Tranquilizers - Overview

Overview

In general, tranquilizers fall into two categories: major tranquilizers and minor tranquilizers. Major tranquilizers are drugs used to treat severe mental illnesses, such as schizophrenia and psychosis (sy-KOH-sis). A mental disease, schizophrenia causes patients to withdraw from reality and suffer other intellectual and emotional disturbances. Psychosis is a severe mental disorder that often causes hallucinations, or visions, and makes it difficult for people to distinguish what is real from what is imagined. Major

Various herbs are used as tranquilizers. DK Limited/Corbis.
Various herbs are used as tranquilizers. © DK Limited/Corbis.

tranquilizers are more commonly called neuroleptics or antipsychotics. These drugs help decrease the symptoms of serious psychiatric disorders by targeting areas of the brain that deal with emotion. They are not typically abused by patients.

Minor tranquilizers, also known as sedative-hypnotic or anxiolytic drugs, are a group of medications that are prescribed to treat sleep and anxiety disorders. Although different sedative-hypnotic and anxiolytic drugs work in the brain in slightly different ways, they all produce a calming effect that is beneficial to patients who cannot sleep or who suffer from severe anxiety attacks. These drugs are among the most abused in the United States.

Minor tranquilizers can also be broken down into two main categories: barbiturates, which are used to treat anxiety, tension, and sleep disorders; and benzodiazepines (BZDs), which can be prescribed to treat anxiety, severe stress reactions, and panic attacks. Panic attacks are unexpected episodes of severe anxiety that can cause shortness of breath, dizziness, sweating, and shaking. (Entries on barbiturates and benzodiazepines are included in this encyclopedia.) The main difference between the two groups is that BZDs target specific receptors (groups of cells that receive stimuli) in the brain instead of affecting the entire brain. Therefore, BZDs do not produce many of the negative side effects associated with major tranquilizers or barbiturates, such as impaired judgment or breathing problems. Most tranquilizers and sleeping pills prescribed as of 2005 belonged to the BZD chemical group because of their higher safety ratings. The best-known examples of BZDs are Ativan, Halcion, Librium, Valium (VAL-eum), and Xanax (ZAN-ex).

History

In some form or another, tranquilizers have been around since ancient times. Virtually every culture discovered the sedative effects of certain herbs and plants growing in nature. (A separate entry on herbal drugs is available in this encyclopedia.) Through years of trial and error, these cultures were able to identify specific plants that—when prepared a particular way—could have a tranquilizing effect. By drying these plants or their roots and grinding them into food or mixing them with liquids, herbalists found that the substances could relieve stress, insomnia, and the symptoms of severe mental disorders in people who consumed them.

Major Tranquilizers

The first major tranquilizer was developed from Rauwolfia serpentina, also known as the Indian snakeroot. Rauwolfia is known for its ability to lower blood pressure. Used for many years in India for the treatment of serious mental illness, it was frequently referred to there as the "insanity herb." Most often, its roots were crushed and consumed in a tea. In 1943 an Indian physician named Rustom Jal Vakil (1911–1974) wrote about the plant's success in treating mental illness. It wasn't long before Western doctors began studying Rauwolfia, hoping that it could help patients with severe psychiatric disorders.

American doctor Robert Wallace Wilkins (1906–2003) of Boston University Medical School conducted extensive research on Rauwolfia serpentina after hearing about its use in India. In 1954, he showed that reserpine, an alkaloidA nitrogen-containing substance found in plants. and the active ingredientThe chemical or substance in a compound known or believed to have a therapeutic, or healing, effect. in Rauwolfia, was successful in treating both high blood pressure and severe psychiatric disorders such as schizophrenia and other psychoses. Almost immediately the new drug (sold under the brand name Serpasil) became the most popular way to treat such disorders.

