Nanotopil® [Phenylpiracetam] Instruction

International Non-Proprietary Name (INN): phenylpiracetam
Dosage form: pills (100 mg)
Structure
1 capsule contains:
Active ingredient: N-carbamoylmethyl-4-phenyl-2-pyrrolidone – 100 mg;
Excipients: lactose monohydrate (milk sugar) – 51.52 mg; potato starch – 46.48 mg; calcium stearate – 2 mg.
Description
Flat-cylindrical pills in white color with light cream or yellowish hue.
Pharmacological classification: nootropic
ATC code: N06BX
Pharmacological action: anti-asthenic, anticonvulsant, anxiolytic, nootropic, neuromodulatory


Pharmacodynamics

Phenylpiracetam acts as a neuromodulator, it exerts an effect on the majority of neurotransmitter systems of the brain. The drug has a pronounced antiamnestic effect, it activates the integrative activity of the brain, promotes memory consolidation, improves concentration and mental activity, facilitates learning processes, accelerates the information transfer between the cerebral hemispheres, increases the resistance of brain tissue to hypoxia and toxic effects, has anticonvulsant action and anxiolytic activity, regulates the processes of activation and inhibition of the central nervous system and improves mood.

Phenylpiracetam 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 glucose utilization, and improves regional blood flow in the ischemic areas of the brain. The drug increases the content of noradrenaline, dopamine, and serotonin in the brain. It neither affects the GABA level or binds to GABA-A and GABA-B receptors, nor has a significant effect on spontaneous bioelectrical activity of the brain. Phenylpiracetam does not influence the respiratory or cardiovascular system. It has a mild diuretic effect and anorectic activity (with a full treatment course). Phenylpiracetam has a moderate activating effect on motor reactions, improves physical performance, antagonizes the catalepsy effect of neuroleptics, and reduces the hypnotic action of ethanol and hexenal.

The psychostimulating effect of Phenylpiracetam prevails in the ideational sphere. The moderate psychoactivating effect of the drug is combined with anxiolytic activity. Phenylpiracetam improves mood and acts as an analgesic by raising the pain threshold. The drug also has an adaptogenic effect enhancing resistance to stress under increased mental and physical loads, fatigue, hypokinesia, immobilization and at low temperatures. Patients, who used Phenylpiracetam, have noted vision improvement (increased acuity, brightness, and fields of vision). The drug improves the blood supply of the lower extremities. It stimulates the antibody response to antigen administration: therefore it shows immunostimulatory properties, but at the same time it does not cause immediate-type hypersensitivity reactions and does not change the allergic inflammatory reaction of the skin caused by the introduction of foreign protein.

A course of treatment does not lead to drug dependence, tolerance, or withdrawal syndromes. The action of Phenylpiracetam appears after a single dose, which is important when using the drug in extreme conditions. Phenylpiracetam does not have teratogenic, mutagenic, carcinogenic, and embryotoxic properties. It is a low-toxic drug: the lethal dose in an acute experiment is 800 mg/kg.

Pharmacokinetics

Phenylpiracetam is quickly absorbed, it penetrates into various organs and tissues and easily passes through the blood-brain barrier (BBB). The absolute bioavailability of the drug, when taken orally, is 100%. Tmax in the blood is 1 hour, T½ is 3–5 hours. Phenylpiracetam is not metabolized in the body and is excreted unchanged: about 40% with urine and 60% with bile and sweat.

Intended uses

  • CNS disoders of various genesis, especially those related to vascular diseases and metabolic disorders in the brain, intoxication (particularly in posttraumatic states and chronic cerebrovascular insufficiency), accompanied by deterioration of intellectual-mnestic functions and reduction of motor activity;
  • neurotic states, manifested by atony, increased exhaustion, decreased psychomotor activity, attention failure and memory impairment;
  • breakdown of the learning process;
  • depressions of mild to moderate severity;
  • psychoorganic syndromes, manifested by intellectual-mnestic disorders and apathetic-abulic phenomena, as well as apathetic states in schizophrenia;
  • convulsive states;
  • obesity (alimentary-constitutional genesis);
  • hypoxia prevention, increasing resistance to stress;
  • correction of the functional state of organism in extreme conditions of professional activity with the purpose of fatigue prevention and increase of mental and physical working capacity;
  • correction of daily biorhythm, inversion of the sleep-wake cycle;
  • chronic alcoholism (in order to reduce asthenia, depression and intellectual-mnestic disorders).


Contraindications

Individual intolerance. It is not recommended for children, pregnant and lactating ladies due to the lack of clinical research data. (+See “With caution”)

With caution: Patients with severe liver and kidneys diseases, severe arterial hypertension, severe atherosclerosis, previous panic attacks, and acute psychotic states accompanied by psychomotor agitation (due to the possible exacerbation of anxiety, panic, hallucinations, and delirium), as well as patients prone to allergic reactions to nootropic drugs of the pyrrolidone group.

Dosage and administration

Phenylpiracetam should be taken orally straight after meals.

The dosage and duration of treatment should be determined individually by the doctor in accordance with the patient’s condition. The average single dosage ranges from 100 to 250 mg and the average daily dosage from 200 to 300 mg. The maximally tolerated dosage is 750 mg per day. If the daily dose does not exceed 100 mg it is recommended to take it once a day in the morning, but if it is more than 100 mg, it should be divided into 2 administrations. Duration of the treatment course can vary from 2 weeks to 3 months, on average 30 days. If necessary, the course can be repeated in 1 month.

To improve performance
100–200 mg once in the morning for 2 weeks (for athletes – 3 days).

Alimentary-constitutional obesity
100–200 mg once a day (in the morning) for 30–60 days.

Side effects

Insomnia (in case of drug administration later than 3 pm). During the first 1–3 days of admission, some patients may suffer psychomotor agitation, hyperemia of the skin, warm flashes, and hypertension.

Overdose

No overdose cases have been reported. If necessary, conduct symptomatic therapy.

Interaction with other drugs

Phenylpiracetam can enhance the effect of CNS stimulators, antidepressants, and nootropics.

Special instructions

It is not recommended to take Phenylpiracetam after 3 pm.

The administration of Phenylpiracetam in patients with excessive psycho-emotional exhaustion resulted from chronic stress, fatigue, and insomnia, on the first day of the treatment can cause a sharp need for sleep. Therefore it is recommended to begin the treatment course on non-working days.

Pregnancy and lactation

Phenylpiracetam is not recommended during pregnancy and lactation.

Influence on the ability to drive vehicles and operate mechanisms

During the course of Phenylpiracetam treatment, it is recommended to avoid carrying out potentially dangerous jobs that require an increased concentration of attention and quick psychomotor reactions, as well as driving vehicles.

Terms of release from pharmacy

On prescription.

Storage conditions

Store in a dry dark place at temperatures no higher than 30°C. Keep out of reach of children.

Shelf life

5 years. Do not use beyond the expiration date printed on the package.

Manufacturer

Valenta Pharm, Russia. www.valentapharm.com/eng/

Instructions