Neurodiclovit

Pharmacological properties

neurodiclovitis is a combination of diclofenac and neurotropic vitamins B1, B6 and B12. like other NSAIDs, diclofenac inhibits the enzyme cog, which converts arachidonic acid into prostaglandins. diclofenac also inhibits the enzyme lipoxygenase. analgesic, anti-inflammatory and antipyretic effects of diclofenac due to inhibition of prostaglandin synthesis.

B vitamins act as coenzymes in the metabolism, including neurology, which positively affects the analgesic effect of diclofenac sodium.

Pharmacokinetics After oral administration, diclofenac is well and completely absorbed from the digestive tract. Bioavailability is independent of food intake. C_max in blood plasma is achieved 1–2 hours after ingestion (on an empty stomach faster than after eating). The vitamins contained in the drug are absorbed in the intestine due to active and passive mechanisms. Distribution and excretion are similar to vitamins that are ingested with food. After oral administration of diclofenac in blood plasma, half the concentration of the drug observed after parenteral administration of the same dose is detected. The therapeutic plasma concentration is about 0.7–2.0 mg / L. Almost 99% of diclofenac binds to plasma proteins, mainly with albumin.

About 60% of the dose taken is excreted by the kidneys in the form of active metabolites, 1% of diclofenac is excreted unchanged. About 30% of the dose is excreted in the form of metabolites through bile, with feces. T_½ diclofenac from blood plasma is about 2 hours. The total systemic clearance of diclofenac from blood plasma is about 250 ml / min.

Impaired renal function does not cause accumulation of the active substance due to increased biliary excretion. Absorption, metabolism and excretion of the drug are not dependent on age.

Indications

Inflammatory and degenerative forms of rheumatic diseases:

• chronic polyarthritis;
• ankylosing spondylitis (ankylosing spondylitis);
• arthrosis;
• spondylitis;
• acute gouty arthritis;
• extraarticular rheumatism of soft tissues;
• neuritis and neuralgia, such as cervical syndrome, lumbago, sciatica.

Application

Capsules should be swallowed whole with a sufficient amount of liquid during meals.

Depending on the severity of the disease, the recommended dose is 1-3 capsules per day, which is equivalent to 50-150 mg of diclofenac, respectively.

Adults For initial therapy, the dose is 2-3 capsules per day. Maintenance dose - 1 capsule 1-2 times a day. The maximum daily dose should not exceed 3 capsules.

Children over the age of 14. The maximum daily dose is 1 capsule 2 times a day.

The duration of treatment is determined by the doctor.

Elderly patients. Although the pharmacokinetics of diclofenac does not depend on age, elderly patients should be selected with caution.

Contraindications

• Hypersensitivity to the components of the drug; stomach ulcer or duodenal ulcer; porphyria, hemorrhagic diathesis, impaired blood formation; Crohns disease, ulcerative colitis; severe heart failure. severe renal and hepatic insufficiency; gastrointestinal bleeding or perforation; erythremia, erythrocytosis, thromboembolism; allergic diseases.

The drug is contraindicated in patients in whom asthma attacks, skin reactions or acute rhinitis are provoked by the use of acetylsalicylic acid or other drugs that inhibit the synthesis of prostaglandins.

Side effects

From the side of the cardiovascular system: heart failure, ag, edema, tachycardia, palpitations, chest pain, myocardial infarction, vasculitis.

On the part of the blood: impaired blood formation (leukopenia, thrombocytopenia, aplastic anemia, panmyelopathy, purpura, agranulocytosis, hemolytic anemia).

From the nervous system: headache, nausea, drowsiness, convulsions, dizziness, paresthesia, memory impairment, anxiety, tremor, aseptic meningitis, taste disturbance, cerebrovascular accident, impaired sensation when touched.

Visual impairment: visual impairment (blurred image, double vision).

Hearing impairment: tinnitus, hearing impairment.

From the gastrointestinal tract: epigastric pain, anorexia, hiccups, nausea, indigestion, gastrointestinal bleeding, gastrointestinal ulcers, accompanied by severe bleeding, perforation and anemia, vomiting, diarrhea, dyspepsia, flatulence, gastritis, colitis (including hemorrhagic colitis and exacerbation of ulcerative colitis or Crohn’s disease), constipation, stomatitis, glossitis, disorders of the esophagus, increased acidity of gastric juice, diaphragm-like intestinal strictures, pancreatitis.

