Pharmacology: Chapter 43 Beta-Lactam Compounds

Front 1

If a person is given penicillin and the person blood is later tested and shows increased peniclloic acid what is occurring?

Back 1

The bacteria have a beta-lactamase that is cleaving penicillin

Front 2

Is penicillin G effective against yersinia and proteus species?

Back 2

no it is not effective against gram - rods but is effective against gram + organisms, gram - cocci like neisesseria and non-beta-lactamase anaerobes

Front 3

What penicllin is used to treat staph and strep that have beta lactamases? What is it not effective against?

Back 3

naficillin; however, it is not effective against enterococci, anaerobic and gram - rods and cocci

Front 4

Why are ampicillin and antipseudomonal penicillins called extended spectrum? How are they like normal penicllin?

Back 4

they have improved action against gram - organisms, but they are susceptible to beta-lactamase activity

Front 5

How do penicillins interfere with bacterial growth?

Back 5

they inhibit transpeptidation

Front 6

What is the function of penicillin binding protein (PBP)?

Back 6

to cross link a terminal alanine of a NAG-NAM subunit to a nearby peptide

Front 7

What are beta-lactams analogs of?

Back 7

D-ala-D-ala substrate

Front 8

What phase of a growth curve are penicillins effective in?

Back 8

log

Front 9

What are the 4 mechanisms of resistance to penicillins?

Back 9

1) beta-lactamase
2) PBP modifaction
3) impaired penetration
4) efflux

Front 10

Do staph a., haemophilus, E. coli have beta-lactamases that are more effective against penicillins or cephalosporins?

Back 10

penicillins

Front 11

What type of beta-lactamase do Psuedomonas aeruginosa and enterobacter have?

Back 11

extended-spectrum beta lactamases that are effective against both cephalosporins and penicllins

Front 12

Are carbapenems susceptible to penicillinases or cephalosporins?

Back 12

neither, but they are susceptible to metallo-beta lactamases and carbapenemases

Front 13

What resulted to give staph resistance to methicillin? What about pneumococci and enterococci resistance to penicillin?

Back 13

altered PBP

Front 14

How do penicllins enter periplasmic space?

Back 14

via porins

Front 15

Do gram + or - bacteria or both produce penicillin efflux pumps?

Back 15

gram -

Front 16

Can penicillins or amoxicillins be given with food?

Back 16

amoxicillins, penicillins bind strongly with proteins in blood and food so if taken with a meal they will bind food protein instead

Front 17

What is the drug of choice for streptococci?

Back 17

penicillin G

Front 18

What is the drug of choice for meningococci?

Back 18

penicillin G

Front 19

What is the drug of choice for enterococci?

Back 19

penicillin G

Front 20

What is the drug of choice for Treponema pallidum and many other spirochetes?

Back 20

penicllin G

Front 21

What is the drug of choice for clostrium species and other gram + rods?

Back 21

penicillin G

Front 22

What is the drug of choice for gram - anaerobic bacteria?

Back 22

penicillin G but only if they don't have beta lactamase

Front 23

What is the drug of choice for pneumococci?

Back 23

penicillin G but they have to be susceptible

Front 24

What 3 penicillins are used to treat staph, strep, and pneumococci that are beta-lactam resistant?

Back 24

methicillin, nafcilliin, isoxazolyl penicillins. Note: these are semisynthetic penicillins

Front 25

Can lysteria and enterococci be treated with semisynthetic penicillins?

Back 25

no

Front 26

What are examples of isoxazolyl penicillin?

Back 26

oxacillin, cloxacillin and dicoxacillin. These are semisynthetic penicillins

Front 27

What are examples of extended spectrum penicillins? Why are they more effective at treating gram - bacteria?

Back 27

aminopenicillins, ampicillin, amoxicillin, carboxypenicillins, ureidopenicillins. they can better penetrate the outer membrane

Front 28

What drugs would you give for bacterial sinusitis and otitis?

Back 28

amoxicillin or ampicillin

Front 29

If a person has a urinary tract infection what drug would you give them?

