Barbiturates (Forensic Science)
The barbiturates are a family of drugs with related chemical structures derived from barbituric acid. In the past, barbiturates were used extensively as sedative-hypnotics—that is, drugs that reduce anxiety and induce sleep. Barbiturates are also used as anticonvulsants and in anesthesia. Because of barbiturates’ significant potential for toxicity, their use has been largely replaced by the safer benzodiazepines, but selected barbiturates are still used in specific applications.
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Effects (Forensic Science)
Barbiturates depress central nervous system (CNS) function in general rather than specific CNS functions. The severity of CNS depression increases with dose, potentially causing significant impairment of psychomotor skills (such as those required for safe driving) and, ultimately, fatal respiratory depression. Dose-dependent effects also extend to the peripheral nervous system, where they manifest primarily as reductions in blood pressure and heart rate. However, at appropriate sedative-hypnotic doses, these latter effects are not hazardous.
At subanesthetic doses, barbiturate effects may include euphoria, reduced anxiety and inhibitions, slurred speech, loss of coordination, and dizziness. CNS depression intensifies with increasing dose; sedation becomes more pronounced, and significant stupor, drowsiness, and loss of coordination may ensue. Anesthetic doses produce coma as well as depressed respiration and blood pressure. Uncontrolled overdose can result in fatal respiratory depression. These effects are intensified in combination with other CNS depressants (such as alcohol or benzodiazepines), and significant impairment or death may occur at lower barbiturate doses (or blood concentrations) when such drugs are coadministered.
Chronic barbiturate use results in the development of tolerance—that is, progressively larger doses are required to achieve a given effect. Repeated administration of and tolerance to the effects of...
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Other Chemical and Pharmacological Properties (Forensic Science)
Barbiturates are weakly acidic and are often prepared as the sodium salts. Their weakly acidic nature becomes important in the design of analytical methods requiring extraction of the drug from a complex forensic sample (for example, blood or tissue). Alteration of the chemical structure results in variation in drug potency (the magnitude of effect at a given dose) and time course of action.
Even in cases where the drug effects last a short time, barbiturates have a relatively long time course within the body. One indicator of this is the half-life of the drug, or the time required for the reduction of drug concentration to 50 percent of its original value. Half-life values for the various barbiturates range from approximately 3 hours to 80 hours. Any drug with a long half-life poses the risk of accumulation in the blood if dosing regimens are not carefully monitored, creating the potential for toxicity. Half-life is also related to the duration of drug action: Typically, a drug with a shorter half-life has a shorter duration of action. This is relevant to forensic investigation, as the half-life is indicative of the time window over which a drug may be detected in the blood; generally, a drug is essentially completely eliminated from the blood within five elimination half-lives.
Duration of action and half-life are important considerations in the choice of a barbiturate for a particular...
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Forensic Analysis and Interpretation of Evidence (Forensic Science)
Law-enforcement personnel may encounter barbiturates in the form of suspicious materials (for example, tablets) requiring identification or quantitative analysis. Forensic scientists may analyze biological samples (such as blood, tissues, urine, or stomach contents) to establish exposure to barbiturates. Correlation of toxic symptoms with measured barbiturate concentration is done in both clinical and forensic settings and in attempts to establish a toxicological cause of death.
Methods used for forensic barbiturate analysis include immunoassay, spectrophotometry, gas or liquid chromatography, and mass spectrometry. Usually, the analysis of biological samples for barbiturates requires preparatory steps to extract the drug from the complex matrix and minimize or eliminate other compounds (such as lipids or proteins) that may be present in those samples that may interfere with analysis, leading to spurious results. The exact nature of the sample preparation steps taken is determined by the nature of the sample being analyzed. Solid samples typically require dissolution or digestion as a first step.
Extraction of drugs from complex samples may be accomplished through the manipulation of chemical conditions (such as pH adjustment) and subsequent partition into a suitable organic solvent system or into a solid phase with subsequent recovery. Following extraction, analysis is typically done...
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Further Reading (Forensic Science)
Baselt, Randall C. Disposition of Drugs and Chemicals in Man. 7th ed. Foster City, Calif.: Biomedical Publications, 2004. Describes the properties and associated tissue concentrations of a wide range of toxic compounds and discusses the techniques used to analyze these chemicals.
_______. Drug Effects on Psychomotor Performance. Foster City, Calif.: Biomedical Publications, 2001. Comprehensive reference work presents information on the impairing effects of a wide range of therapeutic and illicit drugs, including barbiturates.
Brunton, Laurence L., John S. Lazo, and Keith L. Parker, eds. Goodman and Gilman’s the Pharmacological Basis of Therapeutics. 11th ed. New York: McGraw-Hill, 2006. Authoritative advanced textbook explains basic pharmacological principles and the specific pharmacological features of therapeutic agents. Includes some discussion of barbiturates.
Karch, Steven B., ed. Drug Abuse Handbook. 2d ed. Boca Raton, Fla.: CRC Press, 2007. Describes the pharmacological, physiological, and pathological aspects of drug abuse in general, and individual chapters address specific compounds, such as alcohol, as well as specific issues related to drug abuse, such as workplace drug testing.
Levine, Barry, ed. Principles of Forensic Toxicology. 2d ed., rev. Washington, D.C.: American Association for Clinical Chemistry, 2006. Introductory textbook describes the...
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Barbiturates (Encyclopedia of Medicine)
Barbiturates are medicines that act on the central nervous system and cause drowsiness and can control seizures.
Barbiturates are in the group of medicines known as central nervous system depressants (CNS). Also known as sedative-hypnotic drugs, barbiturates make people very relaxed, calm, and sleepy. These drugs are sometimes used to help patients relax before surgery. Some may also be used to control seizures (convulsions). Although barbiturates have been used to treat nervousness and sleep problems, they have generally been replaced by other medicines for these purposes.
These medicines may become habit forming and should not be used to relieve everyday anxiety and tension or to treat sleeplessness over long periods.
