Diclofenac

General characteristics. Structure:

Active agent: sodium diclofenac — 50 mg

Excipients (kernel): cellulose microcrystallic — 5,9 mg, lactoses monohydrate — 28,5 mg, potato starch — 11,1 mg, povidone (polyvinylpirrolidone) — 3,5 mg, magnesium stearate — 1,0 mg.

Excipients (cover): целлацефат — 2,31 mg, titanium dioxide — 0,962 mg, castor oil — 0,269 mg, polysorbate of 80 — 0,886 mg, dye tropeolin - 0 — 0,573 mg.

Pharmacological properties:

Non-steroidal anti-inflammatory drug (NPVP), derivative phenylacetic acid; has antiinflammatory, analgeziruyushchy and febrifugal effect. Not selectively oppressing a tsikpoksigenaza 1 and to a tsikpoksigenaz 2, metabolism of arachidonic acid breaks, reduces amount of prostaglandins in the inflammation center. It is most effective at pains of inflammatory character. As all non-steroidal anti-inflammatory drugs, drug has antiagregantny effect. At rheumatic diseases antiinflammatory and analgeziruyushchy effect of diclofenac promotes considerable reduction of expressiveness of pain, morning constraint, a swelling of joints that improves a functional condition of a joint. At injuries, in the postoperative period diclofenac reduces pain and inflammatory hypostasis. Pharmacokinetics
Absorption — bystry and full, food slows down absorption speed for 1-4 hours and reduces the maximum concentration (Stakh) by 40%. After oral administration of 50 mg Stakh — 1,5 mkg/ml, time of achievement of the maximum concentration (Tstakh) — 2-3 hours. Concentration in plasma is in linear dependence on size of the entered dose. Change of a pharmakokinegika of diclofenac against the background of repeated introduction is not noted. Does not kumulirut at observance of the recommended interval between meals. Bioavailability — 50%. Communication with proteins of plasma — more than 99% (the most part contacts albumine). Gets into breast milk, synovial fluid; Stakh in synovial fluid is observed on 2-4 h later, than in plasma. An elimination half-life (T1/2) from synovial fluid — 3-6 h (concentration of drug in synovial fluid in 4-6 h after its introduction are higher, than in plasma, and remain higher during 12 h). 50% of drug are exposed to metabolism during "the first passing" through a liver. Metabolism results from a repeated or single hydroxylation and a konjyugirovaniye with glucuronic acid. CYP2C9 isoenzyme takes part in metabolism of drug. Pharmacological activity of metabolites is less, than diclofenac.
The system clearance makes 260 ml/min. of T1/2 of plasma — 1-2 h 60% of the entered dose are brought in the form of metabolites through kidneys; less than 1% are removed in not changed look, other part of a dose is removed in the form of metabolites with bile.
At patients with the expressed renal failure (clearance of creatinine less than 10 ml/min.) removal of metabolites increases
with bile, at the same time increase in their concentration in blood is not observed.
At patients with chronic hepatitis or the compensated cirrhosis pharmacokinetic parameters do not change. Diclofenac gets into breast milk.

Indications to use:

Symptomatic treatment of inflammatory and degenerative diseases of a musculoskeletal system (pseudorheumatism, psoriasis, ankylosing spondylitis; gouty arthritis, rheumatic defeat of soft tissues, an osteoarthrosis of peripheral joints and a backbone, including with a radicular syndrome, a tendovaginitis, the bursitis deforming an osteoarthrosis, osteochondrosis). Pain syndrome of weak or moderate expressiveness: neuralgia, a mialgiya, a lumbar ishialgia, the posttraumatic pain syndrome which is followed by an inflammation, postoperative pain, a headache, migraine, альгодисменорея; inflammatory processes in a small basin, including an adnexitis, a proctitis, a dentagra. As a part of complex therapy of infectious and inflammatory diseases of an ear, a throat, a nose with the expressed pain syndrome (pharyngitis, TONSILLITIS, OTITIS). Feverish syndrome at "catarrhal" diseases and flu. Drug is intended for symptomatic therapy, reducing pains and inflammations at the time of use, does not influence progressing of a disease.

