Diclofenac

General characteristics. Structure:

Active ingredient: 0,1 g of diclofenac of sodium.

Excipients: fat firm (витепсол W35) - before receiving suppository weighing 2,3 g.

The medicine having antiinflammatory, analgezruyushchy and febrifugal effect.

Pharmacological properties:

Pharmacodynamics. NPVP derivative of phenylacetic acid; has antiinflammatory, analgeziruyushchy and febrifugal effect. Not selectively oppressing cyclooxygenase 1 and 2 (TsOG-1 and TsOG-2), breaks metabolism of arachidonic acid, reduces amount of prostaglandin (Pg) in the inflammation center. It is most effective at pains of inflammatory character. As all NPVP, drug renders antiagregantny activity.

Pharmacokinetics. At rectal administration time of achievement of the maximum concentration of drug in plasma (TCmax) - 30 min. Concentration in plasma is in linear dependence on size of the entered dose. Change of pharmacokinetics of diclofenac against the background of repeated introduction is not noted. Bioavailability - 50%. Communication with proteins of plasma - more than 99% (the most part contacts alyyobumina).

Gets into breast milk, synovial fluid; the maximum concentration of drug (Cmax) in synovial fluid is observed on 2-4 h later, than in plasma. An elimination half-life of drug (Т½) 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.

Metayobolizm results from a repeated or single hydroxylation and a konjyugirovaniye with glucuronic acid. CYP2C9 isoenzyme also participates in drug metabolism. Pharmacological activity of metabolites is less, than diclofenac. The system clearance makes 260 ml/min. Т½ of plasma - 1-2 h 60% of the entered dose vyvoyoditsya 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 (the clearance of creatinine (CC) less than 10 ml/min.) removal of metabolites with bile increases, at the same time increase in their kontsentrayotion in blood is not observed. At patients with chronic hepatitis or the compensated cirrhosis pharmacokinetic parameters do not change.

Indications to use:

Inflammatory and degenerative diseases of a musculoskeletal system, including the revmatoyoidny, psoriasis, juvenile chronic arthritis ankylosing a spondylitis (бо­лезнь Bekhtereva), an osteoarthrosis, gouty arthritis (at a bad attack of gout of a predpochtiyotelna high-speed dosage forms), a bursitis, a tendovaginitis. Drug предна­значен for symptomatic therapy, reduction of pain and an inflammation for a moment an ispolzovayoniya, does not influence progressing of a disease.

Pain syndrome: head (including migraine) and a dentagra, a lumbago, an ischialgia, an ossalgiya, a nevyoralgiya, a mialgiya, an arthralgia, radiculitis, at oncological diseases, the posttraumatic and postoperative pain syndrome which is followed by an inflammation.

Algodismenorey; inflammatory processes in a small basin, including an adnexitis.

Infectious and inflammatory diseases of ENT organs with the expressed pain syndrome (as a part of complex therapy): pharyngitis, tonsillitis, otitis.

Feverish syndrome at "catarrhal" diseases and flu.

Route of administration and doses:

Rektalno, the adult the initial dose of 100-150 mg/days divided into 2-3 receptions; in not hard cases and at long therapy - 100 mg/days; in addition to oral administration the daily dose (rektalno) should not exceed 150 mg.

At algodismenory (at emergence of the first symptoms) an initial dose of 50-100 mg/days which is raised, if necessary, during several menstrual cycles to 150 mg.

Migraine attack - 100 mg at the first signs of an attack. If necessary - repeatedly 100 mg. In need of continuation of treatment in the next days the daily dose should not exceed 150 mg in several introductions.

To children 14 years - on 1 suppository with a dosage of 50 mg to 2 times a day are more senior.

Features of use:

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.

Because of an important role of Pg in maintenance of a renal blood-groove patients should show a special ostorozhyonost at appointment with a heart or renal failure, and also at a teyorapiya of the elderly patients accepting diuretics and patients at whom on any priyochena decrease in OTsK is observed (including after extensive surgical intervention). If in such cases appoint diclofenac, recommend to konyotrolirovat function of kidneys as a precautionary measure.

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. Diclofenac (as well as other NPVP) can cause a hyperpotassemia.

When performing long therapy it is necessary to control function of a liver, a picture of peyoriferichesky blood, the analysis a calla on the occult blood.

Due to the negative effect on fertility, the women planning to become pregnant are not recommended to use drug. At patients with infertility (including passing an obsledoyovaniye) it is recommended to cancel drug.

During treatment reduction of speed of mental and motor reactions therefore it is necessary to abstain from driving of transport and occupations other potentially dangerous viyoda of activity demanding the increased concentration of attention and speed of psikhomoyotorny reactions is possible.

Side effects:

Often - 1-10%; sometimes - 0,1-1%; seldom - 0,01-0,1%; very seldom - less than 0,001%, including otdelyyony cases.

From the alimentary system: often - epigastric pain, nausea, vomiting, diarrhea, dyspepsia, a meteorism, anorexia, increase in activity of aminotransferases; seldom - 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; very seldom - stomatitis, a glossitis, an esophagitis, nonspecific hemorrhagic colitis, an exacerbation of ulcer colitis or a disease Krone, a lock, pancreatitis, fulminant hepatitis, an exacerbation of hemorrhoids.

From a nervous system: often - a headache, dizziness; seldom - drowsiness; very seldom - sensitivity disturbance (including paresthesia), dysmnesias, a tremor, suyodorog, alarm, cerebrovascular disturbances, aseptic meningitis, a disorientation, a deyopressiya, sleeplessness, night "nightmares", irritability, mental disturbances.

