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Boards Review by Topic > FA Antimicrobial Pharm > Flashcards

FA Antimicrobial Pharm Flashcards

1
Q

Which penicillin has best oral availability?

A

Pen V

Pen G is only IV/IM

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2
Q

How do penicillins work?

A

D-Ala-D-Ala structural analog

Binds PBP’s (transpeptidase) blocking cross-linking

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3
Q

Clinical use for Penicillins

A 
Mostly G(+)
Also G(-) cocci (mainly N meningitidis) and spirochetes
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4
Q

What are the penicillinase sensitive penicillins? (Besides Pen G/V)

A

Amoxicillin, Ampicillin

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5
Q

MOA of penicillinase sensitive penicillins

A

Same MOA as Penicillin, but wider spectrum

Often combined with Clavulanic acid

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6
Q

Which of the penicillinase sensitive penicillins has greater oral bioavailability?

A

Amoxicillin

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7
Q

Use of penicillinase sensitive penicillins

A 
Extended spectrum allows coverage of HHELPSS kill Enterococci
H flu
H pylori
E coli
Listeria
Proteus
Salmonella
Shigella
Enteroccoci
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8
Q

Adverse effects of penicillinase sensitive penicillins

A

Pseudomembranous colitis

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9
Q

What are the penicillinase resistant penicillins?

A

Dicloxacillin, Nafcillin, Oxacillin

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10
Q

MOA of penicillinase resistant penicillins

A

Same as penicillin

Narrow spectrum

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11
Q

Use of penicillinase resistant penicillins

A

Staph aureus

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12
Q

What are the antipseudomonal penicillins?

A

Piperacillin, Ticarcillin

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13
Q

Use of antipseudomonal penicillins

A

Pseudomonas and G(-) rods

Susceptible to penicillinase so use with beta-lactamase inhibitors

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14
Q

What are the beta-lactamase inhibitors?

A

Clavulanic acid
Sulbactam
Tazobactam

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15
Q

Which of the Cephalosporins covers MRSA?

A

5th gen:

Ceftaroline

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16
Q

MOA of Cephalosporins

A

These are beta-lactam drugs but are less sensitive to penicillinase

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17
Q

Name 2 1st gen Cephalosporins and their use

A

Cefazolin, Cephalexin
G(+) cocci
Remember 1st gen PEcK
Proteues, E coli, Klebsiella

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18
Q

Which Cephalosporin is used before surgery to prevent S aureus wound infection?

A

Cefazolin

1st gen

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19
Q

Name 3 2nd gen Cephalosporins and their use

A

Remember FAke FOX FUR
CeFAclor, CeFOXitin, CeFURoxime

Remember HENS PEcK (in addition to G(+) cocci)
H flu, Enterobacter, Neisseria, Serratia, Proteus, E coli, Klebsiella

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20
Q

Name 3 3rd gen Cephalosporins and use

A

Ceftriaxone, Cefotaxime, Ceftazidime

Serious G(-) infections resistant to other beta-lactams

Ceftriaxone: meningitis, gonorrhea, disseminated Lyme disease
Ceftazidime: Pseudomonas

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21
Q

4th gen Cephalosporin and use

A 
Cefepime
G(-), has increased activity against Pseudomonas and G(+)
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22
Q

5th gen Cephalosporin and use

A

Ceftaroline
Broad G(+) and G(-) coverage
Includes MRSA
Does not cover Pseudomonas

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23
Q

Adverse effects of Cephalosporins

A

Disulfiram-like
Vit K deficiency
Increased nephrotoxicity of aminoglycosides

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24
Q

What drugs are Carbapenems?

