1. Chapter 13 Opioids

2. General Classifications • A family of drugs which cause: • Sleep • Stuporous state • Analgesic action • Origins: • Natural • Synthetic

3. Narcotics Are… • The term narcotic currently refers to naturally occurring substances derived from the opium poppy and their synthetic substitutes. • These drugs are referred to as the opioid (or opiate) narcotics because of their association with opium.

4. Narcotics Are… • For the most part, the opioid narcotics possess abuse potential, but they also have important clinical value (analgesic, antitussive). • The term narcotic has been used to label many substances, from opium to marijuana to cocaine.

5. Natural Opiates • Opium, Morphine, Codeine, Thebaine OPIUM CODEINE MORPHINE THEBAINE

6. Semisynthetic Narcotics • Heroin, Hydromorphone, Thebaine deriviatives, Etorphine • Produced by modifying the chemical compounds of natural substances • Morphine heroin and hydromorphone • Thebaine thebaine deriviatives and etorphine

7. Synthetic Narcotics • Meperidine • Methadone • LAAM • Propoxyphene • Fentanyl

8. Endogenous Opioids • Endorphins • Enkephalins • Dynorphins

9. History • From an annual plant • Egyptian and Greek cultures • India and China • Opioids dependence • Writers and Opium • Opium Wars • Started by outside incidents • Britain given the island of Hong Kong for winning

10. Narcotics & the Law • 1906 Federal Food & Drug Act • Prohibits interstate commerce of misbranded drugs • Must list ALL narcotic ingredients • Must list purity of the drug • 1914 Harrison Narcotics Act • Established governmental narcotics control • Outlawed nonmedical use of heroin • Permitted prescription of narcotics • Mistakenly classified cocaine as a narcotic • Eventually forbade dispensing of narcotics to known addicts

11. Production of Narcotics • 1924 – importation of heroin outlawed • 1942 – cultivation of opium banned • 1935 & 1938 – hospital farms for drug treatment • 1970 – Comprehensive Drug Abuse Prevention and Control Act • Consolidated drug laws & became legal foundation for reducing illegal drug use • Created the Controlled Substances Act • Psychoactive drugs other than alcohol, nicotine, and caffeine were categorized into 5 Schedules • Presumed potential for abuse • Current acceptability in medical practice

12. Side Effects • The principle side effects of the opioid narcotics, besides their abuse potential, include: • Drowsiness • Respiratory depression • Nausea, vomiting, and constipation • Inability to urinate • Drop in blood pressure

13. Pharmacological Effects • The most common clinical use of the opioid narcotics is as analgesics to relieve pain. • The opioid narcotics relieve pain by activating the same group of receptors that are controlled by the endogenous substances called endorphins. • Activation of opioid receptors blocks the transmission of pain through the spinal cord or brain stem.

14. Pharmacological Effects • Morphine is a particularly potent pain reliever and is often used as the analgesic standard by which other narcotics are compared. • With continual use, tolerance to the analgesic effects of morphine and other narcotics develops. • Physicians frequently under-prescribe narcotics, because of fear of causing narcotic addiction.

15. What Are The Effects? • Pain Relief • Reduce fears & anxiety • Induce sleep if used alone • Heavy use will cause dependence, tolerance, addiction, withdrawal symptoms • CNS depression without loss of motor control, coordination, or speech • Adverse effects – irregular breathing, euphoria, pupil constriction, cloud mental function

16. Abuse, Tolerance, Dependence, and Withdrawal • All the opioid narcotic agents that activate opioid receptors have abuse potential and are classified as schedule drugs. • Tolerance begins with the first dose of a narcotic, but does not become clinically evident until 2 to 3 weeks of frequent use.

17. Abuse, Tolerance, Dependence, and Withdrawal • Tolerance occurs most rapidly with high doses given in short intervals • Doses can be increased as much as 35 times in order to regain the narcotic effect • Physical dependence invariably accompanies severe tolerance • Psychological dependence can also develop with continual narcotic use

18. Morphine • 1806 morphine was discovered • 10 times as potent as opium • Hypodermic syringe and war time medicine • “Soldier’s disease”

19. Heroin • Heroin is classified as a Schedule I drug • Heroin is the most widely abused illegal drug in European and Far Eastern countries • Until 15 years ago, Heroin was illicitly used more than any other drug of abuse in the U.S. (except for marijuana) • What was it replaced by? • Cocaine

20. HEROIN • Most widely abused opioid – 90% • 300,000 occaisional/800,000 chronic • Over the past 5 yrs. – huge comeback WHY • Initially injected, now more commonly snorted • Media promotion

21. Methods of Administration • Sniffing the powder • Injecting it into a muscle (intramuscular) • Smoked • Mainlining (intravenous injection)

22. Facts on Heroin • Initially thought of having fewer side effects than morphine (medical use), but unaware of high dependencey rate • Illegal for possession – felony offense • Research is being done on effects on cancer tx patients – could move drug to Schedule II

23. Characteristics • Duration of effects : 3 – 6 hours • High Physical dependence • Potency of the drug has increased from 40% to 80% • “China White” – 90% pure • Threat of HIV and AIDS reduced due to smoking or snorting of the drug • Often combined with • Cocaine • Marijuana

24. Rush Quick binding to opioid receptors in the brain Effect on the limbic system CNS depressant can cause death Dependency Rapid development of: psychological and physical dependence Withdrawal symptoms occur about 8 hrs. after last dose taken – symptoms can last as long as 7 – 30 days Continued use due to fear of withdrawal Fetus effects Other Aspects

25. Heroin Addicts And AIDS • Over 50% of IV heroin users have been exposed to the AIDS virus

26. Withdrawal Symptoms • A single “shot” of heroin lasts 4 to 6 hours • After the effects of the heroin wear off, the addict has only a few hours in which to find the next dose before severe withdrawal symptoms begin • Withdrawal symptoms: • runny nose, tears, • minor stomach cramps, loss of appetite, vomiting, diarrhea, abdominal cramps, • chills, fever, aching bones, and muscle spasms

27. Treatment • Methadone • frequently used to help narcotic addicts • Oral methadone relieves the withdrawal symptoms • Can cause psychological and physical dependence

28. Morphine Methadone Fentanyl Hydromorphone Meperidine MPTP Codeine Pentazocine Propoxyphene Other Narcotics