Diclofenac

Diclofenac – drug with anesthetic, febrifugal and antiinflammatory action.

Form of release and structure

Diclofenac is produced in the following dosage forms:

• The tablets covered with a kishechnorastvorimy cover: orange or orange-yellow color, round, biconvex (in blister strip packagings on 10 pieces, on 1, 2, 3, 5, 10 packagings in a cardboard pack; in blister strip packagings on 20 pieces, on 1-3 packagings in a cardboard pack; in dark glass jars on 30 pieces, after 1 bank in a cardboard pack);
• Solution for intramuscular introduction: transparent, from weak-yellow color to colourless, with a characteristic slight smell of benzyl alcohol (in ampoules on 3 ml, on 5 ampoules in blister strip packagings, on 2 packagings in a cardboard pack);
• Ointment for external use: almost white or white color, with a slight specific smell (in aluminum tubas on 30 g, on 1 tuba in a cardboard pack);
• Gel for external use of 1% or 5%: homogeneous, white with a cream or yellowish shade or white color, with a specific smell (in aluminum tubas on 30 or 50 g, on 1 tuba in a cardboard pack);
• Suppositories rectal: a torpedo-shaped form, white with a cream shade or white color (in blister strip packagings on 5 suppositories, on 2 packagings in a cardboard pack);
• Drops eye 0,1%: transparent or almost transparent solution from light yellow color to colourless (in polymeric bottles droppers on 5 ml, on 1 bottle in a cardboard pack).

Enters into structure of 1 tablet covered with a kishechnorastvorimy cover:

• Active agent: sodium diclofenac – 25 mg;
• Auxiliary components: milk sugar (lactose monohydrate), sucrose (granulated sugar), povidone (polyvinylpirrolidone), potato starch, stearic acid.

Structure of a kishechnorastvorimy cover: целлацефат, liquid paraffin, titanium dioxide, medical castor oil, dye tropeolin O.

For intramuscular introduction is a part of 1 ml of solution:

• Active agent: sodium diclofenac – 25 mg;
• Auxiliary components: a mannitol, propylene glycol, benzyl alcohol, sodium hydroxide, sulfite sodium, water for injections.

For external use is a part of 1 g of ointment:

• Active agent: sodium diclofenac – 10 mg;
• Auxiliary components: poly(ethylene oxide)-400, poly(ethylene oxide)-1500, Dimexidum, 1,2 propylene glycol.

For external use is a part of 1 g of gel:

• Active agent: sodium diclofenac – 10 or 50 mg;
• Auxiliary components: the rectified ethanol, propylene glycol, carbomer (карбопол), methylparahydroxybenzoate, троламин (trietanolamine), lavender oil, the purified water.

Is a part of 1 suppository:

• Active agent: sodium diclofenac – 100 mg;
• Auxiliary component: solid fat.

Eye is a part of 1 ml of drops:

• Active agent: sodium diclofenac – 1 mg;
• Auxiliary components: Acidum hydrochloricum (1M solution), глицерилрицинолеат a macrogoal (the polyethoxylated castor oil), dinatrium эдетат a dihydrate, трометамол, chloride a benzalkoniya, Mannitolum, the purified water.

Indications to use

Diclofenac does not render on progressing of a disease of influence, it is intended for symptomatic therapy, reduction of an inflammation and expressiveness of a pain syndrome.

Diclofenac in the form of tablets and suppositories is appointed at the following diseases / states:

• Pain syndrome at oncological diseases, tooth and head (including migraine) pain, an ischialgia, a lumbago, radiculitis, an ossalgiya, a mialgiya, neuralgia, an arthralgia, and also the postoperative and posttraumatic pain syndrome which is followed by an inflammation;
• Musculoskeletal system diseases (degenerative and inflammatory), including an ankylosing spondylitis (Bekhterev's disease), psoriasis, rhematoid, juvenile chronic arthritis, gouty arthritis, an osteoarthrosis, a tendovaginitis, a bursitis;
• Inflammatory processes in a small basin, including an adnexitis;
• Algodismenorey;
• The infectious and inflammatory diseases of ENT organs which are followed by the expressed pain syndrome including tonsillitis, pharyngitis and otitis (as a part of complex treatment).

