Valokordin-Doxylamine, drops 25 mg/ml 20 ml

Pharmacodynamics

A blocker of H₁-histamine receptors from the group of ethanolamines. The drug has soporific, sedative and m-cholinoblocking effects. It shortens the time of falling asleep, increases the duration and quality of sleep, but does not change the phase of sleep.

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

Pharmacokinetics

Mainly metabolized in the liver. It penetrates well through histohematic barriers (including the blood-brain barrier). The elimination half-life varies from 10.1 to 12 hours. The main part of the dose (about 60%) is excreted unchanged in the urine, partially in the intestine.

Indications

Active ingredient

Composition

1 ml of the drug (22 drops) contains:

The active ingredient:

doxylamine succinate – 25.0 mg.

Auxiliary substances:

Ethanol 96% – 450.0 mg,

Mint oil – 1.4 mg,

Purified water – 449.7 mg.

How to take, the dosage

For oral administration.

The drops should be taken with enough fluid (water) 30 minutes to 1 hour before bedtime.

Unless otherwise directed by the physician, the single dose of Valokordin-Doxylamine for adults is 22 drops (corresponding to 25.0 mg of doxylamine succinate). For severe sleep disturbances, the patient may take the maximum dose of the drug, 44 drops (corresponding to 50.0 mg of doxylamine succinate).

The total daily dose should not exceed 44 drops.

Please note that after taking Valocordin-Doxylamine, care should be taken to allow sufficient time for sleep to avoid a delayed response the next morning.

Persons with renal or hepatic impairment

Patients with increased plasma concentrations and decreased plasma clearance of doxylamine recommend that the dose be adjusted downward.

The use in patients over 65 years of age

H1-histamine receptor blockers should be prescribed with caution in this group of patients due to possible dizziness and delayed reactions with danger of falling (for example, in nighttime awakenings after taking sleeping pills).

The duration of administration

In acute sleep disturbances, if possible, single use should be limited. To verify the need for continued treatment with intermittent sleep disturbances, the dose should be gradually reduced no later than 14 days after the start of daily use.

Interaction

In concomitant administration of Valokordin-Doxylamine with antidepressants, barbiturates, benzodiazepines, clonidine, narcotic analgesics (analgesics, anti-cough medications), neuroleptics, anxiolytics, sedatives, H

Special Instructions

Valocordine-Doxylamine contains 55 vol% 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.

Impact on driving and operating machinery

Because of possible drowsiness during the daytime, driving, operating machinery and other activities requiring rapid mental and motor reactions should be avoided.

Contraindications

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

Side effects

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

The most common side effects noted are constipation, dry mouth, accommodation disorders, urinary retention, daytime sleepiness (in this case the drug dose should be reduced).

Rarely (0.01% to 10%) are likely:

Cardiovascular system: tachycardia, heart rhythm disturbances, decreased or increased blood pressure and decompensation of existing heart rhythm disturbances may occur. Changes on the ECG are possible.

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

Nervous system: dizziness, headache.

Visual disorders: increase in intraocular pressure.

Ear and ear labyrinth disorders: tinnitus.

Respiratory system: thickening of bronchial secretion, bronchial obstruction and bronchospasm which may lead to impaired respiratory function.

Gastrointestinal tract: nausea, vomiting, diarrhea, loss or increase of appetite, pain in the epigastrium. In very rare cases life-threatening paralytic intestinal obstruction may occur. Liver dysfunction (cholestatic jaundice) has been reported with therapy with H1-histamine receptor blockers.

To the urinary system: impaired urination.

The skin: allergic skin reactions, photosensitization and thermoregulation disorders may be observed.

Endocrine systems: in patients with pheochromocytoma, taking antihistamines may increase catecholamine release.

General disorders: nasal congestion, fatigue, muscle weakness.

Mental disorders: unwanted effects that depend on individual sensitivity and the dose taken include: delayed reaction time, impaired concentration, low mood. In addition, there is a possibility of so-called “paradoxical” reactions such as anxiety, nervous agitation, psycho-emotional tension, insomnia, nightmares, confusion, hallucinations, tremors. After long-term daily use against the background of abrupt withdrawal of therapy, sleep disturbances may worsen.

The development of tolerance: loss of effectiveness (tolerance) may occur after prolonged use of sedatives.

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

Antherograde amnesia: Even at therapeutic doses, sedatives can provoke anterograde amnesia, especially in the first hours after administration. The risk increases with increasing dose, but can be reduced by sufficiently long uninterrupted sleep (7-8 hours).

Overdose

Symptoms: daytime sleepiness, dilated pupils (mydriasis), accommodation disorders, dry mouth, redness of the face and neck skin (hyperemia), increased body temperature (hyperthermia), sinus tachycardia, impaired consciousness, hallucinations, reduced mood, anxiety, movement coordination disorders, tremors (tremor), involuntary movements (athetosis), convulsions (epileptic syndrome), coma.

The involuntary movements are sometimes precursors to seizures, which may indicate a severe degree of poisoning. Even in the absence of seizures severe doxylamine poisoning may cause development of rhabdomyolysis, which is often accompanied by severe renal failure. In such cases standard therapy with continuous monitoring of creatine phosphokinase activity is indicated. If symptoms of poisoning occur, consult a doctor immediately.

The treatment: symptomatic (m-cholinomimetics, etc.), as a first aid measure activated charcoal (50 g) is indicated.

Pregnancy use

Valocordine-Doxylamine may be used during pregnancy only when the estimated benefit to the mother exceeds the possible risk to the fetus.

Breastfeeding should be stopped during treatment because the active ingredient is excreted into the breast milk.

Similarities