Barbiturates are available only with a physician's prescription and are sold in capsule, tablet, liquid, and injectable forms. Some commonly used barbiturates are phenobarbital (Barbita) and secobarbital (Seconal).
Recommended dosage depends on the type of barbiturate and other factors such as the patient's age and the condition for which the medicine is being taken. Check with the physician who prescribed the drug or the...
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Barbiturates (Encyclopedia of Surgery)
Barbiturates are medicines that act on the central nervous system. They cause drowsiness and can control seizures.
Barbiturates are in the group of medicines known as central nervous system depressants (CNS). Also known as sedative-hypnotic drugs, barbiturates make people very relaxed, calm, and sleepy. These drugs are sometimes used to help patients relax before surgery. Some may also be used to control seizures (convulsions). Although barbiturates have been used to treat nervousness and sleep problems, they have generally been replaced by other medicines for these purposes.
Although barbiturates have largely been replaced by other classes of drugs, some are still used in anesthesiology to induce anesthsia and lower the dose of inhaled anesthetics required for surgical procedures.
Pentobarbital (Nembutal) has been used in neurosurgery to reduce blood flow to the brain. This reduces swelling and pressure in the brain, making brain surgery safer.
Secobarbital (Seconal) may be given by mouth or as a suppository to induce sleepiness and relaxation before local anesthesia or the insertion of a tube into the nose or throat.
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Barbiturates (Encyclopedia of Mental Disorders)
Barbiturates are a large class of drugs, consisting of many different brand name products with generic equivalents, that are used primarily for mild sedation, general anesthesia, and as a treatment for some types of epilepsy. One barbiturate, butalbital, exists only as a component of several headache preparations. The most common members of the barbiturate family are phenobarbital (Luminal)), pentobarbital (Nembutal), amobarbital (Amytal), secobarbital (Seconal), thiopental (Pentothal), methohexital (Brevital), and butalbital (component of Fiorinal and Fioricet). They exist in numerous formulations and strengths.
Barbiturates are used to sedate patients prior to surgery as well as to produce general anesthesia, to treat some forms of epilepsy, and to treat simple and migraine headache. These drugs are highly addictive and are often abused as recreational drugs. Although still commercially available, barbiturates such as secobarbital, pentobarbital, and amobarbital are no longer routinely recommended for the treatment of insomnia because of their ability to cause dependence, tolerance, and withdrawal. These drugs also have significant side effects when taken in large doses and can cause respiratory failure and death....
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Barbiturates (Encyclopedia of Drugs and Addictive Substances)
- Drugs and Fame
- How Is It Taken?
- Usage Trends
- Effects on the Body
- Reactions with Other Drugs or Substances
- Dream Time
- The Law
What Kind of Drug Is It?
Barbiturates (pronounced bar-BIH-chuh-rits) are drugs that act as and are used as sedativesA drug used to treat anxiety and calm people down. or sleeping pills. Because they are depressants, they are often called "downers." According to Lawrence Clayton in Barbiturates and Other Depressants, "Any depressant will kill if taken in a large enough quantity." Accidental overdose can occur quite easily among barbiturate users.
The effects of barbiturates are very similar to those of alcohol and include increased feelings of relaxation, sleepiness, and a decrease in . Barbiturates are habit-forming drugs and should not be used on an everyday basis. They can cause depression in high doses and addiction when taken over a long period of time.
Barbiturates have an extremely high potential for abuse. Ever since their introduction in the early 1900s, barbiturates have been considered addictive drugs. Barbiturates slow down both the mind and the body. In his book A Brief History of Drugs: From the Stone Age to the Stoned Age, Antonio Escohotado pointed to their "high capacity to produce numbness" by putting the user in a state somewhere between drunkenness and sleep. Aside from those effects, he continued, is their "almost inevitable ability to kill in high doses: a detail that converted these drugs into the most common means of committing suicide" from the 1940s through the 1960s.
Discovered in the 1860s
The story of barbiturates began "when a chemist combined animal urine and acid from apples," explained Clayton. That chemist was German professor and future Nobel prizewinner Adolf von Baeyer (1835917). The substance he created became known as barbituric (bar-bih-CHUR-ik) acid. It received its name because Baeyer first produced it on St. Barbara's Day (a day of religious recognition observed each year on December 4) of 1863.
Following Baeyer's discovery, two German researchers, Dr. Joseph von Mering (1849908) and Nobel prizewinner Emil Hermann Fischer (1852919), produced barbital, the first barbiturate. Barbiturates are compounds derived from barbituric acid. Doctors recognizedbarbital'ssleep-enhancingeffectsasfar back as 1882. More than twenty years later, in 1903, barbital was marketed as a sleeping pill under the brand name Veronal. The second barbiturate, phenobarbital, arrived on the scene in 1912 under the name Luminal. Since then, several thousand barbituric acid-type drugs have been . At the beginning of the twenty-first century, only about twelve were still being used.
Barbiturates were found to reduce the activity of nerves that control emotions and bodily functions such as breathing. Because of the drugs' soothing effects, they were commonly prescribed as sedatives for nearly fifty years. Other uses include epilepsyA disorder involving the misfiring of electrical impulses in the brain, sometimes resulting in seizures and loss of consciousness. treatment and anesthesia before surgery.
Intoxicating Effects Lead to Abuse
During the 1930s, many Americans received barbiturate prescriptions to help them sleep or relax. Barbiturates quickly gained a reputation as an intoxicant, a substance that makes users seem drunk. People began taking barbiturates as recreational drugs. They also began the dangerous practice of combining the pills with alcohol to increase the intoxication.
The 1938 Food, Drug, and Cosmetic Act gave authority over drug production to the U.S. Food and Drug Administration (FDA). The federal agency used those powers to restrict access to drugs that had a potential for abuse or misuse. The use of barbiturates without a medical doctor's prescription became illegal in the United States. But that didn't keep the drugs from becoming more and more popular throughout the 1940s.
