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The Major OpiatesThe Major Opiates
Most common used drug for relief of pain Most common used drug for relief of pain Only true Narcotics (stupor, sleep, Only true Narcotics (stupor, sleep,
analgesia)analgesia) compare to marijuana and cocaine which compare to marijuana and cocaine which
have other effects such as euphoria, have other effects such as euphoria, stimulant properties.stimulant properties.
Also cough suppressant & antidiarrea Also cough suppressant & antidiarrea propertiesproperties
““Narcotics” is Greek word for “stupor”Narcotics” is Greek word for “stupor” not for illicit psychoactive drugnot for illicit psychoactive drug
The Major OpiatesThe Major Opiates
Opium derived from juice of poppy plant Opium derived from juice of poppy plant What is an opiate?What is an opiate?
AnalgesicAnalgesic Acts on endorphan/enkephalin receptorsActs on endorphan/enkephalin receptors Antagonized by naloxoneAntagonized by naloxone
Most potent painkiller, but severe dependence Most potent painkiller, but severe dependence
The Major OpiatesThe Major Opiates
Endogenous OpiodsEndogenous Opiods Endorphine, Enkephalin, DynorphinEndorphine, Enkephalin, Dynorphin
in pituitaryin pituitary in pain sensors (spinal cord & midbrain)in pain sensors (spinal cord & midbrain) affective states (amygdala, hippocampus, locus affective states (amygdala, hippocampus, locus
coeruleus, and cerebral cortex)coeruleus, and cerebral cortex) autonomic system (e.g. medulla)autonomic system (e.g. medulla) stomach and intestinesstomach and intestines
Classification of OpiatesClassification of Opiates
3 specific groups of opiates used3 specific groups of opiates used Natural NarcoticsNatural Narcotics
Opium & extracts (morphine, codeine & thebaine)Opium & extracts (morphine, codeine & thebaine)
Semisynthetic NarcoticsSemisynthetic Narcotics Slight changes to chemical composition of morphineSlight changes to chemical composition of morphine E.g. heroinE.g. heroin
Synthetic Narcotics Synthetic Narcotics Not related to morphine, but produce opiate like responsesNot related to morphine, but produce opiate like responses
Classification of OpiatesClassification of Opiates
Opium, morphine, heroin, thebaine & Opium, morphine, heroin, thebaine & codeine referred to as opiatescodeine referred to as opiates
Synthetic Narcotics referred to a synthetic Synthetic Narcotics referred to a synthetic opiates or synthetic opiate-like drugsopiates or synthetic opiate-like drugs
History of OpiumHistory of Opium
Native to Middle East in areas bordering Native to Middle East in areas bordering MediterraneanMediterranean
Also Laos, Thailand, Afghanistan, Mexico & Also Laos, Thailand, Afghanistan, Mexico & ColumbiaColumbia
Use dates back 6000 years to SummariansUse dates back 6000 years to Summarians Egyptians used it medically 3500 years agoEgyptians used it medically 3500 years ago
Excavation of ceramic opium pipe in CypresExcavation of ceramic opium pipe in Cypres Common use among Islamic peoples for medical Common use among Islamic peoples for medical
& recreational purposes& recreational purposes not forbidden in Koran as were alcohol & many other not forbidden in Koran as were alcohol & many other
drugsdrugs
History of OpiumHistory of Opium Arab traders took to India & ChinaArab traders took to India & China
Also, western Europe learned about it from Also, western Europe learned about it from Arabs during crusades Arabs during crusades
1520 Paracelsus & laudanum1520 Paracelsus & laudanum 1680 Thomas Sydenham & his version of 1680 Thomas Sydenham & his version of
laudanumlaudanum Next 200 yrs primary consumption of opium Next 200 yrs primary consumption of opium
is as drinkis as drink
China & OpiumChina & Opium
Up to 1700’s Chinese use limited to Up to 1700’s Chinese use limited to “painkiller”“painkiller”
1818thth century development of opium smoking century development of opium smoking China first laws against Opium use in 1729China first laws against Opium use in 1729
dependence problem recognizeddependence problem recognized
British traded for tea with ChineseBritish traded for tea with Chinese 1773 Brits control of India-begin to supply 1773 Brits control of India-begin to supply
opium to China opium to China basis for Opium wars between China & Britishbasis for Opium wars between China & British
China & OpiumChina & Opium
China tried to control drug problemChina tried to control drug problem 1839 Defiance of European power1839 Defiance of European power
Confiscation of large quantities of opiumConfiscation of large quantities of opium Burned it in CantonBurned it in Canton Start of opium warStart of opium war
Opium WarsOpium Wars
