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

Pharmacodynamics:Diclofenac has anti-inflammatory, analgesic and antipyretic effects. Indiscriminately inhibiting cyclooxygenase 1 and 2, disrupts the metabolism of arachidonic acid, reduces the amount of prostaglandins in the inflammatory focus. 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:

With rectal administration, the maximum concentration in the blood plasma - 1.2 μg / ml is created after 40 - 60 minutes and is linear depending on the dose used. Changes in the pharmacokinetics of diclofenac against the background of repeated administration are not noted, do not accumulate.

The connection with plasma proteins is more than 99% (most of it is associated with albumins). Penetrates into the synovial fluid. The maximum concentration in the synovial fluid is observed 2-4 hours later than in the plasma. The half-life of the synovial fluid is 3-6 hours (the concentration of the active substance in the synovial fluid 4-6 hours after the administration of the drug is higher than in the plasma, and remains higher for another 12 hours). The relationship between the concentration of the drug in the synovial fluid and the clinical efficacy of the drug has not been elucidated.

50% of the active substance 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 enzyme system P450 CYP2C9 is involved in the metabolism of the drug. The pharmacological activity of metabolites is lower than that of diclofenac.

The system clearance is 350 ml / min, the volume of distribution is 550 ml / kg. Half-life from the plasma -2 hours 65% of the administered dose is excreted as metabolites by the kidneys; 1% is displayed 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, the pharmacokinetic parameters of diclofenac do not change.

Diclofenac penetrates into breast milk.

Indications:

The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use, the progression of the disease is not affected. Diseases of the musculoskeletal system (rheumatoid arthritis, psoriatic, juvenile chronic arthritis, ankylosing spondylitis, gouty arthritis, rheumatic soft tissue lesions, osteoarthrosis of the peripheral joints of the spine, including radicular syndrome, tendovaginitis, bursitis).Pain syndrome of mild or moderate severity: neuralgia, lumboschialgia, posttraumatic pain syndrome, accompanied by inflammation, postoperative pain, headache, migraine, algodismenorea, adnexitis, toothache.

In the complex therapy of infectious and inflammatory diseases of the ear, throat, nose with severe pain syndrome (pharyngitis, tonsillitis, otitis).

Apply strictly according to the doctor's prescription.

Contraindications:Hypersensitivity (including to other NSAIDs); complete or incomplete combination of bronchial asthma, recurrent polyposis of the nasal mucosa and paranasal sinuses and intolerance to acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (including in the anamnesis); erosive and ulcerative lesions of the gastric mucosa or duodenum, active gastrointestinal bleeding; inflammatory bowel disease (ulcerative colitis, Crohn's disease) in the phase of exacerbation; period after aortocoronal bypass surgery; Decompensated heart failure; severe hepatic impairment or active liver disease; marked renal failure (creatinine clearance less than 30ml / min), progressive kidney disease, confirmed hyperkalemia; violations of hemostasis (including hemophilia), III trimester of pregnancy, lactation period; children age (up to 18 years for suppositories at 100 mg, up to 15 years for suppositories at 50 mg), rectal bleeding, hemorrhoids, trauma or inflammation of the rectum.

Pregnancy and lactation:

The use of diclofenac is contraindicated in the third trimester of pregnancy (possibly suppressing the contractility of the uterus and premature closure of the arterial duct in the fetus), and in the I-II trimester its use is possible only in cases where the expected benefit for the mother exceeds the potential risk to the fetus. The drug is prescribed in the minimum effective dose.

Diclofenac and its decomposition products in minor amounts pass into breast milk. If it is necessary to use the drug in high doses and for a long time, consider stopping breastfeeding.

Dosing and Administration:

Rectally. Before using the suppository it is recommended to empty the intestine. To adults. Suppositories of 100 mg: 1 suppository once a day.When used concomitantly with oral diclofenac forms, it is rational to use a single dose of 100 mg per night (in this case, the evening intake of oral forms of diclofenac is excluded). Adults and children over 15 years. Suppositories of 50 mg: 1 suppository 2 times a day.

The maximum daily dose is 150 mg. Duration of use of the preparation is not more than 7

days.

Side effects:

Frequency of all side effects: often - 1-10%; sometimes - 0,1-1,0%; rarely - 0,01-0,1%, very rarely - less than 0,001%, including individual cases.

