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N926: Pharmacology > Pharmacodynamics > Flashcards

Pharmacodynamics Flashcards

1
Q

Pharmacodynamics

A

What drug does to body

Effects of drug on the body

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2
Q

Receptor Theory

A

Receptors are macromolecular complexes (usually proteins) embedded in the phospholipid bilayer of a cell membrane.
There are receptors in the body for every physiologic event that occurs and multiple receptors have different actions.
Receptors have active and inactive states.
Binding results in a conformational change in the receptors.

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3
Q

Receptor types

A

Ligand-gated ion channel
G protein couple receptor
Transmembrane with linked enzymatic domain
Intracellular receptor

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4
Q

Ion Channels

A 
Ligand vs voltage gated
Time frame to respond: seconds
Examples:
-nicotinic 
-GABA
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5
Q

G-Protein Coupled Receptors

A 
Family of receptors
Activation of GTP binding proteins
• GTP exchanged for GDP 
• G-⍺ separates from B andY  
• Activates effector
Examples
• Muscarinic/cholinergic 
• Adrenergic
• Dopaminergic 
• 5-HT
• Opioid
 Ligand on receptor -> conformational change-> 2nd messenger-> CAMP-> physiological effect

Take time more time when compared to ion channel

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6
Q

Transmembrane Enzymatic

A

Transmembrane embedded enzyme-linked receptors
-Activation of kinase enzyme
-Phosphorylates a signal molecule to activate
-Biological effects result
Usually involved in growth and development
-Target chemotherapy drugs
Examples:
-Tyrosine receptor kinase (most common)
-Insulin

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7
Q

Intracellular receptors

A 
Proteins found inside the nucleus 
Ligands typically hydrophobic 
Modify gene transcription 
Onset 
Duration of action 
Examples: steroid hormones and vit d
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8
Q

Drug and receptor interaction

A

Chemical substances that bind to receptors are called ligands.
-Endogenous
-Exogenous (drugs)
Drugs cannot make the body do something it is not already capable of

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9
Q

Agonists

A

Bind to a receptor and stimulate the function that receptor serves (shift to activate state)
Affinity for receptor
Causes intrinsic activity

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10
Q

Antagonists

A

Bind to receptor and block the function that receptor serves (stabilizes inactive state)
Affinity for receptor
Competitive vs noncompetitive

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11
Q

Competitive antagonist

A

Reversible (most drugs)

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12
Q

Non-competitive antagonist

A

Non-reversible or binds allosteric site

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13
Q

Allosteric

A

Binding site different than endogenous ligand

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14
Q

Covalent bonding

A

Sharing electron, strongest bond

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15
Q

Ionic bonding

A

“pitchers and catchers”

Transfer of electron

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16
Q

Hydrophobic

A

“oil in water”

17
Q

Van der Waals

A

Transient attraction b/t stable molecules (weakest type of bond)
Think drug binding to proteins

18
Q

Can drugs act without a receptor?

A

Yes, but not many.
Antacids
Osmotic diuretics
Chelating agents

19
Q

Potency (affinity)

A

How much drug to get an effect?

20
Q

Efficacy

A

Does drug produce desired effect

21
Q

Variability

A

“nothing is exactly the same”

22
Q

Slope

A

Margin of safety of the drug, the steeper the slope, the narrower the therapeutic window and smaller the margin of safety

23
Q

Therapeutic index

A

How much more drug required to cause adverse effects

LD50/ED50

24
Q

ED50

A

Effective dose in 50% of the population

25
Q

TD 50

A

Toxic dose in 50% of the population

26
Q

LD50

A

Lethal dose in 50% of the population

27
Q

TD50/ED50

A

Therapeutic window=dose which treats disease effectively while staying within safety margin

28
Q

Therapeutic window

A

How much drug to achieve 100% efficacy

Effect without toxicity

Establishes a range of concentrations considered therapeutic.

  • Above would result in serious harm
  • Below would be inefficacious

The range below the toxic threshold but above sub-therapeutic dosing represents margin of safety

29
Q

Individual variability

A

Genetic differences
Age-older respond to less drug
Gender
Comorbidities-renal disease, decrease protein, increase free floating drug
Dietary and supplements
Alcohol- (chronic use=increase dose, acute=decrease dose)
Drug to drug interactions (fentanyl and midazolam)

30
Q

Down-regulation

A

A state of desensitization resulting from continued stimulation (agonist)
Quantitative-receptors decrease in number
Qualitative- each receptor becomes less responsive
-repeated use of beta agonist for asthma, pain meds

31
Q

Up-regulation

A

Number and sensitivity of receptors due to chronic blockade (antagonist
-Pt taking beta blocker, increased receptors, can’t abruptly stop because more receptors means more of a response (increased likelihood of binding and activating receptors)

32
Q

Interaction

A

Alteration in the therapeutic action of a drug by concomitant administration of other exogenous drugs

33
Q

Addition

A

The combined effect of two drugs is equal to the simple addition of the individual drug effects

1+1=2

34
Q

Synergism

A

The combined effect of two drugs is greater than the sum of their individual effects

1+1=3

35
Q

Potentiation

A

The enhancement of one drug by a second drug that has no detectable action of its own

1+0=3

36
Q

Antagonism

A

The action of one drug opposes another

1+1=0

N926: Pharmacology (4 decks)

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