Nucleic Acid Inhibitors

Question 1

Quinolones (2)

what happens when you fluorinate?

Answer 1

Flouronated derivatives have enhanced potency
Ciprofloxacin
Moxifloxacin

Question 2

Quinolone MOA

Answer 2

Gyrase
Topo II, IV
CIDAL, concentration-dependent killing

Question 3

Quinolone spectrum

Answer 3

Cipro –> aerobic G- (PSEUDOMONAS)
Moxi –> GPC (not MRSA), atypicals, mycobacteria

Burns, OSTEOMYELITIS, enterics, respiratory (DOC for legionella) also CAP/HAP, mycobacterial, UTI’s (pyelonephritis; now an alternative b/c of resistance), prostatitis, anthrax

Question 4

Only oral drug active against pseudomonas?

Answer 4

Ciprofloxacin

Question 5

Quinolone resistance (4)

Answer 5

Gyrase (A/B)
Topo
Porins
Efflux pumps

Question 6

Quinolone pharmacology

Answer 6

IC conc 2-3x serum
CIPRO elimination via URINE
MOXI via LIVER

Question 7

Which quinolone to use in UTI?

Answer 7

Cipro bc better concentration levels in urine than moxi

Question 8

Quinolone adverse effects (Take Photos w a HDD QT)

Answer 8

Cartilage damage --> achilles tendon rupture (don't use in pts with muscle injury
Phototoxicity
Hepatitis
QTc prolongation
Dizziness
Dysglycemias

Question 9

Prophylaxis and tx of anthrax

Answer 9

Quinolones

Question 10

DOC for legionella

Answer 10

Quinolones

Question 11

Rifampin MOA

Answer 11

Inhibit RNA polymerase at B-subunit

CIDAL, conc-independent

Question 12

Rifampin spectrum (MAMS)

Answer 12

MRSA
Staph (w/BL’s for osteomy, endocard, abscess, biofilms)
Mycobacteria (TB)
Atypicals

Question 13

Non-invasive E.coli in gut (also C. diff)

Answer 13

Rifaximin (bc poor oral absorption)

Question 14

Rifampin resistance

Answer 14

MUT in B-subunit

Must be used in COMBO

Question 15

Rifampin dynamics

Answer 15

Crazy lipid soluble

Liver elimination

Question 16

Rifampin SE’s (HOP)

Answer 16

Hepatitis (first month; if later not due to drug)
Stimulate P450 (coumadin, hypoglycemics, contraceptives)
Orange pee

Question 17

Traveller’s diarrhea & relapsing C. diff drug

Answer 17

Rifaximin

Question 18

Infected artificial joints tx

Answer 18

Rifampin

Question 19

Metronidazole MOA

How does it activate?

Answer 19

MOA: active metabolite via reduction of nitro group

Binds/damages DNA

Question 20

Metro spectrum (don’t Protest, B fragile so to C differences)

Answer 20

Anaerobes (B. fragilis, C. diff) BELOW DIAPHRAGM

Protozoa (entamoebae, giardia, trichomonas)

Question 21

Metro resistance

Answer 21

organisms that lack nitro-reductase

would then lead to higher MIC

Question 22

Metro pharmacology

Answer 22

lipid soluble
good CSF distribution
liver excretion

Question 23

Metro SE’s

Answer 23

Peripheral neuritis

Vomiting if taken with alcohol

Question 24

Mild/moderate pseudomembranous colitis

Answer 24

Metronidazole

Question 25

Sulfonamide TMP

Answer 25

Water soluble: sulfamethoxazole

Trimethoprim (55k times tighter binding to bacteria v. humans)

Question 26

TMP-Sulfa MOA

Answer 26

TMP: Inhibit DHF reductase
Sulfa: inhibit dihydropteroate reductase
Enzyme present in both man/bacteria
Liver & kidney (only need to modify dose if both are diseased)

Question 27

Sulfonamide spectrum (new to noca)

Answer 27

Nocardia
Toxoplasma
Pneumo jiroveci

UTI’s, respiratory, pneumocystis pneumonia, typhoid fever, oral therapy of CA-MRSA, burns

Question 28

Trimethoprim (Staph, negatron, pneumo no pseudo)

Answer 28

Gram neg (e.coli, kleb, NOT pseudomonas)
Staph, pneumococci, pneumo jiroveci
WEAK strep

Question 29

TMP-sulfa is not a good drug for?

Answer 29

Strep cellulitis

Question 30

TMP-sulfa SE’s

1 for TMP 2 for sulfa

Answer 30

Trimethoprim: folate deficiency (anemia)
Sulfonamides: rash, crystals in urine

Question 31

Abscess (staph)…rx?

Answer 31

Clinda
Linezolid
Doxycycline/mino
Rifampin w/something
TMP-sulfa