Antibacterial Agents Summary

Front 1

Where do highly polar agents get distributed to?

Back 1

Not well absorbed and are restricted to the vascular system and interstitial space

Front 2

How are highly polar agents excreted?

Back 2

Via the bile and or kidney without prior metabolism

Front 3

What are 3 antibacterials that are highly charged?

Back 3

1) Aminoglycosides
2) Bacitracin
3) Polymyxin B

Front 4

What are 2 antibacterials that are moderately charged?

Back 4

1) Penicillins
2) Cephalosporins (1st gen)

Front 5

What are 5 antibacterial agents that are moderately lipid soluble?

Back 5

1) Cephalopsporine (3rd gen)
2) Oxytetracycline
3) Fluoroquinolones
4) Sulfonamides
5) Nitrofurans

Front 6

What are 6 drugs that are highly lipid soluble?

Back 6

1) Rifampin
2) Chloramphenicol
3) Doxycycline
4) Macrolides
5) Clindamycin
6) Metronidazole

Front 7

What happens to the half life of a weak base when the urine is alkalinized?

Back 7

Half-life increases

Front 8

Are weak acids or weak bases absorbed better in the stomach?

Back 8

Weak acid

Front 9

What 4 antibacterials are weak organic acids?

Back 9

1) Penicillins
2) Cephalosporins
3) Sulfonamides
4) Nitrofurans

Front 10

What 5 antibacterial agents are weak organic bases?

Back 10

1) Aminoglycosides
2) Macrolides
3) Lincosamides
4) Polymyxins
5) Rifampin

Front 11

What antibacterial is largely unaffected by pH?

Back 11

Aminoglycosides
-Chloramphenicol not pH dependent

Front 12

What 2 antibacterials are amphoteric?

Back 12

Tetracycline and fluoroquinolones

Front 13

What 2 antibacterials have specific selective action on bacterial cell walls?

Back 13

Beta-lactams
Bacitracin

Front 14

Beta-lactams are synergistic with what other antibacterial? Why?

Back 14

Aminoglycosides because the intracellular penetration of aminoglycosides is enhanced because beta-lactams inhibit formation of cross-linkages in peptidoglycan layer

Front 15

What 5 antibacterials have a mechanism of action that effects protein synthesis?

Back 15

1) Aminoglycosides-cause misreading of mRNA
2) Tetracyclines-Inhibits binding of tRNA to acceptor site of mRNA-ribosome complex
3) Chloramphenicol-inhibits formation of peptide bonds by inhibiting peptidyl transferase
4) Macrolides-Inhibits translocation of peptidyl tRNA from A to P site on the bacterial ribosome
5) Lincosamides-Chloramphenicol, macrolides and lincosamides all interact w/ the 50s ribosomal subunit and may competitively inhibit one another

Front 16

What antibacterial has a mechanism of action that effects cell membranes and permeability?

Back 16

Polymyxins

Front 17

What antibacterial interferes with intermediary (carbohydrate) metabolism?

Back 17

Nitrofurans

Front 18

What 4 antibacterials work by affecting nucleic acids?

Back 18

1) Sulfonamides & trimethoprim-sequentially inhibit folate metabolism
2) Rifampin-inhibits DNA-dependent RNA polymerase
3) Fluoroquinolones-inhibits DNA gyrase
4) Metronidazole-metabolized to reactive products that damage DNA

Front 19

What 6 antibacterials have a narrow spectrum of activity and only affect gram-positive bacteria?

Back 19

1) Penicillin G
2) Cloxacillin
3) Bacitracin
4) Macrolides
5) Lincosamides
6) Rifampin

Front 20

What antibacterials have a narrow spectrum of activity and are only affective against gram negative bacteria?

Back 20

1) Aminoglycosides
2) Polymyxin B
3) Nitrofurans

Front 21

What antibacterials have a broad spectrum of activity and are effective against gram negative and gram positive bacteria?

Back 21

1) Ampicillin
2) Amoxicillin
3) Ticarcillin
4) Cephalosporins (1st gen mostly +, 3rd gen mostly -)
5) Chloramphenicol
6) Tetracyclines
7) Sulfonamides
8) Trimethoprim/sulfa
9) fluoroquiniolones
10) metronidazole

Front 22

What are 5 antibacterials that are anti-pseudomonas?

Back 22

1) Ticarcillin
2) Cephalosporins (3rd gen)
3) Aminoglycosides
4) Polymyxin B
5) Fluoroquinolones

Front 23

What are 4 antibacterials that are anti-beta-lactamase?

