The Opiates, Smack, H and Tylenol III…….

Psychology 3506

Introduction

Anything like Opium (Morphine)Opiates are naturalOpioids are allNarcotic Analgesics

Sleep, no painNarcotic 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

SyntheticsMethadoneLAHMLevorphanolphenozocine

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 tobaccoSo everyone started smoking opium!

By the early 1800s the Brits loved itThey 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 slowFirst pass metabolismEasy to keep relatively constant levelsGreat for analgesia

Administration and Distribution

Crosses Blood brain and placental barriers

Some metabolites are also psychoactive

Heroin is fasterMonoacetylmorphine

How’s it work?

Even before the receptor was found it was pretty clear there was oneMolecular configuration related to effectMust be endorphins tooReceptor sites discovered, six month later,

enkephalins and endorphins discoveredBeta lipotropin in pituitary

How’s it Work?

Endorphins are found in vessiclesOne of the key indications that you have a

neurotransmitter on your hands

They interfere with NE Ach and DAModulatory properties

Opiate Receptors

Three or four typesMu

Throughout limbic system HP and amygdila

Thalamus and locus coeruleusResponsible for most interesting effectsWeak attraction = great effect

Opiate Receptors

Delta ReceptorLimbic system too, but do not overlap with muCortexHypothalamusNucleus accumbensMedullaMany antipsychotic drugs work on delta

receptors

Opiate Receptors

Kappa ReceptorNucleus accumensVTAHypothalamusThalamus

Sigma ReceptorNot just opioidsPsychotic symptoms

Opiate Receptors

Periaqueductal Grey area is full of opiate receptors When in pain, these are stimulated

Amygdila emotion

Respiratory, cough and vomit centresREWARD 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 REMVivid daydreams though

rush

Effects

Psychiatric like symptomsIncrease in SMA in small doesDecrease with large does

Spontaneous social behaviour ()Low DoesFI increase FR decrease

High DoesBoth 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……

ComaNo surprise here

ODCut with bad stuffLoss of tolerance (shooting gallery effectMixing with other respiratory depressants

More Bad Stuff

Constipation

Cancer?

LifestyleYou get it from criminalsYou share needlesYou get AIDS (21% of IV drug users in the

States also are HIV positive)

Just Say no to Heroin

Reproductive effectsSex hormones dropLow birthweight babiesWelcome 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

MaintenanceMethadoneBritish SystemLAAM