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Codeine

Codeine

Like morphine, codeine is an alkaloid (a naturally occurring base) of opium, a drug made from the milky juice of unripe seed capsules of the opium poppy plant. The opium poppy was once native to Asia Minor (a large penninsula in western Asia between the Black Sea and the Mediterranean), but it is now grown legally and illegally in many parts of the world. Codeine, morphine, opium, heroin, and other opium alkaloidsthe opioidsmake up the class of drugs known as the narcotic analgesics. Because of their ability to relieve pain, narcotic analgesics have been some of the most important drugs in medicine.

An Ancient Pain Reliever

Opium is believed to have been used by the people of Babylonia (an ancient empire in southwest Asia) in 4000 b.c. as a pain reliever and to promote sleep. The first undisputed (certain) writings about poppy juice were by Greek philosopher Theophrastus in the third century b.c. Highly praised by peoples of many civilizations since that time, opium preparations were given the name laudanum (from the Latin word "laudare," meaning "to praise") by the Swiss physician Paracelsus (1493-1541). Beginning in the late 1600s until the discovery of anesthesia in the mid-1800s, a preparation of alcohol and opium, usually given in whisky or rum, was the drug most widely used to prepare patients for surgery.

Although opioids may be physiologically addicting in high doses, they are widely used. The use of heroin, however, is prohibited in the United States today, even in medicine. The abuse of opioids became worse with the introduction of the hypodermic syringe (needle), which made it easier to use opioids more frequently and in greater amounts. In early times, opium was usually smoked or eaten.

Today only a few opioidsmainly codeine, morphine, and papaverineare useful in medicine. Codeine is the least habit-forming of the opioids. It is used to reduce pain and suppress (lessen) coughing. The amount of codeine that is naturally present in opium is small in relation to the amount of morphine found in opium, but codeine can be synthesized by a chemical change in morphine called methylation. Morphine is the most powerful painkiller available, and papaverine is used as a smooth muscle relaxant.

In the nineteenth century scientists began to separate the active ingredients of opium. This resulted in the isolation (separation) of morphine, codeine, heroin, and other opium alkaloids. When German pharmacist Friedrich Wilhelm Seturner isolated morphine from opium in 1805, a new era in drug production and use began. Soon many other new drugs were obtained by isolating active elements from crude drugs. One of these was codeine, which was discovered and named by Pierre-Jean Robiquet (1780-1840) in 1832. The chemical works of E. Merck, established in 1827 to manufacture morphine, began producing codeine the same year the drug was discovered. Years later, Thomas Anderson (1819-1874), a professor of chemistry at the University of Glasgow, Scotland, described the elemental makeup of codeine.

Cocaine Use Today

Today, codeine is commonly used in prescription drugs in combination with aspirin or acetaminophen to relieve pain, which it does by altering the way the brain reacts to painful sensations. It is also a common ingredient in prescription cough medicines. Codeine depresses the cough reflex by acting on a cough center in the part of the brain known as the medulla. It can be addictive, which is why it is only available by prescription. Many cough suppressants that do not contain codeine are available without a prescription. Codeine and other opioids cause nausea and vomiting in some patients.

Opium, morphine, and codeine are among drugs classified as Schedule II in the U.S. Comprehensive Drug Abuse Prevention and Control Act of 1970. This means they have a high potential for abuse and a severe like-lihood of causing physical or psychological dependence. Because of this, the federal government regulates how they are produced and how they are dispensed by pharmacists. It is illegal to make, sell, or use these drugs in any way that does not follow these governmental rules.

In the 1970s scientists discovered naturally occurring opioids in the brai called enkephalins. Many scientists believe a person becomes addicted to opioids because of a deficiency in these natural substances.

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Codeine

CODEINE

Codeine is a natural product found in the opium poppy (Papaver somniferum ). An alkaloid of Opium, codeine can be separated from the other opium Alkaloids, purified, and used alone as an Analgesic (painkiller). It is however most often used along with mild nonopioid analgesics, such as aspirin, acetominophen, and ibuprofen. These combinations are particularly effective; the presence of the mild analgesics permits far lower codeine doses. Using lower doses of codeine has the advantage of reducing side effects, such as constipation. Codeine is one of the most widely used analgesics for mild to moderate pain.

Structurally, codeine is very similar to Mor-Phine, differing only by the presence of a methoxy (-OCH3) group at position 3, instead of morphine's hydroxy (-OH) group. The major advantage of codeine is its excellent activity when taken by mouth, unlike many opioid analgesics. Codeine itself has very low affinity for opioid receptors, yet it has significant analgesic potency. In the body, it is metabolized into morphine, and it is believed that the morphine generated from codeine is actually the active agent. Codeine has also been widely used as a cough suppressant. Codeine can be abused, and problems of abuse have often been linked to codeine-containing cough medicines, since they were once easily obtained over the counter. Chronic dosing with high codeine doses will produce Tolerance and Physical Dependence, much like morphine.

(See also: Papaver somniferum )

BIBLIOGRAPHY

Reisine, T., & Pasternak, G. (1996) Opioid analgesics and antagonists. In J. G. Hardman et al. (Eds.), The Pharmacological Basis of Therapeutics, 9th ed. (pp. 521-555). New York: McGraw-Hill.

Gavril W. Pasternak

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codeine

codeine (koh-deen) n. an analgesic derived from morphine but less potent as a pain killer and sedative and less toxic. It is administered by mouth or injection to relieve pain and by mouth to suppress coughs and treat diarrhoea. Codeine may also be administered orally in combination with paracetamol (as co-codamol) or aspirin (as co-codaprin) for pain relief.

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codeine

codeine (kō´dēn), alkaloid found in opium. It is a narcotic whose effects, though less potent, resemble those of morphine. An effective cough suppressant, it is mainly used in cough medicines. Like other narcotics, codeine is addictive. See drug addiction and drug abuse.

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codeine

codeine White, crystalline alkaloid extracted from opium by the methylation of morphine, with the properties of weak morphine. It is used in medicine as an analgesic to treat mild to moderate pain, as a cough suppressant and to treat diarrhoea.

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codeine

co·deine / ˈkōˌdēn/ • n. Med. a sleep-inducing and analgesic drug, C18H21N03, derived from morphine.

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codeine

codeine A pain-relieving drug that is derived from the plant Papaver somniferum. See opiate; analgesic.

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codeine

codeine •gradine • sanidine •codeine, Roedean •undine • iodine •Aberdeen, gaberdine •almandine • grenadine • Geraldine •caffeine • Delphine • Josephine •morphine • carrageen • aubergine •indigene • hygiene • phosgene •Eugene • Tolkien • Kathleen •Arlene, Charlene, Darlene, Marlene, praline •Hellene, philhellene •Aileen, Raelene, scalene •spring-clean • crimplene • Abilene •Ghibelline • Cymbeline • terylene •vaseline • acetylene • Mytilene •Eileen • colleen • Pauline •mousseline • Hölderlin • nepheline •Evangeline •Jacqueline, Sakhalin •Emmeline • tourmaline • trampoline •gasoline • naphthalene • Rosaleen •rosaline

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Codeine

Codeine

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Codeine is a type of medication belonging to a class of drugs known as opioid analgesics, which are derived from the Papaver somniferum, a type of poppy flower, or are manufactured to chemically resemble the products of that poppy. In Latin, Papaver refers to any flower of the poppy variety, while somniferum translates to mean maker of sleep. The plant has been used for over 6, 000 years, beginning with the ancient cultures of Egypt, Greece, Rome, and China, to cause sleep. Analgesics are drugs which provide relief from pain. Codeine, an opioid analgesic, decreases pain while causing the user to feel sleepy. At lower doses, codeine is also helpful for stopping a cough.

Although codeine is present in nature within the sticky substance latex, which oozes out of the opium poppys seed pod, it is present in only small concentrations (less than 0.5). However, morphine, another opioid analgesic, is present in greater concentrations (10) within the opium poppys latex, and codeine can be made from morphine via a process known as methylation, which is the primary way that codeine is prepared.

Codeine is a centrally acting drug, meaning that it goes to specific areas of the central nervous system (in the brain and spinal cord) to interfere with the transmission of pain and to change perception of the pain. For example, if you have your wisdom teeth removed and your mouth is feeling very painful, codeine will not go to the hole in your gum where the tooth was pulled and which is now throbbing with pain, but rather will act with the central nervous system to change the way you are perceiving the pain. In fact, if you were given codeine after your tooth was pulled, you might explain its effect by saying that the pain was still there, but it just was not bothering you anymore.

Codeines anti-tussive (cough stopping) effects are also due to its central actions on the brain. It is believed that codeine inhibits an area of the brain known as the medullary cough center.

