Pharmacokinetics II Flashcards

1
Q

What are the major body compartments

A

extracellular fluid, intracellular fluid, transcellular fluids, fat

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2
Q

Which type of drugs are effective

A

free drugs

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3
Q

What type of drugs does fat have an important impact on

A

lipophilic drugs

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4
Q

What is drug distribution based on

A

permeability and lipid solubility

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5
Q

What is meningitis

A

bacterial infection of the CNS

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6
Q

What is domperidone

A

antagonist of dopaminergic agonist receptors in chemoreceptor trigger zone

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7
Q

What regulates drug access to the CNS

A

blood brain barrier

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8
Q

Describe a junction in the CNS

A

endothelial cells line blood vessels and form tight junctions

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9
Q

What are tight junctions impermeable to

A

water soluble molecules

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10
Q

What can cross the BBB easily

A

lipid soluble molecules - ethanol and caffeine

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11
Q

What can happen to tight junctions during inflammation

A

become leaky

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12
Q

What can meningitis be treated with

A

iv penicillin

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13
Q

What other factors can influence drug distribution and elimination

A

binding to plasma proteins, partition into specific tissues

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14
Q

What does albumin bind to

A

mainly acidic drugs

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15
Q

What are the two main biochemical reactions for drug metabolism

A

catabolic reactions, synthetic (anabolic) reactions

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16
Q

What do catabolic reactions produce

A

more reactive compounds

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17
Q

What do anabolic reactions involve

A

conjugation

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18
Q

What do anabolic reactions produce

A

inactive product

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19
Q

Where does drug metabolism occur

20
Q

What affect can metabolism have on drug action

A

alter or prolong pharmacological drug action

21
Q

What must drugs cross in order to be metabolised

A

plasma membrane

22
Q

What speeds up drug metabolism

A

microsomal enzymes - cytochrome p450 in the liver

23
Q

What are the stages of aspirin elimination

A

drug forms a derivative - then forms a conjugate

24
Q

How can a drug form a derivative

A

oxidation, hydroxylation, dealkylation, deamination, hydrolysis

25
How does aspirin form its derivative
OCOCH3 group on aspirin is hydroxylated
26
What is the derivative of aspirin
salicylic acid
27
What hydroxylates aspirin into salicylic acid
p450 enzymes
28
What is the conjugate of aspirin
glucoronide
29
Name three important p450 enzymes
CYP1, CYP2, CYP3
30
What are CYP1, CYP2 and CYP3 involved in
drug and steroid metabolism
31
True or false - different iso-forms of p450 react with different drugs
true
32
Name some NSAIDs
ibuprofen, diclofenac, naproxen
33
What is paracetamol turned into
NAPQ1
34
What is a disadvantage of NAPQ1
extremely toxic
35
What is the effect of p450 inducers
increase drug metabolism
36
How do inducers increase drug metabolism
increase transcription of drugs
37
Name drug elimination routes
urine, faeces, milk, sweat, expired air
38
What are the three pathways of drug excretion
renal excretion, GI excretion, lung excretion
39
How does renal excretion of drugs occur
glomerular filtration, active tubular secretion
40
What does the primary organic cation transporter excrete
weak bases
41
What does the time course of clearance of drug concentrations follow
mono-exponential decay
42
What is saturation kinetics
disproportionate increase in steady state plasma concentration
43
Where do lipid soluble drugs accumulate
fat
44
Where are lipid insoluble drugs mainly confined to
plasma and interstitial fluids
45
What does the binding of drugs to plasma proteins reduce
free concentration of drug