Alprazolam was developed by the US pharmaceutical company Upjohn (later acquired by Pfitzer). It entered the German market in 1984 under the name Tafil®. The white, crystalline, virtually insoluble in water powder is one of the benzodiazepines.
In contrast to the classical members of this group, alprazolam has a triazole ring in the molecule. Therefore, it also carries the name triazolobenzodiazepine. Commercially, this preparation is available in the form of tablets and prolonged-release tablets, usually at doses of 0.25 mg, 0.5 mg or 1 mg. The intake takes place orally. The exact dosage is determined by the attending physician.
The anxiolytic, calming, relaxing and sometimes euphoric influence of alprazolam is based on its action on specific messenger substances in the brain. It overcomes the blood-brain barrier and binds to the GABA-A receptors. There, the increasing influx of chloride ions enhances the effect of the inhibitory neurotransmitter GABA within the central nervous system. The nerve cells are thus less sensitive to excitatory stimuli.
The drug taken as a tablet is taken in the intestine to eighty percent in the bloodstream. 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 around 1.0 to 1.2 l / kg. In obese patients, however, it is significantly larger. The plasma half-life is given as about twelve to fifteen hours, but may be prolonged in older male patients.
The biochemical modification of alprazolam takes place in the liver. The active substance is excreted mainly via the urine. The delayed release of the active ingredient in prolonged-release tablets has no influence on its distribution, metabolism and elimination. The serum peak concentration is achieved with this form of medication approximately five to ten hours after ingestion.
The main application of alprazolam is anxiety with significant over-excitability (nervousness). In part, it is also prescribed as adjunct therapy in the treatment of depression. This use is controversial among medical professionals.
Although the drug has been shown to be effective for a short duration of treatment, the prolonged administration may increase the depressive symptoms. Therefore, the drug is not suitable for treatment alone in depression. The Öftern Alprazolam is also used as a sleeping aid. However, there is no indication for this (off-label use). At higher doses, the drug can reduce muscle tension and help prevent epileptic spasms.
At the beginning many patients receive 0.25 mg to 0.5 mg alprazolam three times a day. If necessary, the dose can be increased up to 3 mg daily. After taking partial memory lapses for the time directly after the application occur. Therefore, it is important to ensure a sufficiently long sleep duration of the treated persons.
The most common side effects with alprazolam include drowsiness, somnolence and dizziness. Tiredness, decreased attention, confusion, muscle weakness, headache, movement and gait insecurity, blurred vision and tremor are also not uncommon at the beginning of treatment.
In addition, the use of this drug may cause liver dysfunction, menstrual disorders, loss of appetite, nausea, constipation, hyperprolactinemia, skin reactions and changes in libido.
Children and the elderly can react aggressively after giving Alprazolam and suffer from nightmares, irritability, restlessness and hallucinations. As soon as such symptoms appear, it is recommended to consult the attending physician and stop treatment with this medication.
Alprazolam can make you physically and mentally dependent after just a short time of taking it. The risk of dependency increases with the duration of ingestion and the level of dosage. Particularly at risk are patients who have previously been alcohol, drug or drug addicts. An abrupt withdrawal of the drug causes anxiety, irritability, agitation, headache and muscle pain, in extreme cases, even loss of personality and personality or severe hypersensitivity reactions. Tags: