Instructions Donormil film-coated tablets 15 mg tube No. 10
Composition
active ingredient: doxylamine succinate;
1 tablet contains doxylamine succinate 15 mg;
Excipients: lactose monohydrate; croscarmellose sodium; microcrystalline cellulose; magnesium stearate; hypromellose; macrogol 6000; dye dispersion, which includes hypromellose, titanium dioxide (E 171), propylene glycol, purified water.
Dosage form
Film-coated tablets.
Main physicochemical properties: rectangular white tablets with a double-sided score for division.
Pharmacotherapeutic group
Antihistamines for systemic use. ATX code R06A A09.
Hypnotics and sedatives. ATX code N05C M.
Pharmacological properties
Pharmacodynamics.
Doxylamine succinate is an ethanolamine class H1-histamine receptor blocker with sedative and atropine-like effects. It has been shown to reduce the time it takes to fall asleep and improve the duration and quality of sleep.
Pharmacokinetics.
The maximum plasma concentration (Cmax) is reached on average 2 hours (Tmax) after taking doxylamine succinate.
The mean plasma elimination half-life (T½) is on average 10 hours.
Doxylamine succinate is partially metabolized in the liver by demethylation and N-acetylation. The half-life may be significantly increased in the elderly or in patients with renal or hepatic insufficiency.
The various metabolites formed during the breakdown of the molecule are not quantitatively significant, since 60% of the administered dose is found in the urine in the form of unchanged doxylamine.
Indication
Intermittent insomnia in adults.
Contraindication
Hypersensitivity to doxylamine succinate or to any of the excipients or to other antihistamines.
Acute angle-closure glaucoma in the patient's history or in the family history.
Uretroprostatic disorders with risk of urinary retention.
Special safety precautions
Insomnia can have various causes that do not necessarily require medication, so it is recommended to consult a doctor before starting to use the drug.
Since the drug contains lactose, it is contraindicated in cases of congenital galactosemia, glucose-galactose malabsorption syndrome, and lactase deficiency.
Like all hypnotics or sedatives, doxylamine succinate may exacerbate sleep apnea syndrome (increased number and duration of breathing stops).
H1-antihistamines should be used with caution in elderly patients due to the risk of dizziness, which may increase the risk of falls (for example when people get up at night) with consequences that are often serious in this category of patients.
To prevent drowsiness during the day, it is necessary to remember that the duration of sleep after taking the drug should be at least 7 hours.
Interaction with other medicinal products and other types of interactions
Combinations to avoid.
Alcohol enhances the sedative effect of most H1-antihistamines. Alcoholic beverages and medications containing ethanol should be avoided.
Use with sodium oxybutyrate should be avoided due to increased central nervous system depression. Impaired reaction speed may lead to danger when driving or operating other mechanisms.
Combinations to consider.
With atropine and atropine-like drugs (imipramine antidepressants, most atropine-like H1-antihistamines, anticholinergic antiparkinsonian drugs, atropine antispasmodics, disopyramide, phenothiazine neuroleptics, and clozapine) due to the occurrence of such side effects as urinary retention, constipation, and dry mouth.
With other sedative drugs (morphine derivatives (painkillers, drugs used for cough treatment and substitution therapy), neuroleptics; barbiturates, benzodiazepines; anxiolytics other than benzodiazepines (meprobamate); other hypnotics, sedative antidepressants (amitriptyline, doxepin, mianserin, mirtazapine, trimipramine); sedative H1-antihistamines; centrally acting antihypertensives; others: baclofen, thalidomide) due to increased depression of the central nervous system. Impaired reaction speed may lead to danger when driving vehicles and working with other mechanisms.
With other hypnotics, due to central nervous system depression.
Application features
Insomnia can have various causes that do not necessarily require medication, so it is recommended to consult a doctor before starting to use the medication.
