Pharmacodynamics Flashcards

1
Q

Pharmacodynamics

A

What Meds do to the Body

  • Most drugs bind to cell receptors where they initiate reactions that alter cell’s physiology
  • Some of a drug’s molecules will find target cell, some distributed, metabolized, and excreted
  • Drugs exert primary action at cell level
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2
Q

Medication Actions

A

Pharmacology at

cell level, organism level, and population level

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3
Q

Drug Receptors

A
  • Proteins/Glycoproteins on cell surface, organelle inside cell, or cytoplasm
  • Finite mumber - response plateaud once saturated
  • Downregulation/Upregulation
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4
Q

What happens after a drug is bound to the receptor?

A
  • Ion channel opens/closes
  • Activate biochemical messengers, second messengers (cAMP, cGMP, C++, Inositol Phosphates) - each signal that passes amplified
  • Inhibit/Initiate normal cell function
  • Steroids move right into cell w/o help
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5
Q

What is Affinity

A

Strength of binding b/t drug and receptor

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6
Q

Dissociation Constant (Kp)

A

Measure of a drug’s affinity for a given receptor.

The concentration of a drug needed for 50% receptor occupancy

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7
Q

What is an Agonist

A

Drugs that alter physiology of a cell by binding to plasma membrane or intracellular receptors

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8
Q

What is a Strong Agonist

A

Agonist that causes max effects even though it only occupy a small fraction of receptors

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9
Q

What are Weak Agonists

A

Agonists that need to be bound to many more recptors than a strong agonist does to produce same effect

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10
Q

Partial Agonist

A

Drug that fails to produce max effect even when all receptors are occupied

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11
Q

What is an Inverse Agonist

A

Binds to receptor and causes opposite of an agonist. Doesnt block anything from happening, it just reverses what happens

EX: H2 receptor antagonist

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12
Q

What is an Antagonist?

A

Inhibit/Block actions caused by agonists

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13
Q

Competetive Antagonist

A

Competes with Agonist for Receptors

  • Agonist cant bind to receptor while its occupied by antagonist
  • Antagonism can be overcome by high doses of agonists
  • EX: Reversal agents
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14
Q

Noncompetitive Antagonist

A

Binds to site other than the agonist-binding domain.

  • Induces form change in receptor so that agonist no longer recognizes agonist binding domain
  • Insurmountable - high doses cant defeat this antagonism
  • EX: Warfarin
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15
Q

Irreversible Antagonism

A

Agents compete with agonists for the agonist-binding receptor

  • Antagonists bind permanently to receptor
  • Rate of antagonism can be slowed by high # of antagonist
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16
Q

Efficacy

A

Degree that drug is able to cause max effects

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17
Q

Potency

A

Amount of drug needed to produce 50% of max effect that its capable of causing

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18
Q

Potency vs. Efficacy

A
  • Potency used to compare drugs in same class.
    • Drugs in same class usually have same max efficacy
  • Efficacy used to compare drugs with different mechanisms.
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19
Q

Drug-Response Curves

A
  • Graphs magnitude of drug action against concentration/dose of drug needed to induce action
  • Represents effects and dose of drug within individual rather than population
  • Almost all meds plateau at some point
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20
Q

What must be tested on a drug before they are approved for marketing?

A

Efficacy and Safety must be tested in animal and human population studies

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21
Q

What kind of data is derived from testing a drug’s efficacy and safety?

A

EC50: Effective Concentration 50%

LD50: Lethal Dose 50%

Therapeutic Index

Margin of Safety

22
Q

What is Effective Concentration 50%

A

Effective concentration of drug in 50% of test subjects

23
Q

What is Lethal Dose 50%

A

Drug concentration that induces death in 50% of subjects

24
Q

What is Therapeutic Index

A

Measure of safety of drug

LD50/ED50

25
Q

What is Margin of Safety

A

Margin between therapeutic and lethal dose

26
Q

Pregnancy Category A

A

Adequate and Well-Controlled studies have failed to show risk to fetus in first trimester and later trimesters.

27
Q

Pregnancy Category B

A

Animal studies failed to show risk to fetus and no studies in pregnant women

28
Q

Pregnancy Category C

A

Animal studies show adverse effects on fetus and no studies on humans.

BUT

Potential benefits may warrant use on preggos despite potential risks

29
Q

Pregnancy Category D

A

Positive proof human fetal risk, but potential benefits may warrant use of drug on preggos despite potential risks.

30
Q

Pregnancy Category X

A

Animal and Human studies show fetal abmormalities and the risks clearly outweigh potential benefits

EX: Warfarin, ACE Inhibitors

31
Q

Altered Absorption

A

Drugs may inhibit absorption of other drugs

32
Q

Altered Metabolism

A

Important drug interactions can occur when P450 isoenzymes inhbited or induced

33
Q

Plasma Protein Competition

A

Drugs that bind to plasma proteins may compete with other drugs for protein binding sites.

EX: Drug A bumped out by Drug B may cause Toxic Drug A Levels

34
Q

Altered Excretion

A

Drugs may act on kidney to reduce excretion of specific agents

35
Q

Types of Drug Interactions

A

Addition

Synergism

Potentiation

Antagonism

36
Q

Addition Drug Interaction

A

Combined drugs EQUALS combined reponses of each drug

1+1 = 2

37
Q

Synergism Drug Interaction

A

Combined response GREATER THAN combined response of each drug.

1+1 = 3

38
Q

Potentiation Drug Interaction

A

Drug with no effect enhances effect of second drug

0+1 = 2

39
Q

Antagonism Drug Interaction

A

Drug inhibits effect of other drug

1 + 1 = 0

40
Q

Midazolam is siginificant substrate of CYP3A4. Erythromycin is a CYP3A4 inhibitor. How to manage this drug interaction?

A

You can give same dose, but lingering effects and longer time for awakening

41
Q

Propofol is a strong CYP3A4 inhibitor. What side effects woud you expect from sedatives that are metabolized by this enzyme when given together?

A

Synergistic effect if given with versed.

42
Q

Carbamazepine is a strong CYP3A4 inducer. How might you have to alter dose of Versed if given together?

A

Give higher dose and change drugs

43
Q

Tolerance

A

Decreased response to a drug - dose must be increased for same effect.

44
Q

What is Metabolic Drug Tolerance

A

Drug metabolized more rapidly after chronic use

45
Q

What is Cellular Tolerance

A

Decreased number of receptors - downregulation

46
Q

Drug Dependence

A
  • When patient needs drug to function normally
  • When cessation of drug = withdrawal symptoms
  • Physical and/or Psychological
47
Q

Abuse and Addiction

A

Use of meds not for its intended therapeutic use

Use continues despite negative impacts on health, profession, social interactions

48
Q

Withdrawal

A

Occurs when drug is not given to a person who is dependent

Symptoms often opposite the effects achieved by drug

49
Q

Pregnancy Registries

A

Since it’s unethical for drug testing on preggos, this is where the community can report

50
Q

REMS - Risk Evaluation and Mitigation Strategy

A

Way to track drugs with high risk of very dangerous side effects.