Valocordin Doxylamine Drops 20ml

Active ingredient

Active substance

Doxylamine succinate 25.0 mg.

Excipients

Ethanol 96% 450.0 mg, mint oil 1.4 mg, purified water 449.7 mg.

In a bottle of dark glass 20 ml drops. In the package 1 bottle.

Indications

Symptomatic treatment of recurrent sleep disorders in adults:

-The difficulty of falling asleep.

-Night awakenings.

Pharmacokinetics

It is mainly metabolized in the liver. It penetrates well through histohematogenous barriers (including the blood-brain barrier). The half-life ranges from 10.1 to 12 hours. The main part of the dose (ca. 60%) is excreted unchanged in the urine, and partly in the intestine.

Clinical Pharmacology

Blocker H₁- histamine receptors from the group of ethanolamines. The drug has a sedative, sedative and m-holinoblokiruyuschee effect. Reduces the time of falling asleep, increases the duration and quality of sleep.

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

Pregnanacy and breastfeeding

Valocordin-Doxylamine can be used during pregnancy only when the intended benefit to the mother outweighs the possible risk to the fetus. Breastfeeding should be discontinued during treatment, since the active substance is excreted into breast milk.

Contraindications

• Hypersensitivity to any of the components of the drug.
• Closed angle glaucoma.
• Prostate hyperplasia, urinary retention.
• Lactation period.
• Children's age up to 18 years.

• Liver disease.
• Alcoholism.
• Brain injury or brain disease.
• Pregnancy.

Adverse Effects

The frequency of side effects is given in accordance with the following scale:

• Very often (> 1/10).
• Often (from> 1/100 to <1/10).
• Infrequently (from> 1/1000 to <1/100).
• Rarely (from> 1/10 000 to <1/1000).
• Very rarely (<1/10 000).

Most often marked

Constipation, dry mouth, disturbance of accommodation, urinary retention, daytime sleepiness - in this case, the dose of the drug should be reduced.

Since the cardiovascular system

Often - tachycardia, cardiac arrhythmias, decrease or increase in blood pressure and decompensation of an existing heart rhythm disorder.

Changes on an ECG are possible.

From the hematopoietic system and the lymphatic system

Aplastic anemia and agranulocytosis were very rarely observed.

In extremely rare cases, after the use of antihistamine drugs, changes in the blood picture in the form of leukopenia, thrombocytopenia, and hemolytic anemia may appear.

The nervous system

Often - dizziness, headache.

From the senses

Increased intraocular pressure.

Ear and ear maze disorders: tinnitus.

On the part of the respiratory system

Thickening of the bronchial secretions, bronchial obstruction and bronchospasm, which can lead to deterioration of the respiratory function.

From the gastrointestinal tract

Often - nausea, vomiting, diarrhea, loss or increase in appetite, pain in the epigastrium.

In very rare cases, life-threatening paralytic intestinal obstruction may occur.

Reported abnormal liver function (cholestatic jaundice) during therapy with blockers H₁- histamine receptors.

From the urinary system

Impaired urination

On the part of the skin

Allergic skin reactions, photosensitivity and thermoregulation disorders may occur.

From the endocrine system

In patients with pheochromocytoma, taking antihistamines may lead to an increase in catecholamine release.

Common disorders

Sensation of nasal congestion, fatigue, muscle weakness.

Mental disorders

Undesirable effects that depend on the individual sensitivity and the dose: delayed reaction, impaired concentration, low mood.

In addition, there is a possibility of the appearance of so-called “paradoxical” reactions, such as anxiety, nervous agitation, psycho-emotional stress, insomnia, nightmares, confusion, hallucinations, tremors.

After prolonged daily use against the background of a sudden discontinuation of therapy, sleep disturbances may increase.

Development of tolerance

After long-term use of sedatives, loss of efficacy (tolerance) may occur.

Addiction

As well as taking other sedatives, taking Valocordin-Doxylamine can lead to the development of physical and mental dependence. The risk of addiction increases with increasing doses and duration of treatment and increases in patients with alcohol, drug or drug addiction in history.

Even at the end of the short-term treatment with Valocordin-Doxylamine, due to sudden withdrawal, temporary sleep disturbances may occur again. Therefore, it is recommended, if necessary, to complete the treatment, gradually reducing the dose.

Anterograde amnesia

Even at therapeutic doses, sedatives can provoke anterograde amnesia, especially in the first hours after ingestion. The risk increases with increasing dose, but can be reduced due to a sufficiently long continuous sleep (7-8 hours).

Interaction

While taking the drug Valocordin-Doxylamine with antidepressants, barbiturates, benzodiazepines, clonidine, narcotic analgesics (analgesics, antitussives), neuroleptics, anxiolytics, sedatives, blockers H₁-histamine receptors, central antihypertensive drugs, thalidomide, Baclofen, pizothiphene enhances the inhibitory effect on the central nervous system.

When taken simultaneously with m-anticholinergic blocking agents (atropine, tricyclic antidepressants, antiparkinsonic drugs, atropine antispasmodics, disopyramide, phenothiazine neuroleptics), the risk of such side effects as urinary retention, constipation, dry mouth increases.

Since alcohol enhances the sedative effect of most H blockers.₁-histamine receptors, incl. and the drug Valocordin-Doxylamine, it is necessary to avoid the simultaneous use of alcoholic beverages and drugs containing alcohol.

Overdosage

Symptoms: daytime sleepiness, pupil dilation (Mydriasis), accommodation disturbances, dry mouth, redness of the skin of the face and neck (hyperemia), fever (hyperthermia), sinus tachycardia, disorder of consciousness, hallucinations, decreased mood, anxiety, poor coordination of movements, tremor (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 poisoning with doxylamine can cause the development of rhabdomyolysis, which is often accompanied by severe renal failure. In such cases, standard therapy is shown with constant monitoring of creatine phosphokinase activity.

Treatment: if symptoms of poisoning appear, you should immediately consult a doctor. Symptomatic treatment (m-cholinomimetics, etc.), as a means of first aid, reception of Activated carbon (in the amount of 50 g) is shown.

Dosage and administration

For oral administration.

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

Unless otherwise prescribed by a doctor, a single dose of the drug Valocordin-Doxylamine for adults is 22 drops (which corresponds to 25.0 mg of doxylamine succinate).

For 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, you should take enough time to sleep to avoid a delayed reaction the next morning.

Reception duration

In acute sleep disorders, if possible, confine yourself to a single use. In case of intermittent sleep disorders, to check the need to continue treatment, it is necessary no later than 14 days after the start of daily use to gradually reduce the dose.

Precautionary measures

Valocordin-Doxylamine contains 55% by volume of ethanol (alcohol), i.e. up to 900 mg per dose, which corresponds 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.

Patients with renal and hepatic failure

In connection with the data on the increase in plasma concentration and a decrease in the plasma clearance of doxylamine, a downward dose adjustment is recommended.

Use for patients older than 65 years

Blockers H₁- histamine receptors should be carefully prescribed to this group of patients in connection with possible dizziness and delayed reactions with the danger of falling (for example, during night awakenings after taking sleeping pills).

Influence on ability to drive motor transport and control mechanisms

Due to the possible drowsiness in the daytime, driving a car, working with mechanisms and other activities that require quick mental and motor responses should be avoided.

Storage conditions

Store at temperatures up to 25 ° C.

Keep out of reach of children.