Helex CP - instructions for use, dose, side effects, contraindications

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Dosage form: & nbspsustained-release tablets

Composition:

1 tablet of prolonged action of 0.5 mg contains:

Active substance: alprazolam 0.5 mg.

Excipients: lactose monohydrate (granulate), hypromellose, magnesium stearate, dye Kiwi alu varnish (indigocarmine E-132 + quinoline yellow E-104).

1 tablet of prolonged action 1 mg contains:

Active substance: alprazolam - 1 mg.

Excipients: lactose monohydrate (granulate), hypromellose, magnesium stearate.

1 tablet of 2 mg prolonged action contains:

Active substance: alprazolam - 2 mg.

Excipients: lactose monohydrate (granulate), hypromellose, magnesium stearate, indigo carmine E-132 dye.

Description:

Tablets 0.5 mg: round slightly biconvex tablets of a greenish-yellow color. Tablets 1 mg: round slightly biconvex tablets of white or almost white color.

Tablets 2 mg: round slightly biconvex tablets of light blue color.

Pharmacotherapeutic group:Anxiolytic agent (tranquilizer). List III of the List of narcotic drugs, psychotropic substances and their precursors subject to control in the Russian Federation.

Pharmacodynamics:

Strong substance (approved at the meeting of the Standing Committee on Drug Control on April 17, 2002, Protocol No. 1 / 84-2002)

Alprazolam is a drug from the benzodiazepine group. Stimulates benzodiazepine receptors, supramolecular gamma-aminobutyric acid (GABA) -benzodiazepine-chloronophore receptor complex, leading to activation of the GABA receptor, causing a decrease in the excitability of the subcortical structures of the brain (limbic system, thalamus, hypothalamus), inhibition of polysynaptic spinal reflexes. Has anxiolytic (manifests itself in reducing emotional tension, easing anxiety, fear, anxiety), sedative, moderate sleeping pills (shortens the period of falling asleep, prolongs the duration of sleep, reduces the number of nocturnal awakenings), anticonvulsant, central muscle relaxant effect. 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.

Alprazolam also has the properties of an antidepressant, which is not typical for the classical representatives of the benzodiazepine group.

Virtually no effect on the cardiovascular system.

Pharmacokinetics:

The bioavailability of alprazolam in the administration of sustained-release tablets is similar to bioavailability when taking immediate-release tablets with the exception of slower absorption. Thus, the maximum concentrations (Cmah) of alprazolam after taking long-acting tablets is about half the Cmah after taking pills with the immediate release of alprazolam. Alprazolam reaches Cmah in the plasma after 5-11 hours (TCmah) after ingestion, and during this period its plasma concentrations remain relatively stable.

The pharmacokinetics of alprazolam in doses up to 10 mg is linear. The half-life (T1 / 2) and the concentration of metabolites are almost the same as when taking immediate-release tablets; metabolism and excretion of alprazolam are the same in tablets of both types.

Communication with plasma proteins, mainly with albumins - 80%.Penetrates through the placental and blood-brain barrier, as it penetrates into breast milk. Alprazolam is metabolized in the liver. Metabolites have no clinical significance due to their low plasma concentrations.

Alprazolam and its metabolites are excreted mainly by the kidneys in the form of compounds with glucuronic acid. T1 / 2 varies from 12 to 15 hours, and in the elderly it is, on average, 16 hours (refers to benzodiazepines with an average T1 / 2).

Indications:

The drug is used strictly according to the doctor's prescription:

- Anxiety disorders (including, mixed with somatic diseases, depressive conditions, syndrome, withdrawal in the phase of chronic alcoholism);

- Panic disorders (including those with a phobia).

Contraindications:

- Hypersensitivity to alprazolam or other components of the drug, as well as other benzodiazepines;

- Acute attack of angle-closure glaucoma;

- Coma, shock;

- Myasthenia gravis;

- Acute alcohol poisoning (with the weakening of vital functions), narcotic analgesics, hypnotics;

- Acute respiratory failure, nocturnal apnea;

- Severe chronic obstructive pulmonary disease (COPD) (progression of the degree of respiratory failure);

- Pronounced violations of the liver and kidneys;

- Epilepsy;

- Severe depression and suicidal tendencies;

- Pregnancy (especially I trimester) and lactation;

- Children under 18 years of age (safety and efficacy not studied);

- Galactosemia, Lactase Lactate Deficiency, or Glucose-Galactose Malabsorption Syndrome.

Carefully:

Hepatic / renal failure, cerebral and spinal ataxia, drug dependence in history, hyperkinesia, organic brain diseases, psychosis (possible paradoxical reactions), hypoproteinemia, elderly age.

Pregnancy and lactation:

Benzodiazepines are not recommended with confirmed (especially in the first trimester) or presumptive pregnancy and during lactation.

Dosing and Administration:

Inside, the tablets should be swallowed whole, not chewing 1 or 2 times a day, regardless of food intake. Alprazolam of the Helex ® SR tablets is released slowly.

