Valokordin-Doxylamine, drops 25mg/ml, 20ml

Composition

1 ml of the drug (22 drops) contains:

Active ingredient:

doxylamine succinate – 25.0 mg.

Auxiliary substances:

ethanol 96% – 450.0 mg,

peppermint oil-1.4 mg,

purified water-449.7 mg

Pharmacological action

Pharmacodynamics

Blocker of_H1-histamine receptors from the group of ethanolamines. The drug has a hypnotic, sedative and m-holinoblokiruyushchy effect. Reduces the time of falling asleep, increases the duration and quality of sleep, but does not change the sleep phase.

Doxylamine is rapidly and almost completely absorbed immediately after oral use. The action begins within 30 minutes, the maximum serum concentration of 99 ng / ml is detected 2.0-2.4 hours after oral use of a dose of 25 mg. Duration of action is from 3 to 6 hours.

Pharmacokinetics

It is mainly metabolized in the liver. Penetrates well through histohematic barriers (including the blood-brain barrier). The elimination half-life ranges from 10.1 to 12 hours. The main part of the dose (approx. 60%) is excreted unchanged in the urine, partially in the intestines.

Indications

• Symptomatic treatment of recurrent sleep disorders (difficulty falling asleep and nighttime awakenings) in adults.

Use during pregnancy and lactation

Valocordin-Doxylamine can be used during pregnancy only when the intended benefit to the mother outweighs the possible risk to the fetus.

Breast-feeding should be stopped during treatment, as the Active ingredient is released into breast milk.

Contraindications

• Hypersensitivity to doxylamine and other components of the drug.
• Angle-closure glaucoma.
• Prostatic hyperplasia, urinary retention.
• Childhood and adolescence.

With caution: pregnancy, liver disease, alcoholism, traumatic brain injury or brain diseases.

Side effects

The frequency of side effects is given according to the following scale:

• Very frequent-1/10 of appointments ( > 10%).
• Frequent-1/100 appointments ( > 1% and >
• Infrequent-1/1000 appointments ( > 0.1% and >
• Rare-1/10000 appointments ( > 0.01% and >
• Very rare-less than 1/10000 appointments (

Most frequently reported side effects:  constipation, dry mouth, accommodation disorders, urinary retention, daytime drowsiness (in this case, the dose of the drug should be reduced).

Less often (from 0.01% to 10%) are likely:

Cardiovascular system:  tachycardia, cardiac arrhythmias, decreased or increased blood pressure, and decompensation of an existing cardiac arrhythmia may occur. Possible changes on the ECG.

Hematopoietic system and lymphatic system:  in extremely rare cases, after the use of antihistamines, changes in the blood picture may appear in the form of leukopenia, thrombocytopenia and hemolytic anemia, aplastic anemia and agranulocytosis were very rarely observed.

The nervous system:  dizziness, headache.

Visual disorders:  increased intraocular pressure.

Disorders of the ear and ear labyrinth:  tinnitus.

Respiratory system:  thickening of bronchial secretions, bronchial obstruction and bronchospasm, which can lead to deterioration of respiratory function.

Gastrointestinal tract:  nausea, vomiting, diarrhea, loss or increase of appetite, epigastric pain. In very rare cases, a life-threatening paralytic intestinal obstruction may occur. Hepatic dysfunction (cholestatic jaundice) has been reported during therapy_{with H1}-histamine receptor blockers.

Urinary system:  violation of urination.

Skin conditions:  allergic skin reactions, photosensitization and thermoregulation disorders may occur.

Endocrine system:  in patients with pheochromocytoma, taking antihistamines may lead to increased catecholamine release.

Common disorders:  nasal congestion, fatigue, muscle weakness.

Mental disorders:  undesirable effects that depend on individual sensitivity and the dose taken include: delayed reaction, impaired concentration of attention, low mood. In addition, there is a possibility of the appearance of so-called “paradoxical” reactions, such as anxiety, nervous excitement, psychoemotional tension, insomnia, night “nightmares”, confusion, hallucinations, tremor. After long-term daily use, sleep disorders may increase against the background of sudden discontinuation of therapy.

Developing tolerance:  after prolonged use of sedatives, there may be a loss of effectiveness (tolerance).