Codeine is not as potent a drug as is morphine, so it tends to be used for only mild-to-moderate pain, while morphine is useful for more severe pain. An advantage to using codeine is that a significant degree of pain relief can be obtained with oral medication (taken by mouth), rather than by injection. Codeine is sometimes preferred over other opioid analgesics because it has a somewhat lower potential for addiction and abuse than do other drugs in that class.

Scientists are currently trying to learn more about how codeine and other opioid analgesics affect the brain. It is interesting to note that there are certain chemicals (endorphins, enkephalins, and dynorphins) that are made within the brains of mammals, including humans, which closely resemble opioid analgesics. In fact, the mammalian brain itself actually produces tiny amounts of morphine and codeine. Some of these chemicals are produced in the human brain in response to certain behaviors, including exercise. Exploring how and when human brains produce these chemicals could help scientists understand more about ways to control pain with fewer side effects, as well as helping to increase the understanding of addictive substances and behaviors.

See also Narcotic.

Resources

BOOKS

Katzung, Bertram G. Basic & Clinical Pharmacology. Norwalk, CT: Appleton & Lange, 2002.

Marieb, Elaine Nicpon. Human Anatomy & Physiology. 5th ed. San Francisco: Benjamin/Cummings, 2000.

Rosalyn Carson-DeWitt

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Codeine

CODEINE

OFFICIAL NAMES: Codeine, codeine phosphate, codeine sulfate, methylmorphine

STREET NAMES: T–threes, schoolboy, coties, dors and fours, cough syrup, barr (codeine cough syrup), down (codeine cough syrup), karo (codeine cough syrup), lean (codeine cough syrup), nods (codeine cough syrup)

DRUG CLASSIFICATIONS: Schedule II, III, or V, narcotic


OVERVIEW

Codeine is classified as an opiate analgesic. Analgesics are substances that, when ingested or injected, diminish or relieve pain; opiates are drugs that can be derived from opium. Opiates, along with opioids, the broader group to which opiates belong, are the most effective of all analgesics. All opioids are analgesics, but most analgesics are not opioids.

Many different drugs act as analgesics. One method of classifying these drugs is to separate them into two groups—those that require a doctor's prescription and those that do not. Medications that do not require a doctor's prescription are called over-the-counter (OTC) drugs. OTC analgesics include acetaminophen (Tylenol), aspirin, and ibuprofen. Codeine, a prescription analgesic, is one of the most frequently prescribed medications used worldwide to treat pain.

Pain is universal; everyone experiences different kinds of acute (short-term) pain during their life. However, too much pain for too long, (moderate to severe chronic pain), can be harmful, both physically and psychologically. Approximately one-third of all people in the United States experience moderate to severe chronic pain during their life. Half of all individuals who seek medical attention report pain as their primary complaint.

Codeine and other opioid medications are used medically because of their ability to relieve physical pain—in fact, it is the only reason for their medical use as a group. A broader view of opioids reveals that they also can have profound effects on emotional pain—which is perhaps a frequent, if unconscious, reason for their non-medical use/abuse. Physical and emotional pain often have an inseparable connection between them. Even something as simple as stubbing a toe usually elicits a short, but dramatic, emotional response. However, the primary medical use for codeine is only in the treatment of physical pain.

In considering the analgesic effects of opioids such as codeine, it is important to know that the body has two connected systems, one that signals pain and another that responds to it. Both systems have interacting physical and chemical components. The physical portion includes neurons of the central (brain and spinal cord) and peripheral nervous systems. The chemical portion includes substances that aid in the transmission of signals between nerve cells (neurotransmitters), along with chemicals and proteins that have specific roles in normal nerve cell function. The most important group of neurochemicals in the pain killing system is the endogenous opioids. An "endogenous" substance is something that is naturally produced by the body. Endogenous opioids function as the body's own analgesics.

The body's natural painkilling system, then, involves the interaction of endogenous opioids with neurons that transmit and process pain signals. Opioid medications such as codeine mimic the effects of certain endogenous opioids. However, ingested/injected opioids tend to produce much stronger effects than those of the endogenous variety.

Opioid receptors are the cell-surface proteins which all opioids interact with to produce their effects. An opioid, whether endogenous or in drug form, fits into a receptor somewhat like a key in a lock. Opioid attachment activates the receptor and initiates complex changes in the nerve cell. Activated opioid receptors produce chemical changes that reduce the ability of a nerve cell to transmit pain signals. They also decrease the "perception" of pain by neurons in the brain. In the absence of pain, those same chemical changes can produce euphoria. Loosely translated from Greek, euphoria means "good feeling."

Codeine is extracted from opium. Opium is a chemically complex drug derived from a flowering plant, the opium poppy. The scientific name for the opium poppy is Papaver somniferum, which translated from Greek means "poppy that causes sleep." Opium is produced by drying the thick liquid harvested from the unripe seed capsule of the flower. It contains several different medically important chemicals known as "alkaloids" (nonacidic chemicals), the most important being morphine and codeine.

Societies have used the medicinal properties of opium for several thousand years. Even up to the early part of the twentieth century, opium was used as a medicine to treat a large variety of conditions. For some of those conditions, particularly those involving pain and/or diarrhea, it was a highly effective treatment. However, by modern standards, most of opium's historical uses for illness would be considered medically useless or unsound because of the dangers of opium use.

Two of the most important effects of opium are its abilities to relieve pain and produce euphoria. Euphoria is best described as an exaggerated sense of well-being, possibly with mild elation or a sense of calmness. Opium's ability to produce euphoria may be what prompted its use by so many throughout history as a cure-all. After all, while it may not have had the curative effect on a person's illness that was suspected or promised, it usually made them feel better.

Achieving consistent results with opium has always been difficult. Different methods of production and naturally varying concentrations of morphine and codeine produce widely varying results from one batch to the next. Once the chemical methods became available, scientists were eager to isolate the active ingredient(s), hoping to produce a "pure" analgesic.

Morphine was isolated from opium in 1806, which was a significant step in scientific pharmacology. For the first time, a powerful, pain-relieving medicine was available whose effects were predictable. However, it eventually became clear that the addictive potential of morphine is equal to that of opium, with many of the same side effects. Undaunted, scientists began the quest, which is ongoing, for the "perfect" opioid—a drug with the analgesic power of morphine, but with much milder side effects and little or no addictive potential.

Codeine was extracted from opium in 1832, and was the first partial success in the attempt to discover a safer and less addictive drug. However, with fewer side effects came a less potent analgesic. About 100 mg of codeine are needed to produce the same effect as 10 mg of morphine. It was believed at the time (and it is still debated) that codeine's milder effects on a per weight basis actually result in fewer side effects when equally effective dosages are given (i.e., 100 mg of codeine produces fewer side effects than 10 mg of morphine). For the most part, standard medical practice has been to prescribe codeine for moderate pain, and reserve morphine for more severe pain.

Semi-synthetic and synthetic opioids (meperidine, hydrocodone, fentanyl, etc.) are the result of many attempts to produce effective yet safer analgesics. The fact that both morphine and codeine are still widely used indicates that the newer opioids have been only moderately successful. However, current knowledge of the opioid system makes the goal of producing the perfect (or near-perfect) opioid analgesic a more realistic possibility in the future.

Since the middle of the nineteenth century, most social attention to opium has focused on its use as an illicit drug. In fact, in many ways it has come to symbolize the worst aspects of illegal drugs. This negative social stigma has carried over to the derivatives of opium—the opioid drugs. While there is some basis for this perception, it has unfortunately generated undue fear, even within the medical professions, that anyone using an opioid drug, even someone in pain, is at great risk of becoming addicted.

CHEMICAL/ORGANIC COMPOSITION

Opium typically contains between 0.5% and 3.0% codeine by weight. Chemically, codeine is nearly identical in structure to morphine. The only difference between the two is that codeine contains an extra methyl group (two hydrogen atoms bound to a carbon atom) at one end of the molecule. In fact, once absorbed in the body, an enzyme removes the methyl group (demethylation) from codeine to produce morphine. Thus, codeine itself is not an analgesic.

The enzyme responsible for converting codeine to morphine is known as cytochrome P450 2D6, abbreviated CYP2D6. About 8% of people in the Caucasian population, 6% in the black population, and 1% of Asians have a genetic trait that results in a deficiency of CYP2D6. This means that codeine has little or no effect on them. A large number of other genetic variants of the CYP2D6 enzyme result in a wide variation in how well people metabolize codeine.

INGESTION METHODS

Codeine-containing medications are most often taken orally, either in tablet form or as syrup (also called "elixir"). Codeine may also be given by intramuscular (IM) injection. Intravenous codeine administration is not used because of the risk of causing dangerously low blood pressure (hypotension). Codeine suppositories are given rectally, but usually only in infants and children who have had surgery.

