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

active substance: diclofenac sodium in terms of 100% substance -100 mg; auxiliary substances: podipress LCEE [lactose monohydrate 94,7-98,3%, povidone 3-4%], hypromellose (hydroxypropylmethylcellulose), microcrystalline cellulose, magnesium stearate, silicon dioxide colloid (Aerosil 200), stearic acid.

Sheath composition: hypromellose (hydroxypropylmethylcellulose), macrogol (polyethylene glycol 6000), glycerol (glycerin), talc, titanium dioxide, iron oxide red dye.

Description:The tablets covered with a film membrane of light brown or pinkish-brown color, round, biconcave. Roughness is allowed. At the break of a white tablet with a creamy or yellowish hue of color.

Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug (NSAID).

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, antipyretic and antiplatelet effect. By indiscriminately inhibiting cycloxygenases 1 and 2, it disrupts the metabolism of arachidonic acid, reduces the amount of prostaglandins (Pg) in the inflammatory focus, suppresses the exudative and proliferative phases of inflammation.

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 joint condition.

With injuries, in the postoperative period diclofenac reduces pain and inflammatory swelling.

Pharmacokinetics:Absorption is fast and complete, food slows down the absorption rate. Concentration in plasma: is in linear dependence 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 respecting the recommended interval between doses. IB As a result of sustained release of the active substance, the maximum concentration in the plasma is lower than that obtained when the short-acting drug is administered; however, it remains high for a long time after administration. The maximum concentration is 0.5-1 μg / ml, the time to reach the maximum concentration is 5 hours after taking 100 mg of the prolonged-action tablet. Bioavailability - 50%. 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 remain higher for another 12 hours).

Metabolism: 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 isoenzyme CYP2C9 also participates in the metabolism of dick-lofenac. The pharmacological activity of metabolites is lower than that of diclofenac.

Systemic clearance is 260 ml / min. Half-life 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 dysfunction, 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 liver cirrhosis, pharmacokinetic parameters are the same as in patients without liver disease.

Indications:

Inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid arthritis, psoriatic arthritis, juvenile chronic arthritis, ankylosing spondylitis (Bekhterev's disease); gouty arthritis (in case of an acute attack of gout, quick-acting dosage forms are preferred), rheumatic soft tissue damage, osteoarthritis of peripheral joints and spine, including with radicular syndrome, tendovaginitis, bursitis.

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

Pain syndrome of mild or moderate severity: lumbago, sciatica, neuralgia, myalgia; posttraumatic pain syndrome, accompanied by inflammation, postoperative pain, headache, migraine, toothache, algodismenorea, adnexitis, proctitis. In the complex therapy of infectious and inflammatory diseases of the ENT organs with severe pain syndrome (pharyngitis, tonsillitis, otitis).

Contraindications:

- hypersensitivity to the active substance (including other NSAIDs) or excipients;

- 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 aortocoronary shunting;

- III trimester of pregnancy, lactation period;

- Decompensated heart failure;

- disorders of hematopoiesis, hemostasis disorders (including hemophilia);

- severe hepatic impairment or active liver disease;

- marked renal failure (creatinine clearance less than 30 ml / min), progressive kidney disease, confirmed hyperkalemia;

- children's age till 18 years;

- hereditary lactose intolerance, impaired absorption of glucose-galactose, I deficiency of lactase.

Carefully:

Anemia, bronchial asthma, cerebrovascular disease, ischemic heart disease, chronic heart failure, arterial hypertension, peripheral arterial disease, edematous syndrome, hepatic and renal insufficiency (creatinine clearance 30-60 ml / min), dyslipidemia / hyperlipidemia, diabetes, smoking, inflammatory bowel disease, conditions after extensive surgical interventions, induced porphyria, diverticulitis, systemic connective tissue diseases, pregnancy I-II trimester.

Anamnestic data on the development of gastrointestinal ulcer,the presence of Helicobacter pylori infection, old age, long-term use of NSAIDs, alcoholism, severe physical illnesses.

Simultaneous reception of glucocorticosteroids (for example, prednisolone), anticoagulants (for example, warfarin), antiplatelet agents (for example, acetylsalicylic acid, clopidogrel), 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-100 mg once a day. With algodismenorrhea and migraine attacks - up to 200 mg / day for no more than 1-2 days. If you take 100 mg of prolonged action tablets, if you need to increase the daily dose to 150 mg / day, you can additionally take 1 regular tablet (50 mg). The maximum daily dose is 150 mg.

Side effects:

Often - 1-10 %; sometimes - 0,1-1 %; 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; rarely - gastritis, proctitis,bleeding from the gastrointestinal tract (vomiting with blood, melena, diarrhea with an admixture of blood), gastrointestinal ulcers (with or without bleeding or perforation), hepatitis, jaundice, dysfunction of the liver; very rarely - stomatitis, glossitis, esophagitis, nonspecific hemorrhagic colitis, exacerbation of ulcerative colitis or Crohn's disease, constipation, pancreatitis, fulminant hepatitis.

From the nervous system: often - headache, dizziness; rarely drowsiness;

very rarely - a violation of sensitivity (including paresthesia), memory disorders, tremors, convulsions, anxiety, cerebrovascular disorders, aseptic meningitis, disorientation, depression, insomnia, nightmares, irritability, mental disorders.

From the sense organs: 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: anaphylactic / anaphylactoid reactions, including marked reduction in blood pressure and shock; very rarely - angioedema (including face).

From the cardiovascular system: very rarely - palpitations, chest pain, increased blood pressure, vasculitis, heart failure, myocardial infarction. From the respiratory system: rarely - exacerbation of bronchial asthma (including dyspnea); very rarely - pneumonitis.

From 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.

Overdose:

Symptoms: vomiting, bleeding from the gastrointestinal tract, epigastric pain, diarrhea, dizziness, tinnitus, convulsions, increased blood pressure (BP), respiratory depression, with a significant overdose - acute renal failure, hepatotoxic effect.

Treatment: gastric lavage, the introduction of activated charcoal, symptomatic therapy aimed at eliminating the increase in blood pressure, impaired renal function, seizures, gastrointestinal irritation, respiratory depression.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, the risk of hyperkalemia increases, against the background of anticoagulants, thrombolytic agents (alteplase, streptokin-for, urokinase) - the risk of bleeding (more often from the gastrointestinal tract). Reduces the effects of hypotensive and hypnotics.

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. Paracetamol increases the risk of developing nephrotoxic effects of diclofenac. Reduces the effect of hypoglycemic drugs.

Cefamandol, cefaperazone, 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 the tubular secretion, increase the concentration in the plasma of diclofenac, thereby increasing its toxicity.

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

Special instructions:

To quickly achieve the desired therapeutic effect take 30 minutes before meals. In other cases, take before, during or after eating, without chewing, squeezed with enough water.

Because of the important role of prostaglandins in the maintenance of renal blood flow should be exercised, 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 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.

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. It is necessary to refrain from engaging in potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions. Patients taking the drug should refrain from drinking alcohol.

Form release / dosage:

Tablets of prolonged action, film-coated, 100 mg.

Packaging:

For 10 tablets in a planar cell package.

1, 2 or 3 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:3 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N002242 / 01

Date of registration:16.05.2008

The owner of the registration certificate:AKRIKHIN HFK, JSC AKRIKHIN HFK, JSC Russia

Manufacturer: & nbsp

AKRIKHIN HFK, JSC Russia

Information update date: & nbsp04.03.2016

Illustrated instructions

Instructions

Diclofenac retard-Akrihin (Diclofenac retard-Akrihin)