Phenylpiracetam - Phenotropil - Instructions for Use, Dosage, Side Effects, Reviews

Pharmacological group: Nootropics.

Synonyms: Phenotropil, Carphedon, Phenylpiracetam, Fonturacetam, Fenotropil,

Active substance: N-carbamoylmethyl–4-phenyl–2-pyrrolidone.

Country of manufacturer: Russia.

Phenylpiracetam (INN: fonturacetam, brand names Phenotropil, Carphedon), also called is a phenylated analog of the drug piracetam which was developed in 1983 in Russia where it is available as a prescription drug. Research on animals has indicated that phenylpiracetam may have anti-amnesic, antidepressant, anticonvulsant, antipsychotic, anxiolytic, and memory enhancement effects.

Phenylpiracetam binds to α4β2 nicotinic acetylcholine receptors in the mouse brain cortex with IC50 = 5.86 μM

In rats, scopolamine is used to model memory impairment. It impairs performance in the conditioned passive avoidance reflex test, increases cortical nACh and hippocampal NMDA receptor densities, and decreases striatal D1 and cortical benzodiazepine receptor densities. Phenylpiracetam demonstrates antiamnestic activity by restoring performance in the passive avoidance test and partially reversing each of these scopolamine-induced receptor density changes.

Experiments performed on Sprague-Dawley rats in a European patent for using Phenylpiracetam to treat sleep disorders showed an increase in extracellular dopamine levels after administration. The patent asserts discovery of phenypiracetam's action as a dopamine reuptake inhibitor as its basis.

The peculiarity of this invention compared to former treatment approaches for treating sleep disorders is the so far unknown therapeutic efficacy of (R)-phenylpiracetam, which is presumably based at least in part on the newly identified activity of (R)-phenylpiracetam as the dopamine re-uptake inhibitor.

Because Phenylpiracetam increases physical stamina and provides improved tolerance to cold weather, Phenylpiracetam appears on the lists of stimulants banned for in-competition use by the World Anti-Doping Agency. This list is applicable in all Olympic sports.

Sometimes Phenylpiracetam is mussed up with Methylphenylpiracetam (2-(5-Methyl-2-oxo-4-phenyl-pyrrolidin-1-yl)-acetamide); Methylphenylpiracetam is a derivative of piracetam and a positive allosteric modulator of the sigma-1 receptor. It differs from phenylpiracetam by having a methyl group.

ATC N06BX Other psychostimulants and nootropics.

Nosological classification (ICD–10)

E66.9 Obesity, unspecified;

F07.9 Organic personality disorder and behavior due to illness, injury or brain dysfunction, unspecified;

F10.2 Alcohol dependence syndrome;

F20 Schizophrenia;

F32 Depressive episode;

F33 Recurrent depressive disorder;

F48.9 Neurotic disorder, unspecified;

F81 Specific developmental disorders of learning skills;

F90.0 disturbance of activity and attention;

I67.9 Cerebrovascular disease, unspecified;

R25.2 cramps and spasms;

R41.3.0 * Reduced memory;

R41.8.0 * Disorders Intellectual mnestic;

R45.3 Demoralization and apathy;

R45.7 state of emotional shock and stress, unspecified;

R46.4 Confusion and slow response;

R53 Malaise and fatigue;

T90.9 Consequences unspecified head injury;

Z60.0 Problems related to adaptation to changes in lifestyle;

Z73.6 Restrictions on activity, caused by reduced disability.

Pharmacological action of Phenylpiracetam

Nootropic drug. Has expressed antiamnesic action activates the integrative activity of the brain contributes to the consolidation of memory, improves concentration and mental performance, facilitates learning processes, accelerate the transfer of information between the hemispheres of the brain, increases the resistance of brain tissue hypoxia and toxic effects, has anticonvulsant activity and anxiolytic activity regulates the activation and inhibition of CNS improves mood.

Phenotropil has a positive effect on metabolism and blood circulation of the brain, stimulates the redox processes, increases the body’s energy potential through the utilization of glucose, and improves regional blood flow in the ischemic areas of the brain. Increases of noradrenaline, dopamine and serotonin in the brain.

Does not affect the levels of GABA, does not bind to GABA A - and GABA B receptors, has no appreciable effect on the spontaneous brain activity.

Phenylpiracetam no effect on the respiratory and cardiovascular systems. Has a weakly expressed diuretic effect. Has anorexogenic activity in exchange application.

Phenylpiracetam has moderately activating effect in respect of motor reactions, increases physical performance, has a strong antagonism cataleptic action of neuroleptics, reduces the severity of hypnotic action of ethanol and hexenal.

Stimulating effect Phenylpiracetam prevails in the ideatoric field. Moderate psychoactivating effect of the drug is combined with anxiolytic activity. Phenotropil improves mood, has analgesic effects, increasing the pain threshold.

Phenylpiracetam has an adaptogenic effect, increasing the body’s resistance to stress at elevated mental and physical loads, fatigue, hypokinesia and immobilization at low temperatures.

Against the background of Phenylpiracetam marked improvement in vision (increase sharpness, brightness and field of view).

Phenylpiracetam improves blood flow to the lower extremities.

Phenotropil stimulate antibody production in response to antigen challenge, which indicates its immunostimulatory properties, but at the same time does not cause the development of immediate hypersensitivity reactions and not alter the allergic inflammatory reaction of the skin caused by the introduction of the foreign protein.