Route of administration and doses:

Inside, without chewing, in time or after food, washing down with a small amount of water. To adults and teenagers since 14 years — on 50 mg 2-3 times a day. At achievement of optimum therapeutic effect the dose is gradually reduced and pass to the supporting treatment in a dose 50 mg/days. The maximum daily dose — 150 mg.

Features of use:

For the purpose of bystry achievement of desirable therapeutic effect accept in 30 min. prior to meal. In other cases accept to, in time or after food without chewing, washing down with enough water.
For decrease in risk of development of the undesirable phenomena from a GIT it is necessary to use a minimal effective dose minimum possible short course.
If during administration of drug increase in activity of "hepatic" transaminases remains or increases if clinical symptoms of a hepatotoxic are noted (including nausea, fatigue, drowsiness, diarrhea, a skin itch, jaundice) treatment needs to be stopped. Because of an important role of prostaglandins in maintenance of a renal blood-groove patients should show extra care at appointment with a heart or renal failure, and also at therapy of the elderly patients accepting diuretics and patients at whom for any reason decrease in volume of the circulating blood is observed (for example, after extensive surgical intervention). If in such cases appoint diclofenac, recommend to control function of kidneys as a precautionary measure. At patients with a liver failure (chronic hepatitis, the compensated cirrhosis) the kinetics and metabolism do not differ from similar processes at patients with normal function of a liver. When performing long therapy it is necessary to control function of a liver, a picture of peripheral blood, the analysis a calla on the occult blood. Due to the negative effect on fertility, the women wishing to become pregnant are not recommended to use drug. At patients with infertility (including undergoing inspection) it is recommended to cancel drug.
Influence on ability to driving of motor transport and to control of mechanisms during treatment is possible reduction of speed of mental and motor reactions therefore it is necessary to abstain from driving of motor transport and occupations other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

- From the alimentary system: epigastric pain, nausea, vomiting, diarrhea, dyspepsia, a meteorism, anorexia, increase in activity аминстрансфераз, gastritis, a proctitis, bleeding from a GIT (vomiting with blood, a melena, diarrhea with blood impurity), GIT ulcers (with or without bleeding or perforation), hepatitis, jaundice, an abnormal liver function, stomatitis, a glossitis, injuries of a gullet, diafragmopodobny strictures of intestines, nonspecific hemorrhagic colitis, an exacerbation of ulcer colitis or a disease Krone, a lock, pancreatitis, fulminant hepatitis.
- From a nervous system: headache, dizziness, drowsiness, sensitivity disturbance, including paresthesias, dysmnesias, tremor, spasms, alarm, cerebrovascular disturbances, aseptic meningitis, disorientation, depression, sleeplessness, night "nightmares", irritability, mental disturbances.
- From sense bodys: vision disorder (illegibility of visual perception, diplopia), hearing disorder, sonitus, disturbance of flavoring feelings, вертиго.
- From an urinary system: acute renal failure, hamaturia, proteinuria, intersticial nephrite, nephrotic syndrome, papillary necrosis.
- From bodies of a hemopoiesis: thrombocytopenia, leukopenia, hemolitic and aplastic anemia, agranulocytosis.
- From cardiovascular system: heart consciousness, stethalgia, increase in arterial pressure, vasculitis, heart failure, myocardial infarction.
- From respiratory system: bronchial asthma (including an asthma), a pneumonitis.
- From integuments: skin rash, small tortoiseshell, violent rashes, erythema, including multiformny and Stephens-Johnson's syndrome, Lyell's disease, exfoliative dermatitis, itch, hair loss, photosensitization, purpura, including allergic.
- Allergic reactions: anaphylactic/anaphylactoid reactions, including the expressed lowering of arterial pressure and shock, a Quincke's disease (including persons). Other: hypostases.