Wilkins' work inspired further research, which resulted in the development of other drugs used as major tranquilizers. With neuroleptic and antipsychotic drugs came the possibility that mentally ill patients would not have to spend their lives committed

Patients at a mental hospital lie down as they experience the effects of reserpine in 1957. Without the drug, however, they might have to be put in restraints. Reserpine was the first major tranquilizer. Bettmann/Corbis.
Patients at a mental hospital lie down as they experience the effects of reserpine in 1957. Without the drug, however, they might have to be put in restraints. Reserpine was the first major tranquilizer. © Bettmann/Corbis.

to institutions and under a doctor's strict supervision. Instead, they could return to their homes and families as long as they followed prescribed drug therapy and other treatment.

Minor Tranquilizers

Herbs such as valerian, kava, and lavender produce tranquilizing effects and have been used by various cultures for centuries. There were no alternatives to natural tranquilizers until the 1860s, when the first synthetic minor tranquilizer, bromide, was created. (Synthetic drugs are those created in a laboratory.) But the dangerous side effects it produced made it rather unpopular. The drug caused stomach problems and, if taken for a long time, proved toxic (harmful or poisonous). Bromides were replaced by barbiturates in 1903. Barbiturates are effective in reducing anxiety and causing drowsiness, but can very quickly become addictive or habit-forming. Amytal, Nembutal, and Seconal are all examples of barbiturates.

The danger with barbiturates is the high rate of death connected with overdose. An overdose of barbiturates affects the heart and the respiratory system, causing shortness of breath, extreme drowsiness, and an unusually slow heart rate. The user then slips into a comaA state of unconsciousness from which a person cannot be aroused by noise or other stimuli. and dies. Because of this, chemists knew they had to find an alternative to barbiturates—a drug that could ease anxiety without slowing breathing rates to dangerously low levels. The answer came with the discovery of benzodiazepines.

Drug Therapy Replaces Radical Treatments for Mental Illness

Reserpine was the first drug developed to treat patients with severe psychiatric problems, such as: schizophrenia; paranoia—having abnormal feelings of suspicion and fear; and hallucinations—having visions or seeing things that are not really present. Before reserpine, psychiatric patients suffering from severe mental illnesses had to endure radical treatments. These included: 1) insulin shock therapy, in which a doctor injects the patient with insulin, making blood sugar levels fall so low that the patient becomes comatose, or unconscious; 2) electroconvulsive (ECT) therapy, in which a patient is shocked with electricity; and 3) lobotomy, a surgical procedure that actually removes part of the brain. It is easy to see why the development of reserpine was viewed as a revolutionary treatment for psychiatric patients.

Because of its positive effects in treating not only psychiatric disorders but also high blood pressure, reserpine quickly became a very popular drug. Reserpine lowers high blood pressure in two ways. First, it decreases the heart rate. Second, it opens up blood vessels to improve the flow of blood throughout the body. According to the MedlinePlus Web site, the drug was still being used for this purpose in the early 2000s. However, as of 2005, it was no longer considered the drug of choice for treating patients with mental disorders.

Doctors and researchers soon realized that although the drug was useful in calming upset psychotic patients—those experiencing a dangerous loss of contact with reality that could lead to violence—it caused severe depression in others. There were also other negative side effects, including nightmares, stomach problems, and parkinsonism (PAR-kin-son-izm), which is a disorder of the nervous system that resembles Parkinson's disease. Symptoms of parkinsonism include overall weakness, partial paralysis of the face, trembling hands, and a slowed, shuffling walk. As a result, reserpine has been largely replaced in psychiatric use by other major tranquilizers.

In 1954, Austrian scientist Dr. Leo Sternbach (1908–2005) discovered the first benzodiazepine while conducting research on chemical compounds for the New Jersey-based Hoffmann-La Roche drug company. He did not recognize the importance of his discovery until 1957, when he realized that one of his compounds would make a great tranquilizer. Known as RO 5-0690, the drug eventually became Librium. Sternbach also developed Valium in 1963. Over time, BZDs became popular drugs for the treatment of anxiety and sleep disorders.

Leo Sternbach, the chemist who created Valium, poses with his wife, Herta, in 2003. Sternbach was working with Hoffmann-La Roche when he created the popular tranquilizer. AP/Wide World Photos.
Leo Sternbach, the chemist who created Valium, poses with his wife, Herta, in 2003. Sternbach was working with Hoffmann-La Roche when he created the popular tranquilizer. AP/Wide World Photos.