Diklovit, rectal suppositories 50mg 10pcs

Composition

One suppository contains:  

Active ingredient-diclofenac sodium-50 mg;

The basis for suppositories is solid fat (Vitepsol brand H 15, W 35, Suppository brand NA 15, NAS 50) – until a suppository weighing 1.26 g

is obtained Pharmacological action

Diclofenac has anti-inflammatory, analgesic and antipyretic effects.

Indiscriminately inhibiting cyclooxygenase 1 and 2, it disrupts the metabolism of arachidonic acid, reduces the amount of prostaglandins in the focus of inflammation.

In rheumatic diseases, the anti-inflammatory and analgesic effect of diclofenac significantly reduces the severity of pain, morning stiffness, and joint swelling, which improves the functional state of the joint.

In case of injuries, in the postoperative period, diclofenac reduces pain and inflammatory edema.

 In primary algodismenorrhea, it relieves pain and bleeding.

The maximum concentration in the blood plasma is created after 30-40 minutes and is in linear dependence on the dose used.

Changes in the pharmacokinetics of diclofenac during repeated use are not observed, do not accumulate.

Binding to plasma proteins is more than 99% (most of them are bound to albumins).

Penetrates the synovial fluid. The maximum concentration in synovial fluid is observed 2-4 hours later than in plasma.

The half-life from synovial fluid is H-b h (the concentration of the Active ingredient in synovial fluid 4-6 hours after use of the drug is higher than in plasma, and remains higher for another 12 hours).

The relationship between the drug concentration in synovial fluid and the clinical efficacy of the drug has not been clarified.

Metabolism: 50% of the Active ingredient is metabolized during the” first pass ” through the liver.

Metabolism occurs as a result of repeated or single hydroxylation and conjugation with glucuronic acid.

The P450 CYP2C9 enzyme system participates in drug metabolism. The pharmacological activity of the metabolites is lower than that of diclofenac.

The plasma half-life is 2 hours. 65% of the administered dose is excreted as metabolites by the kidneys; less than 1% is excreted unchanged, the rest of the dose is excreted as metabolites in the bile.

In patients with severe renal insufficiency (creatinine clearance less than 10 ml / min), the excretion of metabolites in the bile increases, while an increase in their concentration in the blood is not observed.

In patients with chronic hepatitis or compensated cirrhosis of the liver, the pharmacokinetic parameters of diclofenac do not change.

Diclofenac passes into breast milk.

Indications

Diseases of the musculoskeletal system (rheumatoid arthritis, psoriatic, juvenile chronic arthritis, ankylosing spondylitis; gouty arthritis, rheumatic soft tissue damage, osteoarthritis of the peripheral joints and spine, including those with radicular syndrome, tendovaginitis, bursitis). Mild or moderate pain syndrome: neuralgia, myalgia, lumboishialgia, post-traumatic pain syndrome accompanied by inflammation, postoperative pain, headache, migraine, algodismenorrhea, adnexitis, toothache. As part of the complex therapy of infectious and inflammatory diseases of the ear, throat, nose with severe pain syndrome (pharyngitis, tonsillitis, otitis media).

Contraindications

Hypersensitivity (including to other NSAIDs), erosive and ulcerative lesions of the gastrointestinal tract (in the acute phase), bleeding from the gastrointestinal tract, “aspirin” asthma, hematopoiesis disorders, hemostasis disorders (including hemophilia), pregnancy, childhood (up to 15 years), lactation, rectal bleeding, hemorrhoids, trauma or inflammation of the rectum. With caution Anemia, bronchial asthma, congestive heart failure, arterial hypertension, ischemic heart disease, edematous syndrome, liver or kidney failure, alcoholism, inflammatory bowel diseases, erosive and ulcerative diseases of the gastrointestinal tract without exacerbation, diabetes mellitus, condition after extensive surgical interventions, induced porphyria, old age, diverticulitis, systemic connective tissue diseases.

