Pharm Block4 Pack2

Front 1

What are the two natural Penicillins?

Back 1

Penicillin G
Penicillin V

Front 2

What is another name for Penicillin V?

Back 2

Phenoxymethyl penicillin

Front 3

What is the difference between the two major natural penicillins?

Back 3

Penicillin G --> oral or parenteral || half-life = 30 min
Penicillin V is ORAL ONLY || half-life = 1 hr

Front 4

Why does Pencillin G require a q 4 hr dosing regimen for severe infections?

Back 4

SHORT HALF LIFE
(only 30 min long)

Front 5

What are the two repository forms of penicillin G that can be given IM?

Back 5

Procaine penicillin G
Benzathine penicillin G

Front 6

What is the difference between Procaine penicillin G
and Benzathine penicillin G?

Back 6

Procaine penicillin G half-life = 6-8 hrs
Benzathine penicillin G half-life = 6 days!!!!

Front 7

What are penicillinase-resistant penicillins also known as?

Back 7

Anti-staphylococcal penicillins

Front 8

What are the 5 penicillinase-resistant Penicillins?

Back 8

METHIcillin
OXAcillin
NAFcillin
CLOXAcillin
DICLOXAcillin

Front 9

What are the half-lives of all the penicillinase-resistant penicillins?

Back 9

ALL are 30 min!

Front 10

Which two penicillinase-resistant penicillins are administered orally?

Back 10

CLOXacillin and DiCLOXacillin

Front 11

What are the 4 extended range penicillins?

Back 11

AMPIcillin
AMOXIcillin
TICARcillin
PIPERAcillin

Front 12

Which two extended-range penicillins can only be administered parenterally?

Back 12

Ticarcillin and Piperacillin

Front 13

What are the half-lives of all the extended-range penicillins?

Back 13

ALL are about 1 hr
*Piperacillin is 1.2 hrs

Front 14

Penicillins have variable oral absorption,
what is their metabolism and excretion like?

Back 14

MINIMALLY metabolized
Excreted in URINE

Front 15

Does anything block the excretion of Penicillins?

Back 15

YES --> Probenecid

Front 16

What is the function of Probenecid?

Back 16

Blocks the urinary excretion of Penicillins

Front 17

Where are Ampicillin and Nafcillin mostly excreted?

Back 17

Biliary Tract

Front 18

Do Penicillins cross into the CNS via the BBB? Prostate? The eyes?

Back 18

Penicillin crosses ONLY MINIMALLY into the CNS, prostate and eye

Front 19

Given the biliary tract excretion of Ampicillin and Nafcillin,
how could this be useful clinically?

Back 19

Liver abscesses or acute cholecystitis can be treated
with these agents b/c they can enter the protected site
*bacteria must be sensitive*

Front 20

What is the mechanism of action of Penicillins? Cidal or static?

Back 20

Interfere with cell wall synthesis
BACTERICIDAL

Front 21

What are the 3 ways Penicillins interfere w/ cell wall synthesis?

Back 21

1. Bind to specific receptors (PBPs) in the bacterial cytoplasmic membrane
2. Inhibit transpeptidase enzymes that cross-link linear peptidoglycan chains
3. Activate AUTOLYTIC ENZYMES

Front 22

What are the 3 mechanisms of resistance to Penicillins?

Back 22

1. Formation of Beta-Lactamases (penicillinases)
2. Mutation of PBP targets
3. Porin alterations (decreased penetration)

Front 23

What mechanism of microbial resistance do Staph have to Penicillin G?

Back 23

Formation of Beta-Lactamases that destroy the drug

Front 24

What mechanism of microbial resistance do Staph have to Methicillin?

Back 24

Mutation of penicillin binding protein targets

Front 25

What is the spectrum of activity of the narrow spectrum Penicillins (G and V)?
Hint: 4 Bugs/groups

Back 25

1.STREP PYOGENES (GAS)
2. Strep pneumococci
3. Some gram positive anaerobes
4. SYPHILIS (Treponoma pallidum)

Front 26

What is the spectrum of activity of Penicillinase-resistant Penicillins?

Back 26

Staph aureus
Staph epidermitis
*only works on sensitive strains (MSSA, MSSE)

Front 27

What do you use for Staph aureus or Staph epidermitis
that are resistant to Methicillin?

Back 27

VANCOMYCIN

Front 28

What is the spectrum of activity of the
extended-range penicillins: Ampicillin and Amoxicillin?

