Aminoglycosides

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Questions and Answers

What other drugs are included in aminoglycosides?

Gentamicin, amikacin, streptomycin, neomycin, kanamycin and apramycin

Why does FARAD recommend not using aminoglycosides in an extra-labeled manner (ELDU)?

  • Due to their poor absorption when administered intramuscularly
  • Due to the risk of residues being detected above maximal limits (correct)
  • Because they are rapidly eliminated through glomerular filtration
  • Because they are ineffective against bacterial infections

Which characteristic of aminoglycosides is due to their structure as large molecules with numerous amino acid groups?

  • They are neutral in physiological pH
  • They are basic polycations that are highly ionized at physiological pH (correct)
  • They easily cross lipid membranes due to their hydrophobic nature
  • They have a high volume of distribution in all species

Which of the following statements is true regarding the absorption of aminoglycosides?

<p>They are rapidly and well absorbed from intramuscular (IM) and subcutaneous (SC) routes. (B)</p> Signup and view all the answers

Which of the following statements about aminoglycoside distribution is true?

<p>They are limited to the extracellular fluid space (B)</p> Signup and view all the answers

The volume of distribution of aminoglycosides is __________ to ___________

<p>Low to moderate.</p> Signup and view all the answers

In neonates, the volume of distribution (Vd) for aminoglycosides is:

<p>Higher due to increased extracellular fluid (B)</p> Signup and view all the answers

After parenteral administration, aminoglycosides reach effective concentrations in which of the following fluids?

<p>Synovial, peri lymph, pleural, peritoneal, and pericardial fluid (B)</p> Signup and view all the answers

Which organ has the highest accumulation of gentamicin over time?

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

Which of the following respectively describes why there’s an increased risk of nephrotoxicity and extended withdrawal times?

<p>Accumulation of aminoglycosides in the renal tubular epithelium (A)</p> Signup and view all the answers

How are aminoglycosides primarily eliminated from the body?

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

How do aminoglycosides half-life change in neonates or animals with renal dysfunction?

<p>They have short half-life that increases in neonates or animals with renal dysfunction. (D)</p> Signup and view all the answers

What effect does halothane anesthesia have on gentamicin pharmacokinetics?

<p>Decreases body clearance and volume of distribution (B)</p> Signup and view all the answers

Why should aminoglycosides not be used with neuromuscular blocking agents?

<p>They are inactivated due to pH incompatibilities (D)</p> Signup and view all the answers

Aminoglycosides can act synergistically with which class of antibiotics?

<p>β-lactams (C)</p> Signup and view all the answers

Nephrotoxic drugs must be avoided when using aminoglycosides

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

How do aminoglycosides enter susceptible gram-negative bacteria?

<p>Active transport using an oxygen-dependent mechanism (B)</p> Signup and view all the answers

What is the target site of aminoglycosides inside bacterial cells?

<p>30S ribosomal subunit (C)</p> Signup and view all the answers

The primary effect of aminoglycosides on bacterial protein synthesis is:

<p>Causing misreading of the genetic code (C)</p> Signup and view all the answers

Aminoglycosides exhibit which type of bacterial killing action?

<p>Dose-dependent bactericidal activity (A)</p> Signup and view all the answers

Why might aminoglycosides fail to kill normally susceptible bacteria?

<p>Increased local acidity from tissue damage reduces their effectiveness (C)</p> Signup and view all the answers

Which of the following conditions can inactivate aminoglycosides?

<p>The presence of purulent debris (B)</p> Signup and view all the answers

Which of the following is NOT a risk factor for aminoglycoside-induced nephrotoxicity?

<p>Alkaline urine pH (C)</p> Signup and view all the answers

Which of the following adverse effects of aminoglycosides is caused by their interaction with nicotinic cholinergic receptors?

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

What can be used to reverse aminoglycoside-induced neuromuscular blockade?

<p>Acetylcholinesterase inhibitors (B)</p> Signup and view all the answers

Which type of ototoxicity is associated with aminoglycosides?

<p>Both vestibular and cochlear damage (C)</p> Signup and view all the answers

What is the primary mechanism of aminoglycoside resistance?

<p>Enzymatic inactivation via genes located on bacterial plasmids (C)</p> Signup and view all the answers

Why are aminoglycosides considered narrow-spectrum antibiotics?

<p>They primarily target aerobic Gram-negative bacteria (B)</p> Signup and view all the answers

Which Gram-negative bacterium is typically susceptible to aminoglycosides?

<p>Pseudomonas aeruginosa (B)</p> Signup and view all the answers

What is the main consideration for therapeutic drug monitoring (TDM) of aminoglycosides?

<p>Timing of sample collection (B)</p> Signup and view all the answers

Why is continuous exposure of bacteria to aminoglycosides a concern?

<p>It causes adaptive resistance (B)</p> Signup and view all the answers

What is the recommended aminoglycoside concentration to achieve efficacy against the targeted pathogen?

<p>At least 8 to 10 times the MIC (C)</p> Signup and view all the answers

How should aminoglycoside dosage be adjusted during therapeutic drug monitoring (TDM)?