Also suppositories apply at the feverish syndrome arising at flu and "catarrhal" diseases.

Drug in the form of solution for intramuscular introduction is appointed for short treatment of pains of various genesis of moderate intensity, including the following indications:

• Musculoskeletal system diseases (psoriasis, juvenile chronic arthritis, the pseudorheumatism ankylosing a spondylarthritis, rheumatic defeat of soft tissues, gouty arthritis, an osteoarthrosis of a backbone and peripheral joints including with a radicular syndrome);
• Algodismenorey, the inflammatory processes proceeding in bodies of a small pelvis including an adnexitis;
• Sciatica, lumbago, neuralgia;
• Postoperative pains;
• The posttraumatic pain syndrome which is followed by an inflammation.

Outwardly Diclofenac in the form of ointment or gel is applied at the following diseases / states:

• Traumatic damages of soft tissues;
• Muscular pains of not rheumatic and rheumatic origin;
• Musculoskeletal system diseases, including the pseudorheumatism ankylosing a spondylarthritis, psoriasis arthritis, an osteoarthrosis of a backbone and peripheral joints;
• Rheumatic defeats of soft tissues.

Diclofenac in the form of eye drops is appointed for treatment of the following diseases / states:

• Inflammatory processes of noninfectious genesis (including a cornea erosion, conjunctivitis, a keratoconjunctivitis, a posttraumatic inflammation of a cornea and conjunctiva);
• The inflammatory process which developed after surgical intervention;
• Miosis inhibition during operations for a cataract;
• Cystous hypostasis of a macula lutea of a retina after carrying out surgical removal of a cataract (treatment and prevention);
• Photophobia after a keratotomy.

Contraindications

Contraindications to use of Diclofenac in the form of tablets and suppositories are:

• Combination (incomplete or full) bronchial asthma and recuring polypose of okolonosovy bosoms and a nose with intolerance of acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (including in the anamnesis);
• Active gastrointestinal bleeding;
• Inflammatory diseases of intestines;
• Erosive cankers of a stomach and duodenum;
• Heavy liver and renal failure (the clearance of creatinine is less than 30 ml in a minute);
• The progressing diseases of kidneys;
• Active diseases of a liver;
• The confirmed hyperpotassemia;
• The period after performing aortocoronary shunting;
• Heavy heart failure;
• The third trimester of pregnancy and the period of a lactation (in the I-II trimesters of pregnancy Diclofenac can be applied in the smallest dosage and according to strict indications);
• Children's age: tablets – up to 6 years; suppositories on 50 mg – up to 14 years, on 100 mg – up to 18 years;
• Hypersensitivity to drug components, and also to other non-steroidal anti-inflammatory drugs.

Additional contraindications are:

• Tablets: glucose galactose absorption disturbance, hereditary lactose intolerance, insufficiency of lactase;
• Suppositories: proctitis.

Diclofenac in these dosage forms should be applied with care to the elderly patients (including receiving diuretics) weakened to patients and patients with low body weight at a peptic ulcer of a stomach and duodenum, a disease Krone, ulcer colitis, liver diseases in the anamnesis, a hepatic porphyria, arterial hypertension, chronic heart failure, considerable reduction of volume of the circulating blood, bronchial asthma, coronary heart disease, cerebrovascular diseases, дислипидемии / a lipidemia, a diabetes mellitus, diseases of peripheral arteries, smoking and alcoholism, a chronic renal failure, existence of an infection of Helicobacter pylori, heavy somatopathies. Also care is demanded by a concomitant use of Diclofenac with glucocorticosteroids (including with Prednisolonum), anticoagulants (including with warfarin), antiagregant (including with acetylsalicylic acid, klopidogrely), selective serotonin reuptake inhibitors (including with tsitalopramy, fluoxetine, paroksetiny, sertraline) and at long use of non-steroidal anti-inflammatory drugs.