Back 28

E. coli, H. pylori, Strep pneumo
Listeria monocytogenes, Enterococci

Also:
Proteus mirabilis, Salmonella, Shigella,
H. influenzae, Moraxella catarrhalis, Borrelia bergdorfi

Front 29

Which bacteria are ALL sensitive to extended range pencillins?

Back 29

ALL LISTERIA ARE SENSITIVE!

Front 30

What is the spectrum of activity of Ticarcillin and Piperacillin?

Back 30

Gram negative microbes esp. PSEUDOMONAS

Front 31

What are the 3 clinical uses of Penicillin?

Back 31

1. Strep Pharyngitis
2. Rheumatic Fever Prophylaxis
3. Syphilis

Front 32

What is the clinical use of penicillinase-resistant penicillins?

Back 32

Staphylococcal infections
*only sensitive strains

Front 33

What are the 5 clinical uses of Ampicillin and Amoxicillin?

Back 33

1. Otitis media
2. Sinusitis
3. Pneumonia
4. UTIs
5. LYME DISEASE*

*Ceftriaxone IV is more effective

Front 34

What are the 2 clinical uses of Ticarcillin and Piperacillin?

Back 34

1. Pseudomonas infections
2. Mixed intra-abdominal infections

Front 35

What are the main toxicities of Penicillins?

Back 35

Allergic hypersensitivity
Hemotologic-penias & Hemolytic anemia (COOMBS POSITIVE)
Nephritis (esp. Methicillin)

Front 36

What are the minor toxicities of Penicillins?

Back 36

Diarrhea (common)
Seizures (high dose penicillin)
Drug fever
Elevated hepatic transaminases

Front 37

What penicillin causes serious diarrhea?

Back 37

Amoxicillin
*especially if combined w/ clavulanic acid to form AUGMENTIN

Front 38

What are the 3 manifestations of penicillin allergic hypersensitivity?

Back 38

1. Anaphylactic reactions
2. Rash
3. Urticaria

Front 39

What is the most nephrotoxic penicillin?
Hint: toxicity led to its disuse

Back 39

Methicillin

Front 40

What steps are taken in a patient w/ suspected Penicillin Allergy?

Back 40

1. Screening --> RAST (blood) test
2. Confirmation --> Skin tests
3. Trial in hospital
4. If positive --> DESENSITIZATION by allergist

Front 41

What are the 3 major FIRST generation Cephalosporins?

Back 41

Cefazolin
Cephalexin
Cefadroxil

Front 42

What is the difference b/w all the FIRST generation Cephalosporins?

Back 42

Cephalexin and Cefadroxil are ORAL equivalents of parenteral Cefazolin

Front 43

What are the 6 SECOND generation Cephalosporins listed?

Back 43

CefUROXIME (P)
CefOXITIN (P)
CefOTETAN (P)
CefUROXIME AXETIL (O)
CefACLOR (O)
CefPROZIL (O)

Front 44

Which Cephalosporin has the longest half-life?

Back 44

Cefotetan --> 3.5 hrs

Front 45

What are the 4 main THIRD generation Cephalosporins?

Back 45

CefOTAXIME (P)
CefTRIAXONE (P)
CefTAZIDIME (P)
CefDINIR (O)

*also Cefpodoxime (O)

Front 46

Which THIRD generation Cephalosporin has the longest half-life?

Back 46

Ceftriaxone --> 8 hrs

Front 47

With a half-life of 2 hrs, what is the only FOURTH generation Cephalosporin?

Back 47

CEFEPIME (P)

Front 48

Cephalosporins undergo renal elimination, how are they absorbed?

Back 48

Variable ORAL absorption ranges b/w 50% and 90%

Front 49

Which 2 Cephalosporins are well excreted into the biliary tract?

Back 49

Cefoperazone (3rd) and Ceftriaxone (3rd)

Front 50

Which third generation Cephalosporin is metabolized in the liver?

Back 50

Cefotaxime

Front 51

Which are the only generation Cephalosporins that
have been proven to reach good CNS levels?

Back 51

THIRD generation!

Front 52

Which two Cephalosporins are the only ones
that have activity against Pseudomonas?

Back 52

Ceftiazidime (3rd) and Cefepime (4th)

Front 53

Which Cephalosporin has the highest activity against Bacteroides fragilis?

Back 53

Cefotetan (2nd)

Front 54

What changes occur in the Cephalosporins' spectrum
of activity as you move up the generations?
Hint: 1st to 4th

Back 54

Initially only gram positive --> then progressively greater activity
against gram negative organisms

Front 55

Which generation Cephalosporin has the greatest gram positive activity?

Back 55

FIRST generation

Front 56

Which generation are good for Listeria, Atypical bacteria, MRSA, or Enterococci?

