Benzodiazepine: Composition, Therapeutic use, Treatment. Benzodiazepine Effects. Reactions with other drugs.

Last modified: Thursday, 25. December 2008 - 6:20 am

Official names: Alprazolam (Xanax), chlorazepate (Tranxene) chlordiazepoxide (Librium, Novopoxide), clonazepam (Klonopin), clorazepate (Tranxene), diazepam (Valium, Vivol), estazolam (ProSom), flurazepam (Dalmane, Novoflupam, Somnol), flunitrazepam (Rohypnol), halazepam (Paxipam), lorazepam (Ativan), nitrazepam (Mogadon), oxazepam (Serax), prazepam (Centrax), quazepam (Doral), temazepam (Restoril), triazolam (Halcion)

Street names: Roofies, tranks, downers, benzos, goof-balls, Mexican, roach, heavenly blues, valo, stupefy, date rape, anxiety

Drug classifications: Schedule IV, depressant

 

Key terms

ANXIETY DISORDERS: A group of mental disorders or conditions characterized in part by chronic feelings of fear, excessive and obsessive worrying, restlessness, and panic attacks. Anxiety disorders include panic disorder, agoraphobia, obsessive-compulsive disorder, Post-traumatic stress disorder, and others.

DOCTOR SHOPPING: A practice in which an individual continually switches physicians so that he or she can get enough of a prescription drug to feed an addiction. This practice makes it difficult for physicians to track whether the patient has already been prescribed the same drug by another physician.

PANIC ATTACKS: Sudden, repeated, paralyzing bouts of extreme fear and anxiety.

PHOBIA: The irrational fear of a specific object or situation that limits normal functioning.

REBOUND: Also known as discontinuation symptoms, these occur when the benzodiazepines are withdrawn. These symptoms are an aspect of withdrawal in which the patient develops anxiety, insomnia, or other serious emotional reactions that are more intense than before treatment with the drug was begun.

 

Overview

Although they have been used for over 30 years, benzodiazepines are still widely prescribed in the treatment of anxiety disorders and other medical conditions. These drugs are classified as sedative-hypnotic agents, which depress or slow down the body. In the past 15 years, the development of the newer selective serotonin reuptake inhibitors (SSRIs) for the treatment of depression and anxiety have pushed benzodiazepines aside as the first treatment choice because the SSRIs as a class of drugs have not yet been found to be addictive.

Benzodiazepines are used to treat a wide range of psychiatric and medical conditions. Because they work so quickly, benzodiazepines are often the first drugs chosen by physicians in treating new or suspected anxiety or psychiatric disorders. Compared to the newer SSRIs, which can often take weeks to have an effect, benzodiazepines can be felt to work within hours. This quick onset of action has both positive and negative sides. On the one hand, people feel better faster. On the other hand, this speediness of effect also makes benzodiazepines more likely to cause addiction than other medications prescribed by psychiatrists and psychologists. Physical and/or psychological dependence may occur within a matter of weeks, depending upon the individual taking them.

When taken alone, benzodiazepines have a relatively good safety record. Even when taken in overdose quantities alone these drugs rarely cause serious consequences. Unfortunately, however, when benzodiazepines are being abused, they may be used in combination with other drugs or alcohol, and it is these combinations that can lead to serious physical consequences, including depressed respiration, coma, and even death.

Historical background

Benzodiazepines were developed in the 1950s as a safer alternative to barbiturates. Currently, about 2,000 different kinds of benzodiazepines are made. In the United States, only about 15 of these are approved by the FDA.

Some of the more commonly prescribed benzodiazepines include the following, which are ranked here approximately according to frequency of use:

• alprazolam (Xanax)

• clonazepam (Klonopin)

• diazepam (Valium)

• lorazepam (Ativan)

• clorazepate (Tranxene)

• oxazepam (Serax)

• prazepam (Centrax)

• clordiazepoxide (Librium)

• halazepam (Paxipam)

The top four — alprazolam, clonazepam, diazepam, and lorazepam — are consistently listed among the top 100 most commonly prescribed medications. Flunitrazepam (Rohypnol) has recently received a lot of attention, especially on college campuses, where its use as a “date rape” drug has placed it on the watch list of students and police. Flunitrazepam is one of the drugs, along with MDMA (ecstasy), used by teenagers and young adults as part of the nightclub, bar, “rave,” or “trance” scene.

Flunitrazepam, also known by the brand name Rohypnol, and by the Street names roofies, R2, Roche, roofinol, rope, rophies, forget-me pill, and Mexican valium, has received more press recently than most of the other benzodiazepines. It comes as a small, white tablet, with “Roche” on one side, and an encircled “1” or “2” on the other side, which indicats the 1-mg or 2-mg dose. It is usually consumed orally, often combined with alcohol, and can also be snorted after crushing the tablets.

