Instructions for Valdicardin oral drops, bottle 20 ml
Composition
active ingredients: phenobarbital, ethyl ester of ɑ-bromoisovaleric acid;
1 ml of solution (24 drops) contains phenobarbital – 18.4 mg, ethyl ester of ɑ-bromoisovaleric acid – 18.4 mg;
Excipients: peppermint oil; hop oil; sodium citrate; citric acid, monohydrate; ethanol 96%; purified water.
Dosage form
Oral drops.
Main physicochemical properties: colorless liquid with a specific aromatic odor and bitter taste. Opalescence is allowed.
Pharmacotherapeutic group
Hypnotics and sedatives. Barbiturates in combination with drugs of other groups. ATX code N05C B02.
Pharmacological properties
Pharmacodynamics.
Valdicardin is a combined drug containing phenobarbital and ethyl bromizovalerianate (ethyl ester of α-bromoisovaleric acid). Depending on the dose, both of these substances have a sedative, hypnotic effect, and in high doses have a narcotic effect. Like other derivatives of barbituric acid, phenobarbital inhibits the inhibitory system of the reticular formation. Ethyl bromizovalerianate exhibits both antispasmodic and sedative properties. At the concentration contained in Valdicardin, ethyl bromizovalerianate acts as a synergist of phenobarbital (rapid onset of effectiveness).
Pharmacokinetics.
Phenobarbital is absorbed rapidly (directly in the stomach). Approximately 35% of it binds to plasma proteins, the part that is not bound to proteins is filtered by the kidneys. Reabsorption occurs at a low pH. Reverse diffusion does not occur due to the alkalinity of the urine. Approximately 30% of phenobarbital is excreted unchanged in the urine, and only a small part of it is oxidized in the liver. With prolonged use, there is an accumulation of the active substance in the blood plasma, as well as induction of liver enzymes. As a result of this induction, the oxidation process of phenobarbital and other drugs is accelerated.
Bromine in ethyl bromisovalerianate is excreted very slowly from the body. If the drug is used for a long time, its accumulation in the CNS occurs, leading to chronic bromine intoxication.
Indication
- Functional disorders of the cardiovascular system;
- neuroses, which are accompanied by increased irritability and a sense of fear;
- psychosomatically caused anxiety;
- states of excitement with pronounced vegetative manifestations;
- sleep disturbance.
Contraindication
Hypersensitivity to the components of the drug, bromine. Acute hepatic porphyria, severe liver and kidney dysfunction, diabetes mellitus, depression, myasthenia gravis.
Medicines containing phenobarbital are contraindicated in alcoholism, drug and drug addiction (including a history); in respiratory diseases with shortness of breath, obstructive syndrome, severe arterial hypotension, in acute myocardial infarction; in depressive disorders with a tendency of the patient to suicidal behavior.
Pregnancy and breastfeeding. Childhood.
Interaction with other medicinal products and other types of interactions
When using the drug with other drugs that depress the central nervous system, a mutual enhancement of the effect (sedative-hypnotic effect) is possible, which may be accompanied by respiratory depression. Phenobarbital enhances the effect of analgesics, anesthetics, anesthetics, neuroleptics, tranquilizers. Alcohol enhances the effect of the drug and may increase its toxicity.
The effect of the drug is enhanced when used with valproic acid preparations.
Phenobarbital, which is part of Valdicardin, can induce liver enzymes and, accordingly, can accelerate the metabolism of some drugs that are metabolized by liver enzymes (including paracetamol, salicylates, indirect anticoagulants, cardiac glycosides (digitoxin), antimicrobials (chloramphenicol, doxycycline, metronidazole, rifampicin), antivirals, antifungals (griseofulvin, itraconazole), antiepileptics (anticonvulsants), psychotropics (tricyclic antidepressants, clonazepam), hormonal (estrogens, progestogens, corticosteroids, thyroid hormones), immunosuppressives (glucocorticosteroids, cyclosporine, cytostatics), antiarrhythmics, antihypertensives (β-blockers, calcium channel blockers), oral hypoglycemic drugs, etc.), due to which the effectiveness of these drugs will be reduced. Phenobarbital may accelerate the metabolism of oral contraceptives, leading to a loss of their effect.
MAO inhibitors prolong the effect of phenobarbital. Rifampicin may reduce the effect of phenobarbital.
When used with gold preparations, the risk of kidney damage increases.
With prolonged simultaneous use with nonsteroidal anti-inflammatory drugs, there is a risk of stomach ulcers and bleeding.
Concomitant use of drugs containing phenobarbital with zidovudine increases the toxicity of both drugs.
The drug increases the toxicity of methotrexate.
Application features
Life-threatening skin reactions such as Stevens-Johnson syndrome and toxic epidermal necrolysis have been reported with phenobarbital. Therefore, if their characteristic symptoms appear (e.g. progressive skin rash, often with blisters, and mucosal lesions), Valdicardin should be discontinued and no further use of phenobarbital-containing medicinal products should be considered. The risk of developing Stevens-Johnson syndrome and Lyell's syndrome is greatest in the first weeks of treatment. Early diagnosis and immediate discontinuation of the drug that may have caused the symptoms of Stevens-Johnson syndrome or toxic epidermal necrolysis allows for the best results in treatment.
If the pain in the heart area does not go away after taking the drug, you should consult a doctor to rule out acute coronary syndrome. It is prescribed with caution in hyperkinesias, hyperthyroidism, adrenal hypofunction, uncompensated heart failure, severe arterial hypotension and constant pain, acute drug intoxication.
Long-term use of Valdicardin is not recommended due to the risk of bromine accumulation in the body and the development of bromine poisoning.
