Alprazolam is used primarily for anxiety and panic disorders. This active ingredient treats only the symptoms, but not the trigger of the symptoms. Due to the sometimes significant side effects, alprazolam is only used when its use is unavoidable.
What is alprazolam?
Alprazolam is used primarily for anxiety and panic disorders. The active ingredient treats only the symptoms, but not the trigger of the symptoms. Alprazolam was developed by the U.S. pharmaceutical company Upjohn (later acquired by Pfitzer). It entered the German market in 1984 under the name Tafil. The white, crystalline powder, which is practically insoluble in water, belongs to the group of benzodiazepines. Unlike the classic representatives of this group, alprazolam has a triazole ring in its molecule. That is why it is called triazolobenzodiazepine. This preparation is commercially available in the form of tablets and sustained-release tablets, usually in doses of 0.25 mg, 0.5 mg or 1 mg. It is taken orally. The exact dosage is determined by the attending physician.
Pharmacologic action
The antianxiety, sedative, relaxing, and sometimes euphoric effects of alprazolam are due to its action on certain neurotransmitters in the brain. It crosses the blood–brain barrier and binds to the GABA-A receptors. There, the increasing influx of chloride ions enhances the effect of the inhibitory nerve messenger GABA within the central nervous system. As a result, the nerve cells become less sensitive to excitatory stimuli. Eighty percent of the active ingredient taken as a tablet is absorbed into the bloodstream in the intestine. After a single oral dose, the maximum plasma level is reached after about one to two hours. Plasma protein binding is seventy to eighty percent. The volume of distribution is approximately 1.0 to 1.2 l/kg. However, it is significantly greater in obese patients. The plasma half-life is reported to be about twelve to fifteen hours, but may be prolonged in elderly male patients. Biochemical metabolism of alprazolam occurs in the liver. The active ingredient is excreted mainly in the urine. The delayed release of the drug in sustained-release tablets does not affect its distribution, metabolism, or elimination. Peak serum concentrations are reached approximately five to ten hours after ingestion with this form of medication.
Medical use and application
The main indication for alprazolam is anxiety with significant hyperexcitability (nervousness). In some cases, it is also prescribed as adjunctive therapy in the treatment of depression. This use is controversial among medical professionals. While it has been shown to be effective for short durations of treatment, prolonged administration may increase depressive symptoms. Therefore, the drug is not suitable for the sole treatment of depression. Alprazolam is also often used as a sleeping pill. However, it has no indication for this (off-label use). At higher doses, the drug can reduce muscle tension and help prevent epileptic convulsions. Initially, many patients receive 0.25 mg to 0.5 mg of alprazolam three times a day. If necessary, the dose can be increased to up to 3 mg daily. After ingestion, memory lapses sometimes occur for the period immediately following use. Therefore, care should be taken to ensure adequate sleep duration in treated subjects.
Risks and side effects
The most common side effects of alprazolam include drowsiness, drowsiness, and dizziness. Fatigue, decreased alertness, confusion, muscle weakness, headache, unsteadiness of movement and gait, visual disturbances, and tremor are also not uncommon at the beginning of treatment. Taking this agent may also cause liver dysfunction, menstrual irregularities, loss of appetite, nausea, constipation, hyperprolactinemia, skin reactions, and alteration of libido. Children and the elderly may react aggressively after alprazolam administration and suffer from nightmares, irritability, agitation, and hallucinations. As soon as such symptoms appear, it is recommended to consult the attending physician and stop treatment with this medication. Even after a short period of use, alprazolam can be physically and psychologically addictive. The risk of dependence increases with the duration of use and the level of dosage.Patients who have previously been addicted to alcohol, tablets or drugs are particularly at risk. Abrupt discontinuation of the drug entails anxiety, irritability, restlessness, headaches, muscle pain, and in extreme cases even loss of reality and personality or severe hypersensitivity reactions.
