Neurodiclovit

Active material: Thiamin, Diclofenac, Pyridoxine, Цianokoʙalamin
When ATH: M01AB55
CCF: NSAIDS in combination with b vitamins
ICD-10 codes (testimony): M05, M10, M15, M45, M46, M54.1, M54.3, M54.4, M79, M79.1, M79.2, N70, N94.4, N94.5, R07, R52.0, R52.2
When CSF: 02.11.01
Manufacturer: LANNACHER HEILMITTEL Ges.m.b.H. (Austria)

Pharmaceutical form, composition and packaging

Capsules hard gelatin, size №1, with a corps of pinkish-yellow and Brown cap; contents of capsules – White granular (diclofenac sodium) and pink powder (vitamins).

Excipients: povidone, methacrylic acid and ethyl acrylate copolymer (Eudrajit NE30D), trijetilacetat, talc, Silicone antivspenivajushhij SE2 MS Agent, gelatin, Titanium dioxide (E171), iron oxide red (E172), iron oxide yellow (E172).

10 PC. – blisters (3) – packs cardboard.

Pharmacological action

NSAIDS in combination with b vitamins. Diclofenac has anti-inflammatory, analgesic, Antiplatelet and antipyretic effect. Nyeizbiratyelino glory glory ugnyetaya 1 e 2, violate metabolism arahidonova acid, reduces the amount of prostaglandins in inflammation. Rheumatic diseases, anti-inflammatory and analgesic effect of diclofenac contributes significantly to reduce the severity of pain, morning stiffness, swelling of joints, that improves the functional condition of the joint. For injuries, postoperative diclofenac reduces pain and inflammation swelling.

Thiamin (vitamin B₁) in the human body as a result of processes of phosphorylation turns into kokarboksilazu, which is a coenzyme of many enzyme reactions. Vitamin B₁ plays an important role in uglevonom, protein and fat metabolism. Actively involved in the processes of neural excitation in the synapses.

Pyridoxine (vitamin B₆) necessary for normal functioning of the central and peripheral nervous system. The phosphorylated form is a coenzyme in the metabolism of amino acids (decarboxylation, pereaminirovanie). Acts as a coenzyme important enzymes, active in nerve tissues. Participates in the biosynthesis of many neurotransmitters – such as dopamine, Serotonin, noradrenelin, adrenaline, E histamine GABA.

Цianokoʙalamin (vitamin B₁₂) is necessary for normal blood formation and maturation of red blood cells, and also participates in a number of biochemical reactions, ensure the functioning of the body – in the transfer of methyl groups, in the synthesis of nucleic acids, squirrel, in the metabolism of amino acids, carbohydrates, lipids. Has a beneficial influence on the processes in the nervous system (the synthesis of nucleic acids and lipid composition and mixture of phospholipids). Coenzyme form cyanocobalamin – methylcobalamin and adenozilkobalamin are required for replication and cell growth.

The combination of b vitamins potentiates analgesic effect of diclofenac.

Pharmacokinetics

Diclofenac

Absorption

Diclofenac absorption rapid and complete. Food slows absorption rate on 1-4 h and lowers C_max on 40%. After intake of diclofenac in the dose 50 mg C_max achieved through 2-3 h and is 1.4 ug / ml. Concentration in the plasma is in linear depending on the size of the dose taken. Bioavailability - 50%.

Distribution

Change the pharmacokinetics of diclofenac amid repeated introduction of no, not koumouliruet. Plasma protein binding - more 99% (a large part of the associated albuminami). It penetrates into synovial fluid. C_max in synovial fluid on 2-4 hours later, than in plasma. Diclofenac is excreted in breast milk. V_d – 550 ml / kg.

Metabolism

50% the active substance is metabolizmu during “first pass” through the liver. Metabolism occurs as a result of multiple or single hydroxylation and conjugating with glukuronova acid. In the metabolism of the drug takes part CYP CYP2S9. Pharmacological activity of metabolites below, than diclofenac.