Side effects

The resulting side effects depend on individual sensitivity, the amount of dose used, and the duration of treatment. The term ” sometimes “is used if side effects are observed in 1-10% of patients, ” rarely ” — in 0.001–1% of patients. Gastrointestinal tract: Sometimes — abdominal pain, bloating, diarrhea, nausea, constipation, flatulence, increased levels of “liver” enzymes, peptic ulcer with possible complications (bleeding, perforation), gastrointestinal bleeding;Rarely-vomiting, jaundice, melena, the appearance of blood in the stool, esophageal damage, aphthous stomatitis, dry mouth and mucous membranes, hepatitis (possibly fulminant course), liver necrosis, cirrhosis, hepatorenal syndrome, changes in appetite, pancreatitis, cholecystopancreatitis, colitis. The nervous system: Sometimes-headache, dizziness; Rarely-sleep disturbance, drowsiness, depression, irritability, aseptic meningitis (more often in patients with systemic lupus erythematosus and other systemic connective tissue diseases), convulsions, weakness, disorientation, nightmares, a feeling of fear. Sensory organs: Sometimes-tinnitus; Rarely-blurred vision, diplopia, impaired taste, reversible or irreversible hearing loss, scotoma. Skin conditions: Sometimes – skin pruritus, skin rash; Rarely-alopecia, urticaria, eczema, toxic dermatitis, erythema multiforme, including Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell’s syndrome), increased photosensitivity, small-point hemorrhages. Genitourinary system: Sometimes-fluid retention; Rarely-nephrotic syndrome, proteinuria, oliguria, hematuria, interstitial nephritis, papillary necrosis, acute renal failure, azotemia. Hematopoietic organs and the immune system: Sometimes-anemia (including hemolytic and aplastic anemia), leukopenia, thrombocytopenia, eosinophilia, agranulocytosis, thrombocytopenic purpura, worsening of the course of infectious processes (development of necrotizing fasciitis). Respiratory system: Rarely-cough, bronchospasm, laryngeal edema, pneumonitis. Cardiovascular system: Rarely-increased blood pressure; congestive heart failure, extrasystole, chest pain. Allergic reactions: Rarely — anaphylactoid reactions, anaphylactic shock (usually develops rapidly), swelling of the lips and tongue, allergic vasculitis. Local reactions with rectal use: Rarely-irritation of the rectal mucosa, mucosal discharge with an admixture of blood, pain during defecation, rectal bleeding.

Interaction

Increases plasma concentrations of 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, thrombolytics (alteplase, streptokinase, urokinase)-the risk of bleeding (more often from the gastrointestinal tract).

Reduces the effects of antihypertensive and hypnotic medications.

Increases the likelihood of side effects of other nonsteroidal anti-inflammatory drugs and glucocorticosteroids (bleeding in the gastrointestinal tract), methotrexate toxicity and cyclosporine nephrotoxicity.

Acetylsalicylic acid reduces the concentration of diclofenac in the blood.

Concomitant use with paracetamol increases the risk of nephrotoxic effects of diclofenac.

Reduces the effect of hypoglycemic agents.

Cefamandol, cefoperazone, cefotetan, valproic acid, and plicamycin increase the incidence of hypoprothrombinemia.

Cyclosporine and gold preparations increase the effect of diclofenac on prostaglandin synthesis in the kidneys, which increases nephrotoxicity.

Concomitant use with ethanol, colchicine, corticotropin, and St. John’s wort increases the risk of gastrointestinal bleeding.

Diclofenac enhances the action of drugs that cause photosensitization.

Drugs that block tubular secretion increase the plasma concentration of diclofenac, thereby increasing its toxicity.

How to take it, course of use and dosage

Rectally. Suppositories are introduced into the rectum, preferably after spontaneous bowel movement or a cleansing enema. After the introduction of the suppository, it is recommended to stay in bed for 20-30 minutes.

Adults and adolescents from 15 years of age: 1 suppository 2-3 times a day.

Concomitant use of Diclovit® with oral forms of diclofenac sodium is possible. The total daily dose of diclofenac sodium should not exceed 150 mg.

With algodismenorrhea (when the first symptoms appear), the initial dose is 50-100 mg/day (1 suppository 1-2 times a day), if necessary, the dose is increased over several menstrual cycles to 150 mg (1 suppository 3 times a day).

Migraine attack — 100 mg (2 suppositories) at the first sign of an attack. If necessary, repeat 100 mg (2 suppositories). If it is necessary to continue treatment in the following days, the daily dose should not exceed 150 mg (3 suppositories) per day.

The duration of treatment is determined by the doctor depending on the severity of the disease.

Overdose

Symptoms: dizziness, headache, rapid breathing, blurred consciousness, in children-myoclonic seizures, nausea, vomiting, abdominal pain, bleeding, impaired liver and kidney function. Treatment: activated charcoal, symptomatic therapy. Forced diuresis and hemodialysis are ineffective.

Special instructions

Patients taking the drug should refrain from activities that require increased attention and rapid mental and motor reactions, as well as alcohol consumption.

Form of production

Rectal suppositories 50 mg. 5 suppositories in a contour cell package.

One or two contour cell packages together with instructions for medical use of the drug are placed in a pack of cardboard.

Storage conditions

At a temperature not exceeding 25 °C. Keep out of reach of children.

Shelf

life is 3 years. Do not use the product after the expiration date.

Active ingredient

Diclofenac

Conditions of release from pharmacies

By prescription

Dosage form

rectal suppositories

Purpose

Children as prescribed by a doctor, Pregnant women in the first and second trimester as prescribed by a doctor, Adults as prescribed by a doctor, Children over 15 years of age

Indications

Swelling after injuries and operations, Migraines, Tendon Inflammation, Bursitis, Lumbago, Rheumatoid Arthritis, Periarthritis, Adnexitis, Gout, Sciatica, Arthritis, Osteoarthritis, Osteoarthritis