Seduxen - instructions for use, dose, side effects, contraindications

Tablets white or white with a creamy shade of color, almost odorless, flat-cylindrical with a bevel, on one side with an engraving “SEDUXEN”, on the other - "5 mg”.

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.

ATX: & nbsp

N.05.B.A.01 Diazepam

Pharmacodynamics:

Diazepam has sedative-hypnotic, anticonvulsant and central muscle relaxant effects. Enhances the inhibitory effect of gamma-aminobutyric acid (GABA), which is one of the main mediators of pre- and postsynaptic inhibition of nerve impulse transmission in the central nervous system (CNS). It has anxiolytic, sedative, hypnotic, miorelaxing and anticonvulsant action. The mechanism of action of diazepam is determined by the stimulation of the benzodiazepine receptors of supramolecular GABA-benzodiazepine-chloro-nophoric complex, leading to activation of the GABA receptor, which causes a decrease in the excitability of the subcortical structures of the brain, inhibition of polysynaptic spinal reflexes.

Pharmacokinetics:

Absorption is high. After ingestion, about 75% is absorbed. Clinical effects appear in half an hour after taking the drug, and the maximum concentration (C_max) is achieved after 2 hours, equilibrium concentrations are achieved with a constant intake after 1-2 weeks. Diazepam lasts for about 12 hours. Bioavailability is 90%.The binding of diazepam to plasma proteins is 94-99%, and in men it is usually higher than that of women.

Diazepam and its metabolites penetrate the blood-brain barrier (BBB) and placental barriers, are found in breast milk in concentrations corresponding to 1/10 of the plasma concentrations. The connection with plasma proteins is 98%. Metabolized in the liver 98-99% to pharmacologically active derivatives (desmethyldiazepam) and less active (temazepam and oxazepam).

It is excreted by the kidneys - 70% (in the form of glucuronides), unchanged - 1-2% and less than 10% - with mildew. The half-life (T_1/2) of desmethyldiazepam 30-100 h, temazepam - 9.5 -12.4 h and oxazepam-5-15 h.

T_1/2 may be prolonged in newborns (up to 30 hours), elderly and senile patients (up to 100 hours) and in patients with hepatic renal insufficiency (up to 4 days).

With repeated use, the accumulation of diazepam and its active metabolites is significant. Refers to benzodiazepines with long T_1/2, excretion after cessation of treatment is slow, because metabolites persist in the blood for several days or even weeks.

Indications:

Treatment of neurotic and neurosis-like disorders with anxiety.

In the complex therapy of psychomotor agitation associated with anxiety.

In the complex therapy of epileptic seizures and convulsions of different etiologies. Apply for conditions accompanied by increased muscle tone (tetanus, acute disorders of cerebral circulation).

In the complex treatment of withdrawal syndrome with alcoholism.

It is also used for premedication and ataralgesia in combination with analgesics and other neurotropic drugs for various diagnostic procedures, in surgical and obstetrical practice.

In the clinic of internal diseases: in the complex therapy of hypertension (accompanied by anxiety, increased excitability), hypertensive crisis, vasospasms, climacteric and menstrual disorders.

Ménière's disease.

In dermatological practice it is used for itching dermatoses.

Insomnia (difficulty falling asleep).

Contraindications:

Hypersensitivity to benzodiazepine derivatives, severe myasthenia gravis, coma, shock, angle-closure glaucoma, a history of addiction (drugs, alcohol, except for alcohol withdrawal and delirium), nighttime apnea syndrome,the state of acute alcohol intoxication with the suppression of vital functions, acute intoxication with drugs that exert a depressing effect on the central nervous system (narcotic, hypnotics and psychotropic drugs), severe chronic obstructive pulmonary disease (risk of progression of respiratory failure), acute respiratory failure, children under 6 years , pregnancy (especially 1 trimester), the period of breastfeeding.

Carefully:

Absence (petit mal) or Lennox-Gastaut syndrome; epilepsy, hepatic and / or renal insufficiency, cerebral and spinal ataxia, hyperkinesis, a tendency to abuse psychotropic drugs, organic brain diseases (paradoxical reactions are possible), hypoproteinemia, elderly age, depression (see "Special instructions").

Dosing and Administration:

Inside. The dose is calculated individually, depending on the patient's condition, clinical picture of the disease, sensitivity to the drug.

Adults appoint 5-15 mg per day, usually for 2-3 hours. In hospital, patients can increase the daily therapeutic dose to 30 mg, and in case of an exacerbation of the condition, if necessary, and taking into account the tolerance to 60 mg.