At that time, researchers in the United States and the United Kingdom began noticing a disturbing trend. Over the years, the production of barbiturates had grown from thousands to millions of doses per year. Higher rates of barbiturate production and consumption seemed to coincide with a growing number of deaths from barbiturate poisoning. As late as 1964, Joel Fort, author of "The Problem of Barbiturates in the United States of America," argued against the wide availability of barbiturates. "Despite conclusive evidence to the contrary," he wrote, "many physicians in the United States appear to think and act as though barbiturates are completely harmless drugs that can be prescribed in unlimited quantities." His report was prepared for the United Nations Office on Drugs and Crime.
Downers and Uppers
The pairing of barbiturates with became a significant problem throughout the United States in the 1940s and 1950s. It all began when record numbers of people started taking barbiturates to help them sleep at night. To counteract the grogginess and lack of energy they suffered the next morning, users would take amphetamines to help them wake up. Amphetamines are stimulantsA substance that increases the activity of a living organism or one of its parts. or "uppers." At night, users still "up" from an amphetamine HIGH would take "downers," or barbiturates, to rid themselves of their extra energy and get to sleep. The next day the drug-taking cycle would start again. The regular use of barbiturates with amphetamines was so widespread by the 1950s that the U.S. government classified them as the most abused drugs in the country.
New Generation, New Drugs
During the 1960s, a new generation of young people began experimenting with a wide variety of mind-altering substances. Barbiturates were among the drugs abused by these new users, mainly because the pills were widely available and frequently used by the generation that came before themheir parents. According to the 1972 Consumers Union Report on Licit and Illicit Drugs, 10 billion barbiturate doses were scheduled for production in 1969 alone. That figure represented an 800-percent increase in the amount produced twentyseven years earlier in 1942.
Passage of the Controlled Substances Act (CSA) in 1970 restricted access to barbiturates in the United States. Another category of anti-anxiety drugs, the benzodiazepines (pronounced ben-zoh-die-AZ-uh-peenz), were promoted as a safer alternative to
barbiturates. Prescriptions for benzodiazepines rose because health providers considered them less addictive than barbiturates, with a lower risk of accidental overdose among users. As barbiturates became harder to obtain, drug abusers turned to other illegal substances during the 1970s and 1980s. U.S. Drug Enforcement Administration (DEA) reports indicate that the use of marijuana, heroin, and cocaine began to rise after 1970.
What Is It Made Of?
Barbiturates are compounds derived from barbituric acid, a substance made from carbon, hydrogen, nitrogen, and oxygen. The uric acid portion of the name is taken from the main ingredient in urine, which provides the basis for barbituric acid.
Barbiturate users often refer to the pills they take in terms of the color of the capsule. These street names include blues or blue dolls for Amytal; reds, red birds, or red devils for Seconal; yellows or yellow jackets for Nembutal; purple hearts for Luminal; and rainbows for Tuinal.
How Is It Taken?
In the United States, barbiturates are manufactured in various forms. Most barbiturates come in pills and capsules that patients swallow. Some are available as liquids that are swallowed. Others are produced in injectable forms. Some abusers have been known to mix up their own injectable liquid barbiturates by crushing pills and combining the powdered drug with water.
Drugs made from barbituric acid are classified in one of four categories: ultrashort-, short-, intermediate-, or long-acting. These categories are defined by the amount of time that it takes for the barbiturate to produce effects in the user and how long those effects last.
DEA reports indicate that drug abusers favor short- and intermediate-acting barbiturates. These types of barbiturates take effect within fifteen to forty minutes of being swallowed, and their depressant effects last from five to six hours. Drugs in this category include amobarbital, aprobarbital, butabarbital, pentobarbital, and secobarbital.
Are There Any Medical Reasons for Taking This Substance?
For many years, barbiturates were used as daytime sedatives. Since the discovery of another type of anti-anxiety drug called benzodiazepine, which is considered safer, barbiturates are not prescribed for this purpose as frequently as they once were.
When combined with an aspirin or nonaspirin pain reliever and caffeine, the barbiturate butalbital is effective in treating severe pain. It is sometimes prescribed to relieve the pain associated with migraine headaches.
As of 2005, barbiturates were used primarily for presurgical and surgical anesthesia. They were being administered to patients in operating rooms under an anesthetist's care. They also continued to be used in the treatment of certain types of epilepsy.
Reactions to barbiturates range from mild sedation to coma and even death. Doctors may prescribe barbiturates as sedatives to calm patients' nerves, reduce tension, or help them sleep. The drugs are also used as an anticonvulsant to control epileptic seizures. The sleep-producing action of barbiturates is used to relax and partially anesthetize patients before some surgical procedures.
At the close of the twentieth century, the DEA reported that barbiturates represented about 20 percent of all depressant prescriptions in the United States.
Barbiturate Use Down Since the Mid-1980s, Says SAMHSA
Recent surveys of drug abuse showed a sharp decline in barbiturate abuse since the mid-1980s. The National Survey on Drug
Use and Health (NSDUH), formerly known as the National Household Survey on Drug Abuse, is a carefully calculated assessment of American drug use. It is conducted by the Substance Abuse and Mental Health Services Administration (SAMHSA) and obtains information on nine different categories of illicit drug use. As of 2005, the latest results available were from the 2003 survey. All of the respondents to the survey were over the age of twelve. They were asked to report "only uses of drugs that were not prescribed for them or drugs they took only for the experience or feeling they caused." Over-the-counter drugs and legitimate uses of prescription drugs were not included.
According to the 2003 NSDUH summary, prescription-type sedatives were placed in a category called "psychotherapeutic drugs." This category also included tranquilizersDrugs such as Valium and Librium that treat anxiety; also called benzodiazepines (pronounced ben-zoh-die-AZ-uhpeens)., pain relievers, and stimulants. About 300,000 Americans over the age of twelve reported using sedatives without a prescription. The authors of the survey noted that "the number of first-time sedative users rose steadily during the late 1960s and early 1970s, and then declined during the early 1980s, remaining below 250,000 per year since 1984." The 2003 estimates were all similar to the corresponding estimates for 2002.
