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28 Cards in this Set

  • Front
  • Back
What are the 2 classes of Energy metabolism agents?
-Sulfonamides
-Trimethoprim
What is the mechanism by which the Sulfonamides inhibit bacteria?
They competitively inhibit Dihydropteroate Synthetase by acting as analogs of PABA
How does the mechanism of the Sulfonamides not block human cell metabolism?
Humans don't rely on folate synthesis; we get it from the diet.
Are the sulfonamides bacteriostatic or cidal?
Bacteriostatic
What are the 2 resistance mechanisms to the Sulfonamides?
-Reduced uptake of the drug
-Mutations in dihydropteroate synthetase
What has happened to the ability of the sulfonamides to act as broad spectrums?
It is much decreased due to overuse
How are the sulfonamides used now?
In combination with other antibacterials
What are the 2 sulfonamides to know?
-Sulfamethoxazole
-Silver sulfadiazine
Why is Sulfamethoxazole the one that is always used synergistically with Trimethoprim?
Because it is the best pharmacokinetic match
What are the 3 infections that Sulfamethoxazole/Trimethoprim are given for?
-UTI's
-Bacillary dysentery
-Typhoid fever
What organism causes
-Bacillary dysentery
-Typhoid fever
BDysentery = Shigella

Typhoid fever = Salmonella
What is Silver sulfadiazine used for?
Preventing infection in burn patients
How is Silver sulfadiazine administered for preventing burn infections?
Topically
How are the sulfonamides metabolized?
By N-acetyltransferase in the liver
What type of enzyme is N-acetyltransferase (NAT)?
Phase II
What can happen as a result of the NAT metabolism of the sulfonamides? Why?
Crystallization in renal tubules and renal damage - the acetyl group decreases their water solubility
So what are 5 adverse side effects of Sulfonamides?
GRiPH
-GI disturbance
-Renal damage (crystals)
-Inhibit Cyp2C9
-Potentiate other drugs
-Hypersensitivity - rash
What makes the rash caused by sulfonamides worse?
Sunlight
What is Trimethoprim an analog of?
Dihydrofolate
So what is the mechanism of Trimethoprim?
Competitive inhibition of Dihydrofolate reductase so it inhibits folate synthesis
How does the combination of Sulfamethoxazole and Trimethoprim work synergisticly?
-Smx decreases the amount of dihydrofolate produced
-Trimethoprim can much more easily outcompete with the DHF for DHF reductase
Is Trimethaprim alone cidal or static?
Static
What is the effect of Bactrim?
Static + Static = Cidal!
What are 2 resistance mechanisms to Trimethoprim?
-Decreased permeability
-Mutations in DHF reductase
What is Bactrim the FIRST choice empiric therapy for?
Uncomplicated UTIs caused by Staphs and enterics
What else is Bactrim the 1st CHOICE for?
Treatment and prophylaxis of Pneumocystis jiroveci
What are 2 other indications for Bactrim?
-Resp tract (h. flu/strep pneumo)
-Ear infections (moraxella)
-GI infections with enterics
In addition to GI effects, rashes, inhibiting Cyp2C9, and renal damage, what can long-term bactrim cause?
Bone marrow suppression
More nausea/vomiting, etc..