Average recommended doses for different conditions:

As an anxiolytic is prescribed inside, but 2.5-10 mg 2-4 times a day.

With alcohol withdrawal syndrome - 10 mg 3-4 times a day in the first 24 hours, followed by a decrease to 5 mg 3-4 times a day.

Elderly, weakened patients, as well as patients with atherosclerosis at the beginning of treatment - inside, 2.5 mg 2 times a day, if necessary, the dose is increased to obtain the optimal effect. Working patients are recommended to take 2.5 mg 1-2 times a day or 5 mg (the main dose) in the evening.

Neurology: spastic conditions of central origin degenerative neurologic diseases - inside, 5-10 mg 2-3 times a day.

In the clinic of internal diseases, 2.5-5 mg 2-3 times a day, if necessary and taking into account the tolerance to 10 mg 4 times a day.

Obstetrics and gynecology: psychosomatic disorders, climacteric and menstrual disorders, gestosis - 2.5-5 mg 2-3 times a day.

Anaesthesiology, surgery: premedication - on the eve of surgery, in the evening - 10-20 mg inside; Pediatrics: appoint with a gradual increase in dose (starting with low doses and slowly increasing them to the optimal dose, well tolerated by the patient), daily dose (can be divided into 2-3 doses,the main, the largest dose, is taken in the evening): inside, from 6 lodges - 2.5 mg, from 7 years and older - 2.5-5 mg. Daily doses - 2,5-5 mg and 10 mg respectively.

Side effects:

From the nervous system: at the beginning of treatment (especially in elderly patients) - drowsiness, dizziness, fatigue, impaired concentration, ataxia, disorientation, slowing of mental and motor reactions, anterograde amnesia (develops more frequently than with other benzodiazepines) ; less often - headache, euphoria, depression of mood, tremor, catalepsy, confusion, dystonic extrapyramidal reactions (uncontrolled body movements), asthenia, muscle weakness, hyporeflexia, dysarthria; extremely rarely - paradoxical reactions (aggressive outbreaks, psychomotor agitation, suicidal tendencies, muscle spasms, confusion, hallucinations, anxiety, sleep disturbances).

On the part of the hematopoiesis: leukopenia, neutropenia, agranulocytosis (chills, hyperthermia, sore throat, unusual unusual fatigue or weakness), anemia, thrombocytopenia.

On the part of the digestive system: dry mouth or hypersalivation, heartburn, hiccough, gastralgia, nausea, vomiting, decreased appetite, constipation; violations of the liver,increased activity of "liver" transaminases and alkaline phosphatase, jaundice.

From the cardiovascular system: palpitation, tachycardia, lowering blood pressure (hereinafter referred to as "blood pressure").

On the part of the genitourinary system: urinary incontinence or retention, impaired renal function, increased or decreased libido, dysmenorrhea.

Allergic reactions: skin rash, itching.

Influence of the fetus: teratogenicity (especially I trimester), CNS depression, respiratory failure and suppression of the sucking reflex in newborns whose mothers used the drug.

Other: addiction, drug dependence; rarely - depression of the respiratory center, impaired vision (diplopia), bulimia, weight loss.

With a sharp decrease in dose or discontinuation of reception - withdrawal syndrome (increased irritability, headache, anxiety, fear, psychomotor excitation, sleep disturbances, dysphoria, spasm of smooth muscles of internal organs and skeletal muscles, depersonalization, increased sweating, depression, nausea, vomiting, tremor, perception disorders, incl. hyperaemia, paresthesia, photophobia, tachycardia, convulsions, hallucinations, rarely psychotic disorders).When used in obstetrics - in newborns - muscular hypotension, hypothermia, dyspnea.

Overdose:

Symptoms: drowsiness, oppression of consciousness of varying severity, paradoxical stimulation, reduction of reflexes to areflexia, reduced reaction to painful irritations, dysarthria, ataxia, visual impairment (nystagmus), tremor, bradycardia, lowering of blood pressure, collapse, inhibition of cardiac and respiratory activity (up to apnea), coma.

Treatment: gastric lavage, forced diuresis, symptomatic therapy (maintenance of breathing and blood pressure), artificial ventilation. As a specific antagonist, flumazenil (in a hospital setting). Hemodialysis is ineffective. The antagonist of benzodiazepines flumazenil not shown epileptic patients who received treatment with benzodiazepines. In such patients, antagonistic action against benzodiazepines may provoke the development of epileptic seizures.

