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physiology > fundamentals of pharmacology > Flashcards

fundamentals of pharmacology Flashcards

1
Q

what is a drug ?

A

a chemical substance of know structure, other than a nutrient or an essential dietary ingredient, which, when administered to a living organism, produces a biological effect

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2
Q

what makes a good medicinal drug ?

A
  • drug can be delivered to its site of action
  • it will act once at the site of action
  • the drug will stay in that place
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3
Q

how are drugs named ?

A
  • chemical name
  • common name
  • proprietary (trade) name
  • therapeutic uses
  • mechanism of action
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4
Q

how do drugs produce their effects ?

A

exogenous molecules that mimic or block the actions of endogenous molecules
bind to molecular targets ( receptors)

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5
Q

what are some examples of receptors in the body ?

A
  • receptors for neurotransmitters or hormone
  • enzyme
  • ion channels
  • carrier or transporter molecules
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6
Q

what effects the binding of a drug ?

A
  • the size and flexibility of the drug
  • ## nature of chemical bonds that form between drug molecule and its binding site
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7
Q

why do drugs have side effects ?

A
  • drug binding isnt completely specific
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8
Q

what is pharmacodynamics

A

what drugs does to the body

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9
Q

what is pharmacokinetics ?

A

what the body does to the drug

how drug is handled by the organism

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10
Q

what are the critical elements of pharmacokinetics

A
  • absorption
  • distribution
  • metabolism
  • excretion
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11
Q

what is absorption ?

A

determines how much and how quickly the drug enters the blood

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12
Q

what is absorption influenced by ?

A
  • drugs molecular size
  • lipid solubility
  • chemical stability
  • the route by which the drug is adminstered
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13
Q

what is distribution?

A

where the drug goes after its been absorbed

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14
Q

what determines the drugs distribution ?

A
  • drugs need to circulate in blood plasma and diffuse into tissue through ECF
  • ability to do this is determined by a drugs water solubility
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15
Q

what can interfere with a drugs distribution ?

A
  • circulation of patient
  • drug sticking to proteins in blood plasma
  • drugs partitioning into fat stores
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16
Q

what is the volume of distribution ?

A
  • the volume the drug would occupy if the total amount administered was dissolved in solution at the same concentration as that found in the blood plasma
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17
Q

what 2 factors determine how long the drug effect will last ?

A
  • metabolism happen in liver

- excretion by the kidneys

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18
Q

what are some routes of excretion ?

A
  • urine
  • faeces
  • sweat
  • bile
  • breath
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19
Q

what is a drugs half life ?

A

the time it takes for the plasma concentration to fall by half
concentration follows monoexponential decline

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20
Q

what is clearance ?

A

the volume of blood plasma cleared of the drug in unit time

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21
Q

how long does the preclinical stages of a drug take ?

A

5-10 years

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22
Q

how many phases is there in clinical development of a drug ?

A

4 phases

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23
Q

what is the first clinical stage ?

A
  • exploratory phase first look into drug reaction on humans
  • last 6 months to a year
  • purpose is to check for safety + tolerability
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24
Q

who is the drugs tested on in phase 1 ?

A
  • healthy volunteers
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25
Q

what is phase II ?

A

divided into 2 :

  • phase IIa
  • phase IIb
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26
Q

what is phase IIa ?

A
  • exploratory phase
  • 50 - 200 patients
  • checks how drug acts
  • dosage and treatment regimen established
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27
Q

what is phase IIb ?

A

confirmatory stage

  • 200 - 500 patients
  • last approx 2 years
  • safety + efficacy compared to placebo/ current treatment
28
Q

what is phase III ?

A

drug tested in 2000-10,000

- evaluation to see how effctive + safe treatment actually is

29
Q

what is phase IV ?

A
  • on going
  • continues when drug is licensed and on market
  • mointers consequences of drug
30
Q

give some examples of drug regulatory bodies :

A

medicines and healthcare regulatory agency (MHRA)
european medicine agency (EMA)
food and drug administration (FDA)

31
Q

What is a concentration- response relationship

A
  • quantified drug effects

- relationship between drug conc and response of drug

32
Q

What is Emax

A

Maximum effect that a drug can produce

33
Q

What is EC50 ?

A

Concentration of drug that produces 50% of maximum response

34
Q

Where do receptors usually insert ?

A

Across the lipid bilayer

35
Q

What 2 main functions can receptors perform ?

A
  • recognition or detection of extracellular molecules

- can bring changes into cell activity

36
Q

What are receptors often named after ?

A

The drugs they bind to

37
Q

What does highly selective receptors lead to ?

A

Less side effects

38
Q

Describe the binding of drugs to receptors

A

Is reversible

D+ R <> DR

39
Q

What is the affinity of a drug for its receptor quantified as ?

A

The molar concentration of drug required to occupy 50% of the receptors at equilibrium

40
Q

What is KD ?

A

The concentration of a drug

41
Q

Describe the relationship of drug affinity and KD :

A

Drugs with hugh affinity have a low KD

42
Q

What do k+1 and k-1 tell ?

A
  • rate constants

- likelihood of forward and backwards reactions occuring

43
Q

How do you calculate rate of forward reactions ?

A

Rate of forward reaction = k+1 [D][R]

44
Q

How do you calculate rate of backward reactions ?

A

Rate of backward reaction = k-1[DR]

45
Q

What happens at equilibrium?

A

Backward rate = forward rate
k-1[DR] = k+1 [D][R]
KD = k-1/k+1 = [D][R]/[DR]

46
Q

What do agonists do ?

A

Bind and activate the receptor

Produces a change in shape of receptor

47
Q

What does efficacy describe ?

A

The ability of drug to activate the receptor

48
Q

What do agonist have ?

A
  • affinity and efficacy
49
Q

What are some examples of natural agonists ?

A
  • adrenaline
  • acetylcholine
  • insulin
50
Q

What are the 2 types of agonists ?

A
  • partial agonists

- full agonists

51
Q

What are full agonists ?

A
  • have high efficacy

- very effective at activating receptors and producing a biological response

52
Q

What are partial agonists ?

A
  • low efficacy

- less effective at activating receptors and producing a biological response

53
Q

How many other receptors do full agonists activate

A

Only a fraction if available receptors

54
Q

How many other receptors are occupied by partial agonists

A

Occupy all available receptors

55
Q

What are antagonist?

A

Act to inhibit the effects of a neurotransmitter or another drug

56
Q

What are competitive antagonist?

A

Compete with the agonist for the same site on receptor molecule
But dont activate it

57
Q

What are non-competitive antagonist?

A

Act at a different site on the receptor

Or another molecule closely associated with it

58
Q

What are reversible competitive antagonist?

A

Used to inhibit the effcets of a neurotransmitter or hormone

59
Q

What are some examples of reversible competitive antagonist?

A
  • pancurobium
  • cetirizine
  • propranolol
60
Q

How can you overcome the inhibitory effects of reversible competitive antagonist?

A

Increase concentration of agonist

61
Q

How do antagonists impact the concentration vs response curve

A

Produce a parallel shift to the right

62
Q

What is the dose ratio ?

A

The ratio of the concentration of agonist producing the same response in the presence and absence of the antagonist

63
Q

What can the dose ratio been used to measure ?

A

Extent of the shift in the position of the agonist curve

64
Q

What is the extent of the shift ?

A

Measures the affinity of the antagonist for the receptor

65
Q

What is pA2 ?

A

The affinity of an antagonist

66
Q

What are the effects of irreversible competitive antagonist on a concentration response curve

A

Shift to the right which isnt parallel

physiology (18 decks)

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