All Drug's Pharmacokinetics Flashcards

1
Q

Caffeine: about

A

religious drinks
- tea (china)
- coffee (ethiopia)

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2
Q

Caffeine: membranes

A
  • simple diffusion to cross membranes and BBB
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3
Q

Caffeine: toxicity

A
  • LD50 = 150 to 200 mg/kg BM
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4
Q

Caffeine: absorption

A
  • RoA = ingestion
  • absorbed by the stomach and small intestines within 45 mins of consumption
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5
Q

Caffeine: half life

A

t1/2 = approx 3 to 4 hours

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6
Q

Caffeine: metabolism

A

metabolised in liver by CYP450 enzyme system

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7
Q

Caffeine: metabolites

A
  • paraxanthine
  • theobromine
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8
Q

Caffeine: elimination

A

primarily eliminated through the kidneys and excreted through urine

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9
Q

Caffeine: potential for abuse and addiction

A
  • very dependence-producing
  • withdrawal effects caused by adenosine receptor density, and therefore adenosine sensitivity (depression, fatigue, irritability, headaches)
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10
Q

Nicotine: about

A
  • alkaloid, organic compound from tobacco plant
  • lipophilic free base
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10
Q

Nicotine: membranes

A
  • simple diffusion to cross membranes and BBB
  • environment pH affects its absorption (small intestine, not stomach)
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11
Q

Nicotine: toxicity

A
  • cancer (90% of all lung cancers)
  • COPD, asthma, emphysema
  • LD50 = 30 to 60mg
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12
Q

Nicotine: absorption

A
  • RoA = inhalation, ingestion, buccal, transdermal
  • inhalation = most addictive
  • transdermal = least addictive because of low dose and speed of delivery to the brain
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13
Q

Nicotine: half life

A

t1/2 = approx 2 hours

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14
Q

Nicotine: metabolism

A

metabolised in the lungs, kidneys, and liver by CYP450 and aldehyde oxidase enzyme systems

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15
Q

Nicotine: metabolites

A

cotinine (t1/2 = approx 16 hours)

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16
Q

Nicotine: elimination

A

primarily eliminated through the kidneys and excreted through urine

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17
Q

Nicotine: potential for abuse and addiction

A
  • very dependence-producing (used as stress relief, weight control, social factor)
  • withdrawal: irritability, anxiety, excessive hunger (blood sugar drop)
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18
Q

Alcohol (ethanol): about

A

fermentation of sugars, anaerobic respiration by yeast - changes the sugars into ethanol and carbon dioxide

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19
Q

Alcohol (ethanol): membranes

A
  • simple diffusion to cross membranes and BBB
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20
Q

Alcohol (ethanol): absorption

A
  • approx 80% absorption from upper intestine
  • total absorption is unaffected by food in stomach
  • avg vol of distribution is 0.54 l/kg
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21
Q

Alcohol (ethanol): half life

A

t1/2 = approx 3 to 5 hours but can vary

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22
Q

Alcohol (ethanol): metabolism

A

95% of alcohol is metabolized by alcohol dehydrogenase enzyme in the liver

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23
Q

Alcohol (ethanol): metabolites

A
  • acetaldehyde first, broken down to acetate
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24
Q

Alcohol (ethanol): elimination

A
  • liver (90%), and urine, sweat and breath
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25
Q

Alcohol (ethanol): potential for abuse and addiction

A

high potential for abuse based on its action in the glutamtergic, GABAergic, dopaminergic, and serotinergic systems
- withdrawal: tremors, irritability, nausea, anxiety, depression

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26
Q

Cocaine: about

A
  • alkaloid
  • from coca plant
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27
Q

Cocaine: membranes

A
  • passive diffusion accross membranes and BBB
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28
Q

Cocaine: human health

A

chronic use: cardiovascular issues due to vasoconstriction

29
Q

Cocaine: absorption

A
  • RoA = ingestion, inhalation, IV, intranasal
  • primarily absorbed through mucous membranes
30
Q

