pharmacology Flashcards

1
Q

what is pharmocology

A

the study of drugs
Structure, targets, and mechanisms of action

Distribution in and handling by the body

Effects on the body, including desirable responses

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2
Q

what is pharmacokinetics

A

what the body does to the drug

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3
Q

what are the main stages of pharmacokinetics

A

administraction
absorption
first pass metabolism
distribution
metabolism
inhibition and induction
excretion

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4
Q

what are the methods administration of drugs

A
  1. oral
  2. injection
  3. inhilation
  4. sublingual or buccal
  5. rectal
  6. epithelial surfaces
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5
Q

what is the absorption of a drug

A
  1. process of transfer of the drug from the site of administration into the general circulation
  2. influences the access to the systemic circulation
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6
Q

what is the distribution of a drug

A

a compound is transferred from the general circulation to other parts of the body and into the tissues

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7
Q

what is first pass metabolism

A

a drug gets metabolized at a specific location in the body that results in a reduced concentration of the active drug upon reaching its site of action or the systemic circulation

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8
Q

what is excretion of a drug

A

the process by which drugs or their metabolites are removed from the body

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9
Q

what are the methods of excretion of drugs

A
  1. renal
  2. biliary
  3. respiratory
  4. dermal
  5. faecal
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10
Q

what is pharmacodynamics

A

what the drug does to the body

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11
Q

what is a theraputic effect of a drug

A

intended biological effect

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12
Q

what is a side effect

A

Undesirable secondary effect - occurs in addition to the desired therapeutic effect

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13
Q

what is the administration of a drug that produces a side effect

A

Administration of a drug or combination of drugs under normal conditions / dose

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14
Q

what do side effect occur

A

interacts with same type of receptor at different sites around the body

Interacts with more than one type of receptor

Most can be predictable by knowing the pharmacology of the drug

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15
Q

What is an adverse effect

A

harmful reaction

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16
Q

what is the administration of a drug that causes an adverse effect

A

Administration of a drug or combination of drugs under normal conditions of use

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17
Q

what is a toxic effect

A

Deleterious, undesired effect; following administration of a higher dose of the drug

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18
Q

what are the molecular mechanisms of action on a receptor

A

(Direct physicochemical effect)
Transport systems
Enzymes
Interaction with the 4 major types of receptors

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19
Q

what is the direct physiochemical effect

A

dont need to bind to a receptor
- bulk forming laxatives
- antacids
- osmotic diurects

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20
Q

how can drugs inhibit an enzyme

A
  • Binding to the active site – enzyme not able to bind to substrate
  • Binding to another site in the enzyme, changing its conformation – enzyme not able to bind to substrate
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21
Q

what are the 4 major types of receptors

A

ligand-gated ion channels
g protein-coupled receptors
kinase-linked receptors
nuclear receptors

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22
Q

what is the speeds of the 4 receptors

A

ligand-gated ion channels- milliseconds
g protein-coupled receptors- seconds
kinase-linked receptors-hours
nuclear receptors-hours

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23
Q

what is a receptor

A

A protein molecule on the surface / inside the cell

A protein recognition molecule for a chemical mediator

A molecule on the surface of a cell (or inside it) that receives an external signal and produces some type of cellular response

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24
Q

what is the drug-receptor interaction

A

A drug can change the amplitude and speed of body functions
A drug modulate intrinsic physiological functions

25
Q

what is an agonist

A

Bind and simulate physiological regulatory effects of endogenous compounds

26
Q

what is a partal agonist

A

an agonist which is unable to induce maximal activation of a receptor population, regardless of the amount of drug applied

27
Q

what is an antagonist

A

Bind but do not have regulatory effects and prevent the binding of the endogenous compounds

28
Q

what is a competitive antagonist

A

binds to the same site as the agonist but does not activate it, thus blocks the agonist’s action

29
Q

what is a non-competitive antagonist

A

binds to an allosteric (non-agonist) site on the receptor to prevent activation of the receptor

30
Q

what is an irreversible antagonist

A

Binds irreversibly to the receptor (but interacts with same part of the receptor)

31
Q

what are the types of non-competitive antagonist

A

irreversible and allosteric effect

32
Q

what is the allosteric effect of anantagonist

A

Interacts with a different part of the receptor

33
Q

what kind of antagnomism is this

A

resersible competitive antagonism

34
Q

what kind of antagonism is this

A

irreversible competitive antanonism

35
Q

what is functional/ physiological antagonism

A

Drugs that have opposing physiological actions at different receptors

36
Q

what is chemcal antagonism

A

Binds to and inactivates the agonist (not the receptor)

37
Q

what is the two-state model of ligand binding theory

A

Receptors can be in active (constitutive activity) or inactive states

38
Q

what is an inverse agonist

A

inverse agonists bind with active receptors, and move them towards the inactive state

39
Q

what is the mechanism for inverse agonists

A

Inverse agonists bind to a receptor and stabilize it in its inactive conformation. So unlike full or partial agonists, they decrease receptor activity.

40
Q

what is drug selectvity

A

drug’s ability to bind to particular receptor, types or subtypes

41
Q

what is Desensitisation or Tachyphylaxis

A

effect of a drug gradually diminishes when it is given continuously or repeatedly

42
Q

what is tolerance

A

a more gradual decrease in responsiveness to a drug

43
Q

what are Drug-Receptor mechanisms

A

Change in receptors
Translocation of receptors

44
Q

what is the drug response relationship

A

A measure of drug activity expressed in terms of the amount required to produce an effect of given intensity

45
Q

what is the measure of potency of the drug

A

A measure of potency: half maximal effective concentration (EC50)

46
Q

In vivo, what is an ED50 (half maximal effective dose)

A

The concentration of a drug, antibody or toxicant which induces a response halfway between the baseline and maximum after a specified exposure time

47
Q

what is cmax

A

is the maximum (or peak) serum concentration that a drug achieves in a specified compartment or test area of the body after the drug has been administered and before the administration of a second dose

48
Q

what is tmax

A

The time it takes for a drug to reach the maximum concentration (Cmax) after administration of a drug that needs to be absorbed

49
Q

what is the half life of a drug

A

Time for plasma drug concentration to reduce by half
Useful to know time taken to reach steady state and time required for drug elimination

50
Q

what is EC50 and ED50

A

EC50 (half maximal effect in an individual) / ED50 (50% subjects respond to a drug)

51
Q

what is TD50

A

toxic dose

52
Q

what is LD50

A

lethal dose

53
Q

what is the theraputic window

A

The range of drug concentrations within which the drug exhibits maximum efficacy (desired effect) and minimum toxicity in the majority of patients

54
Q

what is the theraputic index

A

how the theraputic window is quantified

55
Q

what is the equation for theraputic index

A

TI= TD50/ED50

56
Q

what is the toxic region

A

adverse effects of drug apparent at the concentrations

57
Q

what is the subtheraputic wregion

A

drug concentrations too low for optimal effects

58
Q

what does a large theraputic index mean

A

wide theraputic window

59
Q

what does a small theraputic index mean

A

narrow theraputic window