PHARMA protein Synthesis Inhibitors Flashcards
Bind to 50s subunit and block TRANSLOCATION (step 2)
Macrolides
Bind to 50s subunit and inhibit PEPTIDYLTRANSFERASE
Chloramphenicol
Bind to 30s subunit and inhibit binding of incoming charged aminoacyl-tRNA unit to the acceptor site (step 1)
Tetracyclins
Inhibit formation of initation complex and misread codes
Aminoglycosides
Bind 30s?
Clindamycin
Should not be given with bivalent metal ions like antacids
Tetracyclins
Give 3 tetracyclins
Minocycline
Doxycycline
Tigecycline
Minocycline use
For meningococceal carrier state
DOC for patients with renal insufficiencies
Doxycycline
Broad spectrum but proteus and p aeruginosa are intrinsically resistant
Tigecycline
MLS stands for?
Macrolide
Lincosamide
Streptogramins
Inhibitors of cyp3A4
Macrolides and clindamycin
Prototypic macrolide drug
Erythromycin
Used against gram positive organisms
Erythromycin
Most common reason for discontinuing erythromycin
Adr of GI intolerance(erythromycin activates motillin receptors)
More active against MAC
Clarithromycin
Advantages of clarithromycin over erythromycin
Less gi intolerance
Less frequent dosing
Codrug of choice against chlamydia along with doxycycline
Azithromycin
Clindamycin + aminoglycoside or cephalosporin
Tx of penetrating wounds of the abdomen or gut
Alternative to cotri against moderately severe pneumocystis jiroveci pneumonia in aids patients
Clindamycin + primaquine
For aids related toxoplasmosis of the brain
Clindamycin + pyrimethamine
Always associated with pseudomembranous enterocolitis
Clindamycin
Combination of 2 streptogramins
Quinupristin-Dalfopristin (B and A respectively)
MLS type A resistant organisms are resistant to what streptogramin?
Dalfopristin
Resistance of chloramphenicol
Transacetylase
Approved for tx of infections by staph or vancomycin resistant e. Faecium
Quinupristin dalfopristin
Rarely used because it has lots of adrs
Chloramphenicol
Gray baby syndrome
Chloramphenicol because babies cant glucoronate chloramphenicol yet
Tx for serious rickettsial infections, but not chlamydia
Chloramphenicol
Other adrs of chloramphenicol
Gi disturbance
Bone marrow suppression - dose related and fatal aplastic anemia
Explain how aminoglycosides can be bacteriostatic and bacteriocidal at the same time
Bacteriostatic - interfere with initiation complex of peptide formation
Bacteriocidal - misreading of mrna and coding non functional proteins
Resistance by adenylation acetylation phosphorylation etc
Aminoglycosides
Oxygen dependent, so cant be used on anaerobics
Aminoglycosides
4 reasons why once daily dosing for aminoglycosides is enough
Nephrotoxic
Narrow therapeutic range
High PAE
concentration dependent
ADRS of aminoglycosides
Nephrotoxic Ototoxic Vestibular dysf NM blockade Contact dermatitis
Polar, poorly absorbed, always parenteral
Aminoglycosides
Most ototoxic aminoglycosides
NKA
neomycin
Kanamycin
Amikacin
Most vestibulotoxic aminoglycoside
Streptomycin
Gentamicin
Most nephrotoxic aminoglycoside
NTG
neomycin
Tobramycin
Gentamicin
Adr contact dermatitis
Neomycin
Fifth agent for tb
Streptomycin
Causes deafness in newborn if given in pregnancy
Streptomycin
Used in severe infections, in IM IV or topical form
Gentamicin
Available in inhalational form for p aeruginosa lrti in complicated cystic fibrosis
Tobramycin
For topical and oral use only aminoglycoside
Neomycin and kanamycin
Alternative tx for drug resistant gonorrhea
Spectinomycin
Inhibits protein synthesis by binding to 23s rRNA of 50s subunit
Oxazolinidones
Most common adr of linezolid
Thrombocytopenia