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

Active substanceDiazepam + CyclobarbitalDiazepam + Cyclobarbital

Similar drugsTo uncover

Reladom

pills inwards

Tarkhominsky pharmaceutical factory "Polfa", A.O. Poland

Dosage form: & nbsppills

Composition:

Composition per 1 tablet:

active ingredients:

Diazepam 10 mg

Cyclobarbital calcium 100 mg

Excipients: potato starch, talc, gelatin, sodium carboxymethyl starch, lactose monohydrate.

Description:

Round, flat-cylindrical tablets of white or grayish-white color, with a risk on one side, with a facet on both sides.

Pharmacotherapeutic group:Sleeping Pills

ATX: & nbsp

N.05.C.B.02 Barbiturates in combination with other drugs

Pharmacodynamics:

The drug belongs to the list of psychotropic substances (list III).

The drug Reladorm is a hypnotic drug that reduces the time of falling asleep, deepening and prolonging sleep.

The composition of the drug includes cyclobarbital and diazepam in a ratio of 10: 1. The pharmacological properties of the drug Reladorm are due to the potentiated synergy arising between cyclobarbital and diazepam. As a result of the summation pharmacological effects of both components, as well as their interaction, the time of falling asleep decreases, prolonged and simultaneously deepened sleep, compared with the effects observed after taking only one of these medicines.The effect of the drug Reladorm, in patients with sleep disorders, is 2 times greater than that of cyclobarbital or diazepam taken separately in the amounts contained in the preparation.

Cyclobarbital is a hypnotic drug, a derivative of barbituric acid, with an average duration of action. Has a depressing effect mainly on the central nervous system, especially on the subcortical area (thalamus, hypothalamus, reticular formation of the brain stem, limbic system, some vegetative centers) and the cortex of the brain. Barbiturates, applied in small doses, have a sedative and antiemetic effect, in high doses have a hypnotic and antiepileptic effect; have the ability to cause amnesia. The mechanism of action of the derivatives Barbituric acid is largely associated with the receptor complex, whose structure includes the chloride channel, the GABA-A receptor and the benzodiazepine receptor. This action, unlike 1,4-benzodiazepine derivatives, is nonspecific (absent receptors). Barbiturates affect directly to the chloride channel, act independently of gamma-aminobutyric acid (GABA), even in cases where the ion channel is maximally activated by GABA. Therefore, increasing the dose of the drug increases its activity up to serious toxic complications.

Diazepam is a derivative of 1,4-benzodiazepine. Acts on many structures of the central nervous system - primarily on the limbic system and the hypothalamus, i.e. structures related to the regulation of emotional activity. Like all benzodiazepines, it increases the inhibitory effect of GABAergic neurons in the cerebral cortex, hypocamp, cerebellum, spinal cord and other structures of the central nervous system. The result is a decrease in the activity of various groups of neurons: noradrenergic, cholinergic, dopaminergic and serotonergic. The existence of specific binding sites for benzodiazepines, which are protein structures of the cell membrane, which are associated with a complex consisting of the GABA-A receptor and the chlorine channel, have been established. The action of diazepam is to modulate the "sensitivity" of the GABA-ergic receptor,which leads to an increase in the affinity of this receptor for gamma-aminobutyric acid (GABA), which is an endogenous inhibitory neurotransmitter. The effect of activation of the benzodiazepine receptor or GABA-A is an increase in the intake of chloride ions into the neuron through the chlorine canal. This leads to hyperpolarization of the cell membrane, as a result of which the activity of the neuron is suppressed (i.e., a decrease in the release of the neurotransmitter). Clinically diazepam has an anxiolytic, anticonvulsant, sedative and moderately expressed hypnotic effect; reduces the tone of skeletal muscles. Also diazepam has an anamnestic effect.

Pharmacokinetics:

Cyclobarbital refers to the group of barbiturates of medium duration.

Suction

After ingestion, cyclobarbital is rapidly absorbed from the digestive tract. After taking a dose of 300 mg, the maximum concentration in the blood is reached within 20-180 minutes.

