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Pharmacology 3001 > Pharmacodynamics - Sinal 1 > Flashcards

Pharmacodynamics - Sinal 1 Flashcards

1
Q

What is pharmacology?

A

What drugs are, how they work and what they do

Divided into pharmacodynamics and pharmacokinetics

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2
Q

Drugs

A

Therapeutic agent

Any substance other than food, used in prevention, diagnosis, alleviation and treatment or cure of disease

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3
Q

Pharmacy

A

Concerns with scientific, legal and managerial aspects of dispensing drugs

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4
Q

Pharmacodynamics

A

Study of relationship of drug concentrations to drug effects

Biological effect is proportional to amount of drug-receptor complex

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5
Q

Major classes of receptors targeted

A
  1. Ligand-gated ion channels
  2. Enzyme-linked receptors
  3. G-protein coupled receptors
  4. Ligand-activated transcription factors
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6
Q

Agonist

A

A drug causing receptor to respond in same way as naturally occurring substance
Independent impact on receptor activity

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7
Q

Antagonist

A

Drug that binds to receptor but does not produce a response
Inhibitory effect on naturally occurring substance
Impacts receptor activity only in presence of agonist (lacks efficacy)

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8
Q

B

A

Fraction of total receptors bound

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9
Q

Bmax

A

Maximal faction of total receptors bound

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10
Q

Kd

A

Equilibrium dissociation constant
Drug concentration at which 1/2 of Bmax is achieved
A measure of the inherent affinity of the drug-receptor interaction
Constant and not altered by concentration of drug or receptor number

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11
Q

Saturation point

A

Level out of B/[D] graph because all receptors are saturated

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12
Q

High Kd

A

Low affinity

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13
Q

Low Kd

A

High affinity

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14
Q

Graded dose-response curves

A

Drug dose/Biological effect (%)

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15
Q

Emax

A

Maximum response achieved by the drug

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16
Q

ED50

A

Drug dose where 1/2 Emax is achieved

Also referred to as drug potency

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17
Q

Concentration-Binding Curve

A

Drug concentration/fraction of receptors bound

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18
Q

Quantal Dose-Response Curves

A

Used to describe population rather than single individual responses to drugs
Based on plotting cumulative frequency distribution of responders against the log drug dose, adding bars of histogram

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19
Q

Graded phenomena

A

Infinite number of intermediate states

ie. vessel dilation, blood pressure change, heart rate change

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20
Q

Quantal phenomena

A

All or none

ie. death, pregnancy, pain relief

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21
Q

Potency

A

Amount of agonist needed to produce an effect of a given magnitude
Usually expressed as ED50: dose to achieve 50% of the maximum effect achievable with that agonist

22
Q

Efficacy

A

Maximum effect that can be achieved with a particular agonist
Usually expressed as Emax: maximum effect that can be achieved with that drug

23
Q

Full agonist

A

High/low potency, maximum efficacy

24
Q

Partial agonist

A

High/low potency, reduced efficacy

25
Q

Inverse agonists

A

Stabilize the inactive state or destabilizes the active state
Reduces constitutive receptor activation
Has an independent impact on receptor activity
Opposite effect of agonist: classified as an agonist as it has a functional impact on the receptor

26
Q

Chemical antagonism

A

Direct interaction of two substances in solution such that the effects of one or both is lost
ie. acid and base anticoagulant

27
Q

Physiological antagonism

A

Indirect interaction of two substances with opposing physiological actions
ie. Histamine vs. EN

28
Q

Pharmacological antagonism

A

Blockage of interaction of one substance with receptor by another substance

29
Q

Pharmacological antagonists

A

Bind to receptors but do not activate signal transduction mechanisms
Biological effects derived from blocking ability of agonist to bind/activate receptor

30
Q

Competitive antagonists

A

Bind reversibly to receptor
Inhibition can be overcome by increasing agonist concentration
Primarily affect agonist potency but can still achieve same magnitude of biological affect

31
Q

Non-competitive antagonists

A

Bind irreversibly to receptor or reversibly/irreversibly to allosteric site
Inhibition cannot be overcome by increasing agonist concentration
Primarily affect efficacy

32
Q

IC50

A

Inhibitory concentration

33
Q

Endogenous receptor ligands

A 
Such as hormones and neurotransmitters
Mostly are agonists
Inverse agonists are rare
Antagonists are rare
Some drugs mimic effect of endogenous agonists and some block
34
Q

Epinephrine

A

Full agonist of cardiac beta2-adrenergic receptor to increase rate and force of heart contraction

35
Q

Agouti-related Peptide

A

AGRP
Endogenous inverse agonist
Reduces constitutive receptor activity of melanocortin receptor

36
Q

Kynurenic Acid

A

Endogenous pure antagonist
NMDA receptor antagonist
Physiological role unclear but may play a role in neurotransmission and neuropathologies

37
Q

Isoproterenol

A

Full agonist that mimics epinephrine at cardiac beta2 adrenergic receptor

38
Q

Buprenorphine

A

Partial agonist that mimics endogenous endorphins at n-opiod receptor
Safer analgesic than morphine due to less rest of respiratory depression

39
Q

Superagonists

A

> 100% Emax

Uncommon in clinical practice

40
Q

Propranolol

A

Pure antagonist of epinephrine at cardiac beta2-adrenergi receptor

41
Q

Drug desensitization

A

Effect of drug often diminishes when given continuously or repeatedly
Receptor-mediated and non-receptor mediated mechanisms

42
Q

Receptor mediated drug desensitization

A

Loss of receptor function due to change in receptor conformation
Reduction of receptor number

43
Q

Non-receptor mediated drug desensitization

A

Reduction of receptor-coupled signalling components
Increased metabolic degradation
Physiological adaptation

44
Q

Adverse drug effects

A
  1. Side effect
  2. Toxic reaction
  3. Allergic reaction
45
Q

Side effect

A

Dose dependent
Not directly related to desired effect of drug
Action of drug at other sites to produce undesirable effects

46
Q

Toxic reaction

A

Dose-dependent
Directly related to desired effect of drug
Excessive action of drug at intended target site

47
Q

Allergic reaction

A

Not dose-dependent
Not related to desired effect of drug
Immunologic response to drug and largely unpredictable

48
Q

Cyclosporine

A

Promotes survival of transplanted organs

Increased susceptibility to infection, kidney damage, rash/hives/itching/breathing difficulties

49
Q

Paracelsus

A

It is not the nature of the drug that determines toxicity, but rather the amount
Everything in excess is potentially toxic

50
Q

Therapeutic index

A

Measure of drug safety
Considers dose required for a toxic or other adverse drug effect versus that required for the desired beneficial effect
Toxic ED50/Beneficial ED50
A larger TI indicated a clinically safer drug

51
Q

Therapeutic window

A

Measure of drug safety that considers the range of blood concentration of a drug that are associated with toxic, therapeutic benefit or lack of effect within a population
If drug falls between window, it fulfills clinical role

Pharmacology 3001 (19 decks)

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