Alprazolam is an anxiolytic drug with some antidepressant, hypnotic and anticonvulsant effect. Alprazolam increases the inhibitory effect of gamma-aminobutyric acid in the central nervous system, increases the sensitivity of GABA-receptors to this mediator by stimulating the benzodiazepine receptors of the supramolecular compound GABA-benzodiazepine-chlorinophore.
When taking alprazolam, the muscles are relaxed in the patients. Alprazolam has some anticonvulsant activity. The drug has a mild hypnotic effect facilitates falling asleep, increases the duration of sleep, and also leads to a decrease in the number of nocturnal awakenings. The mechanism of hypnotism of alprazolam is based on its ability to depress the cells of the reticular formation in the brainstem, and to reduce the effects of vegetative, motor and emotional stimuli that negatively affect the process of falling asleep.
When taking Alprazolam in patients, the symptoms of anxiety and fear decrease, as well as a decrease in emotional tension. Alprazolam has practically no effect on the cardiovascular and respiratory system in healthy patients.
After oral administration, the active ingredient is well absorbed in the digestive tract and reaches peak plasma concentrations for 1-2 hours. Bioavailability of the drug Alprazolam is about 80%. Plasma concentrations increase proportionally with an increase in the dose of alprazolam. About 80% of the dose is associated with plasma proteins. Alprazolam penetrates through the hematoplacental and blood-brain barrier, is determined in breast milk. The equilibrium concentrations of alprazolam in plasma are established on the second-third day of therapy.
Metabolized mainly in the liver with the formation of a pharmacologically active substance (alpha-hydroxyl metabolite). Excreted mainly by the kidneys in the form of compounds with glucuronic acid, the half-life of alprazolam reaches 11-16 hours. Alprazolam is practically not cumulated in the body.
Indications for use:
- Alprazolam is used to treat patients with neurotic and neurosis-like disorders, which are accompanied by a sense of anxiety and anxiety.
- Alprazolam may be prescribed to patients with reactive depressive conditions, including those developed against a background of somatic diseases.
- Alprazolam can be used to treat patients with panic disorders, insomnia and withdrawal syndrome (including alcohol and narcotic withdrawal syndrome).
Mode of application:
- Alprazolam is intended for oral administration. The drug Alprazolam is taken regardless of food intake. As a rule, it is recommended to divide the daily dose by 2-3 doses. The duration of therapy and doses of alprazolam are determined individually. When choosing a dose, you should carefully monitor the patient’s condition, tolerability of alprazolam and, taking into account the effect achieved, adjust the dose.
- Adults with panic disorders and depressive states are usually prescribed alprazolam at an initial dose of 0.1-0.2 mg twice or thrice a day. If necessary, 1-2 weeks after the start of therapy, the dose of alprazolam is gradually increased (it is recommended to start increasing the dose from the evening reception, after which increase the morning dose). The recommended therapeutic dose is 3-6 mg of alprazolam per day.
- Weak patients and elderly patients are not recommended to prescribe more than 0.25 mg of alprazolam three times a day. If necessary, it is possible to increase the dose under the close supervision of medical personnel.
- In case of anxiety, sleep disturbances and anxiety, as a rule, taking 0.7-1.5 mg of alprazolam per day is recommended. If necessary, the dose is gradually increased to 3-4.5 mg of alprazolam per day.
- The highest recommended daily dose of alprazolam is 10 mg.
- The duration of therapy for acute conditions is 3-5 days.
- With prolonged therapy, alprazolam is taken up to 3 months.
- Mostly at the beginning of therapy with Alprazolam, patients may develop increased fatigue, drowsiness, attention deficit, dizziness, development of drug dependence, and slowing down of psychomotor reactions. The risk of these side effects is higher in elderly patients.
- Regardless of the age and duration of treatment with alprazolam, patients may develop side effects due to the drug
- On the part of the nervous system: limb tremor, depression, insomnia, headache, memory and movement coordination disorders, confusion. In addition, it is possible to develop speech disorders, outbreaks of aggression, hallucinations and anxiety.
- From the senses: a decrease in visual acuity, a change in taste.
- From the digestive system and metabolism: weight loss, dryness of the oral mucosa, anorexia, nausea, heartburn, stool disorders, decreased liver function, jaundice.
- Others: dystonia, myasthenia gravis, decreased libido, urinary retention, enuresis, dysmenorrhea, impaired renal function.
With a sharp reduction in dose or discontinuation of therapy with Alprazolam, patients may develop withdrawal syndrome, which is accompanied by dystrophy, skeletal muscle spasm and smooth muscle layer of internal organs, sleep disorders, vomiting, tremor, convulsions and excessive sweating.
- Alprazolam is not prescribed to patients who have a history of hypersensitivity reactions to the active or additional components of the drug.
- Alprazolam tablets are not prescribed for patients with lactose intolerance.
- Alprazolam is not used for the therapy of patients with respiratory failure, pronounced impairment of kidney and liver function, myasthenia gravis, acute attack of glaucoma, and acute alcohol poisoning, psychotropic, narcotic or hypnotic drugs.
- Alprazolam is not used in pediatric practice.
- Alprazolam should not be administered to patients with alcoholism (during the period of alprazolam therapy, alcoholic beverages and preparations containing ethyl alcohol are prohibited).
- During the drug Alprazolam should not engage in activities that require increased concentration and speed of psychomotor reactions.
The use of alprazolam during pregnancy and lactation is prohibited. Before starting treatment with alprazolam, women of childbearing age should be excluded from pregnancy and choose a reliable contraceptive. When pregnancy occurs during treatment with alprazolam, you should consult a doctor who will suggest a drug withdrawal plan and assess possible risks to the fetus.
Interaction with other drugs:
- Combined use of alprazolam with antidepressants in patients with endogenous depression is acceptable.
- There is a mutual enhancement of the effect with the simultaneous use of alprazolam with neuroleptic drugs, hypnotics and anticonvulsants, narcotic analgesics, ethyl alcohol and central muscle relaxants.
- With the combined use of the drug with inhibitors of microsomal oxidation, the risk of toxic effects of alprazolam is increased.
- There is a decrease in the effectiveness of alprazolam when combined with inducers of microsomal oxidation.
- Alprazolam increases plasma concentrations of imipramine when used concomitantly.
When taking Alprazolam in doses much higher than recommended (more than 500 mg per treatment), patients may develop confusion, drowsiness, impaired coordination of movements, nystagmus, reduced reflexes, speech disorders, hypertension, and coma.
In case of an overdose of alprazolam, gastric lavage and the appointment of enter sorbent agents are indicated (to reduce the absorption of alprazolam). If necessary, conduct activities and therapy aimed at maintaining the function of the cardiovascular and respiratory system. In the treatment of overdose in hospital conditions, administration of flumazenil is indicated.
- The drug Alprazolam should be stored and transported in its original packaging at a temperature range of 15 to 30 degrees Celsius.
- Alprazolam is recommended to protect from direct sunlight.
- If stored, Alprazolam is suitable for 5 years after release.
- The drug Alprazolam refers to the list number 1 of potent agents.
Before using Alprazolam, you should consult your doctor. These instructions for use are given in a free translation and are intended for reference only. For more information, please refer to the manufacturer’s annotation.