Study Flashcards
Macrolides
Erythromycin, clarithromycin, azithromycin
Macrolides MOA
Blocks peptide formation at the 50s ribosomal subunit to inhibit protein synthesis
Macrolides C vs S
Static
Macrolides PD
Time-dependent
Macrolides pathogens
Broad spectrum
Gram +, Neisseria, Treponema
DOF for atypicals (mycoplasma, legionella, chlamydia)
Macrolides main uses
Used in pregnancy and for penicillin allergies
STI (chlamydia, gonorrhea)
RTI (pharyngitis, otitis, CAP)
Gastroparesis
Do macrolides have MRSA or pseudomonas coverage?
No
Macrolides AE
GI
Increased QTc interval
Macrolides DDI
CYP3A4 inhibitor- increases levels of: warfarin, statins, theophylline, triazolam, carbamazepine, cyclosporine, sildenafil, etc.
Less interactions with azithromycin
Macrolides resistance
Low level resistance is associated with the mef gene (efflux pump)
High levels are associated with target-site modification, Domain 5 is methylated, coded by erm gene, and macrolides cant bind
Oxazolidinones
Linezolid, Tedizolid
Linezolid MOA
Inhibits early protein synthesis at 70s initiation complex
Linezolid S vs C
Static
Linezolid PD
Time-dependent
Linezolid pathogens
Narrow spectrum
Gram (+), MRSA, VRE
Linezolid main uses
Alternative to vanc in MRSA, VRE
Linezolid MRSA or pseudomonas coverage?
MRSA
Linezolid AE
GI, rashes, neuropathy
Warnings: serotonin syndrome, hematologic (weekly CBC)
Lincosamide
Clindamycin
Lincosamide MOA
Binds to 50s, inhibiting protein synthesis
Lincosamide C vs S
Static
Lincosamide PD
Time-dependent
Lincosamide pathogens
Broad spectrum
Gram +, anaerobes, pneumocystis, toxoplasma
Lincosamide main uses
Skin, soft tissue, bone infections Used for its anti-toxin properties IA anaerobes infections Acne, rosacea Toxoplasma, pneumocystis
Lincosamide MRSA/pseudomonas?
No
Lincosamide resistance
Altered target, decreased binding, efflux
Streptogramin
Quinupristin-dalfopristin (Synercid)
Streptogramin MOA
Dalfopristin alters conformation of the 50s ribosome such that affinity for quinuprostin is increased.
Streptogramin s vs c
Synergistically cidal
Streptogramin PD
Concentration-dependent
Streptogramin spectrum
Gram +, MRSA, VRE
Streptogramin MRSA/pseudomonas coverage?
MRSA
Streptogramin AE
Local vein reactions
Arthralgia
Streptogramin DDI
Inhibits 3A4 metabolism
Streptogramin resistance
Increased binding to target, enzymatic inactivation, efflux
Lefamulin MOA
Inhibits protein synthesis through interactions with A and P sites of Domain 5 of 50s subunit
Lefamulin C vs S
both
Lefamulin PD
Time-dependent
Lefamulin pathogens
Strep, staph (MRSA), atypicals
Lefamulin main uses
CAP
Lefamulin MRSA/ pseudomonas?
MRSA
Lefamulin AE
Injection site reactions, insomnia, embryo-fetal toxicity, GI, increased LFTs, QTc prolongation
Lefamulin DDI
Inhibits 3A4
Avoid quinidine, amiodarone, sotalol, procainamide
Lefamulin and food
Food decreases absorption
Aminoglycosides
Gentamicin, Tobramycin, streptomycin, amikacin
Aminoglycosides MOA
Irreversibly binds to the 30s ribosome
Aminoglycosides C vs S
Cidal
Aminoglycosides PD
Concentration dependent
Aminoglycosides pathogens
Primarily gram (-). pseudomonas Gram (+) if synergistic with cell wall agents
Aminoglycosides uses
Severe gram (-) infections (in combo) Gram (+) of synergistic with cell wall inhibitors (endocarditis) Tuberculosis (streptomycin)
Aminoglycosides MRSA/pseudomonas coverage?
Pseudomonas
Aminoglycosides AE
Nephrotoxicity, ototoxicity, neuromuscular blockade
Aminoglycosides resistance
Enzyme modification, altered 30s, efflux
Aminoglycosides PAE
LONG PAE, requires serum concentration monitoring
Tetracyclines
Tetracyclines, doxycyclines, tigecycline
Tetracyclines MOA
Binds to the 30s ribosome, blocking the formation of initiation complex
Tetracyclines C vs S
Static