Chapter 13 Opioids

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.

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.

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

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

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.

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.

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.

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

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

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

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

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

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

Treatment Methadone, LAAM or buprenorphine are frequently used to help narcotic addicts Oral methadone relieves the withdrawal symptoms Methadone can cause psychological and physical dependence Buprenorphine

Other Narcotics Morphine Methadone Fentanyl Hydromorphone Meperidine MPTP Codeine Pentazocine Propoxyphene