8-9: Stimulants and sedatives Flashcards
DOPAMINE
- what kind of neurotransmitter + subtype?
- found where (2) + 2 sub
- used to treat (2)
- receptors? (2)
- 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+
what are the 3 main dopamine pathways?
*ON EXAM!
- all start from where ish?
- nigrostriatal pathway (motor control, Parkinson’s)
- tuberinfundibular pathway (maternal nurturing)
- mesolimbic and mesocortical pathways (or limbo-cortical) (memory, motivation, reward, addiction)
- brainstem!
KNOW THIS
in each of the 3 pathways
- nigrostriatal pathway
- tuberinfundibular pathway
- mesolimbic and mesocortical pathways
what happens when you have LOW vs HIGH dopamine?
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
Coca (monograph):
- SCIENTIFIC NAME:
- PART USED:
- MODE OF ADMINISTRATION:
- BIOACTIVE COMPOUND:
- COMPOUND CLASS:
- USES:
- SCIENTIFIC NAME: erythroxylum coca
- PART USED: leaves
- MODE OF ADMINISTRATION: chewed, insufflation, inhalation
- BIOACTIVE COMPOUND: cocaine
- COMPOUND CLASS: alkaloid
- USES: stimulant + increased endurance
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
- 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
NOT IN EXAM
- 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)
- 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
NOT IN EXAM
- what is the mechanism of action of cocaine?
- leads to increased available what?
- chronic use leads to decreased what?
- effects (6 ish)
- blocks reuptake of monoamine neurotransmitters (dopamine, NE, serotonin) EXAM
- 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
why/how is cocaine addictive?
because it interferes with reuptake of dopamine in mesolimbic dopamine pathway! EXAM!
- cocaine blocks the dopamine transporter (reuptakes dopamine back into pre-synaptic neuron)
Norepinephrine
- what type of neurotransmitter + subtype?
- found where?
- used to treat (3)
- receptors?
- 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
ephedra (monograph)
- SCIENTIFIC NAME:
- PART USED:
- MODE OF ADMINISTRATION:
- BIOACTIVE COMPOUND:
- COMPOUND CLASS:
- USES:
- SCIENTIFIC NAME: ephedra sinica
- PART USED: dried stems, root
- MODE OF ADMINISTRATION: infusion
- BIOACTIVE COMPOUND: ephedrine, pseudoephedrine
- COMPOUND CLASS: alkaloid
- USES: stimulant, thermogenic
- what is the chinese name for ephedra?
- used for what? (10)
- ephedrine alkaloids cause (7)
- side effects (4)
- 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
NOT IN EXAM
EPHEDRINE
- is a CNS ________ similar to what?
- mechanism of action (3 steps)
- 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
EXAM!
PURINES:
- found where (6)
- used to treat what?
- receptors?
- found in brain, heart, kidney, adipose tissue + neurons and glial cells
- supraventricular tachycardia
- ionotropic (P2X receptors, ATP) and metabotropic (P1 and P2Y receptors)
dont need to know receptors
- 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
- purinergic receptors!
- ionotropic P2X receptors binds ATP and evolved a billion years ago –> very conserved
- ATP and adenosine
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?
- 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
EXAM!
CAFFEINE
- CNS _________
- acts as what?
- responsible for what?
- CNS stimulant
- acts as an antagonist for ALL adenosine receptors
- antagonistic effects on the A2A receptor is responsible for alertness
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?
- 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
coffee (monograph)
- SCIENTIFIC NAME:
- PART USED:
- MODE OF ADMINISTRATION:
- BIOACTIVE COMPOUND:
- COMPOUND CLASS:
- USES:
- SCIENTIFIC NAME: coffea arabica
- PART USED: seed
- MODE OF ADMINISTRATION: infusion/percolation
- BIOACTIVE COMPOUND: caffeine
- COMPOUND CLASS: alkaloid
- USES: stimulant
*every plant below all contain Caffeine also!
tea (monograph)
- SCIENTIFIC NAME:
- PART USED:
- MODE OF ADMINISTRATION:
- BIOACTIVE COMPOUND:
- COMPOUND CLASS:
- USES:
- 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
*also contains caffeine!
cocoa (monograph)
- SCIENTIFIC NAME:
- PART USED:
- MODE OF ADMINISTRATION:
- BIOACTIVE COMPOUND:
- COMPOUND CLASS:
- USES:
- 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
yerba maté (monograph):
- SCIENTIFIC NAME:
- PART USED:
- MODE OF ADMINISTRATION:
- BIOACTIVE COMPOUND:
- COMPOUND CLASS:
- USES:
- SCIENTIFIC NAME: Ilex paraguariensis
- PART USED: leaves and stem
- MODE OF ADMINISTRATION: infusion
- BIOACTIVE COMPOUND: theobromine (and caffeine)
- COMPOUND CLASS: alkaloid
- USES: stimulant
guanara (monograph):
- SCIENTIFIC NAME:
- PART USED:
- MODE OF ADMINISTRATION:
- BIOACTIVE COMPOUND:
- COMPOUND CLASS:
- USES:
- SCIENTIFIC NAME: Paullinia cupana
- PART USED: seeds
- MODE OF ADMINISTRATION: roasted
- BIOACTIVE COMPOUND: caffeine
- COMPOUND CLASS: alkaloid
- USES: stimulant
what are 5 plants that contain caffeine?
- which has higher caffeine content?
- guarana (2.5-5% caffeine)
- tea (2.9-4.2%)
- coffee (1-3.2%)
- yerba maté (0.4-2.4%)
- cocoa (0.4-1.2%)
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
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
