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MPharm 2 - PH2114 > Unit 2 - ADME - PK > Flashcards

Unit 2 - ADME - PK Flashcards

1
Q

What does pharmacokinetics describe?

A

The relationship between dose and concentration

- changes with time

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2
Q

What underpins the relationship between dose and therapeutic benefit?

A

Pharmacokinetics
- how body manages drug
Pharmacodynamics
- how the drug affects the body

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3
Q

What physiochemical properties underpin pharmacokinetics and pharmacodynamics to determine patient outcomes?

A 
Solubility in biological fluid
Permeation across biological barriers
Metabolism by enzyme
Secretion by transporters
Interaction with pharmacologic receptor
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4
Q

What is ADME?

A

Mechanisms of how drugs interact with, and are handled by, the body

  • absorption
  • distribution
  • elimination
  • metabolism
  • excretion
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5
Q

What is Absorption in ADME?

A

Process by which unchanged drug proceeds from ‘absorptive barrier’ to circulatory system

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6
Q

What is Distribution in ADME?

A

Process of drug transfer from immediate post-absorption site to tissues

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7
Q

What is Elimination in ADME?

A

Process of irreversible loss of drug from the body via

  • metabolism
  • excretion
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8
Q

What is pharmacokinetics?

A

Quantitative descriptors determined from plasma drug concentration vs time profiles which are used to characterise the drug and predict outcome of drug administration

  • clearance of drug from body (CL)
  • volume of distribution of drug within body (V)
  • elimination half life (T1/2) of drug from body
  • bioavailability (F)
  • fractional availability of dose
  • 0 - 1
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9
Q

What is Disposition in ADME?

A

Distribution
Metabolism
Excretion

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10
Q

What types of biological barriers do drugs need to cross?

A 
Plasma membranes
- lots of different types
Epithelium
- intestinal cells
- enterocytes
Capillary endothelium of vascular beds
- different types
- GI tract
- Blood Brain Barrier
- respiratory system
Transporters
Enzymes
Protein binding
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11
Q

Which processes occur concurrently in the body?

A

ADME

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12
Q

Give examples of formulations which are taken orally?

A

Tablets
Capsules
Emulsions
Suspensions

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13
Q

What are oral formulations subjected to?

A

Hepatic first pass metabolism before distribution

- absorbed into GI tract

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14
Q

Give examples of formulations that enter the bloodstream via the respiratory system

A

Spray
pMDI
DPI
Nebuliser

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15
Q

Give examples of formulations that enter the bloodstream via the skin

A

Patch
Cream
Ointment
Microneedles

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16
Q

Give examples of formulations that enter the bloodstream directly

A 
Implants
- release drug over time
Intravenous injection
Intramuscular injection
Subcutaneous injection
Intradermal injection
17
Q

What role does the circulatory system play regarding ADME?

A

Distribution of drugs around the body

  • opportunity to reach target
  • interact with tissues
  • be eliminated
18
Q

What does a single IV bolus concentration-time profile show?

A 
No absorption phase
Disposition only
- Distribution
- Metabolism
- Excretion
19
Q

What does a continuous IV infusion concentration-time profile show?

A 
Input controlled
No absorption
Disposition only
- Distribution
- Metabolism
- Excretion
20
Q

What does an intermittent IV infusion concentration-time profile show?

A 
Input controlled
No absorption
Disposition only
- Distribution
- Metabolism
- Excretion
21
Q

What does an extravascular single dose concentration-time profile show?

A 
Absorption
Disposition
- Distribution
- Metabolism
- Excretion

sharp Increase in plasma concentration then steady decrease as it gets elimniated

22
Q

What does an extravascular multiple dose concentration-time profile show?

A 
Absorption
Disposition
- Distribution
- Metabolism
- Excretion

fluctuation in plasma concentration but gradually increasing until steady state

23
Q

What is achieved after 5 doses of medication?

A

Steady state

may vary depending on half lives and rate of absorbtion

24
Q

What is the principle of therapeutic drug monitoring?

A

Therapeutic and toxic effects related to concentration

Knowledge of measured drug levels can influence management

25
Q

Why is Therapeutic Drug Monitoring important?

A

Concentration related effects of drug either of lack of efficacy or toxicity are not easily assessed, identified or differentiated early enough by clinical signs alone
Concerns on patient adherence
- are they going to keep taking it
Inter-individual PK variability associated with narrow therapeutic window

MPharm 2 - PH2114 (32 decks)

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