NOOFEN

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT NOOFEN® (NOOFEN)

Composition:

Active ingredient: phenibut;

1 tablet contains 250 mg of phenibut;

Excipients: lactose monohydrate; corn starch; modified pregelatinized corn starch; stearic acid.

Pharmaceutical form. Tablets.

Main physicochemical properties: flat cylindrical tablets of white to white with a yellowish tinge color, with a bevel and a score line on one side.

Pharmacotherapeutic group. Other psychostimulants and nootropic agents.

ATC code N06B X22.

Pharmacological Properties

Pharmacodynamics

Phenibut® is a derivative of γ-aminobutyric acid (GABA) and phenylethylamine.

Its primary effects are anti-hypoxic and anti-amnestic. Phenibut® improves memory and attention, facilitates learning processes, and enhances physical and mental performance. Psychological parameters (attention, memory, speed and accuracy of sensorimotor responses) improve under the influence of Phenibut®. It has been established that Phenibut® increases the neuron's energy potential by improving mitochondrial function.

Phenibut® also possesses tranquilizing properties: it reduces psychoemotional tension, anxiety, fear, emotional lability, irritability, and improves sleep. It prolongs and enhances the effects of sedatives, hypnotics, narcotics, neuroleptics, and anticonvulsants. Phenibut® binds exclusively to GABA-B receptors in the brain, thus exerting a moderate calming effect without causing undesirable sedative effects such as drowsiness, dizziness, reduced attention, or impaired performance. The drug prolongs the latent period and reduces the duration and intensity of nystagmus, demonstrating antiepileptic activity. It does not affect cholinergic or adrenergic receptors.

Phenibut® significantly reduces symptoms of asthenia and vasovagal symptoms, including headache and a sensation of heaviness in the head. In patients with asthenia and emotionally labile individuals, treatment with Phenibut® improves well-being without causing excitation.

Pharmacokinetics

Absorption and Distribution

The drug is well absorbed after oral administration and readily penetrates all tissues of the body. It crosses the blood-brain barrier effectively (approximately 0.1% of the administered dose reaches brain tissue, with notably higher penetration observed in both young and elderly individuals). The highest binding of phenibut occurs in the liver (80%), and this binding is nonspecific.

Biotransformation and Excretion

80–95% of phenibut is metabolized in the liver; the metabolites are pharmacologically inactive.

Distribution in the liver and kidneys is close to uniform, while in the brain and blood it is lower than uniform. A significant amount of administered phenibut can be detected in urine within 3 hours. At the same time, the concentration of the drug in brain tissue does not decrease—phenibut remains detectable in the brain for up to 6 hours. The following day, phenibut is detectable only in urine; it can still be found in urine up to 2 days after administration, although the amount detected constitutes only 5% of the administered dose. With repeated administration, no accumulation is observed.

Clinical characteristics.

Indications.

Asthenic and anxiety-neurotic states: restlessness, fear, anxiety.

Insomnia, nocturnal restlessness in elderly people.

Prevention of stress conditions prior to surgeries or painful diagnostic procedures.

Meniere's disease, dizziness associated with vestibular analyzer dysfunction of various origins.

Prevention of kinetosis (a specific condition characterized by nausea, vomiting, prostration, and vestibular dysfunction caused by being in a moving object such as a ship or airplane).

Stuttering, tics in children aged 8 to 14 years.

As an adjunctive agent in the treatment of alcohol withdrawal syndrome.

Contraindications.

Hypersensitivity to the components of the drug.

Acute renal failure.

Pregnancy and breastfeeding period.

Interaction with other medicinal products and other forms of interactions.

Noofen® can be combined with psychotropic medicinal products, reducing the doses of Noofen® and the concomitantly administered medicinal products.

Noofen® enhances and prolongs the effect of hypnotics, narcotics, neuroleptics, and antiparkinsonian medicinal products.

Special precautions for use

The medicinal product should be used with caution in patients with stomach or intestinal disorders. To protect the mucosa from the irritant effect of phenibut, lower doses should be prescribed to these patients.

In case of prolonged treatment, blood and liver parameters should be monitored.

The medicinal product contains lactose; therefore, it should not be administered to patients with rare hereditary forms of galactose intolerance, lactase deficiency, or glucose-galactose malabsorption syndrome.

