Pharmacology Flashcards

1
Q

Ceftriaxone?

A
  • High binding to albumin
  • Needs to be given as continuous infusion
  • Concentration require to be above MIC
  • It can be given once a day as free fraction is released slowly from albumin
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2
Q

Digoxin for AF ?

A

Not the first choice of drug as it can induce ventricular arrhythmia.

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3
Q

Isoprenaline?

A

Acts mostly on B1 & B2 receptors.

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4
Q

What is pharmacokinetics ? Components?

A

This is what the body does to the drugs

  • Absorption
  • Distribution
  • Metabolism
  • Excretion / Elimination
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5
Q

What is pharmacodynamics?

A

This what the drug does to the body e.g; MIC of bacteria

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6
Q

Consideration of antibiotics? Components?

A
  • Drug
  • Bug
  • Patient
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7
Q

Patient factors affecting antibiotics?

A
  • Organ perfusion
  • Volume of distribution
  • Clearance
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8
Q

Factors affecting pharmacokinetics of drugs ?

A
  • Low albumin
  • Altered volume of distribution
  • Augmented renal clearance
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9
Q

Augmented renal clearance occurs in ?

A
  • Young trauma patients
  • Burns
  • Sepsis
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10
Q

Antibiotics modes of action?

A
  • Cell wall ( Beta-lactam, Vancomycin)
  • DNA/RNA synthesis (Fluoroquinolones, Rifamycins)
  • Folate synthesis (Trimethoprim, Sulfonamides)
  • Cell membrane (Daptomycin)
  • Protein synthesis ( Linezolid, Tetracycline, Macrolides & Aminoglycosides)
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11
Q

Mechanisms of antibiotic resistance ?

A
  • Efflux (Fluoroquinolones, Aminoglycosides, Tetracyclines, B-lactams & Macrolides)
  • Immunity & bypass (Tetracycline, Trimethoprim, Sulfonamides, Vancomycin)
  • Target modification ( Fluoroquinolones, Rifamycins, Vancomycin, Penicillin, Macrolides & Aminoglycosides)
  • Inactivating enzymes (B-lactams, Aminoglycosides, Macrolides & Rifamycins)
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12
Q

MIC? Minimal inhibitory concentration

A

This is the concentration at which there is no more growth of bacteria. Relates to Pharmacodynamics

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13
Q

Examples of Beta-lactam antibiotics?

A
  • Penicillins
  • Cephalosporins
  • Carbapenems
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14
Q

Mechanism of action of antibiotics in relation to MIC ?

A
  • Work by time above MIC (Beta-lactam)

- Work by peak divided by MIC (ex. Gentamicin)

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14
Q

Mechanism of action of antibiotics in relation to MIC ?

A
  • Work by time above MIC (Beta-lactam)
  • Work by (concentration) peak divided by MIC (ex. Gentamicin) - i.e peak above MIC ratio
  • Concentration & time dependent (AUC/MIC)
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15
Q

Resistant bacteria in relation to MIC?

A
  • MIC is higher in resistant bugs

- At least 4 times the MIC

16
Q

Antibiotics - Time dependent ?

A
  • Bata-lactam
  • Carbapenem
  • Linezolid
17
Q

Antibiotics - Concentration dependent?

A
  • Aminoglycosides
  • Metronidazole
  • Fluoroquinolones
18
Q

Antibiotics - Time & Concentration dependent ? AUC:MIC

A
  • Fluoroquinolones
  • Aminoglycosides
  • Glycopeptides (Vancomycin)
  • Tigecycline
19
Q

Antibiotics according to duration above MIC?

A

Carbapenems < Penicillin < Cephalosporins

Thus cephalosporins is the longest in time above MIC and Carbapenems shorter

20
Q

Antibiotics according to duration above MIC?

A

Carbapenems < Penicillin < Cephalosporins

Thus cephalosporins is the longest in time above MIC and Carbapenems shorter

21
Q

Measurement of peak levels of antibiotics is for ?

A

Efficacy

22
Q

Measurement of trough levels of antibiotics is for ?

A

Toxicity

23
Q

What are the determinants of Pharmacokinetics?

A
  • MW
  • Lipid solubility
  • Protein binding
  • Elimination pathways
24
Q

Factors affect pharmacokinetics of drugs ?

A
  • Clearance
  • Volume of distribution
  • Half life
  • Cmax
  • Cmin
  • AUC (0-24)
25
Q

What is clearance?

A

Volume of blood cleared of the drug per unit time

26
Q

What is volume of distribution?

A

The apparent volume of fluid that contains the total drug dose administered at the same concentration as in the plasma.

27
Q

What is half-life?

A

This is the time required for plasma drug concentration to decrease by half

28
Q

What antibiotics are concentration dependent? Cmax/MIC

A
  • Aminoglycosides
  • Metronidazole
  • Fluoroquinolones
29
Q

Antibioitcs which are concentration dependent with time dependent? AUC24/MIC

A
  • Fluoroquinolones
  • Azithromycin
  • Tetracyclines
  • Glycopeptides
30
Q

Time dependent antibiotics T > MIC

A
  • Beta-lactams
  • Carbapenems
  • Linezolid
  • Erythromycin
  • Clarithromycin
  • Clindamycin
31
Q

List hydrophilic antimicrobials?

A
  • Aminoglycoside
  • Beta-lactam (Carbapenem, Cephalosporins, Penicillin)
  • Glycopeptides
  • Lipopeptides
32
Q

List of lipophilic antimicrobials?

A
  • Fluoroquinolones
  • Ketolides
  • Lincosamides
  • Macrolides
  • Metronidazole
  • Streptogramins
  • Tetracycline
33
Q

DIstribution and clearance of lipophilic antimicrobials?

A
  • Tissue distribution limited to extracellular space
  • Renal clearance
  • In sepsis - Need for increased loading dose / Need for increased or decreased maintenance dose
34
Q

Distribution and clearance of lipophilic antimicrobials ?

A
  • Tissue distribution with intracellular accumulation
  • Hepatic clearance
  • In sepsis - No need for increased Loading dose and maiintenance dose adjustment