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(c) McGraw-Hill 2011

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  • Image sources (injection): Royalty-Free/CORBIS (Image Ch13_21InjectArm) Image source (morphine bottle, patent medicine label): National Library of Medicine (Images Ch13_11MorphineBottle, Ch13_15SoothingSyrupMorphine)
  • Image source: US Drug Enforcement Administration (Image Ch13_01OpiumPoppy)
  • Image source (poppy field): Central Intelligence Agency (Ch13_02OpiumField) Image source (poppy pod): US Drug Enforcement Administration (Ch13_03DryOpiumPoppy)
  • Image source (scoring opium seedpod): Central Intelligence Agency (Image Ch13_04ScoringPod) Image source (seed pod): National Institutes of Health (Image Ch13_05OpiumPod) Image source (raw opium): Drug Enforcement Administration (Image Ch13_06RawOpium)
  • Image source: National Library of Medicine (Image Ch13_07OpiumPlantDrawing)
  • Image source: National Library of Medicine (Image Ch13_08DeQuinceyPage) Image source: National Library of Medicine (Image Ch13_09LaudanumBottle)
  • Image source: Library of Congress Prints and Photographs Division (Image Ch13_10OpiumWar)
  • Image source: National Library of Medicine (Image Ch13_11MorphineBottle)
  • Image source: TRBfoto/Getty Images (Image Ch13_12Syringe)
  • Image source (opium den): Library of Congress Prints and Photographs Division (Image Ch13_13OpiumDen) Image source (smoking): World Health Organization/National Library of Medicine (Image Ch13_14OpiumSmoking)
  • Image source: National Library of Medicine (Image Ch13_15SoothingSyrupMorphine)
  • Image source: Medio Images/PictureQuest (Image Ch13_16InjectArm2)
  • Image source: Central Intelligence Agency (Image Ch13_17BlackTarHeroin)
  • Image source: US Drug Enforcement Agency (Image Ch13_18Oxycontin)
  • Figure 13.1 from text
  • Image source: US Drug Enforcement Agency (Image Ch13_19HeroinPowder)
  • Image source: US Food and Drug Administration (Image Ch13_20Paregoric)
  • Image source: Royalty-Free/CORBIS (Image Ch13_21InjectArm1)
  • Naloxone figure from box, p. 315
  • Image source: Creatas/PunchStock (Image Ch13_25DiscardedNeedles)
  • Image sources (injection): Royalty-Free/CORBIS (Image Ch13_21InjectArm) Image source (morphine bottle, patent medicine label): National Library of Medicine (Images Ch13_11MorphineBottle, Ch13_15SoothingSyrupMorphine)

Hart13 ppt ch13 Hart13 ppt ch13 Presentation Transcript

  • Chapter 13 Opioids© 2011 McGraw-Hill Higher Education. All rights reserved.
  • Opioids  Naturally occurring substances derived from the opium poppy have a 6,000-year history of medical use  Opioids relieve pain and suffering and have other medicinal uses  Opioids deliver pleasure and relief from anxiety, so they also have a long history of recreational use© 2011 McGraw-Hill Higher Education. All rights reserved.
  • Cultivation of Opium  Papaver somniferum is an annual flowering plant that grows 3-4 feet high  Most likely origin is the Middle East© 2011 McGraw-Hill Higher Education. All rights reserved.
  • Cultivation of Opium  Opium is produced and available for collection for only a few days of the plant’s life  Opium harvesters use a sharp, clawed tool to make shallow cuts into the unripe seedpods  The resinous substance that oozes from the cuts is scraped and collected  Raw opium is the substance from which morphine is extracted and then heroin is derived© 2011 McGraw-Hill Higher Education. All rights reserved.
