Hypnos®

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT Hypnos®

Composition:

Active ingredient: doxylamine;

0.6 mL (13 drops) contains doxylamine succinate 15 mg;

Excipients: ethanol 96%, peppermint oil, purified water.

Pharmaceutical form. Oral drops, solution.

Main physicochemical properties: clear, colorless liquid with a characteristic odor.

Pharmacotherapeutic group. Hypnotics and sedatives. Other hypnotics and sedatives. ATC code N05CM.

Antihistamines for systemic use. Doxylamine. ATC code R06AA09.

Pharmacological properties.

Pharmacodynamics.

Doxylamine succinate is an H1-histamine receptor antagonist of the ethanolamine class, exhibiting sedative and atropine-like effects. It has been demonstrated to reduce the time required to fall asleep, as well as to improve sleep duration and quality.

Pharmacokinetics.

Maximum plasma concentration (C_max) is reached on average within 1 hour (T_max) after administration of doxylamine succinate.

The average elimination half-life from plasma (T_½) is approximately 10 hours.

Doxylamine succinate is partially metabolized in the liver via demethylation and N-acetylation. The various metabolites formed during degradation are not quantitatively significant, as 60% of the administered dose is excreted in urine as unchanged doxylamine.

Clinical characteristics.

Indications.

Intermittent insomnia in adults.

Contraindications.

• Hypersensitivity to doxylamine succinate, to any of the excipients, or to other antihistamines.
• History of acute angle-closure glaucoma in the patient or family history of this condition.
• Urethroprostatic disorders with risk of urinary retention.

Interaction with other medicinal products and other forms of interaction.

Combinations to be avoided

Alcohol enhances the sedative effect of most H1-antihistamines. Consumption of alcoholic beverages and use of medicinal products containing ethanol should be avoided.

The medicinal product should also not be used concomitantly with sodium oxybate due to increased central nervous system depression. Impaired reaction speed may lead to danger when driving vehicles or operating machinery.

Combinations to be taken into consideration

With atropine and atropine-like medicinal products (tricyclic antidepressants, most anticholinergic H1-antihistamines, anticholinergic antiparkinsonian agents, atropine-containing spasmolytics, disopyramide, phenothiazine neuroleptics, as well as clozapine) due to increased risk of adverse reactions such as urinary retention, constipation, dry mouth.

With other sedative medicinal products (morphine derivatives (analgesics, antitussives, substitution therapy agents), neuroleptics, barbiturates, benzodiazepines, anxiolytics other than benzodiazepines (meprobamate), other hypnotics, sedative antidepressants (amitriptyline, doxepin, mianserin, mirtazapine, trimipramine), sedative H1-antihistamines, centrally-acting antihypertensives, and others: baclofen, thalidomide) due to enhanced central nervous system depression. Impaired reaction speed may lead to danger when driving vehicles or operating machinery.

With other hypnotic agents due to central nervous system depression.

Special precautions for use

Insomnia may have various causes that do not necessarily require pharmacological treatment; therefore, consultation with a physician is recommended before initiating therapy with this medicinal product.

Like all hypnotics or sedatives, doxylamine succinate may exacerbate sleep apnea syndrome (increasing the number and duration of breathing pauses).

The risk of abuse and development of drug dependence is low. However, cases of abuse leading to drug dependence have been reported. Signs of abuse or dependence should therefore be carefully monitored. Treatment duration should not exceed 5 days. The medicinal product is not recommended for patients with a history of substance-related disorders.

Doxylamine succinate remains in the body for approximately 5 elimination half-lives (see section "Pharmacokinetics").

The elimination half-life may be significantly prolonged in elderly patients or in patients with renal or hepatic impairment. With repeated administration, the drug or its metabolites reach steady-state levels much later and at higher concentrations. The efficacy and safety of the medicinal product can only be assessed after steady-state has been achieved.

Dosage adjustment may be required (see section "Dosage and administration").

H1-antihistamines should be used with caution in elderly patients due to the risk of cognitive disorders, sedative effects, slowed reaction time, and/or vertigo/dizziness, which may increase the risk of falls (e.g., when getting up at night), potentially leading to serious consequences in this patient population.

