Drug-Receptor Interactions

Question 1

Definiton of: Pharmacokinetics

Answer 1

Effect of body on drugs (absorption, distribution, metabolism and excretion)

Question 2

Definiton of: pharmacodynamics

Answer 2

effect of the drug on the body (MOA, drug receptor interactions…)

Question 3

Definiton of: potency

Answer 3

depends on the affinity and the efficacy (intrinsic activity) of the drug.

Question 4

Definiton of: Affinity

Answer 4

the avidity of the drug (how tightly it binds to the receptor).

Question 5

Definiton of: Efficacy

Answer 5

the ability of the drug to change the conformation of the receptor once bound to the receptor.

Question 6

Definiton of: Full agonist

Answer 6

can induce a full response from a tissue.

Question 7

Definiton of: Partial agonist

Answer 7

can induce only a partial response from a tissue

Question 8

Definiton of: Selectivity

Answer 8

drugs that interact with receptors have a selectivity for that receptor, however they can stimulate other receptors too in higher concentrations. Drugs are not SPECIFIC they are SELECTIVE

Question 9

Definiton of: Structure-activity relationship

Answer 9

the relationship between the structure of a drug and the activity of it. Adding a methyl group could change the activity of a drug markedly. Can turn an agonist into antagonists and can also change the pharmacokinetics of the drugs very easily.

Question 10

What are the 4 drug target sites:

Answer 10

Receptors, ion channels, transport systems, enzymes

Question 11

What are receptors?

Answer 11

Proteins within cell membranes or in the cytoplasm of the cell.

Question 12

What are the 4 different types of receptors

Answer 12

Ligand gated channel, enzyme linked receptor, G-protein linked receptor, and intracellular receptor

Question 13

what are ion channels

Answer 13

selective pores that allow the transfer of ions down the electrochemical gradient

Question 14

What are the 2 types of ion channels

Answer 14

voltage sensitive (VSSC) and receptor linked/ligand gated ion channels (nAChR)

Question 15

What are transport systems

Answer 15

transport against concentration gradients (e.g. glucose, ions, neurotransmitters…)

Question 16

What are the three ways drugs interact with enzymes

Answer 16

enzyme inhibitors (anticholinesterases), false substrates that result in a different final product that is less effective than the natural final product (methyldopa) and prodrugs which interact with enzymes to become active

Question 17

What happens if you give a partial agonist with a full agonist

Answer 17

means the partial agonist will have antagonist activity as the partial agonist is preventing the full agonist from stimulating a full response

Question 18

Two types of antagonists?

Answer 18

competitive and irreversible

Question 19

what bonds do irreversible antagonists form

Answer 19

Covalent

Question 20

How do you overcome a competitive antagonist

Answer 20

Increase dose of antagonist