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Y2 Pharmaco > Tetracyclines & Aminoglycosides > Flashcards

Tetracyclines & Aminoglycosides Flashcards

(43 cards)

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1
Q

Name the 3 Tetracyclines

A
  1. Tetracycline
  2. Doxycycline
  3. Minocycline
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2
Q

What do Tetracyclines cover/effective against?

A

Broad spectrum (gram pos & negs) & some atypical bacteria

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3
Q

What are the 3 atypical bacteria?

A
  1. Mycoplasma
  2. Legionella
  3. Chlamydia
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4
Q

Diff between bacteriocidal and bacteriostatic

A

Bacteriocidal - kills bacteria
Bacteriostatic - arrests bacteria (only)

E.g. aminoglycosides are bacteriocidal unlike tetracyclines that are bacteriostatic

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5
Q

Name the 3 categories of protein synthesis inhibitors (30S)

A
  1. Tetracyclines
  2. Glycylcycline
  3. Aminoglycosides
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6
Q

Administration of Tetracyclines.

A

Good oral bio-availability => mostly oral admininstration

  • can actl be administered IV but unnecessary lah
  • mostly manufacture in oral forms too
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7
Q

Tetracyclines are similar to Fluoroquinolones in what sense..

A

Cannot be taken w dairy pdts, such as milk

  • or other substances that contain divalent & trivalent cations
  • e.g. Mg or Al antacids or Fe supplements
  • forms non absorbable chelates that decreases absorption
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8
Q

Tetracyclines have inadequate activity against..

A
  1. Pseudomonas aeruginosa
  2. Proteus
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9
Q

Can Tetracyclines be used during pregnancy?

A

big no.
- category D in pregnancy

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10
Q

Which Tetracycline is best for CNS treatment?

A

Doxycycline

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11
Q

Tetracycline (specifically) are eliminated and cleared via..

A

Renal elimination, excreted by kidney

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12
Q

Which tetracycline is effective against MRSAs?

A

Doxycycline

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13
Q

Which Tetracycline is metabolised by the liver before excretion?

A

Minocycline
- thus, tigecycline aslo eliminated via biliary/fecal route
- dose reduction reccomended in pxs w severe hepatic dysfunction

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14
Q

What are Glycylcyclines?

A
  • new class of AB derived from tetracyclines
  • structurally related to minocycline, but altered to 1. Larger spectrum of activity 2. Decreased susceptibility to development of bacterial resistance
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15
Q

Name the only glycylcycline approved for antibiotic use.

A

Tigecycline

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16
Q

What are the 2 common mechanisms of tetracycline resistance?

A
  1. Ribosomal protection
    - bugs produce proteins to prevent AB from binding to ribosomal subunit/displace AB from subunit
  2. Resistance mediated by acquired efflux pumps
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17
Q

How does Tigecycline work against Tetracycline resistant bacteria?

A
  1. Tigecycline modified to have higher affinity to the ribosomal subunit => doesnt get displaced by the proteins
  2. Tigecycline modified to not be a substrate for the bacterial efflux pumps
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18
Q

How is Tigecycline administered?

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A

Only parentally
- aka IV
- poor oral bioavailability

19
Q

Can Tigecycline be given during pregnancy?

20
Q

Elimination & clearance of Tigecycline?

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A

Biliary elimination, Fecal excretion

  • thus, no dosage adjustments needed for pxs w renal impairment
  • dose reduction reccommended in severe hepatic dysfunction
21
Q

Tigecycline is not active against..

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A
  1. Pseudomonas species
  2. Proteus
22
Q

Can Tigecycline be used against MRSA?

23
Q

Can Tigecycline be used against ESBLs?

Study These Flashcards
A

Yes.
- can be used against extended-spectrum β-lactamase producing gram neg bacteria
- useful against carbapenem resistant strains

24
Q

Can Tigecycline be used against Vancomycin-resistant enterococci (VRE)?

