How Do Benzodiazepine Anxiolytics Work?

Benzodiazepine anxiolytics are medications prescribed to treat anxiety and related disorders. Benzodiazepines work on the central nervous system to reduce hyperactivity in the brain and induce a calming effect. Benzodiazepine anxiolytics are also used for sedation, as muscle relaxants and to prevent seizures.

Benzodiazepines work on the limbic system of the brain, which regulates emotional and behavioral responses, and reticular formation which regulates sleep and consciousness. Benzodiazepines stimulate the activity of gamma aminobutyric acid (GABA), a chemical messenger (neurotransmitter) in the brain that inhibits nerve signals.

Benzodiazepines bind to GABA receptors, protein molecules on the surfaces of nerve cells (neuron) that respond to GABA, and increase the inflow of chloride ions, enhancing GABA’s effects. GABA inhibits electrical activity in the brain and produces sedation.

Benzodiazepine anxiolytics may be administered as:

• Oral: Tablets, capsules, solutions and syrups
• Injections:
  • Intravenous (IV): Injected into the vein
  • Intramuscular (IM): Injected into the muscle
• Rectal: Gel applied inside the rectum

Benzodiazepine anxiolytics are used to treat the following conditions:

FDA-Approved

• Anxiety
• Anxiety disorders
• Panic disorder
• Depression with anxiety
• Preoperative apprehension and anxiety
• Seizure disorders
• Acute alcohol withdrawal
• Endoscopy
• Preoperative sedation and anterograde amnesia (short-term loss of memory)
• Anesthesia induction and maintenance
• Sedation of intubated/ventilated patients
• Sedation in the ICU
• Procedural sedation
• Muscle relaxant
• Insomnia (short-term treatment)
• Status epilepticus (a medical emergency, when a seizure lasts longer than five minutes)

Orphan designation:

• Hyperekplexia (a rare hereditary neurological disorder that causes excessive startle reaction to sudden noise or touch)
• Recurrent, acute, repetitive seizures
• Repetitive seizures caused by Dravet syndrome, a rare type of epilepsy
• Organophosphorus poisoning (exposure to a neurotoxic substance that can cause muscle weakness, cramps and paralysis)

Off-label uses:

• Premenstrual syndrome
• Essential tremor
• REM sleep behavior disorder
• Burning mouth syndrome
• Tardive dyskinesia (a neurological disorder that causes involuntary repetitive movements)
• Chronic insomnia
• Chemotherapy-induced nausea and vomiting
• Smoking cessation

Side effects of antianxiety agents may include the following:

• Somnolence (drowsiness)
• Depression
• Headache
• Constipation
• Xerostomia (dry mouth)
• Ataxia (impaired coordination, balance and speech)
• Diarrhea
• Nausea
• Vomiting
• Bloating
• Increased or decreased appetite
• Weight change
• Nasal congestion
• Fatigue
• Lightheadedness
• Sedation
• Dizziness
• Vertigo
• Depression
• Euphoria
• Delirium
• Memory impairment
• Amnesia (memory loss)
• Irritability
• Cognitive disorders
• Insomnia
• Confusion
• Disorientation
• Nervousness
• Disinhibition
• Talkativeness
• Vivid dreams
• Mania and hypomania
• Suicidal ideation and attempt
• Paradoxical reactions such as:
  • Anxiety
  • Excitation and agitation
  • Anger, hostility and aggression
• Dysarthria (speech disorder, slurred speech)
• Asthenia (weakness)
• Akathisia (restlessness)
• Muscle weakness
• Rigidity
• Muscle cramps
• Unsteadiness
• Accidental falls, injuries and fractures
• Extrapyramidal symptoms (drug-induced movement disorders)
• Tremor
• Convulsion/seizures
• Worsening tonic-clonic seizures
• Decreased or increased salivation
• Blurred vision
• Visual disturbances
• Diplopia (double vision)
• Nystagmus (involuntary eye movement)
• Tinnitus (ringing in the ears)
• Edema
• Local effects from IV administration such as:
  • Pain and swelling
  • Phlebitis (inflammation of veins)
  • Thrombophlebitis (phlebitis with blood clot in vein)
  • Carpal tunnel syndrome
  • Tissue necrosis
• Hyperpyrexia (high temperature)
• Hypersensitive reactions such as:
  • Rash
  • Dermatitis
  • Angioedema (swelling in the tissue under the skin or mucous membranes)
  • Peripheral edema
  • Stevens-Johnson syndrome (a rare medical emergency with flu-like symptoms and a painful rash)
• Apnea (cessation of breathing)
• Sleep apnea 
• Respiratory depression
• Decreased respiratory rate
• Oxygen desaturation
• Upper respiratory infection
• Rhinitis (inflammation of the nasal passage)
• Coughing
• Hiccups
• Syncope (fainting)
• Hypotension (low blood pressure)
• Diastolic hypotension
• Hypertension (high blood pressure)
• Diastolic hypertension
• Systolic hypertension
• EEG abnormalities
• Bradycardia (slow heartbeat)
• Tachycardia (rapid heartbeat)
• Blood dyscrasias (disorders) such as:
  • Neutropenia (low blood count of neutrophils, a type of immune cells)
  • Agranulocytosis (low granulocytes, immune cells with granules)
• Difficult micturition (urination)
• Urinary frequency
• Urinary retention
• Incontinence
• Hepatic dysfunction 
• Increased bilirubin (jaundice)
• Increased liver enzymes
• Hepatitis (liver inflammation)
• Hepatic failure
• Menstrual disorders
• Increase or decrease in libido
• Impotence
• Hyperprolactinemia (high prolactin levels in the blood, which can induce abnormal breast milk production and other hormonal disorders)
• Galactorrhea (abnormal milk production and leakage)
• Gynecomastia (breast tissue development in males)

Information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with your doctor or pharmacist to make sure these drugs do not cause any harm when you take them along with other medicines. Never stop taking your medication and never change your dose or frequency without consulting your doctor.

Generic and brand names of benzodiazepine anxiolytic drugs include:

• alprazolam
• Ativan
• Byfavo
• chlordiazepoxide
• chlordiazepoxide/amitriptyline
• clonazepam
• clorazepate
• Diastat
• Diastat AcuDial
• diazepam
• Klonopin
• Librium
• lorazepam
• midazolam
• oxazepam
• remimazolam
• Seizalam
• Tranxene SD
• Tranxene T-Tab
• Valium
• Xanax
• Xanax XR