Instructions for Bioson film-coated tablets, blister pack No. 30
Composition
active ingredients: passionflower herb (Passiflorae herba), doxylamine (doxilamine);
1 tablet contains 300 mg of dry passionflower extract (Passiflorae herba), 3.75 mg of doxylamine hydrogen succinate; excipients: glycine, microcrystalline cellulose, copovidone, crospovidone, pregelatinized starch, colloidal anhydrous silicon dioxide, magnesium stearate, coating for applying the shell Opadry II Blue (polyvinyl alcohol, titanium dioxide (E 171), polyethylene glycol, talc, indigo carmine (E 132), diamond blue (E 133), black iron oxide (E 172)).
Dosage form
Film-coated tablets.
Main physicochemical properties: film-coated tablets from light blue to blue, with a biconvex surface, round in shape, with a specific odor.
Pharmacotherapeutic group
Sleeping pills and sedatives. ATX code N05C M50.
Antihistamines for systemic use. ATX code R06A A09.
Pharmacological properties
Pharmacodynamics
The components of passionflower extract inhibit the conduction of nerve impulses in the spinal cord and brain, reduce the excitability of the central nervous system, which causes a pronounced sedative, mild anti-anxiety and hypnotic effects without symptoms of depression upon awakening. Calming effect in the climacteric and pre-climax periods. It is used for vegetative symptoms on the background of diseases of the nervous and cardiovascular systems (in hypertension, in the recovery period after cerebral vascular crises, neurocirculatory dystonia, in asthenic conditions after infections and other serious diseases). Passionflower eliminates such vegetative symptoms as palpitations, increased sweating.
Doxylamine hydrogen succinate is an ethanolamine class H1-histamine receptor blocker with sedative, hypnotic, and antiallergic effects. It has been shown to reduce the time it takes to fall asleep and improve the duration and quality of sleep.
Pharmacokinetics
Absorption
The maximum plasma concentration (Cmax) is reached on average 2 hours (Tmax) after taking doxylamine succinate.
Biotransformation and excretion
The average plasma half-life (T½) is 10 hours.
Doxylamine succinate is partially metabolized in the liver by demethylation and N-acetylation. The elimination half-life may be significantly increased in the elderly and 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 as unchanged doxylamine.
Indication
Periodic and transient insomnia.
Contraindication
Hypersensitivity to the components of the drug;
pregnancy and breastfeeding;
acute angle-closure glaucoma in the patient's history or in the family history;
urethroprostatic disorders with the risk of urinary retention.
Interaction with other medicinal products and other types of interactions
When used simultaneously with drugs that depress the central nervous system, such as barbiturates and tranquilizers, the sedative and hypnotic effect of the drug is enhanced.
Concomitant use with benzodiazepines is not recommended. Concomitant use with disulfiram should be avoided.
Combinations that are not recommended
Alcohol (as a beverage or as an excipient)
Alcohol enhances the sedative effect of most H1-antihistamines. Reduced alertness may make driving and using machinery dangerous. Alcoholic beverages and medications containing ethanol should be avoided.
Sodium oxybutyrate causes central nervous system (CNS) depression. Reduced alertness may make driving and using machinery dangerous.
Combinations to consider
Anticholinesterase agents
There is a risk of reduced efficacy of anticholinesterase drugs due to antagonistic effects on M-cholinergic receptors.
Other atropine-like drugs (imipramine antidepressants, most H1-antihistamine drugs with atropine-like action, anticholinergic antiparkinsonian drugs, atropine antispasmodics, disopyramide, phenothiazine neuroleptics and clozapine) are associated with an additional risk of atropine-like side effects due to blockade of M-cholinergic receptors.
Other antidepressants that affect the CNS
Morphine derivatives (painkillers; drugs used for cough treatment and substitution therapy), neuroleptics; barbiturates; benzodiazepines; anxiolytics other than benzodiazepines (e.g. meprobamate); hypnotic, sedative antidepressants (amitriptyline, doxepin, mianserin, mirtazapine, trimipramine); sedative H1-antihistamines; centrally acting antihypertensives; baclofen, thalidomide increase the depression of the central nervous system. Reduced alertness can make driving and using mechanisms dangerous.
Morphine-like substances/opioids carry a significant risk of colonic akinesia with severe constipation.
Application features
Special 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 medication.
Use with caution in patients with severe organic diseases of the digestive tract.
