Lecture 2 Flashcards

1
Q

What does ADME stand for in pharmacokinetics?

A

Absorption Distribution Metabolism Elimination

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2
Q

What is volume of distribution?

A

how well a drug is distributed throughout the body based on the concentration of drug in the blood

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3
Q

Would a drug with high lipid solubility and tissue have a high or low Vd

A

High volume of distribution e.g. amitriptyline (anti-depressant)

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4
Q

Would a drug with low lipid solubility and tissue binding have a high or low Vd?

A

Low volume of distribution e.g. warfarin (anti-coagulant)

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5
Q

What is clearance?

A

Virtual volume of blood cleared of drug per unit time

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6
Q

What is total body clearance the sum of?

A

Sum of all clearances occurring simultaneously by different organs in the body

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7
Q

What is creatine?

A

A breakdown product of creatine phosphate in muscles

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8
Q

Why do we measure creatine clearance?

A

Creatinine clearance is a marker for renal function and reflects drug clearance efficiency.

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9
Q

What are the two ways of measuring clearance?

A
  • single blood sample
  • renal clearance= urine collection over 24 hours
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10
Q

How does creatine clearance change with age?

A

Decreases with age

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11
Q

Define first order elimination

A

amount of drug eliminated per unit time is proportional to concentration, constant % of drug eliminated per unit time

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12
Q

What is the elimination rate? (Kel)

A

Proportion of drug eliminated per unit time

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13
Q

What does the elimination rate tell us?

A

Provides a calculation of the time needed to eliminate a proportion of drug

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14
Q

What is the time constant? (1/Kel)

A

Time taken for the concentration to fall to 1/e~ 37%

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15
Q

Define half-life

A

The time required for the amount of drug in the body to decrease by 50%

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16
Q

Can the same drug with two different starting doses have the same half life?

A

Yes

17
Q

What do we use the half life to determine?

A

The dosing interval- the set dosing interval is one half life

18
Q

What is AUC a measure of?

A

A measure of amount of drug absorbed

19
Q

Why would you use a loading dose?

A

For acute conditions e.g. status asthmaticus, quickens therapeutic effect of drugs with long, slow half lives

20
Q

Why would you use a continuous infusion?

A
  • maintains an effective constant plasma drug concentration through equilibrium - prevents toxicity that might occur if the drug is presented too quickly
21
Q

Define zero order kinetics

A
  • constant amount of drug is eliminated per unit time - rate of elimination is independent of plasma drug concentration
22
Q

What does half life depend on?

A

Starting concentration

23
Q

Why must dose adjustments be made for neonates?

A
  • reduced body volume - higher proportion of body is water - less plasma albumin - low renal function - low metabolism
24
Q

Why must dose adjustments be made for the elderly?

A
  • high proportion of fat - less plasma albumin - reduced renal function - low metabolism
25
Q

What is the purpose of therapeutic drug monitoring?

A
  • measure concentration of drug in the body - determine most effective dose or avoid toxicity
26
Q

Examples of drugs that are therapeutically monitored

A
  • cardiac drugs e.g. dioxin - antibiotics e.g. aminoglycosides - antiepileptics e.g. phenytoin - psychiatric drugs e.g lithium
27
Q

Would we measure peak or trough drug concentration to make sure a drug reaches a certain level?

A

Peak

28
Q

Would we measure peak or trough drug concentration to make sure a the drug remains effective?

A

Trough

29
Q

Why do we use urine samples?

A
  • do not need blood sample - useful for drugs which are fully/partially eliminated in the urine
30
Q

Why do we not measure drug concentration in urine?

A

Urine volume is variable and differences affect the total drug concentration depending on (de)hydration