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Protein Synthesis Inhibitors I Flashcards

1
Q

Protein synthesis inhibitors types?

A

Buy AT 30, CCELL(sell) at 50

30S Inhibitors

  1. Aminoglycosides
  2. Tetracyclines

50S Inhibitors

  1. Chloramphenicol
  2. Clindamycin
  3. Erythromycin /Macrolides

MOLD FKS

Mupirocin
Oxazolidinones
Lipopeptides
Disruption of bacterial plasma membrane

Fusidic acid
Ketolides
Streptogramins

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2
Q

Aminoglycosides

  1. MOA
  2. Bacteria MOA
A
  1. Inhibit 30S Ribosomal subunit
  2. Bactericidal
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3
Q

Aminoglycosides drugs?

A

TANGS

Tobramycin
Amikacin
Neomycin
Gentamicin
Streptomycin

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4
Q

Aminoglycosides resistance mechanims-3?

A
  1. Inhibit of transport into cell
  2. Inactivation by enzymes
    -Acetyl transferases
    -Adenyl transferases
    -Nucleotidyl Transferases
  3. Mutation of binding site on 30S ribosomal subunit (Streptomycin Only)
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5
Q

Streptomycin resistance mechanims?

A

Mutation of binding site on 30S ribosomal subunit (Streptomycin Only)

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6
Q

Aminoglycosides antibiotic effect?

A

Prolonged post-antibiotic effect

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7
Q

Aminoglycosides admin & not?

A

IM/IV (Not oral)

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8
Q

Aminoglycosides admin for eye infections?

A

Topical for sight-threatening eye infections

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9
Q

Aminoglycosides S/E and ir/reversible-7?

A
  1. Nephrotoxicity-reversible
    -All of them
  2. Ototoxicty-Irréversible
  3. Neuromuscular Blockage
  4. Liver damage
  5. Headache
  6. Skin Rashs
  7. Fever
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10
Q

Aminoglycosides nephrotoxicity levels in all drugs?

A

GeNeTo

Increased nephrotoxicty

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11
Q

Which aminoglycosides causes deafness in children?

A

Streptomycin

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12
Q

Ototoxicty amnioglycosides intensities?

A

NeoKanAmi

Neomycin
Kanamycin
Amikacin

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13
Q

Vestibulotoxic amnioglycosides intensities?

A

StreGen

Streptomycin
Gentamycin

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14
Q

Aminoglycosides CI?

A
  1. Pregnancy(Streptomycin)
  2. Myasthenia Gravis (Due to neuromuscular blockage)
  3. Renal insufficiency
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15
Q

Aminoglycosides DI-4?

Mention two drugs that cause Nephrotoxic agents

A
  1. General Anaesthetics-prolonged paralysis
  2. NMB-Prolonged paralysis, Resp depression, prolonged apnea
  3. Oto-or-Nephrotoxic agents
    -Vancomycin
    -Amphotericin
    -Above is the increased
    risk of oto-and
    nephrotoxicity
  4. Loop diuretics-Increased risk of ototoxicity
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16
Q

Which aminoglycosides have increased risk of oto-and-nephrotoxicty?

A

Vancomycin

   &

Amphotericin

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17
Q

Tetracyclines

  1. MOA
  2. Bacteria MOA
A
  1. Inhibit 30S ribosomal subunit-prevent the formation of initiation complex
  2. Bacteriostatic
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18
Q

Tetracyclines drugs?

A

Tetracycline
Doxycycline
Minocycline

19
Q

Tetracyclines and glycyclines and name?

A

A new class derived from minocycline(Inf resistant to tetracyclines)

Tigecyline

20
Q

Tetracyclines drugs of choice against?

A
  1. Rickettsia
  2. Chlamydia
  3. Brucellosis
21
Q

Tetracyclines resistance mechanisms?

A

-Decreased intracellular accumulation-Decrease influx or Increase Efflux

-Enzymatic Inactivation

-Production of a protein that interferes with the binding of tetracyclines on the ribosomes

22
Q

Tetracyclines S/E-7?

