aminoglycosides Flashcards

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

A

STREPTOMYCIN

25
Q

 Used topically
 Locally
• In the GIT
• Eliminate bacterial flora

A

NEOMYCIN

26
Q

 Reserved for serious infections resistant to other aminoglycosides

A

NETILMICIN

27
Q

 Aminocylitol related to aminoglycosides
 Back-up drug
 Intramuscular as single dose for gonorrhea

A

SPECTINOMYCIN

28
Q

A. OTOTOXICITY

 Auditory or vestibular damage (or both) maybe irreversible or reversible?

A

IRREVERSIBLE

29
Q

DRUGS RESPONSIBLE FOR

• Auditory impairment

A

Amikacin and kanamycin

30
Q

DRUGS RESPONSIBLE FOR

Vestibular dysfunction

A

Gentamicin and tobramycin

31
Q

OTOTOXICITY Risk is proportionate to the

• High if dosage is not modified in renal dysfunction

A

plasma levels

32
Q

 Increased with the use of loop diuretics

 Contraindicated in pregnancy

A

OTOTOXICITY Risk

33
Q

RESPONSIBLE FOR

• Allergic skin reactions like contact dermatitis

A

Neomycin

34
Q

C.
 Rare
 Curare-like block may occur at high doses

A

NEUROMUSCULAR BLOCKADE

35
Q

is neuromuscular blockade reversible or irre

A

reversible

36
Q

neuromuscular blockade causes

A

respiratory paralysis

37
Q

treatment of neuromuscular blockade

A

Calcium

Neostigmine

38
Q

treatment of neuromuscular blockade requires

A

Ventilatory support

39
Q

nephrotoxicity more common in (2)

A
	Patients concurrently receiving
•	Amphotericin B
•	Cephalosporins
•	Vancomycin
Elderly
40
Q

is nephrotoxicity reversible or irre

A

rever

41
Q

 Most nephrotoxic drugs

A

Gentamicin and tobramycin

42
Q

nephrotoxicity is in the form of

A

acute tubular necrosis