Doxylamine-SZ, 15 mg 30 pcs.

H1-histamine receptor antagonist.

ATX code:

R06AA09.

Pharmacological properties

Pharmacodynamics

A H1-histamine receptor blocker from the group of ethanolamines. It has soporific, sedative and M-cholinoblocking effects. It shortens the time to fall asleep, increases the duration and quality of sleep, and does not change the phase of sleep. The duration of action is 6-8 hours.

Pharmacokinetics

The maximum plasma concentration (Cmax) is reached on average 2 hours after oral administration. The half-life of doxylamine (T1/2) is about 10 hours.

The absorption is high, metabolized in the liver. It penetrates well through histohematic barriers, including the blood-brain barrier.
It is excreted 60% by the kidneys unchanged, partially through the gastrointestinal tract (GIT).

Pharmacokinetics of the drug in special groups of patients

In patients older than 65 years old and in patients with hepatic and renal insufficiency half-life can be prolonged. When repeated courses of treatment, stable plasma concentrations of the drug and its metabolites are reached later and at higher levels.

Indications

Transient sleep disturbances.

Pharmacological effect

Antagonist of H1-histamine receptors.

ATX Code:

R06AA09.

Pharmacological properties

Pharmacodynamics

H1-histamine receptor blocker from the ethanolamine group. It 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 – 6-8 hours.

Pharmacokinetics

The maximum concentration in blood plasma (Cmax) is achieved on average 2 hours after oral administration. The half-life of doxylamine (T1/2) is about 10 hours.

Absorption is high, metabolized in the liver. Penetrates well through histohematic barriers, including the blood-brain barrier.
60% is excreted unchanged by the kidneys, 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 with hepatic and renal insufficiency, the half-life may be prolonged. When 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.

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 drug.

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-anticholinergic, anti-alpha-adrenergic and antiserotonin effects, which can cause dry mouth, constipation, urinary retention, disturbances of accommodation and vision.

Like all sleeping pills or sedatives, doxylamine may worsen sleep apnea (sudden stoppage of breathing during sleep), increasing the number and duration of 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.

Impact on the ability to drive vehicles and operate machinery

Due to possible drowsiness during the daytime, you should avoid driving vehicles, operating machinery and other activities that require increased concentration and speed of psychomotor reactions.

Active ingredient

Doxylamine

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 (Tween-80) – 0.85 mg, talc – 0.68 mg, titanium dioxide E 171 – 0.43 mg.

Pregnancy

Based on adequate and well-controlled studies, doxylamine can be used in pregnant women throughout pregnancy.

If this drug is prescribed 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 stimulating effect in a child, breastfeeding should not be done while using the drug.

Contraindications

hypersensitivity to doxylamine and other components of the drug, or to other antihistamines;
angle-closure glaucoma or family history of angle-closure glaucoma;
diseases of the urethra and prostate gland, accompanied by impaired urine outflow;
congenital galactosemia, glucose-galactose malabsorption, lactase deficiency;
childhood and adolescence (up to 15 years).
With caution

Patients with a history of apnea – due to the fact that doxylamine can aggravate sleep apnea syndrome (sudden cessation of breathing during sleep).

Patients over 65 years of age – due to possible dizziness and delayed reactions with the risk of falls (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 (half-life may increase).

Side Effects

From the gastrointestinal tract: constipation, dry mouth.

From the cardiovascular system: palpitations.

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

From the kidneys and urinary tract: urinary retention.

From the nervous system: drowsiness during the day (in this case, the dose of the drug should be reduced), confusion, hallucinations.

From laboratory parameters: increased level of creatine phosphokinase.

From the musculoskeletal system: rhabdomyolysis.

If any of the adverse reactions indicated in the instructions worsen or you notice any other adverse effects not listed in the instructions, notify your doctor.

Interaction

When taking the drug Doxylamine-SZ simultaneously with sedative antidepressants (amitriptyline, doxepin, mianserin, mirtazapine, trimipramine), barbiturates, benzodiazepines, clonidine, morphine derivatives (analgesics, antitussives), neuroleptics, anxiolytics, sedative H1-antihistamines, central antihypertensive drugs, thalidomide, baclofen, pizotifen, enhance the inhibitory effect on the central nervous system (CNS).

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

Since alcohol enhances the sedative effect of most H1-histamine receptor antagonists, incl. and the drug Doxylamine-SZ, it is necessary to avoid its simultaneous use with alcoholic beverages and medications containing alcohol.

Overdose

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

Involuntary movements are sometimes a precursor to seizures, which may indicate severe poisoning. Even in the absence of seizures, severe doxylamine poisoning can cause rhabdomyolysis, which is often accompanied by acute renal failure. In such cases, standard therapy with constant monitoring of creatine phosphokinase levels is indicated.

If symptoms of poisoning appear, consult a doctor immediately.

Treatment: symptomatic (m-cholinomimetics, etc.), activated carbon is indicated as a first aid remedy (50 g for adults and 1 g/kg body weight for children).

Storage conditions

In a place protected from light, at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life

3 years.

Do not use after the expiration date stated on the package.

Manufacturer

North Star NAO, Russia