Deduction

T_1/2 of the synovial fluid is 3-6 no. Diclofenac sodium concentration in synovial fluid through 4-6 hours after taking the drug more, than in plasma, and stays exceeding plasma values for 12 no. The relationship of drug concentration in the liquid sinovil'noj with clinical efficacy of the drug is unclear. Systemic clearance is 350 ml / min. T_1/2 from plasma- 2 no. 65% imposed dose excreted in the form of metabolites kidneys, less 1% excreted unchanged, the remainder of the dose appears in the form of metabolites with jelchew.

In patients with renal insufficiency (CC <10 ml / min) increases excretion of metabolites in bile, in so doing, increase their concentration in the blood is not observed.

In patients with chronic hepatitis or compensated cirrhosis diclofenac pharmacokinetic parameters do not change.

Vitamins In₁, IN₆, IN₁₂

Vitamins, included in Nejrodiklovita, are water soluble, which excludes the possibility of their accumulation in the body.

Thiamine and pyridoxine are absorbed in the upper small intestine Division, metabolised in the liver and excreted by the kidneys (about 8-10% – in unchanged form). The intake depends on the dose, overdose greatly increases the excretion of thiamine and pyridoxine through the intestines.

The absorption of radio depends to a large extent on the availability of internal factors in the body (in the stomach and upper small intestine Division), in the future delivery of vitamin in the tissue is determined by the transport protein transkobalaminom. After the metabolism in the liver zianokobalamin write mainly jelchew, degree of excretion by the kidneys is variable – from 6 to 30%.

Testimony

• pain syndrome in inflammation of nerevmaticheskoj nature (after injuries, operational and dental surgeries; gynecological diseases – Primary algomenorrhea, adnexitis; inflammatory diseases of Lor-bodies – pharyngitis, tonsillitis, otitis);
• inflammatory and degenerative diseases of joints and spine (chronic polyarthritis, rheumatic and rheumatoid arthritis, ankiloziruyushtiy spondylitis, osteoarthritis, spondilartroz);
• Neuritis and neuralgia (cervical syndrome, lyumbago, sciatica);
• acute gouty arthritis;
• rheumatic soft tissue.

Dosage regimen

The capsules should be taken orally at the time of delivery, with liquid squeezed more liquid.

Adults Nejrodiklovit appoint 1 capsule 3 times per day at the beginning of treatment, as a maintenance dose – 1-2 times / day. Length of therapy depends on the nature and severity of the disease.

Side effect

From the digestive system: >1% -abdominal pain, bloated feeling, diarrhea, nausea, constipation, flatulence, elevated liver enzymes, peptical ulcers with possible complications (bleeding, perforation), gastrointestinal bleeding; <1% -vomiting, jaundice, ground, the appearance of blood in the stool, the defeat of the esophagus, thrush, dryness of mucous membranes (incl. mouth), hepatitis (Perhaps the lightning-fast course), hepatic necrosis, cirrhosis, hepatorenal syndrome, change in appetite, pancreatitis, holecistopankreatit, colitis.

CNS: >1% – headache, dizziness; <1% – sleep disturbance, drowsiness, depression, irritability, aseptic meningitis (more frequently in patients with systemic lupus erythematosus and other systemic diseases of connective tissue), convulsions, generalized weakness, disorientation, nightmares, the feeling of fear.

From the senses: >1% – noise in ears; <1% – blurred vision, diplopia, taste disturbance, reversible or irreversible hearing impairment, scotoma.

Dermatological reactions: >1% – itching, skin rash; <1% – alopecia, hives, eczema, toxic Dermatitis, erythema multiforme exudative (incl. Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), increased photosensitivity, melkotochechnye hemorrhage.

From the urinary system: >1% – fluid retention; <1% -nephrotic syndrome, proteinuria, oligurija, hematuria, interstitial nephritis, papillary necrosis, acute renal failure, azotemia.

From the hematopoietic system: <1% - Anemia (incl. haemolytic and aplastic anemia), leukopenia, thrombocytopenia, eozinofilija, agranulocytosis, trombotsitopenicheskaya purpura.

The respiratory system: <1% -cough, bronchospasm, laryngeal edema, pneumonitis.

