AMINOGLYCOSID
Presented by:-
Ms.Nidhi.G.Manwe
D Pharmacy
INTRODUCTION
Definition:
Aminoglycosides are a group of bactericidal antibiotics that are highly
effective against aerobic gram-negative bacteria.
• They are derived from Streptomyces or Micromonospora species and
used in serious systemic infections.
• Chemical Structure and Source:
• Contain amino sugars linked by glycosidic bonds.
• Examples of sources:
• Streptomyces → Streptomycin, Neomycin.
• Micromonospora → Gentamicin
Origin:
• They are either naturally derived from Streptomyces or Micromonospora
species or semisynthetic derivatives.
Mechanism of Action:
Bind irreversibly to the 30S subunit of bacterial ribosomes.
Cause misreading of genetic code, leading to faulty proteins.
Also inhibit the initiation of protein synthesis.
• Result: Bacterial death (bactericidal effect)
Spectrum of Activity:
Effective against: Aerobic gram-negative bacteria (E. coli, Klebsiella, Pseudomonas)
Limited effect on gram-positive bacteria, unless used with cell wall–active agents
(e.g., penicillin).
• Inactive against anaerobes (oxygen-dependent uptake into bacterial cells)
• Examples of Aminoglycosides:
• Streptomycin
• Gentamicin
• Tobramycin
• Amikacin
• Neomycin
• Kanamycin
• Routes of Administration:
• Parenteral (IV or IM) for systemic infections (oral forms are poorly
absorbed)
• Topical use in creams, ear/eye drops (e.g., neomycin)
• Oral use limited to gut decontamination (not absorbed into
bloodstream)
• Pharmacokinetics:
• Poor oral bioavailability.
• Widely distributed in body fluids but poor penetration into CSF.
• Not metabolized; excreted unchanged via kidneys.
• Short half-life (~2–3 hours); requires multiple daily doses or extended
interval dosing
Adverse Effects (Toxicities):
Nephrotoxicity (dose- and duration-dependent; reversible)
Ototoxicity (affects cochlear or vestibular function; may be irreversible)
Neuromuscular blockade (rare; risk in patients with neuromuscular
disorders)
• Pregnancy Risk: Can cross placenta; may cause fetal harm (hearing loss)
Clinical Uses:
Severe infections caused by gram-negative bacteria (e.g., sepsis, pneumonia,
UTIs)
Tuberculosis (streptomycin as second-line treatment)
Bowel preparation before colorectal surgery (neomycin orally)
• Often combined with β-lactam antibiotics for synergistic effects
Resistance Mechanisms:
Enzymatic modification (acetylation, phosphorylation, adenylation)
Mutation of ribosomal binding site
• Reduced uptake or increased efflux
SUMMARY
Aminoglycosides are bactericidal antibiotics effective
mainly against aerobic gram-negative bacteria.
They inhibit protein synthesis by binding to the 30S
ribosomal subunit.
Common drugs include streptomycin, gentamicin, and
amikacin.
They are used for serious infections like sepsis and UTIs.
Major side effects include nephrotoxicity and ototoxicity.
