Benzodiazepines, a class of psychotic drugs, are the oldest and the most commonly prescribed for a variety of conditions. They are also the most likely to cause dependence.  These drugs, most commonly prescribed for sleep-deprivation, help to induce sleep and cause less awakening at night.

Benzodiazepines or “benzos” as they are also called, are available as tablets or pills and as intramuscular and intravenous injections. They are available in drug stores on prescription only.

How Benzodiazepines Act | Mode of Action

Gamma-aminobutyric acid (GABA) is a naturally occurring amino acid in the body that works as a transmitter of nerve signals (neurotransmitters) in your brain.

Neurotransmitters function as chemical messengers. Gama-aminobutyric acid (GABA) is a brain chemical – an amino acid – that blocks the transmission of signals between the brain cells, thereby decreasing the excitability of the neurons and calming nervous activity. 

Benzodiazepines act on the central nervous system and enhance the effect of GABA, which results in a sedative and hypnotic effect.

Uses of benzodiazepines

Benzodiazepines are effective to treat a variety of psychological and neurological disorders, due to its inhibitory effect on the neurons that trigger stress and anxiety reactions. With their help, your stress and anxiety reactions are subdued.

However, their main uses still lie in the treatment of anxiety and insomnia.

Insomnia

In insomnia, benzodiazepines are initially used for sleep but for short term only because their prolonged use can lead to dependence.

Rapidly acting benzodiazepines with shorter half-lives (i.e., estazolam, triazolam, and temazepam) are preferred.

Anxiety

People who constantly worry and develop anxiety disorders can have problems with their daily activities especially when this problem becomes chronic and lasts for more than six months.

Antidepressants form the first line of treatment while benzodiazepines act as adjuvants. They are given initially to treat the acute symptoms until the antidepressants start to take effect.

 Chlordiazepoxide (Librium), diazepam (Valium), alprazolam (Xanax), lorazepam (Ativan) are mainly used in the treatment of anxiety

Agitation

Lorazepam is the only benzodiazepine that is very well absorbed intramuscularly, and remains the best choice when treating an acute attack of agitation,

Seizures

Benzodiazepines have a strong anti-convulsive property and are effective in preventing seizures. They are the first line of treatment in epilepsy and in status epilepticus. Lorazepam and diazepam are preferred.

Alcohol withdrawal

When an alcoholic with a history of heavy and prolonged alcohol use suddenly stops its consumption, he develops symptoms of alcohol withdrawal syndrome. Such symptoms include tremors, inability to sleep, confusion, anxiety, hallucination, disorientation, and seizures.

Benzodiazepines are the first drugs of choice and help to reduce the withdrawal symptoms. Chlordiazepoxide (Librium), diazepam (Valium), and lorazepam (Ativan) are the drugs from this group that are commonly used for this condition. They can be given orally, intravenously, or intramuscularly.

In surgical and dental patients

Where sedation is required in minor surgical or dental procedures to override the anxiety in the patients, benzodiazepines produce good results.

Anesthesia

Diazepam and Lorazepam are the benzodiazepines used with other drugs to induce anesthesia in patients before surgery.

List of types of benzodiazepines

Below is the list of all types of benzodiazepines (in alphabetical order)

  • alprazolam (Xanax, Xanax XR)
  • clobazam (Onfi)
  • clonazepam (Klonopin)
  • clorazepate (Tranxene)
  • chlordiazepoxide (Librium)
  • diazepam (Valium, Diastat Acudial, Diastat)
  • estazolam (Prosom is a discontinued brand in the US)
  • lorazepam (Ativan)
  • oxazepam
  • temaepam (Restoril)
  • traizolam (Halcion)

How are benzodiazepines used?

Benzodiazepines are relatively fast-acting and begin to act within a few hours, sometimes even less. Initially, the patient is started on a low dose, which is gradually increased until symptoms disappear.

The dose of this drug varies from case to case. Depending on the merits of each case, benzodiazepines are advised two or three times a day or sometimes only one dose may be administered at night.

