Antimicrobials Flashcards
Beta-Lactam Antibiotics:
Penicillins
contain a beta-lactam ring as part of their structure
bactericidal against susceptible MO by blocking bacterial transpeptidase, an enzyme that cross-links polymers of bacterial cell wall
typically used to treat susceptible strep and staph infections
bacteria have developed beta-lactamase enzymes, leading to the development of combo meds containing a beta-lactamase inhibitor
Penicillins: ADME
A: variable absorption; sometimes food affects absorption
D: wide distribution, inc. CSF
M: minimal liver metabolism (except nafcillin/oxacillin, which have hepatic metabolism)
E: rapid and extensive renal elimination
Penicillins: Patient Education
Women on BCP should use alternative method until next period, or at least for one week after abx course complete
GI side effects common, esp. diarrhea
Ideally taken on an empty stomach
Finish entire course of abx
Beta-Lactam Antibiotics:
Cephalosporins
Similar mechanism of action to PCNs, but more stable to many beta-lactamases, and therefore are broader spectrum
General rule of thumb: later generations have better gram negative coverage
Cephalosporins: ADME
A: variable absorption; rate but not total extent affected by food, so may be taken with or without
D: wide, inc. to CSF
M: minimal metabolism, except cefpodoxime is de-esterified in GI tract to active form
E: high percentage excreted in urine
Cephalosporins: Patient Education
Most common side effects are GI
Cross-sensitivity with PCN allergy ranges from 2-12% in studies (give if mild allergy to PCN like rash without urticaria; avoid if severe allergy to PCN)
Ceftriaxone should not be used in premature neonates (can compete with bilirubin for binding sites and result in kernicterus)
Types of Beta-Lactam Antibiotics
Penicillins, Cephalosporins, and Carbapenems (used in acute care setting only, broad spectrum, typically not first-line agents)
Examples of First Generation Cephalosporins & Common Uses
Cephalexin (Keflex), Cefadroxil (Duricef), IV Cefazolin (Ancef)
Often used for simple skin & soft tissue infections
Examples of Second Generation Cephalosporins & Common Uses
Cefuroxime (Ceftin), Cefaclor (Ceclor), Cefprozil (Cefzil)
Often used as an alternate choice for URI
Examples of Third Generation Cephalosporins & Common Uses
Cefpodoxime (Vantin), Cefixime (Suprax), IV Ceftriaxone (Rocephin), IV Ceftazidime (Fortaz or Tazicef), IV Cefotaxime (Claforan or Cefotan)
Part of most protocols for CAP
Examples of Fourth Generation Cephalosporins & Common Uses
IV Cefepime
Clinical role similar to that of third generation cacapabilities
Vancomycin
bactericidal for susceptible gram positive bacteria by inhibiting bacterial cell wall synthesis
po form used to treat C Diff if metronidazole is ineffective
very poor oral absorption, results in no detectable serum level
IV dosing requires monitoring levels and adjustment for patient size and renal function
Examples of Tetracyclines
Vibramycin, Tetracycline, Doxycycline, Minocycline, Demeclocycline
Tetracyclines
four ring chemical structure
bacteriostatic by entering MO (in part by active transport and in part by passive diffusion) and binding to 30s subunit of bacterial ribosome, interfering with protein synthesis
Tetracyclines: ADME
A: divalent cations (calcium, magnesium, iron) bind to drug and inhibit absorption
D: highly protein bound; widely distributed, EXCEPT for CSF
M: concentrated by liver in bile and feces
E: all (except doxycycline) extensively renally excreted as unchanged drug
Tetracyclines: Patient Education
Potential for increased photosensitivity
GI side effects common- take with food
Should not be given to children 8yr or younger (binds to calcium deposits in bone/teeth, causing deformity of bone, tooth enamel dysplasia); avoid in pregnancy for same reason
Examples of Macrolides and Common Uses
Erythromycin, Clarithromycin (Biaxin), Azithromycin (Zithromax)
Firstline in many CAP protocols (generally have good coverage versus atypical bacteria; staph/strep coverage based on local susceptibility patterns)
Treatment of STIs (chlamydia)
Macrolides
macrocyclic lactone ring
bacteriostatic at low concentrations, but bactericidal at higher concentrations
inhibit protein synthesis via binding to 50s ribosomal subunit
*caution in patients with baseline prolonged QT or on other meds that prolong QT (erythromycin and clarithromycin worse than azithromycin)
azithromycin has long half-life (48-96hrs) allowing for shorter abx course (stays in system) due to extensive tissue penetration (exceeds serum concentration; slowly releases from tissues)
Macrolides: ADME
A: clarithromycin and azithromycin more readily absorbed than erythromycin
D: wide, EXCEPT for CSF
M: CYP450 inhibitors; extensive hepatic metabolism
E: < 10% excreted unchanged
Telithromycin (Ketolide class)
structurally related to macrolides
binds to ribosomal subunit 50s to inhibit protein synthesis
second or third line against CAP
hepatoxicity, loss of consciousness, and visual disturbances are serious side effects