Monitoring the Future Results
The results of the 2004 Monitoring the Future (MTF) study were released to the public on December 21, 2004. Conducted by the University of Michigan (U of M), it was sponsored by research grants from the National Institute on Drug Abuse (NIDA). Like the NSDUH results regarding sedative use from 2002 and 2003, the MTF survey results indicate that barbiturate use among twelfth-grade students held steady between 2003 and 2004.
Effects on the Body
Barbiturates are classified as ultrashort-, short-, intermediate-, and long-acting, depending on how quickly they act and how long their effects last. Ultrashort barbiturates such as thiopental (Pentothal) produce unconsciousness within about a minute of (IV) injection. These drugs are used to prepare patients for surgery; other general anestheticsA substance used to deaden pain. like nitrous oxide are then used to keep the patient from waking up before the surgery is complete. Because Pentothal and other ultrashort-acting barbiturates are typically used in hospital settings, they are not very likely to be abused, noted the DEA.
Abusers tend to prefer short-acting and intermediate-acting barbiturates. The most commonly abused are amobarbital (Amytal), pentobarbital (Nembutal), and secobarbital (Seconal). A combination of amobarbital and secobarbital (called Tuinal) is also highly abused. Short-acting and intermediate-acting barbiturates are usually prescribed as sedatives and sleeping pills. These pills begin acting fifteen to forty minutes after they are swallowed, and their effects last from five to six hours. Veterinarians use pentobarbital to anesthetize animals before surgery; in large doses, it can be used to euthanize animals.
Long-acting barbiturates such as phenobarbital (Luminal) and mephobarbital (Mebaral) are prescribed for two main reasons. When taken at bedtime, they help treat . When taken during the day, they have sedative effects that can aid in the treatment of tension and anxiety. These same effects have been found helpful in the treatment of convulsive conditions like epilepsy. Long-acting barbiturates take effect within one to two hours and last twelve hours or longer.
Similar to Alcohol
recreational usersUsing a drug solely to achieve a high, not to treat a medical condition. report that a barbiturate high makes them feel "relaxed, sociable, and good-humored," according to an Independent article. Users typically describe feelings of decreased anxiety, a loss of inhibitions, and an increased sense of confidence. Physical effects include slowed breathing and a lowering of both blood pressure and heart rate.
Like alcohol, barbiturates are intoxicating. During the stage after mild , the user's speech may be slurred and a loss of coordination may become noticeable. Stumbling and staggering are common. Other symptoms include shallow breathing, fatigue, frequent yawning, and irritability.
When taken in high doses, barbiturates can cause serious side effects, including "unpredictable emotional reactions and mental confusion," noted the Independent. Judgment becomes severely impaired and the user may experience mood swings.
The mental effects of barbiturates generally depend on the amount of the drug taken and the strength of the dosage. Generally, a person falls asleep when taking a prescribed dosage at bedtime. But barbiturates remain in the system for a long time. "At normal doses," explained Cynthia Kuhn and her coauthors in Buzzed: The Straight Facts about the Most Used and Abused Drugs from Alcohol to Ecstasy, "the major concern is that they can have sedative effects that outlast their sleep-inducing properties Driving, flying an airplane, or other activities requiring muscle coordination can be impaired for up to a day after a single dose." Some barbiturates can be detected in a user's urine sample days or even weeks after the drug was consumed.
Dependence, Tolerance, and Overdose
Barbiturate use can lead to both psychological and physical dependence. Psychological addiction can occur quickly. Signs of drug dependence include relying on a drug regularly for a desired effect. The addicted abuser believes he or she must take a barbiturate to sleep, relax, or just get through the day. Continued use of barbiturates leads to physical dependence.
As people develop a for barbiturates, they may need more of the drug or a higher dosage to get the desired effect. This can lead to an overdose, which results when a person takes a larger-than-prescribed dose of a drug. "People who get in the habit of taking sleeping pills every night to fall sleep," noted Andrew Weil and Winifred Rosen in From Chocolate to Morphine, "might start out with one a night, progress to two, then graduate to four to get the same effect. One night the dose they need to fall asleep might also be the dose that stops their breathing." Generally, barbiturate overdoses "occur because the effective dose of the drug is not too far away from the lethal dose," explained Dr. Eric H. Chudler on the Neuroscience for Kids Web site.
Symptoms of an overdose typically include severe weakness, confusion, shortness of breath, extreme drowsiness, an unusually slow heartbeat, and darting eye movements. The amount of a fatal dosage of barbiturate varies from one individual to another. However, the lethal dose is usually ten to fifteen times as large as a usual dose. An overdose affects the heart and the respiratory system. The user then falls into a coma and dies.
Clayton pointed out that barbiturates "can have a 'multiplying' effect when taken with other depressants. For example, if someone drinks alcohol and takes a barbiturate, the effect may be ten times stronger than either one taken separately." According to Weil, "many people have died because they were ignorant of this fact."
Older adults and pregnant women should consider the risks associated with barbiturate use. When a person ages, the body becomes less able to rid itself of barbiturates. As a result, people over the age of sixty-five are at higher risk of experiencing the harmful effects of barbiturates, including drug dependence and accidental overdose. When barbiturates are taken during pregnancy, the drug passes through the mother's bloodstream to her fetus. After the baby is born, it may experience withdrawalThe process of gradually cutting back on the amount of a drug being taken until it is discontinued entirely; also the accompanying physiological effects of terminating use of an addictive drug. symptoms and have trouble breathing. In addition, nursing mothers who take barbiturates may transmit the drug to their babies through breast milk.