First WarFirst War 1839-1842 Hong Kong ceded to British (‘til 1839-1842 Hong Kong ceded to British (‘til
1997), Canton & Shanghai opened for trade1997), Canton & Shanghai opened for trade
Second WarSecond War 1858-1860 British joined by French & 1858-1860 British joined by French &
American forcesAmerican forces 20 mill. pounds sterling, opening of 20 mill. pounds sterling, opening of
remaining ports, legalization & regulation of remaining ports, legalization & regulation of opium trade (ended 1906)opium trade (ended 1906)
Difference in Opium UseDifference in Opium Use
Major difference between opium use in China & Major difference between opium use in China & West was method of consumptionWest was method of consumption laudanum laudanum
Identified with Victorian Era Identified with Victorian Era Opening of “respectable parlors”Opening of “respectable parlors”
Chinese smoked it Chinese smoked it Identified with Opium DensIdentified with Opium Dens Ideal of “lazy” ChineseIdeal of “lazy” ChineseSeen as degrading & dirty vice Seen as degrading & dirty vice
Opium & the WestOpium & the West
Western societiesWestern societies Used opium as aspirinUsed opium as aspirin Cheaper than liquorCheaper than liquor No negative public opinionNo negative public opinion No real problem with copsNo real problem with cops Used to sooth infants & childrenUsed to sooth infants & children
Teething, colic or to keep them quiteTeething, colic or to keep them quite Women used it more than maleWomen used it more than male
Greater # addictionGreater # addiction
Problems in the WestProblems in the West
Collision of culturesCollision of cultures Chinese building railroadChinese building railroad 1875 San Francisco outlawed opium dens 1875 San Francisco outlawed opium dens
& opium smoking & opium smoking Laws targeted not at opium (laudanum legal), Laws targeted not at opium (laudanum legal),
but at Chinesebut at Chinese
Federal laws prohibiting opium smoking Federal laws prohibiting opium smoking followed followed
Morphine & the WestMorphine & the West
1803 Sertürner separated morphine from 1803 Sertürner separated morphine from opiumopium Increased dependence potentialIncreased dependence potential Morphine 10 X opium potencyMorphine 10 X opium potency Morpheus; Greek God of dreamsMorpheus; Greek God of dreams
1856 development of hypodermic needle1856 development of hypodermic needle Use became widespreadUse became widespread Doctors began injecting opium solutions (thought Doctors began injecting opium solutions (thought
sidestep addiction-thought purer & safer )sidestep addiction-thought purer & safer ) Used during Civil War for injuries (dependency known Used during Civil War for injuries (dependency known
as “soldier’s disease”)as “soldier’s disease”)
Heroin: From Bad to WorstHeroin: From Bad to Worst
In 1874 British chemist altered morphineIn 1874 British chemist altered morphine but unnoticed until rediscovered in 1898 but unnoticed until rediscovered in 1898 1898 German Heinrich Dreser1898 German Heinrich Dreser
Heroin-altered form of morphine Heroin-altered form of morphine 3X-4 X more potent than morphine 3X-4 X more potent than morphine Thought to be safer than morphineThought to be safer than morphine
Sold by Bayer beginning in lieu of codeine as Sold by Bayer beginning in lieu of codeine as medicine for coughs, bronchitis, tuberculosismedicine for coughs, bronchitis, tuberculosis
Heroin also began to replace morphine in addicted Heroin also began to replace morphine in addicted individuals individuals
Opiates in the USOpiates in the US
By 1900 250, 000 “opium dependent By 1900 250, 000 “opium dependent people” in USpeople” in US
By 1913, 400,000 lbs of opium imported By 1913, 400,000 lbs of opium imported into U.S. for consumption by U.S. into U.S. for consumption by U.S. population of 90 mill. peoplepopulation of 90 mill. people
Laws began cropping up around this Laws began cropping up around this time and formed the cornerstone of time and formed the cornerstone of American drug laws todayAmerican drug laws today
Opiates in US Early 1900’sOpiates in US Early 1900’s
Harrison Act of 1914Harrison Act of 1914 No ban on opiates, but doctors had to No ban on opiates, but doctors had to
register with IRSregister with IRS Decreased prescriptionsDecreased prescriptions
Users not seen as victims but weakUsers not seen as victims but weak heroin drug of choice in black marketheroin drug of choice in black market
Shift of users not women, but white urban adult Shift of users not women, but white urban adult malesmales
Opiates Use in 1960’sOpiates Use in 1960’s
3 Major Social Developments3 Major Social Developments Crackdown cause shortage of heroin & Crackdown cause shortage of heroin &