A

Imipenem, Meropenem, Ertapenem, Doripenem

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25
Q

MOA of Carbapenems

A

Beta-lactam like penicillins and cephalosporins, but broader coverage
Less sensitive to common resistance mechanisms
Imipenem must be administered with Cilastatin to inhibit renal dehydropeptidase I
Meropenem is stable to renal enzyme

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26
Q

Use of Carbapenems

A

Generally only used for MDR bacteria and in patients that are hospitalized because of risk of seizures and to prevent resistance
These are heavy-hitting drugs used often as last resort in life-threatening infections
Cover G(+) cocci, G(-) rods, and anaerobes

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27
Q

Monobactam drug

A

Aztreonam

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28
Q

Monobactam MOA

A

Beta lactam, less susceptible to beta-lactamase, synergistic with aminoglycosides, no cross-allergy with penicillins

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29
Q

Monobactam use

A

G(-) rods only, no G(+) rod or anaerobe coverage

For penicillin allergic patients and those with renal insufficiency that can’t handle aminoglycosides

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30
Q

Is Vancomycin affected by beta-lactamase?

A

No

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31
Q

Vancomycin use

A

G(+) only

MRSA, S epidermidis, Enterococcus, C difficile

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32
Q

Adverse effects of Vancomycin

A

Nephrotoxicity, Ototoxicity, Thrombophlebitis

Diffuse Flushing=Redman Syndrome: can be prevented by pretreatment with antihistamines and slow infusion rate

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33
Q

What are the protein synthesis inhibitors?

A

(Remember: buy AT 30, CCEL (sell) at 50)
30S inhibitors: Aminiglycosides (-cidal), Tatracyclines (-static)
50S inhibitors: Chloramphenicol, Clindamycin (both -static), Erythromycin (Macrolides, -static), Linezolid (variable)

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34
Q

What are the Aminoglycosides?

A

Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin

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35
Q

Aminoglycoside MOA

A

Bactericidal
Irreversibly binds 30S subunit preventing initiation complex and causing mRNA misreading
Requires O2 for uptake, therefore ineffective against anaerobes

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36
Q

Aminoglycoside adverse effects

A

Nephrotoxicity, Neuromuscular blockade, Ototoxicity (especially when used with loop diuretics), Teratogen

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37
Q

Aminoglycoside use

A

Severe G(-) rod infections
Synergistic with beta-lactam antibiotics
Neomycin for bowel surgery

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38
Q

Tetracycline drugs

A

Tetracycline, Doxycycline, Minocycline

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39
Q

Tetracycline MOA

A

Bacteriostatic
Binds 30S subunit preventing attachment of tRNA
Limited CNS penetration

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40
Q

Which of the Tetracyclines can be used in patients with renal failure?

A

Doxycycline because it is eliminated in the feces

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41
Q

Tetracyclines should not be taken with what because it inhibits absorption from the gut?

A

Milk, Antacids, iron containing preps because divalent cations inhibit absorption

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42
Q

Tetracycline use

A

Borrelia burgdorferi, M pneumoniae, Rickettsia, Chlamydia, acne

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43
Q

Tetracycline adverse effects

A

Teeth discoloration, inhibits bone growth in kids, photosensitivity
CI in pregnancy

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44
Q

Chloramphenicol MOA

A

Blocks peptidyltransferase at 50S ribosomal subunit

Bacteriostatic

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45
Q

Chloramphenicol use

A

Meningitis: H flu, N meningitidis, S pneumo
RMSF
Limited use in US because of toxicity, but used abroad because of low cost

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46
Q

Chloramphenicol adverse effects

A

Anemia, aplastic anemia, gray baby syndrome in premature infants because lack liver UDP-glucuronyl transferase

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47
Q

Clindamycin MOA

A

Blocks peptide transfer at 50S

Bacteriostatic

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48
Q

Clindamycin use

A

Anaerobe infections like Bacteroides and Clostridium in aspiration pneumonia, lung abscesses, oral infections
Also effective against invasive GAS infection
Treats anaerobes above the diaphragm whereas Metronidazole treats anaerobes below the diaphragm

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49
Q

Clindamycin adverse effects

A

Pseudomembranous colitis, fever, diarrhea

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50
Q

Linezolid MOA

A

binds 50S

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51
Q

Linezolid use

A

G(+) including MRSA and VRE

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52
Q

Linezolid adverse effects

A

Bone marrow suppression (especially thrombocytopenia), peripheral neuropathy, serotonin syndrome

53
Q

What are the Macrolides?