The dose of the drug is selected individually for each patient based on the severity of the symptoms and individual response to treatment.

If serious unwanted reactions occur, even at the beginning of treatment, the dose of the drug should be reduced.Below is a diagram of the drug that meets the needs of most patients. If patients are required to prescribe higher doses, they should be increased with caution in order to avoid side effects. First increase the evening dose of the drug, and then the day.

Patients who have never taken psychotropic drugs require lower doses of alprazolam than people who have previously taken sedatives, antidepressants and hypnotics. To prevent ataxia and excessive sedation, especially in the elderly and mentally retarded people, therapy should begin with minimal effective doses.

Anxiety Disorders:

Usual initial dose: 1 mg per day, divided, for 1 or 2 admission.

Maintenance therapy: 1 - 4 mg per day, divided into 1-2 admission; the maximum daily dose is 4 mg.

Panic disorders:

Usual initial dose: 0.5 to 1 mg per night.

Maintenance therapy: 4 to 10 mg per day (do not increase more than 1 mg every 3-4 days). The daily dose is given in one or two doses. The average daily dose in clinical trials was 8 mg. The maximum daily dose is 10 mg (it was prescribed in rare cases).

Elderly or mentally retarded patients:

The usual initial dose: 0.5 mg -1 mg per day, divided into one or two doses.

Maintenance therapy: 0.5 mg -1 mg per day. When serious adverse reactions, even at the beginning of treatment, the dose of the drug should be reduced.

Abolition of therapy

The abolition of therapy with the drug should be carried out gradually, as a sharp interruption of the course can cause a "withdrawal" syndrome or "bounce" syndrome. With the withdrawal of the drug, the daily dose should be reduced gradually, no more than 0.5 mg every 3 days. Some patients require an even slower dose reduction (by 0.25 mg every 3 days). If typical "withdrawal symptoms" appear, you should return to the previous dose until the patient's condition is fully stabilized, and then begin again a gradual reduction of the doses until complete withdrawal.

The effectiveness of alprazolam therapy in anxiety disorders of more than 6 months has not been proven. In panic disorders, the drug was effective for 8 months.

The doctor should periodically evaluate the need for drug therapy in each patient.

Side effects:

Classification of incidence of adverse events (World Health Organization (WHO)): very frequent> 1/10

frequent from> 1/100 to <1/10

infrequent from> 1/1000 to <1/100

rare from> 1/10000 to <1/1000

very rare from <1/10000, or at an unset frequency (frequency can not be established according to available data).

From the central (CNS) and peripheral nervous system: at the beginning of treatment (especially in elderly patients): often - drowsiness, dizziness; infrequently - memory loss, headache, tremor, impaired coordination of movements, dystonic extrapyramidal reactions, decreased ability to concentrate, depression; feeling of fatigue, unsteadiness of gait; rarely - dystonia, ataxia, slowing of mental and motor reactions, epilepsy, paradoxical reactions (outbreaks of aggression, psychomotor agitation, fear, suicidal tendencies, muscle spasms, hallucinations, agitation, irritability, anxiety, insomnia), paranoid symptoms, depersonalization, hallucinations, sexual dysfunction, euphoria, confusion, myasthenia gravis, dysarthria.

From the hematopoiesis: leukopenia, neutropenia, anemia, thrombocytopenia; rarely - agranulocytosis.

From the digestive system: dry mouth or salivation, heartburn, - nausea, vomiting, decreased appetite,constipation or diarrhea; very rarely - a violation of liver function, increased activity of "liver" transaminases and alkaline phosphatase, cholestasis, jaundice.

From the genitourinary system: rarely - urinary incontinence, urinary retention, impaired renal function, decreased or increased libido; very rarely - dysmenorrhea, violations of ovulation, gynecomastia.

On the part of the organs of vision: infrequently - diplopia; rarely - increased intraocular pressure.

On the part of the respiratory system: rarely - respiratory failure in patients with chronic nonspecific respiratory diseases.

Allergic reactions: very rarely - anaphylaxis, skin rash, itchy skin.

Other: infrequently - mental and physical dependence, lowering of blood pressure (BP); rarely - anorexia, weakness, decrease or weight gain, tachycardia. With a sharp reduction in dose or discontinuation (especially when taking very large doses and for a long time), it is possible to develop withdrawal syndrome (irritability, nervousness, sleep disorders, dysphoria, spasm of the smooth muscles of the internal organs and skeletal muscles, increased sweating, depression, nausea, vomiting, tremor, perception disorders, hyperacusis, paresthesia, photophobia, tachycardia, convulsions, rarely - acute psychosis).

Influence on the fetus: teratogenicity, CNS depression, respiratory failure and sucking reflex suppression in newborns (when the drug is taken by the mother during pregnancy).

Overdose:

Symptoms: when taking 500 - 600 mg of alprazolam and more - drowsiness, confusion, decreased reflexes, nystagmus, tremor, bradycardia, shortness of breath or shortness of breath, lowering blood pressure, coma.