In exchange application Phenylpiracetam not develop drug dependence and tolerance. When canceling the development of the drug were observed withdrawal.

Action Phenylpiracetam already apparent after a single dose, which is important when using the drug in extreme conditions.

Pharmacokinetics

Absorption and distribution

After intake of rapidly absorbed from the gastrointestinal tract, distributed in various organs and tissues, easily penetrates through the BBB. The absolute bioavailability of the drug when administered to 100%. C max levels achieved after 1 h

Metabolism and excretion of Phenylpiracetam

Phenylpiracetam not metabolized in the body and is excreted unchanged. About 40% is excreted in the urine, 60% - in the bile and then. T 1/2 is 3–5 hours.

Phenylpiracetam Dosage

Mode set individually.

Phenylpiracetam is taken orally immediately after eating.

The average single dose is 100–200 mg, the mean daily dose - 200–300 mg. The maximum daily dose - 750 mg. Recommended to divide the daily dose into 2 doses. Daily dose of 100 mg should be taken 1 time/day in the morning, a daily dose of more than 100 mg should be divided into 2 doses. The duration of treatment may vary from 2 weeks to 3 months. Average duration of treatment is 30 days. If necessary, can be repeated in a month.

To improve efficiency, appoint 100–200 mg 1 time/day in the morning for 2 weeks (for athletes - 3 days).

When alimentary-constitutional obesity - 100–200 mg 1 time/day in the morning for 30–60 days.

Not to take Phenylpiracetam after 15 hours.

Phenylpiracetam Overdose

Currently, the cases of drug overdose Phenylpiracetam reported. If necessary, symptomatic therapy.

Phenylpiracetam Drug Interactions

Phenylpiracetam may increase the effects of drugs that stimulate the central nervous system, anti-depressants and neuroprotective drugs.

Phenylpiracetam at Pregnancy and lactation

Phenylpiracetam should not be administered during pregnancy and lactation ( breastfeeding ) due to the lack of clinical trial data.

Phenylpiracetam not teratogenic, mutagenic and embryotoxic effects.

Phenylpiracetam Side effects

CNS: insomnia (while taking the drug after 15 h).

Some patients in the first 3 days of admission - psychomotor agitation, flushing of the skin, feeling of warmth, increased blood pressure.

Indications for Phenylpiracetam

CNS diseases of various origins, especially diseases of vascular origin or associated with disorders of metabolic processes in the brain and intoxication (particularly in post-traumatic states and phenomena of chronic cerebrovascular insufficiency), accompanied by the deterioration of intellectual-mental functions, decreased motor activity;

Neurotic conditions manifested by lethargy, increased exhaustion, decreased psychomotor activity, impaired attention, memory impairment;

Violations of learning processes;

Mild to moderate depression severity;

Psycho-organic syndromes manifest intellectual mnestic violations and apathy-abulic symptoms and little-apathy of schizophrenia;

Convulsive conditions;

Obesity (alimentary-constitutional genesis);

Prevention of hypoxia, increased 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 improve mental and physical performance;

Correction of daily biorhythms, regulation cycle “sleep-wake”;

Chronic alcoholism (to reduce symptoms of fatigue, depression, intellectual-mental disorders).

Contraindications for Phenylpiracetam

Hypersensitivity to the drug.

Precautions should be prescribed to patients with severe organic liver and kidney failure, severe hypertension, with advanced atherosclerosis, patients who have had previous panic attacks, acute psychotic state, accompanied by psychomotor agitation (as possibly worsening anxiety, panic, hallucinations and delirium) in patients prone to allergic reactions to nootropics pyrrolidone groups.

PhenylpiracetamReviews

Phenylpiracetam - known neuroprotective drugs. Title its active component coincides with the trade name. It is located in the same group with piracetam. This tool is characterized by the ability to work on complex state of mind, the cognitive functions of humans. This is because Phenylpiracetam considerably improves metabolism in the brain: restored circulation, enhanced cleavage of glucose, which increases the amount of energy of the nerve cells. In addition, under the influence of this drug increases the concentration of the regulators of the nervous system such as dopamine, serotonin and norepinephrine. Phenylpiracetam Treatment reduces the body's readiness to seizures, increases pain tolerance. It improves mood, human performance. At the cardiovascular system and respiratory Phenylpiracetam not affected. During the use of this drug improves vision, blood flow to the extremities, ability to tolerate stress. medicines described the ability to maintain health by activating the immune system. For the first reception of this tool shows its beneficial effects on the human body.

As with any other medicinal product reviews about Phenylpiracetam range from the positive to the complete neglect. Interesting and revealing can be called such reports:

- He began to take Phenylpiracetam 200 mg in the morning. Terrific, I wanted to work! It was interesting, there was the inspiration to do something from which previously turn up his nose.

- We have to work a programmer Phenylpiracetam drink, that they might deliver the project. Well, I notice that he seems to think quickly and be more productive. But the emotions that "burned" - as a cyborg sits and works ...
- Nothing is easier to work with him. Only appeared irritability and insomnia happens. And my husband is sleeping well, despite Phenylpiracetam. A fifteen-year son gave - in general no effects.

Based on the foregoing, we can conclude that Phenylpiracetam - effective means. However, his admission should consult with your doctor to foresee and avoid the adverse effects of the drug, such as insomnia. Even if you become a better feel, taking Phenylpiracetam yourself - this improvement can result in health problems. So be sure, even after the fact, and consult with a specialist about the use of the drug, and the reasons that led you to drink it.