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ALCB - Pharma > 5 - Antimicrobials > Flashcards

5 - Antimicrobials Flashcards

1
Q

Antimicrobial coverage of extended spectrum penicillins

  • Amox
  • Ampi
A

Amoxicillin HELPS kill Enterococci

  • Haemophilus influenzae
  • E. coli
  • Listeria monocytogenes
  • Proteus mirabilis
  • Salmonella sp
  • Enterococci
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2
Q

BacteriCIDAL

A

Very Finely Proficient At Murder

  • vancomycin
  • flouroquinolones
  • penicillins
  • aminoglycosides
  • metronidazole
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3
Q

BacterioSTATIC

A

we’re ECSTaTiC about bacteriostatics

  • erythromycin
  • clindamycin
  • sulfamethoxazole
  • trimethoprim
  • tetracycline
  • chlorampenicol
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4
Q

Antipseudomonal Penicillins

A

TCP: Take Care of Pseudomonas

  • ticarcillin
  • carbenicillin
  • piperacillin
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5
Q

First generation cephalosporins cover which microbes

A

PEcK 1st

  • proteus mirabilis
  • E. coli
  • Klebsiella pneumoniae
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6
Q

First gen cephalosporins

A

FADer, help me FAZ my PHarmacology boards!

  • cefadroxil
  • cefazolin
  • cephalothin
  • cephapirin
  • cephradine
  • cephalexin
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7
Q

Second generation cephalosporins cover which microbes

A

HEN PEcKS

  • Haemophilus influenzae
  • Enterobacter aerogenes
  • Neisseria spp.
  • Proteus mirabilis
  • E. coli
  • Klebsiella pneumoniae
  • Serratia marcescens
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8
Q

Second generation cephalosporins

A

in a FAMily gathering, you see your FOXy cousin wearing a FUR coat and drinking TEA.

  • ceFAMandole
  • ceFOXitin
  • ceFURoxime
  • cefoTEtan

FAC! LORA the PROfessional AZhOLE is still on the FONe.

  • ceFAClor
  • LORAcarbef
  • cefPROzil
  • cefmetAZOLE
  • ceFONicid
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9
Q

DOC for gonorrhea

A

Ceftriaxone and Cefixime

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10
Q

3rd gen cephalosporins with anti-pseudomonal activity

A

Pag may pseudomonas, kailangan ma-ICU

  • need ng PERA (cefoPERAzone)
  • sosyal ka, ayaw ng pera pero gusto ng DIME (ceftaziDIME)
  • kailangan malakas like TRIathlete (cefTRIaxone) - case to case basis
  • cefoperazone
  • ceftazidime
  • ceftriaxone
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11
Q

DOC for syphilis

A

Penicillin

  • binds to PBP
  • inhibits transpeptidation in bacterial cell walls
  • narrow spectrum
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12
Q

Anti-pseudomonal cephalosporins

A
  • ceftazidime
  • cefoperazone
  • cefepime
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13
Q

Commonly used against Bacteriodes

A

Ceftizoxime

- 3rd gen

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14
Q

Most active 3rd gen cephalosporins against Penicillin-resistant S. pneumoniae

A
  • ceftriaxone

- cefotaxime

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15
Q

Cell wall inhibitors RESISTANT to beta-lactamase (penicillinase)

A
  • methicillin

- 4th gen cephalosporins (ceftaroline, cefpirome)

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16
Q

Beta-lactam antibiotic reserved for serious life-threatening infections such as pneumonia and sepsis

A

Carbapenem

  • imipenem-cilastatin
  • ertapenem
  • meropenem
  • doripenem

-has wide coverage

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17
Q

It inhibits renal metabolism (hydrolysis) of imipenem by dihydropeptidase

A

Cilastatin

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18
Q

All carbapenems are active against Pseudomonas and Acinetobacted EXCEPT __________

A

Ertapenem

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19
Q

Given with imipenem which will act as dihydropeptidase inhibitor

A

Cilastatin

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20
Q

Cilastatin is added to what carbapenem

A

Imipenem

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21
Q

Carbapenem which has longer half-life but less active against Enterococci and Pseudomonas