<p>Based on Cmax (peak) and Cmin (trough) levels (B)</p> Signup and view all the answers

Why is exposure to a single dose of an aminoglycoside a concern?

<p>It can produce resistant bacterial variants (B)</p> Signup and view all the answers

Why is parenteral administration of aminoglycosides limited?

<p>Risk of toxicity (B)</p> Signup and view all the answers

What are the four considerations to take when a patient is medicated with aminoglycosides?

<p>the PK varies between subjects, the risk of renal failure, the continuous exposure of aminoglycosides to bacteria leads to adaptive resistance, and the concentration of at least 8-10 time MIC of target pathogen should be achieved to get efficacy.</p> Signup and view all the answers

Why is therapeutic drug monitoring (TDM) important for aminoglycosides?

<p>To reduce resistance, toxicity, and confirm therapeutic concentrations</p> Signup and view all the answers

What is measured in therapeutic drug monitoring of aminoglycosides?

<p>Peak and trough concentrations (B)</p> Signup and view all the answers

What can peak and trough concentrations of aminoglycosides be used to calculate?

<p>Elimination half-life (C)</p> Signup and view all the answers

What does an increase in the elimination half-life during aminoglycoside therapy indicate?

<p>Early signs of tubular insult (B)</p> Signup and view all the answers

What is an early and sensitive indicator of nephrotoxicity in patients receiving aminoglycosides

<p>Prolonged elimination half-life (C)</p> Signup and view all the answers

Which aminoglycosides are available for intrauterine (IU) infusion in mares?

<p>Gentamicin (A), Amikacin (D)</p> Signup and view all the answers

Aminoglycosides are not labeled for other ROA in large animals, but commonly administered by IV, IM, SC, intra-articular and IO to horses

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

Which administration route of aminoglycosides achieves the highest concentration in synovial fluid for 24 hours?

<p>Intra-articular (IA) (C)</p> Signup and view all the answers

Which of the following aminoglycosides is available in topical formulations combined with glucocorticoids for dermal and otic application?

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

Which of the following drugs are available in ophthalmic formulations?

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

Which aminoglycoside is available in oral formulations for calves?

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

Neomycin can be used for topical or ocular applications in calves is called _________________

<p>Triple antibiotic</p> Signup and view all the answers

The importance of this group in veterinary medicine is in the treatment of gram ________________ infections caused by __________ pathogens; such as ______________

<p>Negative; enteric ; E. Coli</p> Signup and view all the answers

If gentamicin has developed resistance in Gram negative, what medication can we use instead?

<p>Amikacin</p> Signup and view all the answers

Which aminoglycosides are used to treat Gram-negative and staphylococcal keratitis?

<p>Tobramycin and gentamicin (B)</p> Signup and view all the answers

Why is topical application preferred in the treatment of local infections with aminoglycosides?

<p>It overcomes the problem of toxicity (C)</p> Signup and view all the answers

Which of the following administration routes is recommended for the treatment of septic arthritis or osteomyelitis?

<p>Intra-articular, intraosseous, or intravenous regional perfusion (C)</p> Signup and view all the answers

What is a major limitation of aminoglycoside use in treating infections?

<p>Poor penetration of cellular membranes (A)</p> Signup and view all the answers

Which aminoglycoside is preferred for treating melting corneal ulcers caused by gentamicin-resistant Pseudomonas?

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

In small animals, topical formulations of aminoglycosides are commonly used to treat which condition?

<p>Dermatitis (“hot spots”) (A), Otitis externa (D)</p> Signup and view all the answers

In equine medicine, gentamicin is commonly used for the treatment of ______________________

<p>Septic arthritis</p> Signup and view all the answers

Which aminoglycoside is administered orally in calves for the treatment of scours, despite unproven efficacy?

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

In swine medicine, the aminoglycoside __________, is used orally for the prophylaxis and treatment of ______________

<p>Apramycin; colibacillosis</p> Signup and view all the answers

What is a potential issue with oral apramycin use in poultry for E. coli infections?

<p>Enteritis significantly increases oral absorption, leading to tissue residue concerns (C)</p> Signup and view all the answers

Flashcards

Aminoglycoside drugs

Gentamicin, amikacin, streptomycin, neomycin, kanamycin, and apramycin.

Aminoglycoside ELDU risk

Due to concerns about residue detection exceeding maximum residue limits (MRLs).

Aminoglycoside characteristics

They are basic polycations, highly ionized at physiological pH due to large molecules with amino acid groups.

Aminoglycoside absorption routes

Rapid and well absorbed from intramuscular (IM) and subcutaneous (SC) routes.

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Aminoglycoside distribution

Distribution is limited to the extracellular fluid space.

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Aminoglycoside volume of distribution

Low to moderate.

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Aminoglycoside Vd in neonates

Higher due to increased extracellular fluid.

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Aminoglycoside fluid penetration

Achieve effective concentrations in synovial, perilymph, pleural, peritoneal, and pericardial fluid.

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Gentamicin accumulation

Renal cortex.

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Nephrotoxicity and withdrawal times

Accumulation of aminoglycosides in the renal tubular epithelium.

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