antibiotics 1 Flashcards
provides structural integrity of the cell wall
Peptidoglycan (PG) layer
found in the periplasmic space function to crosslink the peptidoglycan chains
Transpeptidase Enzymes
what are the 4 bacterial targets
cell membrane
cell wall
NA synthesis
protein synthesis
4 abx that affect beta lactams
- penicillins
- cephalosporins
- carbapenems
- monobactams
PCN-G
natural PCN
PCN-V
natural PCN
methicillin
anti-staphylococcal PCN
dicloxacillin
anti-staphylococcal PCN
nafcillin
anti-staphylococcal PCN
oxacillin
anti-staphylococcal PCN
amoxicillin
aminopenicillin
ampicillin
aminopenicillin
piperacillin/tazobactam
Extended-spectrum (PCN’s + BLI combo)
amoxicillin/clavulanate
Extended-spectrum (PCN’s + BLI combo)
ampicillin/sulbactam
Extended-spectrum (PCN’s + BLI combo)
aztreonam
monobactam
imipenem
carbapenems
meropenem
carbapenems
ertapenem
carbapenems
doripenem
carbapenems
MOA of beta-lactam Abx
Inhibit Bacterial Cell Wall Synthesis
1. Drug binds to transpeptidase (aka Penicillin-Binding Proteins [PBP’s])
2. This inhibits bacterial peptidoglycan synthesis preventing bacterial replication (Bacteriostatic)
3. Binding to PBP activates bacterial autolytic enzymes that cause cell wall lysis (Bactericidal)
5 methods of resistance for beta-lactams
- Beta-Lactamase inactivates drug
- β-Lactamases are a large family of hydrolases that catalyze the hydrolysis of the amide bond in the β-lactam ring of penicillins and cephalosporins. - Increased number of beta-lactamases
- Decreased PBP binding affinity for drug - PCP mutation (“MRSA”)
- Diminished cell wall permeability with a loss of porins - (Gram -)
- Development of efflux pump
what must we do about abx resistances
- We MUST be careful in antibiotic selection and use
- We MUST educate patients on completion of antibiotic
spectrum of natural PCN
- g+
- Streptococcus pneumoniae
- some staphylococcus
- bacillus anthracis
- anaerobes (Clostridium perfringens) - g-
- Neisseria meningitides - spirochetes (Treponema pallidum)
natural PCN is first line treatment for ?
- Strep Throat
- Group A Beta-Hemolytic Streptococcus - Syphilis
- Treponema pallidum
cellulitis, meningitis
pros and cons of natural PCN
- Cons
1. Susceptible to hydrolysis by beta lactamase
2. Resistance increasing - Pros
1. Cheap
2. Relatively safe
susceptibility/indications to use antistaphylococcal PCN
- Susceptible to B-lactamase
- Not effective against MRSA infections - Only indicated in the treatment of skin and soft tissue staphylococcal infections**
- Staph aureus and Staph epidermidis
Susceptibility/Indications for aminopenicillins
Same as natural PCN, with better g- coverage
aminoPCN first line treatment
(Amoxicillin)
1. Otitis media
- Haemophilus influenzae
- Streptococcus pneumoniae
- Moraxella catarrhalis
2. Prophylaxis for endocarditis
using aminoPCN alone makes pts more susceptible to ____. combo forms with ____ available
beta lactamase
BLi
2 advantages of aminoPCN over natural PCN
- higher oral absorption = less frequent dosing
- better g- penetration thru cell wall porins = superior g- coverage
amoxicillin/clavulanic acid
PCN/BLi
augmentin
ampicillin/sulbactam
PCN/BLi
unasyn
spectrum of PCN/BLi
same as amoxicillin but better staph coverage
(better g-, pseudomonas, anaerobes)
first line treatment for sinusitis, pneumonia/COPD exacerbations
PCN/BLi (augmentin)
- s. pneumo
- h. flu
- s. aureus
often reserved for more severe or refractory infections
piperacillin/tazobactam
extended spectrum PCN - antipseudomonal PCN
spectrum of extended spectrum penicillins
same as PCN PLUS increased g- including
- pseudomonas*
- proteus*
piperacillin = pseudomonas
indications for antipseudomonal
severe infections
cephalexin
1st gen cephalo
cefazolin
1st gen cephalo
cefadroxil
1st gen cephalo
cefuroxime
2nd gen cephalo
cefoxitin
2nd gen cephalo
cefotetan
2nd gen cephalo
cefaclor
2nd gen cephlo
cefprozil
2nd gen cephalo
ceftriaxone
3rd gen cephalo
cefdinir
3rd gen cephalo
cefixime
3rd gen cephalo
ceftaroline
5th gen cephalo
greater cephalo generation = ? coverage
lower cephalo generation = ? coverage
better g-
better g+
which abx is safe in pregnancy for simple UTI/cystitis
cephalexin
what beta lactam has indications for surgicial prophylaxis and serious MSSA infections
cefazolin (1st gen)
what cephalos have better g- that is commonly used as surgical prophylaxis for vaginal and colorectal procedures?
cefoxitin/cefotetan (2nd)
what abx are often used for 2nd line pharyngitis, sinusitis, OM, upper and lower rsp tract infections
cefuroxime, cefaclor, cefprozil (2nd gen)
what abx is first line treatment for Neisseria gonorrhoeae
ceftriaxone
indications for ceftriaxone (4)
- N. gonorrhoeae*
- pneumococcal coverage*
- abd surgical prophylaxis
- meningitis* - can cross BBB
what is the second line treatment for upper and lower rsp tract infections (2)
3rd gen cephalo - cefdinir, cefixime
indications for 4th gen cephalo
cefepime - severe infections, meningitis - penetrates CSF very well
pseudomonas*
what is the only beta lactam with MRSA and VRE coverage
5th gen cephalo - ceftaroline
spectrum of monobactams
g- only
pseudomonas
NO G+ OR ANAEROBES
Indications for monobactams
severe infections:
- UTI
- bacteremia/sepsis
- inhalation* - CF, rsp infections
imipenem/cilastatin
carbapenems
what is the importance of adding cilastatin to imipenem
prevents inactivation in renal tubule
spectrum of carbapenems
very broad
- g+, g-, anaerobes
- pseudomonas
- susceptible to beta lactamase - not indicated for MRSA
indications for carbapenems
severe infections
- UTI
- meningitis
- chronic DM wounds
- osteomyelitis
- peritonitis/intra-abd infections
what is the most common SE of beta-lactams
GI - N/V/D
more likely with amoxicillin/clavulanate and higher gen cephalo
may need dosage adjustment for beta lactams with…
renal impairment
drug interactions with beta lactams
minimal but can decrease effectiveness of oral contraceptives
what beta lactams cover pseudomonas
- piperacillin/tazobactam (ESP)
- Ceftazidime (3rd)
- cefepime (4th)
- aztreonam (monobactam)
- meropenem (carbepenem)
- doripenem (carbepenem)
- imipenem (Carbapenem)
what carbapenem does not cover pseudomonas
ertapenem
aztreonam
monobactam
what beta lactams have anaerobic coverage
- PCN (g+)
- AminoPCN (g+)
- PCN/BLi
- cefotetan (2nd)
- cefoxitin (2nd)
- carbapenems
cefepime
4th cephalo