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Year 2 Pharma > Drug receptor interactions > Flashcards

Drug receptor interactions Flashcards

1
Q

What is the definition of a drug?

A

A chemical substance that interacts with a biological system to produce a physiological effect

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2
Q

What are the 4 different drug target sites?

A

Receptors
Enzymes
Ion Channels
Transport Systems

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3
Q

Where are most receptors found?

A

They are exposed on the cell surface so drugs can easily get to them

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4
Q

What is the exception to the where most receptors are found?

A

Steroid receptors are found in the nucleus

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5
Q

What are examples of receptor affecting drugs? Name an agonist and an antagonist

A

Ach (agonist)

Atropine (antagonist)

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6
Q

How are receptors activated?

A

NT or hormones

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7
Q

What are examples of drugs that affect ion channels?

A

LA (local anaesthetic)

Ca2+ Channel Blockers (-dipines)

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8
Q

What are the two types of ion channels?

A 
Voltage sensitive (VSCC)
Receptor linked nAChR (nicotinic acetylcholine receptor)
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9
Q

What are ion channels?

A

Selective pores that allow transfer of ions down an electrochemical gradient

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10
Q

What are transport systems?

A

They transport against a concentration gradient eg glucose uptake into cells, ion transporters and neurotransmitters

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11
Q

What are example of drugs that affect transport systems

A

Tricycle antidepressants TCAs

Cardiac glycosides

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12
Q

What is an example of what TCAs do?

A

They can slow down the NA reuptake and deactivation therefore allowing longer time for noradrenaline action to take place.

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13
Q

What are enzymes

A

Catalytic proteins that increase reaction rate

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14
Q

What are examples of drug interactions with enzymes?

A

Enzyme inhibitors eg anticholinesterase
False substrates eg methyldopa
Prodrugs eg chloral hydrate or trichoroethanol

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15
Q

What is similar within receptor families and how many families are there?

A

They have similar structures and transduction systems. There are 4 families

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16
Q

What are examples of non specific drug actions?

A

Antacids - all basic eg Mg/Al hydroxide

Osmotic purgatives - draw water into gut

17
Q

What are non specific drug actions for?

A

Treating patients using the physiochemical properties of the drug

18
Q

What does plasma protein binding react to a drug and what is the result?

A

The drug binds to albumin and causes the inactivation of the drug, providing a reservoir of inactive drug. There is no physiological reaction and is used as drug storage within the body

19
Q

What is an agonist?

A

A ligand - any substance that binds to and stimulates a receptor eg ach or nicotine

20
Q

What is an antagonist?

A

Something that binds to a receptor but doesn’t cause a reaction therefore blocks the receptor and decreases activity eg atropine or hexamethonium

21
Q

What does the potency of a drug depend on?

A

Affinity

Efficacy

22
Q

What does affinity mean?

A

The binding property of a receptor

23
Q

What does efficacy mean?

A

The ‘intrinsic activity’ to do smth to generate a response eg conformational change of a receptor

24
Q

What is a full agnonist

A

It can generate the full response of a receptor

25
Q

What is a partial agonist

A

It can never generate the full response of a receptor

26
Q

What happens when you use a partial and a full agonist at the same time?

A

Partial agonist will generate a slight antagonist effect

27
Q

What is selectivity?

A

The degree to which a drug acts on a given site relative to other sites

28
Q

Why is the term selectivity used instead of specificity?

A

Because specificity means it binds to only one receptor but in high enough doses, a drug will bind to several different receptors and cause some of the unwanted side effects of drugs

29
Q

What is the key factor of an antagonist that is different to agonists?

A

Antagonists have affinity but no efficacy

30
Q

What are the 2 types of receptor antagonists

A

Competitive and Irreversible

31
Q

What is the key property of a competitive antagonist?

A

It binds to the same site as the agonist, and is therefore surmountable (if high conc agonist then it can overcome the antagonist)

32
Q

How can you see surmountable on dose response curve?

A

D-R curve shift to right

33
Q

What are examples of receptor antagonists?

A

Atropine

Propranolol (beta blocker)

34
Q

What is the key property of an irreversible antagonist?

A

If do bind to same site as agonist, binds more tightly than the agonist. OR binds at a different site. Both are insurmountable (and drugs last longer)

35
Q

What is an example of an irreversible antagonist?

A

hexamethonium

Year 2 Pharma (34 decks)

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