OpiatesOpiates

NarcoticsNarcotics

A drug that in therapeutic doses A drug that in therapeutic doses diminishes sensibility, relieves pain, diminishes sensibility, relieves pain, and produces sleep, but in large and produces sleep, but in large doses causes stupor, coma or doses causes stupor, coma or convulsions; any drug with properties convulsions; any drug with properties similar to morphine, identified as a similar to morphine, identified as a narcotic drug by federal law.narcotic drug by federal law.

Gould’s Medical dictionaryGould’s Medical dictionary

SourceSource

Opium poppyOpium poppy Papaver somniferum LPapaver somniferum L Papaver – Greek for poppyPapaver – Greek for poppy Somniferum – Latin – to dream or Somniferum – Latin – to dream or

sleepsleep Grows in India, Turkey, China, Grows in India, Turkey, China,

Mexico, SW Asia, Afghanistan Mexico, SW Asia, Afghanistan

HarvestHarvest

Petals fall from the opium seed podPetals fall from the opium seed pod Approximately two weeks later Approximately two weeks later

unripe pods are incisedunripe pods are incised Opium oozes out and dries in about Opium oozes out and dries in about

24 hours24 hours Then collected by handThen collected by hand

YieldsYields

Four kilos of opium per acreFour kilos of opium per acre 80 mgs per plant80 mgs per plant 10 kilos of opium yield about 1 kilo of 10 kilos of opium yield about 1 kilo of

morphine and morphine to heroin is morphine and morphine to heroin is a 1 to 1 conversiona 1 to 1 conversion

Opium derivativesOpium derivatives

OpiumOpium MorphineMorphine CodeineCodeine ThebaineThebaine

Semi – Synthetic DerivativesSemi – Synthetic Derivatives

Heroin – diacetylmorphineHeroin – diacetylmorphine Eythylmorphine –DionineEythylmorphine –Dionine Dihydrocodeine – ParacodinDihydrocodeine – Paracodin Hydromorpone – DilaudidHydromorpone – Dilaudid Dihydrocodeinone – KycodanDihydrocodeinone – Kycodan Oxycodone - PercodanOxycodone - Percodan

SyntheticsSynthetics

Meperidine – DemorolMeperidine – Demorol Methadone – Methadon, DolophineMethadone – Methadon, Dolophine

Earliest recorded use of opiates, circa Earliest recorded use of opiates, circa 1500 BC in the Ebers papyrus1500 BC in the Ebers papyrus

Pharmacology book (Biruni 1000 AD) Pharmacology book (Biruni 1000 AD) describing opiate dependencedescribing opiate dependence

Early 16Early 16thth century, Paracelsus century, Paracelsus created laudanum, a mixture of wine created laudanum, a mixture of wine and opiumand opium

Dr. Thomas Sydenham (The English Dr. Thomas Sydenham (The English Hippocrates) modified laudanum mixture, Hippocrates) modified laudanum mixture, John Bell HoodJohn Bell Hood

Morphine was isolated by Frederich Serturner Morphine was isolated by Frederich Serturner in 1806in 1806

Codeine (poppy head) was isolated in 1832Codeine (poppy head) was isolated in 1832 English developed trade with China in the English developed trade with China in the

1919thth century through the East India Company century through the East India Company

English developed trade with China in the English developed trade with China in the 1919thth century through the East India century through the East India CompanyCompany

China had the problem of increasing China had the problem of increasing opium addiction and banned the opium addiction and banned the importation of opiumimportation of opium

This lead to the Opium War in 1840 to This lead to the Opium War in 1840 to 1842 in which England took control of 1842 in which England took control of Hong Kong Hong Kong

1853 the hypodermic needle was 1853 the hypodermic needle was inventedinvented

U. S. Civil War lead to the “Soldier’s U. S. Civil War lead to the “Soldier’s Disease”Disease”

Heroin was transformed in 1874, Heroin was transformed in 1874, thought to be 3X more powerful than thought to be 3X more powerful than morphinemorphine

Influx of Chinese laborers caused an Influx of Chinese laborers caused an increase in opium smokingincrease in opium smoking

1890 Heroin was marketed by the 1890 Heroin was marketed by the Germans, may be derived from the Germans, may be derived from the German heroisch meaning heroic, German heroisch meaning heroic, dynamic or powerfuldynamic or powerful

