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Terms Flashcards

(56 cards)

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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

Study These Flashcards
A

Good potential for increasing dose

24
Q

Endogenous Ligand

Study These Flashcards
A

Produced in the body and acts on receptors

25
Full Agonist
Activates all targets, shifts equilibrium to saturate all receptors pool (Ra - D)
26
Competitive Antagonist
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
To increase chance to win competition against **antagonist**...
The concentration of natural ligand should be increased - **If equal number of molecules, the one with the higher affinity will win**
28
Non-Competitive Antagonist
Doesn't bind to receptor at binding site. Binds to another spot and deactivates it
29
Two types of distribution
Localized distribution or widespread distribution (more side effects possible)
30
Increasing lipid solubility means...
harder to move between environments
31
First Order Elimination
When the body eliminates half of the concentration in a particular period of time. Higher concentration, higher rate of elimination **Exponential Decay**
32
Zero Order Elimination
When the body breaks down particular amounts of drug per unit of time **Linear Elimination**
33
Glucuronidation
UDP - UGT Adds a **glucuronosyl** Attacks **nucleophiles**
34
Sulfation
SULTs Adds a **sulfate group** Attacks **nucleophile - alcohol / amine**
35
Glutathione
GSH or GST Adds a **glutathione (GSH)** Attacks **electrophiles**
36
Delayed Drug Effects
Delay can be caused by the time required for **distribution to tissues**; **dissociation of drug from target**
37
Cumulative Effects
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
Hydrophilic (water soluble) drugs are easily eliminated, however, lipid soluble drugs must undergo...
Metabolism to enhance drug elimination by turning lipid soluble to water soluble
39
Phase 1 (Oxidation)
Add small polar groups to drug and removing lipophilic groups to increase water solubility of drug
40
If product from Phase 1 undergoes Phase 2, that means...
The product is **toxic**
41
Phase 2
Adds specific (usually large and bulky) polar functional groups on drug or Phase 1 toxic product
42
Both phases (1 and 2) mostly takes place in the...
Liver
43
Tylenol Metabolism is an example of...
Glutathione (GSH) transferase (GST)
44
Factors that affect drug metabolism:
Genetic Factors; Diet & Environment; Age & Sex; Drug-Drug Interactions Diseases
45
Prodrug
Compound is metabolized after administration to turn into its active form; Will not act as a drug until changed through metabolism
46
Prodrugs helps...
Compounds permeate through target tissue walls if parent drug cannot on its own; Increases absorption
47
Synergism Interaction
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
Pharmacokinetic Principles
Absorption; Distribution; Metabolism; Elimination ADME
49
Drug Permeation
Intercellular, Lipid, Special Carriers, Endocytosis and Exocytosis
50
Intercellular Diffusion
Must be **small, water soluble**
51
Lipid Diffusion
**Lipid soluble** molecules
52
Special Carriers
Transporter proteins for **water soluble** molecules
53
Endocytosis and Exocytosis
For **larger** molecules that do not have any transporter proteins to carry them
54
First Pass Effect
Initial metabolism of drug in the liver that **reduces drug concentration** High effect for oral administration
55
Area Under the Curve (AUC)
Total drug exposure over time; proportional to dose and extent of bioavailability.
56
What does larger AUC mean?
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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