increased smuggling & price increased smuggling & price Increased levels of crimeIncreased levels of crime Increased used by urban minoritiesIncreased used by urban minorities
Peace movement, hippies & drug culturePeace movement, hippies & drug culture Vietnam WarVietnam War
Opiates Use in 1980, 90’sOpiates Use in 1980, 90’s ““Golden Triangle”Golden Triangle”
Laos, Burma & ThailandLaos, Burma & Thailand Afghanistan, Pakistan, Iran & MexicoAfghanistan, Pakistan, Iran & Mexico Dominate heroin supply routeDominate heroin supply route Shift from Turkey as main supplierShift from Turkey as main supplier Opened a large vacuumOpened a large vacuum
Fentanyl “China White” used as surgical Fentanyl “China White” used as surgical anesthetic & prescription painkiller anesthetic & prescription painkiller
10 to 10,000 X stronger than heroin10 to 10,000 X stronger than heroin Sometimes found itself on black marketSometimes found itself on black market
Opiates in 20Opiates in 20thth century US century US Morphine is schedule IIMorphine is schedule II
Heroin schedule I Heroin schedule I In Britain comparably seems as “Schedule II”In Britain comparably seems as “Schedule II”
Schedule I = no accepted medical useSchedule I = no accepted medical use Schedule V = has medical use, not too Schedule V = has medical use, not too
addictiveaddictive most legally used opioids are either most legally used opioids are either
semisynthetic or syntheticsemisynthetic or synthetic no legal U.S. use for heroin - purely illicit drug no legal U.S. use for heroin - purely illicit drug
(in the US) with large worldwide market today (in the US) with large worldwide market today
Opiates in 20Opiates in 20thth century US century US
about 4-5000 metric tons opium produced about 4-5000 metric tons opium produced in 1990 (2,200 lbs)in 1990 (2,200 lbs)
compared to 200-225,000 metric tons compared to 200-225,000 metric tons coca in same yearcoca in same year
Business of OpiatesBusiness of Opiates
opium grown in 2 primary regions of world using opium grown in 2 primary regions of world using simple farming techniquessimple farming techniques
poppies grown, petals fall, small incisions, liquid poppies grown, petals fall, small incisions, liquid oozes out - opiumoozes out - opium
opium - 10% morphine 0.5% codeineopium - 10% morphine 0.5% codeine morphine refined in growing areas then morphine refined in growing areas then
transported or processedtransported or processed heroin - equal amount - then diluted to 1-10%heroin - equal amount - then diluted to 1-10%
Business of OpiatesBusiness of Opiates
extremely profitable as a businessextremely profitable as a business kg morphine in Italy $12,500 - heroin in kg morphine in Italy $12,500 - heroin in
U.S. 1.7 millionU.S. 1.7 million 10 kg opium $300 in production region10 kg opium $300 in production region heroin in New Delhi $10,000heroin in New Delhi $10,000 in U.S. 1.5 millionin U.S. 1.5 million
Absorption, Distribution, Absorption, Distribution, Metabolism & ExcretionMetabolism & Excretion
Most opiates poorly absorbed through GI Most opiates poorly absorbed through GI tract (except codeine)tract (except codeine) Effective nasally and through lungsEffective nasally and through lungs Opium frequently smoked, heroin snortedOpium frequently smoked, heroin snorted Most effective i.v. (heroin 100 times more Most effective i.v. (heroin 100 times more
potent i.v. than orally) potent i.v. than orally)
Absorption, distribution & Absorption, distribution & excretionexcretion
In bloodstream distributed throughout In bloodstream distributed throughout bodybody accumulating in kidney, lung, liver, spleen, accumulating in kidney, lung, liver, spleen,
muscle & brainmuscle & brain
Opiates and blood brain barrier Opiates and blood brain barrier Morphine does not cross BBB wellMorphine does not cross BBB well
only 20% of circulating enters brainonly 20% of circulating enters brain 30-60 min to reach significant brain concentrations30-60 min to reach significant brain concentrations
Absorption, distribution & Absorption, distribution & excretionexcretion
Heroin more lipid soluble so penetrates Heroin more lipid soluble so penetrates BBB betterBBB better
Both morphine & heroin cross placentaBoth morphine & heroin cross placenta heroin converted to morphine once it cross the heroin converted to morphine once it cross the
BBBBBB once crossed BBB codeine 10% converted to once crossed BBB codeine 10% converted to
morphinemorphine
Absorption, distribution & Absorption, distribution & excretionexcretion
Most opiates rapidly metabolized in liver Most opiates rapidly metabolized in liver and excreted by kidneyand excreted by kidney
Half-life about 2.5-3 hrsHalf-life about 2.5-3 hrs Duration of effect 4-5 hrsDuration of effect 4-5 hrs 5-15 mg optimal analgesic dose for 5-15 mg optimal analgesic dose for
