Universal reference book for medicines
Product name: HELEX В® SR (HELEX SR)

Active substance: alprazolam

Type: Tranquilizer (anxiolytic)

Manufacturer: KRKA (Slovenia)
Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..

Anxiolytic agent (tranquilizer), a derivative of triazolo-benzodiazepine.
Has anxiolytic, sedative, hypnotic, anticonvulsant, central muscle relaxant effect. The mechanism of action is to enhance the inhibitory effect of endogenous GABA in the central nervous system by increasing the sensitivity of GABA receptors to the mediator as a result of stimulation of benzodiazepine receptors located in the allosteric center of postsynaptic GABA receptors of the ascending activating reticular formation of the brainstem and intercalary neurons of the lateral horns of the spinal cord; reduces the excitability of subcortical structures of the brain (limbic system, thalamus, hypothalamus), inhibits polysynaptic spinal reflexes.
Severe anxiolytic activity (reduction of emotional tension, alleviation of anxiety, fear, anxiety) is combined with a mildly expressed hypnotic effect;
shortens the period of falling asleep, prolongs the duration of sleep, reduces the number of nocturnal awakenings. The mechanism of hypnotic action is the inhibition of cells of the reticular formation of the brain stem. Reduces the impact of emotional, vegetative and motor stimuli, which break the mechanism of falling asleep.
After ingestion, alprazolam is quickly and completely absorbed from the digestive tract.
C max in blood plasma is achieved within 1-2 hours.
Binding to plasma proteins is 80%.

Metabolised in the liver.

T 1/2 is an average of 12-15 hours. Alprazolam and its metabolites are excreted mainly by the kidneys.

Disturbing conditions, neuroses, accompanied by a sense of anxiety, danger, anxiety, stress, deterioration of sleep, irritability, and somatic disorders;
mixed anxiety-depressive conditions; neurotic reactive-depressive conditions, accompanied by a decrease in mood, loss of interest in the environment, anxiety, loss of sleep, decreased appetite, somatic disorders; anxious states and neurotic depression, developed against a background of somatic diseases; panic disorder in combination and without symptoms of phobia.
It is recommended to use the minimum effective dose. The dose is corrected during the treatment, depending on the effect achieved and the tolerance. If it is necessary to increase the dose, it should be increased gradually, at first in the evening, and then in the daytime reception.
The initial dose is 250-500 mcg 3 times / day, if necessary, a gradual increase to 4.5 mg / day is possible.

For elderly or debilitated patients, the initial dose is 250 Ојg 2-3 times / day, maintaining doses - 500-750 Ојg / day, if necessary taking into account the tolerability dose can be increased.

The abolition or reduction of the dose of alprazolam should be carried out gradually, reducing the daily dose by no more than 500 Ојg every 3 days;
sometimes even slower cancellation is required.
From the side of the central nervous system: at the beginning of treatment (especially in elderly patients) drowsiness, fatigue, dizziness, decreased ability to concentrate, ataxia, disorientation, unsteadiness of gait, slowing of mental and motor reactions;
rarely - headache, euphoria, depression, tremor, memory loss, movement coordination disorders, mood depression, confusion, dystonic extrapyramidal reactions (uncontrolled movements, including the eye), weakness, myasthenia gravis, dysarthria; in some cases, paradoxical reactions (aggressive flashes, confusion, psychomotor agitation, fear, suicidal tendencies, muscle spasm, hallucinations, agitation, irritability, anxiety, insomnia).
On the part of the digestive system: dry mouth or salivation, heartburn, nausea, vomiting, decreased appetite, constipation or diarrhea, impaired liver function, increased activity of hepatic transaminases and alkaline phosphatase, jaundice.

From the hemopoietic system: leukopenia, neutropenia, agranulocytosis (chills, hyperthermia, sore throat, excessive fatigue or weakness), anemia, thrombocytopenia.

From the urinary system: incontinence, urinary retention, renal dysfunction, decreased or increased libido, dysmenorrhea are possible.

On the part of the endocrine system: there may be a change in body weight, libido disorders, menstrual cycle disorders.

From the cardiovascular system: it is possible to reduce blood pressure, tachycardia.

Allergic reactions: skin rash, itching are possible.

