Inhibitors of proteins synthesis Flashcards
Aminglycosides
Gentamicin
Tetracycline
Doxycycline
Macrolides
Azithromycin
Lincosamides
Clindamycin
Oxizolindinones
Linezolid
Inhibition of ribosomal function is _
Bacteriostatic except for aminoglycosides because they cause miscoding of the RNA which is bactericidal
gentamicin mechanism of action
Attraction of negatively charged LPS in out membrane of G- bacteria
Bactericidal (also active against mycobacteria and Protozoal parasites)
peak/MIC
Irreversibly bind to 30S ribosomal subunit stops formation of initiation complex leading to misreading of mRNA and incorrect incorporation of amino acids
Post-antibiotic effect
Residual activity after plasma levels fall below MIC
Gentamicin
Resistance to gentimycin is due to
drug inactivation by bacterial kinase and acetyltransferase
Gentamicin is _toxic
Nephro
Oto (drug accumulation in inner ear)
Doxycycline mechanism of action
Binds to 30S ribosomal subunit to inhibit landing do tRNAs into A-site preventing the addition of amino acids
Doxycycline is active against
G+ and G- bacteria
Atypical bacteria
Tick borne illnesses
Protozoans
Doxycycline resistance due to
TetM (interfere with binding to 30S)
Doxycycline activity is
AUC/MIC
Widely distributed
Doxycycline cannot be given with
Dairy products, iron supplements, Mg-laxatives or antacids due to the formation of insoluble chelates leading to decreased oral absorption
Tetracycline adverse reactions
GI irritation
Photosensitivity
Deposition in bones and teeth leading to discoloration and growth impairment (avoid in pregnant females and children)
_ is the only tetracycline that may be given during pregnancy
Doxycycline
Azithromycin mechanism of action
Bacteriostatic
Binds reversible to 50S subunit to inhibit translocation
Azithromycin is active against
G+ and G- anaerobes
Atypical bacteria
Mycoplasma and protozoal parasites
Resistance to macrolides is due to
High level of methylation of 50S that decreases binding affinity (erm=multi-drug resistance, MLS)
Macrolide adverse reactions
Prolonged cardiac Q-T interval increases arrhythmias
Clindamycin mechanism of action
Binds 50S to block peptide bond formation
Bacteriostatic
Clindamycin adverse reactions
Black box warning for C diff colitis
Linezolid mechanism of action
Binds to 23S rRNA of 50S subunit blocking formation of initiation complex
Linezolid adverse effects
Limited by toxicity (only used against drug resistant infections)
Myelosupression
Lactic acidosis
Black box warning for MAO inhibition, use with antidepressants, and Serotonin syndrome