admin. and elim. Flashcards

(60 cards)

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
where does intraarticular administration go?
into the joint space
26
what is the fastest route of administration?
IV
27
what are the slowest routes of administration
IM and oral
28
how do drugs go from the GI tract to the liver?
portal vein
29
where does first pass metabolism occur?
gut and liver
30
what is first pass metabolism?
when the concentration of the drug is greatly reduced before it reaches the systemic circulation
31
what is a pro-drug?
a biological inactive parent drug that requires a chemical or enzymatic transformation to release active drug
32
Where are pro-drugs converted into the active form?
The liver
33
how are pro-drugs converted into the active form?
liver enzymes cleaves off the carrier molecule, activating the drug rather than the drug just being digested
34
what is the purpose of pro-drugs?
protecting the drug from first pass metabolism in the liver
35
give an example of a pro-drug and how it works
L-dopa - used to treat Parkinsons | As a protected molecule it can cross the BBB
36
advantage of using L-dopa as a prodrug?
smaller dose given which is safer
37
explain how pro-drugs are used in cancer medication?
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
what are the two categories of reactions that happen in the liver?
phase 1 and 2
39
what happens in phase 1 liver reactions?
biotransformation to make drug more water soluble so it can be excreted.
40
name examples of reactions that happen in phase 1 reactions?
oxidation hydrolysis reduction
41
what happens in phase 2 reactions?
synthesis reactions to become more water soluble
42
name examples of reactions that happen in phase 2 reactions?
conjugation with glycine, sulfate, glucuronic acid
43
name the methods of eliminating a drug?
``` renal hepatic breathing sweating urine fecal ```
44
what is the main metabolic organ?
the liver
45
what things can happen to a metabolite that leaves the bile via the liver?
excreted in the kidneys | reabsorbed and go back to the liver
46
what is clearance?
rate of elimination in relation to drug concentration in the plasma
47
how is clearance calculated?
rate of elimination divided by concentration remaining
48
define half life of a drug
time taken for plasma concentration to reduce to half its original concentration
49
how is half life calculated?
volume of distribution divided by clearance x0.7
50
define zero order elimination
the elimination of a constant quantity of a drug per unit time
51
define first order elimination
the elimination of a constant fraction per unit time
52
which order of elimination do most drugs use?
first
53
how many half lives does it take for a drug to be removed from the body?
5
54
what is the therapeutic window?
where a drug has therapeutic effects
55
what is the lag period?
the time before therapeutic effect - time for absorption to happen and drug to get into circulation
56
what is the safe range of a drug?
between the minimum therapeutic concentration and the minimum toxic concentration
57
before how many half lives will accumulation occur?
4
58
what is a loading dose?
a larger dose given to get into the therapeutic range quicker
59
what is a maintenance dose?
maintains the drug in the therapeutic window
60
what factors effect drug metabolism?
``` ethnicity age gender diet environment drug interactions diseases ```