Treatment: gastric lavage, reception of activated carbon. Symptomatic therapy (maintenance of breathing and blood pressure). When acute intoxication - the optimal choice is - the introduction flumazenil (in a hospital setting). T1 / 2 flumazenil 1 hour, which is shorter than T1 / 2 alprazolam; therefore it is necessary to administer repeatedly, in the form of infusions. The recommended initial dose of flumazenil is 0.3 mg intravenously (iv). In the absence of effect, it is necessary to reintroduce in a dose of 0.1 mg until the patient regains consciousness or until a total dose of 2 mg is administered. The same doses are recommended for repeated violations of consciousness. It is possible to administer flumazenil in the form of infusions at a rate of 0.1-0.4 mg / hour. Flumazenil Do not use in patients with epilepsy, t. possibly triggering seizures.

With coma, treatment is symptomatic. Prevention of asphyxia and aspiration of gastric contents. To prevent dehydration, IV administration is required. Effects of the drug after taking very high doses can persist for a long time. Forced diuresis and hemodialysis are of little effect.

Interaction:

With the simultaneous administration of alprazolam (as well as all benzodiazepines) with drugs, oppressive central nervous system (neuroleptics, antidepressants, general anesthetic agents, anticonvulsants and antihistamines) can exacerbate the inhibitory effect on the central nervous system. With the simultaneous administration of alprazolam with other hypnotics or sedatives, the effect can be potentiated.

Alprazolam decreases the effectiveness levodopa in patients with Parkinsonism.

Alprazolam may enhance action alcohol, so patients should refrain from drinking alcohol during the treatment period.

With the simultaneous administration of alprazolam in doses up to 4 mg s imipramine and desipramine, the equilibrium concentrations of the latter in the blood plasma can increase by 31% and 20%, respectively.

Hypotensive drugs can increase the severity of blood pressure lowering.

Simultaneous administration of alprazolam and fluvoxamine causes an increase in the plasma concentration of alprazolam by approximately 30 %.

Inducers of microsomal liver enzymes reduce the effectiveness of alprazolam.

Simultaneous administration of alprazolam with ketoconazole, itraconazole and other antifungal drugs of the azole group, antibiotics - macrolides (erythromycin, oleandomycin, etc.), cimetidine, oral contraceptives with low doses of estrogen, fluoxetine, sertraline, diltiazem, nefazodone can reduce the metabolism of alprazolam in the liver and enhance its effect. The clinical significance of these interactions is not established.

Interaction isoniazid or rifampicin not studied.

Simultaneous application atenolol or disulfiram does not change the pharmacokinetics of alprazolam.

Alprazolam does not affect plasma concentrations phenytoin, and the effect of phenytoin on plasma concentrations of alprazolam has not been studied.

Combined use of benzodiazepines and valproic acid potentially may increase the risk of psychosis, although this effect was not noted in alprazolam.It is possible to increase the toxicity of zidovudine.

Special instructions:

In the process of treatment with alprazolam, patients are strictly prohibited from drinking alcohol (ethanol).

Alprazolam is not recommended for patients with primary signs of depression with psychomotor retardation, as well as for bipolar depression and psychotic symptoms. Because of the increased risk of suicide, all patients with depressive disorders, as well as suicidal thoughts and attempts should be monitored, especially at the beginning of treatment (control of the dose of alprazolam taken).

Long-term treatment should be discontinued gradually (see section "Method of administration and dose"). If the drug is suddenly discontinued, there may be a "cancellation" syndrome, especially if you take longer than 8-12 weeks. Elderly patients and mentally retarded patients should be given a minimum effective dose because they may develop ataxia or excessive sedation. With renal / hepatic insufficiency and long-term treatment, control of the picture of peripheral blood and "liver" enzymes is necessary.

The development of drug resistance and, consequently, the need for increased doses when taking alprazolam are rare. Only resistance to sedative, but not anxiolytic effect is proved.

It is recommended to use caution when using a closed angle glaucoma.

The Helex® SR preparation contains lactose; so the drug should not be taken in patients with galactosemia, with a deficiency of Lappa lactase or glucose-galactose malabsorption syndrome.

Effect on the ability to drive transp. cf. and fur:The drug has an effect on psychophysical abilities, especially if it is taken with alcohol or tranquilizers. During the treatment period, care must be taken when dealing with potentially dangerous activities requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Tablets of prolonged action of 0.5 mg, 1 mg and 2 mg.

Packaging:

10 tablets per blister. By 2, 3, 6 or 9 blisters in a pack of cardboard along with instructions for use.

Storage conditions:

List 1 of the strong BACC.

Store at a temperature not exceeding 30 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use the drug after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-001490/09

Date of registration:03.03.2009

Date of cancellation:2017-04-28

The owner of the registration certificate:KRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO

Manufacturer: & nbsp

KRKA, d.d. Slovenia

Information update date: & nbsp28.04.2017

Illustrated instructions

Instructions

Helex® SR (Helex® SR)