Anxiolytics: What are they? How do they work? Uses, Indications, Mechanism of Action, Dosage, Interactions and Adverse Reactions

They are substances that reduce anxiety and cause a calming effect but without reducing motor or mental functions.

Anxiolytics or anti-anxiety medications are a category of medications used to prevent anxiety and treat anxiety related to various anxiety disorders .

These drugs tend to work fairly quickly and can create habit. Because of this, they are usually only prescribed for short-term use. They are not recommended for people with a history of substance abuse or addiction.

How do anxiolytics work?

Anxiolytics work by targeting key chemical messengers in the brain. This is believed to help decrease abnormal excitability.

Some of the most commonly prescribed anxiolytics are benzodiazepines:

  • Alprazolam (Xanax).
  • Clordiazepóxido (Libriu).
  • Clonazepam (Klonopin).
  • Diazepam (Diastat, Valium).
  • Lorazepam (Ativan).
  • Oxazepam.

Uses and indications

Primarily, anxiolytics are used to treat the symptoms of:

The symptoms of generalized anxiety disorder include extreme worry or fear that lasts for more than six months.

Social phobia is the deep fear of social situations, such as meeting new people or speaking and acting in public. Social phobia can cause physical symptoms such as profuse sweating and nausea. Over time, this disorder can be paralyzing and lead to social isolation .

Uses not approved by the FDA:

  • Agitation.
  • Withdrawal symptoms.
  • Muscle spasms.
  • Sedation.
  • Restless Leg Syndrome.
  • Sleepwalking disorder.

Mechanism

Anxiolytics (benzodiazepines) are drugs that act through the gamma-aminobutyric acid (GABA) A receptor, which regulates the entry of chloride into neurons, resulting in neuronal hyperpolarization.

Dosage

The dosage of the anxiolytics will vary depending on the patient and their history of sedative use.

Although it is similar in many aspects, the choice of agent is often based on its pharmacokinetic properties, especially at the onset of action, half-life and metabolic pathway.

Alprazolam (Xanax) : the initial dose is 0.25 mg two or three times a day; the dose can be increased by 0.5-1 mg per day every 3-4 days; The usual therapeutic dose is 2-3 mg total / day, with daily or three times daily dosing. The maximum dose is 4 mg / day.

Chlordiazepoxide (Librium) : the initial oral dose is 5-10 mg a day to twice a day; the dose can be increased by 5 mg per day; The usual therapeutic dose is 30-40 mg total / day, with daily or three times daily dosing.

An intramuscular dose of 50-100 mg can be administered every 4 hours if necessary for abstinence from alcohol.

Clonazepam (Klonopin) : the initial dose is 0.25 mg a day to twice a day; the dose can be increased by 0.125-0.25 mg daily or twice a day every 2-3 days; The usual therapeutic dose is 1-4 mg total / day in divided doses.

Diazepam (Valium) : the initial dose is 2 mg two to four times a day; the dose can be increased by 1-2 mg per day; The usual therapeutic dose is 15-30 mg total / day, with daily or three times daily dosing. An IM dose of 10 mg may be given every 4 hours if necessary for alcohol withdrawal.

Lorazepam (Ativan) : the initial dose is 0.5 mg twice a day; the dose can be increased by 1 mg per day in divided doses (twice a day or three times a day); The usual therapeutic dose is 2-8 mg total / day, with daily or three times daily dosing.

Oxazepam (Serax) : the initial dose is 10-15 mg per day; the dose can be increased by 10 mg daily in divided doses (three times a day); The usual therapeutic dose is 90 mg total / day, with three times a day dosing.

Dosage according to the patient’s condition

Geriatric

Elderly patients often require lower doses of benzodiazepine due to a slower metabolism of medications.

  • Alprazolam : no dose adjustment is required; increase as needed / tolerated.
  • Chlordiazepoxide : decrease the usual dose by 50%.
  • Clonazepam : no dose adjustment is required; increase as needed / tolerated.
  • Diazepam : use 2 mg a day initially, and increase as needed / tolerated.
  • Lorazepam : use an initial dose of 1 mg / day in divided doses, and increase as needed / tolerated.
  • Oxazepam : the maximum dose is 45 to 60 mg total / day, in divided doses.
Renal
  • Alprazolam : no dose adjustment is required; increase as needed / tolerated.
  • Chlordiazepoxide : patients with renal insufficiency (CrCl less than 10 ml / min) should reduce their doses by 50%.
  • Clonazepam : no dose adjustment is required; increase as needed / tolerated.
  • Diazepam : no dose adjustment is required; increase as needed / tolerated.
  • Lorazepam : dose adjustment is not required for mild to moderate renal impairment; Not recommended for patients with renal insufficiency.
  • Oxazepam : it is not necessary to adjust the dose; increase as needed / tolerated.
Hepatic
  • Alprazolam : no dose adjustment is required; increase as needed / tolerated.
  • Chordiazepoxide : the maximum dose is 20 mg total / day.
  • Clonazepam : no dose adjustment is required; increase as needed / tolerated.
  • Diazepam : reduce the usual dose by 50%.
  • Lorazepam : dose adjustment is not required for mild to moderate hepatic impairment; Not recommended for patients with hepatic insufficiency.
  • Oxazepam : it is not necessary to adjust the dose; increase as needed / tolerated.
The pregnancy

Benzodiazepines are category D drugs, mainly due to concerns about cleft lip / palate and urogenital and neurological malformations; however, recent literature does not show an increased risk of these.

When possible, avoid use during the first trimester.

Minimize use; that is, reserve for the use of PRN if possible.

Weight the benefit vs. the risk of continuing therapy; If necessary, consider an agent with a short half-life, and use sparingly and intermittently.

Consider starting and / or maintaining patients with an antidepressant agent. With the exception of paroxetine (category D), all antidepressants belong to category C.

Avoid use near the time of delivery, as the baby may experience withdrawal symptoms.

Breast-feeding

The long-term effects of exposure are unknown, but all benzodiazepines can cross breast milk; therefore, the baby may experience side effects, which include respiratory depression, sedation, difficulty in breastfeeding and hypotonia .

In general, benzodiazepines may have a longer half-life in babies (who have not developed the mechanisms for metabolism).

If used, choose an agent with a shorter half-life.

Pediatric dosage
  • Alprazolam : safety in children has not been established.
  • Chlordiazepoxide : Not recommended for children under 6 years of age. For children older than 6 years, use 5 mg two to four times per day. This can be increased to 10 mg two or three times a day.
  • Clonazepam : safety in children has not been established.
  • Diazepam : start with 1 mg two to four times per day, and gradually increase as needed / tolerated.
  • Lorazepam : safety in children has not been established.
  • Oxazepam : security has not been established for children under 6 years of age. No guidelines have been established for children between 6 and 12 years of age. For children older than 12 years, use 10-15 mg three or four times a day.
Renal
  • Chlordiazepoxide : Adjustment of the dose may be necessary in children with renal insufficiency.
  • Diazepam : no dose adjustment is required.
  • Oxazepam : it is not necessary to adjust the dose.

Interactions

The following are just some of the medications that interact with anxiolytics (benzodiazepines).

Adverse reactions to anxiolytic drugs

Most benzodiazepines can cause these side effects due to their inhibitory effects on brain neurotransmission:

Withdrawal symptoms

Withdrawal symptoms of benzodiazepines are more common when benzodiazepines with shorter half-lives are used.

  • Convulsions
  • Hallucinations
  • Agitation.
  • Tremors

Warnings

You must use anxiolytics exactly as directed. Misuse of these medications can cause serious effects.

Addiction

Some anxiolytics can create habit. You may develop cravings for some of these medications, especially if you take them too long. Taking anxiolytics for a prolonged period can also lead to tolerance to the medication.

This means that after using the medication for a long time, you need more to get the same effect.

Withdrawal

Check with your doctor before stopping taking these medications. If you suddenly stop taking anxiolytics, you may develop withdrawal symptoms. These may include seizures. However, if you talk to your doctor, they can help you slow down the medication slowly and safely.

Overdose

Do not take more than prescribed. An overdose of an anxiolytic medication can cause coma or death.

Therapies

Anxiolytics are often combined with psychotherapy or cognitive behavioral therapy. Together, they can help improve the quality of life for people with anxiety disorders. For more information, read about talking with a doctor about your anxiety.

Talk to your doctor

Many types of anxiolytics help prevent anxiety and treat anxiety-related conditions. These medications are mainly for short-term use.

Long-term use can be associated with serious effects. Some anxiolytics can be addictive. Tell your doctor if you have a history of substance abuse.

They can prescribe another treatment. If you are interested in other options, read these tips for the prevention of anxiety.