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M4: Pharmacology-Pharmacokinetics > Drug-Receptor Interaction & Dose-Response Graph > Flashcards

Drug-Receptor Interaction & Dose-Response Graph Flashcards

1
Q

Substance that binds to receptors

A

Ligand

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2
Q

Ability of a ligand to bind to a receptor

A

Affinity

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3
Q

Ability of a ligand to activate the receptors

A

Intrinsic activity

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4
Q

Types of Ligands (3)

A
  1. Agonist
  2. Antagonist
  3. Inverse Agonist
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5
Q

Types of Ligands

Affinity + Intrinsic Activity (IA)

A

Agonist

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6
Q

Types of Ligands

Affinity only

A

Antagonist

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7
Q

Types of Ligands

▪️Affinity + ↓IA
▪️Decrease IA

A

Inverse Agonist

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8
Q

Types of Agonist (3)

A
  1. Full Agonist
  2. Partial Agonist
  3. Inverse Agonist
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9
Q

What Type of Agonist is:
▪️ Produces all the effects of the receptor
▪️100% effect
▪️IA=1
▪️Ex. Morphine-mu receptor

A

Full Agonist

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10
Q

What Type of Agonist is:
▪️Produces some of the effects of the receptor
▪️Has a mixed agonist and antagonist action
▪️IA>0 but <1
▪️Ex. Nalbuphine, Tamoxifen

A

Partial Agonist

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11
Q

What Type of Agonist is:
▪️Favors the inactive form of the receptor
▪️ Ligand which produces an effect opposite to that of an agonist occupying the same receptor
▪️IA<0
▪️Ex. All antihistamine

A

Inverse Agonist

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12
Q

Morphine is a full agonist to mu receptor while Nalbuphine is a partial agonist for the same receptor. When taken together, the result is(?)

A

Reduction of Analgesia

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13
Q

Types of Antagonist Based on Mechanism (3)

A
  1. Functional/Physiologic Action
  2. Pharmacologic/Receptor Antagonism
  3. Chemical Antagonism
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14
Q

What Type of Antagonist Based on Mechanism
▪️Produces OPPOSITE EFFECTS by binding to DIFFERENT receptors
▪️2 ligands acting on different receptors, producing opposite effects
▪️Ex. Epinephrine in the management of anaphylaxis

A

Functional or Physiological Antagonism

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15
Q

What Type of Antagonist Based on Mechanism

▪️Produces OPPOSITE EFFECTS by binding to SAME or similar receptors

A

Pharmacologic or Receptor Antagonism

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16
Q

Type of Antagonists Based on Interaction (2)

A
  1. Reversible Antagonism
  2. Irreversible Antagonism
17
Q

What Type of Antagonists Based on Interaction is:

▪️Mabilis : safer
▪️Temporary (DOI:<24hrs)
▪️Weak forces (non-covalent) VDW, H-bond

A

Reversible Antagonism

18
Q

What Type of Antagonists Based on Interaction is:

▪️Matagal : toxic
▪️Permanent (DOI: days to weeks)
▪️Covalent bond
▪️As long as the receptor is viable, effect still present

A

Irreversible Antagonism

19
Q

Type of Antagonists Based on Surmountability (2)

A
  1. Competitive/Surmountable
  2. Non-competitive/Non-surmountable
20
Q

What Type of Antagonists Based on Surmountability is:

▪️ Completely overcome the effect of the antagonist by increasing the dose of the agonist
▪️Quantity based (kung sino mas marami siya ang magbibind sa receptor)
▪️ Inhibitor binds to the active site

A

Competitive/Surmountable

21
Q

What Type of Antagonists Based on Surmountability is:

▪️Kahit gaano mo damihan ang dose ng ligand, hindi na niya maka-counteract yung effect ng isa pang ligand
▪️Inhibitor bind to allosteric site

A

Non-competitive/Non-surmountable

22
Q

What type of antagonism exhibited by the two agents?

Ex:
1. Morphine + Naloxone
2. BZD + Flumazenil
3. ACh + Atropine

A

Pharmacologic/Receptor Antagonism

23
Q

What type of antagonism exhibited by the two agents?

Ex:
1. ACh + NE
2. Histamine + Epi

A

Functional/Physiologic Antagonism

24
Q

What type of antagonism exhibited by the two agents?

Ex:
1. Heparin + Protamine
2. Heavy Metals + Chelating Agent

A

Chemical/Inactivation Antagonism

25
Q

What type of antagonism exhibited by the two agents?

Ex:
1. Activated Charcoal
2. Ipecac Syrup

A

Dispositional/Mechanical Antagonism

26
Q

▪️ Shows the relationship between the degree of response with dose
▪️Plot: Degree of Response VS Dose or Log Dose
▪️Log dose (sigmoidal) dose (hyperbolic)

A

Graded Dose-Response Curve/Graph

27
Q

Maximum achievable response

A

Efficacy (E)

28
Q

Dose required to achieved 50% of efficacy

A

Potency

29
Q

Smallest dose that produces the maximum effect

Efficacy 100%

A

Ceiling Dose

30
Q

Degree of change in response with a change in the dose

A

Slope

31
Q

What type of graph antagonism is

▪️ shifts to the right with the same height for efficacy

A

Competitive antagonist

32
Q

What type of graph antagonism is

▪️ rightward shift; lower height
▪️ increases amount of agonist and non-competitive antagonist, but never reaching max efficacy

A

Non-competitive Antagonist

33
Q

▪️ Shows how a population responds to a given dose
▪️Plot: Cumulative number of Px (Y-axis) VS Log Dose (X-axis)

A

Quantal Dose Response Graph/Curve

34
Q

▪️ Median Effective Dose
▪️Effective Dose in 50% of the give of the given population

A

ED50

35
Q

▪️Median Toxic Dose
▪️Toxic Dose in 50% of the given population

A

TD50

36
Q

▪️Measure of relative safety
▪️Wider/Higher TI=SAFER Drug
▪️TITE

A

Therapeutic Index

M4: Pharmacology-Pharmacokinetics (50 decks)

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