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Pharmacology > Pharmacodynamics > Flashcards

Pharmacodynamics Flashcards

1
Q

Pharmacodynamics

A

Action of drug on body. Determined by the drug-receptor interactions

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2
Q

What initiates biochemical or molecular activity

A

The drug-receptor complex

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3
Q

Drug receptor complex

A

The free drug binds to a receptor (either on a cell or on a plasma protein, etc)

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4
Q

Receptor

A

Any molecule to which a drug can bind and produce a measurable response

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5
Q

Types of receptors

A

Proteins, enzymes, nucleic acids, etc

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6
Q

Types of receptors

A
  1. G-protein
  2. Ligand-gated ion channels
  3. Enzyme linked receptors (insulin)
  4. IC receptors
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7
Q

Ion channels

A

Transmembrane protein channels that regulate the flow of ions across the membrane.

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8
Q

What regulates ion channels

A

The binding of a ligand (in this case the drug)

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9
Q

Example of ion channel

A

Nicotinic receptor stimulated by each results in Na influx, which creates an action potential

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10
Q

Protein receptors (g-protein)

A

7 pass membrane protein, ligand binds to receptor, which causes a release of the IC gamma, alpha, beta proteins and initiates a cascade

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11
Q

second messengers

A

These are receptors that are located inside the cell and are activated from the cascade. Turned on by G protein

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12
Q

Enzyme-linked receptors

A

A protein that spans the membrane once and forms dimers or subunit complexes

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13
Q

What happens when a ligand binds to an enzyme-linked receptor

A

Activates OR inhibits the cytosolic enzyme activity

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14
Q

What are the most common enzyme-linked receptors

A

Those that have tyrosine kinase in their structure (ex: platelet derived growth factory

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15
Q

Intracellular receptor

A

Receptor is entirely inside the cell, the ligand must therefore diffuse into the cell

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16
Q

What type of molecule will interact with an IC receptor

A

something that is lipid soluble

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17
Q

Signal amplification

A

A receptors ability to amplify the signal duration and intensity once it binds with a ligand

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18
Q

What are the 2 features of signal transduction

A
  1. Ability to amplify small signals

2. Mechanisms to protect the cell from excessive stimulation

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19
Q

Examples of chemicals or molecules that induce signal amplification

A
  1. hormones
  2. neurotransmitters
  3. peptides
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20
Q

How does signal amplification occur

A

A single ligand-receptor complex can interact with many G proteins, which multiplies the original signal

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21
Q

Desensitization

A

Occurs when the repeated administration of a drug results in the receptor being desensitized to the action of the drug. Receptors are still present on the cell but are unresponsive to the drug

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22
Q

Tachyphylaxis

A

Repeated drug administration that results in a diminished effect of the drug

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23
Q

Down-regulation

A

Reducing the number of receptors available for ligand (drug) to bind to. Can happen if the receptor undergoes endocytosis and recycled

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24
Q

Prototype drug

A

The first form of the a drug that is used to create alternative forms. Also called lead agents

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25
Q

Pharmacologic classification

A

Classification of a drug is based on what the medication does in the body. (i.e. propranolol is a beta blocker)

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26
Q

Therapeutic classification

A

Classification groups meds by outcomes (i.e. grouping drugs as antihypertensive)

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27
Q

Mechanism of action

A

How the medication actually works in the body (at the cellular or organ level). What the drug will be doing in the body to achieve the therapeutic effect

28
Q

Major adverse reactions

A

Any major side effect that has been reported with the medication

29
Q

Clinically significant drug or diagnostic test interaction

A

Any drug to drug interaction or any way that the drug may interact with a given diagnostic test (i.e. contrast)

30
Q

Contraindications

A

Any reason the drug should not be prescribed to a patient

31
Q

Efficacy

A

The degree to which a drug is able to induce maximal effects

32
Q

Issues with Renal and hepatic function in prescribing meds

A
  1. Dose may need to be reduced if pt has kidney failure or issues
  2. Dose reduction with liver enzyme problems
33
Q

Which patient demographic are liver enzymes underdeveloped

A

Infants and elderly patients

34
Q

Concomitant disease

A

Is a second illness occurring at the same time as a primary illness (i.e. pt with pneumonia complicated by a kidney infection)

35
Q

Concurrent therapy

A

Administering medical treatments at the same time as other therapies.

