Pharmacodynamics Flashcards

1
Q

What is the many type of drug target in the body

A

Enzymes then GPCRs

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2
Q

What unit is used to measure drug concentration

A

Molarity

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3
Q

What must a ligand posses in order to bind to a receptor

A

Affinity

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4
Q

What is intrinsic efficacy

A

The ability to activate a receptor by causing a conformational change

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5
Q

What type of ligand results in an intrinsic efficacy

A

Agonist

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6
Q

What is efficacy

A

The ability of a ligand to cause a response

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7
Q

Why don’t antagonists cause a response

A

They possess no intrinsic efficacy

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8
Q

How is drug receptor binding measured

A

Using radio ligands

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9
Q

What is Kd

A

The drug concentration at 50% bound receptors

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10
Q

What is Kd a measure of

A

Affinity

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11
Q

Why is it good for drugs to have a high affinity for receptors

A

Can use smaller tablets

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12
Q

What graph shape do log[drug] vs bound receptors show

A

Sigmoidal

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13
Q

What is EC 50

A

Effective concentration giving 50% response

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14
Q

Define concentration

A

Known concentration of drugs at a site of action

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15
Q

Define dose

A

Concentration at site of action unknown

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16
Q

What is potency

A

Concentration giving 50% of the maximal response

17
Q

What does potency depend on

A

Affinity and intrinsic efficacy

18
Q

What allows for a maximal response without 100% of receptors bound

A

Spare receptors

19
Q

Why are there spare receptors

A

Due to application of signal transduction pathway

20
Q

Why do we have spare receptors

A

Increase sensitivity (increase/decrease coco of ligand that causes a response) so allows for responses at low drug concentration

21
Q

How do receptor numbers change with low activity

A

Increase (up regulation)

22
Q

How do receptor number change with high activity

A

Decrease (down regulation)

23
Q

What is a partial agonist

A

Agonists with lower intrinsic efficacious so can’t result in a full response

24
Q

When can partial agonists act as a antagonist

A

When there are high levels of full agonist

25
Q

Which opioid acts as a partial agonist

A

Buprenorphine

26
Q

What type of receptors do opioids bind to

A

U-opioids receptors (GPCR)

27
Q

What opioid has a higher intrinsic efficacy than buprenorphine

A

Morphine

28
Q

What dangerous drug bind to u-opioid receptors

A

Heroin

29
Q

What is used to treat heroin addiction.

A

Buprenorphine

30
Q

How can you make a partial agonist into a full agonist

A

Increasing receptor number

31
Q

What are the 3 types of antagonists

A

Reversible, irreversible competitive and irreversible non competitive

32
Q

What does surmountable mean

A

When you increase the agonist concentration it can outcompete competitive antagonists for the binding site