  • History of Opium  Egypt  Papyrus (circa 1500 BC) described specific medical uses  Greece and Rome  Had an important role in Greek medicines  Arabic world  Opium used as a social drug  Use spread to India and China through trade  Arab physicians wrote widely about use of opium preparations  Europe  Opium used widely beginning in the sixteenth century  Physicians developed a preparation called laudanum, a combination of strained opium and other ingredients© 2011 McGraw-Hill Higher Education. All rights reserved.
  • History: Writers and Opium  Writer Thomas De Quincey drank laudanum and wrote a widely read book (1823) about life as an “opium eater”  Other authors who used laudanum included Elizabeth Barrett Browning and Samuel Taylor Coleridge© 2011 McGraw-Hill Higher Education. All rights reserved.
  • History: Opium Wars  1729: Opium smoking outlawed in China, but smuggling was widespread  British East India Company was involved in opium trade, legally in India and illicitly (but indirectly) in China  Pressure grew and eventually war broke out between the British and Chinese© 2011 McGraw-Hill Higher Education. All rights reserved.
  • Morphine  1806: Active ingredient in opium isolated  10 times as potent as opium  Named morphium after Morpheus, the god of dreams  1832: Another alkaloid of opium discovered  Named codeine from the Greek word for “poppy head”© 2011 McGraw-Hill Higher Education. All rights reserved.
  • Morphine  Medically useful characteristics  Clinically useful  Pure chemical  Known potency  Use spread due to two developments  1853: Hypodermic syringe allowed delivery of morphine directly into the blood  Widespread use during war provided relief from pain and dysentery  Many veterans were dependent on morphine, and dependence was later called “soldier’s disease” or “army disease”© 2011 McGraw-Hill Higher Education. All rights reserved.
  • Heroin  Two acetyl groups added to morphine in the laboratory, creating diacetylmorphine  Given the brand name Heroin  Placed on the market in 1898 by Bayer  Three times as potent as morphine due to increased lipid solubility of the heroin molecule  Acts like morphine except that it is more potent and acts more quickly  Marketed as a non-habit-forming substitute for codeine  Later linked to tolerance and dependence© 2011 McGraw-Hill Higher Education. All rights reserved.
  • History of Opioids: Patterns of Abuse  Three types of opioid dependence developed in the U.S. in the second half of the 19th century  Oral intake increased as patent medicines spread  Opium smoking increased after 1850, as Chinese laborers arrived in the U.S.  Injection of morphine—the most dangerous form of use  Number and proportion of Americans dependent on opioids peaked at the start of the 20th century  Possibly as high as 1 percent of the population© 2011 McGraw-Hill Higher Education. All rights reserved.
  • History of Opioids: Patterns of Abuse  Initially, opioid dependence was not viewed as a major social problem  Opium smoking was limited to certain groups  Patent medicines were socially acceptable  Opioid dependence was viewed as a “vice of middle life”  Typical user was a 30-to-50-year-old middle class white woman, wife, and mother  Drugs purchased legally in patent medicines  High drugs levels in patent medicines meant that withdrawal symptoms were severe and relieved only by taking more© 2011 McGraw-Hill Higher Education. All rights reserved.
  • History of Opioids: Patterns of Abuse  Supreme Court decisions about enforcement of the 1914 Harrison Act made opioids difficult to obtain  Result: Changes in the pattern of opioid use  Oral use declined; the primary remaining group of users were those who injected morphine or heroine  Only sources of drugs were illegal dealers  Cost and risk of use increased, so the most potent method (intravenous injection) was favored  Addicts were looked upon as weak and self-indulgent rather than as victims© 2011 McGraw-Hill Higher Education. All rights reserved.
  • History of Opioids: Patterns of Abuse  After the 1914 Harrison Act  Oral use among the white middle class declined  Use between World War I and World War II was limited to particular social groups  After World War II, use of heroin increased in low-income areas of large cities  The 1960s  Regular and irregular heroin use increased in large cities  Heroin use was associated with crime and considered socially unacceptable© 2011 McGraw-Hill Higher Education. All rights reserved.