25
List the indications for/coverage of Tigecycline.
1. MRSA (staphylococci) 2. Multidrug-resistant streptococci 3. Vancomycin-resistant enterococci(VRE) 4. ESBL + carbapenem resistant strains 5. Community acquired pneumonia
26
Briefly list the adverse effects of Tetracyclines & Tigecycline.
1. Gastric discomfort (oesophageal irritation & ulceration) 2. Effects on calcified tissues (staining of teeth, hypoplasia of teeth) 3. Phototoxicity 4. Superinfections e.g. CDAD, thrush 5. Hepatotoxicity 6. Vestibular dysfunction 7. Renal (accumulation of tetracycline in px w pres-existing renal disease)
27
What the effects of Tetracyclines & Tigecycline on the GIT? + how shd the px be advised?
Gastric discomfort - esophageal irritation common - drug shd be eaten on empty stomach - drink plenty of water to reduce esophageal ulceration - do not lie down aft intake of drug
28
Patients on Tetracycline & Tigecycline are at risk of CDAD, why?
Tetracycline & Tigecycline are broad-spectrum ABs => **prolonged use** may cause superinfections as they wipe out all bacteria => e.g. thrush, CDAD, etc (fungal & bacterial superinfections)
29
Use of Tetracycline & Tigecycline may cause _______toxicity & _______toxicity.
Phototoxicity & Hepatotoxicity. - advise px to wear sunscreen and protective eyewear - to protect against severe sunburn
30
List the contraindications of Tetracyclines & Tigecycline.
Not to be used in: 1. pregnant/breast-feeding women or in children less than 8 yrs of age 2. Last half of pregnancy => affects primary teeth 3. Children up to 7/8 yrs => can affect perm teeth (yellow-gray-brown discolouration)
31
What are the 6 NOs for Aminoglycosides.
1. No protein synthesis (inhibition @ 30S ribosomal subunit) 2. Mainly aerobic **N**egative **O**rganisms (spectrum) 3. No during pregnancy 4. No oral administration 5. No CSF penetration 6. **N**ephro & **O**to toxicitiy
32
How are Aminoglycosides cleared and excreted
Renal clearance, excreted thru urine - will need dose adjustment in pxs w renal impairment
33
What does Aminoglycosides not cover?
Anaerobes. - req oxygen for active transport across inner membrane
34
List the 5 Aminoglycoside drugs.
1. Gentamicin 2. Streptomycin 3. Tobramycin 4. Amikacin 5. Neomycin
35
Aminoglycosides cannot be used in anaerobes, why?
1. Aminoglycosides need/are transported across inner membrane via active transport 2. Energy-dependent phase => requires oxygen for pdn of energy 3. Cannot occur under anaerobic conditions.
36
Aminoglycosides are frequently used for __________ therapy for serious infections.
Empiric therapy. - dk what the bug is, prescription of broad spectrum AB is solely calculated decision of observed symptoms - while on empiric therapy, identification of bug occurs - once bug is identified, step down & give targeted therapy
37
Aminoglycosides are primarily effective against..
**aerobic** gram neg bacteria & mycobacteria - acts synergistically with beta lactams against gram pos bacteria
38
Briefly list the 5 adverse effects of aminoglycosides.
1. Ototoxicity - deafness in ear 2. Nephrotoxicity - retention of drug in kidneys 3. Neuromuscular paralysis - note in pxs w myasthenia gravis 4. Hypersensitivity rxns (skin rash) 5. Contraindicated in pregnancy, Cat D
39
Administration of Aminoglycosides
IV/IM
40
Patients prescribed w Aminoglycosides should be tested/monitored for..
1. avoid usage w other nephrotoxic drugs e.g. amphotericin B, vancomycin, NSAIDs & neuromuscular blocking agent 2. therapeutic drug monitoring - peak & trough levels monitored to ensure no accumulation 3. renal function tests - urea, creatinine, electrolytes 4. precautionary measures to be taken when given to pxs w **renal impairment, hearing defects & myasthenia gravis**
41
Resistance to aminoglycosides can occur via
1. increased efflux pumps to reduce effective intracellular concentrations 2. gram neg bacteria produce aminoglycoside inactivating enzymes 3. alteration of 30S ribosomal subunit 4. inhibition of aminoglycoside uptake by bacteria
42
Aminoglycosides are first line for..
First line defence tx for multi-drug resistant (MDR) tuberculosis (mycobacterium tuberculosis
43
Aminoglycosides mostly effective against..
Bacteria that are 1. Aerobic & 2. Gram negs - enterobacteriaceae - klebsiella & e.coli - MDR microbes such as pseudomonas & acinetobacter - is first line against MDR tuberculosis - empiric therapy for serious infections such as epticemia, complicated UTIs, nosocomial RTIs - less effective in anaerobic environments such as abscess or infected bone - also act synergistically w b-lactams against certain gram +ve bacteria

Y2 Pharmaco (22 decks)

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