Contraindications to use of Diclofenac in the form of solution for intramuscular introduction are:

• Digestive tract erosive cankers (in an aggravation phase);
• Hemopoiesis disturbances;
• "Aspirinovy" asthma;
• Pregnancy and period of a lactation;
• Age up to 15 years;
• Hypersensitivity to solution components (including to other non-steroidal anti-inflammatory drugs).

With care Diclofenac (solution) should be applied to patients of advanced age, and also at the induced acute hepatic porphyrias, heart failure, heavy renal failures and a liver.

Outwardly it is contraindicated to apply Diclofenac at the following diseases / states:

• "Aspirinovy" asthma;
• Disturbance of integrity of integuments;
• Third trimester of pregnancy and period of a lactation;
• Age up to 6 years;
• Hypersensitivity to drug components, and also to acetylsalicylic acid or other non-steroidal anti-inflammatory drugs.

Diclofenac in the form of ointment and gel should be applied with care to elderly patients, pregnant women in the I-II trimesters, and also at an aggravation of a hepatic porphyria, digestive tract erosive cankers, heavy functional disturbances of kidneys and a liver, chronic heart failure, bronchial asthma, disturbances of coagulability of blood (including hemophilia, lengthening of a bleeding time, tendency to bleedings).

It is contraindicated to apply eye drops at hypersensitivity to drug components. Diclofenac in drops should be applied with care to patients of advanced and children's age, pregnant women in the I-II trimesters, and also at the acetylsalicylic acid caused by reception bronchial asthma, an epithelial herpetic keratitis (including in the anamnesis), the diseases connected with disturbances of coagulability of blood including hemophilia, tendency to bleedings and lengthening of a bleeding time.

Route of administration and dosage

Diclofenac in the form of tablets should be accepted inside, without chewing and washing down with enough water, it is desirable in 30 minutes prior to meal (for achievement of bystry therapeutic effect). Administration of drug to, in time or after food is also possible.

To children of 15 years and the adult Diklofenak appoint 2-3 times a day 25-50 mg (as much as possible – 150 mg a day). After improvement the dose is gradually reduced and pass to a maintenance therapy – 50 mg a day.

At treatment of a juvenile pseudorheumatism it is possible to increase a daily dose to 3 mg/kg of body weight.

To children drug is usually appointed in the following doses (one-time/daily):

• 6-7 years (20-24 kg) – 25/25 mg;
• 8-11 years (25-37 kg) – 25/50-75 mg;
• 12-14 years (38-50 kg) – 25-50/75-100 mg.

Diclofenac in the form of solution should be entered deeply intramusculary. The single dose for adults makes 75 mg. If necessary not earlier than in 12 hours, perhaps repeated administration of drug. It is necessary to carry out therapy not longer than 2 days then it is necessary to pass to reception of tablets.

Suppositories enter rektalno. The adult usually appoint 100-150 mg a day divided into 2-3 receptions. At long therapy and in not hard cases drug is used on 100 mg a day. If suppositories apply along with administration of drug inside, the total dose of Diclofenac should not exceed 150 mg.

At emergence of the first symptoms of an algodismenorea suppositories appoint 50-100 mg which, if necessary, during several menstrual cycles is increased to 150 mg in an initial daily dose.

At the first signs of an attack of migraine Diclofenac apply 100 mg in a dose. If necessary perhaps repeated introduction in the same dose. If treatment continuation is required, the daily dose should not be more than 150 mg (in several introductions).

To children of 14 years usually appoint on 1 suppository on 50 mg to 2 times a day.

Outwardly to children 12 years are more senior and adults should apply drug, slightly rubbing, on skin 3-4 times a day. The necessary amount of Diclofenac is defined by the size of a painful zone. The single dose makes 2-4 g. Children of 6-12 years should not use more than 2 g of drug to 2 times a day.

Diclofenac in the form of eye drops is dug in before operation in a conjunctival sac on 1 drop of 5 times within 3 hours, right after operation – 3 times on 1 drop, further – 3-5 times a day during time, necessary for treatment.

