Aminoglycosides

Besides streptomycin, which is only used for tuberculostatics, the most important systemically used agents are:

• (Streptomycin)
• Gentamicin
• Tobramycin
• Amikacin
• Fusomycin

Other aminoglycosides are only used topically (gentamicin is used systemically and topically):

• Kanamycin
• Framycetin
• Paromomycin (applied orally, but not absorbed; serves exclusively to reduce the intestinal flora and to eradicate Entamoeba histolytica)

Aminoglycosides are transported through the bacterial cytoplasmic membrane by a secondary active transporter. They inhibit bacterial protein synthesis by binding with high affinity to the 30-S subunit of bacterial ribosomes with subsequent translation disruption. The pathological proteins resulting from reading errors lead to membrane disorders of the bacteria and ultimately cause bactericidal activity in the proliferation and dormant stages of Gram-positive and Gram-negative bacteria.

Bactericidal activity increases depending on concentration. It is recommended to achieve the highest possible peak concentrations by applying the dose once a day in the morning. This also reduces the toxicity of the drugs.

Notice!

Nephrological UAW:

• Reversible nephrotoxicity with proteinuria, cylindruria, hematuria, elevated serum creatinine. Risk factors are an increased total dose and a long therapy duration. Also an elevated valley level leads to increased toxicity (therefore only 1 application)

Neurological UAW:

• neuromuscular blockade (antidote: calcium gluconate)
• Paresthesia
• Ototoxicity (irreversible), especially in cases of impaired renal function. Sympotms are nausea, tinnitus, dizziness, hearing loss. Amikacin mainly causes hearing disorders, gentamycin vestibular disorders, tobramycin both at the same time.
• Myalgias

Opthalmological ADRs:

• Paralysis of the eye muscles

Haematological ADRs:

• Blood count disorders

Heptatological ADRs:

• Transaminase increases

Immunological ADRs:

• allergic reactions up to anaphylactic shock
• Drug Fever

Haematological ADRs:

• thrombocytopenia
• Leukopenia
• Eosinophilia

Pregnancy, lactation, hypersensitivity to aminoglycosides, pre-damage of the vestibular or cochlear organ, terminal renal failure, myasthenia gravis, Parkinson's disease, sulphide hypersensitivity in bronchial asthma.

Cave! Preexisting kidney damage. Good synergistic effect with β lactam antibiotics. Under therapy regular control of BB and kidney values. Therapy duration preferably not more than 10 days! In case of renal insufficiency extension of the dosage intervals. Infusion duration about 30 minutes to avoid a neuromuscular blockade!

Representative of the family of aminoglycoside antibiotics:

• amikacin
• Gentamycin
• Tobramycin

Useful combinations with other antibiotics:

• Aminoglycoside + piperacillin against pseudomonads
• Aminoglycoside + ampicillin against listeria
• Aminoglycoside + Cefalosporine against Klebsiellen