Diclofenac - instructions for use, dose, side effects, contraindications

Excipients (core): cellulose microcrystalline - 5.9 mg, lactose monohydrate - 28.5 mg, potato starch - 11.1 mg, povidone (polyvinylpyrrolidone) - 3.5 mg, magnesium stearate - 1.0 mg.

Excipients (shell): cellulose - 2,31 mg, titanium dioxide - 0,962 mg, castor oil - 0,269 mg, polysorbate 80 - 0,886 mg, tropeolin dye - 0 - 0,573 mg.

Description:Tablets are round, biconvex, covered with a coating from orange-yellow to brown color. Two layers are visible on the cross-section: the shell is from orange-yellow to brown and the core is from white to white with a slightly yellowish hue.

Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug.

ATX: & nbsp

S.01.B.C.03 Diclofenac

M.01.A.B.05 Diclofenac

Pharmacodynamics:Non-steroidal anti-inflammatory drug (NSAID), a derivative of phenylacetic acid; has anti-inflammatory, analgesic and antipyretic effect.Indiscriminately inhibiting cycloxygenase 1 and cycloxygenase 2, disrupts the metabolism of arachidonic acid, reduces the amount of prostaglandins in the inflammatory focus. The most effective for inflammatory pain. Like all non-steroidal anti-inflammatory drugs, the drug has an antiaggregant effect. In rheumatic diseases, the anti-inflammatory and analgesic effect of diclofenac significantly reduces the severity of pain, morning stiffness, swelling of the joints, which improves the functional state of the joint. With injuries, in the postoperative period diclofenac reduces pain and inflammatory swelling.

Pharmacokinetics:Absorption is fast and complete, the food slows the absorption rate by 1-4 hours and reduces the maximum concentration (C max) by 40%. After oral administration of 50 mg Cmax -1.5 μg / ml, the time to reach the maximum concentration (TCmax) - 2-3 hours.

The concentration in the plasma is linear depending on the amount of the administered dose. Changes in the pharmacokinetics of diclofenac against the background of repeated administration are not noted. Do not cumulate while observing the recommended interval between meals.

Bioavailability - 50%. The connection with plasma proteins is more than 99% (most of it is associated with albumins).Penetrates into breast milk, synovial fluid; Stax in the synovial fluid is observed 2-4 hours later than in the plasma. The half-life (T1 / 2) of the synovial fluid is 3-6 hours (the concentration of the drug in the synovial fluid 4-6 hours after its administration is higher than in the plasma, and remain higher for another 12 hours).

50% of the drug is metabolized during the "first pass" through the liver. Metabolism occurs as a result of multiple or one-time hydroxylation and conjugation with glucuronic acid. The isozyme CYP2C9 is involved in the metabolism of the drug. Pharmacological activity of metabolites is less than diclofenac.

Systemic clearance is 260 ml / min. T1 / 2 from the plasma - 1-2 hours 60% of the administered dose is excreted as metabolites through the kidneys; less than 1% is unchanged, the rest of the dose is excreted as metabolites with bile.

In patients with severe renal failure (creatinine clearance less than 10 ml / min), the excretion of metabolites with bile is increased, while there is no increase in their concentration in the blood.

In patients with chronic hepatitis or compensated cirrhosis of the liver, the pharmacokinetic parameters do not change. Diclofenac penetrates into breast milk.

Indications:

Symptomatic treatment of inflammatory and degenerative diseases of the musculoskeletal system (rheumatoid arthritis, psoriatic, ankylosing spondylitis, gouty arthritis, rheumatic soft tissue, osteoarthritis peripheral joints and spine, including radicular syndrome, tenosynovitis, bursitis, osteoarthritis deformans, low back pain).

Pain syndrome of mild or moderate severity: neuralgia, myalgia, lumboschialgia, posttraumatic pain syndrome, accompanied by inflammation, postoperative pain, headache, migraine, algodismenorea; inflammatory processes in the small pelvis, incl. adnexitis, proctitis, toothache. In the complex therapy of infectious and inflammatory diseases of the ear, throat, nose with severe pain syndrome (pharyngitis, tonsillitis, otitis). Feverish syndrome with "colds" and flu.

The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use, the progression of the disease is not affected.