  • History of Opioids: Patterns of Abuse  Heroin use by American troops in Vietnam  Rate of use = about 5 percent  Heroin was  Inexpensive  About 95 percent pure (compared to 5 percent in the U.S.)  Easy to obtain  Most users smoked or sniffed the drug  Most users stopped when they returned to the U.S.  Vietnam experience showed  Under certain conditions, a relatively high percent of individuals will use opioids recreationally  Opioid dependence and compulsive use are not inevitable among occasional users© 2011 McGraw-Hill Higher Education. All rights reserved.
  • History of Opioids: Patterns of Abuse  Production and Purity  Efforts made to lower the number of heroin users  End of the “French connection” in the early 1970s: heroin grown in Turkey, converted to heroin in southern France, and imported into the U.S.  By 1975, most U.S. heroin came from Mexico  Opium processed into morphine by a different process, resulting in pure heroin with a brown or black color, so-called Mexican brown or black tar heroin© 2011 McGraw-Hill Higher Education. All rights reserved.
  • History of Opioids: Patterns of Abuse  Today  Heroin used in U.S. is currently produced mostly in South America, Mexico, and Southeast Asia  Purity of heroin from South America is higher than heroin from Mexico  Average purity of street heroin has increased from about 5 percent to 25 percent since the 1970s  In 2008, the estimated retail purity for Mexican heroin was 40% and 57% for South American Heroin.© 2011 McGraw-Hill Higher Education. All rights reserved.
  • Opioids: Current Patterns of Abuse  Heroin: 0.2 percent of Americans report past-year use  Recent deaths of celebrities, like Michael Jackson and Heath Ledger has reignited concerns about Physicians over prescribing opiod pain medications  Prescription pain relievers (nonmedical use): 5 percent of Americans report past-year use  Most are taken orally  Dependence and toxicity can occur from misuse of prescription opioids  The most popular types are hydrocodone and OxyContin© 2011 McGraw-Hill Higher Education. All rights reserved.
  • Pharmacology: Chemical Characteristics  Raw opium is about 10 percent morphine by weight, and a smaller amount of codeine  With the added acetyl groups, heroin can pass through the blood-brain barrier faster, making heroin more potent than morphine  Researchers searching (unsuccessfully) for ways to separate the analgesic and dependence-producing effects of opioids have developed a variety of prescription pain killers© 2011 McGraw-Hill Higher Education. All rights reserved.
  • Pharmacology: Chemical Characteristics Narcotic agents isolated or derived from opium© 2011 McGraw-Hill Higher Education. All rights reserved.
  • Prescription Narcotic Analgesics  Natural products  Synthetics  Morphine  Methadone  Codeine  Meperidine  Semisynthetics  Oxycodone  Heroin  Oxymorphone  Diamorph (unavailable in U.S.)  Hydrocodone  Hydromorphone  Dihydrocodeine  Propoxyphene  Pentazocine  Fentanyl© 2011 McGraw-Hill Higher Education. All rights reserved.
  • Pharmacology: Chemical Characteristics  Opioid antagonists = drugs that block the action of opioids  Examples: Naloxone (Narcan) and nalorphine  Effects:  Reverse depressed respiration from opioid overdose  Precipitate withdrawal syndrome  Prevent dependent individuals from experiencing a high from subsequent opioid use© 2011 McGraw-Hill Higher Education. All rights reserved.
  • Pharmacology: Mechanism of Action  Opioids act on selective receptors in the brain  Naturally occurring opioid-like products of the nervous system and endocrine glands activate brain opioid receptors  Enkephalins: morphinelike neurotransmitters found in the brain and adrenals  Endorphins: morphinelike neurotransmitters found in the brain and pituitary gland  Natural and synthetic opioid drugs as well endogenous opioids act on multiple types of opioid receptors in the brain© 2011 McGraw-Hill Higher Education. All rights reserved.
