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Pharmacology > 1.2 - Drug-Receptor Interaction > Flashcards

1.2 - Drug-Receptor Interaction Flashcards

1
Q

Features

A
  • Affinity

* Intrinsic Activity

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2
Q

Ability of the ligand to BIND to receptors

A

Affinity

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3
Q

Ability of the ligand to ACTIVATE the receptors

A

Intrinsic Activity

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4
Q

Classification of Ligands

A
  • Agonist
  • Antagonist
  • Allosteric Interaction
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5
Q

Affinity with Intrinsic Activity (IA)

A

Agonist
– Full
– Partial
– Inverse

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6
Q

— IA = 1

— Produces ALL of the expected effects

A

Full Agonist

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7
Q

— IA > 0 but < 1
— Produces SOME of the expected effects
— mixed effect

A

Partial Agonist

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8
Q

NOTE:

A partial agonist in the presence of full agonist will act as an ——

A

Antagonist

– Morphine + Nalbuphine = ⬇️ Analgesia

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9
Q

— IA < 0

A

Inverse Agonist

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10
Q

Affinity WITHOUT Intrinsic Activity

A

Antagonist

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11
Q

Types of Antagonism

A
  • Based on MOA
  • Based on the type of Interaction
  • Based on Surmountability of Interaction
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12
Q

Based on MOA

A
  • Functional Antagonism
  • Receptor Antagonism
  • Chemical Antagonism
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13
Q

– Physiologic Antagonism
– DIFFERENT receptors
– EPI + Histamine

A

Functional Antagonism

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14
Q

– Pharmacologic Antagonism
– SAME receptors
– EPI + B-blockers

A

Receptor Antagonism

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15
Q

– Chemical Reaction
– Protamine + Heparin
– DFO + Fe

A

Chemical Antagonism

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16
Q

Based on the type of interaction

A
  • Reversible Interaction

* Irreversible Interaction

17
Q

– Temporary

– WEAK forces of attraction

A

Reversible Interaction

18
Q

– Permanent

– COVALENT bonding

A

Irreversible Interaction

19
Q

Based on Surmountability of Interaction

A
  • Competitive Antagonism

* Non-competitive Antagonism

20
Q

Completely overcomes the effect of antagonist by increasing the dose of the agonist

A

Competitive Antagonism

- Surmountable

21
Q

✖️ completely overcome the effect of antagonist even by ⬆️ the dose of agonist

A

Non competitive Antagonism

22
Q

Promote/ inhibit binding of agonist receptor by changing configuration of receptor

A

Allosteric Interaction

— Binding site other than the receptor

23
Q

Theories

A
  • Hypothesis of Clark
  • Hypothesis of Paton
  • Hypothesis of Ariens & Stephenson
24
Q

Maximum pharmacologic effect is obtained if ALL receptors are occupied

A

Hypothesis of Clark

25
Q

– Rate Theory

– Maximum pharmacologic effect does not depend on the occupancy of the receptor by the ligand, but on STIMULUS

A

Hypothesis of Paton

26
Q

– Occupancy Theory

– Maximum pharmacologic effect lasts AS LONG AS receptors are occupied

A

Hypothesis of Ariens & Stephenson

Pharmacology (21 decks)

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