Antibiotics Flashcards
MOA: Penicillins
- interfere with PBP to inhibit cell wall synthesis
Resistance: Penicillins
- beta lactamases
- altering porins
- altering PBP
- penicillin efflux pumps
Adverse Rxns: Penicillins
- hypersensitivity
- N/V/D with high doses
What antibiotic class? Methicillin Nafcillin Oxacilin Dicloxacillin
Penicillinase-Resistant Penicillins
MOA: Aminopenicillins
- increased binding affinity to PBP
- increased penetration through outer membrane of Gram negative organisms
What antibiotic class?
Ampicillin
Amoxicillin
Aminopenicillins
MOA: Antipseudomonal Penicillins
- interfere with PBP
- often combined with B-lactamase inhibitor Tazobactam
- broadest spectrum penicillin
MOA: Cephalosporins
- interfere with PBP
Resistance: Cephalosporins
- beta-lactamases
- altering porins
- altering PBP
- cephalosporin efflux pump
compare general penicillins to aminopenicillins
- aminopenicillins have better gram negative coverage, greater binding affinity to PBP, and greater penetration through outer membrane of gram negatives
- also aminopenicillins are often paired with beta lactamase inhibitor
Adverse Rxns: Cephalosporins
- type 1 hypersensitivity reaction
Organisms covered by Gen. 1 Cephalosporins
PEK
P: Proteus mirabilis
E: E. coli
K: Klebsiella
- also gram (+) cocci
Organisms covered by Gen. 2 Cephalosporins
HENS PEK H: H. influenzae E: Enterobacter N: Neisseria S: Serratia
P: Proteus mirabilis
E: E. coli
K: Klebsiella
What are Gen. 3 Cephalosporins used to treat
serious gram negative infections
What cephalosporin is the first line for meningitis
Ceftriaxone
Adverse Rxns: Ceftriaxone
- jaundice in neonates
- biliary pseudolithiasis (gallstones)
What important bacterium is covered by Gen. 4 Cephalosporins
P. aeruginosa
What important bacteria are covered by Gen. 5 Cephalosporins
MRSA
P. aeruginosa
What antibiotic class?
Piperacillin
Antipseudomonal Penicillins
What antibiotic class?
Cefazolin
Cephalexin
Gen. 1 Cephalosporins
What antibiotic class? Cefaclor Cefoxitin Cefuroxime Cefotetan Cefmetazole Cefprozil
Gen. 2 Cephalosporins
“2nd graders wear FAke FOX FUR to TEa parties”
What antibiotic class? Cefotaxime Cefdinir Ceftibuten Ceftazidime Ceftriaxone Cefpodoxie proxetil Cefditoren pivoxil
Gen. 3 Cephalosporins
What antibiotic class?
Cefepime
Gen. 4 Cephalosporins
What antibiotic class?
Ceftaroline fasamil
Ceftolozane
Gen. 5 Cephalosporins
What antibiotic class? Imipenem Meropenem Doripenem Ertapenem
Carbapenems
MOA: Carbapenems
- inhibit PBP
- can penetrate Gram negative bacteria
Resistance: Carbapenems
- carbapenemases
- gram neg bacteria shrink down porin channels so it can’t fit through
Adverse Rxns: Carbapenems
(most often with Imipenem)
- reactions at infusion site
- rash
- N/V/D
- renal failure
- seizures
What is required for use of Imipenem
combination with renal dipeptidase inhibitor (Celastin)
MOA: Monobactams
- inhibits PBP
Adverse Rxns: Monobactams
- increases serum aminotransferases
- skin rashes
Monobactams are used against what organisms
- only gram negative
- only aerobes
What antibiotic class?
Aztreonam
monobactam
MOA: glycopeptides and lipoglycopeptides
- bind D-ALA-D-ALA and inhibits PBP, preventing extension and cross linking of peptidoglycans
- lipoglycopeptides improve this binding
What antibiotic class?
Vancomycin
glycopeptides
What antibiotic class?
Telavancin
Dalbavancin
Oritavancin
Lipoglycopeptides
How must Vancomycin be administered?
IV
Adverse Rxns: Glycopeptides and Lipoglycopeptides
- infusion related reactions (hypotension, tachycardia, flushing
- Red Man Syndrome
- Nephrotoxicity
- Ototoxicity
What drug class?
Clavulanic Acid
Sulbactam
Tazobactam
Beta-lactamase inhibitors
What beta-lactamase inhibitor is often paired with Piperacillin
Tazobactam
MOA: Oxazolidinones
- protein synthesis inhibitors
- bind to P site on 50s to prevent formation of fMET tRNA complex
- bacteriostatic (except bactericidal for strep)
Resistance: Oxazolidinones
- point mutations on 23SrRNA
- methyltransferases modify ribosome
What drug class?
Linezolid
Tedizolid
Oxazolidinones
Oxazolidinones are used against what organisms?
