Med and Behavior Chapter 9 Flashcards
With what drug has there been an upward trend in usage?
Marijuana
What was amphetamine extracted from?
The Ephedra plant
What was LSD extracted from?
the ergot fungus
Drug Schedule
a drugs classification based on its potential for abuse
what is the Controlled Substance Act of 1970?
Identified five schedules or classifications of drugs.
What is cocaine derived from
the coca plant in mountainous regions of South America
What does coca leaves induce when chewed?
A feeling of wellbeing and confidence as well as relief from fatigue
What is most cocaine exported as?
cocaine sulfate or cocaine hydrochloride
How is cocaine made?
1) stomping on leaves in kerosene, benzene, or alcohol
2) Liquid mixture produced is processed with heat and sulfuric acid to isolate cocaine alkaloids and remove waxy residue
3) This results in cocaine sulfate paste which contains as much as 60% cocaine
4) Cocaine paste can be processed into cocaine hydrochloride by mixing it with diluted hydrochloric acid.
How much does a gram of cocaine hydrochloride cost?
About $175
When and by who was the Cocaine alkaloid isolated?
By Freidrich Gaedcke in 1855
What did Gaedcke call cocaine?
erythroxyline
Who named Cocaine, cocaine?
Albert Niemann
What medical purpose does cocaine serve?
As a local anesthetic for surgeries, eyes, nose
What beverages in 1863 was cocaine added to?
Vin Mariani and Coca-cola
What famous psychologist used cocaine and advocated for it?
Freud
What scientific papers and letters did Freud advise people to use Cocaine in?
Cocaine Paper. Specifically Uber Cocaine (about cocaine) in 1884
Harrison Narcotic Tax act in 1914
Prohibited cocaine and misidentified as a narcotic
What drugs are more commonly used as opposed to cocaine for surgery?
Xylocaine and Novocaine
Cocaine hydrochloride (cocaine-HCI) is a water/fat soluble compound?
water soluble
What does cocaine separate into?
cocaine-H+ and Cl- ions
Which ion quickly passes through the cell membrane and into the brain?
Cocaine-H+
How is methylbenzoylecgonine made and taken?
It is made through by dissolving cocaine hydrochloride in mild ammonia solution and is used through vaporizing for inhalation
Why is mehtylbenzoylecgonine called crack?
Because during the production it produces a cracking sound
What is another way to make crack?
By heating cocaine hydrochloride in water and sodium bicarbonate to make freebase cocaine rocks.
What is the half life of cocaine
between 1 and 1.5 hours
How is cocaine distributed throughout the body?
widely
Is cocaine metabolized quickly or slowly into the blood and by the liver?
quickly
What are the principle metabolites of cocaine?
benzoylecgonine and ecgonine.
What is formed when cocaine is used with alcohol?
cocaethylene
Does cocaine or cocaethlyene have a more potent euphoria?
cocaethlyene
What is the half life of cocaethylene?
2.5 hours
What is cocaethlyene particularly toxic to?
Cardiac functioning (hypertension, ventricular arrhythmia, and decreased blood flow)
What does cocaine bind to?
DAT
What does cocaine block?
The reuptake of dopamine
What else does cocaine effect?
NE and 5HT
What is the most important function of cocaine for its psycho simulating and reinforcing effects?
The dopamine transporter binding
What are the subjective euphoric effects of cocaine related to?
the degree of DAT binding
What is the difference between the effects of Ritalin and Cocaine on DAT?
How rapidly DAT blockade occurs after administration
A rapid increase of dopamine activity in what part of the brain is critical for euphoric and reinforcing potential?
The mesolimbic system
Place preference conditioning
An experiment procedure where animals are tested for their preference for an area in an experimental apparatus where drugs had been administered over other areas within the apparatus. A form of Pavlovian conditioning where a place becomes associated with drug effects.
What contributes to enhanced activity of dopamine in the mesolimbic system(nucleus accumbens)
cocaine’s effects on 5HT neurons in the VTA
What makes cocaine good for anesthetic surgery?
It constricts local blood flow
What does cocaine block as a local anesthetic?
voltage-gated Na+ channels
What are Cocaine’s respiratory depressant effects mediated by?
NA+ channel blockade in neurons within the chemosensitive sites of the medulla
What is the first amphetamine compound to be used and what was it extracted from?
ephedrin from ephedra sinica plant
What is the ephedra sinica plant also known as?
ma huang
What has ma huang been used for?
asthma, allergic reactions, and congestion from a cold
What is a recent used for ephedra>
weight loss, increased wakefulness, and performance inhancer.
Who synthesized amphetamine?
Lazar Edeleanu in 1887
What was amphetamine first marketed under and for what?
Benzedrine for inhalant antihistamine
What amphetamine was used for narcolepsy, attention disorders, nasal congestion, and obesity?
dextroamphetamine (Dexedrine)
When did amphetamine production reach its all time high and what was the number?
1970s at 10 billion tablets
What was Benzedrine replaced with?
propylhexedrine
What schedule drug is Dexedrine (dextroamphetamine)
Schedule 2
When was Methamphetamine synthesized, from what, and what is its chemical name?
in 1893, from ephedrine, and desoxyephedrine (methyl-amphetamine)
How does methamphetamine differ structurally from amphetamines?
By the addition of methyl group CH3
What is methamphetamine in a pure form
a crystal (hint the name crystal meth)
Does amphetamines or methamphetamine enter the brain more quickly?
methamphetamine
What creates a greater high, amphetamine or methamphetamine?
Methamphetamine (users prefer)
what is the half life of amphetamines?
10-15 hours
What is amphetamine metabolized into?
p-OH-amphetamine and norephedrine (both inactive)
What is methamphetamine metabolized into?
Amphetamine
What does amphetamines and methamphetamine do?
1) blocking reuptake transporters for NE
2) Increases DA and NE synthetization
3) Reversing the DAT
Dopamine agonism contributes to euphoria and increased cortical arousal through what pathways…
Through the mesolimbic and mesocortical pathways which originate in the VTA and the nigrostriatal which originates in the substantia nigra and projects to basal ganglia
Where does dopamine project to from the VTA?
to the nucleus accumbens, amygdala, and hypothalamus in the mesolimbic. For the mesocortical to the prefrontal cortex
stereotyped behavior
rigid repetitive movements observed in experimental animals after the administration of psychomotor stimulants such as cocaine or amphetamine
Amphetamines increase NE and DA contributing to cortical arousal through what?
The reticular activating system originating in the brain stem
What appetite suppressing peptide does amphetamines increase the expression of?
CART (cocaine and amphetamine-regulated transcript)
What is a compound structurally related to amphetamines’ with powerful euphoric effects?
MDMA (methylenedioxymethamphetamine) or ecstasy
What is a less familiar compound structurally related to amphetamines’ with powerful euphoric effects?
MDA (methylenedioxyamphetamine
What is a nickname for MDMA
Molly
What was MDMA originally used for?
to assist in psychotherapy
What schedule is MDMA?
Schedule 1
What does MDMA produce?
euphoria, increased self-perception, and enhanced sensations, promotion of intimacy with others
What are side effects of MDMA?
increased heart rate and blood pressure, intense sweating, and teeth grinding.
What is the most troubling effect of MDMA?
powerfully neurotoxic effects.
How long do the degenerative effects on cortical serotonergic neurons persist after MDMA use?
many years
Does MDMA use promote an increase or decrease of serotonin synthesis in the frontal cortex?
decrease
Is MDMA a 5HT and Da agonist or antagonist?
agonist
How does MDMA directly increase serotonin activity?
1) increasing release and preventing reuptake
How does MDMA enhance DA activity in the nucleus accumbens?
By blocking DAT and indirectly through enhancing serotonin which regulates DA in the VTA
MDMA is predominantly a what agonist
5HT
what mediates MDMA reinforcing effects in animal self-administration studies?
DA
What are the most striking hallucinations caused by LSD?
the visual (involving color and movement)
synesthesia
A perceptual phenomenon where sensations in one modality are experienced or mixed with another
When and by who was LSD first synthesized?
By Dr. Albert Hofmann in 1938
How fast are peak plasma levels reached with LSD
2 hours
What is the half life of LSD?
Between 2 and 3 hours
What is the most potent psychoactive drug?
LSD
Is there a confirmed lethal dose of LSD?
NO
Side effects of LSD
increased body temperatures, heart rate, blood pressue, pupil dilation, dizziness, and occasional nausea.
Psychological side effects
confusion, acute panic, noticeable distortions in space and time
LSD and psilocybin are partial agonists of what?
5HT
LSD and psilocybin bind with high or low affinity to 5HT receptor subtypes
High
5HT, LSD, and psilocybin have what in common?
an indole structure
How does LSD disrupt serotonin sensory information that is projected from the brainstem to the thalamus and then cortical sensory area
LSD disrupts normal filtering of extraneous sensory information. This results in over stimulation of cortical sensory areas. LSD also increases activity of sensory neurons to stimulation.
What does LSD potentially alter the activity of
medial prefrontal cortex and the anterior cingulate through agonizing 5HT2a receptors
What is the hemp plant that marijuana comes from?
Cannabis sativa
What was the hemp plant used for in colonial times
rope
Marihuana Tax Act of 1937
banned cannabis altogether with costly tax provisions
Who first extracted cannabinols from marihuana in 1846?
The Smith brothers of Scotland
Who extracted THC (tetrahydrocannabinol)
Gaoni and Mechoulam (Israeli chemists
What is the best administration of THC?
smoking
How fast are peak plasma levels reached?
a few minutes
What is the bioavailability of THC in a cigarette
5 mg
What is THC metabolized into?
11-hydroxy-THC in the liver and then 11-nor-9-carboxy-THC before excretion
What is the elimination half life of THC?
24 and 72 hours
Where can cannabanoid receptors be found?
basal gangliam cerebellum, hipppocampus, amygdala, thalamus and the cortex