Dependency:  As with other sedatives, taking Valocordin-Doxylamine can lead to the development of physical and mental dependence. The risk of addiction increases with increasing dose and duration of treatment and increases in patients with a history of alcohol, drug or drug addiction. Even at the end of short-term treatment with Valocordin-Doxylamine, temporary sleep disturbances may occur again due to sudden withdrawal. Therefore, it is recommended, if necessary, to complete the treatment, gradually reducing the dose.

Anterograde amnesia:  even in therapeutic doses, sedatives can cause anterograde amnesia, especially in the first hours after use. The risk increases with increasing dose, but can be reduced by getting enough continuous sleep (7-8 hours).

Interaction

Concomitant use of Valocordin-Doxylamine with antidepressants, barbiturates, benzodiazepines, clonidine, narcotic analgesics (analgesics, antitussives), neuroleptics, anxiolytics, sedatives, _H1-histamine receptor blockers, central antihypertensive drugs, thalidomide, baclofen, pisotifen increases the depressive effect on the central nervous system.

When taken concomitantly with m-cholinoblockers (atropine, tricyclic antidepressants, antiparkinsonian drugs, atropine antispasmodics, disopyramide, phenothiazine neuroleptics), the risk of side effects such as urinary retention, constipation, and dry mouth increases.

Since alcohol increases the sedative effect of most_H1-histamine receptor blockers, including Valocordin-Doxylamine, it is necessary to avoid the simultaneous use of alcoholic beverages and drugs containing alcohol.

How to take, course of use and dosage

For oral use.

Drops should be taken with a sufficient amount of liquid (water) 30 minutes – 1 hour before bedtime.

If the doctor does not prescribe otherwise, then a single dose of Valocordin-Doxylamine for adults is 22 drops (which corresponds to 25.0 mg of doxylamine succinate). In case of serious sleep disorders, the patient can take the maximum dose of the drug – 44 drops (which corresponds to 50.0 mg of doxylamine succinate).

The total daily dose should not exceed 44 drops.

It should be borne in mind that after taking the drug Valocordin-Doxylamine, care should be taken to ensure sufficient time for sleep in order to avoid a delayed reaction the next morning.

Use in special patient groups

Patients with renal and hepatic insufficiency

Due to data on an increase in plasma concentrations and a decrease in plasma clearance of doxylamine, a dose adjustment is recommended in the direction of decreasing.

Use in patients over 65 years of age

_H1-histamine receptor blockers should be used with caution in this group of patients due to possible dizziness and delayed reactions with a risk of falling (for example, when waking up at night after taking sleeping pills).

Duration of admission

In case of acute sleep disorders, if possible, limit yourself to a single application. In order to check the need for continuing treatment with periodic sleep disorders, it is necessary to gradually reduce the dose no later than 14 days after the start of daily use.

Overdose

Symptoms:  daytime sleepiness, pupil dilation (mydriasis), accommodation disorders, dry mouth, redness of the face and neck (hyperemia), fever (hyperthermia), sinus tachycardia, confusion, hallucinations, decreased mood, anxiety, impaired coordination of movements, trembling (tremor), involuntary movements (athetosis), convulsions (epileptic syndrome), coma.

Involuntary movements are sometimes harbingers of seizures, which may indicate a severe degree of poisoning. Even in the absence of seizures, severe doxylamine poisoning can cause the development of rhabdomyolysis, which is often accompanied by severe renal failure. In such cases, standard therapy with constant monitoring of creatine phosphokinase activity is indicated. If you experience symptoms of poisoning, you should immediately consult a doctor.

Treatment:  symptomatic (m-cholinomimetics, etc. ), as a first aid agent, the intake of activated carbon (in the amount of 50 g) is indicated.

Special instructions

Valocordin-Doxylamine contains 55% by volume of ethanol (alcohol), i. e. up to 900 mg per dose, which corresponds to up to 21.87 ml of beer or 9.11 ml of wine per dose. It is dangerous for people with liver diseases, alcoholism, epilepsy, as well as for pregnant women and children.

Influence on the ability to drive motor vehicles and manage mechanisms

Due to possible daytime drowsiness, driving vehicles, working with mechanisms, and other activities that require rapid mental and motor reactions should be avoided.

Form of production

Drops for oral use

Storage conditions

3 years. Shelf life after opening the bottle: 6 months.

Shelf

life Store at a temperature not exceeding 25 °C. Keep out of reach of children.

Active ingredient

Doxylamine

Conditions of release from pharmacies

By prescription

Dosage form

Drops for oral use

Purpose

For pregnant women as prescribed by a doctor, For adults as prescribed by a doctor

Indications

Insomnia