Antibiotics Flashcards
What are the beta lactam classes?
Penicillins
Cephalosporins
Carbapenems
Monobactams
What is the beta lactam MOA?
Beta lactam ring binds to transpeptidase which inhibits bacterial wall synthesis. They can also bind to transpeptidase and cause bacterial autolytic enzymes to be relases and cause cell lysis.
How do bacteria fight against beta lactams?
Beta lactamases
Reduce binding affinity to transpeptidase/PBP
Over production of PBP
Loss of membrane porins
Expression of efflux pumps
What bacteria can natural penicillins be used against?
Gram + (s pneumoniae, staph, b anthrax, anaerobes)
Gram - (n meningitides)
Spirochetes (treponema pallidum/syphylis)
NO MRSA
What is natural penicillin a first line treatment for?
Strep Throat -GABHS
Syphilis
Cellulitis
Meningitis
What are the natural penicillins?
PCN G
PCN V
What are the antistaphylococcal PCNs?
Dicloxacillin
Nafcillin
Oxacillin
When can antistaphylococcal PCNs be used?
Only skin and soft tissue infections
s aureus and s epidermis
NO MRSA coverage
What are the aminopenicillins?
Amoxicillin and ampicillin
What are first line uses for aminopenicillins?
Otitis media (amoxicillin)
Endocarditis prophylaxis
What are the most common causes of otitis media?
S pneumoniae
M catarrhailis
H influenza
What are the advantages of an aminopenicillin over a natural penicillin?
Better oral absorption, longer half life, better gram negative penetration
What are the PCN/Beta lactamase inhibitor drugs?
Amoxicillin/Clavulanic acid (amoxicillin)
Ampicillin/sulbactam (Unasyn)
What does the addition of the BLI do to the susceptibility profile of a PCN/BLI?
Better staph coverage
Overcomes BL resistance
Extends spectrum of activity
What are the first line uses for PCN/BLI?
Sinusitis, PNA, COPD exacerbations
S pneumo, H flu, S aureus
Why not just use a PCN/BLI on everyone?
Increased cost
more GI effects
More severe/refractory infections only
What are the extended spectrum penicillins/antipseudomonal penicillins?
Piperacillin/tazobactam (Zosyn)
What does the extended spectrum penicillins cover that other PCNs do not?
Pseudomonas and proteus
When do you chose a extended spectrum penicillin?
UTI
Peritonitis
Skin/soft tissue
Lower respiratory tract
Septicemia
What is the mechanism of action for cephalosporins?
Beta lactam ring binds to transpeptidase which inhibits bacterial wall synthesis. They can also bind to transpeptidase and cause bacterial autolytic enzymes to be released and cause cell lysis.
What is the difference between cephalosporin generations?
Increasing generations increases Gram - coverage at the cost of gram + coverage
What are the 1st generation cephalosporins?
cephalexin (Keflex)
cefazolin (Ancef)
cefadroxil (Duricef, Ultracef
What bacteria do you use Keflex against?
Staph, strep, E coli
What are common indications for Keflex?
Skin infections
Impetigo
Pharyngitis/otitis media
Cystitis (esp pregnancy)
What are common indications for Ancef (cefazolin)?
Surgical prophylaxis
Serious MSSA infections (endocarditis, PNA, UTI)
(cause IM/IV only)
What are common indications for cefadroxil (Duricef, Ultracef)
Pharyngitis/tonsillitis
Advantage is that it is taken BID
What are the 2nd generation cephalosporins?
Cefuroxime
Cefoxitin
Cefotetan
Cefaclor
Cefprozil
What are the indications for cefoxitin/cefotetan?
surgical prophylaxis for dirty procedures
What are the indications for cefuroxime/cefaclor/cefprozil?
2nd line for pharyngitis, sinusitis, OM, upper and lower respiratory tract infections
What are the 3rd generation cephalosporins?
Ceftriaxone (Rocephin)
Cefdinir (Omnicef)
Cefixime (Suprax)
What are the indications for ceftriaxone (Rocephin)?
1st line for Neisseria gonorrhoeae
Good for pneumococcals
Open abdominal prophylaxis
Meningitis
PID
What are the indications for cefdinir (Omnicef) and Cefixime (Suprax)?
2nd line for upper and lower respiratory infections
Skin and soft tissue infections
What is the 4th generation cephalosporin?
Cefepime (Macipime)
What is the spectrum of cefepime?
Gram +, gram -, and pseudomonas
When do you use cefepime?
Severe infections
Meningitis (bc penetrates CSF)
SAVE THIS DRUG
What is the 5th generation cephalosporin?
Cetaroline
What is the spectrum of coverage for ceftaroline?
Gram +
MRSA
VRE
Which generations of cephalosporins penetrate the CNS?
3 and 4 do well
5 does a little
What is the monobactam?
