Aminoglycodides Flashcards

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1
Q

Modes of antibacterial action : concentration dependent

A
  • 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

Plasma Level + = Kills bacteria faster

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2
Q

MODES OF ANTIBACTERIAL ACTION :
TIME DEPENDENT

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

MIC : Minimum Inhibitory Concentrations

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3
Q

MODES OF ANTIBACTERIAL ACTION : POSTANTIBIOTIC EFFECT

A
  • Aminoglycosides’ killing action continues when the plasma levels have declined below measurable levels
  • It is a phenomenon where the antibiotic continues to inhibit bacterial growth even after the drug has been removed.
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4
Q

MODES OF ANTIBACTERIAL ACTION : POSTANTIBIOTIC EFFECT

A
  • Greater efficacy when administered as a SINGLE LARGE DOSE than when given as multiple smaller doses
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5
Q

AMINOGLYCOSIDES : PHARMACOKINETICS

A
  • Structurally related amino sugars
    attached by glycosidic linkages
  • Polar compounds
  • Not absorbed orally
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6
Q

AMINOGLYCOSIDES : PHARMACOKINETICS

A
  • Given intramuscularly or intravenously
    for systemic effects
  • Limited tissue penetration
  • Do not readily cross the blood-brain barrier
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7
Q

Major mode of excretion

A

Glomerular Filtration

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8
Q

Plasma levels are affected by the changes of ?

A

Renal Function

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9
Q

Excretion is directly propotional to ?

A

Creatine Clerance

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10
Q

With normal Renal funtion, elimination half-life is ?

A

2-3 Hours

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11
Q

Dosage adjsutment must be made in__________to avoid_______?

A

Made in Renal Insufficiency to avoid Toxicity accumulation

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12
Q

Monitoring what levels is needed for safe anf effective dosage selection and adjustment ?

A

Plasma levels

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13
Q

Traditonal Dosing regiments ?

A

2 to 3 times a day

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14
Q

When is the Peak serum levels ?

A

30-60 minuties after administering

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15
Q

Trough serum levels

A

Refers to the lowest concentration of a drug in the bloodstream, reached just before the next dose is administered.

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16
Q

Bactericidal

A
  • Substances that destroys microorganisms.
  • They are Irreversible inhibitors of protien synthesis
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17
Q

Penetration of bacterial cell wall is partly dependent on ?

A

O2 dependent active transport

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18
Q

Transport is enhanced by ?

A

Cell wall synthesis inhibitors
- Due to the accumulation of intermediates in the cell wall synthesis pathway, which increases the concentration of substrates available for transport

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19
Q

Bactericidal

A

Kills the bacteria.
● Something like suicide or homicide
● Actually kills the intended bacteria

20
Q

Minimum Inhibitory Concentration

A

The lowest concentration of an antimicrobial (like an antifungal, antibiotic, or bacteriostatic) drug that will inhibit the visible growth of a microorganism after overnight incubation.
● In-vitro quantitative measure of how much concentration of antibiotic will be able to inhibit the growth of bacteria.

21
Q

Selective Toxicity

A

The aim of antimicrobial therapy is TO KILL or INHIBIT the INFECTIVE ORGANISIM WITHOUT DAMAGING THE HOST.

22
Q

Bacteriostatic

A

Prevents the growth of bacteria.
- Does not kill bacteria but it prevents its reproduction, thereby allowing the immune system to take over.

23
Q

ANTIMICROBIALS

A
  • Drugs that inhibit the growth/replication or kill microorganisms.
    ○ Antibacterial
    ○ Antifungal
    ○ Antiviral
    ○ Antiprotozoal
    ○ Antiparasitic
24
Q

BACTERIAL STRUCTURE

A

○ Cell membrane
○ Nucleus (no nuclear membrane, but has nucleoid structure to contain their chromosomes)
○ Fmbriae
○ Pili
○ Some may develop a capsule

25
Q

Cell membrane

A

Composed of lipid bilayer so it can easily be disrupted with substances that can disrupt the hydrophobics of this structure such as alcohols.

26
Q

Cell wall: Carbohydrate-based

A

For bacteria, it is peptidoglycan (has protein and peptide but mostly composed of carbohydrates).