Distribution

Cyclobarbital strongly binds to blood proteins; easily penetrates into tissues and biological fluids of the body.It also passes through the placental barrier and penetrates into the mother's milk.

Metabolism

Cyclobarbital is metabolized in the liver with the participation of microsomal enzymes to ketocyclobarbital. As a result of hydroxylation of cyclobarbital, more hydrophilic inactive metabolites are formed. Cyclobarbital is a strong inducer of microsomal enzymes responsible for the metabolism of many drugs, including its own (autoinducer). A consequence of this is a decrease and a decrease in the duration of action of concomitantly used drugs undergoing biotransformation with the participation of cytochrome P450. The biological half-life is about 6 hours.

Excretion

Cyclobarbital is almost completely excreted by the kidneys in the form of metabolites.

Diazepam

Suction

Diazepam is well absorbed from the digestive tract; bioavailability is about 98%. When ingestion of 20 mg of diazepam, the maximum concentration in the blood is reached after 50-90 minutes and is 500 ng / ml.

Distribution

Diazepam is bound to 94-99% with blood proteins; passes through the blood-brain barrier.It also passes through the placental barrier and penetrates into the mother's milk. Has a great affinity for adipose tissue.

Metabolism

Diazepam is metabolized in the liver. As a result of this process, two active metabolites are formed N-desidmethyldiazepam and N-methyloxazepam, which are then converted to oxazepam, and he, in turn, binds to glucuronic acid.

The biological half-life is about 24-48 hours and can be prolonged in newborns, elderly patients, patients with impaired liver function and kidney function.

Excretion

Diazepam is excreted mainly by kidneys in the form of metabolites or in unchanged form (about 25%).

Indications:Symptomatic therapy of sleep disorders of different etiologies.

Contraindications:

- Hypersensitivity to 1,4-benzodiazepine derivatives, derivatives of barbituric acid or to any substance included in the preparation.

- Severe respiratory failure, regardless of the cause.

- The syndrome of nocturnal apnea.

- Severe hepatic and renal insufficiency.

- Glaucoma.

- Myasthenia gravis (Miastenia gravis).

- Acute porphyria.

- Poisoning with alcohol or drugs that have a depressing effect on the central nervous system.

- Childhood.

- Pregnant women and breast-feeding mothers.

- Patients of advanced age (over 65 years).

It is not recommended to use the drug Reladorm in patients with psychoses.

In connection with the content of lactose, the drug Reladorm should not be used in patients with rarely encountered hereditary intolerance to lactose, a deficiency of lactase Lappa or glucose-galactose malabsorption.

Carefully:

Liver and (or) renal failure of mild or moderate severity, chronic respiratory failure, mild porphyria, depression, suicidal thoughts and attempts in history, drug, narcotic or alcohol dependence in the anamnesis.

During treatment with the drug Reladorm and within 3 days after its completion, you should not drink any alcoholic beverages.

Dosing and Administration:

The dose and duration of treatment should be strictly according to the doctor's instructions.

Adults

Usually used ½ tablets or 1 tablet an hour before bedtime.

Patients with hepatic and (or) renal failure of mild or moderate severity

Patients with impaired liver function and / or kidneys of mild or moderate severity are recommended to use a lower dose, that is, ½ tablets.

Mode of application

The drug should be taken orally, with a small amount of water. The drug Reladorm recommended take no more than 7 days.

The use of the drug for longer than the recommended time (for example, for several weeks) can lead to drug dependence. In this case, you can not abruptly stop taking the drug. It is necessary to gradually reduce the dose, controlled by the doctor. A sharp discontinuation of taking Reladorm can lead to withdrawal symptoms (sleep and mood disorders, concentration and attention disorders, increased irritability).

In case of missed dose of the drug Reladorm

If the drug was not taken at the appointed time, it is necessary to take it as soon as possible or continue taking the drug in accordance with the recommendations of the doctor.

Do not take a double dose in order to replenish the missed dose!

