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
What are the two main organs of metabolism?
Liver and Kidneys
26
Which drug types are converted to an active form by the liver due to their long half life?
Opiods and Benzodiazepines
27
Why would you want drugs to be metabolised from an inactive to an active form?
Drugs with specific target cells To bypass the GI tract (cancer drugs, viral therapies and anti inflammatories)
28
What is first pass metabolism?
A phenomenon whereby the concentration of a drug greatly reduces before reaching the systemic circulation
29
What 3 main methods of drug admin are subject to first pass metabolism?
1. Buccal/Oral 2. Rectal 3. GI absorption (via hepatic portal vein)
30
Why do children generally metabolise drugs faster?
They have a higher metabolic rate
31
Why do babies require smaller doses of drugs?
Liver functions and other body systems immature
32
Why do you need to be cautious when administering drugs to the elderly?
Body systems are failing - Liver and Kidney function impaired - Heart failure --> reduced kidney and liver blood low
33
How are drugs excreted via the kidneys?
Fat soluble drugs are changed to water soluble for movement into the urine.
34
What are other modes of drug excretion?
- Respiration - Breast Milk - GI tract - Sweat - Hair and Nails (heavy metals)
35
What is a drug half life?
The time required for drug concentration to fall by 50%
36
What occurs in non-linear elimination?
When a drug does not follow half life principles it's concentration can escape the target therapeutic concentration and oversaturate liver enzymes
37
Name some advantages of oral drug admin (3)
Cheap Easy Non invasive
38
Name some disadvantages of oral drug admin (4)
Can't administrate to unresponsive patients Those who are nil by mouth Difficulty/phobia swallowing pills Drug broken down in stomach
39
Name some advantages of IV admin (2)
Rapid effect | Can be used in those who are unresponsive
40
Name some disadvantages of IV drug admin (3)
Invasive (infection and bleeds) Access can be hard (elderly and children) Needle phobias
41
Name some advantages of IM admin (2)
Fast admin | Sustained drug effect
42
Name some disadvantages of IM admin (2)
Less effective in shock (peripheral vasoconstriction) | Slow action initially
43
Name an advantage of 'subcut' admin (1)
Long lasting effect
44
Name a disadvantage of 'subcut' admin (1)
Slow absorption (fat is not very vascular)
45
Name some advantages of topical admin (2)
Targets a specific area | Minimal systemic effect
46
What are some of the factors that would determine what route a clinican may choose to administer a drug?
``` PT compliance Speed of effect Effector Cost Desired effect Drug of choice ```
47
What is pharmacokinetics?
The movement of drugs through the body
48
What does ADME represent?
Absorption Distribution Metabolism Excretion
49
Why is the small intestine so effective at absorbing drugs?
It has a very large surface area (Villi made up of ciliated columnar epithelium)
50
What two main impacts does liver failure have on the pharmacokinetics of a drug?
1. Reduced drug metabolism and clearance | 2. Reduced production of plasma proteins
51
What is the definition of an agonist?
A drug or endogenous mediator that binds to a receptor and activates a cellular response
52
What is the definition of an antagonist?
A drug that reduces or inhibits the action of an agonist