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48 Cards in this Set

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Where do highly polar agents get distributed to?
Not well absorbed and are restricted to the vascular system and interstitial space
How are highly polar agents excreted?
Via the bile and or kidney without prior metabolism
What are 3 antibacterials that are highly charged?
1) Aminoglycosides
2) Bacitracin
3) Polymyxin B
What are 2 antibacterials that are moderately charged?
1) Penicillins
2) Cephalosporins (1st gen)
What are 5 antibacterial agents that are moderately lipid soluble?
1) Cephalopsporine (3rd gen)
2) Oxytetracycline
3) Fluoroquinolones
4) Sulfonamides
5) Nitrofurans
What are 6 drugs that are highly lipid soluble?
1) Rifampin
2) Chloramphenicol
3) Doxycycline
4) Macrolides
5) Clindamycin
6) Metronidazole
What happens to the half life of a weak base when the urine is alkalinized?
Half-life increases
Are weak acids or weak bases absorbed better in the stomach?
Weak acid
What 4 antibacterials are weak organic acids?
1) Penicillins
2) Cephalosporins
3) Sulfonamides
4) Nitrofurans
What 5 antibacterial agents are weak organic bases?
1) Aminoglycosides
2) Macrolides
3) Lincosamides
4) Polymyxins
5) Rifampin
What antibacterial is largely unaffected by pH?
Aminoglycosides
-Chloramphenicol not pH dependent
What 2 antibacterials are amphoteric?
Tetracycline and fluoroquinolones
What 2 antibacterials have specific selective action on bacterial cell walls?
Beta-lactams
Bacitracin
Beta-lactams are synergistic with what other antibacterial? Why?
Aminoglycosides because the intracellular penetration of aminoglycosides is enhanced because beta-lactams inhibit formation of cross-linkages in peptidoglycan layer
What 5 antibacterials have a mechanism of action that effects protein synthesis?
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
What antibacterial has a mechanism of action that effects cell membranes and permeability?
Polymyxins
What antibacterial interferes with intermediary (carbohydrate) metabolism?
Nitrofurans
What 4 antibacterials work by affecting nucleic acids?
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
What 6 antibacterials have a narrow spectrum of activity and only affect gram-positive bacteria?
1) Penicillin G
2) Cloxacillin
3) Bacitracin
4) Macrolides
5) Lincosamides
6) Rifampin
What antibacterials have a narrow spectrum of activity and are only affective against gram negative bacteria?
1) Aminoglycosides
2) Polymyxin B
3) Nitrofurans
What antibacterials have a broad spectrum of activity and are effective against gram negative and gram positive bacteria?
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
What are 5 antibacterials that are anti-pseudomonas?
1) Ticarcillin
2) Cephalosporins (3rd gen)
3) Aminoglycosides
4) Polymyxin B
5) Fluoroquinolones
What are 4 antibacterials that are anti-beta-lactamase?
1) Cloxacillin
2) Aminopenicillins + beta-lactamase inhibitor (e.g. amoxicillin + clavulanate)
3) Cephalosporins
4) Antibacterials that do not have a beta-lactam structure
What are 6 antibacterials that are effective against anaerobes?
1) Penicillins
2) Cephalosporins
3) Chloramphenicol
4) Lincosamides
5) Metronidazole
6) Tetracyclines second choice
What are 2 agents that are definitely not effective against anaerobes?
Aminoglycosides
Fluoroquinolones
What 5 antibacterials are likely to penetrate barrier restricted tissues e.g. CNS?
1) Cephalosporins (3rd gen)
2) Chloramphenicol
3) Doxycycline
4) Trimethoprim/sulfa
5) Rifampin
What 2 antibacterials may achieve therapeutic concentrations in the CNS with meningitis?
Penicillins
fluoroquinolones
What 4 antibacterials are not metabolized, but excreted unchanged in urine or bile?
1) Beta-lactams (active renal transport)
2) Aminoglycosides (renal)
3) Relatively hydrophilic tetracyclines-oxytetracycline (renal, biliary)
4) Polymyxin B (renal)
What are 5 antibacterials that are metabolized?
1) Chloramphenicol (P-450 inhibitor)
2) Doxycycline
3) Lincosamides
4) Trimethoprim
5) Rifampin (p-450 inducer)
What are 4 antibacterials that rely on metabolism and excretion for their elimination?
1) Macrolides (Hepatic/biliary)
2) Sulfonamides (Acetylation/renal)
3) Nitrofurans (Hepatic/renal)
4) Fluoroquinolones (hepatic/active renal transport)
What is the primary adverse effect of penicillin?
Allergic reactions
What are the 2 primary adverse effects of cephalosporin?
Allergic reactions
Nephrotoxicity
What are the 3 primary adverse effects for aminoglycosides?
Nephrotoxicity
Ototoxicity
Neuromuscular blockade
What is the primary adverse effect of chloramphenicol?
Reversible or irreversible (humans) bone marrow suppression
What are the 3 primary adverse effects of tetracyclines?
-Tooth enamel dysplasia
-Nephrotoxicity
-GI disturbances
What are the 2 primary adverse effects of macrolides?
GIT toxicity
Cardiotoxicity
What are the 2 primary adverse effects of Lincosamides?
GIT toxicity
Neuromuscular blockade
What is the primary adverse effect of polymyxin B?
Nephrotoxicity
What is the primary adverse effect of sulfonamides?
Nephrotoxicity
What is the primary adverse affect of Rifampin?
Hepatitis
What is the primary adverse effect of Fluoroquinolones?
Disruption of cartilage structure/development
What are 2 mechanisms that resistance to antibacterial agents may be acquired?
1) Random mutation
2) Transfer of resistance from one bacterium to another
What are 3 methods bacteria use to transfer resistance from one bacterium to another?
1) Conjugation
2) Transduction
3) Transformation
What does conjugation depend on?
Formation of an intercellular bridge
What is transduction?
Resistance-carrying DNA is incorporated within bacteriophages and passed from resistant to sensitive organisms
What is bacterial transformation?
Bacterial incorporation of resistance-carrying DNA that is free in the environment
What 3 properties confer resistance of bacteria?
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
Absorption, distribution, and elimination can be predicted from the _____ and ____ properties of the drug.
Lipid solubility and acid-base properties of the drug