Side effects:

The number and severity of side effects depends on the individual sensitivity of the patient and the dose of the drug

Frequent side effects are: drowsiness, slowing of psychomotor functions, headache and dizziness, confusion and disorientation, ataxia.

Less common are: general weakness, sometimes fainting, feeling dry in the mouth, visual disturbances (blurred vision, diplopia), dysarthria (slurred speech and wrong pronunciation), memory impairment (amnesia), muscle tremor, gastrointestinal disorders, libido disorders, disorders menstrual cycle, liver dysfunction, changes in the morphological composition of blood (leukopenia, agranulocytosis), urinary incontinence, a slight decrease in blood pressure, skin allergic reactions, paradoxical reactions - psychomotor agitation, insomnia, irritability and aggressiveness, muscle tremors, seizures. Paradoxical reactions occur most often when alcohol is consumed during drug treatment, in elderly patients and in patients with mental illness.

If there are: visual disturbances, anuria, a disturbance of the function of the hematopoietic system, an increase in the activity of "liver" enzymes, jaundice, it is necessary to stop the treatment with the drug Reladorm.

Systematic use of the drug for longer than the recommended period may lead to the development of drug dependence, as well as withdrawal symptoms in the event of abrupt cancellation.

Overdose:

As a result of an overdose of Reladorm, the following symptoms may appear: drowsiness, confusion, slurred speech, and in severe cases: ataxia, lowering blood pressure, respiratory failure, coma and even death. Dangerous for life can be poisoning caused by the simultaneous use of the drug Reladorm and alcohol or the drug Reladorm and other drugs that have an inhibitory effect on the central nervous system.

When poisoning with the drug Reladorm, it is necessary to take measures aimed at eliminating as quickly as possible from the body of a non-sucking drug or reducing its absorption from the digestive tract (provoking vomiting, taking activated charcoal, rinsing the stomach - under condition of preserved consciousness), monitoring the main vital functions (breathing, pulse, arterial blood pressure) and, if necessary, conduct appropriate symptomatic treatment.

The specific antidote of diazepam is flumazenil.

Interaction:

Pharmaceutical

Pharmaceutical types of incompatibility are not defined.

Pharmacodynamic

The following drugs enhance the relapsing effect of the Reladorm drug on the central nervous system: narcotic analgesics, antidepressants, MAO inhibitors, general anesthetic drugs (anesthetics), hypnotics, sedatives, and antihistamines, central-action antihypertensives.

Simultaneous use of narcotic analgesics can cause pronounced euphoria, which can lead to a more rapid development of drug dependence.

The use of alcohol during treatment with the drug Reladorm intensifies its inhibitory effect on the central nervous system and can lead to the development of paradoxical reactions such as psychomotor agitation, aggressive behavior, pathological intoxication or the appearance of symptoms of deep inhibition of brain function.

Reladorm reduces the effectiveness of the action of indirect anticoagulants - coumarin derivatives, hypoglycemic drugs, doxycycline, griseofulvin.

Diazepam interacts with levodopa (contributes to the weakening of its action), with phenytoin and preparations that reduce the tone of skeletal muscles (contributes to the enhancement of their action).

Pharmacokinetic

Disulfiram, cimetidine, some antibacterial drugs (for example, erythromycin), antifungal means (for example ketoconazole) and antiviral drugs (for example, ritonavir) inhibit the processes of biotransformation of the active substances of the drug Reladorm, which can enhance the pharmacological effect of this drug.

The drug Reladorm may reduce the effectiveness of oral contraceptive means. It is recommended that non-hormonal methods of contraception be used in patients taking this drug.

Rifampicin, as an inducer of "hepatic" enzymes, accelerates the metabolism of diazepam (promotes increased diazepam clearance) and weakens its pharmacological effect. Such an effect on the metabolism of diazepam can be exerted by theophylline and tobacco smoking.

Barbiturates enhance the metabolism of digoxin, glucocorticosteroids, cyclosporine and theophylline.

Reducing blood pressure caused by the drug Reladorm can enhance the following drugs: angiotensin-converting enzyme inhibitors, α-adrenoblockers, angiotensin II receptor antagonists, blockers of "slow" calcium channels.

