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Herbs > 8-9: Stimulants and sedatives > Flashcards

8-9: Stimulants and sedatives Flashcards

1
Q

DOPAMINE
- what kind of neurotransmitter + subtype?
- found where (2) + 2 sub
- used to treat (2)
- receptors? (2)

A
  • monoamine –> catecholamine
  • brain and brainstem –> substantia nigra (reward, addiction, movement) + hypothalamus (inhibits prolactin release)
  • Schizophrenia, psychosis + Parkinson’s disease
  • NO ionotropic –> all metabotropic: excitatory (D1) or inhibitory (D2) –> both use K+ and Ca2+
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2
Q

what are the 3 main dopamine pathways?

  • all start from where ish?
A
  • nigrostriatal pathway
  • tuberinfundibular pathway
  • mesolimbic and mesocortical pathways
  • brainstem!
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3
Q

in each of the 3 pathways
- nigrostriatal pathway
- tuberinfundibular pathway
- mesolimbic and mesocortical pathways

what happens when you have LOW vs HIGH dopamine?

A

NIGROSTRIATAL PATHWAY
- low: Parkinson’s + Extrapyramidal symptoms (EPS)
- high: Chorea, tics, athetosis –> irregular movement

TUBERINFUNDIBULAR PATHWAY (prolactin)
- low: hyperprolactinemia –> glactorrhea + suppressed GnRH (amenorrhea + impotence, gynecomastia)
- high: inhibits prolactin

MESOLIMBIC AND MESOCORTICAL PATHWAYS
- low: anhedonia (no pleasure) + therapeutic effects of antipsychotics
- high: psychosis, euphoria, hallucinations (schizophrenia), conditioning

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4
Q

Coca (monograph):
- SCIENTIFIC NAME:
- PART USED:
- MODE OF ADMINISTRATION:
- BIOACTIVE COMPOUND:
- COMPOUND CLASS:
- USES:

A
  • SCIENTIFIC NAME: erythroxylum coca
  • PART USED: leaves
  • MODE OF ADMINISTRATION: chewed, insufflation, inhalation
  • BIOACTIVE COMPOUND: cocaine
  • COMPOUND CLASS: alkaloid
  • USES: stimulant + increased endurance
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5
Q

coca leaves
- used for over 1000s years by who?
- how do use it?
- effects of ________ felt after how long? and doesn’t produce _________ –> may be more powerful than _______ in producing good mood
- important contributor to (2) to diet

A
  • South American Indigenous people
  • tiny amount of lime (powdered calcium carbonate) is added + leaf is chewed for 30min (don’t get high if leaf is chewed!)
  • stimulant after a few minutes. no jitterness –> coffee
  • vitamins and minerals
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6
Q
  • how to make cocaine hydrochloride? (3 ish)
  • causes what? (2)
  • effects begin after how long + last how long?
  • addictive? why or why not?
  • risk of (5)
A
  • made by mixing leaves with organic solvent and mashing them –> when solvent evaporates, a coca paste remains –> paste is further refined into cocaine hydrochloride
  • causes loss of contact with reality and euphoria
  • effects being within seconds to minutes and lasts 5-90 minutes
  • addictive due to effects on dopamine reward pathway. high risk of dependence
  • risk of stroke, heart attack, lung problems, blood infections, sudden cardiac death
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7
Q
  • what is the mechanism of action of cocaine?
  • leads to increased available what?
  • chronic use leads to decreased what?
  • effects (6 ish)
A
  • blocks reuptake of monoamine neurotransmitters (dopamine, NE, serotonin)
  • leads to increased available synaptic transmitters
  • chronic use leads to decreased availability of D2 receptors (metabotropic inhibitory receptors of dopamine)
  • causes profound mental stimulation: increased talkativeness, flight of ideas, euphoria and inflated self esteem + fatigue is offset and there’s reduced need for sleep –> feel invicible
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8
Q

why/how is cocaine addictive?

A

because it interferes with reuptake of dopamine in mesolimbic dopamine pathway!
- cocaine blocks the dopamine transporter (reuptakes dopamine back into pre-synaptic neuron)

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9
Q

Norepinephrine
- what type of neurotransmitter + subtype?
- found where?
- used to treat (3)
- receptors?

