Doxylamine-SZ pills 15mg, 30pcs

Composition

1 tablet contains: Active ingredient: doxylamine succinate-15 mg; excipients: microcrystalline cellulose-15.0 mg, croscarmellose sodium-9.0 mg, lactose monohydrate (milk sugar) – 98.2 mg, magnesium stearate-1.4 mg, colloidal silicon dioxide (aerosil) – 1.4 mg; shell composition:  hypromellose-2.04 mg, polysorbate-80 (twin-80) – 0.85 mg, talc-0.68 mg, titanium dioxide E 171-0.43 mg

Pharmacological action

Antagonist of H1-histamine receptors.

ATX code:

R06AA09.

Pharmacological properties

Pharmacodynamics

Blocker of H1-histamine receptors from the group of ethanolamines. It has a hypnotic, sedative and M-holinoblokiruyushchy effect. Reduces the time of falling asleep, increases the duration and quality of sleep, but does not change the sleep phase. Duration of action-6-8 hours.

Pharmacokinetics

The maximum concentration in blood plasma (Cmax) is reached on average 2 hours after oral use. The half-life of doxylamine (T 1/2) is about 10 hours.

Absorption is high, it is metabolized in the liver. Penetrates well through histohematic barriers, including the blood-brain barrier. It is excreted by 60% of the kidneys in unchanged form, partially-through the gastrointestinal tract (GIT).

Pharmacokinetics of the drug in special groups of patients

In patients over 65 years of age, as well as in patients with hepatic and renal insufficiency, the elimination half-life may be prolonged. With repeated courses of treatment, a stable concentration of the drug and its metabolites in the blood plasma is achieved later and at a higher level.

Indications

Transient sleep disturbances.

Use during pregnancy and lactation

Based on adequate and well-controlled studies, doxylamine can be used in pregnant women throughout the entire period of pregnancy. In the case of prescribing this drug in late pregnancy, the atropine-like and sedative properties of doxylamine should be taken into account when monitoring the condition of the newborn. It is not known whether doxylamine passes into breast milk. Due to the possibility of developing a sedative and excitatory effect in the child, breast-feeding when using the drug should not be.

Contraindications

• hypersensitivity to doxylamine and other components of the drug, or to other antihistamines;
• angle-closure glaucoma or a family history of angle-closure glaucoma;
• diseases of the urethra and prostate accompanied by impaired urinary outflow;
• congenital galactosemia, glucose-galactose malabsorption, lactase deficiency;
• children and adolescents (up to 15 years).

With caution

In patients with a history of sleep apnea – doxylamine may worsen nocturnal apnea syndrome (sudden respiratory arrest during sleep).

Patients over 65 years of age – due to possible dizziness and delayed reactions with a risk of falling (for example, when waking up at night after taking sleeping pills), as well as due to a possible increase in the half-life.

Patients with renal and hepatic insufficiency (the elimination half-life may increase).

Side effects

From the gastrointestinal tract:  constipation, dry mouth. From the cardiovascular system:  palpitation sensation. From the side of the visual organ:  visual and accommodation disorders, blurred vision. From the side of the kidneys and urinary tract:  urinary retention. Nervous system disorders:  daytime drowsiness (in this case, the dose of the drug should be reduced), confusion, hallucinations. From the side of laboratory parameters:  increased creatine phosphokinase levels. From the musculoskeletal system:  rhabdomyolysis. If any of the adverse reactions listed in the instructions get worse or you notice any other adverse events that are not listed in the instructions, tell your doctor.

Interaction

When taking Doxylamine-SZ concomitantly with sedative antidepressants (amitriptyline, doxepin, mianserin, mirtazapine, trimipramine), barbiturates, benzodiazepines, clonidine, morphine derivatives (analgesics, antitussives), neuroleptics, anxiolytics, sedatives H1-antihistamines, central antihypertensive drugs, thalidomide, baclofen, pisotifen increases the depressing effect on the central nervous system (CNS). Concomitant use with m-anticholinergic agents (atropine, imipramine antidepressants, antiparkinsonian drugs, atropine antispasmodics, disopyramide, phenothiazine antipsychotics) increases the risk of side effects such as urinary retention, constipation, and dry mouth. Since alcohol increases the sedative effect of most H1-histamine receptor antagonists, including the drug Doxylamine-SZ, it is necessary to avoid its simultaneous use with alcoholic beverages and drugs containing alcohol.

How to take, course of use and dosage

Inside. 1/2-1 tablet a day, with a small amount of liquid,15-30 minutes before bedtime. If treatment is ineffective, the dose may be increased to two tablets on the doctor’s recommendation. The duration of treatment is from 2 to 5 days; if insomnia persists, you should consult a doctor. Use in special groups of patientspatients with renal and hepatic insufficiency: Due to data on an increase in the concentration in blood plasma and a decrease in the plasma clearance of doxylamine, a downward dose adjustment is recommended. Use in patients over 65 years of age: H1-histamine receptor blockers should be used with caution in this group of patients due to possible dizziness and delayed reactions with a risk of falling (for example, when waking up at night after taking sleeping pills). In view of the data on increasing plasma concentrations, decreasing plasma clearance, and increasing half-life, dose adjustment is recommended to decrease.

Overdose

Symptoms:  daytime sleepiness, agitation, pupil dilation (mydriasis), accommodation disorders, dry mouth, redness of the face and neck (hyperemia), fever (hyperthermia), sinus tachycardia, confusion, hallucinations, decreased mood, anxiety, impaired coordination of movements, trembling (tremor), involuntary movements (athetosis), convulsions (epileptic syndrome), coma. Involuntary movements are sometimes harbingers of seizures, which may indicate a severe degree of poisoning. Even in the absence of seizures, severe doxylamine poisoning can cause the development of rhabdomyolysis, which is often accompanied by acute renal failure. In such cases, standard therapy with constant monitoring of creatine phosphokinase levels is indicated. If you experience symptoms of poisoning, you should immediately consult a doctor. Treatment:  symptomatic (m-cholinomimetics, etc. ), as a first aid agent, activated carbon is indicated (in the amount of 50 g for adults and 1 g/kg of body weight for children).

Description

Tablets covered with a film-coated white color, round, biconvex with a risk. On a cross-section, the tablet core is white or almost white in color.

Special instructions

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 medication.

The drug Doxylamine-SZ has a sedative effect, suppresses cognitive abilities and slows down psychomotor reactions. The first generation of H1-antihistamines can have m-cholinoblocking, anti-alpha-adrenergic and anti-serotonin effects, which can cause dry mouth, constipation, urinary retention, accommodation and visual disturbances.

Like all sleeping pills or sedatives, doxylamine can worsen sleep apnea (sudden respiratory arrest during sleep) by increasing the number and duration of sleep apnea attacks.

One tablet of the drug contains 98.2 mg of lactose monohydrate, which should be taken into account in patients with rare congenital galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption.

Influence on the ability to drive motor vehicles and manage mechanisms

Due to possible daytime drowsiness, driving vehicles, working with mechanisms, and other activities that require increased concentration of attention and speed of psychomotor reactions should be avoided.

Storage conditions

In a place protected from light, at a temperature not exceeding 25 °C. Keep out of reach of children.

Shelf

life is 3 years. Do not use after the expiration date indicated on the package.

Active ingredient

Doxylamine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets