Hypnos®

INSTRUCTIONS for medical use of the medicinal product Hypnos®

Composition:

Active substance: doxylamine succinate;

One coated tablet contains doxylamine succinate 15 mg;

Excipients: lactose monohydrate, microcrystalline cellulose, sodium croscarmellose, magnesium stearate, Opadry F85 White.

Medicinal form. Coated tablets.

Main physicochemical properties: oval-shaped coated tablets of white or almost white color, with a double-score line for division.

Pharmacotherapeutic group. Antihistamines for systemic use. Doxylamine. ATC code R06AA09.

Other hypnotics and sedatives. ATC code N05CM.

Pharmacological properties.

Pharmacodynamics.

Hypnos® is a hypnotic agent of the ethanolamine class and belongs to the group of histamine H1-receptor blockers, exerting sedative and M-cholinoblocking effects. It reduces sleep onset latency and improves sleep duration and quality.

Pharmacokinetics.

Maximum plasma concentration is reached 2 hours after tablet administration. The mean elimination half-life from plasma is approximately 10 hours.

Doxylamine succinate undergoes biotransformation in the liver. It is partially metabolized in the liver via demethylation and N-acetylation. The elimination half-life may be significantly prolonged in elderly patients or in patients with renal or hepatic impairment. Various metabolites formed during breakdown are not quantitatively significant, as 60% of the administered dose is excreted unchanged in urine.

Clinical characteristics.

Indications.

Periodic insomnia in adults.

Contraindications.

• Hypersensitivity to any component of the medicinal product or to other antihistamine medicinal products;
• History or family history of acute angle-closure glaucoma;
• Urinary retention (urethral or prostate disorders).

Interaction with other medicinal products and other forms of interaction.

Combinations to be avoided:

• With alcohol, as it enhances the sedative effect of most H1-antihistamines. Consumption of alcoholic beverages and use of medicinal products containing ethanol should also be avoided;
• With sodium oxybate, due to increased central nervous system depression. Impaired reaction speed may be hazardous when driving or operating machinery.

Combinations requiring caution:

• With atropine and atropine-like medicinal products (tricyclic antidepressants, most anticholinergic H1-antihistamines, anticholinergic antiparkinsonian agents, atropine-like spasmolytics, disopyramide, phenothiazine neuroleptics, as well as clozapine) — possible side effects such as urinary retention, constipation, dry mouth;
• With other sedative medicinal products (morphine derivatives (analgesics used for cough treatment and substitution therapy), neuroleptics; barbiturates, benzodiazepines; anxiolytics other than benzodiazepines (meprobamate); sedative antidepressants (amitriptyline, doxepin, mianserin, mirtazapine, trimipramine); sedative H1-antihistamines; centrally acting antihypertensives; others: baclofen, pizotifen, thalidomide) — enhanced central nervous system depression should be considered. Impaired reaction speed may be hazardous when driving or operating machinery;
• With other hypnotics — central nervous system depression should be taken into account.

Special precautions for use.

Insomnia may have various causes that do not necessarily require drug treatment; therefore, it is recommended to consult a physician before starting the use of this medicinal product.

Like all hypnotic or sedative agents, doxylamine succinate may exacerbate the 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 on the medicinal product must be carefully monitored. Treatment duration should not exceed 5 days. The use of this medicinal product is not recommended in patients with a history of disorders caused by psychoactive substance use.

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

The half-life may be significantly prolonged in elderly individuals or in patients with renal or hepatic impairment. With repeated administration, the drug or its metabolites reach steady-state concentrations much later and at higher levels. The efficacy and safety of the medicinal product can only be assessed after reaching steady-state concentrations. Therefore, dose adjustment may be required (see section "Dosage and administration").

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

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 recommended.

To prevent daytime drowsiness, it is important to remember that the duration of sleep after taking the medicinal product should be at least 7 hours.

Important information about excipients.

Since the medicinal product contains lactose, it should not be administered to patients with rare hereditary forms of galactose intolerance, lactase deficiency, or glucose-galactose malabsorption syndrome.

The medicinal product contains sodium; therefore, caution should be exercised when administering it to patients on a sodium-controlled diet.

Use during pregnancy or breastfeeding.

Based on available data, the medicinal product may be used during pregnancy after consultation with a physician. If doxylamine is administered in late pregnancy, the newborn should be monitored for atropine-like and sedative effects of this molecule.

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

Effect on ability to drive vehicles or operate machinery.

Gipnos® affects psychomotor reaction speed (risk of daytime drowsiness); therefore, patients should refrain from driving vehicles or operating machinery. The risk of impaired reaction speed increases if sleep duration is insufficient.

Dosage and Administration.

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

The recommended dose is 7.5–15 mg per day (½–1 tablet per day). If necessary, the dose may be increased up to 30 mg per day (2 tablets per day).

For elderly patients and patients with renal or hepatic impairment, a lower dose is recommended.

The duration of treatment is 2–5 days.

If insomnia persists for more than 5 days, a physician should be consulted regarding the appropriateness of continued use of the medicinal product.

Children.

The medicinal product must not be used in children (under 18 years of age).

Overdose.

Symptoms.

The initial signs of acute poisoning include drowsiness and anticholinergic effects: excitation, mydriasis, 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—a rare complication of severe poisoning—or even coma. Even in the absence of seizures, acute doxylamine poisoning may occasionally cause rhabdomyolysis, which can lead to acute renal failure. This muscular disorder is relatively common and requires systematic screening by measuring creatine phosphokinase activity.

Treatment.

Administration of activated charcoal (50 g for adults and 1 g/kg for children). Symptomatic treatment should be administered if necessary. Anticonvulsants and artificial ventilation of the lungs may be prescribed when indicated.

Side effects.

In the morning, following evening administration of the medicinal product, slowed reactions and dizziness may occur; therefore, to prevent falls, sudden movements should be avoided. Anticholinergic effects may rarely develop: constipation, dry mouth, accommodation disturbances, tachycardia, urinary retention, visual disturbances (accommodation disorders, blurred vision, hallucinations, visual defects), hallucinations, confusion.

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

Allergic reactions may occur, including skin rash and itching.

Cases of abuse and drug dependence have been reported.

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

Reporting of suspected adverse reactions.

Reporting of suspected adverse reactions after marketing authorization of the medicinal product is of great importance. It enables ongoing monitoring of the benefit-risk balance of the medicinal product. Medical and pharmaceutical professionals, as well as patients or their legal representatives, should report all suspected adverse reactions and/or lack of efficacy via the Automated Information System for Pharmacovigilance at the following link: https://aisf.dec.gov.ua.

Shelf life. 3 years.

Storage conditions.

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

Packaging.

10 tablets in a blister pack; 1 blister pack per carton.

Availability.

Over-the-counter (without prescription).

Manufacturer. JSC "Pharmaceutical Company "Darnytsia".

Manufacturer's address and location of business activity.

13, Boryspylska Street, Kyiv, 02093, Ukraine.