A
  • monoamine + catecholamines
  • brain: locus ceruleus, projecting to cortex, arousal, attention + ANS: SNS neurons (effector organs, postganglion neurons)
  • used to treat AHDD, anxiety, cardiac failure
  • NO ionotropic
  • metabotropic: a1 and b1 are excitatory VS a2 and b2 are inhibitory
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10
Q

ephedra (monograph)
- SCIENTIFIC NAME:
- PART USED:
- MODE OF ADMINISTRATION:
- BIOACTIVE COMPOUND:
- COMPOUND CLASS:
- USES:

A
  • SCIENTIFIC NAME: ephedra sinica
  • PART USED: dried stems, root
  • MODE OF ADMINISTRATION: infusion
  • BIOACTIVE COMPOUND: ephedrine, pseudoephedrine
  • COMPOUND CLASS: alkaloid
  • USES: stimulant, thermogenic
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11
Q
  • what is the chinese name for ephedra?
  • used for what? (10)
  • ephedrine alkaloids cause (7)
  • side effects (4)
A
  • ma huang! used in TCM for over 5000 years
  • colds, flu, fever, chills, headaches, edema, asthma, nasal congestion, aching joints and bones, cough and weezing
    EPHRDRINE ALKALOIDS
  • CNS stimulation
  • bronchodilation
  • cardiac stimulation
  • tachycardia
  • diuretic
  • peripheral vasoconstrictor
  • elevated BP
    SIDE EFFECTS
  • trouble sleeping
  • anxiety
  • headache
  • hallucinations
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12
Q

EPHEDRINE
- is a CNS ________ similar to what?
- mechanism of action (3 steps)

A
  • CNS stimulant similar to amphetamines
    1. ephedrine (amphetamine) enters pre-synaptic neuron via Norepinephrine transporter (NET)
    2. enters synaptic vesicle via vesicular monoamine transporter (VMAT)
    3. Norepinephrine (and ephedrine (?)) is released into cytoplasm and released into the synaptic cleft by NET
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13
Q

PURINES:
- found where (6)
- used to treat what?
- receptors?

A
  • found in brain, heart, kidney, adipose tissue + neurons and glial cells
  • supraventricular tachycardia
  • ionotropic (P2X receptors, ATP) and metabotropic (P1 and P2Y receptors)
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14
Q
  • what is the oldest and most abundant receptor in all living organisms?
  • which receptor binds to what molecule?
  • in CNS, (2) play an important role in SLEEP
A
  • purinergic receptors!
  • ionotropic P2X receptors binds ATP and evolved a billion years ago –> very conserved
  • ATP and adenosine
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15
Q

adenosine and sleep pressure
- extracellular adenosine levels in basal forebrain are higher/lower during sleep and higher/lower during sleep deprivation
- adenosine promotes/inhibits sleep –> how?
- increase in adenosine causes what in terms of ATP?
- adenosine regulation of sleep is mediated by which receptors?

A
  • lower during sleep, higher during sleep deprivation
  • sleep promoting substance! decreases activity of cholinergic neurons (BOLD)
  • increase in adenosine reflects increased breakdown of cellular ATP
  • mediated by A1 and A2 receptors
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16
Q

CAFFEINE
- CNS _________
- acts as what?
- responsible for what?

A
  • CNS stimulant
  • acts as an antagonist for ALL adenosine receptors
  • antagonistic effects on the A2A receptor is responsible for alertness
17
Q

caffeine binding
- adenosine binds to adenosine receptor (AR) –> job is to make humans feel what?
- caffeine can also bind AR –> what happens then?
- NE acts as what?
- with caffeine’s effects, what happens to NE?

A
  • tired!
  • caffeine blocks binding of adenosine and stops the feeling of tiredness
  • NE binds to receptors. acts as stimulant
  • with caffeine blocking effects of adenosine, NE may be reduced and brain relies on caffein to remain alert
18
Q

coffee (monograph)
- SCIENTIFIC NAME:
- PART USED:
- MODE OF ADMINISTRATION:
- BIOACTIVE COMPOUND:
- COMPOUND CLASS:
- USES:

A
  • SCIENTIFIC NAME: coffea arabica
  • PART USED: seed
  • MODE OF ADMINISTRATION: indusion/percolation
  • BIOACTIVE COMPOUND: caffeine
  • COMPOUND CLASS: alkaloid
  • USES: stimulant
19
Q

tea (monograph)
- SCIENTIFIC NAME:
- PART USED:
- MODE OF ADMINISTRATION:
- BIOACTIVE COMPOUND:
- COMPOUND CLASS:
- USES:

