back 45

antivirals inhibit stages of viral replication (the virus must be active in order for antivirals to have an effect)

Latent viruses are not undergoing replication, therefore the antivirals have no effect.

Front 46

what is the drug of choice for treatment of herpes simplex virus?

Back 46

Acyclovir
(antiviral, DNA polymerase inhibitor)

Front 47

What is the drug of choice for CMV?

Back 47

Gancyclovir (Cytovene)
(antiviral, DNA polymerase inhibitor)

Front 48

which antiviral is a synthetic guanine nucleoside analog?

Back 48

Acyclovir

Front 49

acyclovir is not useful against which virus? (a virus in the herpes class) Why?

Back 49

CMV
CMV does not have thymidine kinase (TK)

Front 50

describe the acyclovir MOA

Back 50

IRREVERSIBLE TERMINATION OF VIRAL DNA SYNTHESIS

1. phosphorylated by thymidine kinase (TK) in infected cell. TK is a viral encoded enzyme
2. cellular encoded kinases form ACV-triposphate (ACV-TP)
3. ACV acts as a competitive inhibitor of viral DNA polymerase: thus it irreversably terminates viral DNA synthesis

Front 51

acyclovir adverse effects?

Back 51

1. reversible crystalline nephropathy
2. CNS effects

Front 52

valacyclovir is another drug used to treat HSV. What is it's MOA?

Back 52

valacyclovir is a prodrug of Acyclovir. It converts to ACV in the liver (this increases serum ACV levels)
Rest of MOA same as ACV

Front 53

what is the advantage of using Valacyclovir vs. Acyvlovir to treat HSV?

Back 53

less frequent dosing

Front 54

what is the one other drug that is used to treat HSV and what is it's mechanism of action?

Back 54

Famciclovir
Competitive inhibitor of viral DNA polymerase -> stops viral replication

Front 55

when is the best time to initiate antiviral treatment?

Back 55

ASAP after onset of signs and symptoms
ideally 24-48 hrs.

Front 56

which drug is used to treat CMV (seeing as acyclovir won't)

Back 56

Gangcyclovir (GCV)
(DNA polymerase inhibitor)

Front 57

Gangciclovir MOA?

Back 57

1st phosphorylation catalyzed by viral specific protien kinase, results in a competitive inhibitor of DNA polymerase

Front 58

Gangciclovir adverse effects?

Back 58

VERY TOXIC: 32% INTERRUPT OR DISCONTINUE THERAPY

1. Myelosuppression (reversible)
- neutropenia
- thrombocytopenia
2. CNS effects

Front 59

what is the prodrug of gancyclovir called?
what activates the prodrug?

Back 59

Valganciclovir
intestinal and hepatic esterases convert valganciclovir to ganciclovir

Front 60

which antiviral is often used in the following situations:
ganciclovir intolerance
ACV resistant HSV
CMV retinitis

Back 60

Foscarnet

Front 61

MOA of foscarnet?

Back 61

- pyrophosphate analog
- noncompetitive inhibitor of viral DNA Polymerase and reverse transcriptase

Front 62

what is the major adverse effect seen with foscarnet?

Back 62

renal failure, nephrotoxicity

Front 63

what is so special about cidofovir?

Back 63

it is viral independent

Front 64

MOA of cidofovir?

Back 64

1. converted by host cell kinases into active form
2. competitive inhibitor of viral DNA polymerase
3. one insertion slows replication; two halts it

Front 65

Indication of codofovir?

Back 65

CMV retinitis in HIV

Front 66

Two standard therapies for influenza?

Back 66

amantadine
rimantadine

Front 67

difference between amantadine and rimantadine?

Back 67

EQUAL EFFICACY

amantadine - adjust dose in renal failure
rimantadine - safer agent for the elderly (does not require dose adjustments in renal failure)
rimantidine also has 4-10x greater activity than amantadine

Front 68

MOA of amantadine and rimantadine?

Back 68

INHIBITION OF VIRUS UNCOATING

targets M2 protein of influenza A

Front 69

MOA of resistance to amantidine?

Back 69

single mutations in the M2 protien

Front 70

what type of antivirals are Zanamivir and Oseltamivir?

Back 70

Neuraminidase inhibitors

Front 71

MOA of neuraminidase inhibitors

Back 71

scialic acid analogues, inhibit viral neuraminidase -> virus can't exit cell as easily (they clump and don't disperse)

Front 72

spectrum of neuraminidase inhibitors?

Back 72

treatment of influenza A and B

Front 73

how do neuraminidase inhibitors effect the influenza symptoms?

