BIO SCI N153 Lecture Notes - Lecture 14: Reuptake, Partial Agonist, Dopamine Receptor D2
11 May 2018
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N153 Lecture #? (Chapter 12)
Chapter 12: Psychostimulants (cocaine and amphetamines)
I. Cocaine
a. 2 million current users
b. 5 million users prior year
c. 34 million (more than 14% US population) used at least one during life
i. Problem with this data is that some people may be tempted to
lie or give false information, so it is not 100% accurate
d. Cocaine derived from coca leaves
II. National overdose
a. Celebrities that overdosed
i. DJ AM
ii. Whitney Houston
iii. Jeff Rice
iv. Corey Haim
b. Number of overdose deaths for women steady over years
c. Number for men increased as some point but has decreased again
d. Number of overdose in general is higher for men than in women
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III. Coca cultivation
a. Mainly in:
i. Columbia
ii. Bolivia
iii. Peru
b. Processing main in:
i. Bolovia
IV. Pharmacology of cocaine
a. Coca leaves 0.6%-1.8% cocaine
b. When derived into the past, it is 50% cocaine
c. freeasig: dissolig i ater ad addig aoia
d. Highly flammable and explosive
e. Purified form converted into hydrochloride salt and crystallized
i. Cocaine HCL: oral, intranasal, and IV
ii. Free basing
iii. Crack
f. You can detect if someone is using crack or cocaine because of the
specific things you test for in urine (metabolites)
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g. High only lasts about 30 minutes which leads to repeated use within
one session
h. Lipophilic (passes through the BBB)
i. Does not need a transporter so there is not much that will stop
it from passing through
ii. Half life of 0.5 hours to 1.5 hours
1. Half life depends on the form of administration
i. Metabolite
i. Benzoylecgonine
ii. Present for a couple of days after use
j. Alcohol + cocaine cocaethylene
i. Cocaine is usually used in addition to other drugs that will create
a different high because of their interactions
ii. Cocaethylene has similar actions as cocaine but it will last much
longer than just cocaine on its own
V. Mechanism of cocaine action
a. Blocks DA, NE, and 5-HT reuptake transporters
i. Highest affinity for the 5-HT transporter
ii. DA transporter: stimulating, reinforcing, addictive properties
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Document Summary
Coca cultivation: mainly in, columbia, bolivia, peru, processing main in, bolovia. 4: another is novocaine which were both derived from the structure of cocaine. 5: 6-ohda lesion in nacc reduced reinforcing properties of cocaine/amphetamine. Evidence of mechanism in humans: pet imaging, da transporter occupancy approx. Cocaine abuse and chronic exposure: reinforcing, stimulating, euphoric, confidence-enhancing effects, cocaine binges, experimentation begins around 13 to 15 years old. 9: 10 to 15% of users become dependent on the drug, there is specific social groups that will have a more constant drug use and there will be more use and a higher chance of developing dependence. 10: we see that in long access we have autoreceptor sensitivity decreased, cocaine is less effective at inhibiting reuptake, intra and extra cellular da levels are reduced. Cocaine abuse and chronic exposure: high comorbidity rate with depression, anxiety, and personality disorders, comorbidity: if you have one disease it is more likely that you will have another disease, depression.
