Medication

Anxiolytics

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Anxiolytics
Last update: 21-11-2024

How else can it be called?

  • Benzodiazepines

  • Barbiturates

What should we know about anxiolytics?

Anxiolytics are a group of drugs that slow down nervous system functions, producing relaxation or a feeling of calm.

Some of these medications are used in emergency situations because they act quickly, but most require several days or even weeks of treatment to show results.

In any case, the main recommendation is to be evaluated by a doctor who can prescribe the appropriate medication and follow up with a psychiatry specialist.

Mood disorders such as anxiety often require long-term treatments, as well as additional therapies alongside medication.

Anxiolytics are commonly used to treat:

  • Agoraphobia with panic disorder.
  • Generalized anxiety disorder (GAD).
  • Social anxiety disorder (social phobia).
  • Obsessive-compulsive disorder (OCD).
  • Panic symptoms.
  • Insomnia.
  • Seizures.

What are the different types of anxiolytics?

Anxiolytics can be classified into several categories:

  • Medications also used as antidepressants: These are often the first-line treatment for anxiety disorders. They are not suitable for situations requiring immediate relief, as their effects develop gradually over time. They are typically introduced progressively because they can initially increase anxiety in some patients. Despite the slow onset, they provide effective long-term control of anxiety-related conditions and significantly reduce depressive symptoms. Main subtypes:
    • Selective Serotonin Reuptake Inhibitors (SSRIs): Used for anxiety disorders, depression, and obsessive-compulsive disorder (OCD). They may have potential side effects such as sexual dysfunction and, in some cases, an increased risk of suicide. Some examples are: citalopram, escitalopram, fluoxetine, fluvoxamine, paroxetine, sertraline, vilazodone.
    • Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs): Prescribed for the same conditions as SSRIs and have similar side effects. Some examples are: venlafaxine, desvenlafaxine, duloxetine, milnacipran, levomilnacipran.
  • Benzodiazepines: Primarily used for emergency situations due to their rapid calming effect.
  • Barbiturates: Less commonly used today. The most well-known example is phenobarbital.
  • Adrenergic beta-antagonists (Beta-Blockers): Propranolol, nadolol.
  • Other Anxiolytics: Used for specific purposes or conditions. Examples: Clomethiazole, doxylamine, hydroxyzine, zolpidem, zopiclone.

What are benzodiazepines?

Benzodiazepines are fast-acting medications often used in emergency situations.

However, their use as anxiolytic medications has decreased due to several concerns, including:

  • Their potential to cause dependence and abuse.
  • Adverse effects, such as memory impairments.
  • Limited efficacy in treating depression, which is often associated with anxiety disorders.

In addition to their anxiolytic effects (mediated by the inhibition of neuronal circuits in the limbic system), benzodiazepines are used for:

  • Muscle relaxation: Treating muscle spasms.
  • Amnestic effects: During endoscopic procedures (e.g., colonoscopy, upper endoscopy).
  • Seizure management: Such as status epilepticus (e.g., lorazepam, diazepam).
  • Alcohol withdrawal: Prevention and treatment of delirium tremens (e.g., lorazepam).
  • Sleep disorders: For night terror and sleepwalking.
  • Anticonvulsant effects.

Benzodiazepines with anxiolytic properties are categorized based on their duration of action:

  • Long-acting (40–200 hours): Diazepam, clorazepate, flurazepam.
  • Intermediate-acting (20–40 hours): Clonazepam, bromazepam.
  • Short-acting (5–20 hours): Lorazepam, lormetazepam, alprazolam.
  • Very short-acting (1–2 hours): Triazolam, midazolam.

For example, triazolam (2–4 hours) is used as a sleep inducer, but additional medication may be needed for premature awakenings.

Caution is advised when prescribing benzodiazepines in patients with:

  • Liver diseases.
  • Alcohol abuse.
  • Neurological conditions.
  • Poor salivation in children.
  • Glaucoma.
  • Hyperactivity.
  • Kidney or lung diseases.
  • Myasthenia gravis.
  • Porphyria.
  • Pregnancy or breastfeeding.
  • Sleep apnea.

During treatment, the following side effects may occur:

  • Seizures.
  • Fever.
  • Tremors.
  • Muscle weakness.
  • Loss of reflexes.
  • Intense fatigue (asthenia).
  • Involuntary movements.
  • Shallow breathing.
  • Dry mucous membranes (mouth, eyes, nose).
  • Erythematous skin.
  • Low blood pressure (hypotension).
  • Slow pulse.
  • Mental alterations ranging from mild confusion to coma.