Coma, shock, myasthenia gravis, occlusive glaucoma (acute attack or predisposition), acute alcohol poisoning (with impaired vital functions), opioid analgesics, sleeping pills and psychotropic drugs, chronic obstructive airways disease with initial manifestations of respiratory failure, acute respiratory failure, severe depression (suicidal tendencies may manifest), pregnancy (especially I trimester), lactation period, children and adolescence under 18 years, increased
sensitivity to benzodiazepines.
Alprazolam has a toxic effect on the fetus and increases the risk of congenital malformations when used in the first trimester of pregnancy.
Continuous use during pregnancy can lead to physical dependence with the development of withdrawal syndrome in a newborn. Admission to therapeutic doses at a later time of pregnancy can cause depression of the newborn's central nervous system. The use immediately before childbirth or during childbirth can cause a respiratory depression, a decrease in muscle tone, hypotension, hypothermia and a weak act of sucking (a sluggish suckling syndrome of a newborn) in the newborn.
Possible isolation of benzodiazepines with breast milk, which can cause a newborn to sleepiness and obstruct feeding.

In experimental studies, it has been shown that alprazolam and its metabolites are excreted in breast milk.

Caution should be applied to alprazolam in patients with impaired renal function.

Caution should be applied to alprazolam in patients with impaired liver function.

Contraindication: children and adolescence under 18 years.

For elderly or debilitated patients, the initial dose is 250 Ојg 2-3 times / day, maintaining doses - 500-750 Ојg / day, if necessary taking into account the tolerability dose can be increased.

With endogenous depression, alprazolam can be used in combination with antidepressants.
When using alprazolam in patients with depression, there are cases of development of hypomaniacal and manic state.
Caution should be applied to alprazolam in patients with impaired hepatic and / or renal function.

In patients who had not previously taken medications that affect the CNS, alprazolam is effective at lower doses, compared with patients who received antidepressants, anxiolytics or who suffer from chronic alcoholism.

With prolonged use in high doses, it is possible to develop addiction and the formation of drug dependence, especially in patients prone to abuse of medicines.

With a rapid dose reduction or a sharp abolition of alprazolam, withdrawal syndrome is observed, the symptoms of which can range from small dysphoria and insomnia to severe syndrome with abdominal and skeletal muscle spasms, vomiting, sweating, tremors and convulsions.
The withdrawal syndrome is more common in people who have received alprazolam for a long time (more than 8-12 weeks).
Do not use other tranquilizers simultaneously with alprazolam.

The safety of alprazolam in children and adolescents under the age of 18 years is not established.
Children, especially at a young age, are very sensitive to the inhibitory effect of benzodiazepines on the central nervous system.
During the treatment period, do not drink alcohol.

Impact on the ability to drive vehicles and manage mechanisms

During the treatment period, one should refrain from engaging in potentially dangerous activities requiring increased attention and speed of psychomotor reactions (driving vehicles or working with mechanisms).

With the simultaneous use of psychotropic, anticonvulsants, agents and ethanol, the inhibitory effect of alprazolam on the central nervous system is increasing.

With simultaneous application of blockers of histamine H 2 -receptors reduce the clearance of alprazolam and increase the inhibitory effect of alprazolam on the CNS;antibiotics from the group of macrolides - reduce the clearance of alprazolam.

With simultaneous use of hormonal contraceptives for oral administration increase T 1/2 alprazolam.

With the simultaneous use of alprazolam with dextropropoxyphene, CNS depression is more pronounced than in combination with other benzodiazepines, because
it is possible to increase the concentration of alprazolam in the blood plasma.
Simultaneous reception of digoxin increases the risk of developing intoxication with cardiac glycosides.

Alprazolam increases the concentration of imipramine in the blood plasma.

With the simultaneous use of itraconazole, ketoconazole increases the effects of alprazolam.

With the simultaneous use of paroxetine, the effects of alprazolam may be increased, due to the inhibition of its metabolism.

Fluvoxamine increases the concentration of alprazolam in the blood plasma and the risk of developing its side effects.

With the simultaneous use of fluoxetine, an increase in the concentration of alprazolam in the blood plasma is possible due to a decrease in its metabolism and clearance under the influence of fluoxetine, which is accompanied by psychomotor disorders.

It is impossible to exclude the possibility of enhancing the effect of alprazolam with simultaneous use with erythromycin.

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