Back 23

1) Cloxacillin
2) Aminopenicillins + beta-lactamase inhibitor (e.g. amoxicillin + clavulanate)
3) Cephalosporins
4) Antibacterials that do not have a beta-lactam structure

Front 24

What are 6 antibacterials that are effective against anaerobes?

Back 24

1) Penicillins
2) Cephalosporins
3) Chloramphenicol
4) Lincosamides
5) Metronidazole
6) Tetracyclines second choice

Front 25

What are 2 agents that are definitely not effective against anaerobes?

Back 25

Aminoglycosides
Fluoroquinolones

Front 26

What 5 antibacterials are likely to penetrate barrier restricted tissues e.g. CNS?

Back 26

1) Cephalosporins (3rd gen)
2) Chloramphenicol
3) Doxycycline
4) Trimethoprim/sulfa
5) Rifampin

Front 27

What 2 antibacterials may achieve therapeutic concentrations in the CNS with meningitis?

Back 27

Penicillins
fluoroquinolones

Front 28

What 4 antibacterials are not metabolized, but excreted unchanged in urine or bile?

Back 28

1) Beta-lactams (active renal transport)
2) Aminoglycosides (renal)
3) Relatively hydrophilic tetracyclines-oxytetracycline (renal, biliary)
4) Polymyxin B (renal)

Front 29

What are 5 antibacterials that are metabolized?

Back 29

1) Chloramphenicol (P-450 inhibitor)
2) Doxycycline
3) Lincosamides
4) Trimethoprim
5) Rifampin (p-450 inducer)

Front 30

What are 4 antibacterials that rely on metabolism and excretion for their elimination?

Back 30

1) Macrolides (Hepatic/biliary)
2) Sulfonamides (Acetylation/renal)
3) Nitrofurans (Hepatic/renal)
4) Fluoroquinolones (hepatic/active renal transport)

Front 31

What is the primary adverse effect of penicillin?

Back 31

Allergic reactions

Front 32

What are the 2 primary adverse effects of cephalosporin?

Back 32

Allergic reactions
Nephrotoxicity

Front 33

What are the 3 primary adverse effects for aminoglycosides?

Back 33

Nephrotoxicity
Ototoxicity
Neuromuscular blockade

Front 34

What is the primary adverse effect of chloramphenicol?

Back 34

Reversible or irreversible (humans) bone marrow suppression

Front 35

What are the 3 primary adverse effects of tetracyclines?

Back 35

-Tooth enamel dysplasia
-Nephrotoxicity
-GI disturbances

Front 36

What are the 2 primary adverse effects of macrolides?

Back 36

GIT toxicity
Cardiotoxicity

Front 37

What are the 2 primary adverse effects of Lincosamides?

Back 37

GIT toxicity
Neuromuscular blockade

Front 38

What is the primary adverse effect of polymyxin B?

Back 38

Nephrotoxicity

Front 39

What is the primary adverse effect of sulfonamides?

Back 39

Nephrotoxicity

Front 40

What is the primary adverse affect of Rifampin?

Back 40

Hepatitis

Front 41

What is the primary adverse effect of Fluoroquinolones?

Back 41

Disruption of cartilage structure/development

Front 42

What are 2 mechanisms that resistance to antibacterial agents may be acquired?

Back 42

1) Random mutation
2) Transfer of resistance from one bacterium to another

Front 43

What are 3 methods bacteria use to transfer resistance from one bacterium to another?

Back 43

1) Conjugation
2) Transduction
3) Transformation

Front 44

What does conjugation depend on?

Back 44

Formation of an intercellular bridge

Front 45

What is transduction?

Back 45

Resistance-carrying DNA is incorporated within bacteriophages and passed from resistant to sensitive organisms

Front 46

What is bacterial transformation?

Back 46

Bacterial incorporation of resistance-carrying DNA that is free in the environment

Front 47

What 3 properties confer resistance of bacteria?

Back 47

1) Production or bacterial enzymes which destroy or inactivate the drug (e.g. beta-lactamases) or cause production of metabolites which compete for active transport processes
2) Impermeability of the cell wall or cell membranes, which prevents access of drug to the site of action
3) Structural changes in the target site which prevent interaction or binding of the drug

Front 48

Absorption, distribution, and elimination can be predicted from the _____ and ____ properties of the drug.

Back 48

Lipid solubility and acid-base properties of the drug