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Benzodiazepines: Uses, Side-Effects, and Precautions

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Benzodiazepines are a type of tranquilizer used worldwide for their soothing effects. Many controversies surround this class of drugs. Read on for more information on this.

Medically reviewed by

Dr. Vishal Patidar

Published At February 17, 2023
Reviewed AtFebruary 17, 2023

Overview:

Benzodiazepines treat anxiety and insomnia (difficulty falling asleep and staying asleep). They slow down the central nervous system (CNS) and help in muscle relaxation, relief from muscle stiffness due to the conditions of the central nervous system, and epilepsy. They are also used as preoperative medications to help patients relax before surgery. These are synthetic pharmaceutically manufactured drugs in tablets, capsules, and sometimes injectable form. Chlordiazepoxide (Librium) was first synthesized in 1957 and put to use in medicine in 1961. Benzodiazepines are internationally regulated, and some benzodiazepines, like Lorazepam and Diazepam, are used more commonly.

What Are the Indications of Benzodiazepines?

Indications for the use of benzodiazepines include, but are not limited to

  • Anxiety disorders.

  • Insomnia.

  • Acute status epilepticus (Seizure lasting longer than five minutes).

  • Induce amnesia.

  • Spastic disorders.

  • Seizure disorders.

  • Agitation.

How Do Benzodiazepines Work?

The body has a natural chemical called gamma-aminobutyric acid (GABA). This chemical reduces activity in areas of the brain that cause

  • Discussion.

  • Memory.

  • Emotions.

  • Vital functions such as breathing.

Benzodiazepine drugs enhance the effects of GABA on the brain and body. The enhanced effect of GABA on the body results in the following.

  • Relaxation and sleep (Sedation).

  • Reduce anxiety.

  • Relax the muscles.

What Is the Onset of Action of Benzodiazepines?

The metabolism rate of various benzodiazepines differs in their pharmacologically active forms, especially half-lives. The half-life of a medication is the time it takes for half of the drug's active ingredient to be consumed in the body. Short-acting drugs have a half-life of fewer than 24 hours, e.g., Midazolam, mid-acting compounds such as Nitrazepam have a half-life of 24 hours or more, while long-acting compounds such as diazepam have a half-life of 48 hours or more. Such half-lives vary from person to person, and older people tend to eliminate these drugs more slowly, with an increased risk of side effects such as memory loss. Older adults are at significantly higher risk of adverse events such as falls, cognitive decline, and impaired driving ability, although the latter is not limited to older adults.

Habit-Forming:

The drug has highly addictive properties and may lead to abuse. One should not take it for a longer duration at a stretch.

Expiry Date:

Do not use the medicine beyond the expiration date printed on the back of the medicine package.

What Is the Dosage of Benzodiazepines?

dosage-of-benzodiazepines

What Are the Side Effects of Benzodiazepines?

  • Drowsiness: Drowsiness or dizziness are the most frequently reported side effects of this class of drugs. Driving or operating machinery or performing other hazardous jobs can be dangerous while using these medicines. Drinking alcohol in combination with benzodiazepines can worsen the effects.

  • Abnormal Sleep Behavior and Amnesia (Memory Loss): The effect is commonly seen with traditional benzodiazepines. Anterior amnesia is the inability to create new memories, resulting in the inability to remember some or all of the recent past. Some benzodiazepines are known to have powerful amnesiac effects.

  • Hangover Effect: The next day, drowsiness and "hangover effect" - a concern with long-acting benzodiazepines, such as Diazepam or Flurazepam. Sedative side effects may persist into the next day and interfere with daily activities like driving. This risk requires special monitoring in the elderly.

Are Benzodiazepines Safe to Use?

Benzodiazepines should be used for as short a duration as possible. Taking benzodiazepines regularly for more than a few weeks can lead to addiction. Physicians recommend taking them for only two to four weeks. Intermittent use can help avoid addiction.

What Are the Contraindications of Benzodiazepines?