The drug contains lactose, therefore it is contraindicated in cases of congenital galactosemia, glucose-galactose malabsorption syndrome, and lactase deficiency.
The risk of abuse and drug dependence is low. However, cases of abuse resulting in drug dependence have been reported. It is necessary to carefully monitor for signs of abuse or drug dependence. The duration of treatment should not exceed 5 days. The drug is not recommended for use in patients with a history of substance use disorders.
Doxylamine succinate remains in the body for approximately 5 half-lives (see Pharmacokinetics).
The half-life may be significantly longer in the elderly or in those with renal or hepatic impairment. With repeated administration, the drug or its metabolites reach steady state much later and at higher levels. The efficacy and safety of the drug can only be assessed after steady state is reached.
Dose adjustment may be required (see section "Method of administration and dosage").
H1-antihistamines should be used with caution in elderly patients due to the risk of cognitive impairment, sedation, slow reactions and/or vertigo/dizziness, which may increase the risk of falls (for example, when people get up at night) with consequences that are often serious in this category of patients.
In elderly patients with renal or hepatic insufficiency, increased plasma concentrations of the drug and decreased plasma clearance are observed. It is recommended to reduce the dose of the drug.
To prevent drowsiness during the day, it is necessary to remember that the duration of sleep after taking the medicine should be at least 7 hours.
Use during pregnancy or breastfeeding
Based on the available data, doxylamine can be used during pregnancy after consultation with a doctor. If this drug is used at the end of pregnancy, the atropine-like and sedative properties of this molecule should be taken into account when monitoring the newborn.
It is not known whether doxylamine passes into breast milk, therefore it is not recommended to use the drug during breastfeeding.
Ability to influence reaction speed when driving vehicles or other mechanisms
It is necessary to pay attention to the risk of daytime drowsiness, especially in people who drive or operate machinery, which may develop when taking this medication. In cases of insufficient sleep duration, the risk of impaired reaction speed increases.
See section “Interaction with other medicinal products and other types of interactions”.
Method of administration and doses
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 can be increased to 30 mg per day (2 tablets per day).
Elderly patients and patients with renal or hepatic insufficiency are recommended to reduce the dose.
The duration of the treatment course is 2–5 days.
If insomnia persists for longer than 5 days, you should consult a doctor regarding the appropriateness of further use of the drug.
Children.
The medicine should not be used in children under 18 years of age.
Overdose
The first signs of acute poisoning are drowsiness and signs of anticholinergic effects: agitation, dilated pupils, paralysis of accommodation, dry mouth, flushing of the face and neck, hyperthermia, sinus tachycardia. Delirium, hallucinations and athetoid movements are more common in children; sometimes they are precursors of convulsions - rare complications of massive poisoning - or even coma. Even if convulsions do not occur, acute doxylamine poisoning sometimes causes rhabdomyolysis, which can be complicated by acute renal failure. This muscle disorder is common, requiring systematic screening by measuring creatine phosphokinase activity.
Treatment is symptomatic. Early initiation of treatment is recommended with activated charcoal (50 g for adults, 1 g/kg for children).
Side effects
Anticholinergic effects: constipation, urinary retention, dry mouth, visual disturbances (accommodation disorders, blurred vision, hallucinations, visual defect), palpitations, confusion.
Daytime drowsiness: if this effect develops, the dose should be reduced.
Cases of abuse and drug dependence have been reported.
In addition, H1-antihistamine drugs are known to cause sedation, cognitive impairment, and psychomotor impairment.
Expiration date
3 years.
Storage conditions
Store at a temperature not exceeding 25 °C out of the reach of children.
Packaging
10 or 30 tablets in a tube. 1 tube in a cardboard box.
Vacation category
No. 10 - without a prescription;
No. 30 - by prescription.
Producer
UPSA SAS, France.
Address
979, Avenue de Pyrenees, 47520 Le Passage, France.
304, Avenue Dr. Jean Bru, 47000 Agen, France.