Mention one specific for minocycline too

A
  1. Discolouration of nails & teeth
  2. Bone growth retardation
  3. Pseudomembranous colitis (clostridium difficle)
  4. Photosensitivity
  5. Nephrotoxcity & Heptoxicty
  6. Destruction of normal gut flora
  7. Minocycline-Specific S/E
    -Blue-grey pigmentation of
    the skin & acne
    scars=vestibulotoxic
23
Q

Tetracyclines DI & why?

A

-Vit A and other retinoids
-Risk of increased
intracranial pressure BECAUSE tetracycline and a form on Vit A cross the BBB

-Decreased Efficacy of combined oral contraceptives-ALL antibiotics do this

24
Q

Tetracyclines CI-6 & why?

A

-Pregnancy & Children < 8-12 years ‘coz it causes bone retardation

-Myasthenia gravis-tetracyclines have a weak NMB effect

-Systemic lupus erythematosus(Minocycline)

-Hepatic Impairement -causes hepatoxicty as a S/E

-Porphyria

-Elderly-Crosses BBB thus DUH!

25
Chloramphenicol 1. MOA 2. CYP450 3. Admin/Bioavailability
1. Inhibits 50S ribosomal unit-inhibit peptidyltransferase 2. CYP450 Inhibitor 3. Oral-80% bioavailability
26
Chloramphenicol treatment?
-Rickettsidal Infections -Bacterial Meningitis (Crosses BB) -Typhoid Fever -Bacterial eye Infections
27
Chloramphenicol resistance mechanisms?
-Production of Chloramphenicol acetyltransferase -inactivation of the drug
28
Chloramphenicol S/E-3?
BAG -Bone marrow suppression -Aplastic anemia(fatal) -Grey-baby syndrome
29
Chloramphenicol CI?
-Neonates( Grey-baby syndrome) -Pregnancy (3rd trimester) & Lactation
30
Clindamycin 1. MOA 2. Bacteria MOA and differing concentrations
1. Inhibits 50S ribosomal subunit 2. Bacteriostatic at low concentrations & Bactericidal at increased concentrations
31
Clindamycin resistance of mechanisms?
-Mutations of ribosomal binding site -Enzymatic inactivation -usually for protein synthesis
32
Clindamycin S/E-3?
1.Pseudomembranous colitis 2. Transient increased liver enzymes and bilirubin 3. Transient leucopenia eosinophilia, thrombocytopenia and agranulocytosis’
33
Clindamycin S/E?
1. Pseudomembranous colitis 2. Transient increased liver enzymes and bilirubin 3. Transient leucopenia, eosinophillia, thrombocytopenia
34
Clindamycin cautions?
Pregnancy/Lactation
35
Clindamycin and malaria?
Sometimes treated for malaria
36
Macrolides drugs?
1. Erythromycin 2. Azythromycin 3. Clarithromycin
37
Macrolides CYP450 and p-glycoproteins?
Inhibit CYP450 & P-glycoprotein
38
Macrolides 1. MOA 2. Bacteria MOA @ different concentrations? 3. Placenta/BBB 4. Best absorption
1. Inhibits 50s ribosomal subunit 2. Bacteriocidal at increased concentrations and bacteriostatic at decreased concentration 3. Crosses the placenta but not BBB 4. Best absorbed as estolate form
39
Macrolides I?
Respiratory bacterial infections
40
Macrolides treatment?
1. Rickettsial infections (Azythromycin & Clarithromycin) 2. Helicobacter pylori(Peptic ulcer)
41
Which macrolides drugs treat ricketsial infection?
Azythromycin & Clarithromycin
42
Macrolides resistance mechanisms?
-Decreased cell membrane permeability or active efflux -Modification of binding site -Production of esterases that hydrolize macrolides
43
Macrolides S/E?
1. Hepatotoxicity 2. Cholestatic jaudice

Pharmacology (44 decks)

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