Back 56

NONE!
cuz cephalosporins are LAME!

Front 57

Which 4 bugs/groups are Cephalosporins NO GOOD for?
Hint: Cephalosporins are LAME!

Back 57

1. Listeria
2. Atypical bacteria
3. MRSA
4. Enterococci

Front 58

Which two Cephalosporins have good anaerobic coverage?

Back 58

CefOXITIN and CefOTETAN

Front 59

What is the DOC for Borrelia bergdori?
What is an adverse effect of this tx?
How can this be prevented?

Back 59

CEFTRIAXONE
Cholecystitis in young women given IV Ceftriaxone
USE LOWER DOSES

Front 60

What are the 2 clinical uses of FIRST generation Cephalosporins?

Back 60

1. Surgical prophylaxis
2. Soft tissue infections

Front 61

What is the 1 clinical use of SECOND generation Cephalosporins?

Back 61

1. Intra-abdominal infections

Front 62

What is the main group of infections for which we use Ceftriaxone/Cefotaxime?

Back 62

Serious pediatric infections (meningitis, broad spectrum)

Front 63

Which 5 bugs/groups are Ceftriaxone/Cefotaxime NOT used
for when treating serious pediatric infections?

Back 63

1. Listeria
2. Anaerobes
3. MRSA
4. Enterococci
5. Pseudomonas

Front 64

What is the chief clinical use of Ceftazidime?

Back 64

Pseudomonas infections

Front 65

Cefepime, a 4th generation Cephalosporin is used to tx very broad spectrum infections; EXCEPT those caused by what 4 organisms?

Back 65

1. Listeria
2. Anaerobes
3. MRSA
4. Enterococci

Front 66

What are the 3 major toxicities of all Cephalosporins?

Back 66

1. Allergic/ Hypersensitivity
2. Disulfiram-like reaction
3. Phlebitis @ infusion site

Front 67

Which 2 Cephalosporins cause a Disulfiram-like reaction w/ alcohol?

Back 67

Cefamandole and Cefoperazone
*get headache, nausea, vomiting, abdominal pain

Front 68

Which 2 Cephalosporins cause a bleeding diathesis at toxic levels?

Back 68

Cefamandole or Cefoperazone

Front 69

Which Cephalosporin toxicity leads to biliary obstruction?

Back 69

Ceftriaxone (when infused rapidly)

Front 70

What are the 3 Beta Lactam inhibitors?

Back 70

Clavulanic Acid
Sulbactam
Tazobactam

Front 71

Augmentin is combination of Clavulanic Acid and what beta lactam?

Back 71

Amoxicillin

Front 72

Amoxicillin-Clavulanic Acid is called what? How is it administered?

Back 72

AUGMENTIN
Oral

Front 73

Ticarcillin-Clavulanic Acid is called what? How is it administered?

Back 73

TIMENTIN
Parenteral

Front 74

Ampicillin-Sulbactam is called what? How is it administered?

Back 74

UNASYN
Parenteral

Front 75

Piperacillin-Tazobactam is called what? How is it administered?

Back 75

ZOSYN
Parenteral

Front 76

Combining beta lactam antibiotics w/ beta lactamase
inhibitors broaden the spectrum against...

Back 76

S. aureus, H. influenzae
Bacteroides, Moraxella catarrhalis
Gram negative enteric bacteria

Front 77

What is the only monobactam?

Back 77

Aztreonam

Front 78

What are the 3 carbapenems?

Back 78

IMIpenem
MEROpenem
ERTApenem

Front 79

Which Carbapenem has the best CNS penetration?

Back 79

MEROPENEM
*Ertapenem may or may not penetrate BBB

Front 80

Aztreonam (a monobactam) and the Carbapenems are excreted renally. What is administered with Imipenem to inhibit this renal inactivation?

Back 80

CILASTIN
(inhibits renal inactivation by dehydropeptidase1)

Front 81

Are Aztreonam and the Carbapenems susceptible to beta-lactamases?

Back 81

MINIMALLY susceptible to beta-lactamases
EXCEPT if bugs are making ESBLs!!!!
(Extended Spectrum Beta-Lactamases)

Front 82

What is the spectrum of Aztreonam?

Back 82

ONLY gram negative bugs
(including Pseudomonas, NOT anaerobes)

Front 83

What is the spectrum of Carbapenems?

Back 83

VERY BROAD SPECTRUM
Last resort for resistant organisms*

*EXCEPT Listeria, MRSA, some Enterococci,
some Pseudomonas, some anaerobes

Front 84

Which Carbapenem is NOT effective against anaerobes

Back 84

Ertapenem

Front 85

What is the DOC for oral tx of animal bites?