A

Azithromycin, Clarithromycin, Erythromycin

54
Q

Macrolide MOA

A

Prevents translocation by binding the 23S rRNA of 50S

Bacteriostatic

55
Q

Macrolide use

A

Atypical pneumonia (Mycoplasma, Chlamydia, Legionella)
STI’s (Chlamydia)
G(+) cocci (strep infections in patients allergic to penicillin)
B pertussis

56
Q

Macrolide adverse effects

A 
GI motility problems
Arrhythmia from prolonged QT
Acute cholestatic hepatitis
Rash
Eosinophilia
All but Azithromycin inhibit P450
57
Q

Sulfonamide MOA

A

Inhibits folic acid synthesis by Dihydropteroate Synthase inhibition

58
Q

Sulfonamide use

A

G(+), G(-), Nocardia, Chlamydia, SMX for simple UTI

59
Q

Sulfonamide adverse effects

A

Hypersensitivity, hemolysis if G6PD deficient, nephrotoxicity, photosensitivity, displaces drugs form albumin like warfarin
Inhibit P450

60
Q

Dapsone MOA, Use, and Adverse effects

A

Similar to sulfonamide in function, used for Leprosy and prophylaxis for Pneumocystis jirovecii
Hemolysis in G6PD deficiency

61
Q

Trimethoprim MOA

A

Inhibits folic acid synthesis by inhibiting Dihydrofolate reductase

62
Q

Trimethoprim use

A

In combination with sulfonamides to cause sequential block of folate synthesis
UTI’s, shigella, salmonella, Peumocystis jirovecii treatment and prophylaxis, Toxoplasmosis prophylaxis

63
Q

Trimethoprim adverse effects

A

Bone marrow suppression: megaloblastic anemia, leukopenia, granulocytopenia

64
Q

What are the Fluoroquinolones?

A

Ciprofloxacin, Norfloxacin, Levofloxacin, Ofloxacin, Moxifloxacin, Gemifloxacin, Enoxacin

65
Q

Fluoroquinolone MOA

A

Inhibits prokaryote DNA gyrase (topoisomerase II and IV)

66
Q

Fluoroquinolone use

A

G(-) rods of urinary and GI tracts including Pseudomonas

Neisseria and some G(+)

67
Q

Fluoroquinolone adverse effects

A

CI in pregnant and nursing women and kids under 18 because can damage cartilage
May prolong QT
May cause tendonitis and tendon rupture in those over 60 and in patients taking prednisone

68
Q

Daptomycin MOA

A

Lipopeptide that disrupts cell membrane of G(+) cocci

69
Q

Daptomycin use

A

S aureus skin infections (especially MRSA), bacteremia, endocarditis, VRE
Not used for pneumonia because inactivated by surfactant

70
Q

Daptomycin adverse effects

A

Myopathy, rhabdomyolysis

71
Q

Metronidazole MOA

A

Forms toxic free radicals that damage DNA

Antiprotozoal also

72
Q

Metronidazole use

A

Treats anaerobes below the diaphragm whereas Clindamycin treats them above
Giardia, Entamoeba, Trichomonas, Gardnerella, Anaerobes like bacteroides and C difficile
Used with PPI and clarithromycin for triple therapy against H pylori

73
Q

Prophylaxis and treatment for M avium-intracellulare

A

Prophylaxis: Azithromycin, rifabutin
Treatment: Azithromycin or Clarithromycin + ethambutol
Can also add rifabutin or ciprofloxacin

74
Q

Of the TB drugs, which work by inhibiting mycolic acid synth, araginoglycan synth, mRNA synth, and which have unclear mech?

A

Isoniazid: mycolic acid synthesis
Ethambutol: arabinoglycan synthesis
mRNA synthesis: Rifabutin and Rifampin
Unclear: Pyrazinamide

75
Q

What are the Rifamycins?

A

Rifampin, Rifabutin

76
Q

Rifamycin MOA

A

Inhibits DNA dependent RNA polymerase

77
Q

Rifamycin use

A

TB, delay resistance to dapsone in Leprosy, meningococcal prophylaxis

78
Q

What are Rifampin’s 4 R’s?

A

RNA polymerase inhibitor
Ramps up P450
Red/orange body fluids
Rapid resistance if used alone

79
Q

How are Rifampin and Rifabutin different?