Like all sleeping pills or sedatives, doxylamine hydrogen succinate may exacerbate sleep apnea syndrome (increased number and duration of breathing stops).
The risk of abuse and dependence is low, but cases of abuse and dependence have been reported. Close monitoring for signs of abuse or dependence is necessary. Use in patients with substance use disorders is not recommended.
Accumulation risk
Doxylamine succinate remains in the body for approximately 5 half-lives (see Pharmacokinetics).
In elderly patients or in people with impaired renal or hepatic function, the half-life may be significantly prolonged. With repeated administration, the drug or its metabolites reach steady state much later and at a much higher level. Only after reaching steady state can the efficacy and safety of the drug be assessed.
A dose adjustment may be necessary.
Elderly patients
H1-antihistamines should be used with caution in elderly patients, as cognitive impairment, lethargy, delayed reactions and/or dizziness may occur, which increases the risk of falls (for example, when people get up at night) with consequences that are often serious in this category of patients.
Special safety precautions
Elderly patients, patients with impaired renal or hepatic function
Elderly patients should start treatment with the minimum dose.
Increased plasma concentrations and decreased plasma clearance have been observed. A dose reduction is recommended.
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
Do not use during pregnancy and breastfeeding.
Ability to influence reaction speed when driving vehicles or other mechanisms
It is necessary to remember about the risk of daytime drowsiness, which may develop when taking this drug, especially in people who drive vehicles or work with other mechanisms. They should be advised not to use sedatives, sodium oxybutyrate, alcoholic beverages or drugs containing alcohol as concomitant therapy, or when using such combinations to take into account the sedative effect of antihistamines. With insufficient sleep duration, the risk of decreased concentration increases.
During treatment with the drug, you should refrain from driving and working with potentially dangerous mechanisms.
Method of administration and doses
For internal use.
The recommended dose is 1 tablet, if necessary the dose can be increased to 2 tablets. Take the medicine 30 minutes before bedtime.
A dose reduction is recommended for elderly patients and patients with renal or hepatic insufficiency.
The duration of treatment is up to 10 days. If the symptoms persist, you should consult a doctor.
If insomnia persists for longer than 5 days, you should consult a doctor regarding the appropriateness of further use of the drug.
Children
The efficacy and safety of the drug for children under 15 years of age have not been established, therefore its use in this category of patients is not recommended.
Overdose
Symptoms
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 seizures - rare complications of severe poisoning or even coma. Even if seizures 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 the activity of creatine phosphokinase.
Treatment
Treatment is symptomatic. Early initiation of treatment is recommended with activated charcoal (50 g for adults, 1 g/kg for children).
Side effects
The drug is usually well tolerated.
In some cases, adverse reactions may occur and the following disorders may be observed.
On the part of the digestive tract: dry mouth, nausea, vomiting, abdominal pain, constipation.
Cardiovascular system: bradycardia, tachycardia, tachycardia, ventricular tachycardia.
On the part of the immune system: itching, skin rashes, vasculitis, allergic reactions are possible.
On the part of the organs of vision: visual impairment (visual acuity impairment, accommodation impairment, blurred vision).
On the part of the urinary system: urinary retention.
Rhabdomyolysis, increased levels of creatine phosphokinase (CPK) in the blood.
Adverse reactions such as constipation, urinary retention, dry mouth, visual disturbances (impaired accommodation, blurred vision, impaired visual acuity), rapid heartbeat, confusion, hallucinations are manifestations of the anticholinergic effects of the drug.
Lethargy, cognitive impairment, and psychomotor impairment are due to the effects of doxylamine (a first-generation H1-antihistamine drug) on the central nervous system.
In case of daytime drowsiness, the dose of the drug should be reduced.
Cases of abuse and dependence have been reported.
Expiration date
2 years. Do not use the drug after the expiration date indicated on the package.
Storage conditions
Store out of the reach of children, in the original packaging at a temperature not exceeding 25 °C.
Packaging
10 tablets in a blister; 1, 2, 3 and 10 blisters in a cardboard pack.
Vacation category
Without a prescription.
Producer
"Pharma Start" LLC.
Location of the manufacturer and address of its place of business.
Ukraine, 03124, Kyiv, Vaclav Havel Boulevard, 8.
In case of adverse reactions or questions regarding the safety and effectiveness of the medicinal product, please contact the Pharmacovigilance Department of ASINO UKRAINE LLC at the address: Vaclav Havel Boulevard, 8, Kyiv, 03124, tel/fax: +38 044 281 2333.
