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Aminoglycoside antibiotics
Presented by
P. Ruchitha Rao
Application number : aad8e90ced1711e9bfe455404a470379
Academic writing
Department of pharmacology
G. Pulla Reddy college of pharmacy
Contents
• Introduction
• Mechanism of action
• Classification
• Reference
Introduction
• Include streptomycin, neomycin, kanamycin,
amikacin, gentamicin, tobramycin,
sisomicin, netilmicin, and others
• Widely in combination with a β-lactam
antibiotic
– serious infections with gram-negative bacteria
– combination with vancomycin gram-positive
endocarditis
• Treatment of Tuberculosis.
Mechnism of action
Classification
STREPTOMYCIN
• Isolated from a strain of
Streptomyces griseus
• Ribosomal resistance
develops readily -
limiting its role as a
single agent
Clinical Uses
• Mycobacterial Infections
– second-line agent for treatment of tuberculosis
– 0.5–1 g/d - intramuscularly or intravenously
– combination with other agents to prevent emergence of
resistance
• Nontuberculous Infections
– plague, tularemia, and sometimes brucellosis : 1 g/d
i/m in combination with an oral tetracycline.
– Combination with Penicillin
• enterococcal endocarditis
• 2-week therapy of viridans streptococcal endocarditis.
• enterococcal infections
Adverse Reactions
• Fever, skin rashes, and other allergic
manifestations – hypersensitivity
• Pain at the injection site
• Disturbance of vestibular function (irreversible)
—vertigo and loss of balance - proportion to the
Age of the patient, Blood levels of the drug and
duration of administration
• Pregnancy : deafness in the newborn – relatively
contraindicated
GENTAMICIN
• Isolated from
Micromonospora purpurea
• Effective against both
grampositive and gram-
negative organisms
including staphylococci and
coliforms
• Synergistic companion with
β-lactam antibiotics.
• It also inhibits gramnegative
rods - resistant to multiple
other antibiotics
Clinical Uses
• Intramuscular or Intravenous Administration
– Severe infections : gram-negative bacteria which are
resistant to other drugs, especially P. aeruginosa,
Enterobacter sp, Serratia marcescens, Proteus sp,
Acinetobacter sp, and Klebsiella sp.
– Combination with a second agent
• Staphylococcal infections – rapid resistance (poor
permeability)
• Pneumonia - penetration of infected lung tissue is poor
and local conditions of low pH and low oxygen tension
• treatment of endocarditis caused by gram-positive
bacteria – 5–6 mg/kg/d t.d.s., o.d. is equally effective
Adverse Reactions
• Nephrotoxicity - reversible and mild
– 5–25% of patients
– longer than 3–5 days
• Ototoxicity – irreversible
– more than 5 days
– vestibular dysfunction and may be loss of
hearing
Amikacin
• Less toxic semisynthetic derivative of
kanamycin
• Resistant to enzymes that inactivate gentamicin
and tobramcyin
• Widest spectrum of activity
• Uses:
– Same as gentamicin
• Dose : 15mg/kg/day in 1-3 doses
Neomycin
• Topically used in skin, eye and external ear
infections combined with bacitracin or
polymyxin-B to widen antibacterial spectrum
and to prevent emergence of resistant strains
• Orally
– Preparation of bowel before surgery 1 gm TDS
• Bladder irrigation along with polymyxin B
Summery
Drugs Source Active
against
Markate
d name
t/2 Elimana
tion
Contrai
ndicated
Adverse
effects
Streptom
ycin
Streptom
yces
griseus
m.tuberc
ulosis,yer
sinia,
brucella
a
streptope
n
Kidney
disease
Disturba
nce of
hearing
Ototoxici
ty
Nephroto
xicity
Neurotox
ity
Hypersen
sitivity
Gentami
cin
Micromo
nospora
purpuria
Ps.aerugi
nosa,prot
eus,
e.coli,
klebsiella
Genacyn
Gentabac
Gentasol
Renal Kidney
disease
Allergic
responce
s.
Neuromu
scular
problems
Haemoly
tic
anaemia
Nerve
damage
Drug Source Active
against
Markete
d name
t/2 eliminati
on
Contran
dication
Adverse
effect
Neomyci
n
Streptom
yces
fradiae
Gram
negative
bacilli
Gram
positive
cocci
Neo –DP
Polydex-
N
2-3hrs GIT Kidney
disease
Ototoxic
nephroto
xic
kanamyci
n
Streptom
yces
kanamyc
eticus
pseudom
onas
Kanabac 2hrs 30
mins
Urine Ear
disturban
ces
Nephroto
xicity
ototoxicit
y
Amikaci
n
Pseudom
onas
Proteus
Amibac
Cimamak
Kacin
3-4 hrs kidney pregnanc
y
Hearing
loss
Tobramy
cin
Streptom
yces
tenebrari
us
Pseudom
onas
proteus
ACKNOWLEDGEMENT
• Academic writing
Reference
• Basic & Clinical Pharmacology Bertram G.
Katzung Twelfth Edition
• Essential of medical pharmacology - K.D.
