Pharmacology of Aminoglycosides

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Questions and Answers

What is the primary mechanism of absorption for aminoglycosides?

  • Rectal suppositories
  • Oral absorption
  • Not absorbed orally, due to polar compounds (correct)
  • Topical application

What is the primary mode of elimination for aminoglycosides?

  • Lymphatic system
  • Hepatic metabolism
  • Renal elimination (correct)
  • Biliary excretion

What is the percentage incidence of nephrotoxicity associated with aminoglycosides?

  • 2-3%
  • 6-7% (correct)
  • 15-20%
  • 10-12%

What is the effect of concurrent administration of aminoglycosides with neuromuscular blockers?

<p>Neuromuscular paralysis (B)</p> Signup and view all the answers

What is the primary mechanism of antibacterial effect of aminoglycosides?

<p>Bacteriostatic activity (C)</p> Signup and view all the answers

What is the effect of aminoglycosides on myasthenia gravis patients?

<p>Particularly at risk of neuromuscular paralysis (D)</p> Signup and view all the answers

What is the mechanism of action of quinolone antibiotics?

<p>Inhibition of nucleic acid synthesis (B)</p> Signup and view all the answers

Which of the following antibiotics is an antimetabolite?

<p>Sulfonamides (A)</p> Signup and view all the answers

What is the clinical use of sulfonamide antibiotics?

<p>Gram-negative rod infections (B)</p> Signup and view all the answers

Which of the following antibiotics is often used in combination with penicillin G or ampicillin to treat enterococcal infections?

<p>Gentamicin (C)</p> Signup and view all the answers

How is vancomycin eliminated from the body?

<p>Renal filtration (C)</p> Signup and view all the answers

What is a common side effect of vancomycin?

<p>Red man syndrome (C)</p> Signup and view all the answers

Which of the following penicillins is sensitive to beta-lactamase and has a narrow spectrum?

<p>Penicillin G (A)</p> Signup and view all the answers

What is the primary mechanism of elimination for most penicillins?

<p>Active tubular secretion (D)</p> Signup and view all the answers

Which of the following bacteria is NOT typically covered by the spectrum of ampicillin?

<p>MRSA (B), Staphylococci (C)</p> Signup and view all the answers

What is the primary purpose of beta-lactamase inhibitors?

<p>To protect penicillins from inactivation by beta-lactamases (A)</p> Signup and view all the answers

What is the most common side effect of penicillin therapy?

<p>Hypersensitivity (A)</p> Signup and view all the answers

Which of the following penicillins undergoes enterohepatic cycling?

<p>Ampicillin (D)</p> Signup and view all the answers

What is the primary characteristic of benzathine penicillin G?

<p>It is a repository form with a long half-life (B)</p> Signup and view all the answers

Which of the following statements is TRUE about the spectrum of ticarcillin?

<p>It has increased activity against Pseudomonas aeruginosa (B)</p> Signup and view all the answers

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Study Notes

Vancomycin

  • Spectrum: MRSA, Enterococci, Clostridium difficile (backup drug)
  • Resistance: Vancomycin-resistant staphylococcal (VRSA) and enterococcal (VRE) strains
  • Pharmacokinetics: used IV and orally (not absorbed) in colitis, enters most tissues, eliminated by renal filtration
  • Side effects: "Red man syndrome" (histamine release), ototoxicity (permanent, additive with other drugs), nephrotoxicity (mild, additive with other drugs)

Aminoglycosides

  • Mechanism of action: inhibition of protein synthesis
  • Spectrum: gram-negative rods; gentamicin, tobramycin, and amikacin often used in combinations
  • Pharmacokinetics: polar compounds, not absorbed orally, widely distributed into tissues, renal elimination proportional to GFR
  • Side effects: nephrotoxicity (6-7% incidence), ototoxicity (2% incidence), neuromuscular paralysis

Beta-Lactams

  • Subgroups:
    • Narrow spectrum, beta-lactamase sensitive: penicillin G and penicillin V (spectrum: streptococci, pneumococci, meningococci, Treponema pallidum)
    • Very narrow spectrum, beta-lactamase resistant: nafcillin, methicillin, oxacillin (spectrum: known or suspected staphylococci, not MRSA)
    • Broad spectrum, beta-lactamase sensitive: ampicillin and amoxicillin (spectrum: gram-positive cocci, E. coli, H. influenzae, Listeria monocytogenes, Borrelia burgdorferi, H. pylori)
    • Extended spectrum, antipseudomonal, beta-lactamase sensitive: ticarcillin, piperacillin (spectrum: increased activity against gram-negative rods, including P. aeruginosa)
  • Pharmacokinetics: most eliminated via active tubular secretion, dose reduction needed only in major renal dysfunction
  • Side effects: hypersensitivity (5-7% incidence), GI distress, Jarisch-Herxheimer reaction in treatment of syphilis

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