B-Lactams and more! Flashcards
B-lactams consist of Penicillin, Lactamase inhibitors, cephalosporins and Cephamycins, Carbapenems, Monobactams
What is there MOA?
Cross link is usually formed by transpeptidase but B-lactams inhibit this
Also known as PBP
B-lactams are _____ dependent and they are not active against?
Time dependent, not active against MRSA
How can bacteria be resistant to B-lactams and their derivatives? Theres 4
- Inactivation by amidases, B-lactamase, or carbapenamases
- Modification of PBP
- Imparied drug penetration to target PBPs
- Anitbiotic Efflux
What are the B-lactam inhibitors?
What do they do?
Clavulanic Acid, Sulbactam, Tazobactam
Protected hydrolyzed penicillins from inactivation. Extend Spectrum of the penicillin to strains that would otherwise be inactive.
Cephalosporin and Cephamycin what is their purpose?
What are some adverse rxns?
Increase gram negative coverage
Allergy, methylthiotetrazole containing cephs can cause bleeding and disulfiram like rxns
Carbapenems are not active against?
Impenem is administered with?
Good choice for?
- Klebsiella pneumoniae
- And carbapenemase producing strains
- administered with a renal dehydropeptidase, cilastatin
- Good for nosocomial infections and B-lactamase producing GN strains
Monobactams?
Limited to?
No activity againsts? _____ and _____
- Aztreonam
- Limited to aerobic GN rods (including P aeruginosa)
- No activity against GP, or anaerobes
Vancomycin is only active against?
Binds to d-___d-___
Drug of choice for?
Can cause?
- Gram positive
- Binds to d-Ala-d-Ala preventing elongation
- Drug of choice for MRSA
- Time dependent killing
- Redman syndrome
Cyclic Lipopeptide?
Daptomycin
What does daptomycin do?
Effects against? can cause?
- Binds to the cell wall of gram positive causing death
- Effective againsts MRSA, VRE (Vanco-resistant)
- Allergic pneumonitis
Fosfomycin?
MOA?
Used to treat?
Same as?
- Inhibits the bacterial wall synthesis by inhibiting the synthesis of the cell wall building blocks
- Primarily used for uncomplicated lower UTI
- Same as Nitrofurantoin
Tetracyclines?
Tetra, Doxy, Tige all cycline
Tetracyclines are good for treating?
Resistance? 3 ways
- Rickettsia Mycoplasma, Chlamydia, Plasmodium
- Impaired influx or increased efflux
- Productin of proteins that interfere with tetracylcine
- Enzymatic inactivation
Macrolides?
Clari, Azithro, Erythro
Macrolides are used for?
Check for interactions with?
Respiratory infection, Avium, Chlamydia
P450 interaction
Macrolide resistance? 3 ways
- Impaired influx or increase efflux
- Production of esterases that hydrolyze macrolide lincosamide and streptogramin, MLS type B
- Modification of the ribosomal binding site by mutation or by macrolide inducible or constitutive methylase
Lincosamides?
Derivative of the?
Good for?
what type of bacteria
Resistance?
Clindamycin
- Of Lincomycin
- skin and soft tissue infections cause by strep and staph
- Same as macrolides
- Impaired influx or increase efflux
Production of esterases that hydrolyze macrolide lincosamide and streptogramin, MLS type B
Modification of the ribosomal binding site by mutation or by macrolide inducible or constitutive methylase
Streptogramins?
Rapidly ____ for most susceptible organisms ____ , _____ and ____ but not?
Resistance?
- Quinupristin-dalfopristin in 30:70
- bactericidal for MSSA, MRSA, and VRE
- but not Entero Faecalis
- slow with Entero Faesium
- Same as macrolide
Oxazolidinones?
MOA
GOOD for?
AE?
Resistnace?
Linezolid
- Inhibits proteins synth by preventing formation of the ribosome complex
- Good for MSSA, MRSA, VRE entero faecium
- Hematologic AE: Thrombocytopenia myelosuppression
- Different from other protein synth inhibitors
Amino glycosides. 3 main things
- Irreversible inhbitors of protein synthesis, Block the initiation complex
- Miscoding of amino acids
- Block of translocation on mRNA
Aminoglycosides?
______ dependent killing?
_____ killing with cell wall ___ in endocarditis
Good for?
AE?
Amikacin, Gentamicin, Tobramycin
- Cocentration dependent killing
- Synergisitc with cell wall inhibitors
- Nephro and ototoxicity
First, Second, Third, Fourth generation cephalosporins gone over in class?
- Cephalexin, Cefazolin
- Cefprozil, Cefuroxime
- Ceftriaxone, Cefotaxime
- Cefepime
What generation cephalosporin/cephamycin can cross the BBB?
3rd and 4th
- Ceftriaxone, Cefotaxime
- Cefepime