  • Benzodiazepines can cause respiratory depression in susceptible individuals due to their ability to relax the muscle. For this reason, it is contraindicated in people with myasthenia gravis, sleep apnea, bronchitis, and COPD (chronic obstructive pulmonary disease is a chronic inflammatory disease of the lung that obstructs airflow from the lungs).

  • Caution should be exercised when using benzodiazepines in individuals with personality or intellectual disabilities because of common paradoxical reactions. In major depression, they can cause suicidal tendencies and may also be used for suicidal overdoses.

  • Individuals with a history of excessive alcohol consumption and nonmedical use of opioids or barbiturates should avoid benzodiazepines because of the risk of life-threatening interactions with these drugs.

What Are Benzodiazepine Withdrawal Symptoms?

The physical dependence on benzodiazepines can occur in a few patients after heavy therapeutic doses or even after a brief medication period. In general, benzodiazepines ought to be discontinued slowly to limit signs and symptoms such as

  • Sleep disturbances and reversible insomnia.

  • Restlessness.

  • Irritability.

  • High anxiety.

  • Weakness.

  • Blurred vision.

  • Panic attacks.

  • Tremors.

  • Sweating and flushing.

  • Nausea and vomiting.

  • Headache.

  • Convulsions.

  • Psychosis.

  • Illusion.

Shorter-acting drugs produce a faster, more intense withdrawal response, usually occurring within twenty-four hours of stopping. Longer-acting benzodiazepines have slower development of withdrawal symptoms, usually starting a few days after discontinuing use but peaking at about seven days.

The length of time required to complete benzodiazepine withdrawal depends on the individual patient's characteristics, the type of benzodiazepine, the ability to handle withdrawal stress, and the initial reason for using the benzodiazepine. The time it takes to gradually taper off the benzodiazepines usually ranges from four weeks to six months but can last more than a year in certain cases. Rapid withdrawal can cause a severe symptomatic syndrome in many patients. Benzodiazepines should be discontinued at all times under the supervision of a physician.

What Are the Interactions of Benzodiazepines?

Usage of this medicine with any of the following drugs is not recommended. Since this information does not cover all the drugs, referring to a physician is recommended.

  • Phenothiazines.

  • Opioids.

  • Barbiturates.

  • Monoamine oxidase (MAO) inhibitors.

  • Antidepressants.

  • Alcohol.

  • Illicit drugs like heroin (an opiate).

Herbal and Grapefruit Interactions:

Herbal supplements and grapefruit may interact significantly with certain benzodiazepines.

Use in the Elderly:

Some active metabolites are present in a few benzodiazepines (Diazepam, Chlordiazepoxide) that remain in the system for long (long-acting), which can be a problem for patients, especially older patients. Elderly patients may have liver dysfunction and struggle to clear the drug from their system. Side effects such as dizziness, confusion, and instability may persist in older patients prescribed long-acting benzodiazepines. Older people should avoid benzodiazepines and nonbenzodiazepines, as recommended by the Beers Criteria, an expert-authored guide to safe drug use in older adults.

With Alcohol:

Mixing benzodiazepines and alcohol to enhance the effects of both substances are extremely dangerous as they both have a synergistic effect; thus, one should refrain from taking alcohol with benzodiazepines.

In Pregnancy:

It should be avoided during pregnancy and taken under a physician's supervision.

Breastfeeding:

Many benzodiazepines are excreted in breast milk and can cause accumulation and side effects in breastfed infants, such as sedation and feeding difficulties. For this reason, benzodiazepine use during breastfeeding is not recommended. Long-acting benzodiazepines such as diazepam and clobazam are contraindicated in nursing mothers.

Conclusion:

In general, benzodiazepines should be used short-term because they can lead to tolerance, abuse, dependence (addiction), withdrawal, and life-threatening overdose when combined with opioids.

Frequently Asked Questions

1.

What Are Various Benzodiazepine Drugs?