27
Q

Aminoglycosides binds to ____ S ribosomal unit ?

A

30S ribosomal unit

28
Q

Aminoglycosides interfere with protein synthesis like :

A
  1. Blocks formation of initiation complex
  2. Inhibit Translocation
  3. Causes misreading of the code on the mRNA template
29
Q

Aminoglycosides mechanisim of resistance :

A

Resistant due to failure to penetrate into the cell
Examples are :
Streptococci, including S. pneumoniae
Enterococci

30
Q

Clinical Uses : Gentamicin, Tobramycin, Amikacin

A

Serious infections caused by Aerobic
gram (-) bacteria

Providencia (Pseudomonas)
E. coli (Enterobacter)
Klebsiella (Proteus)
Serratia

**GAT = PEKS **

31
Q

Gentamicin, Tobramycin, Amikacin
Used for the following but is not the drug of choice:

A

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

32
Q

Anti-bacterial Synergy

A

if Combined with Penicillin in the treatment
- Pseudomonal Infections
- Listerial Infections
- Enterococcal Infections

Antibiotics + Penicillin = PLE

33
Q

Streptomycin

A

For :
- Tubercolosis
- Plague
- Tularemia
- Multi-Drug-Resistance (MDR) straibs of M. tb resistanct to streptomycin maybe susceptible to amikacin

34
Q

Neomycin, Kanamycin, Paromycin

A

Topical - Neomycin
IM/IV/PO (Orally) - Kanamycin, Paromycin

Active against :
Gram possitive bacteria
Gram negative bacteria
some mycobacteria

Resistant: P aeruginosa, Streptococci

35
Q

Netilmycin

A
  • IM/IV/Topical/Ocular/Intrathecal
  • Reserved for serious infections resistant
    to other aminoglycosides

Intrathecal : administered into the spinal theca

36
Q

Spectinomycin

A

Aminocylitol related to aminoglycosides
* Back-up drug
*Intramuscular as single dose for Gonorrhea
* NOT recommended for treatment of pharyngeal gonococcal infections

37
Q

Toxicity

OTOTOXICITY

A

Auditory or Vestibular damage (or both) maybe
irreversible.

Auditory impairment
- Amikacin and Tanamycin

Vestibular dysfunction
- Gentamicin and Tobramycin

38
Q

OTOTOXICITY

A
  • The risk is proportionate to the plasma levels
  • HIGH if the dosage is not modified in renal dysfunction
  • Increased with the use of loop diuretics
  • Contraindicated during pregnancy

Contraindictated : not advised as a course of treatment

39
Q

NEPHROTOXICITY

A
  • Causes Tubular Necrosis
  • Cause Liver damage
  • It is Reversible
    **- Most Nephrotoxicity **
  • Gentamicin
  • Tobramycin

Gentamicin : Treatment both gram-positive and gram-negative infections, Aerobic Infections.
Tobramycin : Treatment both gram-positive and gram-negative infections, Aerobic Infections.

Both are used to treat Pseudomonas aeruginosa in people diagnosed with cystic fibrosis.

40
Q

NEPHROTOXICITY

A
  • Most common in ELDERLY PATIENTS
  • also patients **concurrently receiving **
  • Am/pho/te/ri/cin B
  • Ce/pha/lo/spoh/orins
  • Van/co/mycin

Amphotericin B : Anti-Fungal
Cephalosporins : Bacterial Antibiotics
Vancomycin : Glycopeptide antibiotic

41
Q

NEUROMUSCULAR BLOCKADE

A
  • Rarely Happens
  • Curare-like block may occur at high doses
  • Causes Respiratory Paralysis
  • It is REVERSIBLE
42
Q

Neuromuscular Blockade Treatment

A
  • Calcium
  • Neostigmine
  • Ventilatory Support
43
Q

Minimum Inhibitory Concentration (MIC)

A
  • The lowest concentration of a chemical that prevents visible growth of bacteria or fungi.
44
Q

When is Trough Serum Levels Measured ?

A

Measured just before the next dose

45
Q

Bacteriostatic

A
  • Substances that inhibits microbial growth.