Cardio-vascular system: <1% -raising hell, congestive heart failure, arrythmia, chest pain, myocardial infarction.

Allergic reactions: <1% – anaphylactoid reactions, anaphylactic shock (usually develops rapidly), swelling of the lips and tongue, sensitization vasculitis.

Other: <1% -deterioration of the current infectious processes (incl. development of Necrotizing fasciita).

Contraindications

• erosive and ulcerative lesions of the gastrointestinal tract (exacerbation);
• gastrointestinal bleeding;
• intracranial bleeding;
• bronchial asthma combined with nasal polyposis;
• violation of hematopoiesis;
• Hemostatic disorders (incl. hemophilia);
• pregnancy;
• childhood;
• lactation (breast-feeding);
• hypersensitivity to the drug (incl. to other NSAIDS).

FROM caution should designate product for anemia, asthma, Congestive heart failure, hypertension, CHD, Edema syndrome, hepatic or renal failure, alcoholism, inflammatory bowel diseases, erosivno-yazvennah TRACT diseases in remission, diabetes, condition after extensive surgery, Inductively porfirii, diverticulum, systemic connective tissue diseases, and elderly patients.

Pregnancy and lactation

The drug is contraindicated in pregnancy and lactation (breast-feeding).

Cautions

During drug treatment Nejrodiklovit should conduct systematic monitoring picture peripheral blood, liver function, kidney, study of fecal blood.

Effects on ability to drive vehicles and management mechanisms

Patients, receiving the drug, You must refrain from activities, require greater attention and rapid mental and motor reactions, use of alcohol.

Overdose

Symptoms: vomiting, dizziness, headache, breathlessness, dizziness, children-mioclauniceskie convulsions, nausea, abdominal pain, bleeding, the liver and kidneys.

Treatment: gastric lavage, administration of activated charcoal. Symptomatic therapy, diurez. Hemodialysis maloeffyektivyen.

Drug Interactions

Together with the use of Nejrodiklovit increases concentration in plasma digoxin, methotrexate, drugs lithium and Cyclosporine.

If you are applying to Nejrodiklovit reduces the effect of diuretics, against kalisberegath dioretikov amplified risk giperkaliemii.

While applying Nejrodiklovita and anticoagulants, thrombolytic funds (al′teplaza, streptokinase, urokynaza) increased risk of bleeding (more frequent gastrointestinal bleeding).

If you are applying to Nejrodiklovit reduces the effects of gipotenziveh and sleeping.

Together with the use of Nejrodiklovit increases the likelihood of side effects of other NSAIDS and CORTICOSTEROIDS (gastrointestinal bleeding), the toxicity of methotrexate and Cyclosporine Nephrotoxicity.

Acetylsalicylic acid reduces the concentration of diclofenac in the blood.

Simultaneous use of Nejrodiklovita with paracetamol increases the risk of nefrotoksicskih effects diclofenac.

If you are applying to Nejrodiklovit reduces the effect gipoglikemicakih funds.

Together with the application Nejrodiklovitom cefamandole, cefoperazone, cefotetan, valproic acid and increase the frequency of plikamicin development gipoprotrombinemii.

Ciclosporin and preparations of diclofenac for influence increase gold synthesis of prostaglandins in the kidneys, that increases the risk of Nephrotoxicity.

The simultaneous appointment Nejrodiklovita with ethanol, colchicine, kortikotropinom, serotonin reuptake inhibitors and drugs St. John's wort increases the risk of gastrointestinal bleeding.

Diclofenac enhances the effect of drugs, cause photosensitivity.

Preparations, block tubular secretion, increase concentration in plasma diclofenac, thereby, increasing its toxicity.

Nejrodiklovit reduces protivoparkinsonicheskuju the effectiveness of levodopa.

Ethanol dramatically reduces the absorption of thiamine (blood levels may be reduced by 30%).

Long-term anticonvulsant treatment can lead to deficiency of thiamine.

The use of colchicine and a biguanide reduces induction radio.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored in a dry, protected from light, inaccessible to children at temperature not exceeding 25 ° C. Shelf life – 2 year.