Pharm- Penicillins

Front 1

Structure of penicillin

Back 1

thiozolide ring
bete-lactam ring
side chain ( differs bw penicillins)

derivative of 6-amino-penicillanic acid

Front 2

Mechanism of penicillin

Back 2

bactericidal
interfere with cell wall synthesis
binds PBP
inhibits transpeptidase enzymes
activation of autolytic enzymes

(loss of cell wall rigidity)

Front 3

Penicillin is INEFFECTIVE against what kind of microbe?

Back 3

microbe with NO cell wall

Front 4

Identify bacterial defense against penicillin.

Back 4

Betalactamase--> cleaves beta lactam ring of penicillin

Front 5

Are penicillins time or concentration dependant?

Back 5

time dependant

Front 6

Pharmacokinetics of Penicillin

Penicillin G vs. Penicillin V:
labile or stabile

Back 6

G: acid labile--> destroyed in stomach
V: acid stable

Front 7

20% of penicillin is metabolized to?

Back 7

penicilloic acid

Front 8

90% excreted by?
10% excreted by?

Back 8

90%: renal secretion
10%: glomerular filtration

Front 9

Tubular secretion of penicillin blocked by _________ to reach high concentrations .

Back 9

probenecid

Front 10

Which 2 drugs are eliminated via biliary tract?

Back 10

Nafcillin
Ampicillin

Front 11

When can Penicillin attain therapeutic concentrations in brain?

Back 11

during inflammation--> leaky BBB

Front 12

Spectrum of activity:
penicillin resistant:

Back 12

TB
rickettsiae
protozoa
fungi
virus
chlamydia

Front 13

penicillin susceptible
treatment for:

Back 13

SCAMED
s-strep
c-clostridium
a-anthrax
m-meningococcal
e-enterococcal
d-diptheria

Front 14

What is the drug of choice for syphillis and actinomycosis?

Back 14

Penicillin

Front 15

Identify classification of penicillins (5)

Back 15

1. acid labile
2. acid resistant
3. Penicillinase resistant penicillins
4. Broad spectrum penicillins
5. anti-pseudomonas penicillins

Front 16

acid labile

Back 16

penicillin G

Front 17

acid resistant

Back 17

penicillin V

Front 18

Penicillinase resistant penicillins

Back 18

CONDOM
C-Cloxacillin
O-Oxacillin
N-Nafcillin (naf for staph)
D-Dicloxacillin
O-oral and parenteral
M-Methicillin (only parenteral)

Front 19

broad spectrum penicillins
oral bioavailibility:

Back 19

ampicillin
amoxicillin

oral bioavailibility:
amoxicillin > ampicillin

Front 20

broad spectrum penicillins affective against:

Back 20

ampicillin and amoxicillin:

Gram neg. and pos. (HELPS)
H-H. Influenza
E-E.coli
L-Listeria monocytogenes
P-Proteus
S-Salmonella

Front 21

anti-pseudomonas penicillins

Back 21

MCAT-P (prep) :
M-mezlocillin
C-carbenicillin
A-azlocillin
T-ticarcillin
P-piperacillin

Front 22

Identify 4 penicillin preparations

Back 22

penicillin G (benzyl penicillin)
procaine penicillin G
Benzathine penicillin G
Penicillin V

Front 23

penicillin G (benzyl penicillin)
type:
mode of admin.:
use:
1/2 life:

Back 23

soluable
IV
used for serious infections ie. meningitis
short 1/2 life

Front 24

Procaine penicillin G
type:
use:
1/2 life:

Back 24

repository form
slow absorption
maintains [therapeutic]
last 12-24hrs
IM injection

Front 25

benzathine penicillin G
use:
mode of admin:

Back 25

prophylaxis
released slowly into circulation
NOT FOR EMERGENCY
IM injection

Front 26

penicillin V:
use:

Back 26

acid resistant
use: mild infections and prophylaxis

Front 27

identify the action of beta-lactamase inhibitors

Back 27

no antibacterial activity
prevent inactivation of penicillins when combined.

Front 28

identify the beta-lactamase inhibitor combinations (4)

Back 28

1. Sulbactam + Ampicillin

2. Clavulanic acid + Amoxicillin (augmentin)

3.Clavulanic acid + ticarcillin (Timentin)
4. Tazobactam + Piperacillin (zosyn

Front 29

synergism
2 ex of drug combination

Back 29

trimethoprim + sulfamethoxazole
penicillin + aminoglycoside

Front 30

potentiation
ex:

Back 30

amoxicillin + clavulanic aicd

Front 31

therapeutic antagonism

Back 31

penicillin + tetracycline
in pneumococcal meningitis

ampicillin +piperacillin in pseudomonas aeruginosa

Front 32

(4) causes of penicillin resistance

Back 32

1. penicillinase
2. decreased penetration into cell
3. altered PBP
4. density of bacterial population

Front 33

adverse effects of penicillin

Back 33

hypersensitivity
maculopapular rash, urticarial rash
fever
brochospasm, vasculitis, dermatitis
Stevens Johnson syndrome
Cross reaction
hemolytic anemia
herxheimer reaction- syphillis
interstitial nephriits- methicillin
superinfection
CNS toxicity-->arachnoiditis
thrombophlebitis

Front 34

herxheimer reaction

Back 34

associated with syphillis
fever
chills
headache and joint pain

Front 35

carbenicillin and ticarcillin cause?

Back 35

platlet dysfunction

Front 36

thrombophebitis occurs with ?

