Stimulants and sedatives

Question 1

Dopamine: where found, acts on what types of receptors

Answer 1

•Found in:

oBrain & Brainstem

• Substantia nigra (reward, addiction, movement)
• Hypothalamus (inhibits prolactin release)
• Receptors

oIonotropic: none

oMetabotropic:

Question 2

Where mesolimbic and mesocortical pathways for dopamine start

Answer 2

VTA (ventral tegmental area)

Question 3

Dopamine can act on three pathways in the brain: mesolimbocortical and two others. List them and say what they are doing

Answer 3

Mesolimbical/mesocortical

Tuberoinfudibular pathway

Nigrostriatal pathway

Question 4

Coca: scientific name, part used,

Answer 4

Erythroxylum coca

Leaves

Question 5

Cocaine: what are the effects (the mechanism of action), risks:

Answer 5

• Addictive due to effects on dopamine reward pathway. High risk of dependence.
• Risk of stroke, heart attack, lung problems, blood infections, sudden cardiac death.
• Blocks reuptake of monoamine neurotransmitters – dopamine, norepinephrine, and serotonin.
• Causes profound mental stimulation: increased talkativeness, flight of ideas, euphoria, and inflated self-esteem. Fatigue is offset and there’s reduced need for sleep.

Question 6

Norepinephrine: where it is found, and what receptors

Answer 6

No ionotropic

Alpha and beta metabotropic

Question 7

Ephedra: scientific name, part used,

Answer 7

Ephedra sinica

Dried stems, roots

Question 8

Ephedra how it is used, where, side effects, allowed in canada/us?

Answer 8

TCM (traditional chinese medicine)

US banned, Health Canada does not have an act to regulate dietary supplements, and issued only a partial ban on the sale of ephedrine-containing products

Question 9

Ephedrine: mechanism of action

Answer 9

Question 10

Where purines are found in, receptors

Answer 10

Question 11

What is the oldest and most abundant receptors in all living organism, function?

Answer 11

• Purinergic receptors are the oldest and most abundant in all living organisms.
• The ionotropic P2X receptor binds ATP and evolved over a billion years ago.
• In CNS, ATP and adenosine play an important role in sleep.

Question 12

Three aspects that regulate sleep

Answer 12

Question 13

What makes you wake up naturally

Answer 13

Cortisol

Question 14

What parts of the night is dedicated to physical and psychological

Answer 14

Until 2 am- physical

after psyhological

Question 15

How adenosine and sleep pressure is related

Answer 15

• Extracellular adenosine levels in basal forebrain are lower during sleep and higher during sleep deprivation.
• Adenosine is a sleep-promoting substance à decreases the activity of cholinergic neurons.
• An increase in adenosine reflects an increased breakdown of cellular ATP.
• Adenosine regulation of sleep is mediated by A₁ and A₂ receptors.

Question 16

Caffeine: how it wakes us up and makes us alert, implications

Answer 16

•Caffeine is a CNS stimulant.•Acts as an antagonist for ALL adenosine receptors.•Antagonistic effects on the A_2A receptor is responsible for alertness.

Question 17

Coffee: scientific name, part used,

Answer 17

Coffee arabica

seed

Question 18

Tea: scientific names, part used,

Answer 18

Camella sinensis

Leaves

Question 19

Cocoa: scientific name, part used,

Answer 19

Theobroma cacao

Question 20

Yerba mate: scientific names, part used

Answer 20

Ilex paraguariensis

Leaves &Stems

Question 21

Is yerba mate is healthier than coffee

Answer 21

Advocates view it as healthful, noting that it contains vitamins, antioxidants, and anti-carcinogens. Heavy use, however, has been correlated with increased incidence of esophageal cancer, which is generally thought to result from the traditional method of consumption: sipping the liquid piping hot through a metal straw out of a heat-retaining gourd.