Tripathi 6th edition
• Lippincott - Modern Pharmacology With
Clinical Applications 6E
• Color Atlas Of Pharmacology, 2Nd Ed
(Lüllmann, Thieme 2000)
• wikipedia
Aminoglycoside Antibiotics Mechanism Classification

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Aminoglycoside Antibiotics Mechanism Classification

  • 1. Aminoglycoside antibiotics Presented by P. Ruchitha Rao Application number : aad8e90ced1711e9bfe455404a470379 Academic writing Department of pharmacology G. Pulla Reddy college of pharmacy
  • 2. Contents • Introduction • Mechanism of action • Classification • Reference
  • 3. Introduction • Include streptomycin, neomycin, kanamycin, amikacin, gentamicin, tobramycin, sisomicin, netilmicin, and others • Widely in combination with a β-lactam antibiotic – serious infections with gram-negative bacteria – combination with vancomycin gram-positive endocarditis • Treatment of Tuberculosis.
  • 6. STREPTOMYCIN • Isolated from a strain of Streptomyces griseus • Ribosomal resistance develops readily - limiting its role as a single agent
  • 7. Clinical Uses • Mycobacterial Infections – second-line agent for treatment of tuberculosis – 0.5–1 g/d - intramuscularly or intravenously – combination with other agents to prevent emergence of resistance • Nontuberculous Infections – plague, tularemia, and sometimes brucellosis : 1 g/d i/m in combination with an oral tetracycline. – Combination with Penicillin • enterococcal endocarditis • 2-week therapy of viridans streptococcal endocarditis. • enterococcal infections
  • 8. Adverse Reactions • Fever, skin rashes, and other allergic manifestations – hypersensitivity • Pain at the injection site • Disturbance of vestibular function (irreversible) —vertigo and loss of balance - proportion to the Age of the patient, Blood levels of the drug and duration of administration • Pregnancy : deafness in the newborn – relatively contraindicated
  • 9. GENTAMICIN • Isolated from Micromonospora purpurea • Effective against both grampositive and gram- negative organisms including staphylococci and coliforms • Synergistic companion with β-lactam antibiotics. • It also inhibits gramnegative rods - resistant to multiple other antibiotics
  • 10. Clinical Uses • Intramuscular or Intravenous Administration – Severe infections : gram-negative bacteria which are resistant to other drugs, especially P. aeruginosa, Enterobacter sp, Serratia marcescens, Proteus sp, Acinetobacter sp, and Klebsiella sp. – Combination with a second agent • Staphylococcal infections – rapid resistance (poor permeability) • Pneumonia - penetration of infected lung tissue is poor and local conditions of low pH and low oxygen tension • treatment of endocarditis caused by gram-positive bacteria – 5–6 mg/kg/d t.d.s., o.d. is equally effective
  • 11. Adverse Reactions • Nephrotoxicity - reversible and mild – 5–25% of patients – longer than 3–5 days • Ototoxicity – irreversible – more than 5 days – vestibular dysfunction and may be loss of hearing
  • 12. Amikacin • Less toxic semisynthetic derivative of kanamycin • Resistant to enzymes that inactivate gentamicin and tobramcyin • Widest spectrum of activity • Uses: – Same as gentamicin • Dose : 15mg/kg/day in 1-3 doses
  • 13. Neomycin • Topically used in skin, eye and external ear infections combined with bacitracin or polymyxin-B to widen antibacterial spectrum and to prevent emergence of resistant strains • Orally – Preparation of bowel before surgery 1 gm TDS • Bladder irrigation along with polymyxin B
  • 15. Drugs Source Active against Markate d name t/2 Elimana tion Contrai ndicated Adverse effects Streptom ycin Streptom yces griseus m.tuberc ulosis,yer sinia, brucella a streptope n Kidney disease Disturba nce of hearing Ototoxici ty Nephroto xicity Neurotox ity Hypersen sitivity Gentami cin Micromo nospora purpuria Ps.aerugi nosa,prot eus, e.coli, klebsiella Genacyn Gentabac Gentasol Renal Kidney disease Allergic responce s. Neuromu scular problems Haemoly tic anaemia Nerve damage
  • 16. Drug Source Active against Markete d name t/2 eliminati on Contran dication Adverse effect Neomyci n Streptom yces fradiae Gram negative bacilli Gram positive cocci Neo –DP Polydex- N 2-3hrs GIT Kidney disease Ototoxic nephroto xic kanamyci n Streptom yces kanamyc eticus pseudom onas Kanabac 2hrs 30 mins Urine Ear disturban ces Nephroto xicity ototoxicit y Amikaci n Pseudom onas Proteus Amibac Cimamak Kacin 3-4 hrs kidney pregnanc y Hearing loss Tobramy cin Streptom yces tenebrari us Pseudom onas proteus
  • 18. Reference • Basic & Clinical Pharmacology Bertram G. Katzung Twelfth Edition • Essential of medical pharmacology - K.D. Tripathi 6th edition • Lippincott - Modern Pharmacology With Clinical Applications 6E • Color Atlas Of Pharmacology, 2Nd Ed (Lüllmann, Thieme 2000) • wikipedia