Interaction:

When diazepam is used in conjunction with other drugs, the following interaction reactions can be observed:

with monoamine oxidase inhibitors (MAO)_,strychnine - antagonism with respect to the effects of diazepine;

with hypnotics, sedatives, narcotic analgesics, other tranquilizers, benzodiazepine derivatives, muscle relaxants, general anesthetics, antidepressants, neuroleptics, alcohol - a sharp increase in the oppressive effect on the central nervous system;

with cimetidine, disulfiram, erythromycin, fluoxetine, as well as with oral contraceptives and estrogen-containing drugs that competitively inhibit liver metabolism (oxidation processes) - possibly slowing the metabolism of diazepam and increasing its plasma concentration;

isoniazid, ketoconazole and metoprolol also slow down the metabolism of diazepam and increase its concentration in the blood plasma;

propranolol and valproic acid increase the level of diazepam in blood plasma;

rifampicin can enhance the metabolism of diazepam and, as a result, reduce its concentration in the blood plasma;

inducers of microsomal liver enzymes - reduce efficacy.

Hypotensive drugs can increase the severity of blood pressure lowering.

Antacid drugs reduce the rate of absorption of diazepam from the gastrointestinal tract.

Clozapine - may increase respiratory depression.

When used simultaneously with cardiac glycosides - it is possible to increase the concentration of the latter in the serum and the development of digitalis intoxication (as a result of competitive connection with plasma proteins).

Reduces the effectiveness of levodopa in patients with Parkinsonism.

Omeprazole prolongs diazepam clearance time.

Psychostimulants reduce the activity of the drug.

It is possible to increase the toxicity of zidovudine.

Theophylline (used in low doses) can reduce sedation. Premedication with diazepam reduces the dose of fentanyl required for an introductory general anesthesia, and shortens the time of onset of general anesthesia.

Special instructions:

It is necessary to observe special care when administering diazepam in severe depression, the drug can be used to implement suicidal intentions.

With renal / hepatic insufficiency and long-term treatment, it is necessary to control the picture of peripheral blood and "liver" enzymes.

The risk of forming drug dependence increases with the use of large doses, a significant duration of treatment, in patients who previously abused alcohol or drugs.Without special instructions should not be used for a long time. Unacceptable abrupt discontinuation of treatment due to the risk of "withdrawal syndrome", however, due to the slow half-life of diazepam, its manifestation is much weaker than in other benzodiazepines.

If such unusual reactions occur in patients, such as increased aggressiveness, psychomotor agitation, anxiety, fear, suicidal thoughts, hallucinations, increased muscle cramps, difficult sleep, superficial sleep, treatment should be discontinued.

The initiation of treatment with diazepam or its abrupt withdrawal in epileptic patients or with epileptic seizures in an anamnesis can accelerate the development of seizures or epileptic status. Has a toxic effect on the fetus and increases the risk of developing congenital malformations when used in the first trimester of pregnancy. Admission of therapeutic doses in later periods of pregnancy can cause oppression of the fetal CNS. Continuous use during pregnancy can lead to physical dependence - there may be withdrawal symptoms in a newborn.

Children, especially at a young age, are very sensitive to the CNS depressing action of benzodiazepines.

Use of at doses higher than 30 mg within 15 hours prior to delivery or during delivery may cause newborn respiratory depression (up apnea), decreased muscle tone, reduced blood pressure. hypothermia, a weak act of sucking (the so-called "sluggish child syndrome"). Elderly patients diazepam should be administered with extreme caution and do not exceed the recommended dose.

It is necessary to carefully evaluate the risk-benefit ratio for prescribing to pregnant women, as well as for patients with kidney and liver diseases.

Effect on the ability to drive transp. cf. and fur:

When taking diazepam, patients are not advised to perform work that requires quick reaction and risk, for example, to drive vehicles and carry out other potentially hazardous activities. During treatment with diazepam, alcohol is not allowed.

Form release / dosage:

Tablets containing 5 mg of diazepam.

Packaging:

For 10 tablets in a contour mesh package, 2 circuit packs with instructions for use in a cardboard pack.

Storage conditions:

Store at temperatures between + 15 and + 30 ° C. Keep out of the reach of children!

Shelf life:

5 years.

Do not use the product after the expiration date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N002110 / 01

Date of registration:27.12.2007

The owner of the registration certificate:GEDEON RICHTER-RUS, CJSC GEDEON RICHTER-RUS, CJSC Russia

Manufacturer: & nbsp

GEDEON RICHTER-RUS, CJSC Russia

Representation: & nbspGEDEON RICHTER-RUS CJSCGEDEON RICHTER-RUS CJSCRussia

Information update date: & nbsp16.08.2010

Illustrated instructions

Instructions

Seduxen (Seduxen)