Encephabol (Pyritinol) - Instructions for Use, Dosage, Side Effects, Reviews
25 Mar 2017
Synonyms: Bonifen, Encefabol, Encepan, Encephabol, Fitina, Piritinol L.CH., Acon, Ai Nao Xing, An Jie De Xin, Bonitrop, Cerbon–6, Encefabol 600 MD, Encefabol Forte, Encefabol, Encephabol, Encephabol forte, Enerbol, Italram, Ling Bo Kang, Memonol, Piritinol Diclorhidrato Mintlab, Piritinol, Pyrithioxin, Pyritil, Pyritinol - New Asiatic Pharm, Pyritinol New Asiatic Pharm, Pyritinol-Hua Nan Pharm, Tian Shu Qing, Xin Te, Yi Shou, Ying Luo En.
Active substance: Pyritinol.
ATC - N06BX02 Pyritinol.
Pharmacological group - Nootropics.
Pyritinol also called pyridoxine disulfide or pyrithioxine (European drug names Encephabol, Encefabol, Cerbon 6) is a semi-synthetic water-soluble analog of vitamin B6 (Pyridoxine HCl).
Nosological classification (ICD–10)
F01 Vascular dementia;
F03 Dementia, unspecified;
F79 Mental retardation, unspecified;
F90.0 disturbance of activity and attention;
I67.9 Cerebrovascular disease, unspecified;
R41.0 disorientation unspecified;
R41.3.0 * Reduced memory;
R41.8.0 * Disorders Intellectual mnestic;
S06 intracranial injury;
T90.5 Effects of intracranial injury.
Encephabol (Pyritinol) Composition, structure and packing
- Encephabol (Pyritinol) Tablets, coated yellow, shiny, round, biconcave. The cross section showed two layers.
Excipients: sodium carmellose 7000 - 1.6 mg magnesium stearate - 3.2 mg colloidal silicon dioxide - 4.8 mg, carboxymethyl sodium - 6.4 mg lactose monohydrate - 19.8 mg, cellulose powder - 24.2 mg, quinoline yellow dye 70% - 30 mcg wax mountain glycol - 80 mcg, gelatin - 800 mcg, acacia gum - 1.7 mg, wheat flour - 8.2 mg titanium dioxide - 9.0 mg, kaolin - 14.2 mg, talc - 14.3 mg, sucrose - 121.69 mg.
- Encephabol (Pyritinol) Oral suspension milky white, viscous, with a fragrant smell.
Excipients: Sodium saccharine dihydrate - 1.1 mg methyl parahydroxybenzoate - 3.25 mg propyl parahydroxybenzoate - 1.75 mg of citric acid monohydrate - 5 mg Potassium sorbate - 6.75 mg Povidone - 50 mg colloidal silicon dioxide - 50 mg Hydroxyethylcellulose - 60 mg, glycerol 85% - 250 mg, 70% sorbitol solution - 750 mg, the essence of natural special - 10 mg, a cocktail of natural essences - 2.5 mg, purified water - 4029.15 mg.
Encephabol (Pyritinol) Pharmacological action
Nootropic drug. Increases pathologically decreased metabolism in the brain tissue that is caused by increasing the capture and utilization of glucose increases the metabolism of nucleic acids and the release of acetylcholine at synapses of the nerve cells, improve cholinergic transmission in the nervous tissue.
Pyritinol helps to stabilize the structure of cell membranes of neurons and their function through the inhibition of lysosomal enzymes, preventing the formation of these free radicals.
Encephabol improves the rheological properties of the blood, erythrocytes increase ductility by increasing the content of ATP in the membrane, which leads to a reduction in blood viscosity and improving blood flow.
Improves blood flow in the ischemic areas of the brain, increasing their oxygenation intensifies glucose metabolism in primary ischemic brain regions. As a result of improved performance memory and restores the metabolic processes in the nervous tissue, which contributes to the full functioning of its cells.
Pharmacokinetics
Absorption and distribution
After taking the drug orally Pyritinol rapidly absorbed from the gastrointestinal tract. Bioavailability is 85% on average (76–93%). After taking the drug orally at a dose of 100 mg C max Pyritinol plasma achieved in 30–60 min.
Plasma protein binding is 20–40%. Pyritinol and its metabolites penetrate the BBB, metabolites accumulate predominantly in the gray matter of the brain. Repeated dose accumulation is observed.
Metabolism and excretion
Pyritinol rapidly biotransformed to form the next major metabolites: 2-methyl–3-hydroxy–4-hydroxymethyl–5-methyl-mercapto-methyl-pyridine and 2-methyl–3-hydroxy–4-hydroxymethyl–5-methyl-sulfonyl-methyl-pyridine. Conjugated metabolites are excreted primarily by the kidneys. The total urinary excretion within 24 h of 72.4–74.2%, with most of the dose was excreted within the first 4 h after administration. Through the intestine displayed only 5%. T 1/2 is about 2.5 hours
Pharmacokinetics in special clinical situations
If the kidney function toxic concentrations are not achieved.
Encephabol (Pyritinol) Dosage
Dosing regimen set individually, depending on the severity of the condition and the effectiveness of therapy.
For the average adult dose is 600 mg/day (2 tabs., Or 10 ml of the suspension 3 times/day).
Newborn Encephabol prescribed with 3 days after birth, 20 mg (1 ml suspension) per day during the month, the drug should be given in the morning. Children aged 2 months to increase the dose of 20 mg (1 mL) each week as long as the daily dose not reach 100 mg (5 ml of suspension).
