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BMS 242 Core Physiology and Pharmacology > Pharmacokinetics II > Flashcards

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

A

liver

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
Q

How does aspirin form its derivative

A

OCOCH3 group on aspirin is hydroxylated

26
Q

What is the derivative of aspirin

A

salicylic acid

27
Q

What hydroxylates aspirin into salicylic acid

A

p450 enzymes

28
Q

What is the conjugate of aspirin

A

glucoronide

29
Q

Name three important p450 enzymes

A

CYP1, CYP2, CYP3

30
Q

What are CYP1, CYP2 and CYP3 involved in

A

drug and steroid metabolism

31
Q

True or false - different iso-forms of p450 react with different drugs

A

true

32
Q

Name some NSAIDs

A

ibuprofen, diclofenac, naproxen

33
Q

What is paracetamol turned into

A

NAPQ1

34
Q

What is a disadvantage of NAPQ1

A

extremely toxic

35
Q

What is the effect of p450 inducers

A

increase drug metabolism

36
Q

How do inducers increase drug metabolism

A

increase transcription of drugs

37
Q

Name drug elimination routes

A

urine, faeces, milk, sweat, expired air

38
Q

What are the three pathways of drug excretion

A

renal excretion, GI excretion, lung excretion

39
Q

How does renal excretion of drugs occur

A

glomerular filtration, active tubular secretion

40
Q

What does the primary organic cation transporter excrete

A

weak bases

41
Q

What does the time course of clearance of drug concentrations follow

A

mono-exponential decay

42
Q

What is saturation kinetics

A

disproportionate increase in steady state plasma concentration

43
Q

Where do lipid soluble drugs accumulate

A

fat

44
Q

Where are lipid insoluble drugs mainly confined to

A

plasma and interstitial fluids

45
Q

What does the binding of drugs to plasma proteins reduce

A

free concentration of drug

BMS 242 Core Physiology and Pharmacology (13 decks)

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