Narcotics (Opioids) Chapter 9

What Are Narcotics? 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.

What Are Narcotics? Figure 09.T01: Commonly Used Opioid Narcotic Drugs and Products

What Are Narcotics? (continued) Abuse rate for prescribed opioid narcotics has gone from 2.2% to 10% in the past 10 years Although opioid narcotics possess abuse potential, they also have important clinical value (e.g., analgesic, antitussive, antidiarrheal). The term narcotic has been used to label many substances, from opium to marijuana to cocaine.

The History of Narcotics Dates back some 600 years (6000-year-old Sumerian tablet) Used / traded in the historic Egyptian, Greek, and Arab cultures (Greek God of sleep = Hypnos) China and opium trade The Opium War of 1839 (Development of the British Island of Hong Kong) Second war = 1856 American opium use (development of morphine and codeine, and the development of the hypodermic needle) Heroine “heroic” drug was introduced in 1898 as an antitussive.

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 and can also reduce the effects of stress.

Pharmacological Effects (continued) Morphine is a particularly potent pain reliever and often is used as the analgesic standard by which other narcotics are compared. With continual use, tolerance develops to the analgesic effects of morphine and other narcotics. Physicians frequently underprescribe narcotics, for fear of causing narcotic addiction.

Pharmacological Effects (continued) The principle side effects of the opioid narcotics, besides their abuse potential, include: Drowsiness, mental clouding Respiratory depression Nausea, vomiting, and constipation Inability to urinate Drop in blood pressure

Signs, symptoms, and Abuse

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

Abuse of Opioid Narcotics 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 and typically expresses when these drugs are used for more than 2–4 weeks. Psychological dependence can also develop with continual narcotic use. © AbleStock

Guidelines to Avoid Prescribed Opiate Abuse Only use opioid analgesics when pain severity warrants Doses and duration of use should be as conservative as possible Patients should store these medications securely to prevent their theft and misuse Do not share with anyone else Doctors should screen patients for abuse risk before prescribing opioid drugs

Guidelines to Avoid Prescribed Opiate Abuse (continued) Patients should be educated about potential abuse problems prior to being prescribed opioid drugs If significant abuse is suspected, the clinician should discuss concerns with patient to find appropriate steps to stop the abuse

Opioid Side Effects Drowsiness Respiratory depression Nausea/vomiting Inability to urinate Constricted pupils Constipation Physical dependence and withdrawal

Heroin Abuse Heroin is classified as a Schedule I drug. One of the most widely abused illegal drugs in the world; accounts for >$120 billion sales/year Illicitly used more than any other drug of abuse in the United States (except for marijuana) until 20 years ago, when it was replaced by cocaine Some of the recent increases in heroin use likely due to increased abuse of prescription opioid painkillers

Heroin Combinations Pure heroin is a white powder. More than 90% of world’s heroin is from Afghanistan. Heroin is usually “cut” (diluted) with lactose. When heroin first enters the United States, it may be 95% pure; by the time it is sold, it may be 3% to 70% pure. If users are unaware of the variance in purity and do not adjust doses accordingly, results can be fatal.

Heroin Combinations (continued) Heroin has a bitter taste and is often cut (diluted) with quinine, which can be a deadly adulterant. Heroin plus the artificial narcotic fentanyl can be dangerous due to its unexpected potency. Heroin is most frequently used with alcohol. Heroin combined with cocaine is called “speedballing.”

Facts About Heroin Abuse What is the estimated number of heroin addicts in the United States? 600,000 – 1,000,000 What are “shooting galleries”? Locations that serve as gathering places for addicts

Heroin and Crime Factors related to crime: Pharmacological effects encourage antisocial behavior that is crime-related Heroin diminishes inhibition Addicts are often self-centered, impulsive, and governed by need Cost of addiction Similar personality of criminal and addict – begin to engage in crime and heroin use at same time

Patterns of Heroin Abuse Heroin has become purer (60% to 70% purity) and cheaper (~$10/bag). Greater purity leads users to administer heroin in less efficient ways. (smoking and snorting) Many youth believe that heroin can be used safely if not injected.

Patterns of Heroin Abuse (continued) Because of its association with popular fashions and entertainment, heroin has been viewed as glamorous and chic, especially by many young people, although lately this attitude has been changing. Emergency room visits due to narcotic overdoses were over 190,000 in 2009.

Stages of Dependence Initially, the effects of heroin are often unpleasant. Euphoria gradually overcomes the aversive effects. The positive feelings increase with narcotic use, leading to psychological dependence. In addition to psychological dependence, physical dependence occurs with daily use over a 2-week period. If the user abruptly stops taking the drug after physical dependence has developed, severe withdrawal symptoms result. (6-12 hrs)

Methods of Heroin Administration Sniffing the powder Injecting it into a muscle (intramuscular) Smoking Mainlining (intravenous injection)

Heroin Addicts and AIDS More than 250,000 patients in United States contracted AIDS by drug injection, of which most were heroin users. Fear of contracting HIV from IV heroin use has contributed to the increase in smoking or snorting heroin. Many who start by smoking or snorting progress to IV administration due to its more intense effects.

Heroin and Pregnancy Heroin use by a pregnant woman leads to: Physical dependence on heroin in the newborn Withdrawal symptoms after birth in the newborn (Note: similar withdrawal occurs in newborns of any woman who uses significant amounts of opiate drugs during pregnancy, including prescribed opiate painkillers)

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

Withdrawal Symptoms

Treatment Methadone or buprenorphine are frequently used to help narcotic addicts. These drugs block withdrawal symptoms. Treatment should also include regular counseling and other supplemental services such as job training. See also Figure 9.1, p 289 (next slide)

Treatment

Other Narcotics (read in class) Morphine Methadone Fentanyl Hydromorphone Oxycodone (OxyContin) Meperidine Buprenorphine MPTP Codeine Pentazocine Tramadol

Narcotic-Related Drugs Dextromethorphan: OTC antitussive

Narcotic-Related Drugs Clonidine: Relieves some of the opioid withdrawal symptoms Naloxone/Naltrexone: Narcotic antagonist; used for narcotic overdoses -- END OF PRESENTATION --