A
  • SCIENTIFIC NAME: camellia sinensis
  • PART USED: leaves
  • MODE OF ADMINISTRATION: infusion
  • BIOACTIVE COMPOUND: epigallocatechin gallate (EGCC)
  • COMPOUND CLASS: catechin polyphenol (no N)
  • USES: antioxidant, anticancer, antimicrobial
20
Q

cocoa (monograph)
- SCIENTIFIC NAME:
- PART USED:
- MODE OF ADMINISTRATION:
- BIOACTIVE COMPOUND:
- COMPOUND CLASS:
- USES:

A
  • SCIENTIFIC NAME: Theobroma cacao
  • PART USED: seeds
  • MODE OF ADMINISTRATION: roasting (seeds)
  • BIOACTIVE COMPOUND: theobromine (can be addictive)
  • COMPOUND CLASS: alkaloid
  • USES: vasodilator, diuretic, heart stimulant
21
Q

yerba maté (monograph):
- SCIENTIFIC NAME:
- PART USED:
- MODE OF ADMINISTRATION:
- BIOACTIVE COMPOUND:
- COMPOUND CLASS:
- USES:

A
  • SCIENTIFIC NAME: Ilex paraguariensis
  • PART USED: leaves and stem
  • MODE OF ADMINISTRATION: infusion
  • BIOACTIVE COMPOUND: theobromine (and caffeine)
  • COMPOUND CLASS: alkaloid
  • USES: stimulant
22
Q

guanara (monograph):
- SCIENTIFIC NAME:
- PART USED:
- MODE OF ADMINISTRATION:
- BIOACTIVE COMPOUND:
- COMPOUND CLASS:
- USES:

A
  • SCIENTIFIC NAME: Paullinia cupana
  • PART USED: seeds
  • MODE OF ADMINISTRATION: roasted
  • BIOACTIVE COMPOUND: caffeine
  • COMPOUND CLASS: alkaloid
  • USES: stimulant
23
Q

what are 5 plants that contain caffeine?
- which has higher caffeine content?

A
  1. guarana (2.5-5% caffeine)
  2. tea (2.9-4.2%)
  3. coffee (1-3.2%)
  4. yerba maté (0.4-2.4%)
  5. cocoa (0.4-1.2%)
24
Q

CNS stimulants!
what is the common name, receptor type, bioactive compound and mechanism of these plants:
NICOTIANA TABACUM
EPHEDRA SINICA
ERYTHROXYLOM COCA
COFFEA ARABICA
CAMELLIA SINENSIS
THEOBROMA CACOA
ILEX PARAGUARIENSIS
PAULLINIA CUPANA

A

NICOTIANA TABACUM
- tobacco –> cholinergic
- cholinergic –> nACh agonist

EPHEDRA SINICA:
- ephedra –> monoaminergic
- ephedrine –> a, b adrenergic agonist (stimulates)

ERYTHROXYLOM COCA:
- coca –> monoaminergic
- cocaine –> blocks monoamine reuptake

COFFEA ARABICA
- coffee –> purinogenic
- caffeine –> adenosine antagonism

CAMELLIA SINENSIS:
- tea –> purinogenic
- caffeine –> adenosine antagonism

THEOBROMA CACOA
- cocoa –> purinogenic
- theobromine –> adenosine antagonism

ILEX PARAGUARIENSIS
- yerba maté –> purinogenic
- caffeine –> adenosine antagonism

PAULLINIA CUPANA
- guarana –> purinogenic
- caffeine –> adenosine antagonism

25
Q

herbal sedatives = what? must what?
- what are 3 mechanisms?

A

plants that induce CNS depression must either facilitate neuron inhibition or inhibit neuronal excitation
1. GABA receptor agonists
- GABAA receptors have allosteric binding sites for benzodiazepines, barbiturates, certain steroids and ethanol
- can also enhance GABA activity by blocking reuptake or increasing its release
2. Glutamate receptor antagonists
- NMDA receptors is involved in memory –> inhibit NMDA may explain why some CNS depressant impair memory
- other excitatory aa receptors include AMPA, kainate receptors and metabotropic glutamate receptors
3. blocking of voltage-gated ion channels
- predominantly anti-seizure drugs

*basically things that act like GABA OR that prevent glutamate

26
Q

valerian (monograph)
- SCIENTIFIC NAME:
- PART USED:
- MODE OF ADMINISTRATION:
- BIOACTIVE COMPOUND:
- COMPOUND CLASS:
- USES:

A
  • SCIENTIFIC NAME: Valeriana officinalis
  • PART USED: root and rhizomes
  • MODE OF ADMINISTRATION: decoction
  • BIOACTIVE COMPOUND: valerenic acid
  • COMPOUND CLASS: sesquiterpene
  • USES: sedative (traditional drug to make you sleep)
27
Q

VALERIAN
- activity may be due to what?
- main components fall into 3 main phytochemical categories –> all have ___
- 2 likely mechanism of action

A
  • may be due to addictive/synergistic effects from several compounds
  • monoterpenes, sesquiterpenes and alkaloids –> all have N!
    1. facilitates GABA release and reversal of uptake
    2. inhibition of GABA breakdown
    = true inhibitor! (bc doesnt act on glutamate or excitation)
28
Q

valerian
- traditionally used to treat what?
- may be useful for treating what?

