Easysleep^® (Tablets) Instructions for Use

Marketing Authorization Holder

Atoll LLC (Russia)

Manufactured By

Ozon, LLC (Russia)

Contact Information

OZON LLC (Russia)

ATC Code

R06AA09 (Doxylamine)

Active Substance

Doxylamine (Rec.INN registered by WHO)

Dosage Form

Easysleep®

Dispersible tablets 15 mg: 30 pcs.

Dosage Form, Packaging, and Composition

Dispersible tablets white or almost white, oval, biconvex, with a score line, with a slight characteristic odor; minor surface roughness is allowed.

Excipients: microcrystalline cellulose (MCC-102) – 267.54 mg, croscarmellose sodium – 17 mg, crospovidone – 17 mg, aspartame – 8.16 mg, citric acid monohydrate – 6.8 mg, lemon flavor – 3.4 mg, magnesium stearate – 3.4 mg, colloidal silicon dioxide – 1.7 mg.

10 pcs. – blister packs (3) – cardboard packs.
15 pcs. – blister packs (2) – cardboard packs.
30 pcs. – blister packs (1) – cardboard packs.

Clinical-Pharmacological Group

Hypnotic drug

Pharmacotherapeutic Group

Systemic antihistamines; alkylamine esters

Pharmacological Action

H₁-histamine receptor blocker from the ethanolamines group. The drug has a hypnotic, sedative and m-anticholinergic effect. Reduces the time to fall asleep, increases the duration and quality of sleep, without changing the sleep phases. Duration of action is 6-8 hours.

Pharmacokinetics

Absorption

Absorption is high. C_max is achieved on average 2 hours after oral administration.

Distribution

Penetrates well through histohematic barriers (including the BBB).

Metabolism

Metabolized in the liver.

Excretion

T_1/2 is about 10 hours.

Excreted 60% by the kidneys unchanged, partially through the gastrointestinal tract.

Special patient groups

In patients over 65 years of age, as well as in hepatic and renal insufficiency, T_1/2 may be prolonged.

When treatment courses are repeated, the equilibrium concentration of the drug and its metabolites in the blood plasma is achieved later and at a higher level.

Indications

For adults and adolescents aged 15 years and older

• Transient sleep disorders.

ICD codes

Dosage Regimen

Orally.

Dissolve the tablet in a small amount of water (10-50 ml or 1/4 glass), the suspension must be stirred before use.

The recommended dose is 1/2 to 1 tablet per day, 15-30 minutes before bedtime.

If treatment is ineffective, on the doctor’s recommendation, the dose can be increased to 2 tablets. The duration of treatment is from 2 to 5 days; if insomnia persists, it is necessary to consult a doctor.

Patients with renal and hepatic impairment

Due to data on increased plasma concentration and decreased plasma clearance of doxylamine, dose adjustment downward is recommended.

Use in patients over 65 years of age

H₁-histamine receptor blockers should be prescribed with caution to this group of patients due to possible dizziness and slowed reactions with the risk of falls (for example, during nighttime awakenings after taking sleeping pills). In view of data on increased plasma concentration, decreased plasma clearance and increased half-life, dose adjustment downward is recommended.

Children

Easysleep^® is contraindicated for use in children from 0 to 15 years.

The dosage regimen for children from 15 to 18 years does not differ from the dosage regimen for adults.

Adverse Reactions

The frequency of adverse reactions is presented using the following gradation: very common (≥ 1/10); common (≥ 1/100 to < 1/10); uncommon (≥ 1/1000 to < 1/100); rare (≥ 1/10000 to < 1/1000); very rare (< 1/10000); frequency unknown (cannot be estimated from the available data).

Nervous system disorders: frequency unknown – daytime drowsiness (in this case, the dose of the drug should be reduced), confusion, hallucinations.

Eye disorders: frequency unknown – visual and accommodation disturbances, blurred vision.

Cardiac disorders: frequency unknown – palpitations.

Gastrointestinal disorders: frequency unknown – constipation, dry mouth.

Musculoskeletal and connective tissue disorders: frequency unknown – rhabdomyolysis.

Renal and urinary disorders: frequency unknown – urinary retention.

Laboratory and instrumental data: frequency unknown – increased CPK level.