At other indications usually appoint 4-5 times a day on 1 drop. Average for a long time therapies – up to 28 days. Before more prolonged use of Diclofenac it is necessary to conduct detailed ophthalmologic examination and exact diagnosis. As a rule, therapy is prolonged from one to several weeks.

Side effects

At use of Diclofenac in the form of tablets development of the following side effects is possible:

• Nervous system: often – dizziness, a headache; seldom – sleep disorders, a depression, irritability, drowsiness, aseptic meningitis (is more often at patients with a system lupus erythematosus and other system diseases of connecting fabric), dreadful dreams, spasms, a disorientation, the general weakness, feeling of fear;
• Digestive tract: often – nausea, diarrhea, a lock, abdominal pain or a spasm, feeling of abdominal distention, a meteorism, a round ulcer with possible complications, increase in activity of "hepatic" transaminases, gastrointestinal bleeding without ulcer; seldom – damage of a gullet, vomiting, a melena, jaundice, emergence of blood to Calais, aphthous stomatitis, holetsistopankreatit, hepatitis (perhaps fulminant current), dryness of mucous membranes (including oral cavities), cirrhosis, a liver necrosis, appetite change, a gepatorenalny syndrome, colitis, pancreatitis (including with the accompanying hepatitis);
• Respiratory system: seldom – a bronchospasm, cough, a pneumonitis, throat hypostasis;
• Cardiovascular system: seldom – increase in arterial pressure; premature ventricular contraction, congestive heart failure, thorax pain;
• Urinogenital system: often – a liquid delay; seldom – an oliguria, a papillary necrosis, a nephrotic syndrome, a proteinuria, intersticial nephrite, a hamaturia, an azotemia, an acute renal failure;
• Integuments: often – skin rash, a skin itch; seldom – a small tortoiseshell, an alopecia, toxic dermatitis, eczema, punctulate hemorrhages, a toxic epidermal necrolysis (Lyell's disease), a mnogoformny exudative erythema (including Stephens-Johnson's syndrome), the increased photosensitivity;
• Sense bodys: often – a sonitus; seldom – scotoma, a diplopia, an illegibility of visual perception, taste disturbance, an irreversible or reversible hearing impairment;
• Bodies of a hemopoiesis and immune system: seldom – anemia (including aplastic and hemolitic anemias), thrombocytopenia, a leukopenia, an agranulocytosis, an eosinophilia, a Werlhof's disease, deterioration in course of infectious processes;
• Allergic reactions: seldom – anaphylactoid reactions, an allergic vasculitis, a paraglossa and lips, an acute anaphylaxis (usually develops promptly).

At use of drug in the form of solution for injections and suppositories similar side effects can be observed. In the place of intramuscular introduction there can be a burning, and also development of an aseptic necrosis, infiltrate and a necrosis of fatty tissue is possible. At use of suppositories in rare instances there can be hypostases.

At external use side effects develop seldom. Usually they are shown in the form of an itch, rash, reddening and burning of local character.

At use of eye drops development of the following disturbances is possible:

• Alimentary system: vomiting, nausea;
• Allergic reactions: a photosensitization, a hyperemia, an itch in eyes, a Quincke's disease of the person, a fever, fever, skin rash, a mnogoformny exudative erythema;
• Local reactions: an illegibility of visual perception (right after an instillation), burning of eyes, opacification of a cornea, an iritis.

Special instructions

At long use of Diclofenac it is necessary to control function of a liver, the analysis a calla on the occult blood and a picture of peripheral blood.

During therapy reduction in the rate of motor and mental reactions in this connection it is necessary to abstain from driving of motor transport and performance of other potentially dangerous types of the works demanding high concentration of attention and bystry psychomotor reactions is possible.

Medicinal interaction

At simultaneous use of Diclofenac with some medicines there can be undesirable effects (consultation of the doctor is necessary).

Terms and storage conditions

To store in protected from light, the place, dry, unavailable to children, at a temperature up to 25 °C.

Period of validity:

• The tablets covered with a kishechnorastvorimy cover and drops eye – 3 years;
• Solution for intravenous administration, suppositories rectal, gel and ointment for external use – 2 years.

After opening of a bottle eye drops can be applied within 4 weeks.