Contraindications:

- Hypersensitivity to the active substance or ancillary components.

- Anamnestic data on an attack of bronchial obstruction, rhinitis, urticaria after taking acetylsalicylic acid or other NSAIDs (complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (including anamnesis).

- Erosive-ulcerative changes in the gastric mucosa or duodenum, active gastrointestinal bleeding.

- Inflammatory bowel disease (ulcerative colitis, Crohn's disease).

- The period after aortocoronary bypass surgery.

- III trimester of pregnancy, the period of breastfeeding.

- Decompensated heart failure.

- Cerebrovascular bleeding or other bleeding and hemostasis disorders.

- Severe hepatic impairment or active liver disease.

- Severe renal insufficiency (creatinine clearance less than 30 ml / min); progressive kidney disease, confirmed hyperkalemia.

- Children up to 14 years.

- Hereditary lactose intolerance, insufficiency of lactase or impaired absorption of glucose and galactose.

Carefully:

Anemia, bronchial asthma, cerebrovascular disease, ischemic heart disease, congestive heart failure, arterial hypertension, peripheral arterial disease, edematous syndrome, hepatic or renal insufficiency, history of liver disease, dyslipidemia, hyperlipidemia, diabetes mellitus, smoking, inflammatory bowel disease, significant decrease in the volume of circulating blood (including after extensive surgical interventions), induced porphyria, diverticulitis, systemic joint diseases Ivetlenkii fabric, pregnancy I-II trimester, creatinine clearance 30-60 ml / min.

Anamnestic data on the development of gastrointestinal ulcer (GI), presence of Helicobacter pylori infection, prolonged use of NSAIDs, frequent alcohol consumption, severe somatic diseases.

Elderly patients (including those receiving diuretics, weakened patients and with low body weight). Simultaneous therapy with anticoagulants (for example, warfarin), antiplatelet agents (for example, acetylsalicylic acid, clopidogrel), oral glucocorticosteroids (for example, prednisolone), selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline).

Dosing and Administration:Inside, without chewing, during or after a meal, with a small amount of water. Adults and adolescents with 14 years of age - 50 mg 2-3 times a day. When the optimal therapeutic effect is achieved, the dose is gradually reduced and switched to maintenance treatment at a dose of 50 mg / day. The maximum daily dose is 150 mg.

Side effects:

From the digestive systemepigastric pain, nausea, vomiting, diarrhea, dyspepsia, flatulence, anorexia, increased activity of aminotransferases, gastritis, proctitis, bleeding from the digestive tract (vomiting with blood, melena, diarrhea with blood impurities), gastrointestinal ulcers (with or without bleeding or perforation) , hepatitis, jaundice, dysfunction of the liver, stomatitis, glossitis, damage to the esophagus, diaphragm-like strictures intestine, nonspecific hemorrhagic colitis, exacerbation of ulcerative colitis or Crohn's disease, constipation, pancreatitis, fulminant hepatitis.

From the nervous system: headache, dizziness, drowsiness, sensitivity disorder, incl.paresthesia, memory disorders, tremors, convulsions, anxiety, cerebrovascular disorders, aseptic meningitis, disorientation, depression, insomnia, nightmares, irritability, mental disorders.

From the sense organs: visual impairment (blurred vision, diplopia), hearing impairment, tinnitus, taste disorders, vertigo.

From the urinary system: acute renal failure, hematuria, proteinuria, interstitial nephritis, nephrotic syndrome, papillary necrosis. On the part of the organs of hematopoiesis, thrombocytopenia, leukopenia, hemolytic and aplastic anemia, agranulocytosis.

From the side of the cardiovascular system: palpitation, chest pain, increased blood pressure, vasculitis, heart failure, myocardial infarction.

From the respiratory system: bronchial asthma (including dyspnea), pneumonitis. From the skin: skin rash, urticaria, bullous eruptions, erythema, incl. multiform and Stevens-Johnson syndrome, Lyell's syndrome, exfoliative dermatitis, itching, hair loss, photosensitivity, purpura, incl.allergic. Allergic reactions: anaphylactic / anaphylactoid reactions, including a marked decrease in blood pressure and shock, angioedema (including facial).

Other: edema.