Back 85

Augmentin

Front 86

What are the 2 clinical uses of Carbapenems?

Back 86

1. Empiric tx of pts that CRASH secondary to infection w/ resistant organisms
2. "Mixed" intra-abdominal and pelvic infections (helps avoid using multiple antibiotics)

Front 87

What are the toxicities of the Carbapenems?
Hint: they are the usual ones

Back 87

GI, Allergic, Renal, Hepatic,
Hematologic, Drug Fever, Bacterial or Fungal Overgrowth

Front 88

What is the major toxicity of Imipenem?

Back 88

Rare neurologic reactions (seizures) w/ HIGH DOSES
or in renal failure pts

Front 89

Which antibiotics is the complex gluco-polypeptide Vancomycin related to?

Back 89

NONE - it's G as fuck
*Most important antibiotic for tx of GRAM POSITIVE bugs

Front 90

Vancomycin (half-life = 6 hrs) is renally excreted and absorbed orally right?

Back 90

WRONG - not absorbed orally!
*so it works well on C. difficile infections in the GI

Front 91

How does Vancyomycin penetrate the CNS, prostate, and eye?

Back 91

POORLY - inadequate penetration

Front 92

What is the mechanism of action of Vancyomycin?
Hint: works on dividing gram positive organisms

Back 92

Irreversibly inhibits biosynthesis of peptidoglycan polymers in cell wall
--> Blocks cell wall synthesis

Front 93

What is the RARE mechanism of microbial resistance against Vancyomycin?

Back 93

Mutation of target binding site

Front 94

What is the spectrum of Vancyomycin?
Hint: it's NARROW

Back 94

Gram Positive Organisms
MRSA, enterococci, and pneumococci
Clostridium difficile

Front 95

What is Vancyomycin the DOC for?

Back 95

Serious infecitons w/ RESISTANT gram positive bugs
MRSA, PCN resistant pneumococci, etc.

Front 96

Is Vancyomycin effective for lung infections?

Back 96

Not really

Front 97

What is Vancyomycin the second DOC for?

Back 97

ORAL tx of Pseudomembranous colitis
*current DOC is Metronidazole

Front 98

What are the 3 toxicities of Vancyomycin? Hint: significant!

Back 98

1. Renal
2. Auditory - dose-related (ADULTS!)
3. "Red Man" Syndrome

Front 99

How can the toxicity "Red Man" syndrome be ameliorated in Vancyomycin tx?

Back 99

SLOW INFUSION

Front 100

Daptomycin, a lipopeptide antibiotic, is administered only which way?

Back 100

IV administration only

Front 101

What is the unique mechanism of action of Daptomycin?
Hint: it is CIDAL, 3 ways of disruption

Back 101

Interferes w/ cell wall synthesis by disrupting:
1. Peptidoglycan synthesis
2. Lipoteichoic acid synthesis
3. Bacterial membrane potential

Front 102

Are there any mechanisms of resistance to Daptomycin?

Back 102

RARE
not yet defined

Front 103

What is the spectrum of Daptomycin? Hint: narrow

Back 103

Gram positive organisms
*includes Linazolid resistant MRSA, VRE, etc.

Front 104

What are the MIC for Daptomycin? What does this mean?

Back 104

MICs tend to be low
VERY SENSITIVE!

Front 105

What are the 3 clinical uses of Daptomycin?

Back 105

1. Skin and soft tissue infections
2. Sepsis
3. Endocarditis

Front 106

Can Daptomycin be used in children?

Back 106

NO - it's not yet approved

Front 107

With a half-life of 9 hrs, Daptomycin is administered once daily,
what is its activity like?

Back 107

Rapid, concentration-dept activity

Front 108

Describe Daptomycin's post-antibiotic effect?

Back 108

Prolonged and concentration-dept post antibiotic effect

Front 109

How is Daptomycin primarily excreted?

Back 109

KIDNEY
(80% total dose)

Front 110

How often is Daptomycin administered?

Back 110

Once daily

Front 111

What are the adverse effects of Daptomycin?

Back 111

1. Transient muscle weakness
2. Myalgias
*due to CPK levels (MM isoenzyme)

Front 112

Previous Daptomycin dosing called for twice-daily administration which led to transient muscle weakness and myalgias due to increased CPK levels, how can this be fixed?

Back 112

ONCE DAILY DOSING --> increases therapeutic-toxicity ratio
(increases efficacy and decreases skeletal muscle adverse effects