Interaction with other medicines:

Increases concentration in plasma of digoxin, a methotrexate, drugs of lithium and cyclosporine.
Reduces effect of diuretics, against the background of kaliysberegayushchy diuretics the risk of a hyperpotassemia amplifies; against the background of anti-coagulants, antiagregant and thrombolytic medicines (an alteplaza, Streptokinasa, an urokinase) increases risk of development of bleedings (more often from digestive tract).
Reduces effects of hypotensive and somnolent medicines.
Increases probability of emergence of side effects of other non-steroidal anti-inflammatory drugs and glucocorticosteroid means (bleedings in digestive tract), toxicity of a methotrexate and nephrotoxicity of cyclosporine. Acetylsalicylic acid reduces concentration of diclofenac in blood. Simultaneous use with paracetamol increases risk of development of nephrotoxic effects of diclofenac. Reduces effect of hypoglycemic means. Tsefamandol, цефопвразон, цефотетан, вальп royevy acid and пликамицин increase the frequency of development of a prothrombinopenia. Cyclosporine and drugs of gold increase influence of diclofenac on synthesis of prostaglandins in kidneys that increases nephrotoxicity. Simultaneous use with ethanol, colchicine, corticotropin, selective serotonin reuptake inhibitors and drugs of the St. John's Wort which is made a hole increases risk of development of bleedings in digestive tract. Diclofenac strengthens effect of the drugs causing a photosensitization.
The drugs blocking canalicular secretion increase concentration in diclofenac plasma, thereby, increasing its toxicity. Antibacterial medicines from group of a hinolon increase risk of development of spasms.

Contraindications:

- Hypersensitivity to active agent or auxiliary components.
- Anamnestic data on an attack of a bronkhoobstruktion, rhinitis, small tortoiseshell after reception of acetylsalicylic acid or other NPVP (a full or incomplete combination of bronchial asthma, the nose recuring a polypose and okolonosovy bosoms and intolerance of acetylsalicylic acid and other NPVP (including in the anamnesis).
- Erosive and ulcer changes mucous stomach or 12-perstny gut, active gastrointestinal bleeding.
- Inflammatory diseases of intestines (ulcer colitis, disease Krone).

- The period after performing aortocoronary shunting.
- III trimester of pregnancy, breastfeeding period.
- Dekompeneyrovanny heart failure.

- Cerebrovascular bleeding or other bleedings and disturbances of a hemostasis.
- The expressed liver failure or an active disease of a liver.
- The expressed renal failure (clearance of creatinine less than 30 ml/min.); the progressing diseases of kidneys, the confirmed hyperpotassemia.
- Children's age up to 14 years.
- Hereditary lactose intolerance, insufficiency of lactase or disturbance of absorption of glucose and galactose.

WITH CARE
Anemia, bronchial asthma, cerebrovascular diseases, coronary heart disease, congestive heart failure, arterial hypertension, diseases of peripheral arteries, edematous syndrome, liver or renal failure, liver diseases in the anamnesis, a dislipidemiya, a lipidemia, a diabetes mellitus, smoking, inflammatory diseases of intestines, considerable decrease in volume of the circulating blood (including after extensive surgical interventions), the induced porphyria, divertikupit, general diseases of connecting fabric, pregnancy the I-II trimester, clearance of creatinine of 30-60 ml/min.
Anamnestic data on development of an ulcer disease of the digestive tract (DT), existence of an infection of Helicobacter pylori, long use of NPVP, frequent alcohol intake, heavy somatopathies.
Elderly patients (including the receiving diuretics weakened patients and with low body weight). Simultaneous therapy by anticoagulants (for example, warfarin), antiagregant (for example, acetylsalicylic acid, клопидогреп), peroral glucocorticosteroids (for example, Prednisolonum), selective serotonin reuptake inhibitors (for example, to tsitalopra, fluoxetine, пароксетин, сертрапин).

Overdose:

Symptoms: vomiting, bleeding from a GIT, epigastric pain, diarrhea, dizziness, a sonitus, a lethargy, spasms, it is rare — increase in the ABP, an acute renal failure, a hepatotoxic action, respiratory depression, a coma.
Treatment: a gastric lavage, absorbent carbon, the symptomatic therapy directed to elimination of increase in arterial pressure, a renal failure, spasms, irritations of digestive tract, respiratory depression. The artificial diuresis, a hemodialysis are ineffective.

Storage conditions:

To store in the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

The tablets covered with a kishechnorastvorimy cover of 50 mg. On 10, 20, 30 tablets place in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished. On 10, 20, 30,40, 50 or 100 tablets place in a container polymeric for medicines. One container or 1, 2, 3, 4, 5, 6, 8 or 10 blister strip packagings together with the application instruction place in a pack from a cardboard.