Contraindications

• Hypersensitivity to doxylamine or other antihistamines, or other components of the drug;
• Closed-angle glaucoma or family history of closed-angle glaucoma;
• Urethral and prostatic diseases accompanied by impaired urine outflow;
• Phenylketonuria;
• Childhood and adolescence under 15 years.

With caution

Like all hypnotic or sedative drugs, Easysleep^® may worsen sleep apnea syndrome (sudden cessation of breathing during sleep), increasing the number and duration of apnea attacks. The drug should be prescribed with caution to patients with a history of apnea.

The drug should be prescribed with caution to patients over 65 years of age – due to possible dizziness and slowed reactions with the risk of falls (for example, during nighttime awakenings after taking sleeping pills), as well as due to a possible increase in T_1/2.

The drug should be prescribed with caution to patients with renal and hepatic insufficiency (T_1/2 may increase).

Use in Pregnancy and Lactation

Pregnancy

Based on adequate and well-controlled studies, Doxylamine can be used in pregnant women throughout the entire period of pregnancy.

If the drug is prescribed in late pregnancy, the atropine-like and sedative properties of doxylamine should be taken into account when monitoring the newborn’s condition.

Breastfeeding period

It is not known whether Doxylamine passes into breast milk. Due to the possibility of developing a sedative or excitatory effect in the child, breastfeeding should not be done while using the drug.

Use in Hepatic Impairment

Use with caution in patients with hepatic insufficiency.

Use in Renal Impairment

Use with caution in patients with renal insufficiency.

Pediatric Use

Contraindicated for use in children and adolescents under 15 years of age.

Geriatric Use

Use with caution in elderly patients over 65 years of age.

Special Precautions

It should be taken into account that insomnia can be caused by a number of reasons for which there is no need to prescribe this drug.

The drug has a sedative effect, suppresses cognitive abilities and slows psychomotor reactions.

First-generation H₁-antihistamines may have m-anticholinergic, anti-α-adrenergic and antiserotonin effects, which can cause dry mouth, constipation, urinary retention, accommodation and vision disorders.

Possible abuse of first-generation H₁-histamine receptor blockers, including Doxylamine, can lead to physical and psychological dependence, which has been reported against the background of intentional intake of higher doses of the drug than recommended.

Excipients

Easysleep^® contains aspartame, a source of phenylalanine. It may be harmful to people with phenylketonuria.

Effect on the ability to drive vehicles and operate machinery

Due to possible daytime drowsiness, driving vehicles, operating machinery and other activities requiring quick mental and motor reactions should be avoided.

Overdose

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

Involuntary movements are sometimes precursors to convulsions, which may indicate a severe degree of poisoning. Even in the absence of convulsions, severe doxylamine poisoning can cause the development of rhabdomyolysis, which is often accompanied by acute renal failure.

Treatment symptomatic (m-cholinomimetics and others), as a first aid measure, taking activated charcoal (in the amount of 50 g – for adults and 1 g/kg of body weight for children) is indicated. In case of severe poisoning, standard therapy with constant monitoring of CPK levels is indicated.

Drug Interactions

When taking Easysleep^® concomitantly with sedative antidepressants (amitriptyline, doxepin, mianserin, mirtazapine, trimipramine), barbiturates, benzodiazepines, clonidine, morphine derivatives (analgesics, antitussives), antipsychotics, anxiolytics, sedative histamine H₁-receptor blockers, central antihypertensive drugs, thalidomide, baclofen, pizotifen, the depressant effect on the central nervous system is enhanced.

When taken concomitantly with m-anticholinergic agents (atropine, imipramine antidepressants, antiparkinsonian drugs, atropine antispasmodics, disopyramide, phenothiazine antipsychotics), the risk of such side effects as urinary retention, constipation, dry mouth increases.

Since alcohol enhances the sedative effect of most H₁-histamine receptor antagonists, including doxylamine, its simultaneous consumption with alcoholic beverages and medicinal products containing alcohol should be avoided.

Storage Conditions

The drug should be stored out of the reach of children at a temperature not exceeding 25°C (77°F) in the original packaging (carton).

Shelf Life

The shelf life is 3 years. Do not use after the expiration date.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.