Reladorm

Reladorm is a hypnotic medication.

[1], [2], [3]

Indications Reladorma

It is used to treat insomnia, which is of a chronic nature, and in addition, with the development of a feeling of irritability or during a short sleep.

Release form

The release of the drug substance occurs in tablets, in an amount of 10 pieces inside a blister pack. A pack contains 1 such package.

Pharmacodynamics

The drug has sedative, anxiolytic, hypnotic, central, anticonvulsant and muscle relaxant properties.

Active components of drugs are diazepam with cyclobarbital. Diazepam is an anxiolytic tranquilizer that helps to reduce the excitability of neurons, and in addition to slowing down the spinal polysynaptic reflexes and potentiating GABA activity.

The drug does not have a muscle relaxant effect of a peripheral nature.

Reladorm reduces the severity of anxiety, anxiety, emotional tension and fear, thereby developing a full-fledged anxiolytic effect.

Cyclobarbital is a hypnotic substance with a powerful sedative effect.

Pharmacokinetics

Cyclobarbital enters the category of barbiturates with an average duration of exposure. After ingestion at high speed absorbed inside the digestive tract. After oral administration of 0.3 g of the substance, Cmax is noted after 20-180 minutes. Cyclobarbital has a strong association with blood protein; it passes easily into biological fluids and tissues, and in addition through the placenta and into the mother's milk.

The exchange processes of cyclobarbital are mostly carried out inside the liver, using microsome enzymes. In the metabolism of the component is transformed into ketocyclobarbital. The hydroxylation of cyclobarbital leads to the formation of hydrophilic metabolic products with no activity. Cyclobarbital has a powerful inducing effect on microsome enzymes that are responsible for the metabolic processes of many drugs, including their own (autoinductor). As a result, there is a reduction and reduction in the duration of exposure of the drugs used in the combination, which are biotransformed with the help of cytochrome P450.

Half-life is approximately 6 hours. Cyclobarbital is almost completely excreted through the kidneys in the form of metabolic products.

Diazepam is well absorbed inside the gastrointestinal tract; bioavailability index - about 98%. After oral administration of 20 mg of a substance, its blood Cmax values are noted after 0.9-1.3 hours and equal to 500 ng / ml. Approximately 94-99% of the substance is synthesized with blood protein. Penetrates through the BBB and the placenta, as well as into the mother's milk. It has an intense affinity for fatty tissue.

Diazepam undergoes intrahepatic metabolism, in which 2 active metabolic products are formed - N-desmethyldiazepam, as well as N-methyloxazepam. Then they are converted to oxazepam, which is then synthesized with glucuronic acid.

The component's half-life is approximately 0.8-2.2 days (it may increase in older people, newborns, as well as people with disorders in the kidneys or liver). Diazepam excretion occurs mainly through the kidneys - in the form of metabolic products and in an unchanged state (approximately 25%).

Dosing and administration

To get a hypnotic effect, the drug is taken 60 minutes before bedtime - 1-well pill.

To achieve a sedative effect, it takes 1-2 times a day to take a quarter or half a tablet.

[5]

Use Reladorma during pregnancy

Reladorm should not be prescribed in the 1st trimester (excluding emergency situations). Taking the medication of a pregnant woman can cause an increase in the rhythm of the heartbeat of the fetus.

At the time of use of the drug should stop breastfeeding.

Contraindications

Main contraindications:

• gipercupian;
• myasthenia;
• the presence of hypersensitivity to cyclobarbital or diazepam;
• the presence of suicidal tendencies in the patient;
• porphyria;
• liver failure;
• elderly age.

