Valocordin-Doxylamine
Valocordin-Doxylamine: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Valocordin-Doxylamine
ATX code: R06AA09
Active ingredient: doxylamine (Doxylaminum)
Producer: KREWEL MEUSELBACH, GmbH (Germany)
Description and photo update: 2018-22-10
Prices in pharmacies: from 171 rubles.
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Valocordin-Doxylamine is a drug with hypnotic, sedative and antihistamine effects.
Release form and composition
Dosage form of the Valocordin-Doxylamine preparation - drops for oral administration: transparent, colorless, with a mint smell (in dark glass dropper bottles of 20 or 50 ml, in a cardboard box 1 dropper bottle).
Composition of 1 ml drops (22 drops):
- active substance: doxylamine succinate - 25 mg;
- auxiliary components: mint oil - 1.4 mg; ethanol 96% - 450 mg; purified water - 449.7 mg.
Pharmacological properties
Pharmacodynamics
Valocordin-Doxylamine belongs to the group of H1-histamine receptor blockers from the group of ethanolamines. It has a sedative, hypnotic, m-anticholinergic and antihistamine effect.
Due to the use of the drug, the time of falling asleep is reduced, the quality and duration of sleep increases, while the sleep phases do not change.
The action of the drug Valocordin-Doxylamine develops within 30 minutes after oral administration, its duration is 3-6 hours.
Pharmacokinetics
Doxylamine is almost completely and rapidly absorbed. The maximum concentration in blood serum is found 2–2.4 hours after taking a single dose (25 mg of doxylamine succinate) and is 99 ng / ml.
Metabolism occurs primarily in the liver. Major metabolites: N-desmethyl doxylamine; N, N-didesmethyl doxylamine and their N-acetyl conjugates. It penetrates well through the histohematological barriers, including the blood-brain barrier.
The half-life ranges from 10.1-12 hours. Approximately 60% of the dose is excreted unchanged in the urine, partially through the intestines.
Indications for use
Valocordin-Doxylamine is prescribed for the symptomatic treatment of recurrent sleep disorders (nighttime awakenings and difficulty falling asleep).
Long-term use of the drug for chronic sleep disorders without medical advice is not recommended.
Contraindications
Absolute:
- hyperplasia of the prostate gland, proceeding with disorders of the outflow of urine;
- acute asthmatic attack;
- bronchial asthma or other respiratory diseases, which are characterized by increased sensitivity of the respiratory tract (which is associated with the mint oil that is part of the drug);
- angle-closure glaucoma;
- pheochromocytoma;
- congenital long QT interval syndrome;
- epilepsy;
- poisoning with alcohol, tranquilizers, neuroleptics, antidepressants, lithium preparations, drugs with hypnotics, narcotic and analgesic effects in acute course;
- combined use with monoamine oxidase inhibitors;
- age up to 18 years;
- period of breastfeeding;
- individual intolerance to the components of the drug, as well as other antihistamines.
Relative (diseases / conditions in the presence of which the administration of Valocordin-Doxylamine requires caution):
- gastroesophageal reflux;
- hepatic and heart failure;
- alcoholism;
- a history of indications of bronchospasm;
- arterial hypertension;
- local damage to the cerebral cortex and a history of seizures (therapy requires special care, since Valocordin-Doxylamine, even in small doses, can cause severe seizures of epilepsy; EEG is recommended; anticonvulsant therapy should not be interrupted);
- chronic shortness of breath;
- achalasia of the cardia;
- pyloric stenosis;
- age over 65;
- pregnancy.
Instructions for the use of Valocordin-Doxylamine: method and dosage
Valocordin-Doxylamine is taken 30-60 minutes before the desired sleep onset, inside with 100-150 ml of liquid (water).
In the absence of other doctor's prescriptions, a single dose is 22 drops (1 ml). In cases of insufficient effectiveness, the dose can be doubled (maximum).
To avoid disturbances in psychomotor reactions after awakening, it is necessary to ensure a sufficient duration of sleep.
In case of acute sleep disturbances, it is recommended, if possible, to limit ourselves to a single use of the drug Valocordin-Doxylamine. To check the need to continue therapy with regular sleep disturbances, you should switch to a gradual dose reduction no later than 14 days after the start of the daily intake.
The duration of use, as a rule, is 2-5 days, the maximum duration of the course is 14 days.
Patients with a probable increased susceptibility to the action of the drug (old age, renal or hepatic insufficiency) are recommended to take Valocordin-Doxylamine in reduced doses.