A

Rifampin ramps up P450 and Rifabutin does not and is therefore preferred for use in HIV patients

80
Q

How is MRSA treated?

A

Vancomycin, Daptomycin, Linezolid, Tigecycline, Ceftaroline

81
Q

How is VRE treated?

A

Linezolid, Streptogramins

82
Q

How are MDR P aeruginosa and Acinetobacter baumannii treated?

A

Polymyxins B and E

83
Q

Amphotericin B MOA

A

Binds ergosterol and creates pores in fungal membrane

AmphoTEARicin

84
Q

Amphotericin B use

A

Serious systemic mycoses
Cryptococcus, Blastomyces, Coccidioides, Histoplasma, Candida, Mucor
Intrathecally for fungal meningitis
Supplement K+ and Mg+ because of altered renal tubule permeability

85
Q

Amphotericin B adverse effects

A

Fever/Chills, hypotension, nephrotoxicity, arrhythmias, anemia, IV phlebitis
Hydration decreases nephrotoxicity

86
Q

Nystatin MOA and use

A

Same MOA as Amphotericin B but topical only

Used most often for candida (oral, diaper, and vaginal)

87
Q

Flucytosine MOA

A

Inhibits DNA and RNA biosynthesis by conversion to 5-FU by cytosine deaminase

88
Q

Flucytosine Use

A

Systemic fungal infections (especially meningitis from Cryptococcus) in combo with Amphotericin B

89
Q

Flucytosine adverse

A

Bone marrow suppression

90
Q

What are the azoles?

A

Clotrimazole, Fluconazole, Itraconazole, Ketoconazole, Miconazole, Voriconazole

91
Q

Azole MOA

A

Inhibit fungal sterol synthesis by inhibiting P450 that converts lanosterol to ergosterl

92
Q

Azole use

A

Local and less serious systemic fungal infections
Fluconazole: chronic suppression of cryptococcal meningitis in AIDS and candidal infections of all types
Itraconazole: Blastomyces, Coccidioides, Histoplasma
Clotrimazole and Miconazole: topical fungal infections

93
Q

Azole adverse

A

Testosterone synth inhibition causing gynecomastia especially with ketoconazole
Liver dysfunction from P450 inhibition

94
Q

Terbinafine MOA, Use, Adverse

A

Inhibits fungal squalene oxidase preventing ergosterol synth
Dermatophytoses especially onychomycosis
Gi upset, headaches, hepatotoxicity, taste disturbance

95
Q

Name the echinocandins

A

Anidulafungin, Caspfungin, Micafungin

96
Q

Echinocandins MOA, Use

A

Inhibits fungal cell wall synth by inhibitingsynth of beta glucan
Invasive aspergillosis, candida

97
Q

Griseofulvin MOA

A

Microtubule function of fungus disrupts mitosis

Deposits in keratin-containing tissues

98
Q

Griseofulvin use

A

Oral treatment of superficial infections, inhibits growth of dermatophytes

99
Q

Griseofulvin adverse

A

Teratogenic, carcinogenic, confusion, headaches, induces P450 and warfarin metabolism

100
Q

Anti-mite and louse therapy

A

Permethrin: blocks Na channels
Malathion: AChE inhibitor
Lindane: Blocks GABA channels

101
Q

Chloroquine use

A

Treats Plasmodium except for P falciparum

Causes retinopathy and puritis

102
Q

How is P falciparum treated?

A

Atovaquone/Proguanil

103
Q

How is life-threatening malaria treated?

A

Quinidine in US

Quinine elsewhere

104
Q

Oseltamivir and Zanamivir MOA and use

A

Inhibit influenza neuraminidase preventing release of progeny virus for influenza A and B

105
Q

Acyclovir, Famciclovir, Valacyclovir MOA

A

Guanosine analogs
Monophosphorylated by HSV and VZV thymidine kinase in infected cells only so few side effects
Inhibits viral DNA polymerase by chain termination

106
Q

Acyclovir, Famciclovir, Valacyclovir use

A 
HSV and VZV
Weak against EBV and no effect in CMV
No effect on latent viruses
Valacyclovir has better oral availability
Famciclovir best for herpes zoster
107
Q

