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The Opiates, Smack, H and Tylenol III……. Psychology 3506. 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. Introduction.
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The Opiates, Smack, H and Tylenol III……. Psychology 3506
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
Introduction • So, there are natural and man made ones • Sap from poppy seeds • Morphine • Codeine Heroin diacetylmorphine 10 times as lipid soluble ‘semisynthetic’
Introduction • Synthetics • Methadone • LAHM • Levorphanol • phenozocine • Longer lasting • Usually taken orally
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……
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
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
Administration and Distribution • Crosses Blood brain and placental barriers • Some metabolites are also psychoactive • Heroin is faster • Monoacetylmorphine
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
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
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
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
Opiate Receptors • Kappa Receptor • Nucleus accumens • VTA • Hypothalamus • Thalamus Sigma Receptor • Not just opioids • Psychotic symptoms
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……….
Effects • Nausea • Constriction of pupils • Disrupts digestive coordination • Drop in sex hormones • Decrease in REM • Vivid daydreams though • rush
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
Effects • Monkey, rats, will work for it • Can be discriminated from other opiates • Can be generalized to other opiates
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
Self Administration • chipping • Maturing out • Titrated when available • Injected, snorted smoked • Monkeys will mainline morphine!
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
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)
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
Treatement • Willpower • Synanon • Antagonist Therapy Maintenance • Methadone • British System • LAAM