Adaptol®

INSTRUCTIONS for Medical Use of the Medicinal Product ADAPTOL® (ADAPTOL)

Composition:

Active substance: teglicoluril;

1 capsule contains teglicoluril 300 mg;

Excipients: methylcellulose, calcium stearate, titanium dioxide (E 171), gelatin.

Pharmaceutical form. Capsules.

Main physicochemical properties: hard gelatin capsules of white color containing powder of white or almost white color, may be in the form of a compressed column that disperses upon touching with a glass rod. Inhomogeneity in particle size is permitted.

Pharmacotherapeutic group.

Agents used in disorders of the nervous system.

Psychoanaleptics and other psychostimulants and nootropic drugs. Teglicoluril.

ATC code N06BX21.

Pharmacological properties.

Pharmacodynamics.

The active ingredient of the medicinal product Adapto® – tegaserod – belongs to the group of anxiolytic medicinal agents. Chemically, tegaserod is structurally similar to natural metabolites of the body: its molecule consists of two methylated fragments of urea incorporated into a bicyclic structure.

Adapto® has moderate tranquilizing (anxiolytic) activity, reducing or alleviating feelings of anxiety, apprehension, fear, inner 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; therefore, Adapto® can be used during working hours or while studying. The drug does not produce euphoria or a sense of elevated mood. For this reason, Adapto® is classified as a daytime tranquilizer. It does not exhibit hypnotic effects but enhances the action of hypnotic agents and improves sleep in cases of sleep disturbances.

In addition to its anxiolytic properties, Adapto® exerts nootropic effects and reduces undesirable adverse reactions caused by neuroleptics and benzodiazepine-class tranquilizers (emotional blunting, excessive sedation, muscle weakness).

The drug improves cognitive functions, enhances attention and mental performance, without stimulating symptoms of productive psychopathological disorders—such as delusions or pathological emotional activity.

Adapto® affects the activity of structures within the limbic-reticular complex, particularly the emotiogenic zones of the hypothalamus, and influences all four major neurotransmitter systems—GABAergic, cholinergic, serotonergic, and adrenergic—promoting their balance and integration, without exerting peripheral adrenolytic effects. The neurotransmitter profile of Adapto® includes a dopamine-positive component. The drug exhibits antagonistic activity against adrenergic and glutamatergic system excitation and enhances the function of inhibitory serotonergic and GABAergic mechanisms in the brain. The drug possesses normasthenic properties.

Adapto® has anti-alcohol effects. In patients with alcoholism, the plasma level of endogenous ethanol is reduced, which is one of the reasons for increased alcohol craving. Adapto® increases the level of endogenous ethanol more effectively than other tranquilizers, thereby reducing alcohol craving.

Adapto® alleviates nicotine withdrawal symptoms.

Pharmacokinetics.

Following oral administration, bioavailability ranges from 77% to 80%; up to 40% of the drug binds to erythrocytes; the remaining 60% remains unbound to blood proteins and circulates freely in plasma, allowing the drug to distribute easily throughout the body and freely cross membranes.

The volume of distribution is 0.9 L/kg. Maximum plasma concentration is reached within 30 minutes; a high concentration level persists for 3–4 hours, then gradually declines. The drug is completely eliminated from the body—55–70% via urine, the remainder via feces in unchanged form—within 24 hours. It does not accumulate in the body and does not undergo biochemical transformation.

Clinical characteristics.

Indications.

Adaptol® is intended for use in adults.

Neuroses and neurosis-like conditions (anxiety, emotional lability, apprehension, and fear).

Cardialgia of various origins (not associated with ischemic heart disease).

To improve tolerance of neuroleptics and tranquilizers.

As part of combination therapy for nicotine dependence, as an agent reducing the craving for smoking.

Contraindications.

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

Interaction with other medicinal products and other forms of interaction.

Adaptol® can be combined with neuroleptics, tranquilizers (benzodiazepines), hypnotics, antidepressants, and psychostimulants.

Special precautions for use.

Habituation, dependence, and withdrawal syndrome have not been observed with the use of Adaptole®.

Use with caution in patients with impaired liver or kidney function and in patients with arterial hypotension.

There have been isolated reports of acute hypersensitivity reactions.

Use during pregnancy or breastfeeding.

Adaptole® readily penetrates into all body tissues and fluids.

There are insufficient data on the safety of using the drug during pregnancy and breastfeeding; therefore, the drug is not recommended for use in pregnant women or women who are breastfeeding.

Ability to influence reaction rate when driving vehicles or operating machinery.

Caution should be exercised when driving vehicles or operating machinery, since the use of the drug may cause a decrease in blood pressure and weakness.

Method of Administration and Dosage.

Adaptol® should be administered orally, independently of food intake.

For adults: 300–600 mg 2–3 times daily. If necessary, the dose may be increased. Maximum single dose – 3 g; maximum daily dose – 10 g.

Duration of treatment course: from several days up to 2–3 months.

For treatment of nicotine dependence, the medicinal product should be used at a dose of 600–1000 mg daily for 5–6 weeks (to achieve this dosage, appropriate dosage forms containing the corresponding amount of active substance must be used).

Dose adjustment is not required for elderly patients or patients with hepatic insufficiency.

Dose correction in patients with renal insufficiency has not been studied. The medicinal product should be prescribed with caution to such patients.

Children.

The drug is not intended for use in children.

Overdose.

Adaptol® has low toxicity. In cases of significant overdose, side effects may be intensified (including allergic reactions, dyspeptic disorders, weakness, temporary reduction in arterial blood pressure and body temperature).

Treatment: gastric lavage should be performed, together with standard detoxification procedures and symptomatic therapy.

No specific antidote is known.

Adverse Reactions.

Adaptol®, like other medicinal products, may cause adverse reactions, although they do not occur in all patients.

Frequency of adverse reactions according to the MedDRA classification (Medical Dictionary for Regulatory Activities):

very common (≥1/10); common (≥ 1/100 to <1/10); uncommon (≥ 1/1000 to <1/100); rare (≥ 1/10 000 to <1/1000); very rare (<1/10 000); frequency not known (cannot be estimated from available data).

Central and peripheral nervous system disorders: rare – dizziness.

Cardiac disorders: rare – decreased arterial blood pressure.

Gastrointestinal disorders: rare – dyspeptic disorders (including nausea, vomiting, diarrhoea).

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 rashes, pruritus, urticaria, angioneurotic oedema) may occur after taking high doses. If an allergic reaction occurs, discontinue the use of the product.

General disorders: rare – decreased body temperature, weakness. If arterial blood pressure and/or body temperature decreases (body temperature may decrease by 1–1.5 °C), there is no need to discontinue the medication. Blood pressure and body temperature return to normal after completion of the treatment course.

Reporting of adverse reactions following marketing authorization of the medicinal product is of great importance. It enables ongoing monitoring of the benefit-risk balance of the product. Healthcare professionals, as well as patients or their legal representatives, are encouraged to 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.

3 years.

Storage conditions.

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

Keep out of reach and sight of children.

Packaging.

10 capsules per blister. 2 blisters per cardboard pack.

Prescription status.

Prescription only.

Manufacturer.

JSC «Olfa» / Olpha AS.

Manufacturer's address and place of business.

Rupnicu iela 5, Olaine, Olaines novads, LV-2114, Latvia.