CARDITAB IC

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT CARDITAB IS

Composition:

Active substances: phenobarbital, ethyl ether of α-bromoisovaleric acid, peppermint oil;

One tablet contains: phenobarbital 7.5 mg, ethyl ether of α-bromoisovaleric acid 8.2 mg, peppermint oil 0.58 mg;

Excipients: β-cyclodextrin, calcium hydrogen phosphate dihydrate, StarLac® (lactose monohydrate, corn starch), mannitol (E 421), potassium acesulfame, citric acid monohydrate, sodium citrate, sodium croscarmellose, crospovidone, colloidal anhydrous silicon dioxide, magnesium stearate.

Pharmaceutical form. Sublingual tablets.

Main physicochemical properties: white or almost white tablets, flat cylindrical shape with beveled edges; slight color variation is permissible; the trade mark of the manufacturer is imprinted on one side of the tablet, a line is marked on the other side.

Pharmacotherapeutic group.

Hypnotics and sedatives. Combined barbiturate preparations. ATC code N05CB02.

Pharmacological properties.

Pharmacodynamics.

A sedative, vasodilatory, spasmolytic agent. Reduces excitability of the central nervous system, exerts a calming effect, facilitates the onset of natural sleep, lowers arterial pressure, relieves and prevents vascular spasms, especially in the heart. Depending on the dose, phenobarbital produces sedative, moderate spasmolytic, or hypnotic effects by suppressing activating influences of the reticular formation centers in the midbrain and medulla oblongata on the cerebral cortex, thereby reducing excitatory impulses to the cerebral cortex and subcortical structures. Ethyl ether of α-bromoisovaleric acid exerts sedative and spasmolytic effects similar to those of valerian extract, caused by stimulation primarily of receptors in the oral cavity and nasopharynx, reduction of reflex excitability in central parts of the nervous system, enhancement of inhibitory processes in neurons of the cerebral cortex and subcortical structures, as well as reduction in activity of central vasomotor centers and direct local spasmolytic action on smooth vascular musculature. At high doses, it also produces a mild hypnotic effect. Peppermint oil exerts a reflex vasodilatory and spasmolytic effect due to stimulation of cold receptors in the oral cavity and reflex dilation predominantly of heart and brain vessels. It relieves spasms of smooth muscle, exerts calming, antiseptic, and mild cholagogue effects.

Pharmacokinetics.

When administered sublingually, absorption begins in the sublingual area, and effects appear within 5–10 minutes. Bioavailability of active substances is high (approximately 60–80%). In patients previously treated with barbituric acid derivatives, the duration of action is shortened due to accelerated hepatic metabolism of phenobarbital, as barbiturates induce liver enzymes. In elderly patients and in patients with liver cirrhosis, phenobarbital metabolism is reduced, resulting in prolonged elimination half-life, which necessitates dose reduction and longer intervals between drug administrations.

Clinical characteristics.

Indications.

Neuroses with increased irritability.

Insomnia.

As part of combination therapy for hypertension and vegetative-vascular dystonia.

Cardialgia, tachycardia.

Intestinal spasms caused by neurovegetative disorders (as a spasmolytic agent).

Contraindications.

Hypersensitivity to the active substances or to any other component of the medicinal product, or to bromine; severe impairment of liver and/or kidney function, acute hepatic porphyria, severe heart failure, acute myocardial infarction, marked arterial hypotension, diabetes mellitus, myasthenia, respiratory diseases with dyspnea and obstructive syndrome; depression and depressive disorders with suicidal tendencies; alcoholism, drug and medication dependence (including in medical history). Pregnancy and breastfeeding period. Childhood.

Interaction with other medicinal products and other forms of interaction.

