All Drug's Pharmacokinetics Flashcards

(72 cards)

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
Alcohol (ethanol): elimination
- liver (90%), and urine, sweat and breath
25
Alcohol (ethanol): potential for abuse and addiction
high potential for abuse based on its action in the glutamtergic, GABAergic, dopaminergic, and serotinergic systems - withdrawal: tremors, irritability, nausea, anxiety, depression
26
Cocaine: about
- alkaloid - from coca plant
27
Cocaine: membranes
- passive diffusion accross membranes and BBB
28
Cocaine: human health
chronic use: cardiovascular issues due to vasoconstriction
29
Cocaine: absorption
- RoA = ingestion, inhalation, IV, intranasal - primarily absorbed through mucous membranes
30
Cocaine: half life
t1/2 = approx 15 to 90 mins
31
Cocaine: metabolism
- minimal liver metabolism (CYP450)
32
Cocaine: metabolites
- norcocaine - benzoylecgonine
33
Cocaine: elimination
primarily eliminated through the kidneys and excreted through urine
34
Cocaine: potential for abuse and addiction
- potential for both physical and psychological dependence - short half life (need for frequent dosing) - withdrawal: tremors, irritability, nausea, anxiety, depression
35
Amphetamines and methamphetamines: membranes
- passive diffusion accross membranes and BBB
36
Amphetamines and methamphetamines: absorption
- RoA = ingestion, intranasal, inhalation, intravenous, intramuscular
37
Amphetamines and methamphetamines: half life
methamphetamines: t1/2 = approx 10 to 12 hours amphetamines: t1/2 = approx 4 to 6 hours
38
Amphetamines and methamphetamines: metabolism
metabolised by the liver by the CYP450 enzyme system
39
Amphetamines and methamphetamines: metabolites
amphetamine
40
Amphetamines and methamphetamines: elimination
primarily eliminated through the kidneys and excreted through urine
41
Amphetamines and methamphetamines: potential for abuse and addiction
- potential for both physical and psychological dependence - withdrawal: tremors, irritability, nausea, anxiety, depression
42
LSD: about
- ergot fungus -1960s
43
LSD: membranes
- passive diffusion accross membranes and BBB
44
LSD: absorption
- RoA = ingestion, sublingual, transdermal - completely absorbed in the GI tract (oral)
45
LSD: half life
t1/2 = approx 2.5 hours
46
LSD: metabolism
- in the liver by CYP2D6, CYP2E1, CYP3A4
47
LSD: elimination
primarily eliminated through the kidneys and excreted through urine
48
LSD: potential for abuse and addiction
- low potential for abuse and physical dependencevery low tolerance can occur
49
Ketamine: about
- dissociative anaesthetic - originally used for veterinary purposes
50
Ketamine: membranes
- passive diffusion accross membranes and BBB
51
Ketamine: absorption
- RoA = ingestion, intranasal, intravenous, intramuscular
52
Ketamine: half life
t1/2 = approx 2 to 3 hours
53
Ketamine: metabolism
metabolised in the liver by CYP450 enzyme system
54
Ketamine: metabolites
norketamine (active drug)
55
Ketamine: elimination
primarily eliminated through the kidneys and excreted through urine
56
Ketamine: potential for abuse and addiction
- potential for both physical and psychological dependence - withdrawal: tremors, irritability, nausea, anxiety, depression
57
Heroin: about
- opioid derived from morphine
58
Heroin: membranes
- passive diffusion accross membranes and BBB
59
Heroin: absorption
- RoA = intravenous, intramuscular, inhalation, intranasal
60
Heroin: half life
t1/2 = approx 2 to 6 mins
61
Heroin: metabolism
metabolised in the liver through hydrolysis using acetylcholinesterase enzymes
62
Heroin: metabolites
morphine
63
Heroin: elimination
primarily eliminated through the kidneys and excreted through urine
64
Heroin: potential for abuse and addiction
- potential for both physical and psychological dependence - short half life (need for frequent dosing) - withdrawal: tremors, irritability, nausea, anxiety, depression
65
Marijuana: about
from the cannabis plant
66
Marijuana: membranes
- simple diffusion accross membranes and BBB
67
Marijuana: absorption
- RoA = inhalation, ingestion, transdermal, sublingual
68
Marijuana: half life
t1/2 = approx 18 to 20 hours
69
Marijuana: metabolism
metabolised in the liver mainly by CYP450 enzymes
70
Marijuana: elimination
primarily eliminated through the liver/bile and excreted through faeces but also eliminated through the kidneys and excreted through urine
71
Marijuana: potential for abuse and addiction
low potential for physical dependence, high potential for psychological dependence for frequent use