Mebicar ic

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT MEBICAR IS

Composition:

Active substance: teglicoluril;

One tablet contains teglicoluril 500 mg (0.5 g);

Excipients: methylcellulose, calcium stearate.

Pharmaceutical form. Tablets.

Main physical and chemical properties: white-colored tablets, flat cylindrical shape, bevelled edges; the company trademark is imprinted on one surface of the tablet, a break line on the other surface.

Pharmacotherapeutic group.

Psychostimulants, drugs used in attention deficit hyperactivity disorder (ADHD), and nootropic agents. Other psychostimulant and nootropic agents. Teglicoluril.

ATC code N06B X21.

Pharmacological Properties

Pharmacodynamics

The active ingredient of the medicinal product, temazepan, is chemically similar to natural metabolites of the body: the temazepan molecule consists of two methylated fragments of urea incorporated into a bicyclic structure.

Mebicar IS affects the activity of limbic-reticular complex structures, particularly the emotiogenic zones of the hypothalamus, and also influences all four main neurotransmitter systems—GABAergic, cholinergic, serotonergic, and adrenergic—promoting their balance and integration, but does not exert peripheral adrenonegative effects. Mebicar IS exhibits antagonistic activity against excitation of adrenergic and glutamatergic systems and enhances inhibitory serotonergic and GABAergic mechanisms in the brain. The drug's neurotransmitter profile includes a dopamine-positive component.

The medicinal product possesses normasthenic properties.

Mebicar IS has moderate tranquilizing (anxiolytic) activity, alleviating or reducing feelings of uneasiness, anxiety, fear, emotional tension, and irritability. The anxiolytic effect of the drug is not accompanied by myorelaxation or impaired motor coordination. The drug does not reduce mental or physical performance, thus it can be used during working hours or while studying. For this reason, Mebicar IS is classified as a daytime tranquilizer. The drug does not exhibit hypnotic effects but enhances the action of hypnotics and improves sleep in cases of sleep disturbances.

In addition to its anxiolytic action, the drug exerts nootropic effects. Mebicar IS improves cognitive functions, enhances attention and mental performance, without stimulating symptoms of productive psychopathological disorders such as delusions or pathological emotional activity.

The drug reduces the severity of adverse effects (emotional blunting, hypersedation, muscle weakness) caused by neuroleptics and benzodiazepine tranquilizers.

The drug has anti-alcohol properties. In patients with alcoholism, one of the reasons for increased alcohol craving is a reduced level of endogenous ethyl alcohol in blood plasma. Mebicar IS, by increasing the level of endogenous ethyl alcohol (to a greater extent than other tranquilizers), reduces alcohol craving.

Mebicar IS alleviates nicotine withdrawal.

The drug does not induce elevated mood or feelings of euphoria.

Pharmacokinetics

Following oral administration, bioavailability is 77–80%; up to 40% of temazepan binds to erythrocytes; the remaining 60% is not bound to blood proteins and remains free in blood plasma, allowing temazepan to distribute freely throughout the body and readily cross membranes. The volume of distribution is 0.9 L/kg. Maximum temazepan concentration in blood serum is reached within 30 minutes, with high levels maintained for 3–4 hours, after which concentrations gradually decline. Temazepan is completely eliminated from the body: 55–70% of the administered dose is excreted in urine, the remainder in feces, unchanged, within 24 hours. Temazepan does not accumulate in the body and is not subject to biochemical transformation.

Clinical characteristics.

Indications.

The medicinal product is intended for use in adults.

Neuroses and neurosis-like conditions accompanied by feelings of anxiety and fear, emotional lability, and restlessness.

Cardialgias of various origins (not related to ischemic heart disease).

For improving tolerance of neuroleptics and tranquilizers.

To be used as part of combination therapy for nicotine dependence as an agent reducing smoking craving.

Contraindications.

Hypersensitivity to temgicoluril or to any of the excipients of the medicinal product.

Interaction with other medicinal products and other forms of interaction.

Mebicar IS can be combined with neuroleptics, tranquilizers (benzodiazepines), hypnotics, antidepressants, and psychostimulants.

Special precautions for use.

Dependence, development of addiction, and withdrawal syndrome associated with the use of temgikoluril have not been established.

The drug should be used with caution in patients with arterial hypotension and impaired liver or kidney function.

There have been isolated reports of acute hypersensitivity reactions.

Use during pregnancy or breastfeeding.

Temgikoluril penetrates well into all tissues and body fluids.

There is insufficient data on the safety of temgikoluril use during pregnancy and breastfeeding; therefore, the drug is not recommended for administration to pregnant or breastfeeding women.

Ability to influence reaction rate while driving or operating machinery.

Caution should be exercised when driving or operating machinery, since the use of temgikoluril may cause decreased arterial pressure and weakness.

Dosage and Administration.

The medicinal product should be taken orally, independently of food intake. Dosage depends on individual patient characteristics and the therapeutic objective of the treatment.

The usual adult dose is 500 mg 2–3 times daily. The dose may be increased if necessary. The maximum single dose is 3 g; the maximum daily dose is 10 g. The duration of treatment ranges from several days to 2–3 months.

As part of complex therapy for nicotine dependence, the medicinal product should be administered at a dose of 500–1000 mg daily for 5–6 weeks.

Dosage adjustment is not required for elderly patients or patients with hepatic impairment.

Dosage adjustment in patients with renal impairment has not been studied. The medicinal product should be administered with caution in such patients.

If one or several doses have been missed, continue treatment according to the previously prescribed regimen.

Children.

The medicinal product is not intended for use in children.

Overdose.

The medicinal product has low toxicity. In cases of significant overdose, adverse effects may be intensified (including allergic reactions, dyspeptic disorders, weakness, transient reduction in blood pressure and body temperature).

Treatment: gastric lavage should be performed, along with administration of standard detoxification methods and symptomatic therapy.

No specific antidote is known.

Side effects

Mebykar IS, like other medicinal products, may cause side effects, although they do not occur in all patients.

Side effects associated with the use of the medicinal product are classified by system organ classes and frequency. Frequency is defined as follows: very common (≥ 1/10), common (≥ 1/100 to < 1/10), uncommon (≥ 1/1,000 to < 1/100), rare (≥ 1/10,000 to < 1/1,000), very rare (< 1/10,000), frequency not known (cannot be estimated from the available data).

Nervous system disorders: rare – dizziness.

Cardiovascular system disorders: rare – decreased blood pressure.

Gastrointestinal disorders: rare – dyspeptic disorders (including nausea, vomiting, diarrhea). In such cases, the dose of the medicinal product should be reduced.

Respiratory system disorders: rare – bronchospasm.

Skin and subcutaneous tissue disorders: rare – allergic reactions (including skin rash, pruritus, urticaria, angioneurotic edema). If an allergic reaction occurs, administration of the medicinal product should be discontinued.

General disorders: rare – decreased body temperature, weakness. If blood pressure and/or body temperature decreases (body temperature may decrease by 1–1.5 °C), administration of the medicinal product need not be discontinued. Blood pressure and body temperature will normalize after completion of the treatment course.

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after medicinal product authorization is important. It allows ongoing monitoring of the benefit-risk balance of the medicinal product. Healthcare and pharmacy professionals, as well as patients or their legal representatives, should report all suspected adverse reactions and lack of efficacy via the Automated Pharmacovigilance Information System at the following link: https://aisf.dec.gov.ua.

Shelf life. 4 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.

Prescription category. Prescription only.

Manufacturer.

Limited liability company "INTERKHIM".

Manufacturer's address and location of its business activity.

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