morphine - addicts 2 g Hmorphine - addicts 2 g H
Opiates Opiates Opium, morphine, codeine Opium, morphine, codeine Derivatives or semisynthetic (minor modification Derivatives or semisynthetic (minor modification
in structure)in structure) heroin, nalorphine, and hydromorphoneheroin, nalorphine, and hydromorphone
Synthesized—have different structures, but Synthesized—have different structures, but similar propertiessimilar properties Meperidine (Demerol)Meperidine (Demerol) Fentanyl (Sublimaze)Fentanyl (Sublimaze)
Proxyphene (Darvon, Darvocet) Proxyphene (Darvon, Darvocet) – lousy analgesic– lousy analgesic
Methadone (Dolophine)Methadone (Dolophine)
Absorption, distribution & excretionAbsorption, distribution & excretion
Have somewhat different pharmacological Have somewhat different pharmacological effectseffects
Differ in potency, duration of action & oral Differ in potency, duration of action & oral effectivenesseffectiveness
Because of differences in pharmacokineticsBecause of differences in pharmacokinetics Heroin more potent than morphine when Heroin more potent than morphine when
injected, but same when taken orally.injected, but same when taken orally. slight modification of heroin from morphine slight modification of heroin from morphine
allows it to cross BBB better—What would this allows it to cross BBB better—What would this do?do?
Absorption, distribution & excretionAbsorption, distribution & excretion
Metabolized into morphine in brainMetabolized into morphine in brain because it gets there quicker, more rapid intense effects.because it gets there quicker, more rapid intense effects. Codeine- 12x less potent that morphine when injectedCodeine- 12x less potent that morphine when injected better absorbed orally (morphine\heroin weak alkaloids)better absorbed orally (morphine\heroin weak alkaloids) Endogenous opiates more potent than heroinEndogenous opiates more potent than heroin But inactivated quicklyBut inactivated quickly Fentanyl-50 times more powerful than heroin (IM)Fentanyl-50 times more powerful than heroin (IM) Used for surgery, but easy for addicts to ODUsed for surgery, but easy for addicts to OD
Medical UseMedical Use
• analgesiaanalgesia
• sedation-markedly differs between sedation-markedly differs between individualsindividuals
poor sedative in generalpoor sedative in general
• anti-diarrhea agentsanti-diarrhea agents extremely effective for dysentery (1800's)extremely effective for dysentery (1800's) were the only effective agents in that timewere the only effective agents in that time
Mechanism of Action Mechanism of Action
act via the endogenous opiate systemact via the endogenous opiate system 1960's discovery of the opiate antagonist 1960's discovery of the opiate antagonist
naloxone (Narcannaloxone (Narcan77)) implication of common receptor site for opiates implication of common receptor site for opiates
actionsactions 1973 Pert and Snyder discovery of "opiate 1973 Pert and Snyder discovery of "opiate
receptors"receptors" led to discovery of several endorphins in 1975led to discovery of several endorphins in 1975
beta-endorphinbeta-endorphin enkephalinenkephalin dynorphindynorphin
Pharmacological ActionsPharmacological Actions
Primary effect of narcotics is sedative-Primary effect of narcotics is sedative-hypnotichypnotic Some cause stimulation immediate after Some cause stimulation immediate after
injectioninjection Cats and some humans are the only mammals that Cats and some humans are the only mammals that
show stimulationshow stimulation
Pharmacological ActionsPharmacological Actions
Primary sites of action - Primary sites of action - CNS and GI tractCNS and GI tract For both medicine and abuse, opiate use due to For both medicine and abuse, opiate use due to
3 actions3 actions AnalgesiaAnalgesia (best for dull continuous, not sharp) (best for dull continuous, not sharp)
still feel sensations, can remain alertstill feel sensations, can remain alert vision, hearing, touch okayvision, hearing, touch okay
EuphoriaEuphoria (dream like state with intense visions) (dream like state with intense visions) ConstipationConstipation (used for diarrhea and dysentery) (used for diarrhea and dysentery)
Pharmacological ActionsPharmacological Actions
Natural pain relief systemNatural pain relief system Used for chronic, not sharp, acute painsUsed for chronic, not sharp, acute pains
childbirth, battlefield injuries, strenuous exercise, childbirth, battlefield injuries, strenuous exercise, acupunctureacupuncture
addiction to exercise related to endorphin releaseaddiction to exercise related to endorphin release
can you be addicted to an endogenous can you be addicted to an endogenous substance?substance?