Continuous long-term use of the drug may cause addiction, drug dependence, withdrawal syndrome, and sudden cessation of use - withdrawal syndrome. Long-term use of the drug is sometimes accompanied by increased psychodynamic activity instead of the expected sedation.
Valdicardin contains 55% by volume of ethanol (alcohol).
The minimum dose of the drug (18 drops) contains 325.57 mg of ethanol, which is equivalent to 8.25 ml of beer or 3.44 ml of wine per dose. Harmful for patients suffering from alcoholism. It should be used with caution in patients with liver disease and epilepsy.
This medicinal product contains less than 1 mmol (23 mg) sodium/dose, i.e. essentially 'sodium-free'.
Use during pregnancy or breastfeeding
Do not use during pregnancy or breastfeeding.
Ability to influence reaction speed when driving vehicles or other mechanisms
Valdicardin weakens the reaction rate. Patients taking the drug should refrain from potentially hazardous activities that require increased attention and speed of mental and motor reactions.
Method of administration and doses
Prescribed for adults.
It is administered orally during meals, diluting a single dose with a small amount of liquid.
The usual dosage is 18-24 drops 3 times a day; if the patient has insomnia, the dose can be increased to 36 drops.
The duration of use of the drug is determined by the doctor.
Children.
There is no experience with the use of the drug in the treatment of children, therefore the drug should not be used in pediatric practice.
Overdose
Symptoms.
Acute (mild to moderate) barbiturate poisoning:
dizziness, fatigue, even a deep sleep from which the patient cannot be awakened.
Hypersensitivity reactions may occur: angioedema, urticaria, itching, rash.
Acute severe poisoning:
deep coma accompanied by tissue hypoxia, shallow breathing, first rapid, then slow breathing, rapid heartbeat, cardiac arrhythmia, low blood pressure, bradycardia, vascular collapse, weakening or loss of reflexes, nystagmus, headache, nausea, weakness, cardiac dysfunction, decreased body temperature, slowed pulse, decreased diuresis.
If poisoning is left untreated, death is possible as a result of vascular insufficiency, respiratory paralysis, or pulmonary edema.
Prolonged use of bromine-containing drugs can lead to bromine poisoning, which is characterized by the following symptoms: a state of confusion, ataxia, apathy, depressed mood, conjunctivitis, colds, acne, or purpura.
Treatment.
Cases of acute poisoning with Valdicardin should be treated in the same way as poisoning with other hypnotics and barbiturates, depending on the severity of the symptoms of poisoning. The patient should be transferred to the intensive care unit. Breathing and circulation require stability and normalization. Respiratory failure is overcome by artificial respiration, shock is stopped by infusion of plasma and plasma substitutes. If a lot of time has passed since the intake, it is necessary to wash the stomach (10 g of activated charcoal powder and sodium sulfate are administered into the stomach). In order to quickly remove the barbiturate from the body, forced diuresis with alkalis, as well as hemodialysis and/or hemoperfusion, can be performed.
Treatment of bromine poisoning: the elimination of bromine ions from the body can be accelerated by administering a significant amount of table salt solution with the simultaneous administration of saluretics.
If hypersensitivity reactions occur, prescribe desensitizing medications.
Adverse reactions
The frequency of adverse reactions is given according to the following classification: very common (≥1/10), common (≥1/100, <1/10), uncommon (≥1/1000, <1/100), rare (≥1/10000, <1/1000), very rare (˂1/10000), frequency unknown (cannot be estimated from the available data).
| Organ systems | Frequency | Adverse reactions |
| On the part of the immune system | Hypersensitivity reactions, including angioedema, allergic reactions (including skin rash, itching, urticaria, facial swelling). |
| From the nervous system | Frequency unknown | Asthenia, weakness, impaired coordination of movements, nystagmus, ataxia, hallucinations, paradoxical excitement, insomnia (in elderly patients), decreased concentration, fatigue, slowed reactions, headache, cognitive impairment. In some cases, drowsiness and mild dizziness, confusion may occur. |
| Cardiovascular system | Frequency unknown | Decreased blood pressure, bradycardia. |
| From the side of the hematopoietic organs | Frequency unknown | Agranulocytosis, megaloblastic anemia, thrombocytopenia, anemia. |
| Gastrointestinal tract | Frequency unknown | Nausea, vomiting, constipation, heaviness in the epigastric region, with prolonged use - impaired liver function |
| Skin and mucous membranes | Frequency unknown | Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome). |
| Respiratory system | Frequency unknown | Difficulty breathing. |
| Musculoskeletal system | Frequency unknown | With prolonged use of drugs containing phenobarbital, there is a risk of impaired osteogenesis and the development of rickets. There have been reports of reduced bone mineral density, osteopenia, osteoporosis, and fractures in patients receiving long-term therapy with phenobarbital. The mechanism by which phenobarbital affects bone metabolism has not been identified. |
Prolonged use of bromine-containing drugs can lead to bromine poisoning, which is characterized by the following symptoms: central nervous system depression, depressed mood, confusion, ataxia, apathy, conjunctivitis, rhinitis, lacrimation, acne, or purpura.
Expiration date
3 years.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 °C.
Keep out of reach of children.
Packaging
20 ml or 50 ml in a bottle; 1 bottle in a pack.
Vacation category
Over-the-counter – 20 ml, prescription – 50 ml.
Producer
LLC "State Enterprise "Pharmaceutical Factory".
Location of the manufacturer and address of its place of business.
Ukraine, 12430, Zhytomyr region, Zhytomyr district, Stanyshivka village, Koroleva st., bldg. 4.
