Index
They are substances that reduce anxiety and cause a calming effect without reducing motor or mental functions.
Anxiolytics or anti-anxiety medications prevent anxiety and treat anxiety related to various anxiety disorders.
These drugs tend to work pretty quickly and can create a 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 vital 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:
- Anxiety disorders
- The disorder is generalized anxiety.
- The social phobia.
- Some are also used as sedatives before anesthesia for medical procedures.
A generalized anxiety disorder’s symptoms 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 amount 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 amount 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 grow as needed/tolerated.
- Lorazepam uses an initial dose of 1 mg/day in divided doses and increases as needed/tolerated.
- Oxazepam: the maximum amount 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 necessary for mild to moderate renal impairment; Not recommended for patients with renal insufficiency.
- Oxazepam is not required to adjust the dose; increase as needed/tolerated.
Hepatic
- Alprazolam : no dose adjustment is required; increase as needed / tolerated.
- Chlordiazepoxide: the maximum dose is 20 mg total/day.
- Clonazepam : no dose adjustment is required; increase as needed / tolerated.
- Diazepam: reduce the usual amount by 50%.
- Lorazepam: dose adjustment is not required for mild to moderate hepatic impairment and; Not recommended for patients with hepatic insufficiency.
- Oxazepam: it is unnecessary 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.
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 maintaining patients with an antidepressant agent. Except for paroxetine (category D), all antidepressants belong to category C.
Avoid use near the delivery time, 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, including 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 six years of age. Use 5 mg two to four times per day for children older than six years. 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 six. 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: Adjusting the dose may be necessary for children with renal insufficiency.
- Diazepam: no dose adjustment is required.
- Oxazepam: it is not required to adjust the quantity.
Interactions
The following are just some of the medications that interact with anxiolytics (benzodiazepines).
- Boceprevir.
- Carbamazepine .
- Clarithromycin .
- Digoxin .
- Disulfiram.
- Fluvoxamina.
- Fosamprenavir.
- Itraconazole .
- Ketoconazole
- Ritonavir.
Adverse reactions to anxiolytic drugs
Most benzodiazepines can cause these side effects due to their inhibitory effects on brain neurotransmission:
- Amnesia.
- Confusion.
- Dizziness.
- Depression.
Withdrawal symptoms
Withdrawal symptoms of benzodiazepines are more common when benzodiazepines with shorter half-lives are used.
- Convulsions
- Hallucinations
- Agitation.
- Tremors
Warnings
It would help if you used anxiolytics precisely as directed. Misuse of these medications can cause serious effects.
Addiction
Some anxiolytics can create a 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 drug.
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 severe effects. Some anxiolytics can be addictive. Tell your doctor if you have a history of substance abuse.
