Instruction for use: Phenibut

Trade name of the drug – Phenibut

International nonproprietary name: Phenibutum

Chemical rational name: γ-amino-β-phenylbutyric acid hydrochloride.

Dosage Form: pills
Composition:
Ingredients: 1 tablet contains:
active ingredient - Phenibutum 250 mg;
Excipients - lactose, potato starch, calcium stearate.
Description:Tablets white, odorless or with a faint odor, round, yellowish tint.
Pharmacotherapeutic group:nootropic agent.

ATX Code N05BX

Pharmacological Properties

Phenibut is a phenyl derivative of GABA and phenylethylamine. It has anxiolytic effects, reduce stress, anxiety, fear, and improve sleep; It extends and enhances the effects of sleeping pills, narcotic drugs and neuroleptic drugs..
Pharmacodynamics. 

Phenibut - nootropic agent facilitates GABA-mediated neurotransmission in the central nervous system (direct effects on the GABA-ergic receptors). Also it has a tranquilizing, psychostimulant, antiplatelet and antioxidant effects.It improves the functional state of the brain due to the normalization of tissue metabolism and effects on cerebral blood flow (increases the volume and the linear velocity of cerebral blood flow, reduces cerebral vascular resistance, improves microcirculation, has antiplatelet effect). It helps reduce or disappearance of feelings of anxiety, tension, anxiety and fear, normalizes sleep, has an anticonvulsant effect.No effect on choline and adrenergic receptors. It extends the latent period and shortens the duration and severity of nystagmus. Reduces the symptoms of fatigue and vasovegetative symptoms (including headache, a feeling of heaviness in the head, sleep disturbances, irritability, emotional lability), enhances mental performance.It improves mental performance (attention, memory, speed and accuracy of sensory-motor reactions). In exchange reception improves physical and mental performance, improves memory, normalizes sleep; It improves the condition of patients with movement and speech disorders.Patients asthenia from the first days of therapy improves mood, increases the interest and initiative (motivation activities) without sedation or excitation.
In the elderly does not cause depression of the central nervous system, muscle-relaxing-effect often absent.
It improves the microcirculation in the eye tissues, reduces the inhibitory effect of ethanol on the central nervous system. The drug has low toxicity, it does not cause allergic effects, as well as teratogenic, embryotoxic and carcinogenic effects.

Pharmacokinetics.

 Absorption of high drug penetrates well in all body tissues and the blood brain barrier (BBB). In about 0.1% of brain tissue enters the administered dose of the drug, with the young and the elderly to a greater extent. Evenly distributed in the liver and kidneys. It is metabolized in the liver -80-95%, the pharmacologically inactive metabolites. Do not cumulated. After 3 hours kidney begins to stand out, with the concentration in brain tissue and does not exhibit reduced in the brain for a further 6 hours. Approximately 5% is excreted by the kidneys unchanged, partly in the bile.

Indications
Asthenic and anxious-neurotic states, worry, anxiety, fear; in children with stuttering and tics; in the elderly - insomnia; for the prevention of anxiety disorders that arise before surgery and painful diagnostic studies. In the complex treatment of alcoholism for the relief of psychopathological and somatic-vegetative disorders with withdrawal syndrome. In combination with detoxication preparation means it can be used to treat pre-delirious states in alcoholism.
Meniere's disease, vertigo associated with dysfunction of the vestibular apparatus of various origins; for the prevention of motion sickness when kinetoses.

Contraindications
Individual intolerance, pregnancy (1 trimester), breastfeeding, children under 2 years.The caution in patients with erosive and ulcerative lesions of the gastrointestinal tract, liver failure.

Dosing and Administration

Inside after eating 2-3-week course. Adults: 250-500 mg 3 times a day. If necessary, after the daily dose increased up to 2500 mg. Children from 2 to 8 years - 50-100 mg; 8 to 14 - 250 mg 3 times a day. The single maximum dose in adults is 750 mg in patients over age 60 -500 mg, for children up to 8 years - 150 mg, from 8 to 14 years - 250 mg.For treatment of alcohol withdrawal syndrome are administered in the first few days of treatment day by 250-500 mg 3 times daily and at bedtime to 750 mg, with a gradual decrease in the daily dose to normal adult.
For the treatment of vertigo with vestibular dysfunction and Meniere's disease appoint 250 mg 3 times daily for 14 days.
To prevent motion sickness take a dose of 250-500 mg once daily for 1 hour before starting pitching, or at the first light of seasickness symptoms. Antiastetic action of Phenibut tablets increases with increasing dose. When the express manifestation of motion sickness (vomiting, etc.) pills inside Phenibut ineffective even at doses of 750-1000 mg.
Side effects
Drowsiness, nausea. Increased irritability, agitation, anxiety, dizziness, headache (with the first receptions), allergic reactions (rash, pruritus).
Overdose
Increased symptoms of side effects: severe drowsiness, nausea, vomiting, fatty liver degeneration (receiving more than 7 g), eosinophilia, decreased blood pressure, renal function. First aid - gastric lavage, activated charcoal and symptomatic therapy.
Interaction with other drugs

With a view to mutual potentiation of drug Phenibut can be combined with other psychotropic drugs, reducing the dose of the drug Phenibut and match them with drugs. It extends and enhances the effects of sleeping pills, narcotic, antipsychotic and anticonvulsant drugs, and alcohol. There is evidence of increased under the influence of anti-Parkinsonian drug Phenibut action means.
Special instructions
With prolonged use it is necessary to monitor liver function and pattern of peripheral blood. It should refrain from potentially hazardous activities that require attention.
Release Form
Tablet 250 mg. 10 tablets in blisters. Blisters to 1; 2; 3; 4; 5 together with instructions for use placed in a pile of cardboard.
Storage conditions
List B. In dry the dark place at a temperature no higher than 25 ° C.
Keep out of the reach of children.
Shelf life
3 years. Do not use beyond the expiration date printed on the package.
Conditions of supply at the pharmacy
On prescription.