beta-lactam inhibitors - cephalosporin

Question 1

 Derivatives of 7-aminocephalosporanic acid

 Contain the beta-lactam ring structure

Answer 1

cephalosporin

Question 2

RoA for cephalosporin

Answer 2

several drugs are available for oral use but most are administered PARENTERALLY

Question 3

 Cephalosporins with side chains undergo

Answer 3

hepatic metabolism

Question 4

Major elimination of Cephalosporins is via

Answer 4

renal tubular excretion

Question 5

Excreted mainly in the bile (2)

Answer 5

Cefoperazone and ceftriaxone (3rd generation)

Question 6

Do not enter the CSF when the meninges are inflamed

Answer 6

1st- and 2nd-generation

Question 7

MoA of cephalosporin

Answer 7

 Bind to PBPs on bacterial cell membranes to inhibit bacterial cell wall synthesis
Mechanism same to penicillin

Question 8

are penicillin and cephalosporin bactericidal?

Answer 8

Yes

Question 9

effect of structural differences from penicillin

Answer 9

Less susceptible to penicillinases produced by staphylococci

Question 10

resistance to cephalosporin is developed through

Answer 10

production of other beta-lactamases
Decrease membrane permeability to the drug
Changes in PBPs

Question 11

MRSA is resistant to which drugs

Answer 11

methicillin
penicillin
cephalosporin

Question 12

1st gen drug given IV

Answer 12

cefazolin

Question 13

1st gen drug given orally

Answer 13

cephalexine

Question 14

1st gen drugs are used against

Answer 14

	Gram (+) cocci
	Staphylococci 
	Streptococci
	E. coli 
	K. pneumoniae

Question 15

what gen drugs are used for Surgical prophylaxis in selected conditions

Answer 15

1st

Question 16

what gen drugs have Minimal activity 
	Gram (-) cocci
	Enteroccoci
	MRSA
	Most gram (-) rods

Answer 16

1st

Question 17

what gen drugs
 Less activity against gram (+)
 Extended coverage for gram (-)

Answer 17

SECOND-GENERATION DRUGS

Question 18

B. fragilis

Answer 18

Cefofetan, cefoxitin

Question 19

H. influenzae or M. catarrhalis

Answer 19

Cefamandole, cefuroxime, cefaclor

Question 20

 Increased activity against gram (-) organisms resistant to other beta-lactam drugs
 Ability to penetrate the blood-brain barrier

Answer 20

3rd gen drugs

Ceftazidime, cefoperazone, cefotaxime

Question 21

active against
	Providencia
	S. marcescens 
	Beta-lactamase producing strains 
	H. influenzae 
	Neisseria

Answer 21

3rd gen drugs

Ceftazidime, cefoperazone, cefotaxime

Question 22

 Less active against enterobacter strains that produce extended-spectrum beta-lactamases

Answer 22

3rd gen drugs

Ceftazidime, cefoperazone, cefotaxime

Question 23

Drug of choice for gonorrhea

Answer 23

Ceftriaxone (IV) and cefixime

Question 24

 More resistant to beta-lactamases produced by gram (-) organisms
 Enterobacter
 Haemophilus
 Neisseria
 Some penicillinase-resistant pneumococci
 Combines the gram (+) activity of 1st gen and wider gram (-) spectrum of 3rd gen

Answer 24

FOURTH-GENERATION DRUGS

Cefepime

Question 25

toxicity of cephalosporin

Answer 25

allergy and other adverse effects

Question 26

1. Allergic reactions manifested as

Answer 26

skin rashes to anaphylactic shock

Question 27

Occurs less frequently than penicillins

Answer 27

allergic rxns

Question 28

cross-hypersensitivity (C or INC)

Answer 28

complete

Question 29

cross-reactivity (C or INC)

Answer 29

incomple

Question 30

 Those with history of ___________ should not be treated with cephalosporin

Answer 30

anaphylaxis to penicillin

Question 31

2. Other adverse effects

Answer 31

 Pain at IM injection site  Phlebitis after IV injection  Increase nephrotoxicity of aminoglycosides

Question 32

 Drugs containing a methlythiotetrazole group  Cefamandole, cefoperazone, cefofetan  May cause ????  Disulfiram-like reactions with ethanol

Answer 32

hypoprothrombinemia