Protein synthesis inhibitors Flashcards
name the protein synthesis inhibitor groups
Tetracyclines, Glycyclines, Aminoglycosides, Macrolides/Ketolides, Others..
Tetracycline group
Demeclocyline, Doxycycline, Minocycline, Tetracycline
Glycycline group
Tigecycline
Aminoglycoside group
Amikacin, Gentamicin, Neomycin, Streptomycin,Tobramycin
Macrolide/Ketolide group
Azithromycin, Clarithromycin, Erythromycin, Telithromycin
Others group
Cloraphenicol, clindamycin, Linezolid, Quinupristin/Dalfopristin
Tetracycline site of action
Reversibly bind to 30S ribosomal subunits
Tetracycline spectrum
Broad spectrum bacteriostatic, gram+ bacilli and gram- rods, and organisms other than bacteria
Organisms effected by tetracyclines
All cocci, Bacillus anthracis+, Vibrio cholerae-, Yersinia prestis-, Clostridium prfringens/tetani, Borelia burgdoferi , Leptospira, Mycoplasma pneumoniae, Chlamydia, Rickettsia rickettsi
Tetracycline distribution
Liver, kidney, spleen and skin, bind to tissue undergoing calcifications,
Tetracycline elimination
Both bile and glomerular filtration (breast milk)
Doxycycline elimination
preferably through bile
Tetracycline Adverse effects
Gastric discomfort, discoloration of teeth and hypoplasia of bone during development, hepatotoxicity in pregnant women with pyelonephritis, phototoxicity, Vestibular problems, Superinfections
Tetracycline Absorption
adequately absorbed after oral ingestion, Do not ingest together with diary products or divalent/trivalent cations because of decreased absorption.
Tetracycline contraindications
Renally impaired patients (except doxycycline) Not use in pregnant women or children under 8 years
Glycylcyclines (Tigecycline) Spectrum
MRSA, Multi resistant Strep pneumo, VRE, B-lactamase producing gram- bacteria, Acinetobacter baumannii
Tigecycline distribution
Distributes rapidly to body tissues, and sould never be used against bacteremia
tigecycline elimination
primarily through bile.
Tigecycline adverse effects
Significant nausea and vomiting, otherwise same as other tetracyclines
Tigecycline interactions
No P450 interaction, Inhibits clearance of Warfarin, diminishes effectiveness of contraceptives.
Tigecycline site of action
Bacteriostatic, reversibly binding to 30S subunit inhibits translation
Aminoglycosides action
Gram- bacilli, diffuse through porin channels, bactericidal bind to 30S
Aminoglycosides spectrum
gram- bacilli, pseudomonas aeruginosa, Only aererobic organisms (unless used together with a B-lactam/Vancomycin)
Clinical use monotherapy
Only UTI
Aminoglycosides adminisration
only parenterally (except neomycin, but is so nephrotoxic that it is only used topically)
Dose calculation (aminoglycosides)
Lean body mass, since aminoglycosides don’t distribute to fat.
aminoglycoside metabolism
is not metabolizes in the body, quickly excreted to urine NB patients with renal impairment
Patient with myasthenia gravis is given an aminoglycoside abx, what would reverse the neuromuscular paralysis?
Calcium gluconate or neostigmine
aminoglycoside acumulation
accumulates in perilymph, endolymph and renal cortex, hence oto- and nephrotoxixcity
aminoglycoside ototoxicity
may lead to deafness, known to affect fetuses in utero
aminoglycoside nephrotoxicity
affects proximal tubular cells, can range from mild renal impairment to ATN
Ketolide
telithromycin
Macrolides site of action
Bids to the 50S subunit inhibits translocation, is bacteriostatic, but can act bacteriocidal in high doses
Erythromycin spectrum
acts on many of the same organisms as Penicillin G, is used in patients with penicillin sensitivity
Clarithromycin spectrum
similar to erythromycin, but additional H. Influenza, Chlamydia, Legionella, Moraxella, Ureaplasma, H. Pylori.
Azithromycin spectrum
Better action against, H. influenza, Moraxella, Chlamydia, Mycobacterium avium.
Telithromycin spectrum
A ketolide, acts on same organisms same as azithromycin, but more effective on resistant strains.
cross-resistance of macrolides
all… erythromycin, azithromycin, clarithromycin , except for the ketolide, telithromycin..
Erythromycin distribution
all body fluids and tissues especially liver, even prostatic fluid, except CSF,
erythromycin accumulation
accumulates in macrophages
Tetracyclines primary use
Mycoplasma pneumo, Chlamydia, Rickettsia, Vibrio.
Tetracyclines secondary use
acne and resp infections for susceptible organisms
Tetracycline specific use
H pylori
Doxycycline spec use
lyme disease, malaria prophylaxis, amebiasis
minocycline spec use
meningococal carrier state
Demeclocycline specific use
inhibits ADH action on kidneys.. used for patients with ADH secreting tumors.