Acyclovir, Famciclovir, Valacyclovir adverse

A

Obstructin crystalline nephropathy and acute renal failure if not adequately hydrated

108
Q

Ganciclovir MOA and use

A

Guanosine analog activated by viral kinase in CMV inhibits DNA polymerase
Used for CMV especially in immune compromised
Valganciclovir better oral availability

109
Q

Ganciclovir adverse

A

Bone marrow suppression and renal toxicity

110
Q

Foscarnet MOA

A

Viral DNA/RNA polymerase inhibitor and HIV reverse transcriptase inhibitor
Binds to pyrophosphate-binding site of enzyme
Does not require kinase activation

111
Q

Foscarnet use

A

CMV retinitis in immune compromised when ganciclovir fails

Acyclovir-resistant HSV

112
Q

Foscarnet adverse

A

Nephrotoxicity

Seizures form electrolyte abnormalities

113
Q

Cidofovir

A

Similar to Foscarnet
DNA polymerase inhibition
Does not require phosphorylation
Used in CMV retinitis and acyclovir-resistant HSV
Has a long half-life
Adverse: nephrotoxicity–coadminister probenecid and IV saline to reduce toxicity

114
Q

How do the -navir HIV drugs work?

A

Protease inhibitors

115
Q

How do the HIV -TEGRavir drugs work?

A

InTEGRase inhibitors

116
Q

NRTI’s MOA and Drugs

A

Nucleot(s)ide Reverse Transcriptase Inhibitors
Abacavir, Didanosine, Emtricitabine, Lamivudine, Stavudine, Tenofovir, Zidovudine
Tenofovir is a nucleotide, all others are nucleosides and require phosphorylation before being active
ZDV can be used for general prophylaxis and in pregnancy to decrease risk of passing on virus

117
Q

NRTI’s adverse

A

Bone marrow suppression (can be reversed with G-CSF and EPO)

118
Q

NNRTI’s MOA and Drugs

A

Inhibit reverse transcriptase at a different place than NRTI’s and don’t require phosphorylation to be active.
Delavirdine, Efavirenz, Nevirapine
Many CI in pregnancy

119
Q

HIV protease inhibitors MOA and drugs

A

Inhibit HIV-1 protease
All end in -navir
Atazanavir, Darunavir, Fosamprenavir, Ininavir, Lopinavir, Ritonavir, Saquinavir
Ritonavir can boost other drug concentrations by inhibiting P450
Rifampin is CI with all these drugs because it induces P450

120
Q

HIV integrase inhibitors

A

Inhibits HIV viral integration into host genome
All end in -tegravir
Raltegravir, Elvitegravir, Dolutegravir

121
Q

HIV fusion inhibitors

A

Enfuvirtide: Binds gp41 inhibiting viral entry
Maraviroc: Binds CCR-5 on surface of T-cells/monocytes inhibiting interaction with gp120

122
Q

What are interferons?

A

Glycoproteins usually synthesized by viral-infected cells that exhibit a range of antiviral and antitumoral properties

123
Q

What is IFN-alpha used for?

A

Treat chronic Hep B and C, kaposi sarcoma, hairy cell leukemia, condyloma acuminatum, renal cell carcinoma, malignant melanoma

124
Q

What is IFN-beta used for?

A

Multiple Sclerosis

125
Q

What is IFN-gamma used for?

A

Chronic granulomatous disease

126
Q

What are the adverse effects of treatment with interferons?

A

These are normally made by viral infected cells so you will have Sx of a viral infection: flu-like Sx, depression, neutropenia, myopathy

127
Q

What drugs are used in Hep C treatment?

A

Ribavirin, Sofosbuvir, Simeprevir

128
Q

Which antimicrobials should be avoided during pregnancy?

A 
Remember: SAFe Children Take Really Good Care
Sulfonamides–kernicterus
Aminoglycosides–ototoxicity
Fluoroquinolones–cartilage damage
Clarithromycin–embryotoxic
Tetracycline–discolored teeth, inhibits bone growth
Ribavirin–teratogenic
Griseofulvin–teratogenic
Chloramphenicol–gray baby

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