Reactions with Other Drugs or Substances
People who abuse inhalants run a very high risk of overdose if they consume barbiturates while on an inhalant high. are also especially dangerous when combined with barbiturates. Barbiturates should not be mixed with alcohol or other drugs, including tranquilizers, muscle relaxants, antihistamines, cold medicines, allergy medicines, and certain pain relievers. The use of barbiturates by people suffering from depression may pose an increased risk of suicide. Children or adults diagnosed with attention-deficit/hyperactivity disorder (ADHD)A disorder characterized by impulsive behavior, difficulty concentrating, and hyperactivity that interferes with social and academic functioning. may experience increased excitability rather than a calming effect when given barbiturates. In addition, these drugs may lower the effectiveness of birth control pills that contain estrogen. Unless they use a barrier-type form of birth control, women taking oral contraceptives may become pregnant while taking barbiturates.
Treatment for Habitual Users
When addicted users stop taking barbiturates, their bodies must adapt to the lack of drugs in their systems. This process is known as withdrawal. If the users have taken barbiturates in large doses or for an extended period of time, a physician should be consulted about the withdrawal process. An attempt to withdraw abruptly from barbiturates can be fatal.
Withdrawal symptoms usually begin eight to sixteen hours after the last pill was taken. Symptoms in users with a long history of barbiturate use may last up to fifteen days, but the severity of the symptoms decreases as the body rids itself of the drug. During withdrawal, users feel anxious, weak, dizzy, and nauseated. They may also experience shakes, tremors, and even seizures. In addition, users could possibly have and become violent or hostile.
In some cases, withdrawal symptoms can be deadly. A physician must establish a plan of gradual withdrawal from this type of drug, usually decreasing the dosage by about 10 percent each day over a ten-day to two-week period. The withdrawal process may occur in a hospital, or treatment may be given on an outpatient basis. Either way, counseling is vital. Users who are treated successfully for their physical addiction must follow through with psychological rehabilitation. Behavioral treatment helps former users avoid barbiturates so
they can remain drug free even when faced with cravings. Long-term support can be found in twelve-step programs and other support groups that meet regularly.
Barbiturates are used to treat anxiety, sleeplessness, muscular tension, and pain. Their calming effect has a serious downside, though. Barbiturates lessen the brain's control over breathing. Respiratory failure is the primary cause of death in cases of barbiturate overdose. Gahlinger pointed out that "since barbiturates reduce the amount of oxygen reaching the brain, the overdosing person who survives may be left with permanent brain damage."
Barbiturate users can develop a tolerance for the drug. As the body becomes used to the presence of barbiturates in the system, the prescribed dose of the drug may lose its effectiveness. Habitual users may find themselves taking more and more pills in stronger and stronger dosages to achieve the effect they once attained on a low dosage of the drug. This cycle often leads to accidental overdose.
Prolonged barbiturate use can shorten a person's attention span and result in memory loss. Both conditions would make it difficult for a person to do well in school or perform on a job. In addition, barbiturates affect the judgment of those who use them, increasing the likelihood of risky behavior. Users of barbiturates are sometimes tempted to drive while drunk because they know that police will not smell alcohol on their breath.
Taking barbiturates to ease depression "is probably the riskiest way of using them," cautioned Weil. Although these drugs may improve the user's mood temporarily, "over time they often increase anxiety and depression, encouraging further drug-taking in a downward spiral that can end in suicide."
When barbiturates first became available in the United States, they could be purchased without a prescription. It did not take long, however, for lawmakers to realize that barbiturates were addictive. On their own, some state governments adopted laws in the mid-1930s that banned the sale of nonprescription barbiturates. In 1938, the U.S. government stepped in, passing the U.S. Food, Drug, and Cosmetics Act. This act gave the FDA regulatory power over new drugs, including barbiturates. This means that drug companies would have to apply to the FDA for approval to manufacture such drugs. Once approved, the FDA would determine whether a new drug would require a medical doctor's prescription.
For more than thirty years, until the passage of the Controlled Substances Act (CSA) of 1970, barbiturates were still widely abused. Under the stiffer terms of the CSA, barbiturates became controlled substances. In other words, their use is regulated by certain federal laws. The CSA called for the assignment of all controlled drug substances into one of five categories called schedules. These schedules are based on a substance's medicinal value, possible harmfulness, and potential for abuse and addiction. Schedule I is reserved for the most dangerous drugs that have no recognized medical use.
Various barbiturates fall into three different schedules: Schedule II, Schedule III, and Schedule IV. Drugs in all of these categories cannot be obtained legally without a medical doctor's prescription. Schedule II drugs are dangerous substances with genuine medical uses that also have a high potential for abuse and addiction. They are accepted for medical use with restrictions. These drugs may lead to severe psychological or physical dependence. Barbiturates in this category include amobarbital (Amytal), pentobarbital (Nembutal), and secobarbital (Seconal and Tuinal).
Schedule III drugs have less of a potential for abuse than drugs placed in Schedules I and II. The drugs have real medical uses, but their abuse can still lead to in those who take them. Barbiturates in this category include aprobarbital (Alurate), butabarbital (Butisol), and butalbital (Fiorinal and Fioricet).
Schedule IV drugs have a low abuse potential when compared to Schedule III drugs. These substances have an accepted medical use, but some patients risk developing a psychological dependence on them. Schedule IV barbiturates include barbital (Veronal), mephobarbital (Mebaral), and phenobarbital (Luminal).
Fines and Jail Time
Possessing barbiturates without a prescription is against the law and can result in up to a year's imprisonment and/or thousands of dollars in fines. The length of the jail sentence and the amount of the fine are increased when a person is convicted of a second or third offense of barbiturate possession. People convicted of distributing or selling barbiturates face lengthy prison terms and fines in the millions of dollars. Selling drugs is a dangerous business for both the buyer and the seller. Illegally distributed Schedule II drugs can kill or seriously injure a user. In cases such as these, the distributor or seller of the substance is considered partially responsible for the user's death and could end up with a lifetime jail sentence.