A
  • stress related symptoms + as a sleeping aid (improving sleep!)
  • may be useful in treating anxiety or other mood disorders
29
Q

chamomile (monograph)
- SCIENTIFIC NAME:
- PART USED:
- MODE OF ADMINISTRATION:
- BIOACTIVE COMPOUND:
- COMPOUND CLASS:
- USES:

A
  • SCIENTIFIC NAME: Matricaria recutita
  • PART USED: dried flowers
  • MODE OF ADMINISTRATION: infusion
  • BIOACTIVE COMPOUND: apigenin
  • COMPOUND CLASS: flavonoid
  • USES: sedative
30
Q

bioactive compound of chamomile?
- mechanisms of action (2)
- 2 effects mediated by what?

A

apigenin!
1. monoamine transport activator (serotonin and dopamine)
2. as a ligand for benzodiazepine receptors
- sedative and anxiolytic effects likely mediated by ability of apigenin to bind to benzodiazepine receptors on GABA_A

31
Q

Kava (monograph)
- SCIENTIFIC NAME:
- PART USED:
- MODE OF ADMINISTRATION:
- BIOACTIVE COMPOUND:
- COMPOUND CLASS:
- USES:

A
  • SCIENTIFIC NAME: Ppier methysticum
  • PART USED: rootstalk
  • MODE OF ADMINISTRATION: infusion
  • BIOACTIVE COMPOUND: kavain
  • COMPOUND CLASS: kavalactone
  • USES: sedative + anxiolytic
32
Q

KAVA
- ________ effects seem to be a combination of Kava’s phytochemicals
- 4 main mechanisms

A
  • psychotropic effects
    1. GABA: facilitates GABA transmission (agonist!)
    2. voltage-gated ion channels: inhibits Na+ channels and subsequent release of glutamate
    3. monoamine: kavalactones inhibit MAO B and reduce inflammation
    4. eicosanoids: Kavain inhibits cycloocygenase (COX), supressing synthesis of thromboxane A2. in turn, lower thromboxane A2 incraeases GABA function
33
Q

herbal sedative summary slide
-name common name, compound and mechanisms (up to 4)
VALERIANA OFFICINALIS
MATRICARIA RECUTITA
PIPER METHYSTICUM
PASSIFLORA INCARNATA
HUMULUS LUPULUS
NEPETA CATARIA

A

VALERIANA OFFICINALIS
- Valerian, sesquiterpines
1. GABA release and reversal of uptake
2. inhibition of GABA breakdown

MATRICARIA RECUTITA
- Chamomile, apigenin
- benzodiazepine agonist (PAM of GABAr)

PIPER METHYSTICUM
- Kava, kavalactones
1. facilitates GABA binding
2. inhibits ion channels
3. MAO inhibitor
4. inhibits TXA2 synthesis

PASSIFLORA INCARNATA
- passionflower, chrysin
- benzodiazepine partial agonist

HUMULUS LUPULUS
- Hops, 2-methyl-3-butene-2-ol
- unknown

NEPETA CATARIA
- Catnip, cis-trans-nepetalactone
- unknown

34
Q

definitions:
CHOREA
TICS
ATHETOSIS
DIURETIC

A

CHOREA
- neurological disorder characterized by jerky involuntary movements affecting especially shoulders, hips and face
TICS
- a habitual spasmodic contraction of the muscles, most often in face
ATHETOSIS
- condition in which abnormal muscle contractions cause involuntary writhing movements. affects some people with cerabral palsy, impairing speech and use of hands
DIURETIC
- causing increased passing of urine

35
Q

DEFINITIONS
- neurological disorder characterized by jerky involuntary movements affecting especially shoulders, hips and face
- a habitual spasmodic contraction of the muscles, most often in face
- condition in which abnormal muscle contractions cause involuntary writhing movements. affects some people with cerabral palsy, impairing speech and use of hands
- causing increased passing of urine

A
  • Chorea
  • Tics
  • Athetosis
  • Diuretic

Herbs (12 decks)

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