It is difficult, but possible, to extract the codeine from tablet and syrup preparations. This is usually done by people who wish to abuse codeine and need higher doses than could be safely taken when it is combined with other medications. Once extracted, the codeine powder is typically mixed with a liquid of some kind and drunk. Since OTC medicines with codeine contain very small amounts of the drug, large quantities must be purchased in order to be able to extract enough codeine to abuse. This can be expensive and cause suspicion in a single pharmacy.

Codeine is not routinely sold in the United States as an individual drug. It is combined instead with one or more other OTC analgesics or cough suppressants into a single compound medication. Codeine is familiar to most people as an ingredient in a series of analgesic preparations in combination with Tylenol-brand acetaminophen. The number after "Tylenol" designates the amount of codeine in each tablet:

  • Tylenol #1 —8 mg codeine (not marketed in the United States)
  • Tylenol #2 —15 mg codeine
  • Tylenol #3 —30 mg codeine
  • Tylenol #4 —60 mg codeine

All combinations contain 300 mg acetaminophen per tablet. Other pharmaceutical companies produce similar preparations that may have slightly different amounts of acetaminophen, but the number designation and codeine quantity stay constant across brands. Some preparations also include up to 30 mg of caffeine to help counteract drowsiness from the codeine.

THERAPEUTIC USE

Codeine is most often used in the treatment of mild to moderate pain that does not respond fully to OTC analgesics. A number of different cough-suppressant (antitussives) medications contain low concentrations of codeine. The effects of codeine on the nerves and muscles of the intestines make it an effective treatment for diarrhea. However, since equally effective OTC medications are available, codeine is now rarely used for this purpose.

For some time, the medical community has debated whether codeine is truly effective in relieving pain and suppressing coughs. Several studies have shown that codeine alone is not significantly more effective than maximum doses of nonprescription analgesics such as acetaminophen or ibuprofen. Most research has shown, however, that codeine added to nonprescription analgesics provides a small but significant benefit. Still, some studies have shown that certain cough medicines are equally effective with or without codeine. More research is needed to resolve this issue.

Even if the physical benefits from codeine were truly minimal, the classification of codeine as a narcotic (implication: "powerful") analgesic might provide a significant placebo effect in some individuals.


USAGE TRENDS

The United States imports about 70% of the world's opium. About 95% of that opium is consumed in the form of schedule III preparations, of which codeine is the most common. Until the mid-1970s, opium had been the main raw material used for the production of morphine and codeine. Since 1978, however, concentrate of poppy straw has been used with increasing frequency for that purpose. "Poppy straw" is a term used for the remainder of the poppy plant—but primarily refers to the seed capsule itself—once the seeds and opium-producing fluid have been removed. The majority of morphine and codeine production now comes from concentrate of poppy straw.

The concentrations of morphine and codeine in both raw opium and poppy straw vary greatly, but morphine concentrations as a percentage of total weight are typically about 10 times greater than are those of codeine. Therefore, processing of opium and poppy straw produces much more morphine than codeine. However, greater quantities of codeine than morphine are required for medical purposes. Based on the discrepancies between production and use of the two drugs, about 80% of morphine is converted into codeine.

The global manufacture of codeine underwent a 22% increase in the 1980s, from 162 tons (147,000 kg) in 1980, to 197 tons (180,000 kg) in 1989. The rate of production increased during the 1990s, with total codeine production reaching 280 tons (255,000 kg) in1999. Overall, a 65% increase in global codeine production occurred in the 20 years between 1980 and 1999. Most codeine goes directly into medications, but some is also used to produce other opioid medications such as dihydrocodeine and hydrocodone. Actual figures for the number of codeine prescriptions written in the United States in any particular year are difficult to obtain, since less than half of all states track these numbers. Of all prescriptions written for opioid analgesics, about 15% are for codeine.

Scope and severity

Just as the medical use of codeine has increased, its misuse and abuse have also increased, although not in proportion. The issue of drug abuse can be analyzed from many different perspectives and categorized in a number of ways. One method is to compare and contrast the abuse of illegal drugs (marijuana, cocaine, etc.) with that of legal drugs (OTC and prescription medications). The majority of national and international attention and resources go toward illegal drug abuse. However, prescription drug abuse is a large and growing proportion of the complete drug abuse picture.

Each year, the National Household Survey on Drug Abuse (NHSDA), conducted by the Substance Abuse and Mental Health Services Administration (SAMHSA) of the United States Department of Health and Human Services, collects statistical data on five drug groups, including marijuana/hashish, psychotherapeutic drugs, cocaine/crack, hallucinogens, and inhalants. The medications included in the psychotherapeutic drug group are stimulants, sedatives, tranquilizers, and pain relievers. Codeine and other opioids constitute the majority of the pain relievers in the group.

In 2000, the NHSDA found 1.7% of all people 12 years and older reported nonmedical use of a psychotherapeutic medication during the previous month. More than 9 million Americans over age 12 reported use at any time during the year. Those in the 18-to 25-year-old age group have the highest rates of drug abuse. In 2000, 3.6% of individuals in that age group reported nonmedical use of prescription drugs in the month prior to when they were surveyed, but less than half that many, 1.6%, reported the same type of drug abuse in 1994. An estimated 1.6 million Americans used prescription pain relievers nonmedically for the first time in 1998. During the 1980s, there were generally fewer than 500,000 first-time users per year.

The Drug Abuse Warning Network (DAWN) is an ongoing program sponsored by SAMHSA. Approximately 500 hospital emergency rooms throughout the United States gather data from admitted patients on drugs of abuse (i.e., the number of times a specific drug is mentioned by ER patients). A study published in the Journal of the American Medical Association in 2000 compared the increase in legitimate medical use of opioids with one indicator of the increase in abuse of those same drugs. Specifically, five opioid drugs—morphine, fentanyl, oxycodone, hydromorphone, and meperidine—as a group showed a cumulative increase in medical use of nearly 250% from 1990 to 1996. Data collected from DAWN for the same time period showed a 7% increase in emergency room mentions of abuse of these drugs. As a proportion of all opioid drugs mentioned, the five drugs studied decreased from 23% in 1990 to 16% in1996. This means that mentions of other opioid analgesics, including codeine (although raw numbers for codeine were not analyzed), increased during that time period by 16%. By comparison, the reports of abuse of illicit drugs increased 110%. Admittedly, the data collected by DAWN evaluates only one facet of the drug abuse problem—drug abuse contributing to emergency room visits. However, from these data at least, it does not appear that a significant increase in medical use of opioid drugs resulted in a proportionate increase in abuse. More studies looking at a broader picture of opioid analgesic abuse are needed.

Age, ethnic, and gender trends

Between 1990 and 1998, abuse of some illegal drugs among teens and young adults leveled off or decreased slightly. However, increases in new users of prescription pain relievers were reported in young teens, age 12–17, as well as in young adults age 18–25. In 2000, the NHSDA found that the youngest teens, age 12–14, reported psychotherapeutic medications as the most frequent drugs of abuse, with that group alone making up 53% of the total of all drug abuse reports. Teens and young adults in the 18–25 age group reported prescription drug abuse at a rate of 36%, while 28% of those over age 26 reported that type of abuse. Most teenagers begin prescription drug abuse by taking someone else's medication, usually someone from their family. Teens are also more likely than adults to be acquainted with someone who sells prescription drugs like codeine illegally.

On the other end of the age spectrum, prescription drug abuse among older adults is also a growing concern. Persons 65 and older comprise 13% of the United States population, but consume about 33% of all prescription drugs. A study of 1,500 elderly patients found that 3% were abusing prescription drugs. Unlike people in younger age groups, however, the elderly are more likely to misuse prescription drugs than abuse them. If abuse does occur, it may begin with misuse due to inappropriate prescribing or the patient not following instructions correctly. Continued misuse may then progress to dependence and abuse, especially with medications such as codeine. Other factors may influence codeine misuse and abuse in older adults. There may be age-related physical changes that influence codeine metabolism, or confusion about the effects codeine can produce. The elderly also have a higher likelihood of other undiagnosed medical conditions, such as depression, that increase the risk for codeine abuse. Finally, a survey of elderly persons admitted to a treatment program found that 70% were female and of the various drugs of abuse in that group, 70% were opioids.

The NHSDA study showed that boys in the youngest age group (12–17) are more likely to experiment with illegal drugs, but girls of that age have a 20% higher rate of prescription drug abuse. In addition, for all teens of that age that abuse prescription drugs, girls are twice as likely to become addicted as boys are. Women are also more likely to abuse and become addicted to prescription drugs in the young- and middle- adult age groups. Part of this may be that women are prescribed potential drugs of abuse more often than men are.