Pharmacological ActionsPharmacological Actions
Opiates also relieve psychological painOpiates also relieve psychological pain anxieties, feelings of inadequacy, hostility & anxieties, feelings of inadequacy, hostility &
aggressionaggression produce extremely pleasant mood states - produce extremely pleasant mood states -
euphoriaeuphoria pain relief due to central effect - no effect on pain relief due to central effect - no effect on
sensory nerve transmissionsensory nerve transmission begins at spinal cord & continues throughout begins at spinal cord & continues throughout
CNSCNS
Abuse PotentialAbuse Potential
Abuse is related to euphoriant actions (CNS Abuse is related to euphoriant actions (CNS action)action)
2 main groupings2 main groupings visual illusions-dream like statesvisual illusions-dream like states clarity of thought and alleviation of clarity of thought and alleviation of
psychological painpsychological pain
Abuse PotentialAbuse Potential
Trance-like state - visual illusionsTrance-like state - visual illusions dream-like images - great deal of claritydream-like images - great deal of clarity doesn't influence sensory inputdoesn't influence sensory input the only perceptual effect is on painthe only perceptual effect is on pain
can alleviate physical paincan alleviate physical pain can alleviate psychological paincan alleviate psychological pain
strong emotionally pleasant feelingsstrong emotionally pleasant feelings
Side EffectsSide Effects
vomitingvomiting very common with first dosevery common with first dose chance-may be due to effect on the chance-may be due to effect on the
vestibular apparatusvestibular apparatus respiratory depressionrespiratory depression
decrease sensitivity to COdecrease sensitivity to CO22
occurs at low doses-those common for occurs at low doses-those common for analgesiaanalgesia
increase dose-increase depressionincrease dose-increase depression most common cause of death in overdosemost common cause of death in overdose
Side EffectsSide Effects
Body temperatureBody temperature resetting of body temperature thermostatresetting of body temperature thermostat
with limited use-lowers temperature by about 1 with limited use-lowers temperature by about 1 degreedegree can persist for a monthscan persist for a months
Sex hormonesSex hormones inhibitedinhibited
males-decreased testosterone levels-males-decreased testosterone levels-decreased sex drivedecreased sex drive
females-decreased estrogen females-decreased estrogen
Side EffectsSide Effects
Cardiovascular effectsCardiovascular effects increased skin blood flow-gives them a warm increased skin blood flow-gives them a warm
feelingfeeling blood pressure decrease upon standing -faintblood pressure decrease upon standing -faint
Pinpoint pupilsPinpoint pupils signs of overdosesigns of overdose seizuresseizures
Catatonia (only at very high doses)Catatonia (only at very high doses)
RECEPTOR TYPES MEDIATING RECEPTOR TYPES MEDIATING OPIOID EFFECTS OPIOID EFFECTS
11
spinal & supraspinal analgesiaspinal & supraspinal analgesia
22
respiratory depressionrespiratory depression GI motilityGI motility nauseanausea euphoriaeuphoria physical dependence (withdrawal symptoms)physical dependence (withdrawal symptoms) pupillary contractionpupillary contraction
RECEPTOR TYPES MEDIATING RECEPTOR TYPES MEDIATING OPIOID EFFECTS OPIOID EFFECTS
(kappa)(kappa)
spinal & supraspinal analgesiaspinal & supraspinal analgesia sedationsedation pupil contractionpupil contraction dysphoria, psychotomimetic dysphoria, psychotomimetic
(delta)(delta)
spinal & supraspinal analgesiaspinal & supraspinal analgesia positive reinforcing effectspositive reinforcing effects modulate activity of modulate activity of receptors receptors
Receptor LocationReceptor Location
receptors - pain modulating regions of receptors - pain modulating regions of brainbrain dorsal horn of spinal corddorsal horn of spinal cord brain stembrain stem PAGPAG thalamusthalamus hypothalamushypothalamus striatumstriatum
Receptor LocationReceptor Location
receptors - broad distributionreceptors - broad distribution deep layers of cerebral cortexdeep layers of cerebral cortex limbic systemlimbic system hypothalamus hypothalamus
receptors - emotional response regions receptors - emotional response regions of brainof brain limbic system (amygdala)limbic system (amygdala) frontal cortexfrontal cortex nucleus accumbensnucleus accumbens