On the part of the kidneys and urinary tract: renal failure, nephrotic syndrome, hematuria, acute renal failure, interstitial nephritis, papillary necrosis, proteinuria.

From the skin and subcutaneous tissues: rash, redness, itching, alopecia, various types of erythema, exfoliative dermatitis, photosensitivity.

On the part of the immune system: allergic reactions, such as bronchospasm, urticaria, anaphylactic / anaphylactoid reactions, Stevens-Johnson syndrome, Lyell syndrome, angioedema.

From the hepatobiliary system: hepatitis, including fulminant hepatitis, jaundice, increased levels of transaminases, rarely acute.

Mental disorders: insomnia, a state of excessive agitation, irritability, disorientation, depression, nightmares, psychotic disorders, malaise.

Common disorders: sodium and water retention in the body, peripheral edema, increased sweating, asthma, pneumonitis.

special instructions

The risk of side effects can be reduced by applying the minimum effective dose for the short time necessary to control the symptom.

Caution should be used in patients with asthma, hay fever, swelling of the nasal mucosa (nasal polyps) or chronic infectious diseases of the respiratory tract.

Patients with a history of blood pressure and / or heart failure should require proper monitoring and consultation, as fluid retention and edema have been reported in the treatment of NSAIDs.

Patients with insufficiently controlled hypertension, heart failure, a history of IHD, peripheral arterial vascular and / or cerebrovascular diseases are prescribed diclofenac after a thorough evaluation. Similar factors should also be considered before taking the drug if the patient is prone to cardiovascular diseases (eg, hypertension, hyperlipidemia, diabetes mellitus, smoking).

Clinical studies and epidemiological data show that the use of diclofenac, especially at high doses (150 mg / day) and over a long period, may be accompanied by a slight increase in the risk of arterial thrombotic complications (myocardial infarction or attack).

During long-term treatment with Neurodiclovitis, it is recommended to monitor peripheral blood counts, liver and kidney function.

Patients with a history of gastric and duodenal ulcer or history of dyspeptic symptoms, with liver, kidney, heart failure, or hypertension require careful medical supervision.

All NSAIDs are characterized by gastrointestinal ulcers, bleeding and perforation (sometimes fatal), which can be noted during the treatment period, against the background of warning symptoms, or in their absence, or in the presence of serious gastrointestinal phenomena in history.In general, such phenomena are most dangerous for elderly patients. In some cases, when patients using diclofenac develop these complications, the drug should be discontinued.

In connection with the use of NSAIDs, including diclofenac, severe, even fatal skin reactions, including exfoliative dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis, have been very rarely reported. A high risk of these reactions was detected at the beginning of therapy, and the development of these reactions is noted in most cases in the first month of treatment. The drug should be discontinued at the first manifestations of skin rash and ulcers of the mucous membrane or any other manifestations of hypersensitivity.

Due to its pharmacodynamic properties, diclofenac can mask the symptoms characteristic of infectious and inflammatory diseases.

With the introduction of vitamin B₁₂ the clinical picture, as well as laboratory tests for funicular myelosis or pernicious anemia, may lose their specificity.

Drinking alcohol and black tea reduces the absorption of thiamine. Drinking sulfite-containing beverages (such as wine) increases the degradation of thiamine.

Patients with neoplasms, with the exception of cases accompanied by megaloblastic anemia and vitamin B deficiency₁₂should not use the drug.

The drug is not used for angina pectoris.

The ability to influence the reaction rate when driving vehicles or working with mechanisms. Although a negative effect on the ability to drive vehicles and work with mechanisms has not been identified, it cannot be ruled out that reactivity may deteriorate due to the undesirable effect of diclofenac on the central nervous system (dizziness, fatigue).

Use during pregnancy and lactation. Due to the lack of clinical data, the simultaneous use of vitamins B₁, AT₆ and B₁₂ not recommended during pregnancy or lactation.

Children. Not recommended for children under 14 years of age.

