Exam 1 pharmacodynamics

Question 1

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

Answer 1

Most effects (beneficial and harmful)

Question 2

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

Answer 2

drug-receptor complex

Question 3

name a drug that doesn’t work through receptors

Answer 3

antacids

Question 4

drug or naturally occurring molecule that acts as the signal

Answer 4

ligand

Question 5

acts as the signal detector

Answer 5

receptor

Question 6

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

Answer 6

receptor

Question 7

recipient of ligand

Answer 7

receptor

Question 8

where are receptors usually located?

Answer 8

on cell surface

Question 9

2 receptor states

Answer 9

inactive

active

Question 10

subtypes of inactive receptor state

Answer 10

inactive, resting vs recovery phase.

Question 11

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

Answer 11

channel-linked receptors/ Ligand-gated ion channels

Question 12

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

Answer 12

Enzyme linked

Question 13

receptor type that Usually involve second messenger systems.

Answer 13

g-protein coupled receptors

Question 14

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

Answer 14

intracellular receptors

Question 15

4 receptor families

Answer 15

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

Question 16

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

Answer 16

Ligand-gated ion channels

Question 17

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

Answer 17

g-protein coupled receptors

Question 18

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

Answer 18

g-protein coupled receptors

Question 19

receptor type that activates second messengers which cause a cellular response

Answer 19

g-protein coupled receptors

Question 20

receptor family where Responses last several seconds to minutes

Answer 20

g-protein coupled receptors

Question 21

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

Answer 21

yes

Question 22

receptor family where Duration of responses is minutes to hours

Answer 22

Enzyme-linked receptors

Question 23

Most receptors of this type have a tyrosine kinase activity

Answer 23

Enzyme-linked receptors

Question 24

receptor family that Commonly effects metabolism, growth, and differentiation

Answer 24

Enzyme-linked receptors

Question 25

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

Answer 25

Intracellular receptors

Question 26

primary targets of intracellular receptors

Answer 26

transcription factors

Question 27

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

Answer 27

Intracellular receptors

Question 28

examples of intracellular receptors

Answer 28

some hormones, corticosteroids

Question 29

Three Important Features of Receptors and Signal Transduction

Answer 29

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

Question 30

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

Answer 30

Signal amplification

Question 31

Down-regulation can occur when what two things happen?

Answer 31

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

Question 32

dysregulation of receptors disease examples

Answer 32

DMII and myasthenia gravis for example

Question 33

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

Answer 33

Up-regulation when receptor is blocked

Question 34

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

Answer 34

agonist

Question 35

Two major types of agonists

Answer 35

full and partial

Question 36

What are full agonists?

Answer 36

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

Question 37

What are partial agonists?

Answer 37

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

Question 38

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

Answer 38

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

Question 39

what are antagonists?

Answer 39

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

Question 40

types of antagonists?

Answer 40

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

Question 41

these block adrenergic receptors

Answer 41

beta blockers

Question 42

beta blockers are an example of ____.

Answer 42

antagonists

Question 43

what is Competitive Antagonism

Answer 43

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

Question 44

What determines binding in Competitive Antagonism?

Answer 44

affinity

Question 45

how can the effects of irreversible antagonism be overcome?

Answer 45

synthesis of new receptors

Question 46

what happens in irreversible antagonism?

Answer 46

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

Question 47

what is Functional antagonism?

Answer 47

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

Question 48

what is Chemical antagonism?

Answer 48

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

Question 49

examples of Functional antagonism

Answer 49

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

Question 50

example of chemical antagonism

Answer 50

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

Question 51

This is sometimes referred to as “physiologic antagonism”

Answer 51

Functional antagonism

Question 52

when does PK antagonism occur?

Answer 52

occurs when some change to ADME results in decreased effect

Question 53

what is Therapeutic index?

Answer 53

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

Question 54

Loss of therapeutic effects over time

Answer 54

tolerance

Question 55

how can tolerance can be overcome?

Answer 55

by increased doses

Question 56

what is Tachyphylaxis

Answer 56

Rapid tolerance that is NOT dose-dependent

Question 57

Unintended, harmful reactions to medicines when given at therapeutic dose

Answer 57

adverse drug rxn

Question 58

Among the leading cause of death in many countries

Answer 58

ADR

Question 59

% of Americans take at least one medication

Answer 59

80%

Question 60

% of Americans that take five or more medicines

Answer 60

30%

Question 61

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

Answer 61

ADRs

Question 62

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

Answer 62

Extension of therapeutic effect

Question 63

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

Answer 63

Allergy- Non-therapeutic

Question 64

Extreme sensitivity Prolonged drug effects Resistance to drug Unusual response are examples to what kind of ADR?

Answer 64

Idiosyncratic-Non-therapeutic

Question 65

medical error type of ADR

Answer 65

Iatrogenic

Question 66

ADR caused by health provider or someone involved in care

Answer 66

Iatrogenic

Question 67

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

Answer 67

Iatrogenic

Question 68

Prescriber Responsibilities regarding ADRs (5)

Answer 68

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

Question 69

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

Answer 69

Pharmacogenomics

Question 70

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

Answer 70

efficacy or toxicity

Question 71

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

Answer 71

CYP450 genes

Question 72

p-glycoprotein polymorphisms is an example of _______.

Answer 72

genes which are responsible for variances in drug metabolism and response

Question 73

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

Answer 73

phenotypes