3- Agonist-Antagonist

1. The capacity of the drug to bind to its receptor

   a. affinity

   b. intrinsic activity

   c. constitutive activity

   d. efficacy

2. What type of antagonism is present between heparin & protamine sulfate

   a. chemical antagonism

   b. physiologic antagonism

   c. pharmacologic antagonism

   d. mechanical antagonism

3. Two drugs acting of the same receptor giving opposite effects

   a. Competitive antagonism

   b. Non- competitive antagonism

   c. pharmacologic antagonism

   d. AOTA

4. Intrinsic activity may refer to the ff, except:

   a. Efficacy

   b. Biologic activity

   c. pharmacologic response

   d. drug & receptor complexation

5. What type of antagonism is present when two drugs produce opposite effects after activating different receptors?

   a. Physiologic antagonist

   b. Pharmacologic antagonist

   c. Chemical antagonist

   d. Irreversible antagonist

6. Heparin + Warfarin

   a. Competitive antagonist

   b. Non-competitive antagonist

   c. Chemical antagonist

   d. Mechanical antagonist

7. it mimics the action of an endogenous compound.

   a. agonist

   b. antagonist

   c. inverse agonist

   d. NOTA

8. The activity of a receptor in the absence of a ligand

   a. bioactivity

   b. constitutive activity

   c. pharmacologic activity

   d. efficacy

9. A drug that provides submaximal effect

   a. Full agonist

   b. partial agonist

   c. inverse agonist

   d. antagonist

Mimic the action of endogenous compounds

Block the effect of agonist

100% response

examples of Full Agonist

a full agonist that mimics endorphin

a full agonist that mimics NE

• <100% response (submaximal effect)

• use for withdrawal symptoms

Examples of Partial Agonist

a partial agonist drug that decrease the cravings for opioids

a partial agonist drug that is smoking deterrant

Full agonist + partial agonist →

opposite effect (Paradoxical effect)

example of Inverse Agonist

expected response for Beta-carbolines activating GABA-A:

actual response for Beta-carbolines activating GABA-A:

TRUE OR FALSE

Inverse agonists are not antagonists

• 2 drugs binding to the same receptor

• Result: Opposite effect

• Aka Equilibrium Competitive Antagonist

• Ionic bond

• Surmount

• Ex: Atropine + Acetylchoine

examples of reversible competitive antagonists

• Aka Non-Equilibrium

• Covalent bond

• Non-surmountable

• Ex: PPI + Hyperacidity

• Allosteric Antagonist

• Irreversible

• Non-surmountable

• agonists activate the receptor first then antagonist binds to allosteric

• REVERSIBLE

• Two drugs acting on independent or independent receptors

• Same activation but different MOA

Physiological Antagonist examples:

Physiological Antagonist is also known as

• NO RECEPTOR

• Direct interaction between agonist & antagonis

Goals of Chemical Antagonist

MOA of Chemical Antagonist:

Examples of Chemical Antagonist