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Aminoglycosides Antibiotics

Aminoglycosides are a class of antibiotics derived from Streptomyces griseous that includes streptomycin, gentamycin, and tobramycin. They work by binding irreversibly to the bacterial 30S ribosomal subunit, interfering with protein synthesis. Aminoglycosides are mainly effective against gram-negative bacteria and some gram-positives. Common uses include treatment of urinary tract infections, tuberculosis, and multi-drug resistant infections. However, they can cause ototoxicity, nephrotoxicity, and neuromuscular blockade as side effects. Resistance develops through bacterial enzymes that inactivate aminoglycosides or interfere with their transport into cells.

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94 views2 pages

Aminoglycosides Antibiotics

Aminoglycosides are a class of antibiotics derived from Streptomyces griseous that includes streptomycin, gentamycin, and tobramycin. They work by binding irreversibly to the bacterial 30S ribosomal subunit, interfering with protein synthesis. Aminoglycosides are mainly effective against gram-negative bacteria and some gram-positives. Common uses include treatment of urinary tract infections, tuberculosis, and multi-drug resistant infections. However, they can cause ototoxicity, nephrotoxicity, and neuromuscular blockade as side effects. Resistance develops through bacterial enzymes that inactivate aminoglycosides or interfere with their transport into cells.

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HlaSoe Win
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Aminoglycosides Antibiotics

- From Streptomyces griseous

Aminoglycosides include:

Streptomycin
Gentamycin
Tobramycin
Amikacin
Netilmicin
Neomycin (poorly absorbed)
Spectinomycin (aminocyclitol antobiotc)(Trobicin)
Kanamycin
Paromomycin
Sisomicin
Frammycetin

Mechanism of Action

- Bactericidal action
- Irreversibly bind 30S-ribosomal subunit
- Interferes complex at the start of codon(AUG) of mRNA
- Block protein synthesis
- Block further translation and premature termination
- Incorporation of incorrect amino acid

Antibacterial Spectrum

- Mainly Gram(-)ve bacteria (Pseudomonas, Proteus, Pasteurella, E.coli, Shigella , Klebsiella, Brucella, Haemophilus)(PESK)
- Some Gram(+)ve bacteria
- Mycobacteria (Streptomycin, Amikacin, Netilmicin, Kanamycin) ( 2nd line drug of TB)
- Anaerobic bacteria are resistant to aminoglycosides

Uses of Aminoglycosides

Streptomycin

- bacterial endocarditis( together with penicillin), plague, tularaemia, tuberculosis

Gentamycin, Tobramycin

- Urinary tract infection

Amikacin, Netilmicin

- Boarder spectrum among aminoglycosides – less toxic


- Resistant to aminoglycoside inactivating enzyme: active against gentamycin and tobramycin resistant bacteria
- Suitable for hospital Gram(-)ve infection
- Reserve drugs for Tuberculosis

Neomycin (poorly absorbed)

- Topically – burns, wounds, dermatitis


- Orally – bowel sterilization in hepatic coma and before intestinal surgery

Spectinomycin

- Drug resistance gonorrhea or gonorrhea in penicillin allergic patients


Kanamycin with Clindamycin - for penetrating abdominal wounds

Paromomycin - intestinal amoebiasis (orally)

Pharmacokinetics

- Highly polar cations, poorly absorbed from GI tract (IM, IV), some drugs locally in GI tract (oral, per-rectal)
- Do not penetrate most cells, CNS and the eyes
- Distributed throughout extracellular space
- High concentration found in renal cortex, endolymph and inner ear
- Excreted unchanged ( use in UTI )
- In renal impairment – toxic blood level
- More active in oxygen rich and alkaline media (alkalinisation of urine in UTI)

Untoward effects (Not safe in pregnancy)

1. Ototoxicity
- Largely irreversible and destruction of vestibular or cochlear sensory cells
a) Vestibular dysfunction ( Gentamycin, Streptomycin, Netilmycin )
-intense headache, vertigo, loss of equilibrium, ataxia, nystagmus, dizziness
b) auditory dysfunction ( Kanamycin, Amikacin )
-tinnitus, fullness in the ear, deafness (potent diuretics potentiate ototoxicity)
2. Nephrotoxicity (Tobramycin, Neomycin, Gentamycin)
- Due to accumulation in proximal tubular cells
- Reduce GFR
- Mild increase plasma creatinine level, albuminuria, hypokalaemia, hypocalcaemia, hypophosphataemia
3. Neuromuscular Blockade ( Reversible )
- Inhibit prejunctional release of Ach
- Respiratory paralysis can occur in Myasthenia gravis (contraindicated)
- Potentiate neuromuscular blocking agents (tubocurarine) – reversed by Calcium gluconate I.V or neostigmine
4. Others
- Rare – hypersensitive reactions
- Vague feelings of paraesthesia of the lips or circumoral region
- Prolong use – Superinfection, diarrhea, malabsorption

Mechanism of Resistance to aminoglycosides

1. Due to bacterial release of aminoglycoside inactivating enzymes


2. Interfere of transport (O2 dependent process) – undergo anaerobic conditions
3. Delete of receptors on 30S ribosomal subunit

Cautions

Incompatibilities with penicillins and aminoglycosides in vitro ( Gentamycin and Carbenicillin )

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