Use during pregnancy or breastfeeding

Animal studies have not revealed mutagenic, teratogenic, or embryotoxic effects of phenibut. However, there are insufficient and well-controlled studies on the safety of phenibut use in pregnant women. Therefore, the use of Noofen® during pregnancy or breastfeeding is contraindicated.

Ability to influence reaction rate while driving or operating machinery

Patients who experience somnolence, dizziness, or other central nervous system disturbances during treatment with this medicinal product should refrain from driving or operating machinery.

Dosage and Administration

Noofen® is taken orally before meals. The tablet should be swallowed whole with sufficient amount of water.

Treatment of asthenic and anxiety-neurotic states in adults: 250–500 mg (1–2 tablets) three times daily. Maximum single doses: for adults – 750 mg; for elderly patients – 500 mg.

The treatment course lasts 2–3 weeks. If necessary, the course may be extended to 4–6 weeks.

Children aged 8 to 14 years: 250 mg (1 tablet) three times daily.

Noofen®, 250 mg capsules, may be used as an alternative dosage form.

The treatment course lasts 2–6 weeks.

Meniere’s disease, vertigo associated with vestibular dysfunction of various origins.

In infectious vestibular dysfunction and Meniere’s disease during exacerbation, Noofen® is administered at 750 mg (3 tablets) three times daily for 5–7 days; after reduction in severity of vestibular disturbances – 250–500 mg (1–2 tablets) three times daily for 5–7 days, followed by 250 mg once daily for 5 days. In milder cases, Noofen® is administered at 250 mg (1 tablet) twice daily for 5–7 days, followed by 250 mg once daily for 7–10 days.

For relief of vertigo in vascular and traumatic vestibular dysfunction: Noofen® is administered at 250 mg three times daily for 12 days.

For prevention of kinetosis: the drug should be taken once at a dose of 250–500 mg one hour before the expected onset of motion sickness or at the first symptoms of motion discomfort.

For management of alcohol withdrawal syndrome: during the first days of treatment, Noofen® is administered at 250–500 mg three times daily and 750 mg at bedtime, with gradual reduction of the daily dose to the usual adult dose.

Patients with hepatic impairment

High doses of the drug may cause hepatotoxicity in patients with hepatic impairment. Lower doses should be prescribed for this patient group.

Patients with renal impairment

There are no data on adverse effects of Noofen® in patients with impaired renal function when administered at therapeutic doses.

No drug dependence or withdrawal syndrome has been observed during use of this medicinal product.

Isolated cases of tolerance to phenibut have been reported in the literature.

Children

The drug may be used in children aged 8 years and older.

Overdose

Noofen® is a low-toxicity medicinal product: hepatotoxicity may occur only with prolonged administration of daily doses of 7–14 g. Data on overdose are limited.

These doses significantly exceed the recommended dose (average therapeutic dose is 500–2000 mg).

Symptoms: somnolence, nausea, vomiting, dizziness.

With prolonged use of high doses, arterial hypotension, acute renal failure, eosinophilia, and fatty liver degeneration may develop.

Treatment: gastric lavage. Symptomatic therapy.

There is no specific antidote.

Adverse Reactions

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

Classification of adverse reactions by frequency of occurrence: 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 the available data).

Central and peripheral nervous system disorders: frequency not known – drowsiness (at the beginning of treatment), headache and dizziness (at doses above 2 g per day; reducing the dose alleviates the intensity of this adverse effect).

Gastrointestinal disorders: frequency not known – nausea (at the beginning of treatment), vomiting, diarrhea, epigastric pain.

Hepatobiliary disorders: frequency not known – hepatotoxicity (with long-term use of high doses).

Immune system disorders: frequency not known – hypersensitivity reactions, including urticaria, erythema, rash, angioneurotic edema, facial swelling, tongue swelling.

Skin and subcutaneous tissue disorders: rare – allergic reactions (rash, pruritus).

Psychiatric disorders: frequency not known – emotional lability, sleep disturbances (these adverse reactions may occur in children if the instructions for use are not followed).

If any adverse reactions not listed in this instruction occur during treatment, or if any of the listed adverse reactions are particularly severe, please consult your physician.

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 in a blister pack. 2 blisters per cardboard box.

Prescription status.

Prescription only.

Manufacturer.

JSC "Olfa" / Olpha AS.

Manufacturer's address.

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