Overdose:Symptoms: vomiting, bleeding from the gastrointestinal tract, epigastric pain, diarrhea, dizziness, tinnitus, lethargy, convulsions, rarely - increased blood pressure, acute renal failure, hepatotoxic effect, respiratory depression, coma. Treatment: gastric lavage, Activated carbon, symptomatic therapy aimed at eliminating the increase in blood pressure, impaired renal function, seizures, irritation of the gastrointestinal tract, respiratory depression. Forced diuresis, hemodialysis are ineffective.

Interaction:

Increases the concentration in the plasma digoxin, methotrexate, lithium and cyclosporine.

Reduces the effect of diuretics, against the background of potassium-sparing diuretics increases the risk of hyperkalemia; on the background of anticoagulants, antiplatelet agents and thrombolytic drugs (alteplase, streptokinase, urokinase) increases the risk of bleeding (more often from the gastrointestinal tract).Reduces the effects of hypotensive and hypnotic drugs. Increases the likelihood of side effects of other non-steroidal anti-inflammatory drugs and glucocorticosteroid agents (bleeding in the gastrointestinal tract), toxicity of methotrexate and nephrotoxicity of cyclosporine.

Acetylsalicylic acid reduces the concentration of diclofenac in the blood. Simultaneous use with paracetamol increases the risk of developing nephrotoxic effects of diclofenac.

Reduces the effect of hypoglycemic agents.

Cefamandol, cefoperazone, cefotetan, valproic acid and plikamycin increase the incidence of hypoprothrombinemia.

Cyclosporine and gold preparations increase the effect of diclofenac on the synthesis of prostaglandins in the kidneys, which increases nephrotoxicity.

Simultaneous use with ethanol, colchicine, corticotropin, selective serotonin reuptake inhibitors and St. John's wort preparations increases the risk of bleeding in the gastrointestinal tract. Diclofenac enhances the effect of drugs that cause photosensitivity.Drugs that block tubular secretion, increase the concentration in the plasma of diclofenac, thereby increasing its toxicity.

Antibacterial drugs from the quinolone group increase the risk of seizures.

Special instructions:

In order to quickly achieve the desired therapeutic effect take 30 minutes before meals. In other cases, take before, during or after a meal unseparating, with enough water.

To reduce the risk of developing adverse events on the part of the gastrointestinal tract, a minimum effective dose should be used with the minimum possible short course.

If the increase in the activity of "liver" transaminases persists or increases during the administration of the drug, if clinical symptoms of hepatotoxicity (including nausea, fatigue, drowsiness, diarrhea, pruritus, jaundice) are noted, treatment should be discontinued.

Because of the important role of prostaglandins in maintaining renal blood flow, care should be taken when assigning to patients with cardiac or renal insufficiency, as well as in the treatment of elderly patients taking diuretics,which for some reason has a decrease in the volume of circulating blood (for example, after extensive surgical intervention). If in such cases appoint diclofenac, recommend as a precautionary measure to monitor kidney function.

In patients with hepatic insufficiency (chronic hepatitis, compensated cirrhosis), the kinetics and metabolism do not differ from similar processes in patients with normal liver function. When performing long-term therapy, it is necessary to monitor liver function, the picture of peripheral blood, the analysis of feces for latent blood.

In connection with the negative effect on fertility, women who want to become pregnant, the drug is not recommended. In patients with infertility (including those undergoing examination) it is recommended to cancel the drug.

Effect on the ability to drive transp. cf. and fur:During the treatment period, it is possible to reduce the speed of mental and motor reactions, so it is necessary to refrain from driving motor vehicles and practicing other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Tablets coated with enteric coating 50 mg.

Packaging:For 10, 20, 30 tablets are placed in a contour mesh box made of a polyvinylchloride film and aluminum foil printed lacquered. 10, 20, 30, 40, 50 or 100 tablets are placed in a polymer container for medicinal products. One container or 1, 2, 3, 4, 5, 6, 8 or 10 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

Storage conditions:Store in a dry, dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:3 years. Do not use the drug after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N002753 / 01

Date of registration:26.05.2008

The owner of the registration certificate:OZONE, LLC OZONE, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Information update date: & nbsp04.03.2016

Illustrated instructions

Instructions

Diclofenac (Diclofenac)