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[MT 6314] Pharmacology & Toxicology > [3S] Aminoglycosides & Spectinomycin PPT > Flashcards

[3S] Aminoglycosides & Spectinomycin PPT Flashcards

1
Q

MODES OF ANTIBACTERIAL ACTION

Treatment of microbial infection with antibiotics
▪Multiple daily dosing
▪Maintain serum concentration level
above the minimum inhibitory concentration (MIC)

A

Aminoglycosides

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2
Q

MODES OF ANTIBACTERIAL ACTION

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

Concentration Dependent

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3
Q

MODES OF ANTIBACTERIAL ACTION

Any antibiotics, including Penicillin and
Cephalosporins
▪Directly related to time above MIC
▪Independent of concentration once the MIC is reached

A

Time Dependent

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4
Q

MODES OF ANTIBACTERIAL ACTION

Aminoglycosides’ killing action continues when the plasma levels have declined below measurable levels

A

Postantibiotic Effect

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5
Q

MODES OF ANTIBACTERIAL ACTION

Greater efficacy when administered as a SINGLE LARGE DOSE than when given as multiple smaller doses

A

Postantibiotic Effect

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6
Q

MODES OF ANTIBACTERIAL ACTION

T/F: Toxicity (in contrast to antibacterial activity)
depends on a critical plasma concentration and
on that time such a level is exceeded

A

T

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7
Q

MODES OF ANTIBACTERIAL ACTION AMINOGLYCOSIDES

T/F: Time above such threshold is longer with
single large dose

A

F; shorter

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8
Q

MODES OF ANTIBACTERIAL ACTION AMINOGLYCOSIDES

T/F: Basis for once-daily dosing protocols

A

T

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9
Q

PKINETICS

  • Structurally related amino sugars attached by glycosidic linkages
  • Polar compounds
A

Aminoglycosides

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10
Q

T/F: Aminoglycosides are absorbed orally

A

F; not absorbed

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11
Q

AMINOGLYCOSIDES PKINETICS

T/F:
- Limited tissue penetration
- Do not readily cross the blood-brain barrier

A

T

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12
Q

PKINETICS

Aminoglycosides:
- Major mode of excretion
- Plasma levels are affected by changes in

A

Glomerular filtration
Renal function

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13
Q

AMINOGLYCOSIDES PKINETICS

T/F: Excretion is directly proportional to creatinine clearance

A

T

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14
Q

AMINOGLYCOSIDES PKINETICS

T/F: Dosage adjustment must be made in renal insufficiency to avoid toxic accumulation

A

T

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15
Q

AMINOGLYCOSIDES PKINETICS

________________ is needed for safe and effective dosage selection and adjustment

A

Monitoring plasma levels

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16
Q

MECHANISM OF ACTION

  • Bactericidal (irreversible) inhibitors of protein synthesis
  • Penetration of bacterial cell wall is partly dependent on O2-dependent active transport
A

Aminoglycosides

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17
Q

MECHANISM OF ACTION

  • Bind to 30S ribosomal unit
  • Interfere with protein synthesis
    1. Block formation of initiation complex
    2. Cause misreading of the code on the mRNA template
    3. Inhibit translocation
A

AMINOGLYCOSIDES

18
Q

MECHANISMS OF RESISTANCE

  • Resistant due to failure to penetrate into the cell
    ▪Streptococci, including S. pneumoniae
    ▪Enterococci
A

AMINOGLYCOSIDES

19
Q

MECHANISMS OF RESISTANCE

  • Plasmid-mediated formation of inactivating
    enzymes
    ▪Primary mechanism of resistance
    ▪Varying susceptibility to the enzyme
A

AMINOGLYCOSIDES

20
Q

MECHANISMS OF RESISTANCE

▪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

21
Q

MECHANISMS OF RESISTANCE

Transferases produced by enterococci can inactivate

A

▪Amikacin
▪Gentamicin
▪Tobramycin

22
Q

MECHANISMS OF RESISTANCE

Receptor protein on the 30S ribosomal subunit
may be deleted or altered as a result of a mutation

A

AMINOGLYCOSIDES

23
Q

CLINICAL USES

Used for the following but is not the drug of choice
▪H. influenzae
▪M. catarrhalis
▪Shigella species

A

GENTAMICIN, TOBRAMYCIN, AMIKACIN

24
Q

CLINICAL USES

  • Not effective for gram (+) cocci when used alone
  • Combination of aminoglycoside and cell wall synthesis inhibitors
A

Antibacterial Synergy

25
Q

CLINICAL USES

Combined with penicillin in the treatment
▪Pseudomonal
▪Listerial
▪Enterococcal infections

A

ANTIBACTERIAL SYNERGY

26
Q

CLINICAL USES

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

Streptomycin

27
Q

Neomycin ROA

A

Topical

28
Q

Kanamycin and paromomycin ROA

A

IM/IV/PO

29
Q

CLINICAL USES

• Active against: Gram-positive bacteria, Gram-negative bacteria, some mycobacteria
• Resistant: P aeruginosa, Streptococci

A

NEOMYCIN, KANAMYCIN, PAROMOMYCIN

30
Q

Netilmicin ROA

A

IM/IV/Topical/Ocular/Intrathecal

31
Q

CLINICAL USES

Reserved for serious infections resistant to other aminoglycosides

A

Netilmicin

32
Q

CLINICAL USES

  • Aminocylitol related to aminoglycosides
  • Back-up drug
A

Spectinomycin

33
Q

CLINICAL USES

Intramuscular as single dose for gonorrhea
- NOT recommended for treatment of pharyngeal gonococcal infections

A

Spectinomycin

34
Q

OTOTOXICITY

Auditory impairment

A

Amikacin, neomycin and kanamycin

35
Q

OTOTOXICITY

Vestibular dysfunction

A

Gentamicin and tobramycin

Book: Streptomycin & Gentamicin

36
Q

TOXICITY

  • Risk is proportionate to the plasma levels
    ▪ High if dosage is not modified in renal dysfunction
  • Increased with the use of loop diuretics
  • Contraindicated in pregnancy
A

Ototoxicity

37
Q

TOXICITY

Acute tubular necrosis
Reversible

A

Nephrotoxicity

38
Q

Most nephrotoxic

A

Gentamicin, Tobramycin & Neomycin

39
Q

NEPHROTOXICITY

Patients concurrently receiving

A

▪ Amphotericin B
▪ Cephalosporins
▪ Vancomycin

40
Q

Neuromuscular Blockade treatment

A

▪ Calcium
▪ Neostigmine
▪ Ventilatory support

41
Q

TOXICITY

Allergic skin reactions like contact dermatitis

A

Neomycin

[MT 6314] Pharmacology & Toxicology (20 decks)

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