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35 Cards in this Set

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Rifampin MoA
Inhibits B-subunit of DNA-dependent RNA polymerase
--> blocks transcription
Rifampin spectrum specific (3)
Excellent activity vs Staph (+MRSA/MRSE), strep, M. tuberculosis
How is resistance with Rifampin
Resistance occurs easily with monotherapy and therefore this drug is always used in combination
Does rifampin penetrate tissue well?
Yes, rifampin has high tissue penetration
Rifampin route
IV/PO 300 mg q12h or 600 mg daily
How is rifampin used and what is it used for?
Used only in combination
-TB: as part of a 3-4 drug regimen
-Staphylococcal infections: endocarditis, osetomyelitis, device infections
Rifabutin class and use
Rifamycin
PO 300 mg daily
TB, M. avium treatment/ppx
Rifaximin class and use
Rifamycin
200 mg TID
Traveler's diarrhea, C. dif
Rifapentine class and use
Rifamycin
600-900 mg weekly
TB
Trimethoprim/Sulfamethoxazole MoA
Bactrim
MoA- interferes with folate synthesis
-SMX: inhibits dihydropteroate synthetase
-TMP: inhibits bacterial dihydrofolate reductase
TMP/SMX dose and route
IV 15 mg/kd/d divided q6h (TMP)
PO 80/400 - 160-800 mg q12h (80 and 160 are TMP)
TMP/SMX specific spectrum (5)
Good activity against
Staph (MRSA), H. influenzae, S. maltophilia, Listeria, Pneumocystis jirovecii
What is TMP/SMX's activity against Pneumococci? Enterobacteriaceae?
Moderate activity for both
Is TMP/SMX used empirically?
No due to high resistance
What drug is treatment of choice for Pneumocystis jirovecii infections and ppx?
TMP/SMX
What drug is treatment of choice for S. maltophilia infections?
TMP/SMX
What are the clinical uses for TMP/SMX
Uncomplicated UTI
bacterial prostatitis
RTI
SSTI
Increasingly for community associated MRSA
Nitrofurantoin MoA
Binds to ribosomal proteins to block translation and inhibit bacterial respiration and pyruvate metabolism
Nitrofurantoin spectrum (specific (1) and general)
Enterococcus and most gram negative except Proteus
What is the dose form of nitrofurantoin?
PO 50-100 mg q6h or 100 mg q12h (macrocrystal)
Uses of nitrofurantoin?
Ppx and treatment of UTI
What dysfunction do you need to look for when considering nitrofurantoin?
Renal dysfunction. Low urine concentrations and increased adverse effects occur in renal dysfuntion
What is an interaction with TMP/SMX that can cause increased bleeding?
Warfarin
How does TMP/SMX affect the CYP system?
Inhibits hepatic metabolism of drugs such as Glipizide, PHT, repaglinide, rosiglitazone
TMP- CYP2C8
SMX- CYP2C9
What is the interaction between TMP/SMX and cyclosporine
TMP/SMX increases the metabolism of cyclosporine
How does TMP/SMX affect renal tubular secretion?
Inhibits renal tubular secretion

Increases amantadine, dapsone, dig, MTX
How does TMP/SMX affect protein binding?
TMP/SMX displaces protein binding

Increases free sulfonylurea and MTX concentrations
T/F TMP/SMX has additive inhibiton of dihydrofolate reductase with drugs such as azathioprine, MTX, or pyrimethamine
True
What CYPs does Isoniazid inhibit?
2C9, 2C19, 3A4

increases PHT, CBZ, diazepam, and warfarin
Why do we want to avoid high doses of APAP with isoniazid?
Isoniazid increases APAP toxic metabolites
We know that rifampin has a ton of interactions.. and is a potent INDUCER of cyp. Name some of the commonly encountered interactions (6)
-Azole antifungals- Itra/keto/voriconazole should not be used.. fluconazole should be decreased by 50%
-Cyclosporin/tacro/sirolimus- narrow therapeutic index; monitor
-Warfarin- monitor INR frequently
-OC- documented failures
-HIV antivirals- use rifabutin instead
-Statins- double or trible the statin dose (don't have to worry about pravastatin)
When should sulfa abx be avoided in pregnancy?
During the last month as it increases the risk of kernicterus in the infant
What is one of the most common reasons for discontinuation of rifampin?
Skin rash
What antibiotic is known for discoloration of tears, sweat, urine, and other body fluids?
Rifampin
can discolor contacts permanently
Do we need to worry about hepato or nephro toxicity with rifampin?
Liver dysfunction/ hepatitis