In the United Kingdom, drugs are regulated by the 1971 Misuse of Drugs Act and the 1986 Medicines Act. The 1971 act placed drugs in three classes: A, B, or C. The most dangerous drugs are called Class A drugs; the least dangerous drugs are in the C category.
Most barbiturates are considered Class B drugs throughout the United Kingdom. If they are used in an injectable form, however, they jump to a Class A rating. The maximum penalty for possession of a Class B drug under UK law is five years of prison, an unlimited fine, or a combination of jail time and a fine. Penalties for supplying or distributing Class B drugs are higher. For Class A drugs, the penalty for possession is seven years in prison, an unlimited fine, or both. The supply penalty for this class could land a seller in jail for life.
For More Information
Brecher, Edward M., and others. The Consumers Union Report on Licit and Illicit Drugs. Boston: Little Brown & Co., 1972.
Clayton, Lawrence. Barbiturates and Other Depressants. New York: Rosen Publishing Group, 1994.
Escohotado, Antonio. A Brief History of Drugs: From the Stone Age to the Stoned Age. Rochester, VT: Park Street Press, 1999.
Gahlinger, Paul M. Illegal Drugs: A Complete Guide to Their History, Chemistry, Use, and Abuse. Las Vegas, NV: Sagebrush Press, 2001.
Hughes, Richard, and Robert Brewin. The Tranquilizing of America. New York: Harcourt, 1979.
Hyde, Margaret O., and John F. Setaro. Drugs 101: An Overview for Teens. Brookfield, CT: Twenty-first Century Books, 2003.
Kuhn, Cynthia, Scott Swartzwelder, Wilkie Wilson, and others. Buzzed: The Straight Facts about the Most Used and Abused Drugs from Alcohol to Ecstasy, 2nd ed. New York: W.W. Norton, 2003.
Schull, Patricia Dwyer. Nursing Spectrum Drug Handbook. King of Prussia, PA: Nursing Spectrum, 2005.
Silverman, Harold M. The Pill Book, 11th ed. New York: Bantam, 2004.
Weil, Andrew, and Winifred Rosen. From Chocolate to Morphine. New York: Houghton Mifflin, 1993, rev. 2004.
Wolfe, Sidney. Worst Pills, Best Pills. New York: Pocket Books, 1999.
Barnett, Jim. "Feds Push Challenge to Assisted Suicide Law." Oregonian (November 10, 2004).
Johnson, Kevin, and Richard Willing. "Ex-CIA Chief Revitalizes 'Truth Serum' Debate." USA Today (April 26, 2002).
Schodolski, Vincent J. "U.S. Seeks to Bury Oregon Suicide Law." Knight Ridder/Tribune News Service (November 27, 2004): p. K6995.
"Sex, Drugs, and Rock 'n' Roll." Independent (January 28, 1996): p. 8.
Weathermon, Ron, and David W. Crabb. "Alcohol and Medication Inter-actions." Alcohol Research & Health, vol. 23, no. 1 (1999): pp. 40-54.
"2003 National Survey on Drug Use and Health (NSDUH)." U.S. Department of Health and Human Services, Substance Abuse and Mental Health Services Administration. http://www.oas.samhsa.gov/nhsda.htm (accessed June 30, 2005).
"Barbiturates." U.S. Department of Justice, Drug Enforcement Administration. http://www.usdoj.gov/dea/concern/barbiturates.html (accessed June 30, 2005).
Fort, Joel. "The Problem of Barbiturates in the United States of America." United Nations Office on Drugs and Crime. (accessed June 30, 2005).
Glatt, M. M. "The Abuse of Barbiturates in the United Kingdom." United Nations Office on Drugs and Crime. (accessed June 30, 2005).
Monitoring the Future. http://www.monitoringthefuture.org/ and http://www.nida.nih.gov/Newsroom/04/2004MTFDrug.pdf (both accessed June 30, 2005).
"Prescription Drugs: Abuse and Addiction." National Institute on Drug Abuse (NIDA) Research Report Series. http://www.drugabuse.gov/ResearchReports/Prescription/ (accessed June 30, 2005).
See also: Alcohol; Benzodiazepine; Tranquilizers
Barbiturates (World of Forensic Science)
The term barbiturate is a name given to a group of drugs that function by depressing the activity of the central nervous system. Their principal effect is to reduce stress and bring the user a feeling of calm. Often, this sedation can help someone fall asleep. This is why barbiturates are often termed sleeping pills.
Barbiturates were first made over a century ago by the Bayer laboratories in Germany. They take their name from barbital, which was the first barbiturate used medically, in the first decade of the twentieth century.
Aside from their stress relief, the nervous system alteration induced by barbiturates can also be beneficial in the management of diseases like epilepsy.
Of the dozen or so barbiturates still in common medical use, the speed at which the effects are produced and the length of time the effects persist are the distinguishing features between the drugs.
Some barbiturates produce an effect within seconds of being taken. Others require more time to act but last longer. Finally, those used for sedation before an operation can last for hours.
Barbiturates are important to forensic scientists when they are present in blood samples in excess amounts. This can occur accidentally, since the effective dose of many of the drugs is not too different from a dose that causes harm. One well-known victim of an accidental overdose of sleeping pills was the musician Jimi Hendrix. As well, a barbiturate overdose can be deliberately administered. When present in excessive amounts, the drugs can cause debilitating changes. Sedation can even be so severe that coma and death result.
Forensic investigators can be interested in determining if barbiturates were a factor in someone's illness or death. Recollections of the victim's behavior can be helpful in determining the involvement of barbiturates. For example, side effects of an overdose include slurred speech and unsteady balance. Admittedly, these are also symptoms of excessive alcohol consumption.
More definitive evidence of barbiturate use comes from the chemical demonstration of the drug in tissue samples. Because most barbiturates tend to accumulate in fat deposits in the body, to be released at varying rates depending on the specific drug, a barbiturate may be detectable in tissue specimens recovered even some time after death.
