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BIOM20002 - HSF > Lecture 29 - Introduction to Drugs > Flashcards

Lecture 29 - Introduction to Drugs Flashcards

1
Q

What is the definition of a drug?

What isn’t a drug?

A

A chemical compound of known structure that produces a biological effect.

It is no herbal remedies, or dietary requirements

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2
Q

Which neurotransmitters act on the cardivascular system?

Which receptors?

A

NA and Ad

alpha and beta adrenoceptors

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3
Q

What is the scientific basis of the action of drugs?

A 
Molecular pharmacology
Cell and tissue physiology
Organ pharmacology
Whole body
Population
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4
Q

Give an example of the scientific basis of drugs

A

Thiazide diuretics

  1. Blocks Na+/Cl- transporter
  2. Decrease in Na+/Cl- reabsorption
  3. Increased excretion from kidney
  4. Lower blood volume and BP
  5. K+ loss, hyperglycaemia, gout
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5
Q

What is pharmacodynamics?

A

Effect of a drug on the body

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6
Q

What is pharmacokinetics?

A

What the body does to the drug

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7
Q

What are the generalised targets of drugs?

A
  • Receptors
  • Enzymes
  • Ion channels / transporters
  • Gene transcription / translation
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8
Q

Where are the generalised location of receptors?

A
  • Cell surface
  • Cytosol
  • Nucleus
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9
Q

What are the types of cell surface receptors?

A
  • GPCR
  • Ion channels
  • Tyrosine-Kinase linked
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10
Q

What are the two ways that two cells can interact?

Give examples of each

A

1/ Release of molecules
- hormones

2/ Membrane bound molecules
- immune system

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11
Q

How can such a small molecule bring about a response in a cell?

A

Amplification

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12
Q

Describe the generalised process of amplification

A
  1. One ligand binds to one receptor
  2. Receptor activates many second messengers
    and so on
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13
Q

Describe a drug-receptor interaction that takes in the order of milliseconds to elicit a response

A

ACh - nAChR

At motor endplate

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14
Q

Describe a drug-receptor interaction that takes in the order of seconds to elicit a response

A

NA - Adrenoceptors

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15
Q

Describe a drug-receptor interaction that takes in the order of minutes to elicit a response

A

Insulin - IR

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16
Q

Describe a drug-receptor interaction that takes in the order of hours to elicit a response

A

Cortisol - Glucocorticoid receptor

17
Q

What type of receptor is the nAChR?

A

Ion channel

18
Q

What type of receptor is the mAChR?

A

GPCR

19
Q

What type of receptor is the insulin receptor?

A

Receptor tyrosine kinase

20
Q

What type of receptor are adrenoceptors?

A

GPCR

21
Q

What is the effect of d-Turbocurarine?

A

Blocks Na+ channels

No action potential conductance

22
Q

What is the structure of GPCR?

A 
Receptor: 7TM (heptahelical)
Binding domain extracellularly
Linked to G-protein:
alpha, beta gamma subunits
GDP
23
Q

What is a drug that targets AChE?

What does it then do?

A

Physostigmine

It is an antagonists - prevents the breakdown of ACh

24
Q

What is a drug that targets cyclo-oxygenase?

Describe what happens when it is taken

A

Aspirin

Inhibits the production of inflammatory prostaglandins

25
Q

What is a drug that targets the bcr-abl fusion protein?

What does the drug do?

A

Imatinib

Blocks the kinsase action of the fusion protein

26
Q

Describe the function of receptor tyrosine kinases

A
  1. Ligands bind
  2. Subunits dimerise
  3. Auto-phosphorylation
  4. Tyrosine residue is phosphorylated
  5. Kinase property of the receptor is activated
27
Q

Give an example of a nuclear hormone receptor target

A

Cortisol - GR

28
Q

Describe the action of cortisol

A
  1. Diffuses through membrane
  2. Binds to GR in cytoplasm, chaperon dissociates
  3. GR + cortisol move to the nucleus
  4. Binds to DNA
  5. Change in gene expression
29
Q

What type of hormone is cortisol?

A

Steroid

30
Q

How is chemical signalling controlled?

Give an example of each

A 
1/ Breakdown
- ACh
2/ Reuptake
- NA
3/ Metabolism, Negative feedback
- Insulin
- Cortisol
31
Q

Describe the regulation of NA

A

Once it has acted on the receptors, it is taken back up by the pre-synaptic cell

32
Q

What is the mechanism of action of cocaine in the body?

A

Blocks the reuptake of noradrenaline and dopamine

33
Q

Describe the regulation of insulin in the body

A

Controlled by negative feedback

  1. Glucose in the blood
  2. Increased ATP in cells
  3. K+ channels blocked
  4. Depolarisation
  5. Release of insulin
34
Q

Describe the regulation of cortisol

A
  1. Hypothalamus release CRF
  2. CRF leads to release of ACTH from the pituitary
  3. ACTH releases cortisol from the adrenal gland
  4. Cortisol feeds back negatively on the hypothalamus
35
Q

What is ACTH?

A

Adrenocorticotrophic hormone

36
Q

What is CRF?

A

Corticotropin releasing factor

BIOM20002 - HSF (60 decks)

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