36
Q

Indications

A

A symptom or particular circumstance that indicates the necessity for medical treatment or intervention

37
Q

Absolute contraindications

A

Means the the medication or treatment could cause a life threatening situation

38
Q

Relative contraindications

A

Caution should be used when two drugs or procedures are used together (done if the benefit outweighs the risk)

39
Q

Contraindication

A

Situation in which drug, procedure, surgery, etc should bot be used because it may be harmful

40
Q

Agonist

A

An agent (ligand) that binds to a receptor and elicits a biological response (signals an IC response)

41
Q

What does the magnitude of the drug effect depend on

A

Drug concentration at the receptor site

42
Q

What determines drug concentration at receptor site

A

Pharmacokinetics:

  1. Dose of drug
  2. Rate of absorption
  3. Metabolism
  4. Elimination
43
Q

Potency

A

The amount of drug necessary to produce an effect of a give magnitude

44
Q

The more potent a drug

A

The less time it takes to produce desired effect

45
Q

The less potent a drug

A

The more time it takes to produce desired effect

46
Q

Partial agonist

A

Is a weak agonist or weak drug. It will still bind to a receptor but the IC response is much weaker than with a strong agonist

47
Q

Antagonist

A

Is a drug/ligand that binds to the receptor site and blocks cellular reaction. This will block drugs from interacting with cells and decrease actions of drug

48
Q

What is efficacy dependent upon

A

The # of drug-receptor complexes formed and the efficiency of the cellular response

49
Q

Which drug is more potent: Small EC50 or large EC50

A

Small, because it requires less drug concentration to reach 50% of desired effect

50
Q

Inverse agonist

A

A drug that binds to the same receptor as the agonist but induces the opposite effect of the agonist

51
Q

Competitive antagonist

A

If the antagonist and the agonist bind to the same site on the receptor.

52
Q

What happens in competitive antagonism

A

The competitive antagonist will prevent the agonist from binding to receptors

53
Q

Irreversible antagonists

A

Binding that cannot be overcome by adding more agonist. Blocks the ability for agonist to bind

54
Q

How are the effects of competitive antagonists overcome

A

By adding more agonist

55
Q

What effect does irreversible antagonism have on curve

A

Downward shift of the maximum, and no shift of the curve on the dose axis

56
Q

EC50

A

The amount of drug it takes to reach 50% of desired effect

57
Q

Kd

A

Represents the receptor affinity and is the concentration in which half of the receptors are bound

58
Q

What does a lower Kd mean in relation to potency

A

Means the drug will be more potent. If the Kd is low, then the concentration of the drug that binds 50% of the receptors, means that the time it takes to reach max effect is short = potent

59
Q

Purposeful reaction

A

A reaction from a drug that was intended and/or expected and is beneficial

60
Q

Beneficial reaction

A

A reaction from a drug that is considered positive

61
Q

Inadvertent reaction

A

Opposite of purposeful. The reaction was NOT intended

62
Q

Adverse reaction

A

Opposite of beneficial reaction. Drug that causes a negative outcome

63
Q

Chemical name of the drug

A

Based on molecular structure

64
Q

Generic name

A

These drugs are copies of the brand name drugs. Named by the United States Adopted names council

65
Q

Proprietary name

A

The trade, brand name is owned and chosen by the firm that markets a specific product (zocor)

66
Q

Bioequivalence

A

When 2 drugs have the same bioavailability (rate and extent of absorption are equal)

67
Q

Therapeutic equivalence

A

When 2 drugs are bioequivalents AND they have the same clinical effect/safety profile

Pharmacology (9 decks)

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