Back 73

- reduce signs/symptoms by 1-1 1/2 days
- reduce severity of symptoms

Front 74

which neuraminidase inhibitor is administered as a dry powder inhalation?

Back 74

Zanamivir
(therefore use caution in asthma, COPD)

Front 75

prodrug of zanamivir?

Back 75

oseltamivir

Front 76

which antiviral is a guanosine analog and is effective against RNA viruses?

Back 76

Ribavarin

Front 77

which viruses would you use Ribavarin for? (3)

Back 77

- RSV
- HCV (w/interferon)
- hantavirus

Front 78

how is ribavarin administered?
significance?

Back 78

via aerosol
could be toxic to health care workers and pregnant women

Front 79

adefovir MOA?

Back 79

inhibits HBV DNA polymerase - results in DNA chain termination

Front 80

1. indications for adefovir?
2. advantage?

Back 80

1. chronic HBV
2. 1 time daily dosing

Front 81

MOA of interferons?

Back 81

inhibit viral RNA and DNA synthesis

Front 82

which type of interferon is most commonly used to treat viruses?

Back 82

IFN-alpha

Front 83

what can be done to IFN-alpha to increase its half life?

Back 83

"peglated IFN-a"

IFN covalently bound to polyethylene glycol (PEG)
increases half life by 5x - allows once weekly injections

Front 84

IFN-a is the therapy of choice for which virus?

Back 84

HCV

Front 85

how do you measure the viral burden (load) in an HIV patient?

Back 85

CD4
vRNA copies/mL

Front 86

what are some problems with HIV therapy? (4)

Back 86

1. combination regimens (medically complex)
2. lots of side effects/drug interactions
3. compliance is NECESSARY for success (this is a challenge)
4. Cost

Front 87

what are the two types of antiretroviral drugs?

Back 87

1. NRTI - Nucleoside Reverse Transcriptase Inhibitors
2. NNRTI - Non-Nucleoside Reverse Transcriptase Inhibitors

Front 88

besides the antiretroviral drugs, what other therapies are available for HIV? (2)

Back 88

1. PIs - Protease Inhibitors
2. Fusion Inhibitor

Front 89

HAART stands for?

Back 89

Highly Active Retroviral Therapy
(combination therapy for HIV)

Front 90

what is the MOA of
1. NRTIs
2. NNRTIs

Back 90

1. NRTIs are nucleotide analogs. They prematurely terminate HIV DNA elongation (must be phosphorylated by TP to be active)

2. NNRTIs bind to viral reverse transcriptases (no intracellular phosphorylation)

Front 91

Major difference between NRTIs and NNRTIs?

Back 91

NRTIs must be phosphorylated intracellularly
NNRTIs are not phosphorylated

Front 92

name the first antiviral agent to show benefit in AIDS (it is still a first line anti-HIV medication)

Back 92

Zidofudine (ZDV, AZT)

Front 93

Name 3 uses of zidofuvine (AZT)

Back 93

1. combination HIV therapy

2. reduce vertical HIV transmission to 2%.

3. postexposure prophylaxis for needlesticks and mucosal exposure

Front 94

downside of NRTIs?

Back 94

LOTS of adverse effects
- lactic acidosis
- pancreatitis

Front 95

adverse effect of NNRTIs?

Back 95

P450 inhibitors or inducers - cause drug interactions

Front 96

MOA of protease inhibitors?

Back 96

HIV protease is required for virus production
inhibition prevents replication
* does not need intracellular activation*

Front 97

which two anti HIV agents are either inhibitors or inducers of the P450 system?

Back 97

1. PIs (inhibitor)
2. NNRTIs (some inhibit, some induce)

Front 98

regarding malaria prophylaxis - what has occured that renders the original antimalarial drugs ineffective?

Back 98

chloroquine resistance

Front 99

what prophylactic agent would you use for chloroquine sensitive malaria?

Back 99

chloroquine phosphate

Front 100

name 3 prophylactic antimalarials that can be used in chloroquine resistant areas

Back 100

1. Mefloquine (Larium)
2. Atovaquone/Proguanil (Malarone)
3. Doxycycline

Front 101

LARIUM (mefloquine)
1. dosing
2. adverse effects

Back 101

1. once per week (start 2 wks before, end 4 wks after)
2. GI, sleep disturbances, dreams, rare siezures or psychosis

Front 102

Malarone (atovaquone/proguanil)
1. dosing
2. adverse effects?

Back 102

1. daily (start 1-2 days before, end 7 days after)
2. GI, headache

Front 103

dosing of doxycycline as malarial prophylaxis?

