1. Penicillins
• Beta-lactams; largest and oldest class of antimicrobial agents
• Can cause hypersensitivity reactions, ranging from a mild rash to life-
threatening anaphylaxis
• Seizures can result from very high doses of any beta-lactam (including
cephalosporins and carbapenems)
• MOA: Inhibit transpeptidases (penicillin-binding proteins) in the bacterial
cell wall
• Penicillins have a very short half-life (<2 hours) & must be dosed multiple
times per day
• Most are poorly absorbed leading to diarrhea
• Can take with/without food
• Because of resistance, penicillins are a poor choice for most infections
a. Penicillin V (Penicillin VK®)
i. Good for syphilis, particularly neurosyphilis
b. Amoxicillin (Amoxil®)
i. Frequently prescribed in children
ii. Good for infections of the upper respiratory tract, such as
strep throat and otitis media (ear infection)
c. Amoxicillin/Clavulanate (Augmentin®)
i. Beta-lactam (amoxilcillin) & beta-lactamase inhibitor
(clavulanate) combination
ii. Clavulanate binds to beta-lactamases irreversibly,
preventing the beta-lactamase from destroying the
amoxicillin; this enables the therapeutic beta-lactam
(amoxicillin) to be effective
iii. Good for hospital-acquired (nosocomial) pneumonia
iv. Should be taken with food (at start of meal)
2. Cephalosporins
• Grouped into “generations” that correlate with their spectrum of activity
• All have cross-allergenicity with penicillins (~3-5%)
• Generally more resistant to beta-lactamases than pencillins are
a. Cephalexin (Keflex®)
i. 1st generation
ii. Good for skin & soft tissue infections
iii. Inexpensive and low incidence of adverse effects
b. Cefprozil (Cefzil®), cefdinir (Omnicef®)
i. 2nd generation
ii. Good for upper respiratory tract infections (URIs),
community-acquired pneumonia, and gonorrhea
c. Cefpodoxime (Vantin®)
i. 3rd generation
ii. One of the classes of antibiotics with the strongest
association with Clostridium difficile associated diarrhea
1
, Drug Quiz Summaries: Antibiotics
iii. Cefpodoxime (as well as some 2nd generation
cephalosporins) have the N-methylthiotetrazole (MTT) side
chain that can inhibit vitamin K production & prolong
bleeding. These antibiotics can also cause a disulfuram-like
reaction when co-administered with alcohol (important
counseling point for outpatient use!)
iv. Good for lower respiratory tract infections (ex. pneumonia),
pyelonephritis, meningitis, and skin & soft tissue infections
d. Cefepime (Maxipime®)
i. Only 4th generation cephalosporin
ii. Primarily used for nosocomial infections
iii. Not available by mouth
iv. DON’T WORRY ABOUT THIS DRUG; just on here for
your reference/example of 4th generation cephalosporin
3. Fluoroquinolones
• Near ideal antibiotics; over-prescribing them has quickly led to resistance
• Excellent oral bioavailability (80-100%), low incidence of adverse effects
• Their bioavailability is significantly decreased when administered with
calcium, iron, antacids, milk, or multivitamins, so counsel patients to
separate these agents by at least 2 hours or, if possible, take a week off of
the supplements
• Photosensitivity, GI effects, and headache are the most common side
effects
• Rare but serious side effects usually occur in those with underlying
conditions; hyper/hypoglycemia in diabetes, seizures with seizure
disorders, and prolongation of the QT interval in those with history of
arrhythmia
• Achilles tendon rupture very rarely may occur
• Contraindicated in pregnant patients and children
a. Ciprofloxacin (Cipro®)
i. Good for urinary tract infections (UTIs), unless patient has
history of frequent UTIs
b. Levofloxacin (Levaquin®)
i. Good for community-acquired pneumonia, UTIs,
abdominal infections, skin/soft tissue, & gonorrhea
4. Tetracyclines
• Drugs of choice for uncommon infections such as tick-borne diseases;
alternative to cipro/levo in bioterrorism scenarios
• Oral bioavailability is decreased significantly when administered with
calcium, iron, antacids, milk, or multivitamins; be sure to counsel patient
on separation (same as FQs)
• Most common side effects include photosensitivity and GI side effects
• Can cause esophageal irritation; patients should take the drug with water
& while standing up (if possible)
• Can cause discoloration of developing teeth and are contraindicated in
pregnant women and children <8 years
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