Pharm Test 2 Antimicrobials: Protein Synthesis Inhibitors

Front 1

Tetracyclines

1)MOA
2)CU
3)AE

Back 1

1)enters via passive diffusion and energy dependent transport; and binds REVERSIBLY to 30S, preventing binding of aminoacyl transfer RNA
BACTERIOSTATIC (stops growth, and body kills bug) (dont give with bacteriocidal drugs)

2)Broad Spectrum
Activity against Gram Pos and Gram Neg

3)Teratogenic (can cross placenta) (and excreted in breast milk) (thus FDA Cat D Last Resort Drug)
GI Effects
Discoloration of Teeth, Stunting of Growth
Photosensitivity, Vertigo
Pseudotumor Cerebri
Superinfections

Front 2

Tetracyclines

4)Contra
5)Kinetics
6)Resistance?

Back 2

4)Milk, Antacids (divalent and trivalent cations cause dec oral absorption)
Pregnant (fatal hepatotoxicity)
Kids Under 8

5)Low Oral Absorption
Excreted in Kidney, except Doxycycline(Doxy = Bile)

6)Widespread Resistance d/t cant get in, pumped out, cant bind to ribosome, inactivated by enzymes

Front 3

Tetracycline

Back 3

a tetracycline

Front 4

Minocycline

Back 4

a tetracycline

Reaches Therapeutic levels in CSF

Front 5

Doxycycline

Back 5

a tetracycline

Parenteral

Front 6

Tigecycline (a Glycylcycline)

1)MOA
2)CU
3)AE
4)Contra
5)How do you give?

Back 6

1)Binds Reversibly to 30S
Not subject to same resistance as Tetras (except efflux pumps of Proteus and Pseudomonas)

2)Broad Spectrum
Gram Pos and Gram Neg
Can Use Against Resistant strains, so Reserved for the Bad Stuff
Skin, Soft Tissue, and Intraabdominal Infections, Community Acquired Pneumonia

3)Inhibits Warfarin Clearance (small therapeutic window for Warfarin)
Dec Effectiveness of Oral Contra

4)Pregnancy and Kids Under 8
5)IV

Front 7

Clindamycin

1)MOA
2)CU
3)AE

Back 7

1)IRREVERSIBLY binds to 50S, inhibiting translocation
BACTERIOSTATIC

2)Skin infections with Staph and Strep
Com Acquired ORSA or MRSA
Anaerobic Bacteria Infections (*KNOW THIS)

3)GI
Fatal C. Diff (is resistant, can get suprainfection)
Neutropenia, Impaired Liver Function

Front 8

Clindamycin

4)Given with Primaquine to treat:
5)Given with Primethamine to treat:

6)Prophylaxis for:

Back 8

4)Second line for Aids Related PCP

5)Aids related Toxoplasmosis

6)Endocarditis in valve disease patients (that are penicillin allegic)

Front 9

Aminoglycocides

1)Bacteriocidal or Bacteriostatic
2)Concentration or Time Dependent Killing?
3)When does there killing stop?
4)How many times a day do you give these drugs?

Back 9

1)Bacteriocidal

2)Concentration (higher the concentration of the drug, the more bacteria it kills) (thus one huge dose more effective than giving multiple small doses)(penicillins/cephalasporins are time dependent)

3)Have post antibiotic effect (kill even after drug levels below measureable) (thus can only give this ONCE A DAY)
4)ONCE A DAY

Front 10

Aminoglycosides

5)MOA
6)CU
7)Why Combine with penicillins?

Back 10

5)Passively diffuse and then actively transported (needs O2) (thus not used for Anaerobic bacteria) -> Binds to 30S->blocks formation of complex, causes misreading of mRNA, and breaks polysomes into monosomes

6)Aerobic Gram Neg (req the O2 transport mechanism)

7)penicillins break open the cell wall, so aminoglycoside can reach site of action
Also, penicillins act against gram pos, and this against gram neg, so even broader spectrum

Front 11

Aminoglycosides

8)Resistance
9)How do you give
10)Where are there high levels?
11)AE Effects depend on what?
12)Contra
13)AE
14)On the whole, are they used?

Back 11

8)Plasmid Synthesis of enzymes that inactivate it
Impaired entry of Drug (penicillins can reduce this)
Mutation of 30S Subunit

9)Parenteral
10)Renal Cortex, Inner Ear (thus might have toxic effects here)
11)Both Time (longer in body) and Concentration of drug

12)Ototoxicity
Nephrotoxicity
Neuromuscular Paralysis

13)Pregnancy (FDA Cat D)
14)Not really because too toxic

Front 12

Macrolides

1)Static or Cidal?
2)Used for gram pos or neg?
3)Used to treat patients that are allergic to
4)MOA
5)Its binding site is identical to that of which drugs? this means?

Back 12

1)can be both
2)Both
3)Penicillin
4)Irreversibly to 50S, inhibit translocation
5)Chloramphenicol, Clindamycin (thus those resistant to macrolides, also resistant to these)

Front 13

Macrolides

6)Resistance?

7)Given how?