SEE ALSO Amphetamines; Analytical instrumentation; Autopsy; Death, cause of; Narcotic; Psychotropic drugs.
Barbiturates (Encyclopedia of Drugs, Alcohol, and Addictive Behavior)
Barbiturates refer to a class of general central nervous system depressants that are derived from barbituric acid, a chemical discovered in 1863 by the Nobel Prize winner in chemistry (1905) Adolf von Baeyer (1835-1917). Barbituric acid itself is devoid of central depressant activity; however, German scientists Emil Hermann Fischer and Joseph von Mering made some modifications to its structure and synthesized barbital, which was found to possess depressant properties. Scientists had been looking for a drug to treat anxiety and nervousness but without the dependence-producing effects of OPIATE drugs such as OPIUM, CODEINE, and MORPHINE. Other drugs such as bromide salts, CHLORAL HYDRATE, and paraldehyde were useful sedatives, but they all had problems such as toxicity or they left such a bad taste in patients' mouths that they preferred not to take them. Fischer and von Mering noted that barbital produced sleep in both humans and animals. It was introduced into chemical medicine in 1903 and was soon in widespread use.
By 1913, the second barbiturate, PHENOBARBI-TAL, was introduced into medical practice. Since that time, more than 2,000 similar chemicals have been synthesized but only about 50 of these have been marketed. Although the barbiturates were quickly used to treat a number of disorders effectively, their side effects were becoming apparent. The chief problem, an overdose, can result in respiratory depression, which can be fatal. By the mid-1950s, more than 70 percent of admissions to a poison-control center in Copenhagen, Denmark, involved barbiturates. Additionally, it became apparent that the barbiturates were subject to abuse, which could lead to dependence, and that a serious withdrawal syndrome could ensue when the drugs were abruptly discontinued. In the 1960s, the introduction of a safer class of hypnotic drugs, the BENZODIAZEPINES reduced the need for barbiturates.
Barbiturates are dispensed in distinctly colored capsules making them very easy to identify by the lay public. In fact, users within the drug culture often refer to the various barbiturates by names associated with their physical appearance. Examples of these names include blue birds, blue clouds, yellow jackets, red devils, sleepers, pink ladies, and Christmas trees. The term goofball is often used to describe barbiturates in general. All barbiturates are chemically similar to barbital, the structure of which is shown in Figure 1.
All barbiturates are general central nervous system depressants. This means that sedation, sleep, and even anesthesia will develop as the dose is increased. Some barbiturates also are useful in reducing seizure activity and so have been used to treat some forms of epilepsy. The various barbiturates differ primarily in their onset and duration of
EFFECTS ON THE BODY AND THERAPEUTIC USES
Barbiturates affect all excitable tissues in the body. However, NEURONS are more sensitive to their effects than other tissues. The depth of central nervous system depression ranges from mild sedation to coma and depends on many factors including which drug is used, its dose, the route of administration, and the level of excitability present just before the barbiturate was taken. The most common uses for the barbiturates are still to promote sleep and to induce anesthesia. Barbiturate-induced sleep resembles normal sleep in many ways, but there are a few important differences. Barbiturates reduce the amount of time spent in rapid eye movement or REM sleep very important phase of sleep. Prolonged use of barbiturates causes restlessness during the late stages of sleep. Since the barbiturates remain in our bodies for some time after we awaken, there can be residual drowsiness that can impair judgment and distort moods for some time after the obvious sedative effects have disappeared. Curiously, some people are actually excited by barbiturates, and the individual may even appear inebriated. This paradoxical reaction often occurs in the elderly and is more common after taking phenobarbital.
The general use of barbiturates as hypnotics (SLEEPING PILLS) has decreased significantly, since they have been replaced by the safer benzodiazepines. Phenobarbital and butabarbital are still available, however, as sedatives in a number of combination medications used to treat a variety of inflammatory disorders. These two drugs also are used occasionally to antagonize the unwanted overstimulation produced by ephedrine, AMPHETAMINE, and theophylline.
Since epilepsy is a condition of abnormally increased neuronal excitation, any of the barbiturates can be used to treat convulsions when given in anesthetic doses; however, phenobarbital has a selective anticonvulsant effect that makes it particularly useful in treating grand mal seizures. This selective effect is shared with mephobarbital and metharbital. Thus, phenobarbital is often used in hospital emergency rooms to treat convulsions such as those that develop during tetanus, eclampsia, status epilepticus, cerebral hemorrhage, and poisoning by convulsant drugs. The benzodiazepines are, however, gradually replacing the barbiturates in this setting as well.
It is not completely understood how barbiturates work but, in general, they act to enhance the activity of GABA on GABA-sensitive neurons by acting at the same receptor on which GABA exerts its effects (see Figure 2). GABA is a NEUROTRANSMIT-TER that normally acts to reduce the electrical activity of the brain; its action is like a brake. Thus, barbiturates enhance the braking effects of GABA to promote sedation. There is an area in the brain called the reticular activating system, which is responsible for maintaining wakefulness. Since this area has many interconnecting or polysynaptic neurons, it is the first to succumb to the barbiturates, and that is why an individual becomes tired and falls asleep after taking a barbiturate.
PHARMACOKINETICS AND DISTRIBUTIONThe ultrashort-acting barbiturates differ from the other members of this class mainly by the means by which they are inactivated. Methohexital and its relatives are very soluble in lipids (i.e., fatty tissue). The brain is composed of a great deal of
The other longer-acting barbiturates must be metabolized by the liver into inactive compounds before the effects wane. Since these metabolites are more soluble in water, they are excreted through the kidneys and into the urine. As is the case with most drugs, metabolism and excretion is much quicker in young adults than in the elderly and infants. Plasma half-lives are also increased in pregnant women because the blood volume is expanded due to the development of the placenta and fetus.
