1. The Opiates, Smack, H and Tylenol III…….
Biology/Psychology 3506

3. Introduction Anything like Opium (Morphine) Opiates are natural
Opioids are all
Narcotic Analgesics
Sleep, no pain
Narcotic has a legal meaning, so this is rarely used any more

4. Introduction So, there are natural and man made ones
Sap from poppy seeds
Morphine
Codeine
Heroin
diacetylmorphine
10 times as lipid soluble
‘semisynthetic’

5. Introduction Synthetics Longer lasting
Methadone
LAAM
Levorphanol
Phenozocine
Fentanyl
Longer lasting
Usually taken orally or via patch though some injected.

6. A Little History The Sumerians called it the joy plant
Used extensively in classical ‘medicine’
In 1644 the Chinese Emperor banned tobacco
So everyone started smoking opium!
By the early 1800s the Brits loved it
They still do……

7. A Little History 1875 UK consumption was 10 PUNDS / 1000 people!
Morphine caught on
Temperance movement
Only physicians and pharmacists could sell it
In the US consumption was higher (13 lb)
Civil War

8. Administration and Distribution
Parenterally injected, best route to the brain
Oral administration is slow
First pass metabolism
Easy to keep relatively constant levels
Great for analgesia

9. Administration and Distribution
Crosses Blood brain and placental barriers
Some metabolites are also psychoactive
Heroin is faster
Monoacetylmorphine

10. How’s it work?
Even before the receptor was found it was pretty clear there was one
Molecular configuration related to effect
Must be endorphins too
Receptor sites discovered, six month later, enkephalins and endorphins discovered
Beta lipotropin in pituitary

11. How’s it Work? Endorphins are found in vessicles
One of the key indications that you have a neurotransmitter on your hands
They interfere with NE Ach and DA
Modulatory properties

12. Opiate Receptors Three or four types Mu Throughout limbic system
HP and amygdila
Thalamus and locus coeruleus
Responsible for most interesting effects
Weak attraction = great effect

13. Opiate Receptors Delta Receptor
Limbic system too, but do not overlap with mu
Cortex
Hypothalamus
Nucleus accumbens
Medulla
Many antipsychotic drugs work on delta receptors

14. Opiate Receptors Kappa Receptor Nucleus accumens VTA Hypothalamus
Sigma Receptor
Not just opioids
Psychotic symptoms

15. Opiate Receptors Periaqueductal Grey area is full of opiate receptors
When in pain, these are stimulated
Amygdila
emotion
Respiratory, cough and vomit centres
REWARD SYTEM!!!!!!!
Well, there has to be some good reason to put a needle in your arm……….

16. Effects Nausea Constriction of pupils Disrupts digestive coordination
Drop in sex hormones
Decrease in REM
Vivid daydreams though
rush

17. Effects Psychiatric like symptoms Increase in SMA in small does
Decrease with large does
Spontaneous social behaviour ()
Low Does
FI increase FR decrease
High Does
Both go down

18. Effects Monkey, rats, will work for it
Can be discriminated from other opiates
Can be generalized to other opiates

19. Tolerance and Withdrawal
Tolerance develops quickly
No surprise here
Withdrawal bad, but not as bad as sleeping pills or martinis
6-30 hr
restless
Hot flashes
Goose bumps
Jerky breathing
Puking et al
Kicking the habit

20. Self Administration chipping Maturing out Titrated when available
Injected, snorted smoked
Monkeys will mainline morphine!

21. If its this fun, it can’t be good for you……
Coma
No surprise here OD
Cut with bad stuff
Loss of tolerance (shooting gallery effect
Mixing with other respiratory depressants

22. More Bad Stuff Constipation Cancer? Lifestyle
You get it from criminals
You share needles
You get AIDS (21% of IV drug users in the States also are HIV positive)

23. Just Say no to Heroin Reproductive effects Sex hormones drop
Low birthweight babies
Welcome to Earth, this is your mother, this is your father, the withdrawal symptoms will be over in a couple of days….
More illnesses after birth

24. Treatement Willpower Synanon Antagonist Therapy Maintenance Methadone
British System
LAAM
LAAM Levacetylmethadol