At all age groups, whites are more likely than other racial or ethnic groups to abuse prescription drugs, and many people who abuse these drugs have psychiatric disorders. In 2000, the New England Journal of Medicine published a report on a survey of pharmacies in New York. The data showed that pharmacies in predominantly minority neighborhoods (greater than 60% non-white population) were three times less likely to stock enough opioid drugs to fill prescriptions on demand than were pharmacies in predominantly white neighborhoods. This may be due to financial constraints in trying to maintain inventories of drugs in those minority neighborhood pharmacies. However, it may also be from fear of crime. A number of pharmacies in the United States were burglarized for their opioid drugs, especially the drug OxyContin, in the late 1990s. The events made national headlines, and intensified the debate over the benefits and drawbacks of opioid drugs.

Health professionals (doctors, nurses, dentists, veterinarians, etc.) and their staff may be at risk for codeine abuse because of their ready access to the drug. On the other hand, one would expect health care workers to be at less risk due to their training and knowledge of the effects of drug abuse. In fact, health care workers do not appear to have rates of codeine or other opioid abuse much different from the rest of the population.

MENTAL EFFECTS

Most people describe the euphoria produced by codeine as a pronounced feeling of well-being and calmness. A few people may get a mild stimulant effect and a feeling of elation. Evidence indicates that the euphoria produced by codeine and other opioids is similar to, but stronger than, the perceived feeling from high levels of endogenous opioids in the body—the so-called endorphin rush experienced by some athletes after heavy exercise. Instead of euphoria after a codeine dose, some people report a feeling of dysphoria—a general feeling of discomfort and restlessness. Still other people may just feel drowsy, with no noticeable positive or negative effect on their mood.

It remains a misconception that opioids offer no true analgesic effect, but instead produce a type of euphoria that simply results in one not caring about their pain. With the discovery of opioid receptors in the central nervous system, along with an understanding of how opioids such as codeine affect nerve cells, no dispute remains that opioids are indeed potent pain relievers. Up to a certain limit (usually an amount great enough to produce serious side effects), the more codeine ingested in a single dose, the greater the analgesia and the more pronounced the mental effects would be.

People with moderate or severe pain who take prescribed doses of codeine usually obtain at least some relief from their pain, but generally do not report feelings of euphoria. Those with mild pain who take one of the higher doses of codeine (e.g., Tylenol #4) may experience pain relief along with some euphoria. People who abuse codeine are most likely to experience euphoric feelings, and are at the greatest risk of becoming addicted.

PHYSIOLOGICAL EFFECTS

Other than analgesia, the most common physiological effects produced by medicinal quantities of codeine are nausea, vomiting, constipation, and itching of the skin (pruritis). These symptoms would be considered relatively harmless (benign) side effects. They typically disappear in most people after taking the drug for several days, or by reducing the dosage. If someone has diarrhea prior to using codeine, the physiological side effect of constipation then becomes a medicinal effect for that symptom. For most people, the higher the codeine dose, the more likely side effects will be present or the more severe the side effects will be.

Harmful side effects

Overall, codeine's lower potency results in fewer side effects compared to other drugs in the class. The complication of greatest concern is respiratory depression. Opioids affect the area of the brain that controls breathing. A large enough single dose of any opioid, including codeine, can stop breathing completely, resulting in death. Combining codeine with another central nervous system depressant, such as alcohol or sedatives, is especially risky. Unfortunately, people who abuse codeine often abuse other drugs as well. While drowsiness itself is not a harmful side effect, it can be dangerous when driving or engaging in other activities that require concentration and alertness.

Since most codeine is dispensed as part of a compound preparation, potential side effects of the other drug(s) must also be considered. For instance, someone with stomach ulcers should not take codeine that is combined with a nonsteroidal anti-inflammatory drug (NSAID) such as aspirin or ibuprofen. Another type of risk from a compound preparation relates to codeine abuse. For instance, a person who abuses codeine might routinely take a dose of 100–200 mg of codeine to produce noticeable euphoria. Using Tylenol #3 to obtain this dose would also mean ingesting 1,000–2,000 mg of acetaminophen. Taking that amount of acetaminophen for any extended period presents a risk for liver damage, especially in combination with alcohol.

Long-term health effects

There are very few adverse health effects as far as organ or tissue damage from long-term (years) use of codeine. This is in contrast to most other abused drugs, with alcohol and tobacco being the obvious examples.

The relative lack of any known serious organ or tissue damage produced by codeine use is counterbalanced, however, by its high risk for abuse and addiction. Even though codeine may be the least addictive of the group, opioids are arguably the most addictive drugs known. Drugs with a high risk of addiction also present a high risk for long-term use, which can include either years of continual use or a repeated cycle of use and abstinence. The latter can be especially difficult with codeine given the potentially serious withdrawal symptoms associated with stopping the drug suddenly. Most people with codeine addiction do not seek professional help, and self-treating an addiction usually involves stopping the drug suddenly.

A sudden withdrawal from codeine after a long period of use always results in some withdrawal symptoms. The longer and more serious the abuse, and the more suddenly the drug is stopped, the more difficult and painful the withdrawal symptoms will be. Chronic use of codeine can result in some tolerance to the drug so that higher doses must be taken to obtain the same initial effects. However, the level of tolerance seems to be less in people using codeine legitimately for pain. Long-term use also can lead to physical dependence, a process in which the body adapts to the presence of the drug, resulting in withdrawal symptoms if its use is abruptly stopped. Symptoms of withdrawal can include restlessness, muscle and bone pain, insomnia, diarrhea, runny nose, chills with goose bumps, and involuntary leg movements. The involuntary leg movements associated with opioid withdrawal are what originally lead to the phrase "kicking the habit." The phrase "quitting cold turkey" originated because the goose bumps on a person's skin that often occur during withdrawal resemble cold turkey skin.

REACTIONS WITH OTHER DRUGS OR SUBSTANCES

Using alcohol while taking codeine poses a serious risk. Like codeine, alcohol is a CNS depressant, and the two drugs combined increase the risk of heavy sedation and respiratory depression. Other drugs that should be avoided or used only under a doctor's supervision while taking codeine include benzodiazepines (tranquilizers in the same class as Valium), most antihistamines, and sedatives/hypnotics (sleep medications). Certain types of antidepressants should be used with caution when taking codeine, especially monoamine oxidase (MAO) inhibitors and those in the selective serotonin reuptake inhibitor (SSRI) class. Some codeine abusers use glutethimide (Doriden), a potent tranquilizer, to produce effects similar to heroin increasing the risks for serious side effects and addiction.

TREATMENT AND REHABILITATION

Serious addiction to codeine is not as common as it once was, possibly due to the availability of greater numbers of competing, more potent opioids. The perception by some that addiction to a "weak" opioid like codeine is not serious results in fewer individuals seeking treatment for their codeine addiction. However, in those cases where treatment is needed, codeine addiction should be approached in the same manner as addiction to other opioids, such as heroin or morphine.

Codeine overdose can be treated with the opioid antagonist, Narcan (naloxone). The goal of treating codeine addiction is for the addicted person to stop taking the drug completely and permanently. Most people who overcome codeine addiction do so by themselves, but some may need professional assistance. In either case, it is invaluable for someone to have help and support from friends and family. For chronic addiction (addiction lasting more than one year), codeine may be replaced by methadone, another opioid medication. Methadone is provided to the patient either through a physician or through a qualified drug treatment program. In a structured setting, the patient and health care professionals have a much better chance of controlling drug use with methadone, and eventually may achieve complete abstinence. The benefits of methadone over codeine are that it only needs to be taken once a day, it reduces or eliminates withdrawal symptoms and the craving for codeine, and it has fewer side effects.

PERSONAL AND SOCIAL CONSEQUENCES

Illicit drug use provides little or no personal and social benefits, though codeine and other opioids do offer personal and social medical benefits. However these benefits must be weighed against the potential costs of abuse and addiction for individuals and society.

Most codeine prescriptions are written for Schedule III preparations. These medications provide an important middle ground between two drug groups—less effective OTC and nonnarcotic prescription analgesics on one side, and Schedule II analgesics on the other. Distribution and prescriptions are more tightly regulated for Schedule II than for Schedule III drugs. Consequently, for a patient whose pain level is not severe enough to require a Schedule II drug, yet is too severe for or does not respond well to OTC or other prescription analgesics, codeine can provide an effective compromise.

The social consequences of having a broad range of analgesics to treat chronic pain are significant. Conditions associated with chronic pain are the largest contributors to lost work time and productivity. In addition, home and family life may be disrupted for those whose pain is not effectively treated. Therefore, while a doctor must weigh the risks and benefits of treating with codeine on an individual basis, judicious use of codeine and other opioids would seem to present much greater social benefits than costs.

Personal costs—financial, physical, and emotional—can be significant for those individuals who abuse codeine and become addicted. An established addiction can be expensive to maintain, even with a relatively inexpensive medication (through legal purchase) such as codeine. Many people describe a serious opioid addiction as "all consuming"; everything in their life eventually revolves around obtaining more of the drug. With the drug as their focus, they lose friends, alienate family members, and they may be unable to hold a job. With a lower cost and greater availability compared to other opioids, codeine may serve as a starting point for a progression to more powerful, costly, and addictive Schedule II drugs, not to mention illicit drugs.

