Instruction for use: Helex SR

Trade name of the drug – Helex SR

Active substance: Alprazolam (Alprazolamum)

Dosage Form: Tablets
Composition:

Tablets prolonged action. 1 tablet contains 500 mg of alprazolam. In blisters of 20, 30, 60 or 90 tablets. Packaged in a cardboard box. Tablets, prolonged action, 1 mg or 2 mg. In multiples of 20, 30, 60 or 90 tablets.
Pharmacotherapeutic group:

Anxiolytic (tranquilizer)

ATX Code

N05BA12 Alprazolam

Pharmacological PropertiesPharmachologic effect
Antianxiety drug (tranquilizer), triazolo-benzodiazepine derivative. It has anxiolytic, sedative, hypnotic, anticonvulsant, central muscle relaxant effect. The mechanism of action is to strengthen the inhibitory effect of endogenous GABA in the central nervous system by increasing the sensitivity of the GABA-receptor mediator as a result of stimulation of benzodiazepine receptors located in the allosteric center of postsynaptic GABA-receptor ascending activating reticular formation of the brain stem and lateral horn neurons of the spinal cord; reduces the excitability of the subcortical structures of the brain (the limbic system, thalamus, hypothalamus), polysynaptic inhibits spinal reflexes.
Pronounced anxiolytic activity (reduction in emotional stress, easing anxiety, fear, anxiety), combined with moderate soporific effect; shortens the period of sleep, increases sleep duration, reduces the number of nighttime awakenings. The mechanism of hypnotic action is inhibition of the cells of the reticular formation of the brain. It reduces the impact of emotional, autonomic and motor stimuli that disturb sleep.

Pharmacokinetics
After oral administration, alprazolam is rapidly and completely absorbed from the gastrointestinal tract. Cmax plasma levels reached within 2.1 hours. Binding to plasma proteins is 80%. It is metabolized in the liver. T1 / 2 is an average of 12-15 hours. Alprazolam and its metabolites are excreted primarily by the kidneys.

Indications for Helex SR

Anxiety neurosis and anxiety, stress, anxiety, irritability, sleep disturbance, somatic disorders. Anxiety associated with depression (in the complex therapy). Panic disorder (treatment). Tremor (senile, essential). Insomnia.

Contraindications for Helex SR

Hypersensitivity, coma, shock, myasthenia gravis, angle-closure glaucoma (acute onset or predisposition), acute alcohol poisoning (with the weakening of vital functions), narcotic analgesics, drugs and psychoactive drugs; Severe COPD (degree of progression of respiratory failure), acute respiratory failure; severe depression (suicidal tendencies may emerge); pregnancy (especially the I trimester), lactation, age 18 years (safety and effectiveness are not determined).

Helex SR Dosage and Administration

Individual. It is recommended to use the minimum effective dose. Correcting dose during treatment, depending on the achieved effect and tolerability. If necessary increase dose should be increased gradually, beginning in the evening and then daily intake. The initial dose is 250-500 mg 3 times / day, if necessary, may gradually increase to 4.5 mg / day. For elderly or infirm patients the initial dose of 250 mg 2-3 times / day maintenance dose - 500-750 mg / day, taking into account the tolerance dose can be increased if necessary. The abolition or reduction of the dose of alprazolam should be done gradually by reducing the daily dose of no more than 500 mg every 3 days; sometimes you may need to further slow the cancellation.

Side effect of Helex SR

CNS: at the beginning of treatment (particularly in elderly patients), somnolence, fatigue, dizziness, decreased ability to concentrate, ataxia, disorientation, unsteady gait, mental retardation and motor responses; rarely - headache, euphoria, depression, tremors, memory loss, impaired coordination of movements, depressed mood, confusion, dystonic extrapyramidal reactions (uncontrolled movements, including eye), weakness, myasthenia gravis, dysarthria; in some cases - paradoxical reactions (aggressive outbursts, confusion, agitation, anxiety, suicidal tendencies, muscle spasms, hallucinations, agitation, irritability, anxiety, insomnia).

