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Clinical Life Sciences 2 > Pharmacokinetics > Flashcards

Pharmacokinetics Flashcards

1
Q

Name the 6 main methods of drug administration

A 
Oral 
Intravenous (IV)
Intramuscular (IM)
Intraosseous (IO)
Subcutaneous 
Topical
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2
Q

Where does most drug absorption take place?

A

Small intestine (duodenum - proximal)

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3
Q

How are drugs distributed throughout the body?

A

Bloodstream

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4
Q

Where does the majority of drug metabolism take place?

A

Liver

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5
Q

Where are drugs mainly excreted?

A

Kidneys

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6
Q

What two properties of drugs allow them to be well?absorbed by cells?

A

Fat soluble

Small in size

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7
Q

What two things happen during drug metabolism?

A
  1. Drug broken down by removing fatty acid groups

2. Drug molecule ‘built up’ by adding water soluble groups

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8
Q

What property do drugs need to be excreted via the renal system?

A

Water solubility

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9
Q

List the 4 types of transmembrane proteins

A

Receptors
Pumps
Carriers
Channels/Pores

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10
Q

What is the most common way for drugs to pass through the cell membrane?

A

Simple diffusion

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11
Q

How can drugs use channels?

A

They can utilise or block them

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12
Q

Do pumps/carriers always require energy?

A

No

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13
Q

In drug distribution where does ~1/2 of the drug end up?

A

In tissues

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14
Q

Does a persons fat % affect drug distribution?

A

Yes it varies person to person

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15
Q

What plasma proteins do drugs bind to?

A

Albumin, Globulins and Fibrinogens

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16
Q

Does the brain recieve a higher % of CO than other tissues?

A

Yes

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17
Q

Why is the nervous system a significant reserve for drugs?

A

Due to the high proportion of fat cells (glial cells) contained in it

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18
Q

What are the 3 main features of brain capiliaries which help exclude some drugs from crossing the BBB?

A
  1. One cell thick
  2. Tight junctions
  3. Surrounded by glial cells
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19
Q

What drugs do we want to pass over the BBB? (4)

A

Anaesthetics
Analgesics
Drugs targetting brain (antidepressants)

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20
Q

What is the purpose of the placental barrier?

A

To create a physical barrier between maternal and foetal blood

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21
Q

Where is maternal blood depositied? Where do foetal vessels interact with maternal blood?

A

Lacunae (intervillous spaces)

22
Q

What property of foetal blood vessels helps exclude most toxins?

A

Selective permeability

23
Q

What does metabolism aim to do?

A

Increases water solubility to promote excretion

24
Q

How is metabolism achieved?

A
  1. Addition of water soluble groups

2. Removal of fat soluble groups

25
Q

What are the two main organs of metabolism?

A

Liver and Kidneys

26
Q

Which drug types are converted to an active form by the liver due to their long half life?

A

Opiods and Benzodiazepines

27
Q

Why would you want drugs to be metabolised from an inactive to an active form?

A

Drugs with specific target cells
To bypass the GI tract
(cancer drugs, viral therapies and anti inflammatories)

28
Q

What is first pass metabolism?

A

A phenomenon whereby the concentration of a drug greatly reduces before reaching the systemic circulation

29
Q

What 3 main methods of drug admin are subject to first pass metabolism?

A
  1. Buccal/Oral
  2. Rectal
  3. GI absorption (via hepatic portal vein)
30
Q

Why do children generally metabolise drugs faster?

A

They have a higher metabolic rate

31
Q

Why do babies require smaller doses of drugs?

A

Liver functions and other body systems immature

32
Q

Why do you need to be cautious when administering drugs to the elderly?

A

Body systems are failing

  • Liver and Kidney function impaired
  • Heart failure –> reduced kidney and liver blood low
33
Q

How are drugs excreted via the kidneys?

A

Fat soluble drugs are changed to water soluble for movement into the urine.

34
Q

What are other modes of drug excretion?

A
  • Respiration
  • Breast Milk
  • GI tract
  • Sweat
  • Hair and Nails (heavy metals)
35
Q

What is a drug half life?

A

The time required for drug concentration to fall by 50%

36
Q

What occurs in non-linear elimination?

A

When a drug does not follow half life principles it’s concentration can escape the target therapeutic concentration and oversaturate liver enzymes

37
Q

Name some advantages of oral drug admin (3)

A

Cheap
Easy
Non invasive

38
Q

Name some disadvantages of oral drug admin (4)

A

Can’t administrate to unresponsive patients
Those who are nil by mouth
Difficulty/phobia swallowing pills
Drug broken down in stomach

39
Q

Name some advantages of IV admin (2)

A

Rapid effect

Can be used in those who are unresponsive

40
Q

Name some disadvantages of IV drug admin (3)

A

Invasive (infection and bleeds)
Access can be hard (elderly and children)
Needle phobias

41
Q

Name some advantages of IM admin (2)

A

Fast admin

Sustained drug effect

42
Q

Name some disadvantages of IM admin (2)

A

Less effective in shock (peripheral vasoconstriction)

Slow action initially

43
Q

Name an advantage of ‘subcut’ admin (1)

A

Long lasting effect

44
Q

Name a disadvantage of ‘subcut’ admin (1)

A

Slow absorption (fat is not very vascular)

45
Q

Name some advantages of topical admin (2)

A

Targets a specific area

Minimal systemic effect

46
Q

What are some of the factors that would determine what route a clinican may choose to administer a drug?

A 
PT compliance 
Speed of effect 
Effector 
Cost 
Desired effect 
Drug of choice
47
Q

What is pharmacokinetics?

A

The movement of drugs through the body

48
Q

What does ADME represent?

A

Absorption
Distribution
Metabolism
Excretion

49
Q

Why is the small intestine so effective at absorbing drugs?

A

It has a very large surface area (Villi made up of ciliated columnar epithelium)

50
Q

What two main impacts does liver failure have on the pharmacokinetics of a drug?

A
  1. Reduced drug metabolism and clearance

2. Reduced production of plasma proteins

51
Q

What is the definition of an agonist?

A

A drug or endogenous mediator that binds to a receptor and activates a cellular response

52
Q

What is the definition of an antagonist?

A

A drug that reduces or inhibits the action of an agonist

Clinical Life Sciences 2 (7 decks)

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