Sleepzone^® (Tablets) Instructions for Use

Marketing Authorization Holder

Krka d.d., Novo mesto (Slovenia)

ATC Code

R06AA09 (Doxylamine)

Active Substance

Doxylamine (Rec.INN registered by WHO)

Dosage Form

Sleepzone®

Film-coated tablets 15 mg: 10, 20 or 30 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets from light gray with a slight purple tint to gray with a purple tint, with a score on one side, oval, biconvex.

Excipients : lactose monohydrate, microcrystalline cellulose (type 102), croscarmellose sodium, magnesium stearate.

Film coating: film-forming mixture* (hypromellose, titanium dioxide (E171), macrogol 400, iron oxide black (E172), iron oxide red (E172)).
* The film-forming mixture is a ready-to-use dry mixture of hypromellose, titanium dioxide (E171), macrogol 400, iron oxide black (E172), iron oxide red (E172).

10 pcs. – blisters (1) – cardboard packs.
10 pcs. – blisters (2) – cardboard packs.
10 pcs. – blisters (3) – cardboard packs.

Clinical-Pharmacological Group

Hypnotic drug

Pharmacotherapeutic Group

Histamine H1-receptor antagonist

Pharmacological Action

Histamine H₁-receptor blocker from the ethanolamines group. It has a sedative, hypnotic effect. It reduces the time to fall asleep, increases the duration and quality of sleep, and does not change the phases of sleep. It has an antiallergic effect. It has m-anticholinergic activity.

The severity of the sedative effect is comparable to barbiturates. The duration of action is 6-8 hours.

Pharmacokinetics

After oral administration, C_max in blood plasma is reached on average after 2 hours. T_1/2 is about 10 hours.

Absorption is high, metabolized in the liver. It penetrates well through histohematic barriers (including the BBB). It is excreted 60% by the kidneys unchanged, partially through the gastrointestinal tract.

Indications

Transient sleep disorders.

ICD codes

Dosage Regimen

Administer orally as a single daily dose.

Take 15-30 minutes before bedtime.

Initiate therapy at a dose of 7.5 mg to 15 mg.

If clinically necessary and under medical supervision, increase the dose to a maximum of 30 mg.

Limit the total duration of treatment to 2 to 5 days.

For patients with hepatic impairment, use with caution and consider a dose reduction due to potential for increased plasma concentration and prolonged half-life.

For patients with renal impairment, use with caution and consider a dose reduction due to potential for increased plasma concentration and decreased clearance.

For geriatric patients (over 65 years), use with caution and initiate at the lower end of the dosage range due to increased risk of dizziness, sedation, and falls.

Do not exceed the recommended maximum daily dose.

Adverse Reactions

From the digestive system: constipation, dryness of the oral mucosa.

From the cardiovascular system: palpitations.

From the organ of vision: visual and accommodation disturbances, blurred vision.

From the urinary system: urinary retention.

From the nervous system: daytime sleepiness, confusion, hallucinations.

From laboratory parameters: increased level of creatine phosphokinase.

From the musculoskeletal system: rhabdomyolysis.

Contraindications

Hypersensitivity to doxylamine; angle-closure glaucoma or family history of angle-closure glaucoma; diseases of the urethra and prostate gland accompanied by impaired urine outflow; children under 15 years of age.

With caution: in patients with a history of apnea – due to the fact that Doxylamine may worsen the syndrome of nocturnal apnea (sudden cessation of breathing during sleep); in patients over 65 years of age – due to possible dizziness and slow reactions with the risk of falls (for example, during nighttime awakenings after taking sleeping pills), as well as due to the possible prolongation of T_1/2; in patients with renal and hepatic insufficiency (T_1/2 may be prolonged).

Use in Pregnancy and Lactation

Doxylamine can be used in pregnant women according to indications in recommended doses throughout the entire period of pregnancy. If doxylamine is prescribed in the later stages of pregnancy, the atropine-like and sedative properties of doxylamine should be taken into account when monitoring the condition of the newborn.

Contraindicated for use during breastfeeding due to the possibility of developing a sedative or stimulating effect in the newborn.

Use in Hepatic Impairment

Should be used with caution in patients with hepatic insufficiency.

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

Use in Renal Impairment

Should be used with caution in patients with renal insufficiency.

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

Pediatric Use

Contraindicated for use in children under 15 years of age.

Geriatric Use

Should be used with caution in patients over 65 years of age – due to possible dizziness and slow reactions with the risk of falling (for example, during nighttime awakenings after taking sleeping pills). In view of data on increased plasma concentration, decreased plasma clearance and prolongation of T_1/2, dose adjustment in this category of patients towards a decrease is recommended.

Special Precautions

Like all hypnotic or sedative drugs, Doxylamine may worsen the syndrome of nocturnal apnea, increasing the number and duration of apnea attacks.

Effect on the ability to drive vehicles and mechanisms

During the use of doxylamine, due to possible daytime sleepiness, driving vehicles, as well as other activities requiring quick psychomotor reactions, should be avoided.

Drug Interactions

When doxylamine is taken simultaneously with antidepressants (amitriptyline, doxepin, mianserin, mirtazapine, trimipramine), barbiturates, benzodiazepines, clonidine, morphine derivatives (analgesics, antitussives), neuroleptics, anxiolytics, H1-histamine receptor antagonists, centrally acting antihypertensive drugs, thalidomide, baclofen, pizotifen, the inhibitory effect on the central nervous system is enhanced.

When used simultaneously with atropine and atropine-like agents, imipramine, antiparkinsonian drugs with anticholinergic action, disopyramide, phenothiazine derivatives, the risk of developing anticholinergic side effects (dry mouth, constipation, urinary retention) increases.

When used simultaneously with ethanol, the sedative effect of doxylamine is enhanced; simultaneous use with alcoholic beverages and drugs containing ethanol should be avoided.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

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.