TOLERANCE, DEPENDENCE, AND ABUSE
Repeated administration of any number of drugs results in eventual compensatory changes in the body. These changes are usually in the opposite direction of those initially produced by the drug such that more and more drug is needed to achieve the initial desired effect. This process is called TOLERANCE. There are two basic mechanisms for tolerance development: tissue tolerance and metabolic or pharmacokinetic tolerance. Tissue tolerance refers to the changes that occur on the tissue or cell that is affected by the drug. Metabolic tolerance refers to the increase in the processes that metabolize or break down the drug. This process generally occurs in the liver. Barbiturates are subject to both types of tolerance development.
Tolerance does not develop equally in all effects produced by barbiturates. Barbiturate-induced respiratory depression is one example. Barbiturates reduce the drive to breathe and the processes necessary for maintaining a normal breathing rhythm. Thus, while tolerance is quickly developing to the desired sedative effects, the toxic doses change to a lesser extent. As a result, when the dose is increased to achieve the desired effects (e.g., sleep), the margin of safety actually decreases as the dose comes closer to producing toxicity. A complete cessation of breathing is often the cause of death in barbiturate poisoning (Rall, 1990).
If tolerance develops and the amount of drug taken continues to increase, then PHYSICAL DEPENDENCE can develop. This means that if the drug is suddenly stopped, the tissues' compensatory effects become unbalanced and withdrawal signs appear. In the case of barbiturates, mild signs of withdrawal include apprehension, insomnia, excitability, mild tremors, and loss of appetite. If the dose was very high, more severe signs of withdrawal can occur, such as weakness, vomiting, decrease in blood pressure regulatory mechanisms (so that pressure drops when a person rises from a lying position, called orthostatic hypotension), increased pulse and respiratory rates, and grand mal (epileptic) seizures or convulsions. DELIRIUM with fever, disorientation, and HALLUCINATIONS may also occur. Unlike withdrawal from the opioids, withdrawal from central nervous system depressants such as barbiturates can be life threatening. The proper treatment of a barbiturate-dependent individual always includes a slow reduction in the dose to avoid the dangers of rapid detoxification.
Few, if any, illegal laboratories manufacture barbiturates. Diversion of licit production from pharmaceutical companies is the primary source for the illicit market. Almost all barbiturate users take it by mouth. Some try to dissolve the capsules and inject the liquid under their skin (called skin-popping) but the toxic effects of the alcohols used to dissolve the drug and the strong alkaline nature of the solutions can cause lesions of the skin. Intravenous administration is a rare practice among barbiturate abusers.
Many barbiturate users become dependent to some degree during the course of treatment for insomnia. This type of problem is called iatrogenic, because it is initiated by a physician. In some instances the problem will be limited to continued use at gradually increasing doses at night, to prevent insomnia that is in turn due to withdrawal. However, some individuals who are susceptible to the euphoric effects of barbiturates may develop a pattern of taking increasingly larger doses to become intoxicated, rather than for the intended therapeutic effects (for example, to promote sleepiness). To achieve these aims, the person may obtain prescriptions from a number of physicians and take them to a number of pharmacistsr secure their needs from illicit distributors (dealers). If the supply is sufficient, the barbiturate abuser can rapidly increase the dose within a matter of weeks. The upper daily limit is about 1,500 to 3,000 milligrams; however, many can titrate their daily dose to the 800 to 1,000 milligram range such that the degree of impairment is not obvious to others. The pattern of abuse resembles that of ethyl (drinking) ALCOHOL, in that it can be daily or during binges that last from a day to many weeks at a time. This pattern of using barbiturates for intoxification is more typically seen in those who, from the beginning, obtain barbiturates from illicit sources rather than those who began by seeking help for insomnia.
Barbiturates are sometimes used along with other drugs. Often, the barbiturate is used to potentiate, or boost, the effects of another drug upon which a person is physically dependent. Alcohol and HEROIN are commonly taken together in this way. Since barbiturates are "downers," they also are used to counteract the unwanted overstimulation associated with stimulant-induced intoxication. It is not uncommon for stimulant abusers (on COCAINE or amphetamines) to use barbiturates to combat the continued "high" and the associated motor disturbances associated with heavy and continued cocaine use. Also, barbiturates are used to ward off the early signs of withdrawal from alcohol.
Treatment for barbiturate dependence is often conducted under carefully controlled conditions, because of the potential for severe developments, such as seizures. Under all conditions, a program of supervised withdrawal is needed. Many years ago, pentobarbital was used for this purpose and the dose was gradually decreased until no drug was given. More recently, phenobarbital or the benzodiazepinesHLORDIAZEPOXIDE and diazepamave been used for their greater margin of safety. The reason that the benzodiazepines sometimes work is because the general central nervous system depressantsarbiturates, alcohol, and benzodiazepinesevelop cross-dependence to one another. Thus a patient's barbiturate or alcohol withdrawal signs are reduced or even eliminated by diazepam.
(SEE ALSO: Addiction: Concepts and Definitions; Withdrawal)
CSY, T. Z. (1979). Cutting's handbook of pharmacology: The actions and uses of drugs, 6th ed. New York: Appleton-Century Crofts.
HENNINGFIELD, J. E., & ATOR, N. A. (1986). Barbiturates: Sleeping potion or intoxicant? In The encyclopedia of psychoactive drugs. New York: Chelsea House.
MENDELSON, J. H., & MELLO, N. K. (1992). Medical diagnosis and treatment of alcoholism. New York: McGraw-Hill.
RALL, T. W. (1990). Hypnotics and sedatives: Ethanol. In A. G. Gilman et al. (Eds.), Goodman and Gilman's the pharmacological basis of therapeutics, 8th ed. New York: Pergamon.
WINGER, G., HOFFMAN, F.G., & WOODS, J. H. (1992). A handbook of drugs and alcohol abuse: the biomedical aspects, 3rd ed. New York: Oxford University Press.
SCOTT E. LUKAS