Back 29

amoxicillin or ampicillin

Front 30

If a person has a lower respiratory tract infection what drug would you give them?

Back 30

amoxicillin or ampicillin

Front 31

What drug is effective against shigellosis?`

Back 31

ampicillin

Front 32

What penicillin can be used against L. monocytogenes, gram - cocci, E. coli, Salmonella?

Back 32

ampicillin

Front 33

What organisms is ampicillin not effective against?

Back 33

klebsiella, enterobactor, P. aeruginaosa and many gram- aerobes encountered in hospital settings

Front 34

What are the main penicillin adverse effects?

Back 34

hypersensitivity. They are cross-sensitizing and cross-reacting. Allergic reactions include: anaphylactic shock, serum sickness-type reactions, skin rashes, oral lesions, fever, interstitial nephritis, eosinophilia, and hemolytic anemia

Front 35

If a person has neurosyphillis or endocarditis and was allergic to penicillin would you still give them penicillin?

Back 35

yes but administer it gradually to desensitize the reaction

Front 36

What can happen to people with renal failure if they take penicillin?

Back 36

seizures

Front 37

Which penicillin has adverse reactions with the liver and should be avoided in someone with alcoholism?

Back 37

oxacillin it is an antistaphlococcal

Front 38

A person that just took a large dose of penicillin may have what common reactions?

Back 38

nausea, vomiting and diarrhea

Front 39

Do penicillins or cephalosporins have a broader spectrum of activity?

Back 39

cephalosporins are more resistant to many beta-lactamases and therefore have a broader spectrum

Front 40

Are cephlosporins active against listeria and enterococci?

Back 40

no

Front 41

List the first gen cephalosporins!

Back 41

cefazonlin, cefadroxil, cephalexin, cephalothin, cephapirin, cephradine

Front 42

What are 1st gen cephalosporins active against?

Back 42

very active against gram + cocci

Front 43

Are anearobic cocci sensitive to 1st gen cephs?

Back 43

yes except bacteriodes

Front 44

Is E. coli sensitive to 1st gen cephs?

Back 44

most of time

Front 45

mike collins

Back 45

3 count vodka
balance sour mix
serve in at tall glass
garnish with a orange and a cherry

Front 46

What bacteria are 1st gen cephs the 1st choice of treatment for?

Back 46

rarely any

Front 47

What cephalosporin is used for surgical prophylaxis? What generation is it?

Back 47

cefazolin is gen 1 and penetrates most tissues except CNS so not used for meningitis

Front 48

What are members of the 2nd gen cephalosporin?

Back 48

cefaclor, cefamandole, cefonicid, cefuroxime, cefprozil, loracarbef and

ceforanide, cefoxitin, cefmetazole and cefotetan are effective against anearobes

Front 49

What is the difference between 1st and 2nd gen cephs?

Back 49

2nd gens cover first gens and more gram -

Front 50

2nd gen cephs are still not active against what?

Back 50

P. aerginosa and enterocci

Front 51

What organisms are 2nd gen cephs predominately used against?

Back 51

beta-lactamase H. influenzae and moraxella catarrhalis and primarily used to treat sinusitis, otitis, and lower respiratory infections. Can be used to treat peritonitis and diverticulitis

Front 52

What are 3rd gen cephs?

Back 52

cefoperazone, ceftaxime, ceftazidinme, ceftizoxime, ceftriaxone, cefixime, cefpodoxime proxetil, cefdinir, cefditoren pivoxil, ceftibuten, moxalactam

Front 53

What is the difference between 3rd gen cephs compared to 1st and 2nd gens?

Back 53

3rds cover a wider range of gram - and can cross the blood brain barrier

Front 54

What beta-lactamase containing bacteria are 3rd cephs active against?

Back 54

niesseria and haemophilus

Front 55

Ceftazidime and cefoperazone are active against what organism?

Back 55

P aeruginosa

Front 56

2nd and 3rd gen cephs are hydrolyzed by what enzyme?

Back 56

AmpC beta lactamase

Front 57

Can extended spectrum beta lactamases degrade 3rd gen cephs?