Phenobarbital induces liver enzymes and thus may accelerate the metabolism of certain medicinal products metabolized by these enzymes (including paracetamol, salicylates, indirect anticoagulants, cardiac glycosides (digoxin), antimicrobials (chloramphenicol, doxycycline, metronidazole, rifampicin, sulfonamides), antivirals, antifungals (griseofulvin, itraconazole), antiepileptics (anticonvulsants), psychotropic agents (tricyclic antidepressants), hormonal agents (estrogens, progestogens, corticosteroids, thyroid hormones), immunosuppressants (glucocorticoids, cyclosporine, cytostatics), antiarrhythmics, antihypertensives (β-blockers, calcium channel blockers), oral hypoglycemic agents, etc.). Phenobarbital enhances the effect of analgesics, anesthetics, neuroleptics, and tranquilizers. Phenobarbital may accelerate the metabolism of oral contraceptives, leading to loss of their efficacy. When used concomitantly with other medicinal products that depress the central nervous system, mutual enhancement of effects (sedative and hypnotic effects) is possible, which may be accompanied by respiratory depression. Alcohol enhances the effect of the medicinal product and may increase its toxicity. Possible influence on the blood concentration of phenytoin, as well as carbamazepine and clonazepam. The medicinal product increases the toxicity of methotrexate. Medicinal products with acidic properties (ascorbic acid, ammonium chloride) and preparations containing valproic acid enhance the effect of barbiturates. Patients receiving concomitant treatment with valproate and phenobarbital should be monitored for signs of hyperammonemia. In half of the reported cases, hyperammonemia was asymptomatic and did not necessarily lead to encephalopathy. Monoamine oxidase inhibitors (MAOIs) prolong the effect of phenobarbital. Rifampicin may reduce the effect of phenobarbital. When used together with gold preparations, the risk of kidney damage increases. With prolonged concomitant use of nonsteroidal anti-inflammatory drugs (NSAIDs), there is a risk of gastric ulceration and bleeding. Concomitant use of phenobarbital with zidovudine enhances the toxicity of both medicinal products.

Special precautions for use.

During treatment with the drug, activities requiring increased attention and rapid psychomotor and physical reactions should be avoided.

Alcoholic beverages should be avoided during administration of the medicinal product.

Phenobarbital is contraindicated in depressive disorders associated with a tendency towards suicidal behavior.

Cases of life-threatening skin reactions, including Stevens–Johnson syndrome or toxic epidermal necrolysis (Lyell’s syndrome), have been reported during treatment with phenobarbital. Therefore, if characteristic symptoms occur (e.g., progressive skin rash, often with blisters, and mucosal involvement), treatment with the medicinal product Carditab IS should be discontinued immediately, and medicinal products containing phenobarbital must not be used again under any circumstances. The risk of developing Stevens–Johnson syndrome or Lyell’s syndrome is highest during the first weeks of treatment. Early diagnosis and immediate discontinuation of the suspected causative drug are crucial for achieving optimal treatment outcomes.

Prolonged use of the drug should be avoided due to the potential for phenobarbital accumulation and development of drug dependence, as well as the risk of bromide accumulation in the body and possible bromide poisoning. Barbiturates are known to cause withdrawal syndrome.

If chest pain does not subside after taking the drug, medical advice should be sought to rule out acute coronary syndrome.

The medicinal product should be used with caution in patients with decompensated heart failure (see section "Contraindications"), bronchial asthma (see section "Contraindications"), arterial hypotension (see section "Contraindications"), hyperkinesia, hyperthyroidism, adrenal insufficiency, acute and persistent pain, and acute intoxication with medicinal products.

Before taking the medicinal product Carditab IS, patients with known intolerance to certain sugars should consult their physician. Patients with rare hereditary forms of galactose intolerance, lactase deficiency, or glucose-galactose malabsorption should not take this medicinal product due to its lactose content.

Use during pregnancy or breastfeeding.

Pregnancy

Use of the medicinal product during pregnancy is contraindicated.

Barbiturates increase the risk of fetal abnormalities. Administration of phenobarbital during the third trimester of pregnancy may lead to physical dependence, resulting in withdrawal syndrome in the newborn, manifested by seizures, irritability, and impaired sucking reflex. Use of phenobarbital during labor may cause respiratory depression in the newborn.

Breastfeeding

Use of the medicinal product during breastfeeding is contraindicated.

Phenobarbital passes into breast milk in significant amounts and may suppress the central nervous system of the infant.

Ability to influence reaction speed when operating vehicles or machinery.

The medicinal product may cause impaired motor coordination, reduced psychomotor reaction speed, drowsiness, and dizziness. Therefore, during treatment, patients should avoid operating vehicles or working with hazardous machinery.

Administration and Dosage.

Dosage and duration of treatment depend on the course of the disease and are determined individually by a physician.

For adults, the drug is usually administered sublingually (under the tongue) at a dose of 1–2 tablets 2–3 times daily before meals.

In cases of tachycardia and coronary vessel spasms (cardialgia), the single dose may be increased to 3 tablets.

Children.