This drug is produced legally in countries such as Brazil, Colombia, Ecuador, Mexico, and Peru. It is frequently smuggled into the country disguised as vitamins or in its original packaging as cold medicine. Flunitrazepam is not approved in the United States, but is has been used widely in Texas, and is readily available in Miami, Florida, where it is a growing problem.

The pharmacologic effects of Rohypnol include sedation, muscle relaxation, and anxiety reduction. The sedative effects are said to be seven to 10 times that of diazepam (Valium). In high doses, flunitrazepam can cause malignant hyperthermia, or a sharp increase in body temperature that can cause muscle breakdown and failure of the kidneys and cardiovascular system.

Because it is colorless, tasteless, and odorless, flunitrazepam can be added to beverages and taken unknowingly. After taking this drug, the user can feel intoxicated, then sleepy, for up to eight hours. Speech may become slurred, and judgment impaired. Partial amnesia is a common effect, and for this reason, flunitrazepam has been used in committing date rape or sexual assault. Victims are usually unable to remember the assault, or identify who assaulted them while they were under the effects of flunitrazepam. These effects occur roughly 15-20 minutes after taking the drug, and last for four to eight hours. Deep sedation and respiratory distress are some of the more serious possible effects of Rohypnol, as are blackouts that can last up to 24 hours.

In 1996, Congress passed the Drug-Induced Rape Prevention and Punishment Act of 1996, which increased the federal penalties for those who used any controlled substance to aid them in sexual assault. This law makes it a punishable crime to give someone a controlled substance without that person’s knowledge of it and with the intent to commit a violent crime against that person. It also includes stiffer penalties for those who possess or distribute this drug.

Other benzodiazepines

Benzodiazepines are classified according to how long their effects last and by their potency. The ultra-short acting benzodiazepines include midazolam (Versed) and triazolam (Halcion); the short-acting benzodiazepines include alprazolam (Xanax) and lorazepam (Ativan); the long-acting include chlordiazepoxide (Librium) and diazepam (Valium). High potency benzodiazepines include alprazolam, lorazepam, triazolam, and clonazepam (Klonopin). Low-potency benzodiazepines include chlordiazepoxide, clorazepate (Tranxene), diazepam, and flurazepam (Dalmane).

Because benzodiazepines, as a class, are usually equally effective in treating anxiety (in combination with cognitive-behavioral theraphy), psychiatrists usually select which of these drugs to prescribe based on its side effect profile. This means that the physician will weigh all the individual factors of each patient, and decide which drug is best suited for the patient’s individual needs based on which side effects that person can or cannot tolerate. For example, some of the benzodiazepines are more easily processed by the liver. This may be particularly useful in patients taking birth control pills, propranolol, disulfuram, ulcer medications, and other drugs that may affect liver function. In such cases, lorazepam (Ativan) may be chosen because it has less of an effect on the liver.

Alprazolam (Xanax), lorazepam (Ativan), and oxazepam (Serax) are metabolized and cleared from the body more quickly than the other members of this family, and are therefore more likely to produce withdrawal symptoms when they are discontinued. These three drugs, however, are less likely to produce side effects such as impaired coordination, concentration, and memory; and muscular weakness or sedation.

Benzodiazepines do not depress breathing, blood pressure, or other vital functions, like many of the drugs used to treat psychiatric disorders. They are also less likely to cause damage to the body systems or death in cases of overdose.

Despite this, these agents still present a number of problems for many individuals, including the need for higher doses and addiction. Tolerance and physical and psychological dependence are common with continued treatment with all of these drugs.

When used for a longer period of time, a number of the benzodiazepines will slowly lose their effectiveness, and higher doses may be needed to achieve the desired effects. Further, if any of these medications are discontinued abruptly, withdrawal symptoms can occur, and these can be quite serious. These symptoms can include seizures, insomnia, nervousness, irritability, diarrhea, abdominal cramps, muscle aches, and memory impairment.

Several types of people should not take any of the benzodiazepines, because of the possibility of unwanted side effects. These include the following:

• People who have had previous negative reactions or serious side effects with any benzodiazepine.

• People who fly aircraft, drive, or operate heavy machinery.

• People with a history of drug or alcohol dependence.

• People with Alzheimer’s disease, stroke, multiple sclerosis, or other brain disorders.

• People with anxiety that recurs after benzodiazepines are discontinued.

• People who are seriously depressed.

• Women who are pregnant.

• Women who are breastfeeding.

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