Opiate abuse developed in the mid-Opiate abuse developed in the mid-1919thth century century

Harrison Act in 1914 (drugs secured Harrison Act in 1914 (drugs secured by a physician)by a physician)

WWII heroin use increased in the WWII heroin use increased in the “lower classes”“lower classes”

1960’s saw an increase in the use of 1960’s saw an increase in the use of heroin as well as other drugsheroin as well as other drugs

Vietnam war created the opportunity Vietnam war created the opportunity for increased use of heroin among for increased use of heroin among U.S. military personnelU.S. military personnel

In the 1970’s “black tar” from Mexico In the 1970’s “black tar” from Mexico became available became available

Current use includes upper – middle Current use includes upper – middle class use with purity of heroin class use with purity of heroin increasing (40 to 60 %)increasing (40 to 60 %)

Effects of Opium DerivativesEffects of Opium Derivatives

Primarily an analgesicPrimarily an analgesic Constricted pupils, DREConstricted pupils, DRE Depressed respirationDepressed respiration ConstipationConstipation NauseaNausea DrowsinessDrowsiness EuphoriaEuphoria

ApathyApathy Decreased sexual driveDecreased sexual drive ToleranceTolerance Physical dependencyPhysical dependency

Dosage form and use Dosage form and use (heroin)(heroin)

White powderWhite powder Brown powderBrown powder Black tar – smokedBlack tar – smoked SnortedSnorted InjectedInjected Skin poppingSkin popping Smoked Smoked

Chemical CharacteristicsChemical Characteristics

Raw opium contains 10% morphine Raw opium contains 10% morphine and small amounts of codeineand small amounts of codeine

Heroin is produced by the addition of Heroin is produced by the addition of 2 acetyl molecules thus producing 2 acetyl molecules thus producing diacetylmorphine diacetylmorphine

Fentanyl (pain reliever) resulted in Fentanyl (pain reliever) resulted in improved anesthesiaimproved anesthesia

Narcotic antagonists (Naloxone) can Narcotic antagonists (Naloxone) can reverse overdosesreverse overdoses

Mechanism of ActionMechanism of Action

Leu-enkephalin and met–enkephhalin Leu-enkephalin and met–enkephhalin act like morphineact like morphine

Endorphins found in brain tissueEndorphins found in brain tissue Midbrain (pain reception site) Midbrain (pain reception site)

interactioninteraction Endorphins are released by the Endorphins are released by the

pituitary and perhaps act in the spinal pituitary and perhaps act in the spinal column but have an unsubstantiated column but have an unsubstantiated effect on the braineffect on the brain

Dependence PotentialDependence Potential

Tolerance develops with narcotic Tolerance develops with narcotic drugsdrugs

Psychological dependencePsychological dependence Behavior reinforcement of needle Behavior reinforcement of needle

usageusage

WithdrawalWithdrawal

Peaks in 24 to 36 hoursPeaks in 24 to 36 hours Lasts 3 to 5 daysLasts 3 to 5 days Tearing of the eyesTearing of the eyes Runny noseRunny nose SweatingSweating Dilated pupilsDilated pupils

Loss of appetiteLoss of appetite Gooseflesh “Cold Turkey”Gooseflesh “Cold Turkey” RestlessnessRestlessness IrritabilityIrritability Tremor, convulsionsTremor, convulsions InsomniaInsomnia

DepressionDepression Nausea and vomitingNausea and vomiting Cramps and diarrheaCramps and diarrhea Muscle spasms – Kicking the habitMuscle spasms – Kicking the habit

Toxicity PotentialToxicity Potential

Acute toxicity effects,Acute toxicity effects, RespirationRespiration Decreased mental abilityDecreased mental ability Nausea/vomitingNausea/vomiting

Chronic ToxicityChronic Toxicity

Sores at injection sitesSores at injection sites HIV/AIDSHIV/AIDS HepatitisHepatitis No long-term change in tissues or No long-term change in tissues or

organsorgans

TreatmentTreatment

Narcotic antagonistsNarcotic antagonists MethadoneMethadone LAAM (L-alpha-acetyl-methadol)LAAM (L-alpha-acetyl-methadol) BuprenorphineBuprenorphine Heroin/morphine maintenanceHeroin/morphine maintenance Rapid opioid detoxificationRapid opioid detoxification Delancy StreetDelancy Street

Questions?Questions?