لخّصلي

Aminoglycosides

Mechanism of Action (MOA):

Aminoglycosides bind irreversibly to the 30S ribosomal subunit of bacterial ribosomes, leading to: • Inhibition of protein synthesis. • Misreading of mRNA, causing the production of nonfunctional or toxic proteins. • Disruption of bacterial membrane integrity, ultimately leading to cell death. This bactericidal activity is concentration-dependent.

Classification:

Aminoglycosides are a class of bactericidal antibiotics. Examples include: • Gentamicin • Tobramycin • Amikacin • Streptomycin • Neomycin

Spectrum of Activity:

Aminoglycosides are primarily effective against: • Gram-negative aerobes: E. coli, Klebsiella spp., Pseudomonas aeruginosa, Proteus spp. • Limited activity against Gram-positive organisms, but often used synergistically with beta-lactams or vancomycin for infections caused by Enterococcus spp. or Staphylococcus aureus. • Ineffective against anaerobic bacteria due to oxygen-dependent uptake.

Dosing:

Dosing varies based on the specific drug, indication, and patient factors (e.g., renal function). Typical approaches include: • Gentamicin/Tobramycin: • Conventional dosing: 1–2 mg/kg every 8 hours. • Once-daily dosing: 5–7 mg/kg once daily. • Amikacin: • 15–20 mg/kg once daily. • Adjustments for renal impairment are critical due to nephrotoxicity risks. • Therapeutic drug monitoring (TDM) is often employed to optimize efficacy and minimize toxicity.

Adverse Effects:

Aminoglycosides are associated with significant toxicities, particularly with prolonged use or high doses: • Nephrotoxicity: Reversible damage to renal tubules. • Ototoxicity: Irreversible hearing loss or vestibular dysfunction. • Neuromuscular blockade: Rare but can lead to respiratory paralysis, particularly in patients with underlying neuromuscular disorders or concurrent use of neuromuscular blockers. • Hypersensitivity reactions: Rare.

Aminoglycosides

Mechanism of Action (MOA):

Aminoglycosides bind irreversibly to the 30S ribosomal subunit of bacterial ribosomes, leading to:
• Inhibition of protein synthesis.
• Misreading of mRNA, causing the production of nonfunctional or toxic proteins.
• Disruption of bacterial membrane integrity, ultimately leading to cell death.
This bactericidal activity is concentration-dependent.

Classification:

Aminoglycosides are a class of bactericidal antibiotics. Examples include:
• Gentamicin
• Tobramycin
• Amikacin
• Streptomycin
• Neomycin

Spectrum of Activity:

Aminoglycosides are primarily effective against:
• Gram-negative aerobes: E. coli, Klebsiella spp., Pseudomonas aeruginosa, Proteus spp.
• Limited activity against Gram-positive organisms, but often used synergistically with beta-lactams or vancomycin for infections caused by Enterococcus spp. or Staphylococcus aureus.
• Ineffective against anaerobic bacteria due to oxygen-dependent uptake.

Dosing:

Dosing varies based on the specific drug, indication, and patient factors (e.g., renal function). Typical approaches include:
• Gentamicin/Tobramycin:
• Conventional dosing: 1–2 mg/kg every 8 hours.
• Once-daily dosing: 5–7 mg/kg once daily.
• Amikacin:
• 15–20 mg/kg once daily.
• Adjustments for renal impairment are critical due to nephrotoxicity risks.
• Therapeutic drug monitoring (TDM) is often employed to optimize efficacy and minimize toxicity.

Adverse Effects:

Aminoglycosides are associated with significant toxicities, particularly with prolonged use or high doses:
• Nephrotoxicity: Reversible damage to renal tubules.
• Ototoxicity: Irreversible hearing loss or vestibular dysfunction.
• Neuromuscular blockade: Rare but can lead to respiratory paralysis, particularly in patients with underlying neuromuscular disorders or concurrent use of neuromuscular blockers.
• Hypersensitivity reactions: Rare.