It might seem logical that anyone who goes to great lengths to obtain codeine is addicted, abusing it recreationally, or selling it for profit, but this is not always the case. While the situation is improving, many people with chronic pain still find it difficult to locate a doctor who will prescribe opioid analgesics. A person with chronic pain may show drug-seeking behavior if they find it difficult to obtain prescriptions for the medication. In fact, a doctor treating such a person might mistake the behavior for psychological addiction rather than somewhat desperate attempts to obtain relief for an ineffectively treated condition.

Codeine plays a relatively minor role in the overall picture of opioid prescription drug abuse. Evidence indicates that proper prescribing of codeine for legitimate medical concerns does not greatly increase the risk of addiction and abuse. Those in the medical community agree that more education is needed on both sides to help prevent the potential for abuse and addiction, so that patients truly in need are not denied access to codeine based on misperceptions and fear. The benefits for individuals and society are great when chronic pain is treated safely and effectively.

LEGAL CONSEQUENCES

Whether requiring a written order in a hospital chart (or other inpatient health care institution) or a prescription written on a special form, hospital and community pharmacies exercise special caution when dispensing codeine and other controlled substances. In some cases, a doctor may choose to telephone the patient's pharmacy with the prescription. However, for medication such as codeine, they must provide their DEA number and some relevant medical information. This helps to prevent someone from calling a pharmacy to obtain codeine by impersonating a physician. It is unlikely that anyone other than a physician or dentist would have access to both a valid DEA number and the medical knowledge necessary to sound credible to pharmacy staff when ordering such a medication.

It is illegal to write a prescription or an order for codeine without a valid medical license. Those professionals that may legally write prescriptions or orders for codeine include medical doctors (MD), doctors of osteopathy (DO), podiatrists (PO), dentists (DDS), and veterinarians (DVM). Physicians or dentists who knowingly write multiple prescriptions for patients without a valid medical reason are subject to possible disciplinary action and criminal prosecution. Writing and filling fake prescriptions for profit is a more serious offense. Likewise, it is illegal to obtain, or try to obtain, prescriptions for codeine under false pretenses (fabricated symptoms and scenarios). Nineteen states have a law (a felony in some) prohibiting a patient from obtaining the same controlled substance from multiple prescribers within a limited time period (doctor shopping). Unlike the illegal activities associated with most other drugs, the perpetrators of crimes involving prescription drugs are most often white, middle-class women. Their crimes usually involve doctor shopping and/or prescription forgery.

Many people in the government and medical community fear that increased production of opioid drugs correlates with increased rates of abuse and addiction. Pharmacies were increasingly burglarized for their opioid drugs, which seemed to bolster this argument. However, the newsworthiness of those crimes serves to overemphasize one side of the debate. Studies have consistently shown that patients with chronic pain who use opioids appropriately rarely become addicted. In 2001 and 2002, a number of groups advocating for effective pain management joined with government agencies, including the Drug Enforcement Administration (DEA), to begin a long-term effort to increase the availability of effective pain management drugs for patients, while decreasing the illegal use and abuse of these drugs.

Legal history

In the United States, the Harrison Narcotics Act of 1914 provided the first real regulation of the general sale of opiates. The exceptions were sales to licensed physicians for use on their own patients, and sales to those people who could provide a written prescription from a doctor. The adoption of laws controlling the production and distribution of all prescription medications occurred primarily because of morphine and codeine.

Codeine is a controlled substance in the United States. Its manufacture and distribution are controlled by the Food and Drug Administration (FDA) and the DEA. The majority of other countries have controls similar to those of the United States. International control is overseen by the International Narcotic Control Board (INCB).

Several foreign countries and some states continue to sell medications with small amounts of codeine over the counter. In the United States, though, even OTC codeine medications have restrictions. A person purchasing codeine must be at least 18 years of age and provide valid identification. In addition, their name may be entered in a special logbook maintained by the pharmacy.

Federal guidelines, regulations, and penalties

Injectable forms of codeine are classified under the Controlled Substances Act (CSA) as Schedule II, even though they do not typically contain more than 60 mg per dose. Analgesics containing 15–60 mg of codeine per single dose carry a Schedule III classification (although the upper single dose limit in many states is 90 mg). Schedule III drugs have a lower potential for abuse than drugs in Schedule II, and abuse of the drug may lead to moderate or low physical dependence and/or high psychological dependence.

Medications containing less than 15 mg of codeine per single dose (most contain either 8 mg or 12 mg) are classified as Schedule V. Cough suppressants with codeine make up the majority of this category. Drugs in Schedule V have a low potential for abuse, but abuse may lead to limited physical dependence and/or psychological dependence compared to drugs in Schedule IV.

See also Fentanyl; Heroin; Meperidine; Morphine; Opium; Oxycodone

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Purdue Pharma L.P. "Painfully Obvious: The Effects of Abusing Prescription Drugs." (March 29, 2002). <http://www.painfullyobvious.com>.

United Nations Office for Drug Control and Crime Prevention. <http://www.undcp.org>.

"The Vaults of Erowid: Documenting the Complex Relationship between Humans and Psychoactives." (March 29, 2002). <http://www.erowid.org>.

Organizations

Drug Enforcement Administration (DEA), Information Services Section (CPI), 2401 Jefferson Davis Highway, Alexandria,, VA, USA, 22301, <http://www.usdoj.gov/dea>.

National Institute on Drug Abuse (NIDA), National Institutes of Health, 6001 Executive Boulevard, Room 5213, Bethesda, MD, USA, 20892-9561, (301) 443-1124, (888) 644-6432, [email protected], <http://www.drugabuse.gov/NIDAHome.html>.

Office of Disease Prevention and Health Promotion, U.S. Department of Health and Human Services, 200 Independence Avenue SW., Room 738G, Washington, DC, USA, 20201, (202) 401-6295, <http://odphp.osophs.dhhs.gov>.

Office of FirstGov c/o GSA, 750 17th Street, NW, Suite 200, Washington, DC, USA, 20006-4634, <http://www.whitehousedrugpolicy.gov>.

SAMHSA-Center for Substance Abuse Prevention (CSAP),(301) 443-0365.

Substance Abuse and Mental Health Services Administration (SAMHSA), U.S. Dept. of Health and Human Services, 5600 Fishers Lane, Rockville,, MD, USA, 20857, (301) 443-6239, [email protected], <http://www.samhsa.gov>.

Substance Abuse and Mental Health Services Administration (SAMHSA)/Center for Substance Abuse Treatment (CSAT), 5600 Fishers Lane, Rockville, MD, USA, 20857, (301) 443-5700, [email protected], <http://www.samhsa.gov>.

U.S. Food and Drug Administration (FDA), 5600 Fishers Lane, Rockville, MD, USA, 20857-0001, (888) 463-6332, <http://www.fda.gov>.

Scott J. Polzin, MS

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Codeine

Codeine

Codeine, a natural product of the opium poppy, is one of the most widely used analgesics (painkillers) for mild to moderate pain. Most codeine medications combine a dose of codeine with mild analgesics such as aspirin, acetaminophen (e.g., Tylenol), and ibuprofen (e.g., Advil). The presence of the mild analgesics permits far lower codeine doses. Using lower doses of codeine can reduce its side effects, such as constipation and nausea.

see also Analgesic; Opiate and Opioid Drug Abuse.

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Codeine

Codeine

Codeine is a type of medication belonging to a class of drugs known as opioid analgesics, which are derived from the Papaver somniferum, a type of poppy flower , or are manufactured to chemically resemble the products of that poppy. In Latin, Papaver refers to any flower of the poppy variety, while somniferum translates to mean "maker of sleep." The plant has been used for over 6,000 years, beginning with the ancient cultures of Egypt, Greece, Rome, and China, to cause sleep . Analgesics are drugs which provide relief from pain . Codeine, an opioid analgesic, decreases pain while causing the user to feel sleepy. At lower doses, codeine is also helpful for stopping a cough.

Although codeine is present in nature within the sticky substance latex which oozes out of the opium poppy's seed pod, it is present in only small concentrations (less than 0.5). However, morphine , another opioid analgesic, is present in greater concentrations (10) within the opium poppy's latex, and codeine can be made from morphine via a process known as methylation, which is the primary way that codeine is prepared.

Codeine is a centrally acting drug, meaning that it goes to specific areas of the central nervous system (in the brain and spinal cord) to interfere with the transmission of pain, and to change your perception of the pain. For example, if you have your wisdom teeth removed and your mouth is feeling very painful, codeine will not go to the hole in your gum where the tooth was pulled and which is now throbbing with pain, but rather will act with the central nervous system to change the way you are perceiving the pain. In fact, if you were given codeine after your tooth was pulled, you might explain its effect by saying that the pain was still there, but it just was not bothering you anymore.