Side effects
Possible adverse reactions (> 10% - very often;> 1% and 0.1% and 0.01% and <0.1% - rarely; <0.01% - very rarely; with an unknown frequency - if it is impossible to assess the reported incidence of disorders):
- psyche: decreased concentration of attention and speed of psychomotor reactions, depression, paradoxical reactions (in the form of anxiety, agitation, anxiety, insomnia, nightmares, confusion, hallucinations, tremors); with abrupt withdrawal after prolonged daily use - rebound insomnia;
- lymphatic system / blood: in exceptional cases - leukopenia, thrombocytopenia, hemolytic anemia; very rarely - aplastic anemia and agranulocytosis;
- endocrine system: with pheochromocytoma - an increase in the release of catecholamines;
- cardiovascular system: arrhythmia, tachycardia, decompensated heart failure, increased or decreased blood pressure; possibly - changes in the ECG;
- nervous system: drowsiness, dizziness, headache; rarely - convulsions;
- organ of vision / hearing: disturbances of accommodation, increased intraocular pressure, tinnitus;
- digestive system: autonomous adverse reactions, including constipation and dry mouth, possible nausea, diarrhea, vomiting, epigastric pain, increased or decreased appetite; very rarely - paralytic intestinal obstruction (is life-threatening);
- respiratory organs: bronchial obstruction, thickening of bronchial secretions, bronchospasm (can cause impaired lung function);
- musculoskeletal system: muscle weakness;
- biliary tract and liver: impaired hepatic function (cholestatic jaundice);
- subcutaneous tissue, skin: photosensitivity, allergic skin reactions, impaired thermoregulation;
- kidneys, urinary tract: impaired urination;
- others: fatigue, nasal congestion, lethargy, recurrence of insomnia (a gradual dose reduction is recommended); anterograde amnesia (especially within the first hour after taking it; the likelihood of its occurrence is dose-dependent, the risk is reduced due to continuous prolonged sleep), physical / mental dependence (the likelihood increases with the duration of treatment / dose, as well as against the background of drug and alcohol dependence, including indications in history).
The frequency and severity of adverse reactions can be reduced by careful individual selection of the daily dose. Elderly patients are more likely to experience adverse reactions and, as a result, the risk of falls is higher.
With regular use, the effectiveness of Valocordin-Doxylamine may decrease (addiction).
Overdose
The main symptoms: hallucinations, convulsive syndrome, dilated pupils, daytime sleepiness, paresis of accommodation, dry mouth, fever, disturbance of consciousness, reddening of the skin of the neck or face, impaired coordination of movements, sinus tachycardia, decreased mood, increased anxiety, involuntary movements, tremor, coma.
In some cases, involuntary movements are harbingers of seizures, which may indicate a severe degree of poisoning. Even in the absence of seizures, poisoning with Valocordin-Doxylamine can lead to rhabdomyolysis, which often occurs with severe renal failure (standard therapy is shown with constant monitoring of creatine phosphokinase activity).
There is information about the development of acute pancreatitis and acute renal failure after taking 500 mg of doxylamine in the treatment of persistent insomnia.
In case of an overdose, symptomatic (including m-cholinomimetics and drugs with an anticonvulsant effect) and supportive therapy (including artificial ventilation) are performed. As a means of first aid, activated carbon is prescribed (for adults - 50 g, for children - 1 g / kg). In cases of taking a large amount of the drug, gastric lavage or induction of vomiting is performed. The use of analeptics is contraindicated as it can lead to the development of convulsive syndrome. With arterial hypotension, due to the possibility of a paradoxical increase in the severity of hypotension, alpha and beta adrenostimulants, including epinephrine (adrenaline), are not prescribed (the use of norepinephrine is advisable).
Drugs with beta-adrenostimulating action should be avoided, since their use can lead to increased vasodilation. In case of severe poisoning (loss of consciousness, cardiac arrhythmias) or the appearance of an anticholinergic syndrome (while ensuring ECG monitoring), an antidote can be prescribed - physostigmine salicylate. With repeated epileptic seizures, drugs with an anticonvulsant effect are indicated. Due to the increased likelihood of respiratory depression, their appointment is possible only in cases where it is possible to carry out artificial ventilation.
The effectiveness of forced diuresis in the case of doxylamine overdose has not been established; hemodialysis, peritoneal dialysis and hemofiltration have not been studied, however, due to the large volume of distribution of the active substance, these methods are unlikely to be effective.
special instructions
The composition of the drug Valocordin-Doxylamine contains ethanol, which can be dangerous in the presence of liver diseases, alcoholism, epilepsy, as well as for pregnant women.
