Pharma Cardinal 1

Question 1

Efficacité: Define In terms of pharmacodynamics

Efficacité

Answer 1

It is defined as the maximal response of medication
You can contrast a complete agonist versus a partial agonist and their maximal response at Max concentration
a complete agonist will have a stronger maximal response

Question 2

Define power in terms of pharmacodynamics

Puissance

Answer 2

Power is defined as the amount of those required to give the same response where the medication requires less dose for a larger response is them one that is stronger
The more the curve is to the left the medication is stronger for example
This is sort of like the affinity of the drug for the receptor

Question 3

Can two medication have the same efficacy but the different strength?

Answer 3

Yes they can
You can think of two medications where the dose to get a large response is different but at maximum saturation the maximum response is the same

Question 4

What type of agonist is morphine

Answer 4

It is a complete agonist

Question 5

What type of agonist is buprénorphine

Answer 5

Partial agonist

Question 6

What is the standard medication that we use to compare the strength of other opioids

Answer 6

Morphine ten mg

Question 7

What type of agonist is fentanyl

Answer 7

A complete agonist

Question 8

What type of agonist is hydromorphone

Answer 8

Complete agonist

Question 9

What receptor do all opioids act on

Answer 9

The mu opioid receptor

Question 10

Explain the law of mass action

Answer 10

It stays at the interaction between an agonist and a receptor is reversible
Which leads to
An increase in agonist means more agonist will be bound to the receptor
A decrease in agonist means that less agonist will be bound to receptor
Depending on how much agonist is bound to the receptor that’s how much pharmacological effect we will get
A + R ->A-R → réponse biologique

Question 11

What is the law of receptor occupation

Answer 11

It states that the intensity of a biological effect for medication is proportional to the amount of receptors that are occupied times the maximum tissue activity times the property of the drug

Question 12

Define CE50

Answer 12

The concentration of drug required to reach 50% of Max effect

Question 13

What is R*?

Answer 13

It is receptor that has been bound to a agonist and is in its active confirmation
It could also have spontaneous activity without binding to anagonist

Question 14

What is the difference between a partial and complete agonist in terms of receptor activity

Answer 14

A complete agonist will stabilize the receptor in its active form
A partial agonist will not be able to stabilize the receptor in its active form so the receptor will switch between the two states

Question 15

What is constitutive activity

Answer 15

It is when a gpcr receptor does the transition from R to R* spontaneously

Question 16

Why do we say that a partial agonist can also act as a antagonist

Answer 16

the partial agonist does an incomplete stabilization of the receptor
The complete agonist does a complete stabilization of the receptor in its active configuration
It is the competition for the receptor between the complete and the partial agonist that leads to the partial agonist becoming an antagonist

(here there is no concept of affinity yet)

Question 17

What is the key requirement for an inverse agonist

Answer 17

First of all an inverse agonist is basically an antagonist
It reduces the spontaneous activity of the Receptor
The requirement is therefore that the receptor must have some basal or constitutive activity

Question 18

Can you have an inverse agonist that is complete or partial

Answer 18

Yes this is not reserved to +agonist

Question 19

What is methadone

Answer 19

It is a complete agonist but with the long half-life

Question 20

what is naloxone
don’t talk about properties just what it is

Answer 20

it is a neutral antagonist

Question 21

Can a partial agonist be stronger than a complete agonist

Answer 21

Yes for example buprénorphine is twenty five times stronger than morphine although it is a partial agonist

Question 22

Discuss bioavailability of naloxone

Answer 22

It has a trash baio availability orally sublingually
It must thus be administered intramuscularly or intravenously usually used to prevent opioid overdose

Question 23

Describe the beauty of buprénorphine-naloxone

Answer 23

naloxone doesnt do anything when administered orally. So why give it?
Because if they try to break it and burn it to inject it, they will be injecting naloxone so they will lose the effect. Instead of just giving buprenophine