aminoglycosides Flashcards

(42 cards)

1
Q

 Some drugs and aminoglycosides
• As the plasma level is increased above the MIC, the drug kills an increasing proportion of bacteria at a more rapid rate

A

conc dependent

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2
Q

 Any antibiotic, including penicillins and cephalosporins
• Directly related to time above MIC
• Independent of concentration once the MIC is reached

A

TIME DEPENDENT

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3
Q

 Structurally related amino sugars attached by glycosidic linkages

A

aminoglycosides

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4
Q

are aminoglycosides polar or not

A

polar

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5
Q

RoA of aminoglycosides

A

 Given intramuscularly or intravenously for systemic effects

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6
Q

Are aminoglycosides absorbed orally?

A

no

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7
Q

tissue penetration of aminoglycosides (full partial limited)

A

Limited

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8
Q

 Does it readily cross the blood-brain barrier

A

no

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9
Q

 Major mode of excretion

A

Glomerular filtration

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10
Q

 Excretion is directly proportional to —- clearance

A

creatinine

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11
Q

With normal renal function, elimination half-life is

A

2-3 h

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12
Q

 Peak serum levels

 Measured at

A

30-60 minutes after administration

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13
Q

 Trough serum levels

 Measured when

A

just before the next dose

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14
Q

MoA of AG

A

 Bactericidal (irreversible) inhibitors of protein synthesis

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15
Q

 Penetration of bacterial cell wall is partly dependent on ___________

A

O2-dependent active transport

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16
Q

 Transport is enhanced by ________

A

cell wall synthesis inhibitors

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17
Q

 Bind to _____ AND Interfere with protein synthesis

A

30S ribosomal unit

18
Q

ag interfere with protein synthesis by

A
  1. Block formation of initiation complex
    1. Cause misreading of the code on the mRNA template
    2. Inhibit translocation
19
Q

MECHANISMS OF RESISTANCE

A

 Failure to penetrate into the cell

 Plasmid-mediated formation of inactivating enzymes

20
Q

• Primary mechanism of resistance

A

Plasmid-mediated formation of inactivating enzymes

21
Q


 Catalyze the acetylation of amine functions
 Transfer of phosphoryl or adenyl groups to the O2 atoms of hydroxyl groups on the aminoglycoside

A

Group transferases

22
Q

transferases produced by enzyme can inactivate

A
  • Amikacin
  • Gentamicin
  • Tobramycin
  • Not streptomycin
  • Netilmicin is less susceptible and is active against more strains of organisms
23
Q
for Serious infections caused by aerobic gram (-) bacteria 
•	E. coli 			Enterobacter
•	Klebsiella		Proteus
•	Providencia		Pseudomonas
•	Serratia
A

GENTAMICIN, TOBRAMYCIN, and AMIKACIN

24
Q

 Tuberculosis
 Plague
 Tularemia
 Multi-drug-resistant (MDR) strains of M. tb resistant to streptomycin maybe susceptible to amikacin

25
 Used topically  Locally • In the GIT • Eliminate bacterial flora
NEOMYCIN
26
 Reserved for serious infections resistant to other aminoglycosides
NETILMICIN
27
 Aminocylitol related to aminoglycosides  Back-up drug  Intramuscular as single dose for gonorrhea
SPECTINOMYCIN
28
A. OTOTOXICITY |  Auditory or vestibular damage (or both) maybe irreversible or reversible?
IRREVERSIBLE
29
DRUGS RESPONSIBLE FOR | • Auditory impairment
Amikacin and kanamycin
30
DRUGS RESPONSIBLE FOR | Vestibular dysfunction
Gentamicin and tobramycin
31
OTOTOXICITY Risk is proportionate to the | • High if dosage is not modified in renal dysfunction
plasma levels
32
 Increased with the use of loop diuretics |  Contraindicated in pregnancy
OTOTOXICITY Risk
33
RESPONSIBLE FOR | • Allergic skin reactions like contact dermatitis
Neomycin
34
C.  Rare  Curare-like block may occur at high doses
NEUROMUSCULAR BLOCKADE
35
is neuromuscular blockade reversible or irre
reversible
36
neuromuscular blockade causes
respiratory paralysis
37
treatment of neuromuscular blockade
Calcium | Neostigmine
38
treatment of neuromuscular blockade requires
Ventilatory support
39
nephrotoxicity more common in (2)
```  Patients concurrently receiving • Amphotericin B • Cephalosporins • Vancomycin Elderly ```
40
is nephrotoxicity reversible or irre
rever
41
 Most nephrotoxic drugs
Gentamicin and tobramycin
42
nephrotoxicity is in the form of
acute tubular necrosis