Introduction To Pharmacology

Question 1

Outline the development of propranolol

Answer 1

Antagonist- the first beta-blocker still used today to treat angina, anxiety and hypertension
Blocks effects of agonists

Question 2

What is an agonist

Answer 2

A ligand that binds to a receptor and alters the receptor state resulting in a biological response.
Conventional agonists increase receptor activity, whereas inverse agonists reduce receptor activity

Question 3

Outline antagonists

Answer 3

A drug that reduces the action of another drug, generally an agonist. Many antagonists act at the same receptor macromolecule as the agonist

Question 4

outline affinity

Answer 4

How well the ligand binds to a receptor or enzyme, ion channel transporter etc.

Question 5

Outline efficacy

Answer 5

How well the ligand increases or decreases a response

Question 6

Outline the receptor concept

Answer 6

The active principle binds to the external binding site of a receptor. A G-protein couples the receptor to an effector enzyme and produces the desired response
A reversible antagonist competes with the agonist at the same binding site and reduces its effects.