Question 22

Guarana: scientific name, part used,

Answer 22

Paullinia cupana

Seeds

Question 23

Summary table for 5 plants, highest to lowest caffeine content

Answer 23

Cocoa

Yerba Mate

Coffee

Tea

Guarana

Question 24

Caffeine intoxication: signs

Answer 24

• Overdose of caffeine occurs >400 mg.
• Symptoms are comparable to other stimulants: restlessness, fidgeting, anxiety, excitement, insomnia, flushing, increased urination, GI disturbance, muscle twitching, irritability, irregular or rapid heart beat, rambling flow of thought and speech.

Question 25

What is the target action of plants that act as sedatives, what each receptor is responsible to do

Answer 25

* Plants that induce CNS depression must either facilitate neuron inhibition or inhibit the neuronal excitation. * 1) GABA Receptor Agonists oCan also enhance GABA activity by blocking its reuptake or increasing its release. * 2) Glutamate Receptor Antagonists * 3) Blocking of voltage-gated ion channels.

Question 26

GABA receptors have allosteric binding sites for\_\_\_

Answer 26

obenzodiazepines, barbiturates, certain steroids, and ethanol.

Question 27

Why some sedatives impair memory

Answer 27

Glutamate receptor (NMDA) is involved in memory, sedatives block glutamate receptors

Question 28

Excitatory amino acids receptors are

Answer 28

AMPA, kainate receptors, and metabotropic glutamate receptors (mGluR).

Question 29

Anti seizure drugs predominantly act on

Answer 29

Blocking of voltage-gated ion channels.

Question 30

Valerian: scientific name, part used

Answer 30

* Valeriana officinalis* * Root& rhizomes*

Question 31

Valerian bioactivity; main classes; likely mechanism of action

Answer 31

* Valerian’s bioactivity may be due to additive / synergistic effects from several compounds. * Main components fall in 3 main phytochemical categories: oMonoterpenes• oSesquiterpenes oAlkaloids Two likely mechanism of action. 1.Facilitates GABA release and reversal of uptake.2.Inhibition of GABA breakdown.

Question 32

What is apigenin

Answer 32

A yellow colored flavonoid that is found in chamomile, but also in celery and other plants Apigenin→ sedative

Question 33

Chamomile: latin name, part used,

Answer 33

Matricaria recutita Dried flowers

Question 34

Apigenin: potential mechanism

Answer 34

•Apigenin has several potential mechanisms of action oAs a monoamine transport activator. oAs a ligand for benzodiazepine receptors •Sedative and anxiolytic effects likely mediated by the ability of apigenin to bind to benzodiazepine receptors on GABA_A

Question 35

Kava: latin name, part used

Answer 35

Piper methysticum Rootstalk

Question 36

Kava potential mechanism of action

Answer 36

* Psychotropic effects seem to be a combination of kava’s phytochemicals. * 4 main mechanisms: 1. **GABA:** Facilitates GABA transmission 2. **Voltage-gated ion channels:** Inhibits Na⁺ channels and subsequent release of glutamate. 3. **Monoamine:** Kavalactones inhibit monoamine oxidase B and reduce inflammation. 4. **Eicosanoids:** Kavain inhibits cyclooxygenase (COX), suppressing synthesis of thromboxane A₂. In turn, lower thromboxane A₂ increases GABA function.

Question 37

Passiflora incarnata: what common name, compound, what does it do, action

Answer 37

Passionflower Chrysin Benzodiazepine partial agonist

Question 38

Humulus lupupus and nepeta cataria: what is common and the difference

Answer 38

Hops and catnip are both sedatives, unknown mechanism, but different active compounds Hops:2-methyl-3-butene-2-ol Catnip: *Cis-trans*-nepetalactone

Question 39

What is chorea

Answer 39

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

Question 40

What are tics

Answer 40

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

Question 41

What is athetosis

Answer 41

Question 42

What is diuretic

Answer 42

•causing increased passing of urine.

Question 43

What is going to have in Nigrostriatal pathway (movement) when dopamine low/high

Answer 43

Question 44

What is going to have in Mesocorticolimbic pathway (mood/reward) when dopamine low/high

Answer 44

Question 45

What is going to have in Tuberoinfundubular pathway (no prolactin) when dopamine low/high

Answer 45