2: Drug movement in the body Flashcards

1
Q

What are the four processes making up the fates of drugs in the body?

A

Absorption

Distribution

Metabolism

Excretion

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2
Q

What is absorption?

A

Process by which drugs enter the body from their site of administration

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3
Q

What is distribution?

A

Movement of drug from site of administration, through the bloodstream, and into the tissues

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4
Q

What is metabolism of a drug?

A

Conversion of active drug to a less active form by enzymes

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5
Q

Where does drug metabolism usually occur?

A

Liver

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6
Q

What is excretion of a drug?

A

Removal of drug from the body

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7
Q

Where does drug excretion usually occur?

A

Kidneys

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8
Q

In which two organs are ingested drugs absorbed?

A

Stomach

Small intestine

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9
Q

By which circulation do ingested drugs reach the liver?

A

Portal circulation

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10
Q

Where do drugs go once they have been metabolised in the liver?

A

Kidneys for excretion

usually

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11
Q

Drugs with (high / low) lipid solubility will be absorbed more quickly.

A

high

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12
Q

Drugs with (high / low) lipid solubility will be absorbed slowly.

A

low

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13
Q

Can ions move easily across the phospholipid bilayer?

A

No

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14
Q

An acid (donates / accepts) protons.

A base (donates / accepts) protons.

A

Acids are proton donators

Bases are proton acceptors

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15
Q

Only the (ionic / unionised) forms of drugs move easily across the phospholipid bilayer.

A

unionised

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16
Q

How is pH calculated?

A

pH = -log10[H+]

17
Q

What is pKa?

A

Acid dissociation constant

i.e pH at which drug is 50/50 ionised/unionised

18
Q

Acidic drugs become (more / less) ionised in an acidic environment.

How does this affect their lipid solubility?

A

less

Greater absorption due to increased lipid solubility (unionised)

19
Q

Basic drugs become (more / less) ionised in a basic environment.

What effect does this have on their lipid solubility.

A

less

Greater absorption due to increased lipid solubility (unionised)

20
Q

Where does the overwhelming majority of absorption occur?

A

Small intestine

21
Q

What is motility?

A

Rate of stomach emptying and food movement through the intestines

22
Q

Apart from drugs, what affects gastrointestinal motility?

A

Presence of food in the GI tract (see satiation signals)

23
Q

In the presence of food, gastrointestinal blood flow (increases / decreases).

What cardiovascular condition can this cause?

A

increases

Angina

24
Q

What is oral availability?

A

The amount of drug which reaches the systemic circulation after oral ingestion

or

amount in system circulation / amount ingested

25
Q

What is systemic availability?

A

The fraction of drug which reaches the systemic circulation after absorption

or

amount in system circulation / amount absorbed

26
Q

What is the systemic availability (%) of IV drugs?

A

100%

27
Q

What is oral administration?

A

Ingestion by mouth

28
Q

What is sublingual administration?

A

Drug held under the tongue

29
Q

What is buccal administration?

A

Drug held against the inside cheek

30
Q

What is rectal administration?

A

Drug inserted via the rectum

31
Q

What is intravenous administration?

A

Drug administered via veins

32
Q

What is intramuscular administration?

A

Drug injected directly into muscle

33
Q

What is subcutaneous administration?

A

Drug administered under the skin

34
Q

What is inhalational administration?

A

Drug is breathed in (e.g nebulised salbutamol)

35
Q

What is transdermal administration?

A

Drug is applied to skin (e.g patches)

36
Q

What is topical administration?

A

Drug is applied to specific skin surfaces / mucous membranes

37
Q

Only (ionised / unionised) drugs move readily by diffusion.

A

unionised

because cell membranes are impermeable to ions.

38
Q

What is volume of distribution (Vd)?

What is the unit?

A

Amount of drug in body / Plasma concentration

Litres (L)