Side effects Reladorma

The severity and number of adverse symptoms are determined by the size of the portion and the sensitivity of the patient in relation to drugs. Among the manifestations:

• lesions affecting NS: often headaches, drowsiness, disorientation or confusion, and in addition, inhibition of reaction, ataxia and dizziness. Occasionally there is tremor or anger, and mood deteriorates. In addition, dysarthria rarely develops, accompanied by slurred speech, memory or accommodation disorder, abnormal behavior, and anterograde amnesia. In addition, emotional fluctuations, impoverishment of emotions, psychosis and nightmarish dreams, as well as incorrect pronunciation of words are rarely observed;
• disorders of visual function: visual impairment (diplopia or fuzziness);
• digestive disorders: disorder in the digestive tract, hypersalivation, dry oral mucosa, nausea or constipation;
• problems with the work of the kidneys and urinary ducts: the delay or incontinence of the urethra;
• lesions of connective tissue and musculoskeletal structure: the appearance of tremor;
• disorders of the CVS activity: an insignificant decrease in blood pressure values, bradycardia, vegetative signs, arrhythmia and heart failure (this includes cardiac arrest);
• symptoms of the respiratory system: the suppression of respiratory processes (this includes the lack of respiratory function);
• systemic disorders: feeling of general weakness (occasionally fainting occurs);
• lesions of the subcutaneous layer and epidermis: manifestations of allergies on the skin;
• disorders of the GIB and liver: a disorder in the liver. Jaundice develops individually or there is an increase in indicators of alkaline phosphatase and transaminases;
• signs of breast and reproductive organs: menstrual cycle disorder or libido;
• lesions affecting the lymph and blood: a disorder of the morphological blood composition (development of leukopenia or agranulocytosis);
• mental disorders: the appearance of paradoxical reactions (such as a feeling of excitement (also psychomotor) or aggressiveness, insomnia, seizures and tremor). In the form of a paradoxical reaction, there is also an increase in the feeling of hostility and anxiety, an increase in muscle tone (mainly in the elderly and children) and hallucinations. Often, such manifestations develop in older people and people with mental illnesses, and besides after drinking alcohol;
• other: pain in the joints, weakness in the muscles and an increase in the likelihood of fractures and falls (usually in older people).

Systematic administration of drugs for many weeks can cause drug dependence or withdrawal syndrome when abruptly stopping the use of the drug.

In mild forms of withdrawal, attention disorder, anxiety and headache occur. It is also possible the appearance of dizziness, nausea, feelings of irritability, hyperhidrosis, vomiting, and in addition to these disorders of perception, muscle spasms and colic. In addition, heartbeat may increase and appetite may be lost. Sometimes there are cramps or delirium.

Older patients, who often have a combination disorder and a feeling of fatigue, are extremely sensitive to negative symptoms.

Children, the elderly and those with hypoprothrombinemia may develop a tendency to increase the incidence of adverse sedation.

In the event of jaundice, visual disorders and disorders of the hematopoietic system, urinary incontinence and an increase in the activity of liver enzymes, it is necessary to cancel the use of reladorm.

[4]

Overdose

When poisoning occurs, symptoms such as a feeling of confusion or drowsiness, as well as unintelligible speech.

Severe intoxication can lead to the development of symptoms that threaten the patient’s health and life.

To eliminate the violations, gastric lavage is performed and the use of activated carbon is prescribed.

An antidote to reladorm is the substance flumazenil.

Interactions with other drugs

The drug can potentiate the activity of sedative drugs, antidepressants, antipsychotics and opiates.

Use with substances that slow down the oxidation of microsomes, prolongs the half-life of reladorm.

The drug destroys the metabolic processes of the substance phenytoin.

The drug is not compatible with griseofulvin, oral contraception, doxycycline, GCS, ethyl alcohol and anticoagulants.

[6], [7]

Storage conditions

Reladorm is required to be kept in a dark place, closed from small children. Temperatures - no higher than 25 ° C.

Shelf life

Reladorm can be used within 36 months from the date of manufacture of the drug.

Application for children

You can not prescribe medication in pediatrics.

Analogs

Analogues of drugs are such means as Corvaltab, Bellamintal, Belloid with Valocordin and Corvalol with Corvaldine.

Reviews

Reladorm receives quite good reviews from patients. If you follow the instructions and use them according to the indications, it demonstrates high efficiency.