Cocaine: half life

A

t1/2 = approx 15 to 90 mins

31
Q

Cocaine: metabolism

A
  • minimal liver metabolism (CYP450)
32
Q

Cocaine: metabolites

A
  • norcocaine
  • benzoylecgonine
33
Q

Cocaine: elimination

A

primarily eliminated through the kidneys and excreted through urine

34
Q

Cocaine: potential for abuse and addiction

A
  • potential for both physical and psychological dependence
  • short half life (need for frequent dosing)
  • withdrawal: tremors, irritability, nausea, anxiety, depression
35
Q

Amphetamines and methamphetamines: membranes

A
  • passive diffusion accross membranes and BBB
36
Q

Amphetamines and methamphetamines: absorption

A
  • RoA = ingestion, intranasal, inhalation, intravenous, intramuscular
37
Q

Amphetamines and methamphetamines: half life

A

methamphetamines: t1/2 = approx 10 to 12 hours
amphetamines: t1/2 = approx 4 to 6 hours

38
Q

Amphetamines and methamphetamines: metabolism

A

metabolised by the liver by the CYP450 enzyme system

39
Q

Amphetamines and methamphetamines: metabolites

A

amphetamine

40
Q

Amphetamines and methamphetamines: elimination

A

primarily eliminated through the kidneys and excreted through urine

41
Q

Amphetamines and methamphetamines: potential for abuse and addiction

A
  • potential for both physical and psychological dependence
  • withdrawal: tremors, irritability, nausea, anxiety, depression
42
Q

LSD: about

A
  • ergot fungus
    -1960s
43
Q

LSD: membranes

A
  • passive diffusion accross membranes and BBB
44
Q

LSD: absorption

A
  • RoA = ingestion, sublingual, transdermal
  • completely absorbed in the GI tract (oral)
45
Q

LSD: half life

A

t1/2 = approx 2.5 hours

46
Q

LSD: metabolism

A
  • in the liver by CYP2D6, CYP2E1, CYP3A4
47
Q

LSD: elimination

A

primarily eliminated through the kidneys and excreted through urine

48
Q

LSD: potential for abuse and addiction

A
  • low potential for abuse and physical dependencevery low tolerance can occur
49
Q

Ketamine: about

A
  • dissociative anaesthetic
  • originally used for veterinary purposes
50
Q

Ketamine: membranes

A
  • passive diffusion accross membranes and BBB
51
Q

Ketamine: absorption

A
  • RoA = ingestion, intranasal, intravenous, intramuscular
52
Q

Ketamine: half life

A

t1/2 = approx 2 to 3 hours

53
Q

Ketamine: metabolism

A

metabolised in the liver by CYP450 enzyme system

54
Q

Ketamine: metabolites

A

norketamine (active drug)

55
Q

Ketamine: elimination

A

primarily eliminated through the kidneys and excreted through urine

56
Q

Ketamine: potential for abuse and addiction

A
  • potential for both physical and psychological dependence
  • withdrawal: tremors, irritability, nausea, anxiety, depression
57
Q

Heroin: about

A
  • opioid derived from morphine
58
Q

Heroin: membranes

A
  • passive diffusion accross membranes and BBB
59
Q

Heroin: absorption

A
  • RoA = intravenous, intramuscular, inhalation, intranasal
60
Q

Heroin: half life

A

t1/2 = approx 2 to 6 mins

61
Q

Heroin: metabolism

A

metabolised in the liver through hydrolysis using acetylcholinesterase enzymes

62
Q

Heroin: metabolites

A

morphine

63
Q

Heroin: elimination

A

primarily eliminated through the kidneys and excreted through urine

64
Q

Heroin: potential for abuse and addiction

A
  • potential for both physical and psychological dependence
  • short half life (need for frequent dosing)
  • withdrawal: tremors, irritability, nausea, anxiety, depression
65
Q

Marijuana: about

A

from the cannabis plant

66
Q

Marijuana: membranes

A
  • simple diffusion accross membranes and BBB
67
Q

Marijuana: absorption

A
  • RoA = inhalation, ingestion, transdermal, sublingual
68
Q

Marijuana: half life

A

t1/2 = approx 18 to 20 hours

69
Q

Marijuana: metabolism

A

metabolised in the liver mainly by CYP450 enzymes

70
Q

Marijuana: elimination

A

primarily eliminated through the liver/bile and excreted through faeces but also eliminated through the kidneys and excreted through urine

71
Q

Marijuana: potential for abuse and addiction

A

low potential for physical dependence, high potential for psychological dependence for frequent use