Aminoglycosides - 10 Qs Flashcards

1
Q

What are Aminoglycosides?

A

Water soluble PSEUDOGLYCOSIDES

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2
Q

What Aminoglycosides are from streptamine moiety?

A

Kanamycin
Tobramycin
Gentamycin
Neomycin

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3
Q

What Aminoglycosides are from 2-Deoxystreptamine moiety?

A

Paromomycin

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4
Q

Are Aminoglycosides stable?

A

Yes.

They are stable in a wide range of PH (2-11)

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5
Q

What’s the MOA of Aminoglycosides?

A

BacteriCIDAL

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6
Q

Which Aminoglycosides is the exception to the all bactericidal rule

A

Spectinomycin (which is bacterioSTATIC)

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7
Q

Name target for Aminoglycosides

A

Ribosomal DNA in the 30S ribosomal subparticle

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8
Q

Effect of Aminoglycosides used in low doses on target?

A

Cause mistranslation and nonsense protein formation => inh protein synthesis

This is unique for cidal AB, usually static are the ones that inh protein synthesis

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9
Q

Why are B-lactam usually combined with Aminoglycosides?

A

To take further advantage of the damaged cell wall (buz the nonsense protein become part of the membrane and let in lots of drugs)

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10
Q

When are Aminoglycosides given orally?

A

To act in the gut - local action

Otherwise, given IV/ IM

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11
Q

What’s the spray tobramycin solution used for?

A

Sprayed into the lungs for d successful tx of P. aeruginosa inf in cystic fibrosis pts

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12
Q

What are Aminoglycosides usually reserved for?

A

For serious inf cuzed by gram (-) org becuz of serious toxicity which is often delayed at onset

Though, they have activity against gram (+), there are better agents for these

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13
Q

What m.o. are Aminoglycosides ineffective against

A

Anaerobes

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14
Q

How does resistance occur primarily?

A

A. Reduced permeability to Aminoglycosides

B. deactivating enzymes (R-factor controlled) via
N-acetylation, O-phosphorylation, O-adenylation

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15
Q

List AEs of Aminoglycosides.

A

Ototoxicity
Nephrotoxicity
Curare-type neuromuscular blockade

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16
Q

What’s Kanamycin sulfate

A

A fermentation pdt that’s a mixture of 3 comps, but Kanamycin A is predominant.

17
Q

Main use of Kanamycin sulfate

A

Part of anti-TB cocktail

18
Q

What’s kanamycin active against?

A

Mycobacterium kansasii
M. Marinum
M. intracellulare

19
Q

What m.o. are usually resistant to Aminoglycosides?

A

Anaerobes

P. Aeruginosa

20
Q

Name drugs in the Aminoglycosides class that are part of anti-TB cocktail.

A

Kanamycin sulfate

Amikacin sulfate

21
Q

What’s Amikacin sulfate?

A

Semi-synthetic pdt of Kanamycin

22
Q

What does Amikacin contain that inh enzymes?

A

Hydroxyaminobuteryl amide (HABA)

23
Q

Use of Tobramycin sulfate

A

For difficult inf including gentamicin resistant P. Aeruginosa

24
Q

Which Aminoglycosides has a diff source of origin from d others?

A

Gentamicin

25
Q

What’s Gentamicin from?

A

Micromonospora purpurea

26
Q

Why’s Gentamicin useful as a broad spectrum for difficult pathogens?

A

Some targets for enzyme inactivation are missing.

T/4 resistance may not dev so rapidly

27
Q

Are Aminoglycosides clinically stable with B-lactams?

A

No.

Admin separately I.e. not in the same vial, but they can be admin same time

28
Q

Which Aminoglycosides is never used systemically?

A

Neomycin sulfate.

Only used topically

29
Q

Which Aminoglycosides can be used to lower cholesterol?

A

Neomycin sulfate

30
Q

Main use of Parmomycin sulfate

A

Used PO for suppression of gut flora and amoebic dysentery (Entamoeba Histolytica)

31
Q

What’s unique about Spectinomycin hydrochloride?

A

Unusual tricyclic ring

Only bacterioSTATIC Aminoglycosides

32
Q

What’s the primary use of Spectinomycin hydrochloride?

A

Used as a single bolus IM injection against PPNG (Penicillase Producing N. Gonorrhoeae)

33
Q

Any significant SE for Spectinomycin?

A

No significant Ototoxicity or nephrotoxicity when used as a single bolus IM inj

34
Q

Which Aminoglycosides is given as a single IM bolus injection for the treatment for PPNG?

A

Spectinomycin