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1

what are the protein synthesis inhibitors?

30s: tetracyclines, aminoglycosides
50s: Macrolides, Clindamycin, Streptogramins, Oxazolidinones

2

doxycycline excretion: renal?

not renal - hepatic and fecal

3

Tetracycline: MOA, Spectrum, bactericidal or static?

Bacteriostatic
MOA: 30s subunit (protein)
spectrum: BROAD (+ and -).
-atypicals: ricksettsia (ticks, mites, fleas, lice), chlamydia, mycoplasmic pneumoniae
-spirochete: lyme disease

4

tetracycline resistance

3 possible ways:
-efflux pump (bacteria expels drug out of cell)
-enzymatic inactivation
-bacteria proteins that prevent binding of drug to ribosome
*resistance to one tetracycline DOES NOT mean to resistance to all

5

Additions to spectrum of tetracyclines: doxycycline and minocycline

doxy: atypical: CAP, malaria, prophylaxis
mino: P. Acnes

6

PK of tetracyclines

Oral administration
Absorption decreased by:
Divalent cations ( Ca, Fe, Mg or Al)
Diary products
Antacids (don't take with these)
=reduced bioavailability when with foods

poor CNS penetration

7

super infection can occur with what type of antibiotic?

any broad spectrum (most often cause is candida or Cdiff)

8

serious adverse effects of tetracycline

Skin: photosensitivity
Staining of teeth
Bind to calcium deposited in newly formed bone or teeth in young children and fetal teeth during pregnancy
Teeth fluorescence/discoloration
Enamel dysplasia

Fetal bone deformities
Deposit in bone leading to deformity or growth inhibition

CONTRAINDICATED in pregnant women, infants, children < 8 years or younger
"TETRAcycline = TERATogenic"

9

Glycycline --> tigecycline

Tetracycline derivative (semisynthetic of minocycline)
(IV drug)
MOA: 30s subunit
Spectrum: BROAD (+ and -) including MRSA, VRE
anaerobes
atypical- legionella (CAP)

clinical uses: CAP, infections of deep tissue and intra-abdominal

10

aminoglycosides

"GNATS" - all "mycin" except Amikacin
Gentamycin
Neomycin
Amikacin
Tobramycin
Streptomycin

11

post antibiotic effect is most common in what type of abx?

those that inhibit protein/DNA/RNA.
PAE- suppression of bacterial growth after brief drug exposure

12

PK of aminoglycosides: Absorption, distribution, elimination

abs: only IV (occassional IM) or topical (conjunctivitis)
-hospital drug
distribution: good, no CSF or eye (unless topical) but can use for meningitis with other drugs if inflamed and synergistic (beta lactams)
elimination: renal, MUST make dose adjustment w/ kidney failure. (monitor serum drug levels )

13

aminoglycosides are good to treat what?

gram neg serious infections: bacterial meningitis, sepsis, (endocarditis), osteomyelitis, etc)

14

aminoglycosides adverse effects

ototoxic, nephrotoxic, neuromuscular blockade

15

triple antibiotic ointment

neomycin (gram- and gram +, too nephrotoxic for oral or IV- hence ointment)
polymixin (gram -)
bacitracin (gram +)

16

"mean GNATS caNNOT kill anaerobes"

mean (aminoglycosides)
GNATS: gentamycin, neomycin, amikacin, tobramycin, streptomycin
NNOT: nephrotoxicity, neuromuscular blockade, ototoxic, teratogen (oto and nephro for fetus too)

17

erythromycin is used mostly for what?

acne (only macrolide that is bacteriostatic instead of cidal

18

fidaxomicin use for?
MOA, spectrum, adverse

Cdiff but VERY expensive
MOA: thought of as macrolide but binds to RNA polymerase and stops protein binding
Spectrum: NARROW- CDiff (gram +)
Adverse: bowel obstruction or GI hemorrhage

19

macrolides

"FACE" fidaxomycin, azithromycin, clarithromycin, erythromycin
..or girls names - "FrIDA, AZI, CLARe, ERYn"

20

macrolide MOA and spectrum

MOA: 50s subunit
spectrum: gram + cocci

21

atypical pneumonias

chlamydia, mycoplasma, legionella(CAP)

22

macrolides- drug resistance patterns

primarily why we dont use erythromicin anymore
1. target modification- prevent abx to ribosome bind
2. efflux
3. drug inactivation

23

z pack

axithromycin: - LONG half life- different Dosing - “Zpack” - pt only takes for 5 days but actually stays in system for 10 days - increases pt compliance
EASIER IS BETTER -

24

macrolide excretion

bile and feces

25

generally use macrolides for what clinical uses?

STIs and CAP

26

adverse effects of MACROlides

"MACRO"
GI Motility (usual stomach upset)
Arrhythmia
acute Cholestatic hepatitis
Rash
Eosinophilia

-erythro and clindo are worst for these, Azithromycin is best to use to limit adverse effects
-first 2 most important

27

Erythromycin and Clarithromycin have what significant danger?

drug interaction- inhibit CYP34A - increases serum levels of other drugs (esp. statins and warfarin)

28

treatment of anerobes above and below diaphram

above: clindamycin
below: metronidazole

29

abx most common cause of superinfection Cdiff

Clindamycin and fluoroquinolones

30

Clindamycin: MOA, Bactericidal?, Spectrum

MOA: 50s subunit (tunnel)
bacterioSTATIC
spectrum: gram + cocci (strep and staphy) MRSA, MSSA
anerobes- above diaphragm