With the introduction of benzodiazepines such as chlordiazepoxide (Librium) and diazepam (Valium) in the early sixties, a new era has started in the treatment of insomnia and fear. These tranquilizers were more efficient and much safer than the older drugs such as barbiturates, meprobamate and glutethimide. Over the years, benzodiazepines have remained the most popular sedatives. Since the mid-80s, new alternatives have conquered the market. However, benzodiazepines remain hugely preferred.
More than 12 benzodiazepines are available in the market. These drugs have a common basic chemical structure. One by one, they increase activity at receptors for the neurotransmitter gamma-aminobutyric acid (GABA). This transmitter inhibits the activity of neurons, slowing down the brain and nervous system so that one can relax. They also promote sleep when taken before going to sleep. Benzodiazepines mainly differ in how quickly they are absorbed, how long their effects last, and how long it takes to leave the body.
They are prescribed for severe muscle cramps, tremors, acute attacks, and alcohol and drug withdrawal symptoms. But their main field of application is still the treatment of anxiety and insomnia.
Benzodiazepines are uniquely efficient when taken by mouth or administered intravenously for the rapid relief of acute anxiety and agitation. They can also be used to calm a person before surgery or to calm someone who is terrified of flying.
In patients with panic disorder, they reduce anticipatory anxiety and the resulting tendency to avoid places and situations that could trigger a panic attack. Benzodiazepines may also be useful in the treatment of generalized anxiety disorders.
Side effects of benzodiazepines
Short-term use of tranquilizers is relatively safe, especially compared to many other drugs. They can be used by people with most medical conditions and in combination with most other medications. An overdose is almost never fatal. Because benzodiazepines can carry some risk of birth defects, doctors are cautious about prescribing these drugs to pregnant women.
The most common side effect is fatigue or daytime sleepiness. Short-acting drugs can cause people to wake up at night. At higher doses, benzodiazepines can affect physical coordination and balance, increasing the risk of falls and other accidents. Some benzodiazepines can impair memory, making learning and retaining new information more difficult. Older people are more sensitive to all of these side effects.
Alcohol intensifies almost all side effects. Therefore, doctors do not recommend the use of alcohol or at least minimize alcohol consumption while using this medication.
Addiction hazard from benzodiazepines
Because the neurons adapt to the presence of these drugs and are underactive when tapered, benzodiazepines can cause physical dependence and withdrawal symptoms. With longer-acting drugs, the withdrawal reaction usually develops after a month or two. Shorter acting agents produce a shorter and more intense reaction that starts within 24 hours of withdrawal. With benzodiazepines leaving the body more slowly, symptoms begin several days after withdrawal and peak in about a week.
The most common withdrawal symptoms are restlessness, irritability, insomnia, muscle tension, weakness, blurred vision and an accelerated heart rate. Sometimes these symptoms are difficult to distinguish from those of recurring insomnia or anxiety. It is rare for a patient to have seizures or hallucinations after abrupt withdrawal from a short-acting benzodiazepine.
To facilitate withdrawal, the dose is gradually reduced. If the patient has been using these agents for a long time, the process can take months. Sometimes a longer-acting drug is replaced with a shorter-acting drug to make withdrawal easier.
After a few months of use, physical dependence on benzodiazepines is almost universal. However, it is uncommon for people to develop the kind of cravings seen in opioid use disorder.
Benzodiazepines alternatives: antidepressants
In general, antidepressants, especially selective serotonin reuptake inhibitors (SSRIs) such as sertraline (Zoloft), are as effective and even safer than benzodiazepines for the long-term treatment of panic disorders and generalized anxiety. Antidepressants have the advantage of relieving depression as well as anxiety and they create less risk of dependence. But because antidepressants take longer to work, benzodiazepines are often prescribed to temporarily help patients. The dose of benzodiazepine is gradually reduced as the antidepressant takes effect.
Benzodiazepines alternatives: other drugs
Buspirone (BuSpar), used to treat chronic anxiety, enhances the effect of the neurotransmitter serotonin. It is less effective than benzodiazepines and takes longer (several weeks) to work, but is less likely to cause physical dependence.
A recently introduced treatment for insomnia, Ramelteon acts on the receptors for melatonin, a hormone that helps regulate the body's circadian (24-hour) cycles. It is approved for long-term use.
Antihistamines are over-the-counter medicines that are sometimes used as a sedative. Diphenhydramine (Benadryl) is the most common. Side effects include daytime sleepiness and blurred vision.
Treatment without drugs
Exercise, muscle relaxation training, yoga, breathing training, and hypnosis can be used to relieve insomnia as well as anxiety. Psychotherapy of various kinds is useful for the long-term treatment of both. The most carefully studied and often the best alternative to benzodiazepines and related drugs is cognitive behavioral therapy.
For insomnia, this cognitive behavioral approach can change sleep habits as well as the ways of thinking about sleep. Patients learn to go to bed only when they are sleepy. It is also recommended not to use a television or electronics for at least an hour before going to bed. Instead, they learn to use relaxation techniques and breathing exercises. Visualizing calming scenes or hearing neutral sounds can also help you fall asleep. They also learn to recognize and change unrealistic ideas, such as the belief that without drugs they will never be able to sleep well.
Cognitive behavioral therapy examines and analyzes thoughts and feelings. Special attention is given to those who can provoke or relieve anxiety. As the therapist helps to become aware of unrealistic thinking, they also learn new ways to respond to frightening situations and practice techniques for anticipating and relaxing.
Most studies have shown that cognitive behavioral therapy is just as effective as drugs and their effects last longer. A combination of drugs and cognitive behavioral therapy can be more effective than either alone. But in some studies of insomnia, cognitive behavioral therapy has been found superior to the combination alone, possibly because patients are less committed to the behavioral and cognitive techniques when they know they can fall back on a drug.
Cognitive behavioral therapy has few risks. The main drawback is that it requires training and experience that many clinicians lack.