Diclofenac has anti-inflammatory, analgesic, antipyretic and antiplatelet effect. Non-selectively inhibiting cyclooxygenase 1 and 2, it violates the metabolism of arachidonic testosterone cypionate reviews acid, reduces the amount of prostaglandins in inflammation. In rheumatic diseases inflammatory and analgesic effect of diclofenac contributes to a significant reduction in the severity of pain, morning stiffness, swelling of the joints, which improves the functional condition of the joint. When trauma, postoperative diclofenac reduces pain and inflammatory edema.
Thiamine (vitamin B 1 in the human body as a result of phosphorylation converted into kokarboksilazu which is a coenzyme of many enzyme reactions. Vitamin B1 plays an important role in carbohydrate, protein and fat metabolism . Actively involved in the processes of neural excitation in the synapses.
pyridoxine (vitamin B 6 ) is necessary for normal functioning of the central and peripheral nervous system. The phosphorylated form is a coenzyme in the metabolism of amino acids (decarboxylation, transamination, etc.). It acts as a coenzyme important enzymes active in nerve tissues involved in the biosynthesis of many neurotransmitters -. such as dopamine, serotonin, noradrenelin, adrenaline, histamine and GABA.
cyanocobalamin (vitamin B 12 ) is necessary for normal hematopoiesis and maturation of red blood cells and is also involved in a number of biochemical reactions, life support the body – in the transfer of methyl groups in the synthesis of nucleic acid, protein, amino acid metabolism, carbohydrates and lipids. Has a beneficial effect on the processes in the nervous system (the synthesis of nucleic acids and lipid composition of cerebrosides and phospholipids).
Coenzyme form cyanocobalamin – methylcobalamin and adenosyl cobalamin are necessary for the replication and growth of cells.
The combination of B vitamins potentiates the analgesic effect of diclofenac.
Absorption of diclofenac – fast and full, the food slows the absorption rate of 1 – 4 hours and reduces the maximum concentration of 40%. Following oral administration of 50 mg maximum concentration (Cmax ) – 1.4 mg / ml is achieved through -. 2-3 hours Plasma concentration is linearly dependent on the size of the dose administered.
Changes in the pharmacokinetics of diclofenac on the background of multiple doses is not marked, not accumulates.
Bioavailability – 50%. Relationship testosterone cypionate reviews to plasma proteins – more than 99% (most associated with albumin). It penetrates into the synovial fluid; maximum concentration observed in the synovial fluid for 2-4 hours later than in plasma. The half-life of 3-6 hours synovial fluid (active agent concentration in the synovial fluid after 4-6 h after administration is higher than in plasma, and remains higher for a further 12 hours).The relationship of concentration of the drug in liquid sinovilnoy clinical drug efficacy is not clear. Metabolism 50% of the active substance is metabolised during the “first pass” through the liver. Metabolism occurs as a result of single or multiple hydroxylation and conjugation with glucuronic acid. The metabolism of the drug is involved enzyme system P450 CYP2C9. . The pharmacological activity of metabolites is lower than diclofenac
Systemic clearance is 350 ml / min, the volume of – 550 ml / kg. . The half-life of plasma -2 hours 65% of the administered dose is excreted as metabolites by the kidneys; less than 1% is excreted unchanged in the rest of the dose is excreted as metabolites in the bile. In patients with severe renal impairment (creatinine clearance less than 10 mL / min) increases the excretion of metabolites in the bile, thus increasing their concentration in the blood is not observed.
In patients with chronic hepatitis or cirrhosis compensated diclofenac pharmacokinetic parameters are not changed. Diclofenac passes into breast milk.
The vitamins that make up the Neyrodiklovita, are water-soluble, thus eliminating the possibility of their accumulation in the body. Thiamine and pyridoxine are absorbed in the upper small bowel, is metabolized in the liver and excreted by the kidneys (about 8-10% – unchanged). The degree of absorption depends on the dose, an overdose greatly increases the excretion of thiamine, and pyridoxine through the intestines. Absorption of cyanocobalamin depends to a large extent on the presence of intrinsic factor in the body (in the stomach and upper small intestine), in the future delivery of the vitamin in the tissue is determined by the transport protein transcobalamin. After hepatic metabolism cyanocobalamin derived mainly in the bile, the degree of renal excretion is variable – from 6 to 30%.
Indications Pain syndrome with non-rheumatic inflammation of nature
- after injuries, surgical and dental procedures;
- gynecological diseases – primary algomenorrhea, adnexitis;
- inflammatory diseases of the ENT sphere – pharyngitis, tonsillitis, otitis media;
- Inflammatory and degenerative joint and spine diseases (chronic arthritis, rheumatic and rheumatoid arthritis, ankylosing spondylitis, osteoarthritis, spondilartroz);
- Neuritis and neuralgia (cervical syndrome, lumbago, sciatica)
- Acute gouty arthritis;
- Rheumatism of soft tissue.Contraindications:
Hypersensitivity to the drug (including to other. NSAIDs), erosive and ulcerative lesions of the gastrointestinal tract (exacerbation), bleeding from the gastrointestinal tract, intracranial hemorrhage, bronchial asthma combined with polyposis nasal mucosa, violation of hematopoiesis, hemostasis disorders testosterone cypionate reviews (including hemophilia), pregnancy, child, lactation.Precautions
Anemia, asthma, congestive heart failure, hypertension, coronary heart disease, edema syndrome, liver or kidney failure, alcoholism, inflammatory bowel disease, erosive and ulcerative diseases of the gastrointestinal tract without exacerbation, diabetes, a condition after major surgery interventions induced porphyria, old age, diverticular disease, systemic connective tissue diseases.