There is no experience with the use of this medicinal product for the treatment of children (under 18 years of age); therefore, the drug is contraindicated in patients of this age group.

Overdose.

Overdose may occur with frequent or prolonged use of the drug due to accumulation of its components. Long-term continuous use may lead to dependence and symptoms of withdrawal syndrome (psychomotor agitation, etc.).

Symptoms of mild or moderate acute barbiturate poisoning: dizziness, increased fatigue, even deep sleep from which the patient cannot be awakened. Hypersensitivity reactions may also occur: angioedema, itching, rash (including urticaria).

Symptoms of severe acute barbiturate poisoning: central nervous system depression progressing to deep coma, accompanied by tissue hypoxia; shallow breathing, initially rapid and later slowed, respiratory depression up to respiratory arrest; cardiovascular depression, including arrhythmias, decreased arterial pressure, up to collapse-like state; lowered body temperature, reduced diuresis, tachycardia or bradycardia, diminished or absent reflexes, nystagmus, headache, nausea, weakness.

If poisoning is not treated, death may occur due to circulatory failure, respiratory paralysis, or pulmonary edema.

Treatment: symptomatic therapy (primarily monitoring of vital functions: respiration, pulse, blood pressure). Cases of acute poisoning with the medicinal product Carditab IS should be managed as poisoning with other hypnotics and barbiturates, depending on the severity of symptoms. Patients may require intensive therapy. It is necessary to stabilize and normalize respiration and circulation. Respiratory failure is managed by artificial ventilation; shock is treated by infusion of plasma and plasma substitutes. If little time has passed since drug intake (not more than 6 hours), gastric lavage should be performed, followed by administration of an adsorbent (activated charcoal) and sodium sulfate. To accelerate elimination of barbiturates from the body, forced alkaline diuresis, hemodialysis, and/or hemoperfusion may be performed.

Prolonged use of medicinal products containing bromine may lead to bromine poisoning.

Symptoms of bromine poisoning: central nervous system depression, depression, confusion, ataxia, apathy, conjunctivitis, rhinitis, lacrimation, acne, purpura.

Treatment: elimination of bromide ions from the body can be accelerated by administration of a large amount of sodium chloride solution along with saluretic agents.

In case of hypersensitivity reactions, desensitizing medicinal agents should be administered.

Side effects.

In individual cases, the following adverse reactions may occur:

Immune system side effects: hypersensitivity reactions, including angioneurotic edema, skin rash (including urticaria), pruritus;

Nervous system side effects: asthenia, weakness, ataxia, impaired motor coordination, nystagmus, hallucinations, paradoxical excitation, decreased concentration, increased fatigue, slowed reaction time, headache, cognitive disturbances, insomnia (mainly in elderly patients), somnolence, dizziness, confusion, depression;

Gastrointestinal side effects: nausea, vomiting, constipation, epigastric heaviness; with prolonged use – liver function disturbances;

Hematological side effects: thrombocytopenia, agranulocytosis, anemia, megaloblastic anemia;

Cardiovascular side effects: arterial hypotension, bradycardia;

Respiratory side effects: dyspnea;

Skin and subcutaneous tissue side effects: increased skin photosensitivity (photosensitization), polymorphic exudative erythema, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome), exfoliative dermatitis;

Musculoskeletal side effects: with prolonged use of products containing phenobarbital, there is a risk of impaired osteogenesis. Cases of decreased bone mineral density, osteopenia, osteoporosis, and fractures have been reported in patients receiving long-term phenobarbital therapy. The mechanism of phenobarbital's effect on bone metabolism has not been established.

Other side effects: increased body temperature, enlarged lymph nodes, leukocytosis, lymphocytosis, leukopenia, collapse.

With prolonged use of phenobarbital, folate deficiency, impotence, drug dependence, and withdrawal syndrome may develop. Withdrawal syndrome usually occurs after abrupt discontinuation of the drug and is typically accompanied by nightmares and nervousness.

Shelf life. 3 years.

Storage conditions.

Store in the original packaging at a temperature not exceeding 25 °C.

Keep out of reach of children.

Packaging.

10 tablets in a blister; 1 blister per carton.

6 tablets in a blister.

Availability. Over-the-counter.

Manufacturer.

Limited liability company "INTERKHIM".

Manufacturer's address.

40-A, 21st km of Starokyivska Road, Odessa, 65025, Ukraine.