Heroin and Other Narcotics:

1. Natural Narcotics

The term "narcotic," derived from the Greek word for stupor, originally referred to a variety of substances that dulled the senses and relieved pain. Today, the term is used in a number of ways. Some individuals define narcotics as those substances that bind at opiate receptors (cellular membrane proteins activated by substances like heroin or morphine), while others refer to any illicit substance as a narcotic. In a legal context, narcotic refers to opium, opium derivatives, and their semi-synthetic substitutes. Cocaine and coca leaves, which are also classified as "narcotics" in the Controlled Substances Act (CSA), neither bind at opiate receptors, nor produce morphine-like effects and are discussed in the section on stimulants. For the purposes of this discussion, the term narcotic refers to drugs that produce morphine-like effects.

Picture of a doctor's hypodermic syringe kit, circa 1900.
Doctor's hypodermic syringe kit, circa 1900

Narcotics are used therapeutically to treat pain, suppress cough, alleviate diarrhea, and induce anesthesia. Narcotics are administered in a variety of ways. Some are taken orally, transdermally (skin patches), intranasally, or injected. They are also available in suppositories, and more recently in "troches," a form of narcotics that can be sucked like candy. As drugs of abuse, they are often smoked, sniffed, or injected. Drug effects depend heavily on the dose, route of administration, and previous exposure to the drug. Aside from their medical use, narcotics produce a general sense of well-being by reducing tension, anxiety, and aggression. These effects are helpful in a therapeutic setting but contribute to their abuse.

Narcotic use is associated with a variety of unwanted effects including drowsiness, inability to concentrate, apathy, lessened physical activity, constriction of the pupils, dilation of the subcutaneous blood vessels causing flushing of the face and neck, constipation, nausea, vomiting, and most significantly, respiratory depression. As the dose is increased, the subjective, analgesic (pain relief), and toxic effect become more pronounced. Except in cases of acute intoxication, there is no loss of motor coordination or slurred speech as occurs with many depressants.

Among the hazards of illicit drug use is the ever-increasing risk of infection, disease, and overdose. Medical complications common among narcotic abusers arise primarily from adulterants found in street drugs and in the non-sterile practices of injecting. Skin, lung, and brain abscesses, endocarditis (inflammation of the lining of the heart), hepatitis, and AIDS are commonly found among narcotic abusers. While pharmaceutical products have a known concentration and purity, clandestinely produced street drugs have unknown compositions. Since there is no simple way to determine the purity of a drug that is sold on the street, the effects of illicit narcotic use are unpredictable and can be fatal. Physical signs of narcotic overdose include constricted (pinpoint) pupils, cold clammy skin, confusion, convulsions, severe drowsiness, and respiratory depression (slow or troubled breathing). Most narcotic deaths are a result of respiratory depression.

With repeated use of narcotics, tolerance and dependence develop. The development of tolerance is characterized by a shortened duration and a decreased intensity of analgesia, euphoria, and sedation, which creates the need to consume progressively larger doses to attain the desired effect. Tolerant users can consume doses far in excess of the dose they initially started with.

Chronic narcotic use is associated with physical dependence and a withdrawal or abstinence syndrome when drug use is discontinued. In general, shorter acting narcotics tend to produce shorter, more intense withdrawal symptoms, while longer acting narcotics produce a withdrawal syndrome that is protracted but less severe. Although unpleasant, withdrawal from narcotics is rarely life threatening. The withdrawal symptoms associated with heroin/morphine addiction are usually experienced shortly before the time of the next scheduled dose. Early symptoms include watery eyes, runny nose, yawning, and sweating. Restlessness, irritability, loss of appetite, nausea, tremors, and drug craving appear as the syndrome progresses. Severe depression and vomiting are common. The heart rate and blood pressure are elevated. Chills, alternating with flushing and excessive sweating, are also characteristic symptoms. Pains in the bones and muscles of the back and extremities occur, as do muscle spasms. At any point during this process, a suitable narcotic can be administered to dramatically reverse the withdrawal symptoms. Without intervention, the syndrome will run its course, and most of the overt physical symptoms will disappear within 7 to 10 days.

The psychological dependence associated with narcotic addiction is complex and protracted. Long after the physical need for the drug has passed, the addict may continue to think and talk about the use of drugs and feel strange or overwhelmed coping with daily activities without being under the influence of drugs. There is a high probability that relapse will occur after narcotic withdrawal when neither the physical environment, nor the behavioral motivators that contributed to the abuse have been altered.

