Pharm 4 - Pharmacokinetics and Drug Metabolism Flashcards

1
Q

State the 5 stages of the journey of a drug through the body.

A
Administration
Absorption
Distribution
Metabolism
Excretion
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2
Q

What is the difference between enteral and parenteral administration?

A
enteral = using GI tract
parenteral = everything but the GI tract
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3
Q

What are the advantages of IV administration?

A

Rapid + high bioavailability

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4
Q

State two ways in which drug molecules move around in the body.

A

Bulk Flow Transfer

Diffusion transfer

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5
Q

State 4 ways drugs can cross lipid membrane barriers.

A

Diffusion through lipid membrane if lipid enough
Diffusion across aqueous pores
carrier moleculues
pinocytosis

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6
Q

Most drugs are either …

A

weak acids or weak bases

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7
Q

Which factors affect the ratio of ionized to non-ionised drug?

A

pKa of the drug

pH of the environment

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8
Q

Describe and explain the difference in absorption of aspirin in the stomach and in the small intestine.

A

Aspirin has a pKa of 3.4
in the acidic conditions of stomach, aspirin takes an unionised form.
because it is unionised it is rapidly absorbed.

in the small intestine, the pH is much more basic, higher pKa than the pKa of aspirin. So aspirin exists in an ionised form. This is not absorbed quickly.

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9
Q

What is ion trapping?

A

Some ionised aspirin will enter systemic circulation
there it will exist in an ionised form
because it is ionised it cannot move into tissues

therefore ‘trapped’

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10
Q

State 4 factors affecting drug distribution

A

Regional blood flow
extracellular binding
capillary permeability
localisation in tissues

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11
Q

In which state can albumin bind to drugs, ionised or non-ionised?

A

Both

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12
Q

State three types of capillary architecture.

A

Continuous
Fenestrated
Discontinuous

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13
Q

Give a broad example of localisation of a drug in tissue.

A

Lipophilic drugs tend to localise in fatty tissue e.g. brain and testes

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14
Q

What are the two main routes of drug excretion?

A

Kidneys - main

Liver

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15
Q

What type of molecules tend to get excreted via the biliary route?

A

Large molecular weight molecules

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16
Q

Via what form of molecular movement do most drugs tend to get excreted into the urine?

A

Active secretion

17
Q

What happens to drug-protein complexes at the glomerulus?

A

Not filtered into the filtrate

18
Q

Where does active secretion of acids and bases occur in the nephron?

A

Proximal Convoluted Tubules

19
Q

What can happen to lipid soluble drugs in the proxiaml and distal convoluted tubules?

A

Could be reabsorbed

20
Q

Why might treatment with iV sodium bicarbonate increase aspirin excretion?

A

IV sodium bicarbonate will increase pH of blood

so aspirin is more ionised and more water soluble so more likely to be excreted by kidneys

21
Q

What is the main purpose of the active transport systems that secrete drugs into the bile?

A

There to excrete bile acids but drugs can hitch a ride

22
Q

What is a potential problem with biliary excretion of xenobiotics?

A

enterohepatic cycling - reabsorbed

23
Q

Define bioavailabily.

A

The proportion of the administered drug that is available within the body to exert its pharmacological effect

24
Q

Define apparent volume of distribution

A

the volume in which a drug appears to be distributed

25
Q

Define biological half life

A

time taken for the concentration of a drug to fall to half its original value

26
Q

Define clearance

A

Volume of plasma cleared of drug per unit time

27
Q

Define first order kinetics

A

when the rate of excretion of a drug is proportional to the concentration remaining within the body

e.g. more drug in body = more excretion

28
Q

Define zero order kinetics

A

Constant amount of the drug is removed from the body per unit time

29
Q

What does zero order kinetics suggest about the enzymes involved?

A

Saturated