Codeine's anti-tussive (cough stopping) effects are also due to its central actions on the brain. It is believed that codeine inhibits an area of the brain known as the medullary cough center.

Codeine is not as potent a drug as is morphine, so it tends to be used for only mild-to-moderate pain, while morphine is useful for more severe pain. An advantage to using codeine is that a significant degree of pain relief can be obtained with oral medication (taken by mouth), rather than by injection. Codeine is sometimes preferred over other opioid analgesics because it has a somewhat lower potential for addiction and abuse than do other drugs in that class.

Scientists are currently trying to learn more about how codeine and other opioid analgesics affect the brain. It is interesting to note that there are certain chemicals (endorphins, enkephalins, and dynorphins) which are made within the brains of mammals , including humans, and which closely resemble opioid analgesics. In fact, the mammalian brain itself actually produces tiny amounts of morphine and codeine! Some of these chemicals are produced in the human brain in response to certain behaviors, including exercise . Exploring how and when human brains produce these chemicals could help scientists understand more about ways to control pain with fewer side effects, as well as helping to increase the understanding of addictive substances and behaviors.

See also Narcotic.


Resources

books

Berkow, Robert, and Andrew J. Fletcher. The Merck Manual of Diagnosis and Therapy. Rahway, NJ: Merck Research Laboratories, 1992.

Katzung, Bertram G. Basic & Clinical Pharmacology. Norwalk, CT: Appleton & Lange, 1992.

Marieb, Elaine Nicpon. Human Anatomy & Physiology. 5th ed. San Francisco: Benjamin/Cummings, 2000.


Rosalyn Carson-DeWitt

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Codeine

Codeine


What Kind of Drug Is It?

Codeine is an opiate analgesic, meaning it is a pain reliever derived from the opium poppy plant. Its powers of pain relief—and its side effects—are many times weaker than the related opiates morphine and heroin. (An entry for each of these drugs is available in this encyclopedia.)

Doctors sometimes prescribe pills containing combinations of codeine and over-the-counter (OTC) analgesics, such as Tylenol (acetaminophen) or aspirin, for pain relief after minor surgery, or for bone breaks and sprains, migraine headaches, or other pain that is expected to pass fairly quickly. The other most common use for codeine is in cough syrup. The drug acts on the part of the brain that controls coughing.

In the United States and many other countries, a prescription is necessary to obtain products containing codeine. This is because the drug is addictive, or habit-forming. It also can produce unpleasant side effects such as constipation and nausea. When codeine is abused, it is either ingested in its cough syrup form at greater-than-prescribed doses or extracted from prescription pills through chemical "cooking." In either case, taking a large dose of codeine can be fatal, because it can cause the user to stop breathing.

According to Paul M. Gahlinger in Illegal Drugs: A Complete Guide to Their History, Chemistry, Use, and Abuse, codeine "is by far the most commonly used narcotic in the world," especially in the form of cough syrup. Codeine's qualities as a pain reliever have been recognized since the early 1800s. Chemically speaking, opiate medications such as codeine mimic the brain's own natural mechanisms for suppressing pain. Codeine actually reduces the ability of the brain's nerve cells to transmit pain signals. The reason it works better than the body's own mechanisms is because it floods the brain with chemical messages in a more powerful way than the brain's chemistry can on its own.

Official Drug Name: Codeine, codeine phosphate, codeine sulfate, methyl morphine

Also Known As: T-threes, schoolboy, coties, dors and fours; cough syrup with codeine is known as: syrup, barr, karo, lean, nods, down, drank

Drug Classifications: Schedule I, codeine methylbromide and codeine-N-oxide; Schedule II, methyl morphine; Schedule III, codeine combinations with acetaminophen, aspirin, or ibuprofen; Schedule V, prescription cough syrup preparations containing codeine

recreational use of codeine, in the absence of pain, can produce feelings of euphoria (pronounced yu-FOR-ee-yuh). Such feelings bring on a state of extreme happiness and well-being in users. However, when the effects of the drug wear off, the user is often


left with a sensation of depression or nervousness. This leads to a desire to take more of the drug. This is how the cycle of addiction begins. For this reason, doctors and pharmacists use caution when prescribing or dispensing medications containing codeine. Still, codeine abusers have found ways to obtain the drug illegally. In some parts of the United States, cough syrup abuse has contributed to growing numbers of emergency room visits for drug overdoses.

Overview

Humans like to experiment. They do this in art, music, medicine, technology, science, and other fields. For thousands of years, some have also experimented with using mind-altering drugs found in plants and animals. The first real evidence of opium poppy use in the historical record dates back 6,000 years to ancient Mesopotamia (the current nation of Iraq). Descriptions of poppy use for pain relief can be found in Egyptian papyrus records. Later, ancient Greek farmers learned that the most potent, or strongest, part of the poppy plant was found in the sap that oozes from the ripened seed bulbs. The word "opium" is actually derived from a Greek word meaning "sap." Historical records also reveal that ancient Romans used opium as a painkiller, a poison, and a means of suicide, varying their doses accordingly.

During the Middle Ages (c. 500–c. 1500) and the Renaissance period (spanning the fourteenth through the seventeenth centuries), physicians and alchemists experimented with poppy sap. In 1524, Swiss scientist Paracelsus (1493–1541) created laudanum, a mixture of opium and alcohol. All by itself, laudanum is a bitter-tasting substance. When mixed with wine, better-tasting herbs, or syrups, however, it became one of the most popular cure-alls of the late 1800s and early 1900s. The use of tinctures and elixirs containing opium became so commonplace in nineteenth-century Europe that the practice even found its way into literature. Fictional detective Sherlock Holmes, created by Sir Arthur Conan Doyle (1859–1930), even visited an opium den to solve a crime.

Morphine, the most active ingredient in opium, was discovered in 1803 by a young German pharmacist's assistant, Friedrich Sertürner (1783–1841). The drug was far more powerful than crude opium and also far more addictive. Attempts to lessen the habit-forming aspects of morphine led to further experimentation with poppy sap. In 1832, the codeine compound was separated from the sap for the first time. Its name comes from the Greek word kodeia, meaning "poppy head."


At first, nineteenth-century scientists thought they had finally found what they had been seeking: a painkiller that did not produce euphoric side effects and was not addictive. However, they were wrong. When taken in large doses, codeine produces the same effects as morphine, including addiction. The only difference is that it is five to ten times weaker than morphine.

Scientists did discover some qualities of codeine that made it popular. It works as a painkiller when taken orally (by mouth). In comparison, morphine and heroin are usually injected or snorted through the nose. Codeine also was effective at suppressing coughs, and it quickly found its way into cough syrups. Like the more powerful opiates, codeine causes constipation by working on the nerves and muscles in the intestines. Therefore, it was used to treat diarrhea.

Throughout the twentieth century, knowledge about opiate analgesics increased. In 1900, codeine could be found in a variety of OTC medications for adults and children. The Harrison Narcotics Act of 1914 set new regulations on the sale of opiates, making them illegal unless prescribed to a patient by a licensed physician. Since then, drug companies have developed analgesics that contain combinations of painkillers such as aspirin and codeine, or Tylenol and codeine. A prescription for pure codeine, however, is rarely ever given.

By 2000, all OTC sales of codeine-containing products had ended in the United States. The drug is legally available in America only if prescribed by a doctor, a dentist, or a veterinarian. Nevertheless, it is still manufactured in large quantities. At the turn of the twenty-first century, total codeine production worldwide approached 300 tons.

What Is It Made Of?

Codeine is a controlled substance in the United States. This means that the U.S. Food and Drug Administration (FDA) and the Drug Enforcement Administration (DEA) supervise its manufacture and distribution. Opium is sometimes harvested by slicing the plant's seed pods and extracting the sap. In 2005, however, machines were available to slice the entire mature poppy plant into bits and grind those bits into powder. According to Gahlinger, "Each year, more than 600 tons of opium powder are legally imported into the United States for legitimate medical use."

Pure opium can be separated into three different drugs: morphine, codeine, and thebaine. Most of the codeine used in the United States is synthesized from morphine by a process called methylation (pronounced meh-thuh-LAY-shun). Codeine is an organic, or naturally occurring, compound that contains carbon, hydrogen, nitrogen, and oxygen. Its chemical formula is C18H21NO3. Codeine is also an alkaloid. Curiously, while most of the prescription codeine is derived from morphine, when the drug is ingested, the human liver turns the codeine back into morphine. Therefore, the compound works on the brain in the same way morphine does.

How Is It Taken?