Back 36

nerve dysfunction
occurs with IM and IV administration

Front 37

Imipenem
use:
inactivated by:
given along with:
AE:

Back 37

beta lactam antibiotic
resistant to betalactamases
used for: aerobic, anerobic, gram +, gram -
Not used for: MRSA or c.difficile

inactivated by renal dehyrdropeptidase
given with cilastatin

Front 38

Meropenen
does it need to be given with Cilastatin?

Back 38

beta lactam antibiotic
does NOT require cilastatin
no seizures

Front 39

Aztreonam (IV)
Key feature:
Use limited to:
AE:

Back 39

No cross reactivity
synergy with AG

use limited to:
gram negative Klebsiella
pseudomonas
serratia

AE:skin rash, N/V, increased LFT

Front 40

Bacitracin
mechanism of action;
mode of admin:
use:

Back 40

interfere with isoprenyl phosphase (cell wall synthesis)

Topical use ONLY! systemic--> nephrotoxic

use:
furunculosis, impetigo, carbuncle
pyoderma
abscesses

Front 41

Bacitracin active IN VITRO against:

Back 41

H. influenza
staph
strep
clostridium
salmonella
shigella
proteus
pseudomonas

Front 42

Vancomycin
mechanism of action

Back 42

tricyclic glycopeptide
inhibits cell wall synthesis
interfere with D-alanine-D-alanine precursors

Front 43

Vancomycin
tx for:

Back 43

pseudomembranous colitis
MRSA

pneumonias
empyemas
endocarditis
osteomyelitis
soft tissue abscess
penicillin resistant pneumococcal infection

Front 44

Vancomycin AE:

Back 44

T. phlebitis
pain
chills
rash
fever
flushing- RED MAN or red neck syndrome
hypotension

Ototoxic and nephrotoxic agent --> neutropenia

Front 45

Vancomycin resistance due to:

Back 45

1.cytoplasmic protein that reduces access of drug

2. VRE- use D-alayl-D-lactate as precursor to cell wall (less affinity for drug)

Front 46

Cycloserine
mechanism of action:

Back 46

competitively inhibits conversion of L-alanine --> D-alanine and linkage

Front 47

Cycloserine bacterial suseptability

Back 47

mycobacterium TB strains resistant to streptomycin, isoniazids and PAS

atypical mycobacterium

Front 48

Cycloserine
Kinetics:

Back 48

oral absorption
CSF penetration : good
50% excreted unchanged

Front 49

Cycloserine AE:

Back 49

psychosis
delirium
confusion
headache
convulsions
tremors

Front 50

cycloserine
Uses:

Back 50

2nd line tx for:
TB
CNS nocardia (sulf. 1st)

Front 51

Cephalosporins divided into 4 generations based on...

Back 51

1------------------------------->4
time of launch
decrease gram + coverage
increase gram - coverage
increase CNS penetration
increase resistance to b-lactamase
most eliminated thru kidney, some renal
all bactericidal

Front 52

Cephalosporins are ineffective against...

"Cephalosporins are LAME!"

Back 52

LAME

L-Listeria monocytogenes
A-Atypical (mycoplasma, Legonella, C. pneumonia)
M-MRSA
E-Enterococci

Front 53

Identify 3 drugs secreted via Biliary Tract:


remaining drugs secreted via kidney

Back 53

1. cefamandole
2. cefoperazome
3. ceftriaxone

Front 54

1st generation cephalosporins
active against what organisms

Back 54

good activity: gram +
ie. pneumo, strep and staph

ok activity: gram -

p. mirabilis
e.coli
K. moraxella

Front 55

(1st)Parenteral cephalosporins:

Back 55

cefa-zolin
cepha-lothin
cepha-pirin

Front 56

(1st)Oral cephalosporins:

Back 56

cepha-lexin
cefa-DROXIL
cephra-dine

* doesnt enter CNS ~ not used for meningitis

Front 57

2nd generation
None enter CNS except 2: which ones?

Back 57

cefuroxime
cefaclor

Front 58

(2nd) effective against:

Back 58

P. mirabilis
E.coli
K. pneumonia
Enterobacter aerogenes

N. gonococci
H. influenza
G+ strep
strep p
anerobes

Front 59

(2nd) identify 2 oral drugs:
key feature?

Back 59

cefaclor
cefuroxime

*** enter CNS

Front 60

(2nd) identify Parenteral drugs: (6)

Back 60

1.cefuroxime- csf
2. cefotetan
3. cefoxitin (b.fragilis)
4. cefamandole (biliary exc)
5.cefonicid
6. ceforanide

Front 61

3rd generation
IM Ceftriaxone is DOC for ___.
*good CSF penetration*

Back 61

DOC-gonorrhea

Front 62

(3rd) oral drugs

Back 62

cefixime

Front 63

(3rd) parenteral

Back 63

cefo-peraz-one
cef-triax-one
mox-alactam
cef-tizo-xime
ceft-azi-dime
cefotaxime

Front 64

identify 4th generation cephalosporin:

Back 64

CEFEPIME

Front 65

compare 3 and 4th generation cephalosporin

Back 65

extended spectrum of activity
increased stability from hydrolysis by b-lactamases

Front 66

4th generation
use:

Back 66

gram negative resistant bacilli of 3rd generation cephalosporins

Front 67

Cephalosporin
Adverse effects

Back 67

cross sensitivity
hypoprothrombinemia
alcohol interaction
hemolytic anemia
nephrotoxicity

Front 68

cefamandole
cefotetan
cefoperazone

Back 68

all contain methylthiotetrazxole

inhibits vitamin K --> hypoprothrombinemia

Front 69

which cephalosporins with AE that cause alcohol interaction:

Back 69

cefamandole
cefotetan
cefoperazone
** disulfiram like interactions**

Front 70

high doess of cephalothin causes...

Back 70

nephrotoxicity