PED1003/L01 Intro to Drug Action Flashcards

1
Q

Define pharmacology.

A

What the drug does to the body
What the body does to the drug

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2
Q

Where do drugs typically come from? (2)

A

Plants or fungi

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3
Q

Where is aspirin derived from?

A

Willow tree bark

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4
Q

Where is morphine derived from?

A

Opium poppy

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5
Q

Where is psilocybin derived from?

A

‘Magic’ mushroom

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6
Q

How are synthetic drugs created in the laboratory? (3)

A

Novel medicinal chemistry
Identical to natural compounds (mimics)
Derived from natural compounds

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7
Q

Define pharmacodynamics.

A

The effect of the drug on the body

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8
Q

What molecular interactions does pharmacodynamics focus on? (3)

A

Targets for drug action
How drugs act at target
How drug produces action within cell

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9
Q

How is the influence of drug concentration on magnitude of response shown?

A

Graphically with dose-effect relationships

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10
Q

What does study of pharmacodynamics allow?

A

Determine appropriate dose range for patients
Compare efficacy and safety of one drug to another

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11
Q

What is the distance between 2 lines on a dose-response curve called?

A

Therapeutic window

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12
Q

Define pharmacokinetics.

A

The effect of the body on the drug

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13
Q

Give the phases involved in pharmacokinetics. (4)

A

Absorption into blood
Distribution into ICF and ECFs of tissues
Metabolism - inactivation through enzymes
Excretion through urine, bile or faeces

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14
Q

What does study of pharmacokinetics allow? (3)

A

Determination of:
Route of administration
Frequency of dosing
Treatment duration

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15
Q

Give 3 other considerations of drugs.

A

Hydrophobicity
Ionisation of drug (pKa)
Conformation of target
Stereochemistry of drug

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16
Q

Give 3 targets for drug action.

A

Receptors
Ion channels
Carrier molecules
Enzymes

17
Q

What is the drug target of salbutamol?

A

B2 adrenoreceptor
For asthma

18
Q

What is the drug target for lidocaine?

A

Voltage-gated sodium ion channel
Local anaesthetic

19
Q

What is the drug target for aspirin?

A

Cyclooxygenase
Analgesic

20
Q

What is the drug target for omeprazole?

A

Proton pump
Anti-ulcer

21
Q

Give 2 factors that alter drug interaction with targets.

A

Shape
Charge distribution

22
Q

Explain the difference between an agonist and an antagonist.

A

Agonists act as a pseudosubstrate
Antagonists inhibit

23
Q

How do many diseases arise?

A

Abherrant cell signalling

24
Q

Briefly describe how an antagonist works.

A

Binds to a receptor which inhibits agonist response/blocks binding

25
Q

Give the 4 receptor sub-types.

A

Ligand-gated ion channels
G-protein coupled
Enzyme (kinase) linked receptors
Intracellular receptors

26
Q

Describe the effects of benxodiazepine on GABA receptors. (4)

A

Binds to allosteric site
Alters structure of receptor
GABA binds
Enhances the effects of GABA

27
Q

What do all adrenoreceptors have in common?

A

All subunits activated by adrenaline/noradrenaline

28
Q

Describe the function of a1 adrenoreceptors.

A

Activates PLC
Vasoconstriction

29
Q

Describe the function of a2 adrenoreceptors.

A

Inhibit adenylyl cyclase
Auto-inhibition of neurotransmitter release

30
Q

Describe the function of B1&2 adrenoreceptors.

A

Stimulate adenylyl cyclase
B1 - accelerated HR
B2 - bronchodilation

31
Q

Briefly describe the action of receptor tyrosine kinases.

A

Ligand binding
Dimerisation
Autophosphorylation

32
Q

Give 2 examples of nuclear oestrogen receptor substrates.

A

Estradiol
Tamoxifen

33
Q

Describe class I nuclear receptors. (3)

A

Located in cytoplasm
Form homodimers
Ligands are endocrine

34
Q

Describe class II nuclear receptors. (3)

A

Present in nucleus
Form heterodimers
Ligands are lipids