Codeine (Encyclopedia of Drugs and Addictive Substances)

• Overview
• How Is It Taken?
• "Tylenol by the Numbers"
• Effects on the Body
• Treatment for Habitual Users
• Consequences
• Fact or Fiction: Codeine's Reputation

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 reliefnd its side effectsre many times weaker than the related opiates 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 constipationAn inability to have a bowel movement. and . 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 narcoticA painkiller that may become habit-forming; in a broader sense, any illegally purchased drug. 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.

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

Codeine is prescribed to relieve pain after minor surgeries as well as pain resulting from broken bones, sprains, and migraine headaches. © Steve Prezant/Corbis.

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. 1500) and the Renaissance period (spanning the fourteenth through the seventeenth centuries), physicians and experimented with poppy sap. In 1524, Swiss scientist Paracelsus (1493541) 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 tincturesCombinations of an active drug and a liquid alcohol. and 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 (1859930), even visited an opium denDarkly lit establishments, often in the Chinatown section of big cities, where people went to smoke opium; many dens had beds, boards, or sofas upon which people could recline while experiencing the effects of the drug. to solve a crime.

Morphine, the most active ingredient in opium, was discovered in 1803 by a young German pharmacist's assistant, Friedrich Sertürner (1783841). 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."

The name "codeine" comes from the Greek word kodeia, meaning "poppy head." The drug is derived from opium poppy sap. © Vo Trung Dung/Corbis.

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 from morphine by a process called methylation (pronounced meh-thuh-LAY-shun). Codeine is an organicA term used to describe chemical compounds that contain carbon., or naturally occurring, compound that contains carbon, hydrogen, nitrogen, and oxygen. Its chemical formula is C₁₈H₂₁NO₃. Codeine is also an . 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 agent for clearing the airways of phlegmPronounced FLEM; thick, germ-filled mucus secreted by the respiratory system.. 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.

Tylenol 3 contains codeine and is available by prescription only. Copyright 2002 Thomson MICROMEDEX. All rights reserved.

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.

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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 , 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 drugsHarmful and addictive substances that are manufactured illegally in homemade labs., 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.

In Houston, Texas, an entire culture has sprung up around cough syrup abuse, including a type of rap music called "screw." © Chris Coxwell/Corbis.

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 , Robert Davis Jr. (1971000), also known as DJ Screw, died of a codeine overdose at his recording studio.

The popularity of screw musicnd cough syrup abuses 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 marketThe illegal sale or trade of goods; drug dealers are said to carry out their business 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 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 usersspecially childreno 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 endorphinsA group of naturally occurring substances in the body that relieve pain and promote a sense of well-being., 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; 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, insomniaDifficulty falling asleep or an inability to sleep., 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 (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 , with benzodiazepinesA type of drug used to treat anxiety., with the antidepressant drugs known as monoamine oxidase inhibitors (MAOIs), or with , amphetaminesPronounced am-FETT-uh-meens; stimulant drugs that increase mental alertness, reduce appetite, and help keep users awake., 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 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.

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.

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

Various drug kits are available to determine if people are using drugs illegally. Tests are available for codeine, amphetamines, cocaine, heroin, marijuana, methadone, morphine, and opium alkaloids, among others. TEK Image/Photo Researchers, Inc.

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."

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