Carditab ic

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT CARDITAB IS

Composition:

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

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

Excipients: β-cyclodextrin, calcium hydrogen phosphate dihydrate, StarLac® (lactose monohydrate, corn starch), sodium croscarmellose, crospovidone, colloidal anhydrous silicon dioxide, magnesium stearate.

Pharmaceutical form. Tablets.

Main physico-chemical properties: tablets are white or almost white, flat cylindrical in shape with a bevelled edge; slight color variation is acceptable; the company trademark is imprinted on one side of the tablet, a score line is present on the other side.

Pharmacotherapeutic group.

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

Pharmacological Properties

Pharmacodynamics

A sedative, vasodilatory, and spasmolytic agent. Depending on the dose, phenobarbital exerts sedative, moderate spasmolytic, or hypnotic effects. It helps reduce excitability of the central nervous system, produces a calming effect, facilitates the onset of natural sleep, lowers arterial pressure, and relieves or prevents vascular spasms, especially in the heart. Ethyl ether of α-bromoisovaleric acid produces sedative and spasmolytic effects similar to those of valerian extract; at higher doses, it also produces a mild hypnotic effect. Peppermint oil exerts a reflex vasodilatory and spasmolytic effect. It relieves spasms of smooth musculature and produces calming, antiseptic, and mild cholagogue effects.

Pharmacokinetics

The effect of the drug develops within 15–45 minutes and lasts for 3–6 hours. 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, the metabolism of phenobarbital 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 due to 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 gravis, respiratory diseases with dyspnea and obstructive syndrome; depression and depressive disorders with suicidal tendencies; alcoholism, narcotic and drug dependence (including in medical history). Pregnancy and lactation period. Pediatric age.

Interaction with other medicinal products and other forms of interactions.

Phenobarbital induces liver enzymes and thus may accelerate the metabolism of certain drugs metabolized by these enzymes (including paracetamol, salicylates, indirect anticoagulants, cardiac glycosides (digoxitin), antimicrobial agents (chloramphenicol, doxycycline, metronidazole, rifampicin, sulfonamides), antiviral, antifungal (griseofulvin, itraconazole), antiepileptic (anticonvulsant), psychotropic (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 blood concentrations 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 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, there is a risk of gastric ulcer formation and bleeding. Concurrent use of phenobarbital with zidovudine enhances the toxicity of both medicinal products.

Special precautions for use.

During treatment with this medicinal product, activities requiring increased attention and rapid psychomotor reactions should be avoided.

Alcoholic beverages should be avoided during the use of this medicinal product.

Phenobarbital is contraindicated in depressive disorders associated with a patient's tendency towards suicidal behaviour.

Life-threatening skin reactions, including Stevens-Johnson syndrome or toxic epidermal necrolysis (Lyell’s syndrome), have been reported during phenobarbital treatment. Therefore, if characteristic symptoms occur (e.g. progressive skin rash, often with blisters, and mucous membrane involvement), the use of the medicinal product Carditab IS should be discontinued immediately, and any further use of medicinal products containing phenobarbital must be strictly avoided. The risk of developing Stevens-Johnson syndrome and Lyell’s syndrome is highest during the first weeks of treatment. Early diagnosis and immediate discontinuation of the medicinal product suspected of causing symptoms of Stevens-Johnson syndrome or toxic epidermal necrolysis are crucial for achieving optimal treatment outcomes.

Prolonged use of the medicinal product 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 bromism. Barbiturates are known to cause withdrawal syndrome.

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

The medicinal product should be used with caution in 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 sugar intolerances should consult their physician. This medicinal product should not be administered to patients with rare hereditary conditions such as galactose intolerance, lactase deficiency, or glucose-galactose malabsorption due to its lactose content.

Use during pregnancy or breastfeeding.

Pregnancy

Use of this 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 feeding difficulties. Use of phenobarbital during labour may cause respiratory depression in the newborn.

Breastfeeding

Use of this 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 the reaction rate when operating vehicles or machinery.

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

Dosage and Administration.

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

Adults are usually prescribed 1–2 tablets of the medicinal product 2–3 times daily before meals.

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

Children.

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

Overdose.

Overdose is possible with frequent or prolonged use of the medicinal product, related to the accumulation of its components. Long-term continuous use may lead to dependence and the development of withdrawal syndrome symptoms (psychomotor agitation, etc.).

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

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

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

Treatment: symptomatic therapy (primarily monitoring of vital functions: respiration, pulse, arterial pressure). Cases of acute poisoning with the medicinal product Carditab IS should be treated as poisoning with other sedatives and barbiturates, depending on the severity of poisoning 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 a short time has passed since ingestion of the drug (not more than 6 hours), gastric lavage should be performed, followed by administration of a sorbent (activated charcoal) and sodium sulfate. To accelerate elimination of barbiturates from the body, forced alkaline diuresis, as well as 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 diuretic agents.

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

Side effects

In individual cases, the following adverse reactions may occur:

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

Nervous system disorders: asthenia, weakness, ataxia, impaired coordination of movements, nystagmus, hallucinations, paradoxical excitation, decreased concentration, increased fatigue, slowed reaction time, headache, cognitive disorders, insomnia (mainly in elderly patients), drowsiness, dizziness, confusion, depression;

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

Hematopoietic system disorders: thrombocytopenia, agranulocytosis, anemia, megaloblastic anemia;

Cardiovascular disorders: arterial hypotension, bradycardia;

Respiratory system disorders: dyspnea;

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

Musculoskeletal system disorders: 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 tissue metabolism has not been established.

Other: elevated body temperature, enlarged lymph nodes, leukocytosis, lymphocytosis, leukopenia, collapse.

With prolonged use of phenobarbital, folic acid deficiency, impotence, drug dependence, and withdrawal syndrome may develop. The withdrawal syndrome usually occurs after abrupt discontinuation of the drug and is 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 or 2 blisters per carton.

6 tablets in a blister.

Availability: Over-the-counter.

Manufacturer:

"INTERSIM" Limited Liability Company.

Manufacturer's address and place of business activity:

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