Lecture 4: Stimulants and Sedatives Flashcards

1
Q

Dopamine - Location

A

Brain and brainstem (substantia nigra, hypothalamus)

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2
Q

Dopamine - receptors

A

1) ionotropic - none
2) metabotropic:
- D1: Excitatory (K and Ca transport)
- D2: Inhibitory (K and Ca transport)

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3
Q

name the dopamine pathways

A

1) reward pathway - mesolimbic pathway and mesocortical
2) nigrostriatal pathway
3) tuberoinfundibular pathway

Refer to the slide

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4
Q

coca - scientific name

A

Erythroxylum coca

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5
Q

coca - part used

A

leaves

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6
Q

coca - bioactive compound

A

cocaine

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7
Q
  1. why is it so addictive

2. risks of cocaine use

A
  1. due to effects on dopamine reward pathway

2. risk of stroke, heart attack, lung problems, blood infections, sudden cardiac death

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8
Q

Effects of cocaine with mechanism

A

loss of contact with reality and profound mental stimulation - more talkative, flight of ideas, reduced need for sleep, and inflated self esteem.

mechanism:
- it interfere with reuptake of dopamine in the mesolimbic dopamine pathway

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9
Q

chronic use of cocaine leads to:

A

decreased availability of D2 receptors

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10
Q

Norepinephrine (adrenaline) - branch of NS

A

sympathetic

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11
Q

norepinephrine receptors

A

1) ionotropic: none
2) metabotropic:
- alpha 1 and beta 1 : excitatory
- alpha 2 and beta 2: inhibitory

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12
Q

ephedra -scientific name

A

Ephedra sinica

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13
Q

ephedra - parts used

A

dried stems, root

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14
Q

ephedra - bioactive compound

A

ephedrine, pseudoephidrine

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15
Q

ephedrine - mechanism

A
  • it is a CNS stimulator
    1. it enters pre - synaptic neutron via the norepinephrine transporter
    2. enters the synaptic vesicle via the vesicular monoamine transporter
    3. norepinephrine is released into cytoplasm and released into the synaptic cleft by norepinephrine transporter
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16
Q

Purines - receptors

A
  1. ionotropic : P2X receptors - found in neurons and glial cells in the PNS and CNS (ATP)
  2. metabotropic:
    • P1: Adenosine - found in brain, heart, kidneys, and adipose tissue
      - P2Y: ATP, ADP, UTP, UDP - found in brain, heart, kidneys, and adipose tissue
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17
Q

in the CNS , ATP and adenosine play an important role in ——–

A

sleep

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18
Q

sleep and adenosine levels

A

extracellular levels of adenosine in basal forebrain is lower during sleep and higher during sleep deprivation

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19
Q

adenosine decreases the activity of ————

A

cholinergic neurons

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20
Q

adenosine regulation of sleep is mediated by —- and —- receptors

A

A1,A2

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21
Q

Adenosine levels and ATP

A

increase in adenosine levels reflects an increased breakdown of ATP

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22
Q

caffeine acts as an —— for all adenosine receptors

A

antagonist

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23
Q

caffeine primarily binds to the —– receptors

A

A2a

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24
Q

long term exposure to caffeine

A

it blocks the effects of adenosine, norepinephrine may be reduced and the brain relies on caffeine to remain alert

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25
Q

coffee - scientific name

A

coffea arabica

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26
Q

coffee - parts used

A

seeds

27
Q

coffee - bioactive compound

A

caffeine

28
Q

tea - scientific name

A

camellia sinensis

29
Q

tea - parts used

A

leaves

30
Q

tea - bioactive compound

A

Epigallocatechin gallate (EGCG)