Aztreonam (Azactam)
What generation cephalosporin are monobactams closest to?
3rd/4th generation
What is the susceptibility of aztreonam?
Gram -
Pseudomonas
No gram + or anaerobes
When do you use aztreonam?
Severe UTIs (E coli)
Bacteremia/Sepsis
Inhalation (for CF respiratory infections)
What are the carbapenems?
Imipenem/cilastatin
Meropenem
Ertapenem
Doripenem
What is the susceptibility of carbapenems?
Very broad spectrum
Gram +
Gram -
Anaerobes
Pseudomonas
NO MRSA
When to use a carbapenem?
Severe infections only
UTI
Meningitis
Peritonitis/intra abd infections
Resistant wounds (chronic diabetic)
Osteomylitis
What are the common side effects of beta lactams?
GI (N/V/D)
Vaginal candidiasis
What are adverse events for beta lactams?
Hypersensitivity
C dif
Nephritis
Anemia, thrombocytopenia
CNS toxicity
How many people claim to be allergic to PCNs? How many are actually allergic?
10%, <1%
How are beta lactams metabolized? Excreted?
hepatic metabolism and renal secretion
What monitoring should you do for beta lactams?
CBC with prolonged treatment for neutopenia
Kidney function for prolonged treatment
What pregnancy category are beta lactams?
B
What are the drug interactions of beta-lactams?
Decrease the effectiveness of oral contraceptives
What drug is a glycopeptide?
Vancomycin
What is the MOA of vancomycin?
Binds to D-ala D-ala in the peptidoglycan preventing the formation of peptidoglycan and phospholipids, this weakens the cell wall and inhibits replication
How can bacteria be resistant to vancomycin?
Bacteria alter the binding site to D-ala D-lac so vanc cannot bind. Seen in VRE.
What is the spectrum of vancomycin?
Gram + cocci and bacilli
Specifically MRSA and C diff
What are the indications for vancomycin?
MRSA
Severe C dif
How is vanc metabolized and excreted?
Not metabolized but is renally excreted, must adjust for renal impairment
What is the pregnancy category for vancomycin?
B for oral and C for IV
Must do benefit risk assessment
What does vancomycin dosing rely on?
Body weight and CrCl,
Has narrow therapeutic window that needs to be monitored via trough levels or AUC (MRSA) 30 minutes before and 1-2h after each dose
When is steady state of vanc reached?
4th dose in normal renal concentration
What are the adverse effects of vancomycin?
Red man syndrome
Nephrotoxicity
Ototoxicity
What drugs are aminoglycosides?
Gentamicin
Tobramycin
Amikacin
Streptomycin
What is the MOA of aminoglycosides?
Bind to the 30s subunit which inhibits bacterial protein synthesis which is bacteriostatic. They suppress bacterial growth for a little after stopping ABx.
How do aminoglycosides gain resistance?
Chromosomal mutation of 30s
Enzymatic destruction of ABx
Lack of permeability through cell wall
Efflux pumps
What is the spectrum of aminoglycosides?
Gram -
Mycobacterium tuberculosis (Atypical)
NO Gram +
What are the BBW for aminoglycosides?
Ototoxicity
Nephrotoxicity
Neuromuscular paralysis
Which aminoglycoside is topical?
Neomycin
Which aminoglycoside is a ophthalmic drop?
Tobramycin
What are aminoglycosides most commonly paired with?
A PCN such as ampicillin + Gentamycin to make a broad spectrum therapy
What pregnancy category are aminoglycosides?
D for do not use
What is dosing of aminoglycosides based off of?
Weight and renal function, monitor peak and trough levels
What monitoring needs to be done with aminoglycosides?
BUN/Cr
Audiometry for long term, high doses
What drugs are tetracyclines?
Tetracycline
Doxycycline
Minocycline
What is the MOA of tetracycline?
Bind 30S ribosomal subunit and block tRNA binding (bateriostatic)
How to bacteria resist tetracyclines?
Efflux pumps
Enzyme deactivation
What is the spectrum of activity of tetracyclines?
Gram +
Gram -
MRSA
Atypicals (Mycoplasma, Rickettsiae, Chlamydiae, Spirochetes)
What are the first line indications for tetracyclines?
Lyme Disease
Rocky Mountain Spotted Fever
Cholera
Acne
Chlamydia
CAP
What are the contraindications for tetracyclines?
Children <8-9 years old, <13 is not preferred
Pregnancy and nursing
What is the metabolism of tetracyclines?
Metabolized in liver and excreted via urine and bile
What should tetracycline not be taken with?
TUMS/antacids
What are the adverse effects of tetracyclines?
GI distress
Hepatotoxicity
Photosensitivity
Vertigo
Candida infections
C diff
What drugs are macrolides?
Azithromycin (Zithromax)
Erythromycin
Clarithromycin
What is the MOA of macrolides?