In sleep disorders, benzodiazepines should be taken about 30 minutes before going to sleep and in case of a stomach upset, this pill should be taken after food or with milk.

If you have been taking this drug over some time, you should not stop it abruptly, but its dose should be gradually tapered off. This is because abrupt withdrawal can lead to symptoms of withdrawal syndrome.

Secondly, its dose or period of prescription should not be increased as it can cause tolerance and therefore, increasing doses may be required, which is not advisable. Nowadays, non-benzodiazepines are used more because of this drawback of benzodiazepines.

Side effects and drawbacks

  • Benzodiazepine withdrawal syndrome. Physical and psychological dependence develop and sudden stopping of these pills gives rise to withdrawal symptoms such as anxiety and rebound insomnia. These pills have to be withdrawn in tapering doses.
  • When regularly taken, these pills lose their effectiveness within about 4 weeks and a subsequent larger dose may be required. This is because the brain receptors lose their sensitivity and become resistant to this drug.
  • The quality of sleep is hampered with the promotion of light sleep and loss of deep sleep and REM sleep.
  • During the next day, you experience grogginess and drowsiness with a lack of mental alertness, which can be significant.
  • There is impaired memory, loss of coordination, and reduced reaction time when you use these pills.
  • The use of these sleeping pills can cause a hangover.
  • These drugs can worsen sleep apnea if present.
  • Benzodiazepines do not cure insomnia and only help you to fall asleep and once you stop the pills, you are again faced with sleeplessness.
  • Overdose can cause dangerous deep unconsciousness.

Contraindications or Precautions when using Benzodiazepines

You do not take benzodiazepines if you are associated with the following conditions or have a history of the following diseases.

  • During pregnancy and lactation – birth defects have been reported in babies when pregnant mothers have resorted to benzodiazepines.
  • Liver and/or kidney diseases
  • Bronchitis, asthma, and Chronic Obstructive Pulmonary Disease (COPD)
  • Myasthenia gravis
  • Apnea,
  • Epilepsy,
  • Glaucoma
  • Depression (can cause suicidal tendencies)
  • Allergy to the drug

Drug Interactions

Inform your doctor if you are taking any other medicines because benzodiazepines should not be taken with certain OTC or prescription medicines. These drugs include

  • Antidepressants
  • Antiepileptic drugs
  • Drugs, which cause sedation such as opioids and barbiturates
  • Narcotic medications for pain such as codeine
  • Anesthetics
  • Antihistamines
  • Muscle relaxants
  • Prescription analgesics (pain killers)

Benzodiazepines can cause severe nervous system depression when combined with the above medications. Some more drugs that should not be taken with benzodiazepines are:

  • Oral contraceptives increase the blood levels of benzodiazepines and thereby the risk of potential side effects.
  • Cimetidine (used to treat ulcers) too similarly increases the risk of side effects.
  • Some antibiotics and antifungal agents decrease the rate of excretion of benzodiazepines from the body, which can cause the drug to accumulate in the body and increase the potential of its side effects.
  • Elderly people should not take benzodiazepines because there is an increased risk of dependence, memory impairment and loss of motor coordination.

Benzodiazepines and Alcohol

  • You should abstain from alcohol when taking benzodiazepines because these two interact and can cause life-threatening complications. Benzodiazepines cause severe nervous system depression when combined with alcohol as alcohol intensifies the depressive action of benzodiazepines.

Benzodiazepine overdose

Benzodiazepines are safe if you stick to the prescribed dose. That is why they are so widely prescribed.

However, if you take them in large unsafe doses or with some other synergistically acting drugs, these drugs can be deadly.

Signs and symptoms of overdose include:

  • Slower breathing rate
  • Damp skin
  • Low blood pressure
  • Dilated pupils
  • Sluggish  reflexes
  • A feeble and fast  pulse
  • Bluish lips
  • Coma
  • Death

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