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BIO200 > Terms > Flashcards

Terms Flashcards

1
Q

Pharmacodynamics

A

what the DRUG does to the BODY
- Determines how drug is classified

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2
Q

Pharmacokinetics

A

what the BODY does to the DRUG
- How the drug is absorbed, distributed, metabolized, & eliminated from body
- Important for determining kind of drug

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3
Q

Effector Mechanism

A

Drug alters cell communication
- Communicates effect of DRUG-TARGET interaction to the cell

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4
Q

Orphan Receptors

A

Unknown ligands = potential drug discoveries

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5
Q

Types of Effector Systems

A
  • Regulatory proteins
  • Enzymes
  • Structural proteins
  • Transport proteins
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6
Q

Conformational Change

A

Drug binding to protein target
- Affects of protein SHAPE and FUNCTION

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7
Q

Drug binding can cause effect…

A

Directly or Indirectly

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8
Q

Targets exist in two states:

A
  • Inactive = Ri
  • Active = Ra
    Both forms are always in equilibrium
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9
Q

Constitutive Activity

A

Mostly in active state, in absence of ligand

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10
Q

Inert Binding Site

A

Drug binding to non-regulatory target
- No effect on biological function

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11
Q

Selectivity

A

Receptors will decide what the drug does

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12
Q

Drug-Target interactions are determined by concentration

A

The more drug concentration C, the more drug effect E.
- Effect increases as dose increases

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13
Q

Emax

A

The max. effect that can be produced by a drug
- Very close to toxicity

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14
Q

EC50

A

The concentration of drug that produces 50% of the max. effect
- Calculates the dose

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15
Q

Bmax

A

Fraction of the free receptors decreases with increasing drug/ligand, until saturation occurs
- Number of free receptors

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16
Q

Kd

A

Equilibrium Dissociation Constant
Concentration of free drug (mol/L) when receptors are 50%

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17
Q

Low Kd

A

High affinity

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18
Q

High Kd

A

Low affinity

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19
Q

Log Scale

A

Small changes in concentration makes a big change in effect

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20
Q

Indirect = Enzymes

A

Biological response may reach the max, before full saturation

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21
Q

Direct = Ion Channels

A

Effect depends on how many drug molecule binds to how many receptors

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22
Q

Occupancy-Response Relationship

A

Max. response may occur without max. occupancy of the receptors
- A lot of spare receptors will make EC50 not the same as Kd

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23
Q

Spare Receptors

A

Good potential for increasing dose

24
Q

Endogenous Ligand

A

Produced in the body and acts on receptors

25
Q

Full Agonist

A

Activates all targets, shifts equilibrium to saturate all receptors pool (Ra - D)

26
Q

Competitive Antagonist

A

Competes with endogenous ligand to bind to the same pocket
- Does not have any effect if no endogenous agonist (there must be competition)
- Stabilizes receptors in their inactive form

27
Q

To increase chance to win competition against antagonist…

A

The concentration of natural ligand should be increased
- If equal number of molecules, the one with the higher affinity will win

28
Q

Non-Competitive Antagonist

A

Doesn’t bind to receptor at binding site. Binds to another spot and deactivates it

29
Q

Two types of distribution

A

Localized distribution or widespread distribution (more side effects possible)

30
Q

Increasing lipid solubility means…

A

harder to move between environments

31
Q

First Order Elimination

A

When the body eliminates half of the concentration in a particular period of time.
Higher concentration, higher rate of elimination
Exponential Decay

32
Q

Zero Order Elimination

A

When the body breaks down particular amounts of drug per unit of time
Linear Elimination

33
Q

Glucuronidation

A

UDP - UGT
Adds a glucuronosyl
Attacks nucleophiles

34
Q

Sulfation

A

SULTs
Adds a sulfate group
Attacks nucleophile - alcohol / amine

35
Q

Glutathione

A

GSH or GST
Adds a glutathione (GSH)
Attacks electrophiles

36
Q

Delayed Drug Effects

A

Delay can be caused by the time required for distribution to tissues;
dissociation of drug from target

37
Q

Cumulative Effects

A

Irreversible anti-cancer agents

Action = irreversible binding; drug binds to target immediately after absorption
Delayed Effect = blocks cell division leading to cell death
Response = slowing tumour growth

38
Q

Hydrophilic (water soluble) drugs are easily eliminated, however, lipid soluble drugs must undergo…

A

Metabolism to enhance drug elimination by turning lipid soluble to water soluble

39
Q

Phase 1 (Oxidation)

A

Add small polar groups to drug and removing lipophilic groups to increase water solubility of drug

40
Q

If product from Phase 1 undergoes Phase 2, that means…

A

The product is toxic

41
Q

Phase 2

A

Adds specific (usually large and bulky) polar functional groups on drug or Phase 1 toxic product

42
Q

Both phases (1 and 2) mostly takes place in the…

A

Liver

43
Q

Tylenol Metabolism is an example of…

A

Glutathione (GSH) transferase (GST)

44
Q

Factors that affect drug metabolism:

A

Genetic Factors;
Diet & Environment;
Age & Sex;
Drug-Drug Interactions
Diseases

45
Q

Prodrug

A

Compound is metabolized after administration to turn into its active form;
Will not act as a drug until changed through metabolism

46
Q

Prodrugs helps…

A

Compounds permeate through target tissue walls if parent drug cannot on its own;
Increases absorption

47
Q

Synergism Interaction

A

Effects of two chemicals taken together is greater than the sum of their separate effect at the same dose;
Increases effect when both are taken together

48
Q

Pharmacokinetic Principles

A

Absorption; Distribution; Metabolism; Elimination
ADME

49
Q

Drug Permeation

A

Intercellular, Lipid, Special Carriers, Endocytosis and Exocytosis

50
Q

Intercellular Diffusion

A

Must be small, water soluble

51
Q

Lipid Diffusion

A

Lipid soluble molecules

52
Q

Special Carriers

A

Transporter proteins for water soluble molecules

53
Q

Endocytosis and Exocytosis

A

For larger molecules that do not have any transporter proteins to carry them

54
Q

First Pass Effect

A

Initial metabolism of drug in the liver that reduces drug concentration
High effect for oral administration

55
Q

Area Under the Curve (AUC)

A

Total drug exposure over time;
proportional to dose and extent of bioavailability.

56
Q

What does larger AUC mean?

A

Body is exposed to high amount of drug for a longer period of time; longer duration of drug elimination.

BIO200 (3 decks)

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