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Pharmacology > Protein Synthesis inhibitors > Flashcards

Protein Synthesis inhibitors Flashcards

1
Q

Aminoglycosides mechanism

A

Block association of 50S subunit with 30S-m RNA complex (static)
ii. Misreading of code-incorporation of wrong amino acid. (cidal)

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2
Q

Linezolide(50S) mechanism

A

Block association of 50S subunit with 30S-m RNA complex (static)

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3
Q

The drugs that prevent Amino acid interaction with the acceptor site

A

Tetracycline(30S)
Streptogramin(50S)

Block the attachement of aminoacyl t RNA to acceptor site(static)

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4
Q

Chloramphenicol act by

A

Blocking Formation of peptide bonds

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5
Q

Mechanism of Chloramphenicol

A

Inhibit activity of peptidyl transferase(-static)

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6
Q

Macrolide & Clindamycin(50S)

work by

A

Blocking Translocation

Mechanism: Inhibiting peptidyl t RNA from acceptor to donor site(static)

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7
Q

Name Tetracyclines

A

TETRACYCLINE
DEMECLOCYCLINE
DOXYCYCLINE - Lipid soluble, lyme disease. Most affective.

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8
Q

Tetracyclines chelate metal ions—Ca2+, Al3+, Fe2+, Mg2+

Not absorbed therefore..

A

do not administer with food, milk, antacids, etc.

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9
Q

Tetracyclines are concentrated in

A

Concentrates in teeth, bone, liver (bile), kidney

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10
Q

Tetracyclines can cross the

A

cross the placenta and are excreted in milk

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11
Q

All tetracylines are excreted through urine except

A

Doxycycline

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12
Q

Tigecycline useful for?

A

Treatment of complicated skin and skin structure infections caused by susceptible organisms, including:
Methicillin-resistant Staphylococcus aureus
Vancomycin-sensitive Enterococcus faecalis
Treatment of complicated intra-abdominal infections

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13
Q

New approved tetracycline analog

A

Tigecycline

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14
Q

Adverse Effects of Tetracyclines

A
  1. G.I.T.: N/V, diarrhea are the most common (superinfection, alters intestinal flora)
  2. Bone and Teeth: Tetracyclines concentrate in growing teeth and bone. Their use by pregnant women or children under 8 yrs of age may cause discoloration of teeth and hypoplasia of the enamel, resulting in yellow-brown or gray mottling of front teeth.
  3. Liver & Kidney: TCNs may cause potentially severe Nephrotoxicity (except Doxycycline) and Hepatotoxicity in the form of fatty degeneration.
  4. Phototoxicity (don’t go in the sun otherwise you’ll get rashes) , Demeclocycline leading to erythema, and exacerbating the sunburn.(classic V-neck shaped bright red rashes in the sun exposed area
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15
Q

Resistance to Tetracyclines is by

A

Decreased uptake of tetracyclines– efflux pumps are major mediators.

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16
Q

Tetracyclines have become resistant because of

A

Indiscriminate use/overuse of tetracyclines

(clinical and agricultural) has fostered the emergence of resistance

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17
Q

Chloramphenicols (50s) are both

A

Bacteriostatic

Broad spectrum

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18
Q

Adverse affects of Chloramphenicols

A

Anemia due to bone marrow depression (Dose Dependant)
Aplastic anemia
Probably idiosyncratic reaction (genetic)
Not strictly dose- and time-related, but more common with prolonged use
USUALLY IRREVERSIBLE AND FATAL

Gray Baby syndrome
Newborns and infants are poor glucuronidator’s (H.Influenzae induced Meningitis)

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19
Q

Chloramphenicols inhibit the metabolism of drugs by?

A

Inhibits CYTP450

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20
Q

Chloramphenicol are used to treat

A

Typhoid fever & Rocky Mountain spotted fever in children & meningitis in both adult & chidren ; ace-in-the-hole drug

21
Q

Some Macrolides are

A 
Anything with THRO
ERYTHROMYCIN BASE
ERYTHROMYCIN ESTERS
AZITHROMYCIN
CLARITHROMYCIN
22
Q

Macrolide adverse affects

A

1) GI distress –due to direct stimulation of motilin receptor by all macrolides - CAUSE INCREASED Peristalsis –most common (exception Clarithromycin).

