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Non-Medical Prescribing Pharmacology Flashcards > PharmoDynamics > Flashcards

PharmoDynamics Flashcards

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USMLE® Step 1 flashcards
1
Q

for drugs to produce their effects they must act on the body at cellular level. The five modes of drug-body action are

A

receptors, enzymes, carrier molecules (transport system) , ion channels

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2
Q

Drug action receptors are found where ?

A

cell membranes

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3
Q

drug action receptors are what type of cell

A

proteins

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4
Q

‘agonist’ drug effect is ? (receptors)

A

mimics a substance is the body naturally produces

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5
Q

‘antagonist’ drug effect is?(receptors)

A

block a natural receptors

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6
Q

what is a partial agonist drug effect(receptors)

A

not as effective as agonist, may be beneficial if people are getting a lot of side effects . i.e. morphine to buprenorphine patch

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7
Q

ion channels are located where

A

cell membrane

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8
Q

ion channel functions

A

to allow ions to transport in and out of the cell

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9
Q

ion examples

A

sodium, k, ca, mg

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10
Q

medications which affect ion channels aim to do what

A

can block the ion channels within the cell preventing ions leaving

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11
Q

example of an ion channel medication

A

calcium channel blockers

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12
Q

Calcium channel blockers do what

A

prevent an influx of ca into the heart muscle - prevent ca coming into the cell, leading to an excitable state which starts contraction

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13
Q

drug modulators (Ion channel)

A

these drugs bind to a receptor on the ion channel , changing the shape - may make it narrower or larger, resulting in a faster or slower flow

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14
Q

drugs that work on enzymes - what is an enzyme

A

it needs to be present for a chemical reaction to occur - catalyst for the reaction to occur, the enzyme has to already be present.

i.e. the drug gets changed into its metabolite by the enzyme i.e. Codeine is given, it is changed by the enzyme into its metabolite - morphine

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15
Q

pro drug example (enzymes)

A

codeine

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16
Q

enzyme inhibitor

A

prevents the enzyme from doing its job

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17
Q

enzyme inhibitor example drug

A

ace inhibitor (angiotensin converting enzyme inhibitor)

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18
Q

Carrier proteins/molecule example drug

A

sertraline
work by extending the life of serotonin

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19
Q

What is a receptor

A

a specialist area on the cell wall within the cellular cytoplasm, the drug will have an affect when it binds with the receptors.

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20
Q

4 Main types of cell receptors

A
  • Ligand-gated ion channels/ionotropic receptors
  • Guanine nucleotide-binding protein (G-protein) receptors
  • Kinase-linked receptors
  • Nuclear receptors
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21
Q

A ligand is a

A

molecule that binds to a receptor. It can be a hormone, neurotransmitter, intracellular messenger molecule or exogenous drug.

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22
Q

G- proteins are found within the cell, are linked to what and activate after what

A

to the receptor and activate after drug molecule binding.

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23
Q

Kinase linked receptors produce a

A

cascade of events after drug binding that lead to drug action.

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24
Q

Nuclear receptors are located

A

WITHIN the cell nucleus and require the drug molecule to cross the nuclear membrane.

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25
Q

Gaba A receptor is what type?

A

Ligand gated ion channel which binds benzodiazepines

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26
Q

G-Protein examples are

A

Adreno-receptors and histamine receptors

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27
Q

Kinase-Linked receptors target what

A

Insulin, cytokine receptors

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28
Q

Nuclear receptors target what

A

thyroid & steroid receptors

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29
Q

Receptors are affected by

A

both internal mechanisms and external factors and so affect the way the body adapts to drugs.

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30
Q

A drug that binds to a receptor and causes activation is called an

A

agonist

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31
Q

A drug that binds to a receptor and prevents activation is called an

A

antagonist

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32
Q

Antagonists are

A

chemical molecules or drugs that bind to their target receptors to prevent naturally occurring substances within the body from binding to them.

33
Q

An agonist is a

A

chemical molecule that has the ability to activate a receptor’s cellular activity and promote a response. Many hormones, neurotransmitters and drugs act as agonists.

34
Q

As well as agonists and antagonists, there are also

A

partial agonists and inverse agonists. They can be competitive and non-competitive in their actions.

35
Q

autonomic nervous system receptor name

A

adrenoceptors

36
Q

b1 adrenoceptors are located where

A

in the heart

37
Q

b1 adrenoceptors when activated do what

A

increase HR

38
Q

b2 adrenoreceptors are located where

A

in smooth muscle inc. airway

39
Q

when b2 adrenoreceptors are activated what happens

A

the smooth muscle of the airway relaxes

40
Q

Specificity is ?

A

Chemical messengers interact with receptors by forming chemical bonds with them. Because chemical messengers and receptors are three-dimensional objects they have distinct shapes.

The shapes that fit best together allow the most bonds to form. In this way a receptor is able to distinguish between a chemical messenger - the true signal, and a similar compound that fits less well.

