Antibiotics Flashcards
Mechanism of Action
Penicillins
beta-lactam antibiotic
binds to penicillin binding proteins:
- Inhibit transpeptidase cell wall cross link
- Activation autolysin
weakens the cell wall
results in bacterial cell lysis
SE of Penicillins
- CNS toxicity (hallucinations, delusions, seizures)
Renal dose adjustment required - Anaphylaxis 7/100 people
- GI upset
- Blood dyscaria
- phlebitis if IV
Penicillins and pregnancy
safest antibiotic
PBPs only exist in bacteria
Safe in pregnancy, infancy, childhood, old age
Amoxicillin safe in breast feeding
First line treatment for pregnancy UTIs
Penicillin G and V Coverage
Gram positive bacteria
Anaerobic Spirochettes (Treponem pallidum - syphillus)
Penicillin is used to treat…
Meningitis - streptococcus pneumoniae
Group A strep infections (GAS)
Syphillus
MOA and SE of Cephalosporins
MOA:
beta-lactam antibiotic
weaken cell wall
bind PBP
*same as penicillins
- CNS toxicity (renal dose adjustment required)
- Disulfram reaction (acetaldehyde build up if you drink)
- C. diff infections (during and post)
- Bleeding (inhibits Vitamin K coagulation factor synthesis)
Which Cephalosporins cross the BBB
Third generation
- Cefixime, Cefotaxime, Ceftazidime, Ceftriaxone
Fourth Generation
- Cefepime
Fifth Generation (USA only)
- Ceftaroline
Which Cephalosporins cover pseudomonas infections?
Third generation (ceftazidime)
Fourth generation
(cefepime)
Which cephalosporins cover MRSA infections
Fifth generation
Ceftaroline
First generation Cephalosporins
Cephalexin
Cefazolin
Cefadroxil
*cross reactivity with penicillin 1%
contraindicated with penicillin anaphylaxis
Second generation cephalosporins
Cefaclor
cefuroxime
cefoxitin
cefprozil
cefotetan
Third generation cephalosporins
Cefotaxime
Ceftriaxone
ceftazidime
Cefixime
Fourth and fifth generation cephalosporins
Cefepime
ceftaroline
Penicillins
Penicillin G
Penicillin V
Cloxicillin
Amoxicillin/Clavulanate
Ampicillin/Sulbactam
Pipperacillin/tazobactam
Carbapenems MOA and route
beta-lactam antibiotic
bind to PBPs 1. transpeptidase inhibitor 2. autolysin disinhibitor
Imipenem
Meropenem
Ertapenem
*IV Only
Prescribing considerations and contraindications of carbapenems
IV only
gram positive, negative, pseudomonas infections - broad spectrum, empric
Do not give alone to treat pseudomonas to avoid resistance (prescribe with pipperacillin/tazobactam and/or aminoglycosides)
Contraindicated with VPA (seizures)
Renal dose adjustment
1% cross reactivity with penicillins
Super infections
Carbapenem SE
N/V/D
superinfections
hypersensitivity
cross reactivity with penicillins 1%
seizures with VPA
Mechanism of action carbapenems
- inhibition transpeptidase
- activation autolysin
Disrupt cell wall synthesis resulting in bacterial lysis
Only active against actively growing and dividing bacteria
Resistant against beta-lactamases - do not need to prescribe sulbactam, clavulanate, or tazobactam
Mechanism of action cephalosporins
- Inhibition transpeptidase
- Activation autolysin
Disrupt cell wall synthesis resulting in lysis of bacteria
*beta-lactam antibiotic
same as penicillins and carbapenems
3rd and 4th resistant against beta lactamases, BBB penetration, and pseudomonas coverage
5th generation MRSA coverage
Cephalosporins SE, and pregnancy
SE:
N/V/D, c.diff
disulfram reaction
neuerotoxicity
cross reaction with penicillins 1% first generaitons
bleeding risk
safe in pregnancy
safe in breastfeeding
3rd generations used to treat infants
dose reduction in kidney disease
Vancomycin
Mechanism of Action
Disrupts cell wall synthesis by binding to cell wall precursors - peptidoglycans
Results in cell lysis
Not absorbed systemically through PO administration - too big
Vancomycin
SE
Ototoxic - high pitch, low pitch, blance
Nephrotoxic - casts, proteinuria
Blood trough level (low trough)
TDM required
Monitor BUN, creatinine clearance
Pathophysiology of
C. Difficile
Antibiotics kill microbiome
Overgrowth of bad bacteria such as C. Diff
Toxin A and B produced and damage colon
Inflammation, pus, watery diarrhea
Gram positive, spore forming bacteria
First line treatment: Metronidazole IV and Vancomycin PO
Vancomycin and Pregnancy
PO vancomycin does not get absorbed systemically (too big, hydrophilic), safe in pregnancy and breast feeding
Vancomycin Coverage
Gram positive bacteria and MRSA
MRSA (gram positive cocci in clusters) - methicillin resistance, PBP different shape
C. difficile (gram positive bacilli)
Fosfomycin Coverage
Gram positive,
Gram negative,
Pseudomonas
*Cannot be used to treat pyelonephritis/renal infections (systemic) - too big to be absorbed
Fosfomycin mechanism of action
Prevents production of the building blocks of the cell wall peptidoglycan layer
Disrupts cell wall synthesis
Penicillin and Cephalosporin Drug interactions
Oral contraceptives
Probenicid (increases level)
Synergistic with aminoglycosides
Antibiotics that inhibit 50S Ribosome Subunit
Macrolides (Azithromycin, Erythromycin, Clarithromycin)
Licosamides (Clindamycin, linomycin)
Linezolid
Macrolide SE
- Prolonged QT interval
- Ototoxic
- Diarrhea (Motilin receptors) and metallic taste in mouth
- Elevated LFTs (biliary clearance)
- Renal dose adjustment needed
Macrolide Drug interactions
Inhibition CYP450
Synergistic with beta-lactam antibiotics
Macrolide coverage
Atypical infections (GERD, CAP, STIs)
Gram positive, gram negative (no pseudomonas coverage)
Erythromycin Drug Interactions
CYP3A4 metabolism
Cardiac death increases 6x when prescribed with CYP3A4 inhibitors
- CCB
- Azoles
- HIV protease inhibitors
- Anti-depressants
Inhibits CYP450 Enzyme, increasing level of
- warfarin
- theophylline
- carbamazepine