Back 103

daily (starting 1-2 days before, end 4 wks after)

Front 104

use of suladiazene + pyrimethamine?
(Fansidar)

Back 104

can be used as a self treatment dose in the event of onset of malaria

Front 105

which antimalarial targets the latent liver forms of malaria? (not the erythrocytic forms like the others do)

Back 105

Primaquine

Front 106

what is the firstline protozoal/antihelminth?

Back 106

metronidazole

Front 107

what are some other uses for metronidazole?

Back 107

1. anaerobic infections
2. C. difficile colitis, Trichomoniasis, BV, giardia, amebiasis

Front 108

metronidazole side effects? (4)

Back 108

metallic taste
GI upset
DISULFRAMLIKE EFFECT WITH ETOH
carcinogenic?

Front 109

what is mebendazole used to treat?

Back 109

treats worms (intestinal nematodes)

Front 110

How does mebendazole work?

Back 110

PARALYZES WORMS
binds to helminthic beta-tubulin and prevents microtubule assembly

Front 111

difference between mebendazole and albendazole?

Back 111

albendazole has greater efficacy as a 1x dose
also has a very broad spectrum

Front 112

use of pyrantel pamoate

Back 112

drug can be used as an alternative to mebendazole or albendazole to treat nematodes

Front 113

why is TB so hard to treat?

Back 113

resistance keeps evolving

*leading cause of death worldwide*

Front 114

signs of active TB

Back 114

+ sputum culture
+ acid fast stain
+ CXR
+ PPD

Front 115

signs of latent TB

Back 115

+ PPD
have had previous infectious process

Front 116

what is the most widely used TB medication?

Back 116

Isoniazid (INH)
(unless TB is INH resistant)

Front 117

most serious adverse effect of INH?

Back 117

liver toxicity
(can develop hepatitis)

MUST MONITOR LIVER FUNCTION

Front 118

MOA of Rifampin (RIF)
what else does it cover?

Back 118

inhibits DNA dependant RNA polymerase of mycobacterium

(also covers strep, MRSA, Bacteroides fragilis and more)

Front 119

what is the problem with RIF?

Back 119

resistance develops rapidly

(To minimize, prescribe with another drug)

Front 120

metabolism of Rifampin?

Back 120

p450 ACTIVATOR

MANY drug interactions
(ie. OCs)

Front 121

adverse effects of Rifampin?

Back 121

- body secretions are an orange color
- hepatotoxicity

Front 122

hallmark side effect of ethambutol (ETB)?

Back 122

retrobulbar neuritis
(dose related)
(monitor eye exams)

Front 123

which TB drug should you not combine with Rifampin? Why?

Back 123

Pyrazinamide (PZA)
severe hepatotoxicity

Front 124

recommendations for latent TB treatment?

Back 124

min. 9 months of INH
-OR-
Rifampin for 4 mo. (less effective than INH)

Front 125

what is a major cause of TB treatment failure?

Back 125

noncompliance

Front 126

how is the problem of compliance with TB medications resolved?

Back 126

DOTs (Directly Observed Treatment) - directly monitor medicine taking

Front 127

which two drugs are associated with parenteral infusion reactions from too fast of administration?

Back 127

vancomycin
amphotericin B

Front 128

what is a major limiting factor (adverse effect) in amphotericin B use?

Back 128

nephrotoxicity
(can be reduced if saline infusion is given before each dose)

Front 129

MOA of Flucytosine?

Back 129

inhibits function of RNA and DNA. (Converted to 5-fluoruoracil, a chemotherapeutic)

Front 130

which antifungal group is used routinely, are safest, and has the widest spectrum?

Back 130

Azoles

Front 131

MOA of Azoles?

Back 131

inhibit synthesis of ergesterol - results in altered membrane permeability. (inhibits cyp-450 dependant fungal enzyme)

Front 132

what is unique about the metabolism of ketoconazole?

Back 132

orally administered: requires acid to solubilize the tablet

Front 133

which azole is a better choice than ketonazole?

Back 133

Itraconazole
(broader spectrum, less side effects)

Front 134

which azole has the highest CSF penetration?
significance?

Back 134

Fluconazole
(great drug for cryptococcus meningitis)

Front 135

arrange from lowest to highest spectrum of activity:
ketoconazole
voriconazole
fluconazole
itraconazole

Back 135

ketoconazole
itraconazole
fluconazole
voriconazole

Front 136

indications for voriconazole?

Back 136

Many, but for the most part has been reserved for severe fungal infections

Front 137

what is the drug of choice to treat dermatophytes?

Back 137

terbinafine
terbinafine > azoles > griseofulvin

Front 138

what is the best strategy for treatment of onychomycosis with terbinafine?

Back 138

pulse dosing (daily 1 week out of 4)