  • Medical Uses  Pain relief  Reduces the emotional response to pain and diminishes the patient’s awareness of, and response to, the aversive stimulus  Typically causes drowsiness but does not induce sleep  Treatment of intestinal disorders  Reduces colic and counteracts diarrhea and the resulting dehydration  Acts by decreasing the number of peristaltic contractions  An opium solution known as paregoric is still available for relief of diarrhea© 2011 McGraw-Hill Higher Education. All rights reserved.
  • Medical Uses  Cough suppressant  Codeine has long been used to reduce coughing  It remains available in prescription cough medications  Nonprescription cough remedies contain the opioid analogue dextromethorphan  It produces hallucinogenic effects at high doses© 2011 McGraw-Hill Higher Education. All rights reserved.
  • Dependence Potential  Tolerance  Tolerance develops to most effects from both medical and recreational usage  Higher doses needed to maintain effects  Cross-tolerance exists among all the opioids  Psychological processes play a key role in tolerance  Dependent individuals develop a conditioned reflex response to the stimuli associated with taking the drugs© 2011 McGraw-Hill Higher Education. All rights reserved.
  • Dependence Potential  Physical dependence  Symptoms of withdrawal appear in sequence following the timing of the most recent dose and the individual’s history of use  Opioid withdrawal is unpleasant but rarely life- threatening  Methadone (long-lasting synthetic opioid) produces withdrawal symptoms that appear later and are less severe than those from heroin© 2011 McGraw-Hill Higher Education. All rights reserved.
  • Withdrawal Syndrome Symptoms Approximate hours after previous dose Signs Heroin or Methadone Morphine Craving for drugs, anxiety 6 24 Yawning, perspiration, running nose, teary eyes 14 34-48 Increase in above signs plus pupil dilation, goose bumps, tremors, hot and cold flashes, aching bones and 16 48-72 muscles, loss of appetite Increased intensity of above, plus insomnia; raised blood pressure; increased temperature, pulse rate, respiratory 24-36 rate and depth; restlessness; nausea Increased intensity of above, plus curled-up position, vomiting, diarrhea, weight loss, spontaneous ejaculation 36-48 or orgasm, hemoconcentration, increased blood sugar© 2011 McGraw-Hill Higher Education. All rights reserved.
  • Dependence Potential  Psychological dependence  Positive reinforcement  Positive effects reliably follow use of the drug  Negative reinforcement  Use of the drug removes withdrawal symptoms  Fast-acting injectable opioids are most likely to lead to dependence© 2011 McGraw-Hill Higher Education. All rights reserved.
  • Toxicity Potential  Acute toxicity  Opioids depress respiratory centers in the brain  Breathing becomes slower and shallower  Effects with alcohol are additive  Opioid overdose triad  Coma  Depressed respiration  Pinpoint pupils  Clouding of consciousness  Occasionally, nausea and vomiting  Can be counteracted with naloxone© 2011 McGraw-Hill Higher Education. All rights reserved.
  • Toxicity Potential  Chronic toxicity is associated with injection method of use  Infections and the spread of blood-borne diseases© 2011 McGraw-Hill Higher Education. All rights reserved.
  • Life of a Heroin User  Three to four injections needed daily to prevent withdrawal  Expensive habit (cost of drugs and paraphernalia)  Risk of overdose due to variable potency of different batches  Health problems associated with injection habit  Skin infections  Blood-borne infections  Masking of early symptoms of illness  Some users “mature out”© 2011 McGraw-Hill Higher Education. All rights reserved.
  • Misconceptions and Preconceptions  Not all users experience euphoria from initial dose  Tolerance to negative effects may develop more rapidly than tolerance to positive effects  Withdrawal is often similar to a mild case of the intestinal flu  People usually don’t become dependent after one dose  Current users:  Probably about one million opioid-dependent Americans and two to three times that many heroin chippers (occasional users)© 2011 McGraw-Hill Higher Education. All rights reserved.
  • Chapter 13 Opioids© 2011 McGraw-Hill Higher Education. All rights reserved.