We refer to this as specificity. Consequently epinephrine binds with adrenoceptors, histamine binds with histamine receptors and so on.

41
Q

salbutamol is a

A

ß2 agonist that causes dilation of the airway and you might have guessed that its action makes it especially useful in an asthma attack

42
Q

Q: What does variability in the T-half of drugs refer to?

A

A: Variability in the half-life of drugs, such as caffeine (2.5-4 hrs), which can be influenced by genetic factors and other variables.

43
Q

Q: How can the graph of drug clearance be described in terms of variability?

A

A: The graph can be bimodal, showing two groups: fast clearers and slow clearers.

44
Q

Q: What is meant by genetic variability in drug half-life?
.

A

A: It refers to the differences in how individuals metabolize and clear drugs, often due to variations in their enzyme systems

45
Q

Q: What are some drugs that show variability in metabolism?

A

A: Phenytoin, debrisoquine, and mercaptopurine.

46
Q

Q: What risk is associated with the muscle relaxant suxamethonium?

A

A: It can cause prolonged paralysis in 1 in 3,000 people due to genetic variability.

47
Q

Q: How do Chinese people metabolize alcohol differently?

A

A: They produce higher levels of acetaldehyde, leading to flushing of the skin and palpitations.

48
Q

Q: What is a notable cardiovascular effect of propranolol in Chinese people?

A

A: They are more sensitive to its cardiovascular effects.

49
Q

Q: How do Afro-Caribbeans compare in sensitivity to the cardiovascular effects of propranolol?

A

A: Afro-Caribbeans are less sensitive to these effects compared to Chinese people.

50
Q

Q: Why are older people more likely to experience drug interactions?

A

A: Older people are particularly likely to be on multiple medications.

51
Q

Q: In what two main ways can a drug alter the response to another drug?

A

A: Through pharmacodynamic effects and pharmacokinetic responses.

52
Q

Q: What is a pharmacodynamic effect in drug interactions?

A

A: It is an alteration in the response to the drug with no alteration in the concentration of the drug.

53
Q

Q: When are changes due to drug concentration interactions particularly important?

A

A: These changes are of importance if the drug in question has a narrow therapeutic window.

54
Q

Q: What are the main reasons for variation in drug response?

A

A: Age, genetic factors (polymorphisms), idiosyncratic reactions, disease, and drug interactions.

55
Q

tolerance is defined as

A

decreased response to the same dose of drug that occurs with repeated administration

56
Q

reasons for tolerance

A

reduced absorption, increased elimination (enzyme induction) reduced receptor sensitivity

57
Q

Tolerance - reduced receptor sensitivity ?what happens

A

Tachyphylaxis

58
Q

Tachyphylaxis is what

A

receptors become less sensitive, reduction in the numbers of receptors, reduction in the sensitivity, vacuolisation (caught up in little vacuoles)

59
Q

What drug is prone to tolerance

A

Opiates

60
Q

list the four main targets for drugs

A

receptors, enzymes, ion channels, carrier proteins

61
Q

four main targets for drugs and explain how drugs interact with each of these

A

receptors - recognition molecules , agonist, antagonists,
Enzymes
ion channels - alter electrical potential
carrier protein - if we inhibit them we get a build up of substrate

62
Q

explain the term exogenous

A

from outside the body

63
Q

explain the term endogenous

A

from inside the body (made in the body)

64
Q

explain the term agonist

A

a ligand that binds to and stimulates a receptor

65
Q

explain the term antagonist

A

a ligand that binds to and does not stimulate a receptor, blocking it from being able to be stimulated

66
Q

explain the term partial agonist

A

a ligand that binds to a receptor and partially stimulates it

67
Q

Explain how a G-Protein linked receptor produces a response

A

if an agonist binds - it causes GTP to bind to the G protein which will then interact with a enzyme most commonly adenylate cyclase which will then stimulate cAMP which will then diffuse into the cells, which will make changes in the cell by activating enzymes (amplifying the response)

68
Q

Receptors can be what?

A

Agonist or antagonist (also partial agonist and inverse agonists)

69
Q

Ion channels can be what?

A

blockers or modulators

70
Q

enzymes can be what?

A

inhibitory, false substrate or prodrug

71
Q

carrier proteins can be what?

A

normal transport or inhibitor

72
Q

Receptor - Agonist - Direct will do what

A

open the ion channel or close it

73
Q

Receptor - Transduction mechanisms - will do what

A

Enzyme activation/inhibition, ion channel modulation, DNA transcription

74
Q

Ion channel blocker will do what

A

permeation blocked

75
Q

ion channel modulator will do what

A

increase or decrease opening probability

76
Q

enzyme inhibitor will do what

A

normal reaction inhibited

77
Q

enzyme false substrate will do what

A

produce an abnormal metabolite

78
Q

enzyme prodrug will do what

A

active drug will be produced

79
Q
A

Non-Medical Prescribing Pharmacology Flashcards (3 decks)

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