Ortophen, pills 25mg, 20pcs

Composition

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of 1 tab. contains:

Active ingredients:

diclofenac sodium 25 mg

Pharmacological action

of NSAIDs, a derivative of phenylacetic acid. It has a pronounced anti-inflammatory, analgesic and moderate antipyretic effect. The mechanism of action is associated with inhibition of the activity of COX, the main enzyme of arachidonic acid metabolism, which is a precursor of prostaglandins, which play an important role in the pathogenesis of inflammation, pain and fever. The analgesic effect is caused by two mechanisms: peripheral (indirectly, through suppression of prostaglandin synthesis) and central (due to inhibition of prostaglandin synthesis in the central and peripheral nervous systems).

In vitro concentrations equivalent to those achieved in the treatment of patients do not inhibit the biosynthesis of cartilage proteoglycans.

In rheumatic diseases, it reduces joint pain at rest and during movement, as well as morning stiffness and swelling of the joints, and helps to increase the volume of movement. Reduces post-traumatic and post-operative pain, as well as inflammatory edema.

With post-traumatic and postoperative inflammatory phenomena, it quickly relieves pain (occurring both at rest and during movement), reduces inflammatory edema and edema of the postoperative wound.

Inhibits platelet aggregation. With prolonged use, it has a desensitizing effect.

Pharmacokinetics

After oral use, it is absorbed from the gastrointestinal tract. Food intake slows down the rate of absorption, but the degree of absorption does not change. About 50% of the Active ingredient is metabolized during the” first pass ” through the liver. With rectal use, absorption is slower.

The time to reach_cmax in plasma after oral use is 2-4 hours, depending on the dosage form used, after rectal use – 1 hour, after intravenous use-20 minutes. The concentration of the Active ingredient in plasma is linearly dependent on the amount of the applied dose.

It doesn’t accumulate. Binding to plasma proteins is 99.7% (mainly with albumin). Penetrates the synovial fluid, _cmax is reached 2-4 hours later than in plasma.

It is largely metabolized with the formation of several metabolites, among which two are pharmacologically active, but to a lesser extent than diclofenac.

The systemic clearance of the Active ingredient is approximately 263 ml / min. T_1/2 from plasma is 1-2 hours, from synovial fluid – 3-6 hours.

Approximately 60% of the dose is excreted as metabolites by the kidneys, less than 1% is excreted unchanged in the urine, and the remainder is excreted as metabolites in the bile.

Indications

Inflammatory and degenerative diseases of the musculoskeletal system, including rheumatoid, psoriatic, juvenile chronic arthritis, ankylosing spondylitis (ankylosing spondylitis), osteoarthritis, gouty arthritis, bursitis, tendovaginitis. The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use, and does not affect the progression of the disease.

Pain syndrome:  headache (including migraine) and toothache, lumbago, sciatica, ossalgia, neuralgia, myalgia, arthralgia, sciatica, cancer, post-traumatic and postoperative pain syndrome accompanied by inflammation.

Algodismenorrhea:  inflammatory processes in the small pelvis, including adnexitis.

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

Contraindications

Hypersensitivity (including to other NSAIDs), complete or incomplete combination of bronchial asthma, recurrent nasal and paranasal sinus polyposis and intolerance to acetylsalicylic acid (ASA) or other NSAIDs (including in the anamnesis), erosive and ulcerative lesions of the stomach and duodenum, active gastrointestinal bleeding, inflammatory bowel diseases, severe liver and heart failure; the period after the procedure coronary artery bypass grafting; severe renal insufficiency (creatinine clearance less than 30 ml/min), progressive kidney disease, active liver disease, confirmed hyperkalemia, pregnancy (third trimester), lactation, children (up to 6 years-for enteric coated tablets 25 mg).

Hereditary problems of lactose intolerance, glucose-galactose malabsorption, and lactase deficiency.

With caution. Peptic ulcer of the stomach and duodenum, ulcerative colitis, Crohn’s disease, a history of liver disease, hepatic porphyria, chronic heart failure, arterial hypertension, significant decrease in the volume of circulating blood (BCC) (including after extensive surgery), elderly patients (including those receiving diuretics, weakened patients and patients with low body weight), bronchial asthma, concomitant use of corticosteroids (including prednisone), anticoagulants (including warfarin), antiplatelet agents (including ASA, clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline), IHD, cerebrovascular diseases, dyslipidemia/hyperlipidemia, diabetes mellitus, peripheral arterial diseases, smoking, chronic renal failure (creatinine clearance 30-60 ml/min), the presence of Helicobacter pylori infection, long-term use of NSAIDs, alcoholism, severe somatic diseases.