There are two major patterns of narcotic abuse or dependence seen in the United States. One involves individuals whose drug use was initiated within the context of medical treatment who escalate their dose by obtaining the drug through fraudulent prescriptions and "doctor shopping" or branching out to illicit drugs. The other pattern of abuse is initiated outside the therapeutic setting with experimental or recreational use of narcotics. The majority of individuals in this category may abuse narcotics sporadically for months or even years. Although they may not become addicts, the social, medical, and legal consequences of their behavior are very serious. Some experimental users will escalate their narcotic use and will eventually become dependent, both physically and psychologically. The younger an individual is when drug use is initiated, the more likely the drug use will progress to dependence and addiction.

Opium

Opium poppy
Opium poppy, Papaver somniferum

The opium poppy plant, Papaver somniferum, is the source for non-synthetic narcotics. It was grown in the Mediterranean region as early as 5000 B.C., and has since been cultivated in a number of countries throughout the world. The milky fluid that seeps from incisions in the unripe seed pod of this poppy has, since ancient times, been scraped by hand and air-dried to produce what is known as opium. A more modern method of harvesting is by the industrial poppy straw process of extracting alkaloids from the mature dried plant. The extract may be in liquid, solid, or powder form, although most poppy straw concentrate available commercially is a fine brownish powder. More than 500 tons of opium or equivalents in poppy straw concentrate are legally imported into the United States annually for legitimate medical use.

There were no legal restrictions on the importation or use of opium until the early 1900s. In the United States, the unrestricted availability of opium, the influx of opium-smoking immigrants from East Asia, and the invention of the hypodermic needle contributed to the more severe variety of compulsive drug abuse seen at the turn of the 20th century. In those days, medicines often contained opium without any warning label. Today, there are state, federal, and international laws governing the production and distribution of narcotic substances.

Although opium is used in the form of paregoric to treat diarrhea, most opium imported into the United States is broken down into its alkaloid constituents. These alkaloids are divided into two distinct chemical classes, phenanthrenes and isoquinolines. The principal phenanthrenes are morphine, codeine, and thebaine, while the isoquinolines have no significant central nervous system effects and are not regulated under the CSA.

Morphine

Morphine is the principal constituent of opium and ranges in concentration from 4 to 21 percent. Commercial opium is standardized to contain 10-percent morphine. In the United States, a small percentage of the morphine obtained from opium is used directly (about 20 tons); the remaining is converted to codeine and other derivatives (about 110 tons). Morphine is one of the most effective drugs known for the relief of severe pain and remains the standard against which new analgesics are measured. Like most narcotics, the use of morphine has increased significantly in recent years. Since 1998, there has been about a two-fold increase in the use of morphine products in the United States.

Morphine is marketed under generic and brand name products including MS-Contin®, Oramorph SR®, MSIR®, Roxanol®, Kadian®, and RMS®. Morphine is used parenterally (by injection) for preoperative sedation, as a supplement to anesthesia, and for analgesia. It is the drug of choice for relieving the pain of myocardial infarction and for its cardiovascular effects in the treatment of acute pulmonary edema. Traditionally, morphine was almost exclusively used by injection. Today, morphine is marketed in a variety of forms, including oral solutions, immediate and sustained-release tablets and capsules, suppositories, and injectable preparations. In addition, the availability of high-concentration morphine preparations (i.e., 20-mg/ml oral solutions, 25-mg/ml injectable solutions, and 200-mg sustained-release tablets) partially reflects the use of this substance for chronic pain management in opiate-tolerant patients.

Codeine

Codeine is the most widely used, naturally occurring narcotic in medical treatment in the world. This alkaloid is found in opium in concentrations ranging from 0.7 to 2.5 percent. However, most codeine used in the United States is produced from morphine. Codeine is also the starting material for the production of two other narcotics, dihydrocodeine and hydrocodone. Codeine is medically prescribed for the relief of moderate pain and cough suppression. Compared to morphine, codeine produces less analgesia, sedation, and respiratory depression, and is usually taken orally. It is made into tablets either alone (Schedule II) or in combination with aspirin or acetaminophen (i.e., Tylenol with Codeine®, Schedule III). As a cough suppressant, codeine is found in a number of liquid preparations (these products are in Schedule V). Codeine is also used to a lesser extent as an injectable solution for the treatment of pain. Codeine products are diverted from legitimate sources and are encountered on the illicit market.

Thebaine

Thebaine, a minor constituent of opium, is controlled in Schedule II of the CSA as well as under international law. Although chemically similar to both morphine and codeine, thebaine produces stimulatory rather than depressant effects. Thebaine is not used therapeutically, but is converted into a variety of substances including oxycodone, oxymorphone, nalbuphine, naloxone, naltrexone, and buprenorphine. The United States ranks first in the world in thebaine utilization.

Drawing of a woman and two children advertising Mrs. Winslow's soothing syrup for children teething.
Opiate-based syrups were once popular for treating children with teething and dysentery.
Source: U.S. Drug Enforcement Administration   Next Page