Inhibits protein synthesis and translocation needed to replicate by binding to the 50S subunit
How do macrolides gain resistance?
50s subunit target modification
Efflux pumps
Degradation enzymes
What is the spectrum of activity of macrolides?
Gram +
Gram -
Atypicals
What are first line indications for macrolides?
CAP
Chlamydia
Legionella
Diphtheria
COPD
(2nd line OM, pharyngitis)
Can you use z-pack for sinusitis?
No. Use augmentin
Which has broader coverage of the macrolides?
azithromycin (also the only IV one)
What is the metabolism and excretion of macrolides?
Metabolized by liver, eliminated in bile, caution with liver impairment
What are the adverse effects of macrolides?
GI, N/D and C diff
Hepatotoxicity
Prolonged QT interval
Ototoxicity
What pregnancy category are macrolides?
Preg B
What is the MOA of clindamycin?
Same as macrolides, Inhibits protein synthesis and translocation needed to replicate by binding to the 50S subunit
What is the spectrum of activity for clindamycin?
Gram +
MRSA (some strains)
Anaerobes
What are indications for clindamycin?
Oral abscesses
Endocarditis prophylaxis
Bacterial Vaginosis
MRSA skin/soft tissue infections
What are the side effects of clindamycin?
Diarrhea, nausea
skin rashes
What is the BBW for clindamycin?
C diff
What pregnancy category is clindamycin?
B
What drugs are quinolones?
Ciprofloxacin
Levofloxacin
Moxifloxacin
What is the MOA of quinolones?
Inhibition of DNA gyrase and topoisomerase causes rapid bactericidal activity
How do bacteria resist quinolones?
Mutation in chromosomal genes of gyrase and topoisomerase
Efflux pump
Decreased cell wall permeability
What is the spectrum of activity of quinolones?
Gram - > gram +
Moxifloxacin also has anaerobic
When is cipro used vs Levo and moxi?
Cipro is belly button down
Levo/Moxi are belly button up
What are the first line indications for quinolones?
Otitis external (C/L)
Opthalmic infections (C/L)
Pyelonephritis (C)
Prostatitis (C)
Traveller’s diarrhea (C)
Anthrax (C)
URI/PNA with comorbidities (L/M)
What is the metabolism of quinolones?
Liver metabolism and urine/feces excretion
What are the contraindications for quinolones?
Prolonged QT/arrhythmias
Myasthenia Gravis
Can you use quinolones in kids?
Yes if necessary but not first line
What is the pregnancy rating of quinolones?
C
What is the BBW for quinolones?
Tendonitis/tendon rupture
What are the adverse reactions from quinolones?
GI Distress
Hepatotoxicity
Nephrotoxicity
Glucose changes
Seizures
Photosensitivity
C diff
HA/Dizziness
What is the MOA of Bactrim?
folate reductase inhibitor and folate synthesis inhibitor
What are the first line indications for Bactrim?
MRSA (outpatient)
UTI/cystitis
Prevention of P jiroveci
(option for Legionella and pneumonia)
What is the metabolism and excretion of Bactrim?
Liver metabolism and excreted by kidneys
Who should not get Bactrim?
Folate deficient
(poor nutrition, alcoholics)
What are the adverse reactions to Bactrim?
Megaloblastic anemia
N/V/D
Photosensitivity
Hepatotoxicity
What pregnancy category is Bactrim?
C
What is the MOA of Macrobid?
Inhibits bacterial enzymes and damages DNA
What is the coverage of Macrobid?
E coli in the urine
What are contraindications for Macrobid?
Renal impairment
Pregnancy
What are common adverse effects of Macrobid?
N/V
What is the MOA of Flagyl
Disrupts microbial DNA
What is the spectrum of activity for Flagyl?
Gram +
Gram -
Anaerobes
Protozoans
What are the first line indications for Flagyl?
Trichomonas
Bacteria Vaginosis
C diff
Amebiasis
Giardiasis
How is Flagyl metabolized?
Metabolized by liver and excreted by kidneys
What are the adverse reactions for Flagyl?
GI distress N/V/D
Metallic taste
Disulfiram-like reaction
What is a CI for Flagyl?
Alcohol use
What is the BBW for flagyl?
Cancer causing in mice and rats
What is Silvadene used for?
Topical burn cream
What is sulfacetamide use for?
Solution or ointment for ophthalmic infections
What is Daraprim used for?
Antiparasite/antimalarial
What is bacitracin used for?
topical ointment against staph/strep
What is polymyxin B used for?
Ophthalmologic drops for pseudomonas in the eye
What is chloramphenicol used for?
Almost never used but can be used as ophthalmic solution or IV, very broad spectrum
What is mupirocin used for?
Impetigo/skin infections
Can be used to decolonize MRSA with chlorhexidine