Interactions

The combined appointment of neurodiclovitis and other drugs can cause an increase or decrease in effectiveness:

increase:

• plasma lithium and digoxin levels;
• the risk of gastrointestinal bleeding with concomitant glucocorticoid therapy;
• the severity of side effects of other NSAIDs;
• the effectiveness of potassium-sparing diuretics (potassium level control);
• the effectiveness of drugs that inhibit platelet aggregation;
• level and toxicity of methotrexate. NSAIDs should be avoided less than 24 hours before or after treatment with methotrexate;

decrease:

• the effectiveness of diclofenac with furosemide and other loop diuretics;
• the effectiveness of diclofenac antihypertensive drugs;
• plasma concentrations of diclofenac and acetylsalicylic acid;
• absorption of vitamin B₁₂ when combined with colchicine, PAS, neomycin and antidiabetic agents such as biguanidine.

Concomitant use with levodopa is contraindicated, since vitamin B₆ may reduce the severity of the antiparkinsonian effect of levodopa.

Like other NSAIDs, when used with diuretics or antihypertensive drugs (for example, β-adrenergic blockers and calcium channel blockers, ACE inhibitors) can reduce their antihypertensive effect. Therefore, a combination of such drugs should be prescribed with caution, and patients (especially the elderly) should periodically monitor blood pressure. Patients should consume enough water, and at the beginning and after completion of concomitant therapy, renal function should be periodically monitored, in particular when diuretics and ACE inhibitors are used due to the increased risk of nephrotoxicity.The simultaneous use of systemic NSAIDs and selective serotonin reuptake inhibitors can increase the risk of gastrointestinal bleeding.

The simultaneous use of diclofenac and antidiabetic drugs is possible, while the effectiveness of the latter does not change. However, there are separate reports of the development in such cases of both hypoglycemia and hyperglycemia, which necessitated a change in the dose of sugar-lowering drugs during the use of diclofenac. For this reason, it is recommended that blood glucose levels be monitored during therapy. The simultaneous use of diclofenac and colestipol or colestyramine reduces the absorption of diclofenac by approximately 30 and 60%, respectively. Drugs should be taken at intervals of several hours. Enzyme stimulating agents, such as rifampicin, carbamazepine, phenytoin, St. Johns wort (Hypericum perforatum) and others, are theoretically capable of reducing the concentration of diclofenac in blood plasma. The effect of NSAIDs on the synthesis of prostaglandins in the kidneys may enhance cyclosporin nephrotoxicity. There are separate reports of the development of seizures in patients receiving both quinolone derivatives and NSAIDs.

The action of thiamine is inactivated by 5-fluorouracil, since the latter competitively inhibits thiamine phosphorylation to thiamine pyrophosphate.

Antacids reduce the absorption of thiamine. Loop diuretics, such as furosemide, inhibiting tubular reabsorption, with prolonged therapy can cause increased thiamine excretion and, thus, reduce thiamine levels.

Concomitant use with pyridoxine antagonists (e.g. isoniazid, hydralazine, penicillamine or cycloserine), oral contraceptives may increase the need for vitamin B₆.

Overdose

Symptoms of diclofenac overdose and intoxication - an increase in the frequency of side effects from the gastrointestinal tract and central nervous system. symptomatic therapy.

In the case of severe diclofenac poisoning, the development of acute renal failure and liver damage are possible.

Vitamin B₁: has a wide therapeutic range. After oral administration, no symptoms were detected. When taking very high doses (10 g), a curariform effect is noted, suppressing the conduction of nerve impulses.

Vitamin B₆: exhibits very low toxicity. Long-term use (more than 6-12 months) in doses of 50 mg of vitamin B₆ daily may lead to peripheral sensory neuropathy. Excessive Vitamin B Use₆ in doses of 1 g / day for several months can lead to neurotoxic effects. Neuropathies with ataxia and sensitivity disorders, cerebral seizures with changes in the EEG, as well as in some cases hypochromic anemia and seborrheic dermatitis were described after administration of 2 g / day.

Vitamin B₁₂: After parenteral administration (in rare cases, after oral administration), allergic reactions, eczematous skin disorders and a benign form of acne were observed above the recommended doses. With prolonged use in high doses, a violation of the activity of liver enzymes, pain in the heart, hypercoagulation is possible.

Storage conditions

In a dry, dark place at temperatures up to 25 ° C.