Prescription codeine is available in several forms. Tylenol 3, for instance, is a pill containing 300 milligrams of acetaminophen and 30 milligrams of codeine. Some oral medications containing codeine also contain low doses of caffeine to counteract the sedating effects of the codeine. Pill-form medications containing codeine are swallowed, and their pain-relieving effects can last from three to six hours.

Liquid cough syrups containing various strengths of codeine are usually combined with an expectorant agent for clearing the airways of phlegm. Phlegm must be spit up, or expectorated, to improve a patient's breathing. Cough remedies with codeine and expectorants are taken by the spoonful every four hours with a full glass of water.

Are There Any Medical Reasons for Taking This Substance?

Codeine-containing medications are usually prescribed to relieve pain or control coughs. Pills containing codeine and other analgesics are typically used for mild to moderate pain that is expected to go away within days or weeks. Cough syrups containing codeine are usually prescribed for dry coughs that keep a patient up at night.

"Tylenol by the Numbers"


People experiencing levels of pain that will not respond to over-the-counter drugs can sometimes receive prescription pain relievers containing various dosages of codeine. Tylenol-brand acetaminophen is one product that contains codeine in its prescription form. These drugs are assigned the numbers one through four to indicate their various strengths. Here's a quick rundown of "Tylenol by the Numbers":

  • Tylenol with Codeine No. 1 (more commonly referred to as Tylenol 1) contains 8 milligrams of codeine and 300 milligrams of acetaminophen.
  • Tylenol with Codeine No. 2 (more commonly referred to as Tylenol 2) contains 15 milligrams of codeine and 300 milligrams of acetaminophen.
  • Tylenol with Codeine No. 3 (more commonly referred to as Tylenol 3) contains 30 milligrams of codeine and 300 milligrams of acetaminophen.
  • Tylenol with Codeine No. 4 (more commonly referred to as Tylenol 4) contains 60 milligrams of codeine and 300 milligrams of acetaminophen.

The brand-name product Fiorinal with Codeine contains aspirin, butalbital (a barbiturate), caffeine (a stimulant), and codeine. This prescription drug is used primarily for relief of migraine headache pain.

To Cough, or Not to Cough

It is important to note that cough syrups containing codeine can actually be dangerous for patients with certain kinds of respiratory illnesses. Coughing is the body's natural way of clearing fluids out of the lungs and bronchial tubes. Because codeine works on the brain to quiet a cough, users may experience a buildup of unwanted fluids that block their airways. As noted in the journal Pediatrics, "Cough suppression may adversely affect patients … by pooling of secretions, airway obstruction, [and] secondary infection." In other words, patients run the risk of choking on their own secretions, and these secretions may serve as a source of infection that can spread throughout the body. Therefore, cough syrups with codeine are not prescribed for patients with asthma, allergies, cystic fibrosis, or pneumonia.

In the early part of the twentieth century, codeine was commonly prescribed for diarrhea. However, it is rarely used for that purpose anymore. Likewise, the use of codeine-enhanced products for migraine headaches is being phased out with the introduction of more effective non-narcotic medications for migraine pain.

How Effective Is Codeine?

Reports in Chemist & Druggist and the Western Journal of Medicine both cited recent studies comparing codeine-containing and noncodeine-containing pain relievers. The evidence suggests that pain relievers with codeine prove no more effective than plain, over-the-counter analgesics. In addition, "patients receiving codeine were more likely to stop therapy because of side effects," wrote Sanjay Arora and Mel E. Herbert in the Western Journal of Medicine. The researchers went on to state that codeine's pain-relieving powers are largely a "myth."

Usage Trends

The continued research on opiates, both natural and synthetic, has produced a new generation of pain-fighting drugs that are related to but more powerful than codeine. Brand-name pills such as Percocet, Percodan, and OxyContin contain oxycodone, which is synthesized from thebaine. (An entry on oxycodone is available in this encyclopedia.) Hydrocodone, another relative of codeine, is six times stronger than codeine and can be found in generic form or in brand-name pills such as Vicodin, Lortab, and Lorcet.

According to a 2003 online report by the Drug Abuse Warning Network (DAWN), abuse of prescription painkillers "has risen dramatically in the U.S. Of particular concern is the abuse of pain medications containing opiates." Unlike club drugs or designer drugs, opiates can be obtained from a doctor legally. This has led to addiction among senior citizens, who sometimes fail to understand the dosage directions, as well as upper- and middle-class users of any age who would tend to shun illegal street drugs. Celebrities such as political commentator Rush Limbaugh and comedian George Carlin have made the news for undergoing treatment for prescription opiate addiction.


Although prescription opiate abuse is rising, the trend of codeine abuse, in particular, fell more than 60 percent between 1994 and 2001, according to the 2003 DAWN Report. Because codeine is dispensed most commonly in combination with other agents, it is less likely to be a drug of choice for an abuser, particularly if that abuser can obtain OxyContin, Vicodin, or other stronger medications.

In certain regions of the United States, however, codeine abuse continues to be a problem. In Houston, Texas, an entire culture has sprung up around cough syrup abuse, including a type of rap music called "screw." In this type of rap, songs are re-mixed, slowed down, and chopped to sound like a skipped recording. One of the pioneers of screw music, Robert Davis Jr. (1971–2000), also known as DJ Screw, died of a codeine overdose at his recording studio.

The popularity of screw music—and cough syrup abuse—is reported to be spreading across the southern United States. Kristen Mack noted in the Houston Chronicle that a Memphis, Tennessee-based rap group, Three 6 Mafia, had a locally popular single called "Sippin on Syrup." Mack wrote that in 2001, Houston-area "police confiscated 125 gallons of illegal codeine. Each year, they say, they encounter more abuse and more people coming to Houston looking for 'syrup.'… Everyone agrees that Houston is ground zero for this 'quiet epidemic."'

Cough syrup with codeine is more readily available in Texas because codeine is sold in small quantities over-the-counter in Mexico. Smugglers stockpile as many doses as they can, take them across the Mexican-U.S. border, and sell them on the street. Mack reported that in 2002, eight ounces of cough syrup could fetch $200 on the black market. Users typically mix the medication with soft drinks or alcohol.

Effects on the Body

Most people who use codeine for its prescribed purposes experience few side effects. A bothersome cough disappears, perhaps with some drowsiness. Post-surgical pain decreases, perhaps with some nausea. When the medical problem goes away, the patient stops using the pills or cough syrup with no significant after-effects.

Ingesting the drug at higher-than-prescribed doses, some users may experience a sense of well-being, along with a loss of inhibitions and feelings of drowsiness or light-headedness. Other users have reported the opposite effect: a sense of discomfort and restlessness. Because codeine is taken orally, the user might not feel the effects of the drug for a half an hour to an hour after ingestion. The sensations last several hours and then slowly diminish. Users might feel nauseated or their skin might itch. An overdose can cause users—especially children—to stop breathing. In the event that a codeine abuser stops breathing, rapid administration of the drug naloxone (Narcan) will reverse the effects of the opiate. However, the patient must be diagnosed by a doctor very quickly.

The most profound effect of codeine and other related opiates is psychological. Flooding the brain with opioids from drug use causes the brain to stop producing naturally occurring endorphins, or pleasure-enhancing hormones. Then, when the effects of the drug wear off, the user may feel uncomfortable, anxious, and irritable. He or she might have trouble relaxing or sleeping. Many abusers take another high dose of the opiate in order to restore that feeling of well-being. Such abuse leads to serious problems with addiction.

Addiction to opiates like codeine can happen swiftly; withdrawal can be a difficult and lengthy ordeal. Almost immediately, the codeine abuser who stops taking the drug experiences a host of unpleasant symptoms, including restlessness, anxiety, insomnia, muscle and bone pain, diarrhea, chills that produce goose bumps (hence the term "cold turkey"), and leg tremors ("kicking the habit"). The patient may yawn frequently and feel more sensitivity to pain. These flu-like symptoms usually last for a few days.

What makes opiate addiction so hard to beat is the lasting effects on the brain. The recovering codeine abuser will just "not feel good" psychologically as the brain readjusts to producing its own endorphins. Cynthia Kuhn, Scott Swartzwelder, and Wilkie Wilson described this situation in Buzzed: The Straight Facts about the Most Used and Abused Drugs from Alcohol to Ecstasy. "There is a dysphoria (the just-feeling-lousy feeling), which may be the reverse of opiate-induced euphoria. Withdrawing opiate addicts just feel bad, and they feel bad in a way that they know [taking more] opiates will solve. The craving for a fix can last for months, long after the physical symptoms have abated," or gone away.

Reactions with Other Drugs or Substances

Pharmacists dispensing drugs containing codeine usually warn users that side effects can include drowsiness, dizziness, nausea, and constipation. These substances should not be used with other tranquilizers or sedatives, with benzodiazepines, with the antidepressant drugs known as monoamine oxidase inhibitors (MAOIs), or with antihistamines, amphetamines, or alcohol. Patients taking products that contain codeine must use care when operating automobiles or machinery. When used briefly and specifically for its prescribed purpose, a product containing codeine will not produce extreme side effects.

