Pharmacokinetics Flashcards

1
Q

What is pharmacokinetics?

A

how the body affects a specific substance after administration

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What is drug absorption?

A

the passage of a drug from the site of administration into the plasma

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What is bioavailability?

A

the fraction of the initial dose that gains access to the systemic circulation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Name five sites of administration

A

Intra-venous
Oral
Inhalational
Dermal (Percutaneous)
Intra-nasal

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Which site of administration has 100% bioavailability?

A

Intra-venous

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

How can drugs travel around the body?

A

Bulk flow transfer (through bloodstream)
Diffusional transfer (molecule by molecule across lipid membranes)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What is pinocytosis?

A

Cell membrane forms vesicle which envelops drug and releases it on the other side of the membrane. Rarely used for drug transport

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

How do most drugs move across cell membranes?

A

Across lipid membranes or through transport proteins

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Which drugs can diffuse across lipid membranes?

A

Lipid soluble drugs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What are most drugs ?

A

Weak acids or weak bases

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What two forms can weak acids/bases exist as?

A

Ionised or unionised

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What happens to a weak acid in its ionised state?

A

Donates protons

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What happens to a weak base in its ionised state?

A

Accepts protons

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Which state is more lipid soluble: ionised or unionised?

A

Unionised

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What determines the state of the drug?

A

pKa (dissociation constant) and pH

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

When will a weak acid be more unionised?

A

When pH decreases (below its pKa)

17
Q

When will a weak base be more unionised?

A

When pH increases (above it’s pKa)

18
Q

Is drug distribution uniform?

A

No - different tissues will be exposed to different amounts of the drug

19
Q

How does regional blood flow affect distribution?

A

Different tissues receive differing amounts of the cardiac output.

More drug will be distributed to those tissues that receive most blood flow

20
Q

What happens to drugs once they enter systemic circulation?

A

They bind to plasma proteins

21
Q

What determines the amount of drug bound to plasma proteins?

A

The free drug concentration
The affinity for the protein binding sites
The plasma protein concentration

22
Q

Which drugs are more heavily bound to plasma proteins?

A

Weak acids

23
Q

How does the concept of tissue localisation apply to drug distribution?

A

Lipid soluble drugs will localise in lipid environments and water soluble drugs will localise in aqueous environments due to the drug equilibrium

24
Q

What is drug metabolism?

A

The conversion of drugs to metabolites that are as water soluble as possible and easier to excrete

25
Q

What is the major metabolic tissue?

A

The liver

26
Q

What are the main enzymes responsible for metabolism?

A

P450 enzymes

27
Q

What are the two phases of drug metabolism?

A

Phase 1 - add a reactive polar group by reduction, oxidation or hydrolysis

Phase 2 - add a substituent group to make the drug inactive and less lipid soluble

28
Q

What are prodrugs?

A

Drugs which require hepatic metabolism to become active

29
Q

What is an issue with oral drug administration?

A

They will be metabolised by the liver before they enter the systemic blood supply, leading to little active drug being circulated

30
Q

Name four routes of drug excretion

A

Via lungs
Via breastmilk
Via kidney (urine)
Via liver (bile)

31
Q

What are the three phases of excretion via the kidneys?

A

Glomerular filtration
Active tubular secretion
Passive diffusion across the tubular epithelium

32
Q

Which drugs are excreted by glomerular filtration

A

drugs under 20,000

33
Q

What is the most important method of drug excretion through the kidney?

A

Active tubular secretion through the proximal tubule, 80% of blood passes through here

34
Q

What does passive diffusion often lead to?

A

Reabsorption of particularly lipid soluble drugs

35
Q

Which factors influence reabsorption?

A

Drug metabolism - phase 2 metabolites are reabsorbed less

Urine pH - weak acids reabsorbed at low pH, weak bases reabsorbed at high pH

36
Q

How are drugs excreted through liver?

A

In faeces

37
Q

What is enterohepatic recycling?

A

Gut bacteria hydrolyse glucuronide metabolites making them more lipid soluble and increases their reabsorption. Leads to prolonged drug effects