Adaptol

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT ADAPTOL® (ADAPTOL)

Composition:

Active substance: teglicanol;

1 tablet contains 500 mg of teglicanol;

Excipients: methylcellulose, calcium stearate.

Pharmaceutical form. Tablets.

Main physicochemical properties: round, flat-cylindrical tablets of white or almost white color, with a bevel and a score line on one side of the tablet.

Pharmacotherapeutic group.

Agents used in disorders of the nervous system.

Psychoanaleptics and other psychostimulants and nootropic drugs. Teglicanol.

ATC code N06BX21.

Pharmacological Properties

Pharmacodynamics

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

Adaptole® has moderate tranquilizing (anxiolytic) activity, alleviating or reducing feelings of uneasiness, anxiety, fear, inner emotional tension, and irritability. The anxiolytic effect of the drug is not accompanied by myorelaxation or impaired motor coordination. The medicinal product does not reduce mental or physical activity; therefore, Adaptole® can be used during working hours or while studying. The drug does not induce euphoria or a sense of elevated mood. For this reason, Adaptole® is classified as a daytime tranquilizer. It does not exhibit sedative effects but enhances the action of sedatives and improves sleep in cases of sleep disturbances.

In addition to its anxiolytic properties, Adaptole® exerts a nootropic effect and reduces adverse side effects caused by neuroleptics and benzodiazepine-type tranquilizers (emotional depression, excessive calming effect, muscle weakness).

The drug improves cognitive functions, enhances attention and mental performance, without stimulating symptomatology of productive psychopathological disorders – delusions, pathological emotional activity.

Adaptole® 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, but does not exert peripheral adrenonegative effects. The neurotransmitter profile of Adaptole® 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 medicinal product possesses normasthenic properties.

Adaptole® has anti-alcohol effects. In patients with alcoholism, plasma levels of endogenous ethanol are reduced, which is one of the causes of increased alcohol craving. Adaptole® increases endogenous ethanol levels more than other tranquilizers, thereby reducing alcohol craving.

Adaptole® alleviates nicotine withdrawal symptoms.

Pharmacokinetics

After oral administration, bioavailability is 77–80%; up to 40% of the drug binds to erythrocytes; the remaining 60% remains unbound to blood proteins and circulates freely in blood 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 and remains high for 3–4 hours, then gradually declines. The drug is completely eliminated from the body (55–70% excreted in urine), the remainder is excreted unchanged in feces within 24 hours. It does not accumulate in the body and is not subject to 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 complex therapy for nicotine dependence, as an agent reducing smoking craving.

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®.

Adaptole® should be used 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® penetrates well into all tissues and body fluids.

There are insufficient data on the safety of using the medicinal product during pregnancy and breastfeeding; therefore, the administration of the drug is not recommended to pregnant women and women who are breastfeeding.

Ability to influence reaction rate when driving or operating machinery.

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

Method of Administration and Dosage

Administer Adapitol® orally, regardless of food intake. The usual adult dose is 500 mg 2–3 times daily.

The maximum single dose is 3 g; the maximum daily dose is 10 g.

The duration of treatment course ranges from several days up to 2–3 months.

For the treatment of nicotine dependence, the medicinal product should be administered 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).

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

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

Children

There is no experience with use in children.

Overdose

Adapitol® has low toxicity. In cases of significant overdose, adverse 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, along with general supportive decontamination measures and symptomatic therapy.

There is no known specific antidote.

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 (≥1/1,000 to <1/100); rare (≥1/10,000 to <1/1,000); very rare (<1/10,000); frequency not known (cannot be estimated from 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, thoracic and mediastinal disorders:
Rare: bronchospasm.

Skin and subcutaneous tissue disorders:
Rare: allergic reactions (including skin rashes, pruritus, urticaria, angioneurotic oedema) may occur after intake of high doses. If an allergic reaction occurs, discontinue the use of the product.

General disorders and administration site conditions:
Rare: decreased body temperature, weakness.
If a decrease in arterial blood pressure and/or body temperature occurs (body temperature may decrease by 1–1.5 °C), there is no need to discontinue the product. Blood pressure and body temperature normalize after completion of the treatment course.

Reporting of suspected adverse reactions after authorization of the medicinal product is important. It allows continuous monitoring of the benefit-risk balance of the product. Medical and pharmaceutical professionals, as well as patients or their legal representatives, are encouraged to report any 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 per blister; 2 blisters per carton.

Prescription status.

Prescription only.

Manufacturer.

JSC "Olfa" / Olpha AS.

Manufacturer's address.

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