During therapy, regular monitoring of heart function is required, since there are reports of ECG changes, in particular, changes in the repolarization phase (in particular, elderly patients and patients with heart failure should take this into account).
Valocordin-Doxylamine can aggravate the course of sleep apnea syndrome (in the form of an increase in the number and duration of attacks of sudden respiratory arrest during sleep).
Influence on the ability to drive vehicles and complex mechanisms
When driving motor vehicles, it is necessary to take into account the likelihood of a negative effect of Valocordin-Doxylamine on the ability to actively participate in road traffic, especially in cases of combined use with alcohol. In this regard, it is recommended to avoid driving a car (at least during the first phase of therapy). In each case, the decision must be made by the doctor.
Application during pregnancy and lactation
- pregnancy - taking the drug is possible after assessing the benefit / risk ratio;
- lactation period - therapy is contraindicated, since the active ingredient penetrates into breast milk.
Pediatric use
According to the instructions, Valocordin-Doxylamine is not prescribed for children under 18 years of age.
With impaired renal function
It is necessary to carry out therapy with renal failure with caution (dose adjustment may be required).
For violations of liver function
It is necessary to carry out therapy with hepatic insufficiency with caution (dose adjustment may be required).
Use in the elderly
Patients over 65 years of age should be prescribed Valocordin-Doxylamine with caution, which is associated with an increased risk of dizziness, the danger of loss of balance and the likelihood of falling during nighttime awakenings (dose adjustment may be required).
Drug interactions
Possible interactions:
- baclofen, thalidomide, pizotifen, antidepressants, codeine-containing analgesics, antipsychotics, narcotic analgesics, barbiturates, benzodiazepines, anxiolytics, antitussives and sedatives, other blockers of H1-histamine receptors, central antihypertensive drugs (antihypertensive drugs), antihypertensive drugs on the central nervous system;
- ethanol, ethanol-containing drugs: enhancing the sedative effect of Valocordin-Doxylamine (the combination is recommended to be avoided);
- antiarrhythmics, protease inhibitors, antipsychotics, beta-blockers, immunosuppressants, antiepileptic drugs and other drugs metabolized with the participation of CYP2, CYP3A and CYP2A enzymes: a significant increase in their activity, the possibility of developing an interaction cannot be ruled out;
- monoamine oxidase inhibitors: the development of arterial hypotension, depression of respiratory function and the central nervous system;
- drugs with m-anticholinergic activity (tricyclic antidepressants, atropine and antispasmodics containing atropine, monoamine oxidase inhibitors, antiparkinsonian drugs, phenothiazine antipsychotics, disopyramide): an unpredictable increase and lengthening of the anticholinergic effect of Valocordin-Doxylamine, the likelihood of the appearance of disorders such as Valocordin-Doxylamine increases urine, dry mouth, paralytic intestinal obstruction, increased intraocular pressure;
- photosensitizing drugs: additive photosensitizing effect;
- salicylates, aminoglycosides, diuretics and other ototoxic drugs: masking the initial signs of damage to the inner ear (dizziness, ringing in the ears, confusion);
- epinephrine (to eliminate arterial hypotension): a paradoxical increase in the severity of hypotension; in shock conditions, the use of norepinephrine is indicated.
During the period of therapy, the results of skin tests may be false negative.
Analogs
Donormil, Reslip are analogues of Valocordin-Doxylamine.
Terms and conditions of storage
Store at temperatures up to 25 ° C. Keep out of the reach of children.
The shelf life is 5 years.
After opening the package, the drug can be used for 6 months.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Valocordin-Doxylamine
According to reviews, Valocordin-Doxylamine is an affordable and effective drug that normalizes sleep. It is recommended to pre-consult with a doctor and strictly adhere to the indicated dosage during therapy. The development of side effects (lethargy, drowsiness) are rarely reported.
Price for Valocordin-Doxylamine in pharmacies
The approximate price for Valocordin-Doxylamine (20 or 50 ml per package) is 180-250 or 230-240 rubles.
Valocordin-Doxylamine: prices in online pharmacies
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Drug name Price Pharmacy |
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Valocordin-Doxylamine 25 mg / ml drops for oral administration 20 ml 1 pc. 171 r Buy |
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Valocordin-Doxylamine drops for internal approx. 25mg / ml 20ml 222 r Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