Receptor LocationReceptor Location
opioid induced euphoria not well understoodopioid induced euphoria not well understood seems to involve seems to involve 22 receptors & also receptors & also definitely not definitely not
opioids act as modulators and inhibit release of opioids act as modulators and inhibit release of excitatory amino acid neurotransmittersexcitatory amino acid neurotransmitters all act via second messenger systemsall act via second messenger systems found on presynaptic nerve terminalsfound on presynaptic nerve terminals also found to serve as cotransmitters (released with also found to serve as cotransmitters (released with
NE NE
Tolerance & DependenceTolerance & Dependence
develop with repeated usedevelop with repeated use More rapidly and to greater degree as potency More rapidly and to greater degree as potency
increasesincreases Heroin & methadone develop different patterns Heroin & methadone develop different patterns
for withdrawalfor withdrawal Heroin withdrawal begins 4-5 hrs after last doseHeroin withdrawal begins 4-5 hrs after last dose
strong flu like symptomsstrong flu like symptoms greatest magnitude of symptoms between 24-72 hrsgreatest magnitude of symptoms between 24-72 hrs pretty much done in a couple of weekspretty much done in a couple of weeks
Tolerance & DependenceTolerance & Dependence
Methadone withdrawal 24-48 hrs after last doseMethadone withdrawal 24-48 hrs after last dose withdrawal symptoms reported to be less intensewithdrawal symptoms reported to be less intense however, much greater durationhowever, much greater duration can take months to clear all withdrawal symptomscan take months to clear all withdrawal symptoms
Methadone admin subcu for analgesiaMethadone admin subcu for analgesia Same potency as morphine, half potency as heroinSame potency as morphine, half potency as heroin
More effective orally than bothMore effective orally than both Suppresses opiate withdrawalsSuppresses opiate withdrawals actions 3 to 4 time longer than morphineactions 3 to 4 time longer than morphine
Tolerance & DependenceTolerance & Dependence
Why do we pay for people to be maintained on Why do we pay for people to be maintained on methadone?methadone?
1) effective orally - limits needle use1) effective orally - limits needle use
2) long duration action2) long duration action
3) effective dose remains stable3) effective dose remains stable
4) cheap4) cheap
5) does not produce euphoria as well 5) does not produce euphoria as well actually blocks to heroinactually blocks to heroin
6) prevents opiate withdrawal6) prevents opiate withdrawal
TreatmentTreatment
Therapeutic groups (Synanon & Daylop)Therapeutic groups (Synanon & Daylop) In West Berlin- 15% abstained compared to 4%In West Berlin- 15% abstained compared to 4%
Elimin of cond craving (to drug related stim) through Elimin of cond craving (to drug related stim) through extinction & class condextinction & class cond
Mostly blocking narcotic effectsMostly blocking narcotic effects Antagonist break up drug taking from reinforcementAntagonist break up drug taking from reinforcement Naloxone (NarcanNaloxone (Narcan77)-not too effective)-not too effective Naltrexen (TrexenNaltrexen (Trexen77 or ReVia or ReVia77) block up to 3 days) block up to 3 days What may be a problem with antagonist?What may be a problem with antagonist?
TreatmentTreatment
Substituting narcotics w/less disruptive Substituting narcotics w/less disruptive (Methadone)(Methadone) Developed by Nazis in WWIIDeveloped by Nazis in WWII
Dole and Nyswander (1976)—narcotic addicitionsDole and Nyswander (1976)—narcotic addicitions
Gave large levels of methadoneGave large levels of methadone Despite addiction went back to school, got jobs Despite addiction went back to school, got jobs
etc.,etc.,
TreatmentTreatment
Withdrawal symptoms in addicts with Withdrawal symptoms in addicts with naloxone adminnaloxone admin
Administer both heroin & naloxone Administer both heroin & naloxone repeatedly togetherrepeatedly together no tolerance or dependence developsno tolerance or dependence develops interesting way to see what receptor type interesting way to see what receptor type
mediates what responsesmediates what responses