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MUSC Pharmacology > Exam 1 pharmacodynamics > Flashcards

Exam 1 pharmacodynamics Flashcards

1
Q

_____ are the result of interactions between drug and a receptor on or within a cell

A

Most effects (beneficial and harmful)

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2
Q

what initiates alterations in biochemical and/or molecular activity through signal transduction?

A

drug-receptor complex

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3
Q

name a drug that doesn’t work through receptors

A

antacids

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4
Q

drug or naturally occurring molecule that acts as the signal

A

ligand

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5
Q

acts as the signal detector

A

receptor

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6
Q

Pharmacologically, this is any biologic molecule to which a drug binds and produces a measurable response

A

receptor

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7
Q

recipient of ligand

A

receptor

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8
Q

where are receptors usually located?

A

on cell surface

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9
Q

2 receptor states

A

inactive

active

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10
Q

subtypes of inactive receptor state

A

inactive, resting vs recovery phase.

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11
Q

type of receptors where Ligand binds on receptor and opens channel which allows ions through

A

channel-linked receptors/ Ligand-gated ion channels

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12
Q

type of receptors where ligand binds to receptor outside of cell, activates inside of cell and enzyme generates product.

A

Enzyme linked

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13
Q

receptor type that Usually involve second messenger systems.

A

g-protein coupled receptors

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14
Q

receptor type where Receptors are fully inside cell, and the drug molecule needs to go through membrane to get inside of cell.

A

intracellular receptors

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15
Q

4 receptor families

A
  1. Ligand-gated ion channels
  2. Enzyme linked
  3. g-protein coupled receptors
  4. intracellular receptors
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16
Q

receptor family where Response is very rapid, i.e. few milliseconds

A

Ligand-gated ion channels

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17
Q

receptor family where Ligand binding results in activation of the G proteins which causes dissociation and the subsequent interaction with other cellular effectors

A

g-protein coupled receptors

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18
Q

type of Receptors that can be down-regulated to prevent over-stimulation and they are recycled constantly

A

g-protein coupled receptors

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19
Q

receptor type that activates second messengers which cause a cellular response

A

g-protein coupled receptors

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20
Q

receptor family where Responses last several seconds to minutes

A

g-protein coupled receptors

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21
Q

can more than one G protein can be associated with each receptor to amplify the signal?

A

yes

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22
Q

receptor family where Duration of responses is minutes to hours

A

Enzyme-linked receptors

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23
Q

Most receptors of this type have a tyrosine kinase activity

A

Enzyme-linked receptors

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24
Q

receptor family that Commonly effects metabolism, growth, and differentiation

A

Enzyme-linked receptors

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25
Q

receptor family where Ligand must be lipophilic (to through membrane)

A

Intracellular receptors

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26
Q

primary targets of intracellular receptors

A

transcription factors

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27
Q

receptor family that Often takes hours-days-months to get outcomes

A

Intracellular receptors

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28
Q

examples of intracellular receptors

A

some hormones, corticosteroids

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29
Q

Three Important Features of Receptors and Signal Transduction

A
  1. Signal amplification
  2. Desensitization and down-regulation of receptors
  3. Up-regulation when receptor is blocked
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30
Q

what is particularly important to receptors that respond to hormones, neurotransmitters, and peptides

A

Signal amplification

31
Q

Down-regulation can occur when what two things happen?

A
  1. Receptor undergoes endocytosis and is recycled after some period of time
  2. Receptor is degraded which reduces total number of receptors
32
Q

dysregulation of receptors disease examples

A

DMII and myasthenia gravis for example

33
Q

This mainly occurs when receptor-blocking drugs are given over periods of time and/or at high doses

A

Up-regulation when receptor is blocked

34
Q

An ________ binds to a receptor and influences the normal physiologic response

A

agonist

35
Q

Two major types of agonists

A

full and partial

36
Q

What are full agonists?

A

activate the receptor to result in maximal (“normal”) physiologic response of the endogenous ligand

37
Q

What are partial agonists?

A

partially activate the receptor to result in a response that is less than the maximal endogenous response

38
Q

third uncommon type of agonist is inverse. what does inverse agonist do?