Special instructions:

Decision on the treatment of insomnia should be preceded by a thorough analysis of the existing disorders; it is necessary to exclude other possible causes of insomnia (somatogenic, psychogenic, bad habits).

The drug Reladorm should be used under strict medical supervision.

The use of benzodiazepines or drugs of similar action, as well as barbiturates, can lead to the development of mental and physical drug dependence. The risk of developing drug dependence increases with the dose and duration of treatment and increases in patients with a history of addiction to other drugs, as well as in patients with alcohol dependence. The combination of benzodiazepine and cyclobarbital increases the potential for the development of drug dependence and toxicity of the drug Reladorm.

In the case of the development of drug dependence, a sharp discontinuation of the use of the drug Reladorm may lead to the emergence of an abstinence syndrome. Characteristic manifestations of the withdrawal syndrome are: headache, muscle pain, psychomotor agitation and emotional stress, motor anxiety, confusion and disorientation, increased irritability, insomnia.In severe cases, there may be: loss of sense of reality surrounding (derealization), personality disorder (depersonalization), increased sensitivity to touch (tactile hyperesthesia), increased sensitivity to auditory and visual stimuli (acoustic and light hyperesthesia), a feeling of "crawling" and numbness limbs, hallucinations or seizures.

The drug Reladorm can cause antegrade amnesia. This condition is most often observed a few hours after taking the drug, especially in a large dose. It is recommended to use the drug Reladorm an hour before bedtime and provide conditions for a continuous 7-8 hour sleep.

The drug Reladorm can cause paradoxical reactions, such as motor anxiety, psychomotor agitation, increased irritability, aggressiveness, nightmares, hallucinations, psychoses, somnambulism, personality disorders, pronounced insomnia and other behavioral side effects. These reactions are much more frequent in elderly patients, or in patients with alcohol dependence.

In the event that such symptoms appear, stop immediately the treatment with Reladorm.

The drug Reladorm should be used with great care in patients with renal and hepatic insufficiency of mild or moderate severity, as well as in patients with chronic respiratory failure, such patients should receive lower doses of the drug.

It is not recommended to use the drug Reladorm in patients with psychoses.

The drug Reladorm should be used with great caution in patients with symptoms of endogenous depression. Suicidal thoughts may appear in these patients. In connection with the possibility of deliberate overdose, these patients should prescribe the drug Reladorm in smaller doses, that is ½ pills.

The drug should be used with caution in patients prone to suicidal actions. it can cause deterioration.

The drug Reladorm should be used with great care in patients with alcohol, drug or drug dependence in history. These patients during the reception of the drug Reladorm should be under strict control, tk.are at risk of developing addiction and mental dependence.

The drug Reladorm should be used with caution in patients with an uncomfortable form of porphyria. The use of the drug may lead to an increase in the symptoms of this disease.

During prolonged therapy with Reladorm, periodic studies of the morphological composition of the peripheral and the conduct of functional liver samples are shown.

During treatment with the drug Reladorm and within 3 days after its completion, you should not drink any alcoholic beverages.

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

During treatment with the drug Reladorm and within 3 days after it is completed, you can not drive vehicles and engage in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Tablets, 10 mg + 100 mg.

Packaging:

10 tablets per blister (PVC / aluminum foil).

For 1 blister, along with instructions for use in a cardboard box, equipped with stickers to control the first opening.

Storage conditions:

The drug belongs to the list of psychotropic substances (list III).

Store in a dry, dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N015736 / 01

Date of registration:26.03.2010

The owner of the registration certificate:Tarkhominsky pharmaceutical factory "Polfa", A.O.Tarkhominsky pharmaceutical factory "Polfa", A.O. Poland

Manufacturer: & nbsp

TARCHOMIN PHARMACEUTICAL WORKS POLFA, S.A. Poland

Representation: & nbspFARMEXPERT LLCFARMEXPERT LLCRussia

Information update date: & nbsp02.09.2013

Illustrated instructions

Instructions

Reladom (Reladorm)