Actitropil (Tablets) Instructions for Use

Marketing Authorization Holder

Pharmstandard-Lexredstva OJSC (Russia)

ATC Code

N06BX (Other psychostimulants and nootropic drugs)

Active Substance

Fonturacetam (Rec.INN registered by WHO)

Dosage Forms

	Actitropil	Tablets 50 mg: 30 or 60 pcs.
		Tablets 100 mg: 30 or 60 pcs.

Dosage Form, Packaging, and Composition

Tablets from white to white with a yellowish or brownish tint, flat-cylindrical, with a bevel, marbling is allowed.

Excipients: microcrystalline cellulose 101 – 9 mg, povidone K17 (low molecular weight polyvinylpyrrolidone K17) – 20 mg, hypromellose (hydroxypropylcellulose) – 10 mg, sodium bicarbonate – 10 mg, stearic acid – 1 mg.

10 pcs. – contour cell blisters (3) – cardboard packs.
10 pcs. – contour cell blisters (6) – cardboard packs.
15 pcs. – contour cell blisters (2) – cardboard packs.

Tablets from white to white with a yellowish or brownish tint, flat-cylindrical, with a score on one side and a bevel, marbling is allowed.

Excipients: microcrystalline cellulose 101 – 18 mg, povidone K17 (low molecular weight polyvinylpyrrolidone K17) – 40 mg, hypromellose (hydroxypropylcellulose) – 20 mg, sodium bicarbonate – 20 mg, stearic acid – 2 mg.

10 pcs. – contour cell blisters (3) – cardboard packs.
10 pcs. – contour cell blisters (6) – cardboard packs.
15 pcs. – contour cell blisters (2) – cardboard packs.

Clinical-Pharmacological Group

Nootropic drug

Pharmacotherapeutic Group

Nootropic agent

Pharmacological Action

Nootropic agent. It has a pronounced anti-amnesic effect, activates the integrative activity of the brain, promotes memory consolidation, improves concentration and mental activity, facilitates learning processes, accelerates the transmission of information between the cerebral hemispheres, increases the resistance of brain tissue to hypoxia and toxic effects, has an anticonvulsant effect and anxiolytic activity, regulates the processes of activation and inhibition of the central nervous system, improves mood.

It has a positive effect on the metabolic processes and blood circulation of the brain, stimulates redox processes, increases the energy potential of the body through the utilization of glucose, improves regional blood flow in ischemic areas of the brain. It increases the content of norepinephrine, dopamine and serotonin in the brain.

It does not affect the GABA content level, does not bind to GABA_A and GABA_B receptors, and does not have a noticeable effect on the spontaneous bioelectrical activity of the brain.

It does not affect the respiratory and cardiovascular systems. It has a mild diuretic effect. It has anorexigenic activity with course use.

It has a moderately activating effect on motor reactions, increases physical performance, has a pronounced antagonism to the cataleptic effect of neuroleptics, and reduces the severity of the hypnotic effect of ethanol and hexenal.

The psychostimulating effect predominates in the ideational sphere. The moderate psychoactivating effect of the drug is combined with anxiolytic activity; it improves mood, has an analgesic effect by increasing the pain sensitivity threshold.

It has an adaptogenic effect, increasing the body’s resistance to stress under conditions of increased mental and physical stress, fatigue, hypokinesia and immobilization, and at low temperatures.

Against the background of the drug use, an improvement in vision is noted (increase in acuity, brightness and visual fields); blood supply to the lower extremities improves.

It stimulates the production of antibodies in response to antigen administration, which indicates its immunostimulating properties, but at the same time does not cause the development of immediate hypersensitivity reactions and does not alter the allergic inflammatory skin reaction caused by the introduction of a foreign protein.

The effect manifests itself after a single dose, which is important for use in extreme conditions.

Pharmacokinetics

After oral administration, it is rapidly absorbed from the gastrointestinal tract, distributed in various organs and tissues, and easily penetrates the BBB. The absolute bioavailability of the drug when taken orally is 100%. C_max in the blood is reached after 1 hour. It is not metabolized in the body and is excreted unchanged. About 40% is excreted in the urine, 60% in bile and sweat. T_1/2 is 3-5 hours.

Indications

Diseases of the central nervous system of various origins, especially vascular diseases or those associated with disorders of metabolic processes in the brain and intoxication (in particular, in post-traumatic conditions and phenomena of chronic cerebrovascular insufficiency), accompanied by deterioration of intellectual and mnestic functions, decreased motor activity; neurotic conditions manifested by lethargy, increased exhaustion, decreased psychomotor activity, impaired attention, memory deterioration; learning disabilities; mild and moderate depression; psycho-organic syndromes manifested by intellectual and mnestic disorders and apathetic-abulic symptoms, as well as sluggish-apathic conditions in schizophrenia; convulsive conditions; obesity (alimentary-constitutional origin); prevention of hypoxia, increasing resistance to stress; correction of the functional state of the body in extreme conditions of professional activity in order to prevent the development of fatigue and increase mental and physical performance; correction of the daily biorhythm, regulation of the sleep-wake cycle; chronic alcoholism (to reduce the symptoms of asthenia, depression, intellectual and mnestic disorders).

ICD codes

Dosage Regimen

Administer orally. The dosage regimen is individual and must be determined by a physician based on the specific indication, patient age, and clinical situation.

For adults, the typical single dose is 50 mg to 100 mg. The maximum single dose should not exceed 100 mg.

Take tablets two to three times daily. The maximum daily dose is 300 mg.

To prevent insomnia, administer the last dose of the day no later than 3 PM.

The duration of the treatment course is typically 2 to 4 weeks or as long as clinically indicated. A second course may be prescribed after a 1-month interval.

For the prevention of hypoxia and increasing resistance to stress, use a dose of 50 mg to 100 mg once daily for 1-2 weeks.

For the correction of performance under extreme conditions, use a dose of 100 mg to 200 mg as a single administration.

In patients with severe hepatic or renal impairment, use with caution and potentially at a reduced dose.

In elderly patients, initiate therapy at the lower end of the dosing range and titrate carefully.

Do not use in children or adolescents under 18 years of age.

Adverse Reactions

From the central nervous system insomnia (when taking the drug after 3 PM).

In some patients during the first 3 days of administration – psychomotor agitation, skin hyperemia, feeling of heat, increased blood pressure.

Contraindications

Childhood, pregnancy, lactation (breastfeeding), hypersensitivity to fonturacetam.

Use in Pregnancy and Lactation

Should not be prescribed during pregnancy and lactation (breastfeeding) due to the lack of clinical trial data; it does not have teratogenic, mutagenic or embryotoxic effects.

Use in Hepatic Impairment

With caution in patients with severe organic liver lesions.

Use in Renal Impairment

With caution in patients with severe organic kidney lesions.

Pediatric Use

The drug is contraindicated for use in children and adolescents under 18 years of age.

Geriatric Use

Use with caution in elderly patients to avoid worsening of concomitant diseases.

Special Precautions

It should be used with caution in patients with severe organic lesions of the liver and kidneys, severe arterial hypertension, with pronounced atherosclerosis; in patients who have previously experienced panic attacks, acute psychotic conditions accompanied by psychomotor agitation (since exacerbation of anxiety, panic, hallucinations and delusions is possible); in patients prone to allergic reactions to nootropic drugs of the pyrrolidone group.

It should be taken into account that with excessive psycho-emotional exhaustion against the background of chronic stress and fatigue, chronic insomnia, a single dose of fonturacetam on the first day can cause a sharp need for sleep.

Drug Interactions

May enhance the effect of drugs stimulating the central nervous system, antidepressants and nootropic drugs.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.