A

causes receptor to be inactive state so there is no biologic response

39
Q

what are antagonists?

A

Bind to receptors but do not active them so results in blockade preventing binding of endogenous ligand

40
Q

types of antagonists?

A

Competitive/reversible antagonists (blocks binding)
Irreversible antagonists (blocks binding)
Functional and chemical antagonism

41
Q

these block adrenergic receptors

A

beta blockers

42
Q

beta blockers are an example of ____.

A

antagonists

43
Q

what is Competitive Antagonism

A

when Both antagonist and agonist can bind to receptor so they compete

44
Q

What determines binding in Competitive Antagonism?

A

affinity

45
Q

how can the effects of irreversible antagonism be overcome?

A

synthesis of new receptors

46
Q

what happens in irreversible antagonism?

A

The drug binds covalently or with very high affinity to the active site of the receptor which prevents anything else from activating the receptor

47
Q

what is Functional antagonism?

A

when the ligand acts at a completely separate receptor and initiate effects that are functionally opposite those of the agonist

48
Q

what is Chemical antagonism?

A

when a chemical modifies or sequesters the agonist so that it is incapable of binding to and activating its receptor

49
Q

examples of Functional antagonism

A

histamine at the H1 histamine receptors v. epinephrine at the β2-adrenergic receptors in bronchial smooth muscle

50
Q

example of chemical antagonism

A

protamine sulfate basic (positive charge) protein binds to heparin with is acidic (neg charge)

51
Q

This is sometimes referred to as “physiologic antagonism”

A

Functional antagonism

52
Q

when does PK antagonism occur?

A

occurs when some change to ADME results in decreased effect

53
Q

what is Therapeutic index?

A

ratio of dose that produces toxicity to the dose that produces a clinically desired or effective response in a population of individuals

54
Q

Loss of therapeutic effects over time

A

tolerance

55
Q

how can tolerance can be overcome?

A

by increased doses

56
Q

what is Tachyphylaxis

A

Rapid tolerance that is NOT dose-dependent

57
Q

Unintended, harmful reactions to medicines when given at therapeutic dose

A

adverse drug rxn

58
Q

Among the leading cause of death in many countries

A

ADR

59
Q

% of Americans take at least one medication

A

80%

60
Q

% of Americans that take five or more medicines

A

30%

61
Q

700,000 ED visits and 120,000 hospitalizations annually are caused from ____.

A

ADRs

62
Q

Low BP after antihypertensive and
Fungal overgrowth after antibiotics
are examples of what type if ADR

A

Extension of therapeutic effect

63
Q

type of ADR that occurs when IgE-mediated response leads to increased release of inflammation mediators

A

Allergy- Non-therapeutic

64
Q

Extreme sensitivity
Prolonged drug effects
Resistance to drug
Unusual response

are examples to what kind of ADR?

A

Idiosyncratic-Non-therapeutic

65
Q

medical error type of ADR

A

Iatrogenic

66
Q

ADR caused by health provider or someone involved in care

A

Iatrogenic

67
Q

these are examples of what type of ADR?
20 U of insulin ordered but the “U” was read as 0 and 200 units administered

10 mg methotrexate ordered daily but should be weekly

Patient’s caregiver applies 6 pain patches at one time because they were not counseled to remove each one when applying a new one

A

Iatrogenic

68
Q

Prescriber Responsibilities regarding ADRs (5)

A 
Ensure the “rights”
Use minimally effective dose
Evaluate patient and family history
Evaluate possible interactions
Patient education
69
Q

Study of how genetic makeup affects an individual’s response to drugs

A

Pharmacogenomics

70
Q

Difference in gene expression or single-nucleotide polymorphisms correlates with ______.

A

efficacy or toxicity

71
Q

Several known genes which are responsible for variances in drug metabolism and response. most common variations are associated with what gene?

A

CYP450 genes

72
Q

p-glycoprotein polymorphisms is an example of _______.

A

genes which are responsible for variances in drug metabolism and response

73
Q

different ______ lead to variations in ability, or lack thereof, to metabolize some medications

A

phenotypes

MUSC Pharmacology (10 decks)

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