Children aged 1 to 7 years is prescribed in a daily dose of 50 mg to 300 mg depending on the indication (2.5–5 ml suspension for 1–3 times/day).
For children older than 7 years of daily dose ranges from 50 mg to 600 mg (for 2.5–10 or 1–2 ml of the suspension tab. 1–3 times/day).
Should take the drug during or after meals. Sleep disturbances last daily dose should not be taken in the evening or at night. Note that in 1 teaspoon - 5 ml of suspension.
The duration of treatment depends on the clinical picture of the disease. In acute conditions and appointment of the drug in high doses noticeable therapeutic effect is achieved within a few hours or days.
In chronic diseases (including the effects of traumatic brain injury or dementia) conspicuous therapeutic success achieved after 2–4 weeks of treatment. Optimal and sustainable effect is usually 6–12 weeks. Duration of treatment for chronic diseases should be at least 8 weeks.
In infants at high risk for perinatal pathology average duration of treatment is 6 months, with 3 months you should check whether the indications for further treatment.
Encephabol (Pyritinol) Overdose
Symptoms: increased side effects.
Treatment: gastric lavage, the appointment of activated charcoal. If necessary, symptomatic therapy.
Encephabol (Pyritinol) Drug Interactions
With simultaneous application Encephabol can potentiate the side effects of penicillamine, sulfasalazine, gold and drugs.
Clinically significant interaction Encephabol with other drugs is not established.
Encephabol (Pyritinol) at Pregnancy and lactation
If necessary, use during pregnancy or Encephabol lactation (breastfeeding) should be related to the anticipated benefit to the mother and the potential risk to the fetus or infant.
Pyritinol crosses the placental barrier in small amounts excreted in breast milk.
In experimental studies have established the presence of a teratogenic or embryotoxic effect Pyritinol.
Encephabol (Pyritinol) Side effects
From the digestive system: nausea, vomiting, diarrhea, rarely - loss of appetite, changes in taste sensitivity, abnormal liver function (increase in transaminases, cholestasis).
CNS: possible sleep disorders, rarely - increased irritability, headache, dizziness, fatigue.
Other: allergic reactions of varying severity, usually manifested as a rash on the skin or mucous membranes, itching, fever.
Using the drug on the testimony at the recommended doses development of side effects is unlikely.
Encephabol (Pyritinol) Indications
Symptomatic treatment of dementia syndrome (including primary degenerative dementia, vascular dementia, and mixed forms), accompanied by impaired memory, thinking, ability to concentrate, fatigue, lack of motivation and intentions, affective disorders;
Primary degenerative dementia, vascular dementia, and mixed forms;
Symptomatic treatment of chronic disorders of mental capacity;
Traumatic encephalopathy;
Cerebral arteriosclerosis;
The consequences of encephalitis;
Mental retardation;
Cerebroasthenic syndrome in children;
Encephalopathy in children.
Encephabol (Pyritinol) Contraindications
Absolute contraindications
Hypersensitivity to Pyritinol.
Relative contraindications
Kidney disease in history;
Expressed human liver;
Pronounced changes in peripheral blood;
Acute autoimmune diseases (including systemic lupus erythematosus);
Myasthenia gravis;
Pemphigus.
Encephabol (Pyritinol) Cautions
In patients with rheumatoid arthritis and other chronic diseases of the joints occurs hypersensitivity to compounds which include the SH-group, including to Pyritinol. These patients have a high risk of hypersensitivity reactions, immunopathological reactions, as well as violations of taste sensitivity and liver function. During the treatment of this category of patients requires systematic monitoring of common blood, urine, liver function, immunological parameters.
Suspension should not be administered to patients with Encephabol fructose intolerance, as the substance is formulated Sorbolo.
Hypersensitivity reactions to the drug may occur in patients with hypersensitivity to D-penicillamine, as the latter is similar to the chemical structure Pyritinol (thiol groups).
Use in Pediatrics
Not recommended to prescribe a drug in the evening and at night, children with increased excitability.
Effects on ability to drive vehicles and management mechanisms
When using Encephabol indicated, as a rule, there are no restrictions for those activities that require attention, rapid psychomotor reactions. However, given the likelihood of individual differences in response of individual patients to the drug at the beginning of treatment and dose increase should be considered the possibility of breaking the speed of psychomotor reactions.
Encephabol (Pyritinol) Reviews
Kate, 37 years, Encephabol - Improves memory, clears headaches, soothes.It nootropic medicine. Encephabol well tolerated, improves memory and its concentration, motor skills, the child becomes calmer, reduced or completely pass headaches.
Encephabol prescribed for condition after stroke, in anxiety disorders, with fatigue encephabol well appointed.
The price of this drug to 400 rubles, but we were given free encephabol as son undergoing rehabilitation at a rehabilitation center.
Encephabol happens both in tablets, suspensions and the son encephabol discharged tablets.
But do not take not a solution, it helps to develop a child, he became calmer, and less head aches, not crazy.
Nadya, 31 years, My daughter was prescribed Encephabol due to speech delay. At the age of 2 g. 7 months. was about 10 simple words. Pills month dose - 2.5 ml x 2 times per day. A little over a month since the beginning of reception of a preparation and daughter clear progress. Surprising every day new words, although some of them are hard to recognize, but because until then refused to speak at all. I am pleased!