Side effects

From the gastrointestinal tract:  more often than 1% – abdominal pain or spasm, bloating, diarrhea, nausea, constipation, flatulence, increased activity of “liver” tranaminases, peptic ulcer with possible complications (bleeding, perforation), gastrointestinal bleeding without ulcers; less often than 1%-vomiting, jaundice, melena, the appearance of blood in the stool, esophageal damage, aphthous stomatitis, dry mucous membranes (including the oral cavity liver necrosis, cirrhosis, hepatorenal syndrome, changes in appetite, pancreatitis (including concomitant hepatitis), cholecystopancreatitis, colitis.

Nervous system disorders:  more often 1% – headache, dizziness; less often 1% – sleep disturbance, drowsiness, depression, irritability, aseptic meningitis (more often in patients with systemic lupus erythematosus and other systemic connective tissue diseases), convulsions, general weakness, disorientation, nightmares, fear.

From the side of the senses:  more often 1% – tinnitus; less often 1% – blurred vision, diplopia, taste disorders, reversible or irreversible hearing loss, scotoma.

From the side of the skin:  more often 1% – pruritus of the skin, skin rash; less often 1% – alopecia, urticaria, eczema, toxic dermatitis, erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome), increased photosensitivity, small-point hemorrhages.

From the genitourinary system:  more often 1% – fluid retention; less often 1% – nephrotic syndrome, proteinuria, oliguria, hematuria, interstitial nephritis, papillary necrosis, acute renal failure, azotemia.

Hematopoietic and immune system disorders:  less often than 1% – anemia (including hemolytic and aplastic anemia), leukopenia, thrombocytopenia, eosinophilia, agranulocytosis, thrombocytopenic purpura, worsening of the course of infectious processes (including the development of necrotizing fasciitis).

Respiratory system disorders:  less than 1% – cough, bronchospasm, laryngeal edema, pneumonitis.

From the cardiovascular system:  less than 1% – increased blood pressure; congestive heart failure, extrasystole, chest pain.

Allergic reactions:  less than 1% – anaphylactoid reactions, anaphylactic shock (usually develops rapidly), swelling of the lips and tongue, allergic vasculitis.

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 NSAIDs 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.

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

How to take it, course of use and dosage

Inside.

To achieve the rapid desired therapeutic effect, take 30 minutes before meals.In other cases, take before, during or after a meal, in an undigested form, washed down with a sufficient amount of water. Adults and adolescents from 15 years of age – 25-50 mg 2-3 times a day.

When the optimal therapeutic effect is achieved, the dose is gradually reduced and switched to maintenance treatment at a dose of 50 mg / day. The maximum daily dose is 150 mg.

In juvenile rheumatoid arthritis, the daily dose can be increased to 3 mg / kg of body weight.

The approximate mode of use of the drug is shown in the table:

Overdose

Symptoms: vomiting, dizziness, headache, shortness of breath, confusion, in children-myoclonic seizures, nausea, vomiting, abdominal pain, bleeding, impaired liver and kidney function.

Treatment: gastric lavage, use of activated charcoal, symptomatic therapy aimed at eliminating increased blood pressure, impaired renal function, convulsions, irritation of the gastrointestinal tract, respiratory depression. Forced diuresis and hemodialysis are ineffective.

Special instructions

In patients with hepatic insufficiency (chronic hepatitis, compensated cirrhosis of the liver), the kinetics and metabolism do not differ from similar processes in patients with normal liver function.

During long-term therapy, it is necessary to monitor liver function, peripheral blood picture, and fecal occult blood analysis.

During the treatment period, the speed of mental and motor reactions may decrease, so it is necessary to refrain from driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Storage conditions

Store the drug in a dry place, protected from light, out of reach of children at a temperature not exceeding 25°C.

Shelf

life is 3 years.

Active ingredient

Diclofenac

Conditions of release from pharmacies

By prescription

Dosage form

Tablets