From sense bodys: often - вертиго; very seldom - a vision disorder (an illegibility a zreyoniya, a diplopia), a hearing disorder, a sonitus, disturbance of flavoring feelings.

From an urinary system: very seldom - an acute renal failure, a geyomaturiya, a proteinuria, intersticial nephrite, a nephrotic syndrome, papillary нек­роз.

From bodies of a hemopoiesis: very seldom - thrombocytopenia, a leukopenia, gemoliticheyosky and aplastic anemia, an agranulocytosis. Allergic reactions: anaphylactic / anaphylactoid reactions, including the expressed sniyozheniye of the arterial pressure (AP) and shock; very seldom - a Quincke's disease (including persons).

From cardiovascular system (CCC): very seldom - heartbeat, a stethalgia, increase in the ABP, a vasculitis, the heart failure (HF), a myocardial infarction.

From respiratory system: seldom - bronchial asthma (including an asthma); very seldom - a pneumonitis.

From integuments: often - skin rash; seldom - a small tortoiseshell; very seldom - violent rashes, an erythema, including multiformny and Stephens-Johnson's syndrome, a Lyell's disease, exfoliative dermatitis, an itch, a hair loss, a photosensitization, a purpura, including alyolergichesky. Other: seldom - hypostases.

Interaction with other medicines:

Increases concentration in plasma of digoxin, lithium drugs.

Reduces effect of diuretics, against the background of kaliysberegayushchy diuretics the risk of development of a hyperpotassemia amplifies; against the background of anticoagulants, the antiagregantny and thrombolytic medicines (M) (an alteplaza, Streptokinasa, an urokinase) the risk of development of bleedings increases (more often than a GIT).

Reduces effect hypotensive and HP hypnotic drugs.

Increases probability of emergence of side effects of other NPVP and glucocorticosteroids (bleeding in a GIT), toxicity of a methotrexate and nephrotoxicity of cyclosporine (due to increase in their concentration in plasma).

ASK reduces concentration of diclofenac in blood.

Reduces effect of hypoglycemic HP. Paracetamol increases risk of development of nefrotoksichny effects of diclofenac.

Tsefamandol, лефоперазон, цефотетан, valproic acid and пликамицин increase the frequency of development of a prothrombinopenia.

Cyclosporine and drugs of gold increase influence of diclofenac on synthesis of Pg in kidneys that is shown by increase in nephrotoxicity.

Selective serotonin reuptake inhibitors increase risk of development of bleedings from a GIT.

Co-administration with ethanol, colchicine, corticotropin and drugs of the St. John's Wort which is made a hole increases risk of development of bleedings in a GIT.

The HP causing a photosensitization increase the sensibilizing effect of diclofenac to ultra-violet radiation.

The HP blocking canalicular secretion increase concentration in diclofenac plasma, thereby increasing its efficiency and toxicity.
Antibacterial HP from group of a hinolon - risk of development of spasms.

Contraindications:

Hypersensitivity (including to other NPVP), a full or incomplete combination of bronchial asthma, the nose recuring a polypose and okolonosovy bosoms and intolerance of atsetilsaliyotsilovy acid (ASK) or other NPVP (including in the anamnesis), erosive cankers of the zheluyodochno-intestinal path (ZIP) and a 12-perstny gut, an active gastrointestinal krovoteyocheniye, inflammatory diseases of intestines, a heavy hepatic and cordial nedostatochyonost; the period after performing aortocoronary shunting; a heavy renal nedostayotochnost (KK less than 30 ml/min.), the progressing diseases of kidneys, an active disease of a peyochena, the confirmed hyperpotassemia, pregnancy (the III trimester), the lactation period, children's age (up to 14 years - for suppositories of rectal 50 mg, up to 18 years - for suppositories of 100 mg); proctitis.

With care. The peptic ulcer of a stomach and 12-perstny gut (in the anamnesis), ulcer colitis, a disease Krone, liver diseases in the anamnesis, a hepatic porphyria, the chronic heart failure (CHF), arterial hypertension, considerable decrease in the volume of the circulating blood (VCB) (including after extensive surgical intervention), elderly patients (including the receiving diuretics weakened patients and with low body weight), bronchial asthma, odnovremenyony reception of glucocorticosteroids (GKS) (including Prednisolonum), anticoagulants (including warfarin), antiagregant (including ASK, a klopidogrela), selective serotonin reuptake inhibitors (including a tsitaloprama, fluoxetine, a paroksetin, sertraline), the coronary heart disease (CHD), cerebrovascular diseases, dislipidemiya/a lipidemia, sugar diayobt, diseases of peripheral arteries, smoking, the chronic renal failure (CRF) (KK of 30-60 ml/min.), existence of an infection of Helicobacter pylori, long use NPVP, alcoholism, heavy somatopathies, pregnancy (I and II trimesters).

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: the symptomatic therapy directed to elimination of increase in the ABP, a renal failure, spasms, irritations of a GIT, respiratory depression; in case of wrong oral administration of suppositories the gastric lavage, reception of aktivirovanyony coal is recommended. The artificial diuresis, a hemodialysis are ineffective (in connection with a considerable svyayozyyu with proteins and intensive metabolism).

Storage conditions:

In the dry, protected from light place at a temperature not above 20 °C. To store in the place, unavailable to children, the Period of validity 2 years. Not to use after the expiry date specified on packaging

Issue conditions:

According to the recipe

Packaging:

Suppositories rectal 100 mg. On 5 suppositories in a blister strip packaging from a PVC film. 2 blister strip packagings together with the application instruction place in a pack from a cardboard.