31
Q

Cocoa - scientific name

A

Theobroma cacao

32
Q

Cocoa - parts used

A

seeds

33
Q

cocoa - bioactive compound

A

Theobromine

34
Q

Yerba Mate - scientific name

A

Ilex paraguariensis

35
Q

Yerba Mate - parts used

A

leaves and stem

36
Q

Yerba Mate - bioactive compound

A

Theobromine

37
Q

heavy use of Yerba Maté

A

increased incidence of esophageal cancer,

38
Q

Guarana - scientific name

A

Paullinia cupana

39
Q

Guarana - parts used

A

seeds

40
Q

Guarana - bioactive compound

A

Caffeine

41
Q

Rank the following from the most caffeine content to the least:
Tea, cocoa, coffee, Yerba Mate, Guarana

A
  1. Guarana
  2. Tea
  3. Coffee
  4. Yerba Mate
  5. Cocoa
42
Q

overdoes of caffeine occurs at:

A

> 400 mg

43
Q

symptoms of caffeine intoxication

A

restlessness, fidgeting, anxiety, insomnia, excitement, flushing, increased urination, GI disturbance, muscle twitching, irritability, irregular or rapid heart bear, rambling flow of through and speech
* comparable to other stimulants

44
Q

ways through which herbal sedatives work

A
  • they must either cause neuron inhibition or inhibit the neuronal pathway
    1. GABA receptor agonist: GABAa receptors have allosteric binding sites for bento, barb, certain steroids and ethanol; can also enhance GABA activity by blocking its reuptake or increasing its release
    2. glutamate receptor antagonist: inhibition of NMDA may explain why does sedatives impair memory. other excitatory receptor are AMPA, kainite and metabotropic glutamate receptors (mGluR)
    3. Blocking of voltage gated ion channels: *predominantly anti-seizure drugs
45
Q

Valerian - scientific name

A

Valeriana officinalis

46
Q

Valerian - parts used

A

Roots and rhizomes

47
Q

Valerian - bioactive compound

A

valerenic acid

48
Q

main components of valerian that have a synergistic activity

A
  1. monoterpenes
  2. Sesquiterpenes
  3. Alkaloids

Refer to the slides for examples of each

49
Q

likely mechanism of action(s) of valerian

A
  1. facilities GABA release and reversal of uptake

2. inhibition of GABA breakdown

50
Q

promising evidence that Valerian can improve —–

It also may be useful in treating —–

A

sleep, anxiety

51
Q

Chamomile - scientific name

A

Matricaria recutita

52
Q

Chamomile - parts used

A

dried flowers

53
Q

Chamomile - bioactive compound

A

Apigenin

54
Q

apigenin - mechanism of action(s)

A
  1. as a monoamine transport activator

2. as a ligand for benzodiazepine receptors on GABAa - thus, enhancing the effect of GABA

55
Q

Kava - scientific name

A

Piper methysticum

56
Q

Kava - parts used

A

Rootstalk

57
Q

Kava - bioactive compound

A

Kavain

58
Q

mechanism(s) of Kava

A
  1. GABA: facilities GABA transmission
  2. Voltage gated ion channels: inhibits sodium channels and subsequent release of glutamate
  3. Monoamine: Kavalactones inhibit monoamine oxidase B and reduce inflammation
  4. Eicosanoids: Kavain inhibits cyclooxygenase (COOX), suppressing synthesis of thromboxane A2. In turn, lower thromboxane A2 increases GABA function.
59
Q

Kava’s psychotropic effect is due to:

A

combination of its phytochemicals

60
Q

name 6 herbal sedatives

A
  1. Chamomile
  2. Kava
  3. Valerian
  4. Passion flower
  5. Catnip
  6. Hops
61
Q

Chorea

A

a neurological disorder characterized by jerky involuntary movements affecting especially the shoulders, hips, and face

62
Q

Tics

A

a habitual spasmodic contraction of the muscles, often in the face

63
Q

Athetosis

A

a condition in which abnormal muscle contractions cause involuntary writhing movements. It affects some people with cerebral palsy, impairing speech and use of the hands

64
Q

diuretic

A

causing increased passing of urine