Xanax (Alprazolam): Dosage, Side Effects, Interactions
Alprazolam is used for the symptomatic treatment of anxiety. The indication applies only to anxiety disorders when they are severe or disabling, or when the disorder causes the patient to experience extreme discomfort.
How Xanax works
Alprazolam belongs to the benzodiazepine derivatives. Benzodiazepines are composed of a seven-membered 1,4-diazepine ring and a benzene ring. A 5-aryl substituent is typical and can be found in almost all representatives.
Alprazolam is a medium-acting benzodiazepine. It acts on the gamma-aminobutyric acid (GABA) receptors in the brain. GABA is a neurotransmitter that has a depressant effect on the central nervous system, resulting in sedative and anxiolytic properties.
The active ingredient alprazolam and the other benzodiazepines also have sedative, hypnotic, muscle relaxant and anticonvulsant properties in addition to their anxiolytic effect.
After oral administration, alprazolam is rapidly absorbed. Oral bioavailability is 80%. Maximum plasma concentrations are reached 1-2 hours after oral administration.
After a single dose, plasma levels are directly proportional to the dose administered. Alprazolam is 70% bound to serum proteins.
The main metabolites excreted in the urine are α-hydroxyalprazolam and a benzophenone derivative. The latter has almost no pharmacological activity. In plasma, α-hydroxyalprazolam and 4-hydroxyalprazolam are the main metabolites. α-Hydroxyalprazolam is comparable to alprazolam in its biological activity, whereas 4-hydroxyalprazolam has a 10-fold lower activity. The plasma levels of the metabolites are low, the plasma half-lives comparable to alprazolam.
The mean half-life is 12-15 hours. Like triazolam , alprazolam has a significantly shorter plasma elimination half-life compared to the other benzodiazepine derivatives. This is significantly increased in older patients. Alprazolam and its metabolites are mainly excreted in the urine.
The optimal dosage of alprazolam depends on the severity of the symptoms and the patient’s response.
The starting dosage is 0.25-0.5 mg 3 times a day. If necessary, the dose can be increased at 3-4 day intervals, increasing the evening dose first before increasing the daytime dose. The maintenance dosage is 0.5 mg to a maximum of 3-4 mg/day, divided into several individual doses.
Elderly patients, debilitated patients or patients with renal or hepatic impairment
The starting dose in elderly patients is 0.25 mg 2 or 3 times a day. If necessary, the dose can be increased at intervals of 3-4 days. The maintenance dosage is a maximum of 1.5 mg/day, divided into several individual doses.
A lower dose of a maximum of 0.75 mg/day in divided doses is recommended for elderly frail patients or debilitated patients with renal or hepatic impairment.
Children and young people
Because the safety and effectiveness of alprazolam in children and adolescents under 18 years of age has not been established, its use is not recommended.
Alcohol-dependent patients and patients who have never been treated with psychotropic substances before
These patients require lower doses than patients who have already taken psychotropic substances. To avoid excessive sedation, it is recommended that the lowest effective dose be used.
Duration of treatment
The duration of treatment should be as short as possible, with the total duration of therapy including the withdrawal phase not exceeding a period of 8-12 weeks. However, in certain cases, longer treatment may be necessary and the patient’s condition should be reassessed before treatment is continued. The need for treatment with alprazolam and the corresponding dosage should be regularly reviewed in each patient.
Dose reduction and discontinuation of treatment
If side effects occur, the dose should be reduced. When discontinuing, the dose should also be reduced gradually, whereby the daily dose of alprazolam should be reduced to a maximum of 0.5 mg every 3 days. If necessary, some patients may be discontinued in even smaller increments.
Alprazolam side effects are listed below in order of frequency.
- Drowsiness (especially at the start of treatment and at higher doses).
- Lack of appetite
- Confusion (especially at the start of treatment and at higher doses)
- Depression (especially in the case of a depressive predisposition)
- Ataxia (especially at the start of treatment and at higher doses)
- Difficulty concentrating
- Blurred vision (especially at the start of treatment and at higher doses)
- Tantrums, aggressive behavior and other paradoxical reactions
- Dystonia (especially at the start of treatment and at higher doses)
- Liver dysfunction
- Musculoskeletal weakness (especially at the start of treatment and at higher doses)
- Urinary retention
- Sexual Dysfunctions
- Menstrual irregularities
- Weight changes
- Increase in intraocular pressure
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