2) Hepatotoxicity–Especially with erythromycin estolate
Cholestatic jaundice

3) Blocks CYP450 but not azithromycin
4) QT prolongation (erythromycin

23
Q

Telithromycin used in

A

Macrolide resistant Streptococcus pneumoniae

24
Q

Azithromycin is good because

A

Minimal P450-based interactions (excreted by kidney)
Tissue levels 10-100 x plasma levels; t ½ = 2 - 4 days
Active against Mycobacterium avium-intracellulare in AIDS patients (an exception where bacteriostatic is used in an immunocompromised condition-Hence very high dose required )
Only macrolide safe in Pregnancy.

25
Q

Clindamycin treats

A

Narrow spectrum,
some gm +ve - staph aureus
*example main cause of osteomyletis is staph aureus, this drug will stay in the bone and kill it.

Anaerobic - Bacteroides fragilis

26
Q

Clindamycin can be used for

A
  1. Endocarditis prophylaxis
  2. Clinical value in Osteomyelitis (only caused by Staph.Aureius)
  3. Plevic Inflammatory Disease:
    Inpatient:Clindamycin plus gentamicin followed by doxycycline
    Outpatient:ceftriaxone followed by doxycycline

Clostridium superinfections ,

27
Q

Streptogramins is

A

Potent inhibitor of CYP3A4
Wide range of ONLY gram +ive bacteria including
-Staphylococci that are resistant to Methicillin, Quinolones, and Vancomycin;
-Pneumococci that are resistant to Penicillin; and
-E. faecium strains resistant to Vancomycin.

28
Q

Linezolid

A

Primary indication– Vancomycin-resistant E. faecium , VRE & PNSP

Adverse effects—bone marrow suppression (Platelets), superinfection

29
Q

Aminoglycosides

A 
STREPTOMYCIN
NEOMYCIN
GENTAMICIN 
TOBRAMYCIN
AMIKACIN
NETILMYCIN
30
Q

Amino glycosides are used

A

Used against drug-resistant gonococci or in penicillin allergic patients with gonorrhea

31
Q

Adverse effects of AG’s

A

Should be given once a day because its bactericidal - therefore less toxicity.

Nephrotoxicity -because its water soluble
Ototoxicity
Contact Dermatitis - because of neomycin (triple antibiotic ointment - neosporin)
Neuromuscular blockade (decreased Ach)

32
Q

AG’s are used for

A

In combination with a cell wall inhibitor like penicillin
1. Gram negative bacteria aerobic - e.coli
2. P. aeruginosa
2. enterococcal, staph or viridans
TB
DOC - bubonic plague and tolaremia

33
Q

Neomycin

A

Used in Hepatic Encephalopathy

34
Q

Clindamycin mechanism of action?

A

Block 50s subunit

35
Q

Macrolides mechanism of action

A

Block 50s subunit

36
Q

Drugs the block the formation of the initiation complex?

A

Aminoglycosides and Linezolid

37
Q

Translocation inhibitors

A

Clindamycin and Macrolides

38
Q

Amino glycosides enter through?

A

O2 dependent channel, therefore they’re not useful against anaerobes.

39
Q

What is the only amino glycoside given topically?

A

Neomycin

40
Q

Resistance to aminoglycosides is by?

A

Bacteria producing conjugating enzymes, causes aminoglycosides to be conjugated faster and eliminated fast.

41
Q

Tetracyclines work by inhibiting the?

A

30s subunit and prevent elongation. Prevent tRNA attachment to the A site.

42
Q

Tetracyclines are broad spectrum antibiotics that work on?

A

H.pylori, Borrelia bugdorferi, Rickettsia

Doxycycline - Lyme disease

43
Q

Drugs that cause phytotoxicity (rashes upon sun exposure)

A

Tetracyclines
Sulfonomides
Quinolones

44
Q

Macrolide are useful for treating

A 
Atypical organisms - chlamydia, mycoplasma, 
Legionella 
Campylo
Mycobacterium Avium
H. pylori
45
Q

Macrolide resistance is caused by

A

Bacteria methylates the 50s subunit therefore the drug cannot recognize the 50s to bind to.

46
Q

Side effect of Clindamycin

A

causes pseudomembranous colitis

47
Q

Clindamycin resistance is caused by?

A

Bacteria methylates the 50s subunit therefore the drug cannot recognize the 50s to bind to.

48
Q

Linezolid treats and side effects?

A

treats: VRSA

Side effects BM suppressionBacteria methylates the 50s subunit therefore the drug cannot recognize the 50s to bind to

Pharmacology (8 decks)

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