In elderly patients with renal or hepatic impairment, increased plasma concentrations of the drug and reduced plasma clearance have been observed. A reduced dose of the medicinal product is therefore recommended.

To avoid daytime drowsiness, it is important to ensure that sleep duration after taking the medicinal product is at least 7 hours.

Important information on excipients

This medicinal product contains 55 vol.% ethanol (ethyl alcohol), corresponding to 135 mg/270 mg/540 mg of ethyl alcohol per single dose (equivalent to 3.28 mL/6.56 mL/13.12 mL of beer or 1.36 mL/2.73 mL/5.46 mL of wine). The product may be harmful to individuals suffering from alcoholism. The ethyl alcohol content should be taken into account in pregnant women and breastfeeding women, and in patients at risk, such as those with liver disease or epilepsy.

Use during pregnancy or breastfeeding

Pregnancy

Based on available data, doxylamine may be used during pregnancy after consultation with a physician. If this medicinal product is administered towards the end of pregnancy, the anticholinergic and sedative properties of this molecule should be considered when monitoring the newborn.

Breastfeeding

It is unknown whether doxylamine passes into breast milk; therefore, the use of this medicinal product is not recommended during breastfeeding.

Ability to influence reaction speed when driving or operating machinery

Caution regarding the risk of daytime drowsiness is required, particularly when the medicinal product is used concomitantly with alcohol (see section "Interaction with other medicinal products and other forms of interaction") in patients who drive or operate machinery. The risk of impaired reaction speed is increased in cases of insufficient sleep duration. Therefore, driving, operating machinery, and other potentially hazardous activities should be avoided, at least during the initial phase of treatment.

Dosage and Administration.

For oral use. Take 15–30 minutes before bedtime.

The recommended dose is 7.5–15 mg (7–13 drops) per day. If necessary, the dose may be increased up to 30 mg (26 drops) per day. The drops should be taken with sufficient amount of liquid, approximately ½ glass of water.

In elderly patients and patients with renal or hepatic impairment, a reduced dose is recommended.

The duration of treatment is 2–5 days.

If insomnia persists for more than 5 days, consult a physician regarding the appropriateness of continuing the medication.

Children.

The medication must not be used in children under 18 years of age.

Overdose.

The initial signs of acute poisoning include drowsiness and anticholinergic effects: excitation, dilated pupils, accommodation paralysis, dry mouth, facial and neck flushing, hyperthermia, and sinus tachycardia. Delirium, hallucinations, and athetoid movements are more commonly observed in children and may sometimes precede seizures—rare complications of massive poisoning—or even coma. Even in the absence of seizures, acute poisoning with doxylamine may occasionally cause rhabdomyolysis, which can lead to acute renal failure. This muscular disorder is relatively common, necessitating systematic screening through measurement of creatine phosphokinase activity.

Treatment is symptomatic. In early-stage management, activated charcoal is recommended (50 g for adults, 1 g/kg for children).

Side effects

Anticholinergic effects: constipation, urinary retention, dry mouth, visual disturbances (accommodation disorder, blurred vision, hallucinations, visual defects), tachycardia, confusion.

Daytime drowsiness: if this effect occurs, the dose should be reduced.

Cases of drug abuse and development of drug dependence have been reported.

In addition, it is known that H1-antihistamine medicinal products may produce sedative effects, cognitive disorders, and psychomotor impairment.

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after authorization of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are required to report any suspected adverse reactions through the national reporting system.

Shelf life. 3 years.

After opening the bottle – 6 months.

Storage conditions.

Store in the original packaging at a temperature not exceeding 25 °C. Keep out of reach of children.

Packaging.

5 ml in a dropper bottle; 1 dropper bottle per pack.

Availability.

Over-the-counter.

Manufacturer. JSC "Pharmaceutical Company "Darnitsya".

Manufacturer's address and location of its business activities.

13, Boryspylska Street, Kyiv, 02093, Ukraine.