Protein Synthesis Inhibitors I Flashcards
Protein synthesis inhibitors types?
Buy AT 30, CCELL(sell) at 50
30S Inhibitors
- Aminoglycosides
- Tetracyclines
50S Inhibitors
- Chloramphenicol
- Clindamycin
- Erythromycin /Macrolides
MOLD FKS
Mupirocin
Oxazolidinones
Lipopeptides
Disruption of bacterial plasma membrane
Fusidic acid
Ketolides
Streptogramins
Aminoglycosides
- MOA
- Bacteria MOA
- Inhibit 30S Ribosomal subunit
- Bactericidal
Aminoglycosides drugs?
TANGS
Tobramycin
Amikacin
Neomycin
Gentamicin
Streptomycin
Aminoglycosides resistance mechanims-3?
- Inhibit of transport into cell
- Inactivation by enzymes
-Acetyl transferases
-Adenyl transferases
-Nucleotidyl Transferases - Mutation of binding site on 30S ribosomal subunit (Streptomycin Only)
Streptomycin resistance mechanims?
Mutation of binding site on 30S ribosomal subunit (Streptomycin Only)
Aminoglycosides antibiotic effect?
Prolonged post-antibiotic effect
Aminoglycosides admin & not?
IM/IV (Not oral)
Aminoglycosides admin for eye infections?
Topical for sight-threatening eye infections
Aminoglycosides S/E and ir/reversible-7?
- Nephrotoxicity-reversible
-All of them - Ototoxicty-Irréversible
- Neuromuscular Blockage
- Liver damage
- Headache
- Skin Rashs
- Fever
Aminoglycosides nephrotoxicity levels in all drugs?
GeNeTo
Increased nephrotoxicty
Which aminoglycosides causes deafness in children?
Streptomycin
Ototoxicty amnioglycosides intensities?
NeoKanAmi
Neomycin
Kanamycin
Amikacin
Vestibulotoxic amnioglycosides intensities?
StreGen
Streptomycin
Gentamycin
Aminoglycosides CI?
- Pregnancy(Streptomycin)
- Myasthenia Gravis (Due to neuromuscular blockage)
- Renal insufficiency
Aminoglycosides DI-4?
Mention two drugs that cause Nephrotoxic agents
- General Anaesthetics-prolonged paralysis
- NMB-Prolonged paralysis, Resp depression, prolonged apnea
- Oto-or-Nephrotoxic agents
-Vancomycin
-Amphotericin
-Above is the increased
risk of oto-and
nephrotoxicity - Loop diuretics-Increased risk of ototoxicity
Which aminoglycosides have increased risk of oto-and-nephrotoxicty?
Vancomycin
&
Amphotericin
Tetracyclines
- MOA
- Bacteria MOA
- Inhibit 30S ribosomal subunit-prevent the formation of initiation complex
- Bacteriostatic
Tetracyclines drugs?
Tetracycline
Doxycycline
Minocycline
Tetracyclines and glycyclines and name?
A new class derived from minocycline(Inf resistant to tetracyclines)
Tigecyline
Tetracyclines drugs of choice against?
- Rickettsia
- Chlamydia
- Brucellosis
Tetracyclines resistance mechanisms?
-Decreased intracellular accumulation-Decrease influx or Increase Efflux
-Enzymatic Inactivation
-Production of a protein that interferes with the binding of tetracyclines on the ribosomes
Tetracyclines S/E-7?
Mention one specific for minocycline too
- Discolouration of nails & teeth
- Bone growth retardation
- Pseudomembranous colitis (clostridium difficle)
- Photosensitivity
- Nephrotoxcity & Heptoxicty
- Destruction of normal gut flora
- Minocycline-Specific S/E
-Blue-grey pigmentation of
the skin & acne
scars=vestibulotoxic
Tetracyclines DI & why?
-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
Tetracyclines CI-6 & why?
-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!
Chloramphenicol
- MOA
- CYP450
- Admin/Bioavailability
- Inhibits 50S ribosomal unit-inhibit peptidyltransferase
- CYP450 Inhibitor
- Oral-80% bioavailability
Chloramphenicol treatment?
-Rickettsidal Infections
-Bacterial Meningitis (Crosses BB)
-Typhoid Fever
-Bacterial eye Infections
Chloramphenicol resistance mechanisms?
-Production of Chloramphenicol acetyltransferase
-inactivation of the drug
Chloramphenicol S/E-3?
BAG
-Bone marrow suppression
-Aplastic anemia(fatal)
-Grey-baby syndrome
Chloramphenicol CI?
-Neonates( Grey-baby syndrome)
-Pregnancy (3rd trimester) & Lactation
Clindamycin
- MOA
- Bacteria MOA and differing concentrations
- Inhibits 50S ribosomal subunit
- Bacteriostatic at low concentrations & Bactericidal at increased concentrations
Clindamycin resistance of mechanisms?
-Mutations of ribosomal binding site
-Enzymatic inactivation -usually for protein synthesis
Clindamycin S/E-3?
1.Pseudomembranous colitis
- Transient increased liver enzymes and bilirubin
- Transient leucopenia eosinophilia, thrombocytopenia and agranulocytosis’
Clindamycin S/E?
- Pseudomembranous colitis
- Transient increased liver enzymes and bilirubin
- Transient leucopenia, eosinophillia, thrombocytopenia
Clindamycin cautions?
Pregnancy/Lactation
Clindamycin and malaria?
Sometimes treated for malaria
Macrolides drugs?
- Erythromycin
- Azythromycin
- Clarithromycin
Macrolides CYP450 and p-glycoproteins?
Inhibit CYP450 & P-glycoprotein
Macrolides
- MOA
- Bacteria MOA @ different concentrations?
- Placenta/BBB
- Best absorption
- Inhibits 50s ribosomal subunit
- Bacteriocidal at increased concentrations and bacteriostatic at decreased concentration
- Crosses the placenta but not BBB
- Best absorbed as estolate form
Macrolides I?
Respiratory bacterial infections
Macrolides treatment?
- Rickettsial infections (Azythromycin & Clarithromycin)
- Helicobacter pylori(Peptic ulcer)
Which macrolides drugs treat ricketsial infection?
Azythromycin & Clarithromycin
Macrolides resistance mechanisms?
-Decreased cell membrane permeability or active efflux
-Modification of binding site
-Production of esterases that hydrolize macrolides
Macrolides S/E?
- Hepatotoxicity
- Cholestatic jaudice