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pharmacology > admin. and elim. > Flashcards

admin. and elim. Flashcards

1
Q

define bioavailability

A

how much of a drug gets through the liver to get an active response

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2
Q

how long does oral administration take?

A

30-90 minutes

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3
Q

advantages of oral administration?

A

cheap

easy

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4
Q

when a drug is taken orally, where does it then go?

A

to the gut (GI system) and then to the liver

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5
Q

how long does IV admin take?

A

2-3 minutes

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6
Q

what is the bioavailability of oral?

A

10-50%

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7
Q

what is the bioavailability of IV?

A

100%

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8
Q

how long does intramuscular and subcutaneous take?

A

10-20 minutes

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9
Q

how do you administer a drug subcutaneously?

A

into fat deposition

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10
Q

how do you administer a drug intramuscularly?

A

into the muscle

quad or deltoid administration

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11
Q

when would you use IM or subcutaneous?

A

when you want a slower release of the drug but to bypass 1st metabolism of the liver

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12
Q

how long does rectal administration take?

A

5-10 minutes

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13
Q

how is the drug metabolised rectally?

A

by the liver via the anterior mesenteric artery

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14
Q

how does inhalation of the drug work?

A

goes to the lungs then the bloodstream

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15
Q

how does transdermal work?

A

patches applied to the skin then enters the bloodstream

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16
Q

how does topical work?

A

applied directly to the skin so it has a local action

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17
Q

how are transdermal and topical different?

A

transdermal - into bloodstream

topical - local effect

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18
Q

what is sublingual?

A

under the tongue

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19
Q

why is sublingual administration so fast?

A

underneath the tongue has such a rich blood supply and it bypasses the liver

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20
Q

how does intranasal work?

A

into the nose

local or into blood stream

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21
Q

how does intrathecal work

A

into the cerebrospinal fluid into the ventricular system or into the bloodstream

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22
Q

what is an advantage of intrathecal administration?

A

bypasses the BBB to allow drugs to work on the brain

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23
Q

what is epidural administration?

A

outside of the spinal dura

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24
Q

when is epidural administration used?

A

local anaesthetic for peripheral nerve and spinal nerve

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25
Q

where does intraarticular administration go?

A

into the joint space

26
Q

what is the fastest route of administration?

A

IV

27
Q

what are the slowest routes of administration

A

IM and oral

28
Q

how do drugs go from the GI tract to the liver?

A

portal vein

29
Q

where does first pass metabolism occur?

A

gut and liver

30
Q

what is first pass metabolism?

A

when the concentration of the drug is greatly reduced before it reaches the systemic circulation

31
Q

what is a pro-drug?

A

a biological inactive parent drug that requires a chemical or enzymatic transformation to release active drug

32
Q

Where are pro-drugs converted into the active form?

A

The liver

33
Q

how are pro-drugs converted into the active form?

A

liver enzymes cleaves off the carrier molecule, activating the drug rather than the drug just being digested

34
Q

what is the purpose of pro-drugs?

A

protecting the drug from first pass metabolism in the liver

35
Q

give an example of a pro-drug and how it works

A

L-dopa - used to treat Parkinsons

As a protected molecule it can cross the BBB

36
Q

advantage of using L-dopa as a prodrug?

A

smaller dose given which is safer

37
Q

explain how pro-drugs are used in cancer medication?

A

tumour specific gene delivery
enzyme expression so that prodrug can bind
toxic drug is given as a prodrug and only targets cancer cells which have the enzyme
cytotoxic drug kills the tumour cell
cell dies and drug goes to neighbouring drugs - bystander effect

38
Q

what are the two categories of reactions that happen in the liver?

A

phase 1 and 2

39
Q

what happens in phase 1 liver reactions?

A

biotransformation to make drug more water soluble so it can be excreted.

40
Q

name examples of reactions that happen in phase 1 reactions?

A

oxidation
hydrolysis
reduction

41
Q

what happens in phase 2 reactions?

A

synthesis reactions to become more water soluble

42
Q

name examples of reactions that happen in phase 2 reactions?

A

conjugation with glycine, sulfate, glucuronic acid

43
Q

name the methods of eliminating a drug?

A 
renal
hepatic
breathing
sweating
urine
fecal
44
Q

what is the main metabolic organ?

A

the liver

45
Q

what things can happen to a metabolite that leaves the bile via the liver?

A

excreted in the kidneys

reabsorbed and go back to the liver

46
Q

what is clearance?

A

rate of elimination in relation to drug concentration in the plasma

47
Q

how is clearance calculated?

A

rate of elimination divided by concentration remaining

48
Q

define half life of a drug

A

time taken for plasma concentration to reduce to half its original concentration

49
Q

how is half life calculated?

A

volume of distribution divided by clearance x0.7

50
Q

define zero order elimination

A

the elimination of a constant quantity of a drug per unit time

51
Q

define first order elimination

A

the elimination of a constant fraction per unit time

52
Q

which order of elimination do most drugs use?

A

first

53
Q

how many half lives does it take for a drug to be removed from the body?

A

5

54
Q

what is the therapeutic window?

A

where a drug has therapeutic effects

55
Q

what is the lag period?

A

the time before therapeutic effect - time for absorption to happen and drug to get into circulation

56
Q

what is the safe range of a drug?

A

between the minimum therapeutic concentration and the minimum toxic concentration

57
Q

before how many half lives will accumulation occur?

A

4

58
Q

what is a loading dose?

A

a larger dose given to get into the therapeutic range quicker

59
Q

what is a maintenance dose?

A

maintains the drug in the therapeutic window

60
Q

what factors effect drug metabolism?

A 
ethnicity
age
gender
diet
environment
drug interactions
diseases

pharmacology (5 decks)

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