From the digestive system: often - epigastric pain, nausea, vomiting, diarrhea, dyspepsia, flatulence, anorexia, increased activity of aminotransferases; rare gastritis, proctitis, bleeding from the digestive tract (vomiting with blood, melena, diarrhea with a trace of blood), gastrointestinal ulcers (with or without bleeding or perforation), hepatitis, jaundice, impaired liver function; very rarely - stomatitis, glossitis, esophagitis, nonspecific hemorrhagic colitis, exacerbation of ulcerative colitis or Crohn's disease, constipation, pancreatitis, fulminant hepatitis, exacerbation of hemorrhoids.

From the nervous system: often - headache, dizziness; rarely - drowsiness; very rarely - a violation of sensitivity (incl.paresthesia), memory disorders, tremors, convulsions, anxiety, cerebrovascular disorders, aseptic mognite, disorientation, depression, insomnia, nightmares, irritability, mental disorders.

From the senses: often - vertigo; very rarely - visual impairment (blurred vision, diplopia), hearing impairment, tinnitus, a violation of taste sensations.

From the urinary system: very rarely - acute renal failure, hematuria, proteinuria, interstitial nephritis, nephrotic syndrome, papillary necrosis.

From the hematopoiesis: very rarely - thrombocytopenia, leukopenia, hemolytic and aplastic anemia, agranulocytosis.

Allergic reactions: rarely anaphylactic / anaphylactoid reactions, including a marked decrease in blood pressure (BP) and shock; very rarely angioedema (including facial).

From the cardiovascular system (SSS): very rarely - palpitations, chest pain, increased blood pressure, vasculitis, heart failure (CH), myocardial infarction.

On the part of the respiratory system: rarely - bronchial asthma (including dyspnea); very rarely - pneumonitis.

On the part of the skin: often - skin rash; rarely - hives; very rarely - bullous eruptions, erythema, incl. multiform and Stevens-Johnson syndrome, Lyell's syndrome, exfoliative dermatitis, itching, hair loss, photosensitivity, purpura, incl. allergic.

Other: rarely - swelling.

Overdose:

Symptoms: vomiting, bleeding from the gastrointestinal tract, epigastric pain, diarrhea, dizziness, tinnitus, lethargy, convulsions, rarely - increased blood pressure (AD), acute renal failure, hepatotoxic effect, respiratory depression, coma.

Treatment: symptomatic therapy aimed at eliminating the increase in blood pressure, violations of kidney function, seizures, irritation of the gastrointestinal tract, respiratory depression; in case of erroneous oral administration of suppositories, gastric lavage is recommended, and activated charcoal is taken. Forced diuresis, hemodialysis are ineffective (due to the significant connection with proteins and intensive metabolism).

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, thrombolytic agents (alteplase, streptokinase, urokinase) - the risk of bleeding (more often from the gastrointestinal tract).

Reduces the effects of hypotensive and hypnotics.

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 administration with ethanol, colchicine, corticotropin and preparations of St. John's wort 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.

Simultaneous use with paracetamol increases the risk of developing nephrotoxic effects of diclofenac.

Increases the likelihood of side effects of other NSAIDs and glucocorticosteroids (gastrointestinal bleeding), toxicity of methotrexate and nephrotoxicity of cyclosporine.

Acetylsalicylic acid reduces the concentration of diclofenac in the blood.

Reduces the effect of hypoglycemic agents.

Special instructions:

Patients taking the drug should refrain from activities that require increased concentration of attention and rapid mental and motor reactions, alcohol consumption. During the treatment, the drug should monitor the pattern of peripheral blood, liver, kidney function, examination of feces for the presence of blood. 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, special care should be taken in appointing patients with cardiac or renal insufficiency, as well as in the treatment of elderly people taking diuretics and patients who for any reason have a decrease in circulating blood volume (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. To reduce the risk of development are undesirable); phenomena from the gastrointestinal tract, the minimum effective dose should be used as little as possible in a short course. Patients taking the drug should refrain from drinking alcohol.

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:

Suppositories rectal 50 mg, 100 mg.

Packaging:5 suppositories per contour cell packaging made of polyvinyl chloride film. 2 contour mesh packages together with instructions for use in a pack of cardboard.

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

Shelf life:

2 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LS-000757

Date of registration:31.08.2010

The owner of the registration certificate:FARMENT FIRM, LLC FARMENT FIRM, LLC Russia

Manufacturer: & nbsp

FARMENT FIRM, LLC Russia

Information update date: & nbsp15.02.2016

Illustrated instructions

Instructions

Diclofenac (Diclofenac)