Protein Synthesis Inhibitors Flashcards
1
Q
Aminoglycosides
A
- Binds to 30s ribosome
- Are bactericidal
- NO anaerobic activity
- Concentration dependent
- Combined with beta lactams can treat sepsis (gram - )
- Combined with beta lactams or vancomycin can treat endocarditis (enterococus, gram +)
2
Q
3 Mechanisms of Aminoglycosides
A
1) blocks formation of ribosome complex
2) blocks proof reading- leading to misreads so the wrong amino acids are made
3) blocks ribosomal translocation on mRNA (Bactericidal/irreversible)
3
Q
Streptomycin
A
-Aminoglycoside
4
Q
Kanamycin
A
-Aminoglycoside
5
Q
Gentamicin
A
-Aminoglycoside
6
Q
Tobramycin
A
-Aminoglycoside
7
Q
Amikacin
A
-Aminoglycoside
8
Q
Neomycin
A
-Aminoglycoside
9
Q
Aminoglycoside warnings
A
- Nephrotoxicity (reversible)
- Ototoxicity (irreversible)
10
Q
Tetracyclines
A
- Bind to 30s ribosome
- Prevents binding of incoming tRNA
- Bacteriostatic
- Effective against; gram+, gram-, and atypicals
11
Q
Tetracycline
A
- Tetracycline
- Short acting
- Don’t use in children 6 to 12, will mess up their teeth
12
Q
Doxycycline
A
- Long acting tetracycline
- Eliminated in the Bile
- Covers CAP and MRSA
13
Q
Minocycline
A
- Minocin
- Long acting tetracycline
- Covers P. acnes, meningitis, gonorrhea, Chlamydia, and MRSA
14
Q
Tigecycline
A
-Longest acting tetracycline
15
Q
Tetracycline Interactions
A
- Take on an empty stomach
- Dairy
- Antacids
- Iron
- Zinc
- All lower absorption
16
Q
Doxycycline
A
- Doryx
- Tetracycline
17
Q
Macrolides
ACE
A
- Bind reversibly to the 50s
- Mainly covers Atypicals (STDs) and mycobacteria
- Orally absorbed
18
Q
Azithromycin
A
- Zithromax
- Macrolide antibiotic
- Long half life
- Does NOT use CYP450
19
Q
Clarithromycin
A
- Biaxin
- Macrolide antibiotic
- Short half life
20
Q
Erythromycin
A
-Makes you poop (in low doses)
21
Q
Fidaxomicin
A
- New Macrolide antibiotic
- Stays localized in the gut
- Covers C. diff
22
Q
Lincosamide
A
- Binds reversibly to 50s ribosome to block exit of polypeptide
- Spectrum= gram +(MRSA) and anaerobes (B. fragilis)
- Box warning: May cause C. diff
23
Q
Clindamycin
A
- Cleocin
- Lincosamide
- Covers B. fragilis (anaerobe)
- Covers gram + (MRSA)
- Black box warning-C.diff
24
Q
Streptogramins
A
- Bind reversibly to the 50s ribosome
- Blocks the exit of the polypeptide
- Active against gram + cocci (Except for E. faecalis)
25
Dalfopristin + Quinupristin
- Streptogramins
- Dalfopristin increases the binding affinity of Quinupristin
- When used together they are bactericidal
- May cause prolonged QT interval
- CYP3A4 metabolized
26
Streptogramins
- Binds to 23s rRNA to prevent the assembly of ribosome
- 100% orally bioavailable
- Bacteriostatic in general
- Bactericidal for streptococcus
- Covers gram + (MRSA and E. faecium)
- Used for serious vancomycin resistant infections
27
Linezolid
- Zyvox
| - 1st generation Oxazolidinone
28
Tedlizolid
-2nd generation Oxazolidinone
29
Synercid
- Dalfopristin + Quinupristin
| - Streptogramin
30
Drugs that cover P. aeruginosa
1) Ceftriaxone (3rd gen cephalosporin)
2) Cefepime (4th gen cephalosporin)
3) Aztreonam (Monobactam)
31
Drugs that cover MRSA
1) Ceftaroline (5th gen cephalosporin)
2) Doxycycline (tetracycline)
3) Minocycline (tetracylcine)
4) Clindamycin (Lincosamide)
32
Drug of choice for S. pnumoniae
-Ceftazidime + Avibactam (3rd gen cephalosporin)
33
Which drug covers E. faecalis
- Quinupristin + Dalfopristin
| - Streptogramins
34
What covers E. faecium
- Linezolid
| - Oxazolidinones
35
Moxifloxacin
- Avelox
| - Fluoroquine antibiotic
36
What drives ototoxicity in Aminoglycosides
- Mitochondria have similar ribosomes to bugs
- So abx may attack the hosts mitochondria
- This damage leads to ototoxicity
37
Name some aminoglycosides
| -ycin,-icin
- Neomycin
- Kanamycin
- Gentamicin
- Amikacin
- Plazomicin (zemdri)
38
If a drug follows the rule of five then..
- It is orally bioavailable
| - If not try IV or inhalation
39
Tobraycin Inhalation
-Can be used for cystic fibrosis patients
40
Plazomicin (Zemdri)
- New Aminoglycoside
| - Administered IV
41
MoA of Macrolides
- Bind to 50s subunit
- Inhibit the translocation of tRNA
- 14 or 15 membered rings
42
Azithromycin
- Macrolide
- Long half life
- No potential for ketal
- Acid stable
43
Lincosaindes structure
-Contain thiomethyl aminooctoside, amide linked to Nmethly derivaive
44
Tetracycline structure
- Contains 4 fused six member rings
- Act on 30s ribosomal subunit
- Inhibits elongation of protein chain
45
Purpose of adding amines
- Adds on a bit of lipophilicity
| - Increasing half life of the drug
46
Tigecycline
- Tetracycline
- Half life > 24hrs
- Resistant to efflux pumps
- Can overcome some resistance
47
Tedizolid strength
- Has the ability to be given IV or orally
| - Good for patients trying to get out of the hospital
48
Why is Chloramphenicol not used
- Due to toxicities
- Binds to 50s subunit
- Can see in medical tourists
