Beta Lactams Flashcards
Beta-lactams MOA
Bind to penicillin binding proteins (PBPs)
Inhibit cross-linking of peptidoglycan in the cell wall -> autolysis -> cell death
Natural Penicillin Examples
Pen G (IV) Benzathine Pen (IM) Pen V K (PO)
Natural penicillin: NO ACTIVITY
Staph
Natural Penicillin: TOC
Strepto
Clostridium perfringens
Natural Penicillin: Good for
Gram positive: (P/AP)
Natural penicillin: GN coverage
Minimal (resistance)
Maybe N. meningitidis (doesn’t pass BBB well but MIC90)
Natural Penicillin ADE
Seizures
Neutropenia
Hypersensitivity
AIN/renal tubular disease
Natural penicillin: DDI
OAT 1/3 (pretomanid, teriflunomide, fexinidazole)
Probenecid
Natural penicillin: Renal dosing adj?
Yes
PRP: Examples
Nafcillin (IV)
Oxacillin (IV)
Dicloxacillin (PO)
PRP: TOC
MSSA
PRP: NO ACTIVITY
MRSA
entero
GN
PRP: Good activity
strepto
PRP: GI ADE
Dicloxacillin
PRP: ADEs
Hepatotoxicity, increase serum transminases, neutropenia, AIN, renal tubular disease
Naf/Ox: local – inj site reactions, phlebitis
Diclo: GI upset
PRP: Nafcillin DDI
3A4 (azole, anti-epileptics, statins, transplant meds, etc.)
PRP: Dicloxacillin DDI
3A4: transplant meds, carbamazepine
2C19: fosphyenytoin/phyenytoin, omeprazole
PRP: Renal dosing adj?
NO
PRP: Nafcillin excretion
Feces
PRP: Oxacillin excretion
Bile/urine
PRP: Dicloxacillin excretion
Feces/urine
Amino P: NO ACTIVITY
Staph aureus
Amino P: TOC
Entero
Listeria
Amino P: same as penicillin against ___ but broader
Strepto
Amino P: Good
P/AP
Amino P: GN
Limited E.coli and P. mirabilis (younger pt w/o abx exposure)
H. influenzae if beta-lactamse neg (otitis media or sinusitis)
Amino P: ADE
Derm - erythema multiforme, exfoliative dermatitis, skin rash, urticaria
Neutropenia, leukopenia, anemia, eosinophilia
AIN (rare)
Amox: GI Upset
Amino P: DDI
NONE
Amino P: Renal adj dosing?
YES
Pen+B: Examples
Ampicillin/sulbactam (IV)
Amoxicillin/clavulanate (PO) – Augmentin!
Piperacillin/tazobactam (IV)
Pen+B: Added activity against ___
MSSA
Pen+B: NO ACTIVITY
MRSA
Pen+B: Same as ampicillin or penicillin for ___ and ___
Entero
Strepto
Pen+B: TOC
Oropharyngeal infections (GPA: P/AP) GNA: BPF
Amp/sulb + amox/clav: CAP (H. influenza, M. catarrhalis) // Animal bites (Pasteurella multocida, capnocytophaga spp.)
Piper/tazo: increased KEP coverage and P. aeruginosa
Pen+B: DDI
Derm: Skin rash, urticaria, pruritus
Pancytopenia, thrombocytopenia
Increased LFTs, hepatitis
AIN
Amox/clav: GI upset
Pen+B: DDI
Piper/tazo + vanco increases nephrotoxicity risk
1st Gen Cephalosporin: Examples
Cefazolin (IV)
Cephalexin (PO)
Cefadroxil (PO)
1st Gen Cepha: Cefazolin TOC for
MSSA
1st Gen Cephalo: NO ACTIVITY
MRSA
Entero
1st Gen Cephalo: Good coverage
All Strepto
Most cover peptostrepto
GN: KEP
GNA: limited BPF
1st Gen Cephalo: ADE
Diarrhea
LFT elevation
Hypersensitivity (< penicillin)
1st Gen Cephalo: DDI
Warfarin
Probenecid
2nd Gen Cephalosporin: Examples
Cefuroxime (IV/PO) Cefprozil (PO) Cefaclor (PO) Cefotetan (IV) * Cefoxitin (IV) *
*cephamycins
Cephamycin examples
Cefotetan
Cefoxitin
2nd Gen Cephalo: NO ACTIVITY
MRSA
Entero
GN: Non fermenters (PAS)
2nd Gen Cephalo: Good coverage
All strepto
GPA: Peptrostrepto
Increased KEP
CAP bacteria: H influenza, M. catarrhalis
Best anaerobe activity: cephamycins
Of the 2nd gen cephalosporins, which drugs had best anaerobe activity
cephamycins: cefotetan and cefoxitine
3rd Gen Cephalosporins: Examples
Ceftriaxone (IV) Cefotaxime (IV) Ceftazidime (IV) Cefdinir (PO) Cefditoren (PO) Cefixime (PO) Cefpodoxime (PO) Ceftibuten (PO)
3rd and 4th gen cephalo are ___ active than 1st and 2nd gen for GP
LESS
3rd and 4th gen cephalo are ___ active than 1st and 2nd gen for GN
MORE
