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Drug Development > Clinical studies to measure pharmacokinetics > Flashcards

Clinical studies to measure pharmacokinetics Flashcards

1
Q

Why is Pharmacokinetics important in drug development?

A

Enables us to find out how safe and efficacious a drug is.

They also help determine drug dose and dosing schedules.

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2
Q

What is pharmacokinetics

A

the movement of drugs in the body.

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3
Q

What is the importance of pre-clinical studies?

A

used to predict safety and efficacy of drugs in animal studies.

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4
Q

What are the two disciplines of pre-clinical trials

A

Toxicology and general pharmacology

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5
Q

Why are pharmacokinetic studies important?

A

ADME parameters
safety and efficacy
Helps to determine the half -life of a drug (prediction of drug safety profile)

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6
Q

Why is plasma concentration important?

A

An important predictor of drug effect

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7
Q

What are the key determinants of plasma concentration?

A

Absorption
Distribution
Metabolism
Excretion

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8
Q

What is clearance?

A

metabolism and excretion

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9
Q

Where can PK information be summarised?

A

Investigator brochure

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10
Q

List the effects of PK on physiology (ADME):

A

GI tract (A,M)
Liver (M,E)
Kidneys (M,E)
Blood/Blood flow (D, protein binding)

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11
Q

what is the effect of decreased kidney function on PK?

A

Decreased elimination and protein binding

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12
Q

what is the effect of intestinal disease on PK?

A

Impaired absorption

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13
Q

what is the effect of liver disease on PK?

A

decreased first pass metabolism and elimination.

fluid retention

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14
Q

what is the effect of congestive heart failure?

A

decreased GI absorption and elimination.

altered volume of distribution

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15
Q

what is the effect of ageing on PK?

A

decreased first pass metabolism, protein binding, hepatic and renal excretion.

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16
Q

what does the rate and extent of distribution depend on?

A

Blood flow
active transport. diffusion
plasma protein binding (albumin) tissue binding
disease

17
Q

what is the distribution of plasma?

A

5% proportion of total body fluid.

18
Q

what is the distribution of interstitial fluid?

A

15%

19
Q

what is the distribution of intracellular fluid?

A

35%

20
Q

what is the distribution of intracellular fat?

A

20%

21
Q

What is the aim of drug metabolism?

A

to decrease drug activity.

to convert lipid soluble drugs into more polar water soluble metabolites to be excreted in bile or urine.

22
Q

where does drug metabolism take place

A

in the liver as phase 1 and 2 reactions

23
Q

what drug is an exception to liver metabolism?

A

codeine

Gut wall have enzymes that contribute to metabolism (CYP450)

24
Q

what is phase 1 metabolism?

A

converting molecules into simpler forms

25
Q

what is phase 2 metabolism?

A

conjugation, making molecules more water soluble.

26
Q

what enzymes are involved in metabolism phase 1?

A

monoamine oxidase

alcohol dehydrogenase

27
Q

what are the routes of excretion?

A

kidney
Biliary
sweat/breath/breastmilk

28
Q

what is renal excretion?

A

Glomerular filtration proximal tubule

proximal and distal tubules

29
Q

what is biliary excretion?

A

active transport/secretion e.g. Rifampicin

Into Bile and Faeces

30
Q

what are the parameters for plasma concentration?

A

Cmax = max conc.
Tmax = time taken to reach max conc.
t1/2 (half-life) = time taken for drug conc. to fall by 1/2
area under the curve

31
Q

what does the area under the curve signify?

A

the total amount of drug the system is exposed to for the entire time course

32
Q

what are the conceptual parameters?

A

clearance
bioavailability
volume of distribution

33
Q

what is bioavailability?

A

proportion of drugs reaching systemic circulation

34
Q

what are the factors influencing bioavailability

A

pharmaceutical preparation
physiochemical interaction
patient factos
1st pass metabolism

35
Q

What is the investigator brochure?

A

a comprehensive summary of the preclinical and clinical pharmacology data for the investigational medicinal product (for first in human trial, there will be no clinical data available).

36
Q

What is the investigational medicinal product dossier?

A

It contains information related to the quality, manufacture and control of the investigational medicinal product.

Drug Development (10 decks)

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