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Aminoglycosides Overview

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Aminoglycosides Overview

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ABID OFFICIAL CHANNEL
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Aminoglycosides

Aminoglycosides
Drugs included in this group are
Streptomycin
Gentamycin
Tobramycin
Neomycin
Kanamycin
Amikacin
Sesomycin
Netilmicin
Aminoglycosides

Aminoglycosides have hexose ring


either streptidene in streptomycin or 2-
deoxysteptamine in other
aminoglycosides to which various amino
sugars are attached.
Aminoglycosides
Mechanism of Action

Aminoglycosides are irreversible inhibitors of


protein synthesis of bacteria.
They passively diffused through porin
channels across the outer membrane. Then the drug
is actively transported across the cell membrane
into the cytoplasm by an oxygen dependant process,
transport is coupled to a proton pump.
This transport is increased by cell wall active
drugs such as Pencillin and Vancomycin.
They bind to specific 30S microsomal subunit
proteins and thus the protein synthesis is inhibited.
How resistance develops

 Production of transferase enzyme or


enzymes
 Impaired entry of Aminoglycoside into the
cell
 The recepter protein on the 30S ribosomal
subunit may be altered or absent
Pharmacokinetics

 Concentration dependant killing

 Post antibiotic effect


ADVERSE EFFECTS

 Ototoxicity

 Nephrotoxicity

 Respiratory Paralysis
Antidote

Calcium gluconate

Neostigmine
CLINICAL USES

 Bactericidal
 Used against Gm negative enteric
bacteria (Bacteremia and Sepsis)
 Endocarditis
 Tuberculosis
ALL AMINOGLYCOSIDES HAVE NO
ACTIVITY AGAINST ANAEROBES
STREPTOMYCIN

 Obtained from streptomyces


griseus
 Second line drug for the
treatment of T.B.
 Plague
 Brucellosis
 Endocarditis
STREPTOMYCIN

Adverse effects

 Fever
 Skin rash
 Pain at the site of injection
 Vertigo
 Loss of balance
STREPTOMYCIN

CONTRAINDICATED IN PREGNANCY
CAN CAUSE DEAFNESS IN NEWBORN
GENTAMYCIN
 Obtained from micromonospora purpurea

 Effective against both Gm negative and


Positive organisms

 Can be given alone or in combination with


beta lactam antibiotics against Psedomonas,
Proteus, Klebseilla

 Available in form of creams, ointments and


solutions
GENTAMYCIN

 In Meningitis given intrathecally but not in


neonates

 Now a days for Meningitis it is replaced by


third generation cephalosporin

 Nephrotoxicity is reversible while


Ototoxicity is irreversible
TOBRAMYCIN
 It is more active against Pseudomonas
 Tobramycin and Gentamycin are
clinically interchangeable
 Available in the form of solution for
inhalation for the treatment of
Pseudomonas aeruginosa in lower
respiratory tract infection
 Dose: 300mg BD regardless of age and
weight
AMIKACIN

 Synthetic derivative of Kanamycin, less


toxic than the parent

 Resistant to many enzymes that inactivate


gentamycin and tobramycin

 Mycobacterium Tuberculosis is also


susceptible
NETILMICIN

It is similar to gentamicin and tobramycin


but due to addition of ethyl group to the
1-amino position of the 2-
deoxystreptamine ring.
NEOMYCIN & KANAMYCIN

 They are closely related

 Paromomycin also belong to this group

 They are widely used in bowl preparation


for elective surgery
NEOMYCIN & KANAMYCIN

 CLINICAL USES
 Topical
 Oral
THANK YOU

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