Pharmacokinetics (AS) Flashcards

1
Q

What is pharmacokinetics?

A

quantitative description of changes in conc of drug in body over time after dosing

ADME

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2
Q

interaction between fluoxetine and amitriptyline

A
  • fluoxetine increases plasma concentration of amitriptyline
  • fluoxetine inhibits metabolism of amitriptyline and inc its plasma conc

-> pharmacokinetic interaction

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3
Q

interaction between fluoxetine and tramadol

A
  • serotonin syndrome can occur
  • both inc availability of serotonin
  • happens without change in the conc of either drug

-> pharmacodynamic interaction

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4
Q

drugs that need regular pharmacokinetic monitoring

A
theophylline
lithium
methotrexate
ciclosporin
cardioselective agents (digoxin)
aminoglycosides (gentamicin)
anti-convulsants (phenytoin)
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5
Q

TDM

A

therapeutic drug monitoring

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6
Q

why to indicidualise dosage regimens

A
  • therapeutic index of drug is small
  • standard dose doesn’t always produce expected results
  • signs of toxicity may be hard to recognise
  • metabolites may be effective AND toxic
  • inter-patient variability factors
  • disease states can alter patients’ PD parameters
  • social habits can alter parameters
  • protein binding
  • non-compliance
  • overdoses
  • route of admin
  • drug interactions
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7
Q

drug that smoking effects

A

theophylline

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8
Q

factors that affact absorption of drugs

A
  • pH/surface tension
  • food/mucus/other drugs
  • emptying time
  • motility
  • disease
  • posture (maybe)
  • brand substitution
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9
Q

factors that affect distribution of drug

A
  • perfusion (blood supply)
  • binding (to R/plasma proteins)
  • membrane (can drug cross?)
  • drug (physiochem properties)
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10
Q

What does k stand for?

A

elimination rate constant

  • > FRACTION of drug eliminated per unit time
  • > unit = minute-1 or hr-1
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11
Q

What does K=0.25 per hour mean?

A

25% is eliminated from the body per hour

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12
Q

What does V stand for?

A

volume of distribution

-> hypothetical vomume of fluid in which the total amount of drug in the body would need to be distributed to give a conc equal to the conc measured in plasma

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13
Q

What does high vol of distribution mean?

A
  • drug distributes better to the peripheries
  • need large vol to contain the total amount of drug
  • distributes everywhere
  • will need go give a high dose of drug to get the plasma conc
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14
Q

How to calculate dose based on vol of distcibution?

A

conc required x V

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15
Q

vol of distribution for drug that binds tightly to tissues

A

high V

  • small proportion found in plasma
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16
Q

V for drug that binds tightly to plasma proteins

A

low V

-> large proportion found in plasma

17
Q

What is clearance (Cl)?

A

describes efficiency of irreversible elimination of drug from body

removal of drug from plasma in a given unit of time

18
Q

formula for clearance

A

Cl = K x V

elimination rate constant x vol of distribution

19
Q

2 most important parameters for determining drug pharmacokinetics

A

clearance

volume of distribution

20
Q

What is half life?

A

time taken for the conc of drug to be reduced by one half

21
Q

How many half lives for drug to be effetively eliminated?

A

approx 5 - 7 half lives

22
Q

equation for half life

A

half life = 0.693/k

ln2/k

23
Q

PK changes in elderly patients

A
  • altered absorption
    changes in distribution
  • hepatic metabolism
  • renal excretion
24
Q

PK changes in paediatrics

A
  • drug response
  • oral drug absorption
  • distribution
  • metabolism
  • excretion
25
Q

eooers withn TDM

A
  • assuming pt at seady state
  • assuming pt actuallt taking drug as prescribed
  • assuming pt receiving drug as prescribes
  • not knowing when drug conc measured in relation to dose administration
  • assuming pt is static and changes in condition don’t affect clearance
  • not considering drug interactions
26
Q

When does oraldose usually reach peak conc?

A

1-2hrs after oral dosei

26
Q

When does oraldose usually reach peak conc?

A

1-2hrs after oral dosei

27
Q

When does oral dose usually reach peak conc?

A

1-2hrs after oral dose

28
Q

what to suspect if a level is unusual

A
  • admin time not recorded accurately
  • dose administration error
  • blood drawn at incorrect time
  • blood drawn before steady state
  • blood drawn from wrong site
  • sample storage (degredation/haemolysis)