A

Ertapenem

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22
Q

All 3rd gen cephalosporins are renally excreted EXCEPT ___________

A
  • cefoperazone

- ceftriaxone

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23
Q

All 3rd gen cephalosporins penetrate BBB EXCEPT ____________

A
  • cefoperazone

- cefixime

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24
Q

3rd gen cephalosporin that has very good CNS penetration

A

Ceftriaxone

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25
Q

3rd gen cephalosporins should be reserved against serious infection EXCEPT ______________

A
  • ceftriaxone

- cefixime

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26
Q

It is used for infections resistant to beta-lactamases produced by G (-) rods
- silver bullet

A

Aztreonam

- monobactam

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27
Q

Beta-lactamase inhibitors

A

CST

  • clavulanic acid (amox)
  • sulbactam (ampi)
  • tazobactam (piperacillin)
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28
Q

Plasmid encoded B-lactamases organisms

A

GESH

  • gonorrhea
  • E. coli
  • streptococci
  • H. influenzae
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29
Q

Inducible chromosomal B-lactamases organisms

A

PES

  • pseudomonas
  • enterobacter
  • serratia
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30
Q

4th gen cephalosporin for MRSA

A

Ceftaroline

- bactericidal

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31
Q

Inhibits cell wall synthesis by binding to D-Ala-D-Ala terminus which will inhibit transglycosylation eventually preventing elongation and cross-linking of peptidoglycan chain

A

Glycopeptide
Vancomycin

  • Teicoplanin
  • Dalbavancin
  • Telavancin
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32
Q

A/E: Red Man Syndrome

A

Vancomycin

  • treated by slowing rate of infusion
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33
Q

What formulation of vancomycin (glycopeptide) is used for pseudomembranous colitis

A

Oral

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34
Q

VRSA and VRE are due to _________

A

D-Ala-D-Lactate formation

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35
Q

These glycopeptides are not absorbed in the GIT thus used for bacterial enterocolitis

A

TT

  • teicoplanin
  • telavancin
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36
Q

Glycopeptide that has very long half-life (6-11 days) which permits 1/week dosing and is more active than Vancomycin

A

Dalbavancin

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37
Q

Drugs of Last Resort

A

I AM your Last Shot at Victory

  • imipinem
  • amikacin
  • meropenem
  • linezolix
  • streptogramins
  • vacomycin
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38
Q

Peptide antibiotic which interferes with a late stage in cell wall synthesis in G(+)

A

Bacitracin

  • NEPHROTOXIC!!!
  • topical ONLY
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39
Q

Used for drug-resistant TB (2nd line) which blocks INCORPORATION of D-Ala into the pentapeptide side chain of the peptidoglycan

A

Cycloserine

  • neurotoxic
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40
Q

It binds to cell membrane causing DEPOLARIZATION and RAPID CELL DEATH

Rapidly inactivated by pulmonary surfactants

A

Daptomycin

  • G(+) including sepsis and endocarditis
  • A/E: myopathy - requires creatine phospholinase monitoring
  • inactivates by pulmonary surfactants
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41
Q

Inactivates UDP-N-acetylglucosamine-3-enolpyruvyltransferase which is important in peptidoglycan synthesis

A

Fosfomycin

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42
Q

Protein synthesis inhibitors

A

AT (30s) CELLS (50s)

  • aminoglycosides
  • tetracycline
  • Chloramphenicol
  • erythromycin (macrolides)
  • lincosamides (clindamycin)
  • linezolid
  • Streptogramins
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43
Q

All protein synthesis inhibitors are bacterioSTATIC except ___________ to the following bugs:

  • haemophilus
  • neisseria
  • bacteroides
  • s. pneumoniae
A
  • aminoglycosides
  • streptogramins
  • chloramphenicol
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44
Q 
All protein synthesis inhibitors are bacterioSTATIC EXCEPT:
- aminoglycosides
- streptogramins
- chloramphenicol
 to the following bugs \_\_\_\_\_\_\_\_\_\_\_\_\_\_\_
A
  • haemophilus
  • neisseria
  • bacteroides
  • s. pneumoniae
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45
Q

Drug that this bacteriostatic BUT CIDAL to:

  • haemophilus
  • neisseria
  • bacteroides
  • s. pneumoniae
A

Chloramphenicol

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46
Q

Chloramphenicol is bacteriostatic but CIDAL to what bugs:

A
  • haemophilus
  • neisseria
  • bacteroides
  • s. pneumoniae
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47
Q

Gray baby syndrome

A

Chloramphenicol

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48
Q

Administration of Chloramphenicol will cause this condition that is characterized by:

  • decreased RBCs
  • cyanosis
  • CV collapse
  • ashen gray skin
A

Gray Baby Syndrome

Premature neonates are deficient in hepatic glucuronosyl transferase
- glucuronidation of chloramphenicol

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49
Q

Causes tooth enamel dysplasia/discoloration

A

TEETHracycline

Tetracycline

Block aTTachment of T-RNA to acceptor site

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50
Q

Broadest spectrum and longest half life tetracycline

A

Tigecycline (30-36 hours)

51
Q

All tetracyclines are excreted renally EXCEPT

A

Doxycycle

- bile

52
Q

Tetracycline that is given only through IV and is unaffected by common tetracycline resistance mechanisms

A

Tigecycline

53
Q

Macrolide uses:

  • erythromycin
  • azithromycin
  • clarithromycin
  • telithromycin
  • roxithromycin
A
  • CAP
  • pertussis
  • diphtheria
  • chlamydia
54
Q

Macrolide that may cause rare fulminant hepatic failure

A

Telithromycin

55
Q

All macrolides inhibit CYP450 except

A

Azithromycin

56
Q

Macrolide that has the high distribution of volume and longest half-life

A

Azithromycin

57
Q

Macrolide used for macrolide-resistance

A

Telithromycin

- may cause rare fulminant hepatic failure

58
Q

Resistance of macrolide is due to:

A
  • Development of efflux pumps

- Production of methylase enzyme

59
Q

Resistance of chloramphenicol is due to:

A

Formation of acetyltransferase that inactivates drug

60
Q

Resistance of tetracycline is due to:

A
  • Development of efflux pumps for active extrusion of tetracyclines
  • formation of ribosomal protection proteins that interfere with tetracycline binding
61
Q

Lincosamide drugs

A
  • clindamycin
  • lincomycin

A/E: pseudomembranous colitis (C. difficile overgrowth)

For PCP pneumonia

G(-) aerobes are resistant because of poor penetration through outer membrane

62
Q

Linsamide resistance is due to:

A
  • methylation of binding siyes and enzymatic inactivation
63
Q

Anaerobic infections ABOVE the diaphragm

A

Clindamycin

64
Q

Anaerobic infections BELOW the diaphragm

A

Metronidazole

65
Q

Used for drug-resistant G(+) cocci such as Staphylococci and E. faecium (MRSA, VRSA, VRE)

  • inhibits CYP450 (multiple drug reactions)
  • A/E: injection site reactions, severe arthralgia/myalgia syndrome
A

Streptogramin
- cidal

Quinipristin-Dalfopristine

66
Q

Used for drug-resistant G(+) cocci such as Staphylococci and E. faecium (MRSA, VRSA, VRE) + Corynebacteria, Listeria

A/E: serotonin syndrom (with ssri), optic neuritis, BM suppression

A

Oxazolidinone

  • Linezolid
  • Tedizolid

Binds to 23s subunit of 50s

67
Q

Oxazolidinone (linezolid) resistance is due to:

A

Decreased affinity of drug to binding site

68
Q

Macrolides mneomic

A

CRATE

  • clarithromycin
  • Roxithromycin
  • Azithromycin
  • Telithromycin
  • Erythromycin
69
Q

Class of antibiotic that has POST-ANTIBIOTIC EFFECT

A

Aminoglycosides
- killing continues when their plasma levels have declined below measurable levels
PROTOCOL BASIS:
- shorter with single large dose than multiple small doses

Quinolones
- interfere with bacterial DNA synthesis

70
Q

How is aminoglycoside bacteriCIDAL?

A
  • because of misreading
  • it occupies a large space in P site that will cause misreading
  • concept of STOP CODON
71
Q

Aminoglycoside that has the NARROWEST therapeutic window

A

Amikacin

Aminoglycosides in general:

  • not absorbed if oral
  • better: IM/IV
  • not readily cross BBB
  • excretion: Glomerular filtration
72
Q

Class of antimicrobial that has synergistic effect with cell wall inhibitors (enhancement of transport)

A

Aminoglycosides

GNATS NOT

  • gentamicin
  • neomycin
  • amikacin
  • Tobramycin
  • Streptomycin
  • Nephrotoxic
  • Ototoxix
  • Teratogen
73
Q

MOA of aminoglycosides

A

Bind to 30S:

  • block formation of initiation complex
  • cause misreading of the code (mRNA template)
  • inhibit translocation
74
Q

Resistance to aminoglycosides

A
  • plasmid-mediated formation of inactivating enzymes (group transferases)

Amikacin - often resistant

Streptomycin resistance - changes to ribosomal binding site

75
Q

Streptomycin resistance is due to:

A

Changes in the ribosomal binding site

76
Q

Aminoglycoside that is often resistant to many enzymes that inactivate orher aminoglycosides

A

Amikacin

- has the narrowest therapeutic window

77
Q

Aminoglycosides need ______ for uptake

A

Oxygen (O2)

  • DOES NOT work on ANAEROBIC conditions
78
Q

Aminoglycoside drugs

A

GNATS

  • gentamicin
  • neomycin
  • amikacin
  • tobramycin
  • streptomycin
79
Q

Most vestibulotoxic and nephrotoxic aminoglycosides

A
  • gentamicin
  • tobramycin

Cumulative ototoxicity with loop diuretics

80
Q

Aminoglycoside used in multi drug-resistant TB (2nd line)

A

Amikacin

  • least resistance
  • narrowest therapeutic window

Cycloserine

  • Cell wall inhibitor used for drug-resistant TB (2nd line)
  • blocks incorporation of D-ala into the pentapeptide
  • neurotoxic
81
Q

Aminoglycoside that causes congenital deafness

A

Streptomycin

82
Q

Aminoglycoside used to TB, tularemia, bubonic plague, brucellosis, enterococcal endocarditis

A

Streptomycin

  • has widespread resistance due to changes in the ribosomal binding site
  • given with Pens: for enterococcal endocarditis, TB plague, tularemia
83
Q

Most ototoxic aminoglycoside

A

Kanamycin and amikacin

84
Q

Aminoglycoside that is limited to topical and oral use

85
Q

Reverse neuromuscular blockade of aminoglycosides (Neomycin/Kanamycin/Paromomycin)

A

Calcium gluconate and neostigmine

86
Q

Aminoglycoside used for visceral leishmaniasis

A

Paromomycin

87
Q

Aminoglycoside used for drug-resistant gonorrhea and gonorrhea in penicillin-allergic patients

A

Spectinomycin

  • no cross resistance with other gonorrheal drugs
  • IM
88
Q

Aminoglycoside that has anemia as side effect

A

Spectinomycin

89
Q

Aminoglycosides that causes skin reactions

A

Neomycin and streptomycin

90
Q

Protein synthesis inhibitor - inhibits translocation process during protein synthesis

A

Fusidic acid or Na Fusidate

  • isolated from fermentation of Fusidium coccineum
  • topical for skin pathogens including S. aureus
91
Q

Isolated from fermentation of Fusidium coccineum

A

Fusidic acid or Na Fusidate

  • inhibits translocation process during protein synthesis
  • topical for skin pathogens including S. aureus
92
Q

Antifolate drugs that is weakly acid that have a common chemical nucleus resembling p-aminobenzoic acid (PABA)

A

Sulfonamides

93
Q

Antifolate drug that is weakly basic

A

Trimethoprim

- reaches high concentrations in prostatoc and vaginal fluids

94
Q

Competitive inhibitor of dihydropteroate SYNTHASE

A

Sulfonamides

  • bacteriostatic
  • selective toxicity results from the inability of mammalian cells to syntesize folic acid
  • compete with PABA
95
Q

Selective inhibitor of dihydrofolate REDUCTASE

A

Trimethoprim

- bacteriostatic

96
Q

Resistance to antifolate drugs

A

Plasmid-mediated and results from:

  • decreased intracellar accumulation of the drugs
  • increased production of PABA by bacteria
  • decrease in sensitivity of dihydropteroate synthase to sulfonamides
97
Q

Antifolate drug that inhibit dihyrdopteroate synthase for burn infections

A

Silver sulfadiazine / Mafenide acetate

98
Q

Antifolate drug that can cause metabolic acidosis and penetrate eschar

A

Mafenide acetate

99
Q

Sulfonamide that is only for lower UTI

A

Sulfisoxazole

100
Q

DOC for toxoplasmosis

A

Sulfadiazine-Pyrimethamine

101
Q

Antifolate drug 2nd line agent for Malaria

A

Sulfadoxine-Pyrimethamine

102
Q

Antifolate drug that is used for lower UTI and may be safely given to patients with sulfonamide allergy