7b)Effect of Erithromycin, Clarithromycin, and Telithromycin on CYPP450

Back 13

6)Reduced permeability, inc efflux, esterase that breaks it down, mutation of ribosomal binding site

7)Orally

7b)inhibits cypp450

Front 14

Macrolides:

Effect of food on Oral bioavailability Absorption of:
8)Erythromycin
9)Azithromycin
10)Clarithromycin
11)Telithromycin
12)Azithromycin distribution is different from the rest because:

Back 14

8)Decrease
9)Decrease
10)Increase
11)Stable
12)Azithromycin is more in tissues and macrophages (rest more in plasma)

Front 15

Macrolides Half Life and Elimination

13)Erythromycin
14)Azithromycin
15)Clarithromycin

Back 15

13)2 hrs; Bile

14)2 to 4 days; kidney

15)6 hrs; metabolized by liver, excreted by kidney

Front 16

Macrolides

16)AE
17)Special AE of Telithromycin
18)Contra AE of Telithromycin

Back 16

16)Jaundice
Ototoxicity (thus dont give with aminoglycosides, because both cause it)

17)Prolongs QT
18)Myasthenia Gravis

Front 17

Macrolides

Why would you give:

19)Erythromycin
20)Clarithromycin
21)Azithromycin
22)Telithromycin

Back 17

19)If allergic to Penicillin G (all 4 of them can be used)

20)Prophylaxis and treatment of M. avium and H. pylori

21)Chlamidya (urethritis
Community aquired Strep Pneumonia

21)Community acquired pneumonia

Front 18

Chloramphenicol

1)Use Restricted to:
2)Static or Cidal?
3)MOA

Back 18

1)Life threatening infections because very toxic (Very Broad Spectrum)
2)Static (thus if immunocompromised wont work, because need body to kill bacteria, this just stops growth)

3)enters via active transport and binds REVERSIBLY to 50S, and prevents attachment of RNA ->preventing formation of peptide bonds; Also inhibits protein synthesis in mitochondrial ribosomes (causes bone marrow toxicity

Front 19

Chloramphenicol

4)Which orgs are highly susceptible?

5)Which orgs are NOT susceptible?

6)How can orgs get resistance?

Back 19

4) H.influenzae, N.meningitides, Bacteroides

5)P. aeruginosa, Chlamydiae

6)Can code for Acety CoA Transferase (Inactivates drug **KNOW THIS)

Front 20

Chloramphenicol

7)Kinetics

8)AE

9)Commonly used for:

Back 20

7)Secreted into breast milk, enters CSF, Inhibits Hepatic Oxidases (eg: cypp450)

8)Bone Marrow Toxicity (Aplastic Anemia)
Gray Baby Syndrome (cant break drug down ->drug accumulates->Cyanosis)

9)Topically for Ear and Eye Infections (otherwise just life threatening infections)

Front 21

Streptogramins (Quinupristin/Dalfopristin)

1)Only given as:
2)Static or Cidal?
3)CU
4)Kinetics?

Back 21

1)Combination (30%/70%)
2)bactericidal
3)Reseved for treatment of Vancomycin Resistant E. FAECIUM
4)Very long post antibiotic effect
Inhibits CYP 3A4

Front 22

Streptogramins

5)MOA
6)Resistance?
7)Not effective Against:
8)What adds to the effect of these drugs?
9)Why not give with statins?

Back 22

5)Bind to 50S subunit (quinupristin binds to different site than dalfopristin, causes synergistic effect)

6)Uncommon, because even if mutation at one site, drug can bind to other site
7)Enterococci FAECALIS
8)They are metabolized to equally effective metabolites
9)Because both drugs cause arthralgia and myalgia

Front 23

Linezolid

1)Static or Cidal
2)MOA
3)CU
4)Not Active against
5)AE

Back 23

1)Static, but cidal against Strep and Clostridum perfringens

2)binds to unique site on 23 ribosome subunit of 50S->inhibits formation of 70S initiation complex

3)Drug Resistance Organisms (can use if Vancomycin fails) (reserved for very serious)
Gram Pos infection of Skin, RT
TB

4)Enterobacteriae, Pseudomonas
5)Inhibits MAO'Is ->interacts with adrenergic, serotenergic drugs

Front 24

3 Drugs use for Multi drug Resistant Organisms

Back 24

Vancomycin, Dactromycin, Linezolid

Front 25

Erhthromycin

Back 25

Macrolide

Front 26

Clarithromycin

Back 26

Macrolide

Front 27

Azithromycin

Back 27

Macrolide

Front 28

Telithromycin

Back 28

Macrolide

Front 29

Amikacin

Back 29

Aminoglycoside

Front 30

Gentamicin

Back 30

Aminoglycoside

Front 31

Tobramycin

Back 31

Aminoglycoside

Front 32

Streptomycin

Back 32

Aminoglycoside

Front 33

Neomycin

Back 33

Aminoglycoside

Front 34

Netilmicin

Back 34

Aminoglycoside

Front 35

Quinupristin

Back 35

Streptogramin

Front 36

Dalfopristin

Back 36

Streptogramin

Front 37

Groups

1)Broad Spectrum
2)Moderate Spectrum
3)Narrow Spectrum

Back 37

1)Tetracycline, Tigecycline, Chloramphenicol, Clindamycin

2)Macrolides, Aminoglycosides

3)Linezolid, Streptogramins

Front 38

DOC

1)Chlamidya
2)Mycoplasma
3)Spirochetes
4)Anaerobic (eg: Clostridium)
5)Gram Neg (eg: Cholera)
6)Gram Pos Bacilli (eg: Anthrax)
7)Rocky Mountain Spotted Fever

Back 38

1-7 = Tetracycline

Front 39

1)Drug used for Complicated Skin, Soft Tissue, and Intra abdominal Infections (and Comm Acquired Pneumonia)

2)Drug combo used to treat Enterococcal Carditis

3)Aminoglycoside used to treat Plague and Tularemia

4)Aminoglycoside only used Topically?

Back 39

1)Tigecycline

2)Gentamicin and Penicillin

3)Streptomycin

4)Neomycin

Front 40

1)Chloramphenicol used as Alternative Drug for what infections?

2)Chloramphenicol used as backup drug for what infections?

Back 40

1)Rickettsia, Rocky Mountain, Anaerobic

2)Severe Salmonella Infections