Back 57

yes

Front 58

Ceftriaxone and cefotaxime are approved to treat what?

Back 58

meningitis from pneumococci, meningococci, H influenzae and enteric gram - rods but not L monocytogenes

Front 59

What is a 4th gen ceph?

Back 59

cefepime

Front 60

Is cefepime susceptible to extended spectrum beta lactamases?

Back 60

yes, note it is a 4th gen ceph

Front 61

What organisms is cefepime good for?

Back 61

P aerginosa, Enterobacteriacae, S. aureus, S pneumonaie, haemophilus and neiseria becuase it penetrates CNS... it is a 4th gen ceph

Front 62

What are adverse affects of cephalosporins?

Back 62

hypersensitivities: anaphylaxis, fever, skin rashes, nephritis, granulocytopenia, hemolytic anemia

Front 63

What are the toxicities of cephs?

Back 63

hypoprothrominemia and bleeding disorders that can be corrected with supplemental vit K. Act like disulfuram

Front 64

What organisms are targeted by monobactams?

Back 64

aerobic gram - rods including psuedomonas

Front 65

What drug is a monobactam?

Back 65

aztreonam

Front 66

What can hydrolyze monobactams?

Back 66

AmpC and extended spectrum beta lactamases

Front 67

Can aztreonam cross the CNS barrier?

Back 67

yes, it can be used for severe menigitis

Front 68

What are examples of carbapenems?

Back 68

doripenem, ertapenem, imipenem and meropenem

Front 69

What is imipenem effective against?

Back 69

it is a carbapenem effective against p. aeruginosa, gram +, many gram - and anearobes.

Front 70

Is imipenem susceptible to beta lactamases?

Back 70

only metallo beta lactamase

Front 71

Can carbapenems penetrate CNS?

Back 71

yes

Front 72

When is carbapenem used?

Back 72

only when resistance to other drugs is present, as with p. aeruginosa and penicillin resistant pneumococci

Front 73

What organisms naturally produce vancomycin?

Back 73

strep orientalis and amycolatopsis orientalis

Front 74

What organisms is daptomycin active against?

Back 74

gram + particularly staph

Front 75

What is the MOA of vancomycin?

Back 75

It binds to the D-ala-D-ala terminus and inhibits the transglycosylase form elongating the peptidoglycan chain

Front 76

Is vancomycin bacteriostatic or bactericidal?

Back 76

bactericidal

Front 77

What is vancomycin reserved for?

Back 77

methicillin resistant staph causing endocarditis or sepsis or meningitis,

Front 78

What is the most common side effect of vancomycin?

Back 78

red man or red neck syndrome caused by histamine release

Front 79

What is daptomycin active against?

Back 79

gram + bacteria, particularly staph

Front 80

what is the MOA of daptomycin?

Back 80

it inserts into the cell membrane via a calcium dependent insertion of its lipid tail. this causes depolarization of the cell membrane with potassium efflux and cells die rapidly

Front 81

What is the MOA of fosfomycin?

Back 81

it inhibits very early bacterial wall synthesis. it is an analog of phosphoenolpyruvate. it inhibits the cytoplasmic enzyme enolpyruvate transferase by covalently binding to the active site. it blocks the addition of phosphoenolpyruvate to UDP-N-acetylglucosamine acid which is the first step in the formation of UDP-N-acetylmuramic acid.

Front 82

How is fosfomycin taken into cell?

Back 82

via glycerophosphate or glucose 6 phosphate

Front 83

What is bacitracin active against?

Back 83

gram +

Front 84

What is the MOA of bacitracin?

Back 84

inhibits cell wall formation by interfering with dephosphorylation in cycling of the lipid carrier that transfers the peptidoglycan subunits out of cytoplasm

Front 85

What does cycloserine act against?

Back 85

Gram + and Gram -

Front 86

What is cycloserine mostly used against? (first line)

Back 86

mycobacterium tuberculosis

Front 87

What is cycloserines MOA?

Back 87

it is an analog of D-ala and inhibits the incorporation of D-ala into peptidoglycan chain synthesis