A

Trimethoprim

103
Q

Antifolate drugs that is co-administered with Leucovorin to limit bone marrow toxicity

A

Pyrimethamine

104
Q

Class of antibiotics that displace bilirubin binding sites leading to kernicterus

A

Sulfonamides

105
Q

Toxicities of sulfonamides

A
  • hypersensitivity
  • gastrointestinal distress
  • hematotoxicity
  • nephrotoxicity
  • drug interactions
106
Q

Class of antibiotics that displace protein binding affecting levels of warfarin and methotrexate

A

Sulfonamides

107
Q

Drug interactions seen in sulfonamides

A
  • displace protein binding affecting levels of warfarin and methotrexate
  • displace bilirubin binding sites leading to kernicterus
108
Q

What class of antibiotics will you see greater coverage for G(+) organisms as you increase the generation?

A

Quinolones

Cephalosporins
- increase generation, increase G(-) activity

109
Q

MOA of Quinolones

A

Interfere with DNA synthesis by inhibiting:

  • Topoisomerase II (DNA Gyrase) - G(-) which prevents relaxation of supercoiled DNA
  • Topoisomerase IV - G(+) which interferes with the separation of replicated chromosomal DNA during cell division
110
Q

Class of antibiotic that may damage growing cartilage and cause arthropathy

A

Quinolones

111
Q

Resistance to Fluoroquinolones

A
  • decreased intracellular accumulation of the drug via production of efflux pumps
  • changes in porun structure
  • changes in the sensitivity of the target enzymes via point mutations in the antibiotic binding regions
112
Q

Quinolone that is 2nd line drug to TB

A

Ciprofloxacin and others
- 2nd gen quinolones
Levofloxacin and others
- 3rd gen

Other:

  • norfloxacin
  • ofloxacin
  • lemofloxacin
  • enoxacin

2nd line TB drugs

  • cycloserine (blocks incorporation of D-ala into the pentapeptide) - drug-resistant TB
  • streptomycin (aminoglycoside) - multi drug-resistant TB
113
Q

Class of antibiotics that enhance the toxicity of methylxanthine (theophylline)

A

Quinolones

114
Q

Quinolone that is most active against G(-) esp Pseudomonas

A

Ciprofloxacin

115
Q

General properties of Quinolones:

  • good oral bioavailability
  • high volume of distribution
  • half-life: 3-8 hours
  • absorption impeded by antacids
  • elimination bia kidneys by tubular secretion (may compete with probenecid)

EXCEPT

A

Moxifloxacin

  • 3rd gen quinolone
  • NEVER USE for UTI
  • hepatic elimination
116
Q

Quinolone withdrawn due to severe cardiotoxicity (arrhythmias)

A

Grepafloxacin

117
Q

Quinolone withdrawn due to DM (cause hyperglycemia)

A

Gatifloxacin

118
Q

Quinolone that can be used against C. trachomatis

A

Ofloxacin

- 2nd gen

119
Q

Quinolone that can be used in CAP caused by:

  • Chlamydia
  • Legionella
  • Mycoplasma
A

Levofloxacin

- has superior activity against G(+) including S. pneumoniae

120
Q

Newest members of Quinolones that are considered to have the BROADEST SPECTRUM of activity with increased activity against anaerobes anf atypical agents

A

Moxifloxacin and Gemifloxacin

121
Q

Quinolones that can cause QT prolongation

A
  • gemifloxacin
  • levofloxacin
  • moxifloxacin
122
Q

Quinolones that has the WIDEST spectrum of activity

- enhanced activity against anaerobes

A

4th gen quinolones

  • trovafloxacin (hepatotoxic)
  • alatrofloxacin
  • prulifloxacin
  • clinafloxacin
123
Q

MOA of Metronidazole (Nitroimidazole, Antiprotozoal)

A

Reactive reduction by ferredoxin forming free radicals that distupt electron transport chain

  • A/E: metallic taste; Disulfiram reaction

Clara took the Pre-Med Test in the PM

  • chlorpropamide
  • cefoPerazone
  • cefaMandole
  • cefoTetan
  • Procarbazine
  • Metronidazole
124
Q

DOC for ameobiasis, giardiasis and pseudomembranous colitis

A

Metronidazole

ALCB - Pharma (13 decks)

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