The common benzodiazepines drugs are as follows:
- Diazepam.
- Alprazolam.
- Lorazepam.
- Clonazepam.
- Temazepam.
- Chlordiazepoxide.

2.

What Are the Uses of Benzodiazepines?

The uses of benzodiazepines are as follows:
- Insomnia.
- Anxiety.
- Muscle relaxation.
- Treat seizures.
- Alcohol withdrawal.

3.

What Is the Mode of Action of Benzodiazepines?

Benzodiazepines increase the brain's neurotransmitter activity. The drug binds to the GABA receptor and leads to the movement of the chloride neurons into the post-synaptic neuron. GABA limits the brain's neuron activity, leading to reduced brain activity. The drug helps in muscle relaxation and sedatives. It reduces anxiety and seizures. 

4.

What Is a Good Benzodiazepine Drug for Anxiety?

Benzodiazepines help treat anxiety. It elongates the GABA activity and promotes relaxation and calm. These drugs can be given short-term because prolonged use can lead to intolerance. These can be used as a regular treatment or alternative if selective serotonin reuptake inhibitors do not work.

5.

Are Benzodiazepines Sedatives?

Benzodiazepines can be used as sleeping pills. The Healthcare may prescribe Tamazepam for a short duration for a week or less, because of intolerance. It helps the patient stay asleep. Furthermore, the healthcare provider may recommend the patient cognitive behavioral therapy for insomnia.

6.

Can Benzodiazepines Use for Depression?

Benzodiazepines are not anti-depressant. These drugs can stabilize the patient's mood. The drugs used to cure depression are selective serotonin reuptake inhibitors or monoamine oxidase inhibitors. Benzodiazepines can be used with antidepressants. The drug is limited in depression because of side effects like sedation.

7.

What Is More Secure Than Benzodiazepines?

The safer drugs than benzodiazepines are as follows:
- Selective serotonin reuptake inhibitors.
- Serotonin-norepinephrine reuptake inhibitors.
- Melatonin agonists.
- Buspirone (anxiolytic drug).

8.

Can Benzodiazepines Be Taken Daily?

Taking benzodiazepines daily is not safe. Due to prolonged drug use, some patients may be dependent or intolerant. High doses of benzodiazepines also face the same effect. The side effect includes drowsiness and sedation. These drugs are given for a short time due to their adverse effects.

9.

What Is a Major Threat of Benzodiazepines?

The threats of benzodiazepines are as follows:
- Dependence.
- Addiction.
- Intolerance.
- Withdrawal symptoms.
- Cognitive impairment.
- Drug interactions.
- Drowsiness.
- Confusion.
- Blurred vision.
- Dizziness.

10.

What Are the Contraindications of Benzodiazepines?

The contraindications of benzodiazepines are as follows:
- Bronchitis.
- Sleep apnea.
- Myasthenia gravis.
- Allergic to drugs.
- Respiratory problems.
- Pregnancy.
- Breastfeeding.
- Elderly population.

11.

What Are the Benefits of Benzodiazepines?

The benefits are as follows:
- Reduce anxiety.
- Maintenance of sleep.
- Muscle relaxation.
- Prevent seizures.

12.

What Are Natural Benzodiazepines?

No natural benzodiazepines are available. These are not found in the plants. They are manufactured to cure anxiety, seizures, and muscle spasms. The natural substance present in these drugs are:
- Lavender and chamomile.
- Nutritional supplements.

13.

Are Benzodiazepines Used for Stress?

Benzodiazepines can treat stress because it is an antianxiety drug. It provides short-term relief from stress. In case of chronic stress, the drug can not be taken due to the dependence and intolerance of the drug. Chronic stress needs cognitive behavioral therapy and meditation.

14.

What Are the Effects of Benzodiazepines on the Brain?

Benzodiazepines affect the brain. The effects are:
- Regulations of emotions.
- Sedative effects.
- Help in controlling seizures.
- Relax skeletal muscles.
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Dr. Vishal Patidar
Dr. Vishal Patidar

General Medicine

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