4bby1040

Question 1

affinity high vs low

potent?

Answer 1

the higher affinity a drug has to a specific receptors, the more likely the bind and stay bounds to it - higher potent
the lower affinity a drug has to a specific receptors, the less likely the drug will bind and stay bounds to it - low potent

Question 2

Potency

Answer 2

the drug concentration required to produce a given level of biological response
Comparing EC50 values for two drugs with the same action allows us to calculate their relative potencies AKA potency ratio

Question 3

In virtue
definiton
response

Answer 3

drug effect on a tissues or cells kept alive outside the body
Measure the change in the (tension of muscle or activity of enzyme)

Question 4

In Vivo

Answer 4

drug effects are studied in the living animal/human

Question 5

Ex Vivo

Answer 5

tissues or organ is removed from an animal that has been treated with a drug and testing for the long-term effect the drug has on the organ function

Question 6

the max effect (EMAX)

Answer 6

indicates the max responses the drug can produces (concentration-response graph)

Question 7

EC50

Answer 7

The molar concentration of a drug that produce 50% of the maximum response for the drugs

Question 8

M potency ratio

Answer 8

M= EC50(test)/EC50(standard)
Or
Log M = Log EC50(test) – Log EC50 (standard)

A potency ratio (M) less than 1 , this means the test drug is more potent than the standard drug

M is greater than 1 than the standard drug is more potent than the test drug

Question 9

Bioassay:

Answer 9

It’s a technique where the potency of a drug is determined by measuring the biological response it produces

Comparing the low and high concentration of one drug to the low and high concentrations of another drug

Question 10

Therapeutic index:

Answer 10

Is the ratio between the toxic doses and the dose producing the desired therapeutic effect

Higher Therapeutic index is, the less chance of the drug producing toxic side effects

Therapeutic Index = LD 50 / ED 50

LD 50 = lethal does in 50 % of population
ED 50 = Effective does in 50% of population

Question 11

Receptor

Answer 11

a protein - random collisions between the drug molecules and receptor

Question 12

Affinity:

Answer 12

The molar concentration of drug required to occupy 50% of the receptors at equilibrium

( binds to the receptor)

Question 13

Kd

Answer 13

a measure of the affinity of a drug for a receptor

a drug with high affinity will have a low Kd

Question 14

Efficacy

Answer 14

The ability of a drug to activate a receptor

Response

Question 15

Agonists

Answer 15

bind and activate the receptor contain efficacy
a conformational change
lead response to the tissues/ cells

Question 16

Agonists full/ partial - affinity/ efficacy

Answer 16

Full: Has affinity and high efficacy – maximal response every time
Partial: has affinity but low efficacy – low effective – fail to produce max response

Question 17

Antagonist

Answer 17

Acts as inhibits
Inhibits the effects of neurotransmitter or hormones

acts on the receptor

Question 18

antagonists forms
chemical
pharmacokinetic
physiological

Answer 18

1) Chemical: use one drug to chemically inactivate another – receptors are not involved
2) Pharmacokinetic: one drug alters the way the body deals with another – receptors are not involved
3) Physiological: Two drugs act to produce opposing effects- cancelling each other out

Question 19

Competitive antagonists

Answer 19

Complete with the agonist for the same site on the receptor molecule – don’t activate it –has affinity but zero efficacy – can be reversible or irreversible (covalent bond)

Question 20

Non-competitive antagonists:

Answer 20

Act at a different site on the receptor or another molecule - can be reversible or irreversible (covalent bond)

Question 21

Reversible competitive antagonists
overcome?
shift?

Answer 21

• Can be overcome by increasing the concentration of the agonist – its surmountable
• Parallel shift to the right

Question 22

Irreversible competitive antagonist

overcome?

Answer 22

• the inhibition they produce is not overcome by increasing the agonist concentration- it’s not surmountable

Question 23

with efficacy / no efficacy - response

Answer 23

with - forms is a response

without -does not form a response