3rd Gen Cephalo: _____ is TOC against invasive strep
Ceftriazone
3rd Gen: Limited and NO ACTIVITY
Limited MSSA
NO MRSA
NO entero (except ceftriaxone + ampicillin for E. faecalis endocarditis)
GN: non-fermenters (PAS) (except ceftazidime) Limited GNA (BPF)
3rd Gen: ____ is TOC for KEP
Ceftriaxone
3rd Gen: ADE
Diarrhea
OBSTRUCTIVE BILIARY TOXICITY
LFT elevations
Hypersensitivity (less than penicillins)
3rd Gen: DDI
Warfarin
Probenecid
3rd Gen: Ceftriazone elimination
Bile
3rd Gen: Ceftriaxone dosing freq
QD or BID
3rd Gen: ___ undergoes deacetylation in liver
Cefotaxime
4th gen: Examples
Cefepime
4th gen is ___ active than 1st and 2nd gen
LESS
4th gen: Limited and NO ACTIVITY
Limited MSSA
NO MRSA
NO entero
Limited GNA (BPF)
T/F: Cefepime has broader activity against all GN
True
4th gen: TOC
P. aeruginosa
4th Gen: Good for
All strep
4th gen: ADE:
Diarrhea
LFT elevation
ENCEPHALOPATHY, SEIZURES
Hypersensitivity (
4th gen: DDI
Warfarin
Probenecid
Which generation has greatest GP coverage?
5th gen
5th Gen: Examples
Ceftaroline
5th Gen: Limited NO ACTIVITY
NO Entero
NO GN: Non-fermenters (PAS)
Limited GNA (BPF)
5th gen: Great for
MSSA
MRSA
All strepto
Most cover peptostrepto
KEP
CAP germs: H. influ, M. catarrhalis
All gens EXCEPT which gen has NO activity for MRSA and entero // Good activity for strepto
5th Gen (ceftaroline)
Which gens have limited activity for GNA (BPF)
All gens
Which gens have NO activity for GN non-fermenters (PAS)
2nd, 3rd, 5th
Which gens have KEP coverage
1st, 2nd, 3rd, 5th
Which gen can cause encephalopathy and seizures
Gen 4
Which gen can cause obstructive biliary toxicity?
Gen 3
What are common ADEs for cephalosporins?
Diarrhea
LFT elevation
Hypersensitivity (
What are common DDIs for all cephalosporins
Warfarin
Probenecid
Adv. gen GP activity is similar to __ and__ gen
3rd and 4th
Carbapenem Examples
Ertepenem
Imipenem
Meropenem
Doripenem (D/C**)
Carbapenems: Seizure risk order (increase > decrease)
Imi > Mero > erta
Carbapenem NO ACTIVITY
MRSA
GN: Non-fermenters (PAS) – except imi and mero active against P. aeruginosa
Carbapenems: Good activity
MSSA
Strepto
KEP (including ESBL-producing strains)
Anerobes
Carbapenem: ADE
N/V/D
Headache
Seizure (imi>mero>erta)
Hypersensitivity - maculopapular rash
Carbapenem: DDI
Valproic acid
Probenecid
Carbapenems: Renal adj dosing?
YES
Carba+B: Examples
Meropenem-vaborbactam
Imipenem-relebactam
Carba+B: NO Activity
MRSA
Limited entero
stenotrophomonas maltophilia (from PAS)
Carba+B: ADE
N/V/D
Headache
Hypersensitivity - maculopapular rash
Carba+B: DDI
Valproic acid
Probenecid
Carba + P: Renal adj dosing?
YES
Monobactam example
Aztreonam
Aztreonam MOA
Same as beta-lactam but specifically high affinity for PBP3
Aztreonam ONLY ___ activity
GN
Aztreonam Coverage
ONLY GN
KEP (not for ESBL or KPC but active against MBLs)
TOC: P. aeruginosa (if B-L intolerant or allergic)
No activity other non-fermenters
Aztreonam ADE
N/V/D
Rash
Aztreonam: DDI
NONE
Cell function: Macrophage/monocyte
Antigen presenting cell
Surveillance of antigens
Cell function: Neutrophils
Defense against BACTERIA and FUNGUS
Cell function: Eosinophils
Defense against PARASITES
Response against allergic rxn
Cell function: Basophils
Allergic response
Cell function: B-lymphocytes
Antibody production
Antigen presenting cell
Cell function: T-lymphocyte
Cellular immunity against VIRUS and TUMORS
Regulation of immune system
Differential: WBC breaks down into (2)
Granulocytes
Agranulocytes
Differential: Granulocytes break down into (1) (3)
Polymorphonuclear granulocytes (PMNs) break down into
- neutrophils
- basophils
- eosinophils
Differential: Agranulocytes break down into (2)
Lymphocytes (B-lymph, T-lymph)
Monocytes (macrophages)