Dosage and administration
The capsules should be taken orally with meals, with liquid squeezed abundantly liquid. Usually 1 capsule 1-3 times a day.
Adults Neurodiclovit 1 capsule – in the beginning of treatment, 3 times a day as a maintenance dose – 1-2 times a day. The duration of therapy depends on the nature and severity of the disease.
Side effects Gastrointestinal system: more than 1% – abdominal pain, feeling of bloating, diarrhea, nausea, constipation, flatulence, increased levels of “liver” enzymes, peptic ulcer with possible complications (bleeding, perforation), gastrointestinal bleeding; less than 1% – vomiting, jaundice, melena, blood in stool, esophageal lesion, aphthous stomatitis, dryness of mucous membranes (including the mouth), hepatitis (possibly fulminant course), hepatic necrosis, cirrhosis, hepatorenal syndrome, appetite change, pancreatitis ., holetsistopankreatit, colitis Nervous system: more than 1% – headache, dizziness; less than 1% – insomnia, drowsiness, depression, irritability, aseptic meningitis (usually in patients with systemic lupus erythematosus and other connective tissue diseases), cramps, weakness, disorientation, nightmares, feeling of fear. sensory organs: more than 1% – noise in ears; less than 1% – blurred vision, diplopia, disturbance of taste, reversible or irreversible hearing loss, scotoma. Skin:more than 1% – itching, skin rash; less than 1% – alopecia, urticaria, eczema, chronic dermatitis, erythema multiforme exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome), increased photosensitivity, melkotochechnye hemorrhage. Urogenital: more than 1% – delay liquid; less than 1% – nephrotic syndrome, proteinuria, oliguria, hematuria, interstitial nephritis, papillary necrosis, acute renal failure, azotemia. hematopoiesis organs and the immune system: less than 1% – anemia (including haemolytic and aplastic anemia), leukopenia, thrombocytopenia, eosinophilia, agranulocytosis, thrombocytopenic purpura, worsening of infectious processes (including the development of necrotising fasciitis). Respiratory system: less than 1% – cough, bronchospasm, laryngeal edema, pneumonitis. Cardiovascular system: less than 1% – increase in blood pressure; congestive heart failure, arrythmia, chest pain, myocardial infarction. Allergic reaction: less than 1% – anaphylactoid reaction, anaphylactic shock (usually develops rapidly), swelling of the lips and tongue, allergic vasculitis.
Overdose Symptoms: vomiting, dizziness, headache, shortness of breath, dizziness, children -mioklonicheskie cramps, nausea, abdominal pain, bleeding, liver and kidney function. Treatment: gastric lavage, administration of activated charcoal, symptomatic therapy, forced diuresis. Hemodialysis is ineffective.
Interaction with other drugs
increases the plasma concentration of digoxin, methotrexate, lithium and cyclosporine drugs. Reduces the effect of diuretics, potassium-sparing diuretics in the background increases the risk of hyperkalemia; amid anticoagulants, thrombolytic agents (alteplase, streptokinase, urokinase) – risk of bleeding (usually from the gastrointestinal tract). Reduces the effects of antihypertensive and hypnotic drugs.
Increases the likelihood of side effects of other NSAIDs and glucocorticosteroid agents (bleeding in the gastrointestinal tract), the toxicity of methotrexate and cyclosporine nephrotoxicity.
Aspirin reduces the concentration of diclofenac in the blood.
Simultaneous use of testosterone cypionate reviews paracetamol increases the risk of nephrotoxic effects of diclofenac .
Reduces the effect of hypoglycemic agents.
Tsefamandol, ceftazidime, tsefotetan, valproic acid and plikamitsin increase the incidence of gipoprotrombinemii.
Cyclosporine and preparations of gold increases the influence of diclofenac on the synthesis of prostaglandins in the kidneys, which increases renal toxicity.
Concurrent administration of ethanol, colchicine, corticotrophin reuptake inhibitors Hypericum drugs and serotonin increases the risk of bleeding in the gastrointestinal tract.
diclofenac increases the effects of drugs that cause photosensitization.
drugs that block tubular secretion, increase the diclofenac concentration in plasma, thereby increasing its toxicity.
Neurodiclovit reduces levodopa antiparkinsonian efficacy. Ethanol dramatically reduces the absorption of thiamine (blood levels may be reduced by 30%). Long-term treatment with anticonvulsants can lead to a deficiency of thiamine. The use of colchicine and biguanide reduces the absorption of cyanocobalamin.
In the period of drug treatment should be systematic monitoring of peripheral blood, testosterone cypionate reviews liver, kidney, feces study on the presence of blood. Patients receiving the drug should refrain from activities requiring increased attention and rapid mental and motor reactions, the use of alcohol.