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FUN F > F9 Introduction to pharmacokinetics (ADME) > Flashcards

F9 Introduction to pharmacokinetics (ADME) Flashcards

1
Q

what is pharmacokinetics?

A
  • the movement of the drug (ADMET)
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2
Q

what is pharmacodynamics?

A
  • the effect of the drug on the body
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3
Q

how can drugs access their target sites?

A

direct to site
- easy for skin, eye, gut, lung
- much more difficult for other sites but can be done

indirect
- via systemic circulation (blood)
- introduces problems of loss or dilution
- how will drug reach target site only?
- certain body places can only be accessed through systemic circulation

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4
Q

what does the umbrella term ‘elimination’ involve?

A
  • metabolism
  • excretion
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5
Q

what are the main routes for drug administration?

A
  • inhalation
  • oral
  • injection
  • transdermal
  • rectal
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6
Q

what is the inhalation administration method of drugs preferred for?

A
  • gases
  • volatiles
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7
Q

what is the oral administration method of drugs preferred for?

A
  • tablets
  • capsules
  • solutions
  • buccal
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8
Q

what is the injection administration method of drugs preferred for?

A
  • intravenous
  • intramuscular
  • subcutaneous
  • intrathecal
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9
Q

what is intrathecal administration of drugs?

A
  • in the spinal cord into the spinal fluid
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10
Q

what is the transdermal administration method of drugs preferred for?

A
  • patch
  • cream
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11
Q

what is absorption in ADME and what routes of administration require this?

A
  • drug must enter the bloodstream from the site of administration
  • all routes other than intravenous injection require an absorption step
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12
Q

what is the site of absorption for oral administration?

A

somewhere along the GIT

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13
Q

what is the site of absorption for transdermal administration?

A

across the skin

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14
Q

what is the site of absorption for hypodermic injection administration?

A

from injection site (muscle, adipose tissue)

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15
Q

what is the site of absorption for lung administration?

A
  • alveolar surface
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16
Q

what feature makes molecules more likely to passively diffuse across a lipid bilayer?

A

more lipophilic = more likely to passively diffuse

17
Q

describe the distribution step of ADME

A
  • drug travels in systemic circulation after absorption
  • perfuses all organs and tissues of the body
  • closed system: drug makes continuous and multiple passes around the body and allows drugs to reach organs due to passing through continuously
18
Q

what determines drug distribution?

A
  • drug binding to plasma proteins
  • structure of vascular endothelium
  • accumulation in tissue depots
19
Q

how does the drug binding to plasma proteins affect drug distribution?

A
  • reversible binding can ferry drug around the circulation
  • very high affinity binding can limit escape from the plasma and limits ability of drug to into the tissues
20
Q

how does the structure of vascular endothelium affect drug distribution?

A
  • there are pores between endothelium cells in most vessel beds
  • some special cases = blood brain barrier and placenta
21
Q

describe the blood brain barrier in terms of distribution

A
  • capillary cells into brain have tightly packed endothelial cells and have an additional layer of these cells
  • this makes the access to the brain tightly regulated
22
Q

describe the placenta in terms of distribution

A
  • has the capacity to protect the foetus from harmful components of the blood
23
Q

how does the accumulation in tissue depots affect drug distribution?

A
  • protein binding sites (including target!)
  • adipose tissue
24
Q

state the body parts in the highly-perfused lean tissue group

A
  • blood cells
  • heart
  • lung
  • liver
  • kidney
  • glands
  • brain
  • blood-rich organs so lots of blood gets to these
25
Q

state the body parts in the poorly-perfused lean tissue group

A
  • muscle
  • skin
26
Q

state the body parts in the fat group

A
  • adipose tissue
  • bone marrow
27
Q

state the body parts in the negligible perfusion group

A
  • teeth
  • hair
  • bone
  • tendon
  • cartilage
  • extremely minute blood flow
28
Q

what is the liver packed full of?

A
  • broad-spectrum metabolic enzymes
  • many isoforms
  • many substrates
  • many reactions
  • many products
29
Q

what are the 2 phases that occur to drugs in the liver and what is their purpose?

A
  1. redox reactions to add charge and/or reactive centres
  2. conjugation reactions to add bulky groups
  • purpose is to make drug into a form that can easily be excreted from the body by the kidney
30
Q
A
31
Q

how does excretion mainly occur?

A
  • mainly in the urine via the kidney
  • some large drugs are excreted in bile
  • can also occur in other ways eg. via the lung, but this isn’t as common
32
Q

what are the 3 key stages of excretion?

A
  • passive filtration
  • active secretion
  • reabsorption
33
Q
A

FUN F (9 decks)

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