Doctors prescribing pain relievers containing codeine must carefully check the patient's records for other medications that will adversely interact with codeine. These substances include sleeping pills, tranquilizers, antihistamines, anti-anxiety medications, and any other medicine that produces sedation. Using alcohol and codeine at the same time greatly increases the likelihood of breathing problems. Mixing codeine with illegal substances such as hallucinogens or designer drugs can be fatal.

Additionally, higher doses of prescription pain relief pills containing codeine and/or acetaminophen, ibuprofen, and aspirin can cause severe, sometimes fatal, reactions. Over-the-counter analgesics taken in large doses can lead to stomach bleeding, liver failure, and other organ damage.

Treatment for Habitual Users

As previously described, stopping opiate use abruptly (or going "cold turkey") takes both a physical and psychological toll on the user. Someone wishing to end a codeine addiction can find assistance from a licensed physician who may prescribe methadone to ease the symptoms of withdrawal. Methadone is itself an opiate, but it works differently in the body. It releases slowly, so that the user does not feel a rush of euphoria or a backlash when the euphoria ends. Recovering addicts slowly reduce the dosage of methadone under a doctor's care until they become drug-free. (An entry on methadone is available in this encyclopedia.) Another drug, buprenorphine, also provides some sedating effects while blocking the brain's absorption of opiates.

Any successful drug-treatment program requires some sort of psychological intervention. Former users have reported remarkable benefits from talk therapy and the support of other recovering addicts. Narcotics Anonymous is built on the philosophy of the better-known Alcoholics Anonymous. The organization offers free group therapy, online information, telephone hotlines, and other services to recovering addicts worldwide, no matter what type of drug abuse led to their addiction.

Words from a "Junkie"


Experimental American author William S. Burroughs (1914–1997) was very honest and open about his experiences as an opiate addict. Here, in a passage from his novel Junkie, he describes the process of drug withdrawal.

"The last of the codeine was running out. My nose and eyes began to run, sweat soaked through my clothes. Hot and cold flashes hit me as if a furnace door was swinging open and shut. I lay down on the bunk, too weak to move. My legs ached and twitched so that any position was intolerable, and I moved from one side to the other, sloshing about in my sweaty clothes." Burroughs added: "Almost worse than the sickness is the depression that goes with it. One afternoon I closed my eyes and saw New York in ruins. Huge centipedes and scorpions crawled in and out of empty bars and cafeterias and drugstores on Forty-second Street. Weeds were growing up through cracks and holes in the pavement. There was no one in sight."

Consequences

Interestingly enough, opiate use alone does not produce any lasting damage to the brain or other organs. But that does not mean that codeine can be abused without harmful consequences. Codeine users are likely to combine the drug with other substances ranging from alcohol to hallucinogens, sometimes with fatal results. Attraction to codeine may encourage users to try its stronger relatives, heroin and morphine. Even if the user restricts ingestion simply to codeine, addiction changes behavior in self-destructive ways. In order to obtain their supply of drugs, users may engage in burglary, theft, drug dealing, or prostitution. Under the influence of opiates, addicts eat poorly and ignore symptoms of bad health. So while codeine abuse may not lead to organ damage, its effect on the overall level of good health can be devastating.

The Law

Codeine is a controlled substance. The FDA and the DEA strictly oversee its legal production. Therefore, possession of codeine without a prescription is illegal. Laws for possession and distribution of codeine vary from state to state and may even vary depending on the strength of the dose. For instance, in Massachusetts, possession of pure codeine is a "Class A" offense, carrying a penalty of up to two years in prison and $2,000 in fines. But Massachusetts also has a "Class C" distinction, with lesser penalties, for some prescription opiates containing lower dosages of the drug. In 2002, possession of small quantities of codeine in Texas was considered a misdemeanor with a minimal fine.

Federal penalties for possession of a controlled substance include up to a year in jail for the first conviction, and between $1,000 and $100,000 in fines. A second conviction carries the penalty of fifteen days to two years in prison with up to $250,000 in fines. A third conviction requires ninety days to five years in prison with a maximum $250,000 fine.

There are other ways to break the law in search of codeine. It is illegal to "doctor shop." This is a process whereby a user seeks multiple prescriptions by visiting more than one doctor and "fakes" a set of symptoms that might lead those doctors to prescribe the drug the user wants. It is illegal to bring over-the-counter purchases of codeine into the United States from other countries that sell it. It is also illegal to extract the codeine from analgesic compounds like Tylenol 3. Again, jail time and fines vary from state to state.

Fact or Fiction: Codeine's Reputation


Some people think that prescription opiates are always addictive, and those who use them for any amount of time will become drug addicts. This is not true. Studies show that when prescription painkillers are used as directed, and discontinued when no longer needed, they carry no danger of addiction.

Over time, certain drugs begin to lose their effectiveness, and users need to take more and more of the drug to achieve the original results. Some critics think that codeine users with chronic pain will develop a tolerance to opiates, but this theory has not been proven. Increased doses of codeine only seem to be necessary if the degree of pain experienced by patients worsens as a serious disease progresses.

Prescription painkillers containing codeine have a reputation for bringing on troublesome side effects. Some of the side effects are rumored to be so horrible that patients refuse to take the drug. This is not necessarily the case. In fact, carefully supervised use of prescription painkillers results in a few, easily tolerated side effects.

Drug Tests

Because the liver turns codeine into morphine, the use of prescription products containing codeine can produce a positive urine test for codeine and morphine. Positive tests for the drug can be obtained as many as three to four days after the last use. Curiously enough, as much as a teaspoon of poppy seeds used in baking and on


bagels can also produce a positive drug test for opiates. According to Gahlinger, there is "no direct way to be sure whether a urine test positive for morphine or codeine is due to poppy seeds or to drugs. Eating a single poppy seed bagel can result in a positive drug test for up to three days."

For More Information

Books

Burroughs, William S. Junkie. New York: Ace Books, 1953. Reprinted as Junky. New York: Penguin Books, 2003.

Clayman, Charles B. The American Medical Association Encyclopedia of Medicine. New York: Random House, 1989.

Gahlinger, Paul M. Illegal Drugs: A Complete Guide to Their History, Chemistry, Use, and Abuse. Las Vegas, NV: Sagebrush Press, 2001.

Kuhn, Cynthia, Scott Swartzwelder, and Wilkie Wilson. Buzzed: The Straight Facts about the Most Used and Abused Drugs from Alcohol to Ecstasy, 2nd ed. New York: W. W. Norton, 2003.

Silverman, Harold M. The Pill Book, 11th ed. New York: Bantam Books, 2004.

Periodicals

Arora, Sanjay, and Mel E. Herbert. "Myth: Codeine Is a Powerful and Effective Analgesic." Western Journal of Medicine (June, 2001): p. 428.

"Avoid Codeine Combinations." Chemist & Druggist (May 22, 1999): p. 9.

Harris, Mikal. "Cough Syrup Becomes Addictive Street Drug." St. Louis Post-Dispatch (July 21, 2000).

Mack, Kristen. "From Bayou City to 'City of Syrup': 'Quiet Epidemic' of Codeine Abuse Centered in Houston, Officials Say." Houston Chronicle (February 10, 2002): p. 37.

Monaco, John E. "Uncommonly Common Poisonings in Children." Pediatrics for Parents (September, 1997): p. 6.

"Use of Codeine- and Dextromethorphan-Containing Cough Remedies in Children." Pediatrics (June, 1997): p. 918.

Walling, Anne D. "Codeine Plus Acetaminophen: Benefits and Side Effects." American Family Physician (November 15, 1996): p. 2302.

Web Sites

"Controlled Substances Schedules." U.S. Department of Justice, Drug Enforcement Administration, Diversion Control Program.http://www.deadiversion.usdoj.gov/schedules/schedules.htm (accessed June 30, 2005).

"Legal Penalties for Drug Offenses: Commonwealth of Massachusetts Penalties and Federal Penalties." University of Massachusetts, Lowell. http://www.uml.edu/student-services/dean/policies/ (accessed March 8, 2005).

"Narcotic Analgesics: In Brief." The DAWN Report.http://www.oas.samhsa.gov/2k3/pain/DAWNpain.pdf (accessed June 30, 2005).

"Texas Study Warns of Codeine Cough Syrup Abuse." U.S. Department of Justice, Drug Enforcement Administration, Diversion Control Program.http://www.deadiversion.usdoj.gov/pubs/nwslttr/spec2000/texas.htm (accessed June 30, 2005).

See also: Heroin; Methadone; Morphine; Opium; Oxycodone

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