From the digestive system: dry mouth or salivation, heartburn, nausea, vomiting, loss of appetite, constipation or diarrhea, abnormal liver function, increased activity of hepatic transaminases and alkaline phosphatase, jaundice.

From hemopoiesis system: leucopenia, neutropenia, agranulocytosis (chills, pyrexia, sore throat, extreme tiredness or weakness), anemia, thrombocytopenia.

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

From endocrine system: the change in body weight, libido disorders, menstrual disorders. Since the cardiovascular system: possible decrease in blood pressure, tachycardia.

Allergic reactions: possible skin rash, itching.

Helex SR at Pregnancy and breast-feeding
The drug is contraindicated during pregnancy. If necessary, the appointment during lactation should abandon breastfeeding.

Cautions when taking the drug Helex SR
Contraindicated in severe hepatic dysfunction. With great care the drug is prescribed to patients with mild to moderate hepatic impairment.

Overdose of Helex SR

Symptoms: incoordination, depression of consciousness of varying severity, hypotension, respiratory depression; in more severe cases - coma, respiratory arrest and cardiac arrest.

Treatment: If the patient is conscious, induce vomiting is necessary, otherwise the show intubation and gastric lavage. Helex SRabsorption from the gastrointestinal tract decreases the appointment of activated carbon and mineral laxatives. The patient should be kept under observation in the intensive care unit. In severe cases, especially with respiratory failure shows the use of a specific benzodiazepine antagonist flumazenil receptors.

Interaction
There mutual enhancement effect, while the appointment of antipsychotic (neuroleptics), hypnotics or antiepileptic drugs, as well as central muscle relaxants, narcotic analgesics, ethanol and drugs for general anesthesia. Inhibitors of microsomal oxidation in liver enzymes increase and inductors alprozalama reduce the concentration in plasma (may change the effectiveness of alprazolam). Alprazolam may increase the severity of blood pressure lowering on a background of antihypertensive drugs. When concomitant administration of clozapine may increase the respiratory depression. Reduces the effectiveness of levodopa in patients with Parkinson's disease. It may increase the toxicity of zidovudine.

SPECIAL INSTRUCTIONS

During treatment Helex SRpatients strictly prohibited the use of ethanol. The efficacy and safety of the drug in patients younger than 18 years have not been established. In renal / hepatic failure and prolonged treatment is necessary to monitor the pattern of peripheral blood and "liver" enzymes. Patients not taking psychoactive drugs earlier, "responsible" for the drug at lower doses compared to patients taking antidepressants, anxiolytics or suffering from alcoholism. When endogenous depression Helexcan be used in combination with antidepressants. In the application of Helex SRpatients with depression were cases of hypomania and mania. Like the others. Benzodiazepines, Helex SRhas the ability to cause drug dependence during chronic administration in high doses (more than 4 mg / day). With the sudden discontinuation of Helex SRmay experience a syndrome of "lifting" (depression, irritability, insomnia, sweating, etc.), Particularly during chronic administration (more than 8-12 weeks). If you have patients with such unusual reactions, as increased aggressiveness, acute state of excitement, anxiety, suicidal thoughts, hallucinations, increased muscle cramps, difficult to fall asleep, shallow sleep, treatment should be discontinued. The gestation period is used only in exceptional cases and only for the "life" testimony. It has a toxic effect on the fetus and increase the risk of birth defects when used in the I trimester of pregnancy. Therapeutic dose in the later stages of pregnancy can cause depression of the central nervous system of the newborn. The constant use during pregnancy may lead to physical dependence with the development of the syndrome of "cancellation" of the newborn. Children, especially at a younger age, are very sensitive to the CNS depressant effects of benzodiazepines. Using just before birth or during labor may cause neonatal respiratory depression, decreased muscle tone, hypotension, hypothermia and a weak act of sucking (syndrome "flaccid child"). During the period of treatment must be careful when driving and other lesson. Potentially hazardous activities that require high concentration and psychomotor speed reactions.

Storage conditions

In a dry, dark place at a temperature of 10-30 ° C.
Keep out of the reach of children.
Shelf life

3 years.
Do not use beyond the expiration date printed on the package.
Conditions of supply of pharmacies
On prescription.