- primarily gram (+)
- MRSA
- Vancomycin-RSA
Adverse Rxns: Oxazolidinones
1) Myelosuppression (thrombocytopenia)
2) Mitochondrial toxicity (optic neuritis, peripheral neuropathy, lactic acidosis)
3) Drug-Drug Interaction (linezolid inhibits MOA which makes it interact with SSRIs –> Serotonin Syndrome)
MOA: Macrolides and Ketolides
- inhibit protein synthesis
- binds to 50s
- bacteriostatic
What drug class? Erythromycin Azithromycin Clarithromycin Fidaxomicin
Macrolides
What drug class?
Telithromycin
ketolides
Resistance: Macrolides and Ketolides
1) active drug efflux
2) shielding of ribosome
3) degradation of antibiotic
4) 50s subunit mutations
Adverse Rxns: Macrolides and Ketolides
- N/V/D
- anorexia
- arrhythmias (QT elongation)
- cholestatic hepatitis –> jaundice
- Hypersensitivity
What drug class?
Dalfopristin
Quinupristin
Streptogramins
MOA: Streptogramins
- bind to 50s
- inhibit protein synthesis
- bactericidal when combined
Quinupristin –> inhibits elongation
Dalfopristin –> enhances Quinupristin
Streptogramins are used against what organisms?
- gram (+) cocci (resistant strep, Penicillin resistant S. pneumoniae, MRSA)
- some gram (-)
Resistance: Streptogramins
- inactivation of dalfopristin will render quinupristin inactive
- altering quinupristin’s binding site on 50s
- drug efflux
Adverse Rxns: Streptogramins
- infusion site reaction (pain, arthralgia, myalgia)
MOA: Tetracyclines and Glycylcyclines
- bind 30s, preventing aminoacyl tRNA from entering A site
- bacteriostatic
- accumulates intracellularly
What drug class? Doxycycline Tetracycline Minocycline Demeclocyline
Tetracyclines
What drug class?
Tigecycline
Glycylcyclines
Adverse Rxns: Tetracyclines and Glycylcyclines
- GI irritation (N/V/D)
- effects on bone and teeth (brown teeth in children)
- risk of C. diff
**do not give in pregnancy
Resistance: Tetracyclines and Glycylcyclines
1) decreases intracellular concentration of antibiotic
2) increased dislodging of antibiotic from target
3) enzymatically inactivated
Tetracyclines and Glycylcyclines are used against what organisms?
- mostly gram (+)
- anaerobes
MOA: Aminoglycosides
- bind to 30s
- introduce errors in protein synthesis
- bacteriocidal
What drug class? Gentamycin Neomycin Tobramycin Streptomycin Amikacin Paromomycin
Aminoglycosides
Resistance: Aminoglycosides
- anaerobes
- enzymatic inactivation that prevents binding to 30s
- decreased intracellular transport due to mutation or deletion of porins
- mutations to 30s
What are aminoglycosides often paired with?
a B-lactam to expand coverage to Gram positives
Adverse Rxns: Aminoglycosides
- nephrotoxicity
- ototoxicity (vestibular damage and auditory damage)
**do not give to pregnany women
MOA: Fluoroquinolones
- inhibit bacterial topoisomerase (DNA gyrase) and topoisomerase IV
- blocks cell division and separation of replicated chromosomal DNA
Adverse Rxns: Fluoroquinolones
- 3-17%: GI effects
- C. diff
- 1-11%: headaches/dizziness
- tendon rupture
- QT prolongation (Torsades de pointes)
Resistance: Fluoroquinolones
- mutations to quinolone binding region on DNA gyrase or topoisomerase IV
- active drug efflux
- increased shielding proteins
What drug class? Ciproflaxacin Levoflaxacin Oflaxacin Gemifloxacin Gatifloxacin Moxifloxacin
Fluoroquinolones
MOA: Sulfonamides
mimic PABA and block PABA binding todihydropterase synthase, inhibition formation of tetrahydrofolate
MOA: Trimethoprim
inhibits dihydrofolate reductase
Resistance: Sulfonamides
- bacterial overproduction of PABA
- reduced binding of sulfamethoxazole to dihydropteroate synthase
- increase mutation dihydropterase synthase
- decreased bacterial permeability
Resistance: Trimethoprim
- decreased bacterial permeability
- increased dihydrofolate reductase
- increased mutation dihydrofolate reductase
Adverse Rxns: TMP
- anemia
- leukopenia
- granulocytopenia
Adverse Rxns: SMX
- N/V
- photosensitivity
- fever
- urticaria
- Stevens-Johnson Syndrome
What drug class?
TMP-SMX
Sulfonamides and Benzylpyrimidines
MOA: Polymyxins
- act as cationic detergents to perturb the membrane of gram negatives
What drug class?
Polymyxin B
Colistin
Polymyxins
Resistance: Polymyxins
- rare
- Klebsiella and Actintobacter
- all gram positives
Adverse Rxns: Polymyxins
- systemic parenteral administration leads to nephrotoxicity with neuro effects (slurred speech, vertigo, parasthesias, apnea, weakness)
(topicals are tolerated well)