Benzodiazepines can cause dependence, so they should be used only for short-term treatments.

It may take approximately three weeks for the body to adjust after stopping treatment. During this period, symptoms like skin sensitivity, intestinal discomfort, vision changes, hypotension, confusion, and sleep disturbances can occur.

Combining benzodiazepines with alcohol enhances their effects and is dangerous. In pregnancy and breastfeeding they are not recommended because benzodiazepines pass through the placenta and into breast milk, posing risks to the fetus or newborn.

Alprazolam may reduce libido, cause erectile dysfunction, or result in lack of orgasm.

Clonazepam may increase libido and, in some cases, cause gynecomastia in men.

Diazepam and quazepam may alter libido and menstrual cycles in women or cause impotence in men.

Barbiturates

Barbiturates are medications derived from barbituric acid that act on the central nervous system, producing relaxing or anesthetic effects.

They have anxiolytic, hypnotic, and anticonvulsant properties.

Due to their potential to cause dependence or addiction, barbiturates are now rarely used. Benzodiazepines are generally preferred as they are less toxic in cases of overdose.

Although their use has declined, barbiturates are still prescribed for specific conditions, including:

  • Migraines.
  • Epilepsy.
  • Sedation.

Adrenergic beta-antagonists

Adrenergic beta-antagonists are medications used to manage physical symptoms of anxiety, such as those associated with performance situations like public speaking.

They may cause arterial hypotension (low blood pressure) as a side effect. Examples include propranolol and nadolol.

Propranolol is also used to treat social phobia. It is typically recommended to take propranolol one to two hours before the anticipated anxiety-inducing situation.

Other anxiolytics

There are other medications that have anxiolytic effects:

  • Clomethiazole: Used in older people for restlessness, agitation, or severe insomnia when other treatments have not been effective or are contraindicated.
  • Doxylamine: It has sedative effects and is suitable for inducing sleep.
  • Hydroxyzine: Used to treat anxiety in adults.
  • Zolpidem: This is a hypnotic used for the short-term treatment of insomnia in adults, when insomnia is debilitating or causing severe anxiety.
  • Zopiclone: It is a sleep-inducing agent used for the short-term treatment of insomnia in adults.

Active ingredients and brand names of anxiolytics

  • Selective serotonin reuptake inhibitor (SSRIs)
    • Citalopram
    • Escitalopram
    • Fluoxetine
    • Fluvoxamine
    • Paroxetine
    • Sertraline
    • Vilazodone
  • Serotonin–norepinephrine reuptake inhibitor (SNRIs)
    • Desvenlafaxine
    • Duloxetine
    • Levomilnacipran
    • Milnacipran
    • Venlafaxine
  • Long-acting benzodiazepines
    • Chlordiazepoxide
    • Clobazam
    • Clorazepate
    • Diazepam
    • Flurazepam
    • Halazepam
    • Ketazolam
    • Pinazepam
    • Prazepam
    • Quazepam
  • Intermediate-acting benzodiazepines
    • Bromazepam
    • Camazepam
    • Clonazepam
    • Flunitrazepam
    • Nitrazepam
  • Short-acting benzodiazepines
    • Alprazolam
    • Bentazepam
    • Brotizolam
    • Clotiazepam
    • Loprazolam
    • Lorazepam
    • Lormetazepam
    • Oxazepam
    • Temazepam
  • Very short-acting benzodiazepines
    • Midazolam
    • Triazolam
  • Long-acting barbiturates
    • Phenobarbital
  • Intermediate-acting barbiturates
    • Amobarbital
  • Adrenergic beta-antagonists
    • Nadolol
    • Propranolol
  • Other non-barbiturate anxiolytics or hypnotics alone
    • Buspirone
    • Clomethiazole
    • Doxylamine
    • Febarbamate
    • Hydroxyzine
    • Meprobamate
    • Methaqualone
    • Zolpidem
    • Zopiclone
  • Anxiolytic or hypnotic associations
    • Diazepam + pyridoxine
    • Diazepam + sulpiride
    • Doxylamine + pyridoxine
Medically reviewed by Yolanda Patricia Gómez González Ph.D. on 21-11-2024

Bibliography

  • First Aid for the Basic Sciences: Organ Systems (3rd Ed) 2017, Tao Le, William L. Hwang, Vinayak Muralidhar, Jared A. White and M. Scott Moore, ISBN: 978-1-25-958704-7, Pag. 513.

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