Description
Latin name
ORTOFEN
Release form
Tablets.
Packing
Per pack 20 pcs.
Pharmacological action
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 COX activity – the main enzyme of arachidonic acid metabolism, which is a precursor to prostaglandins, which play an important role in the pathogenesis of inflammation, pain and fever. The analgesic effect is due to two mechanisms: peripheral (indirectly, through the suppression of prostaglandin synthesis) and central (due to inhibition of prostaglandin synthesis in the central and peripheral nervous system).
In vitro at concentrations equivalent to those achieved in treating patients does 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, contributes to an increase in range of motion. Reduces post-traumatic and postoperative pain, as well as inflammatory edema.
In post-traumatic and postoperative inflammatory events, it quickly relieves pain (occurring both at rest and during movement), reduces inflammatory edema and edema of the postoperative wound.
Suppresses platelet aggregation. With prolonged use it has a desensitizing effect.
Pharmacokinetics
After oral administration, it is absorbed from the digestive tract. Eating slows down the rate of absorption, the degree of absorption does not change. About 50% of the active substance is metabolized during the first passage through the liver. With rectal administration, absorption is slower. The time to reach Cmax in plasma after oral administration is 2-4 hours, depending on the dosage form used, after rectal administration – 1 hour, intramuscular administration – 20 minutes. The concentration of the active substance in the plasma is linearly dependent on the size of the applied dose.
Does not cumulate. Plasma protein binding is 99.7% (mainly with albumin). It penetrates into the synovial fluid, Cmax is reached 2-4 hours later than in plasma.
is significantly metabolized to form several metabolites, two of which are pharmacologically active, but to a lesser extent than diclofenac.
Systemic clearance of the active substance is approximately 263 ml / min. T1 / 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, the rest is excreted in the form of metabolites with bile.
Indications
Inflammatory and degenerative diseases of the musculoskeletal system, including rheumatoid, psoriatic, juvenile arthritis, ankylosing spondylitis (ankylosing spondylitis), osteoarthritis, gouty arthritis, bursitis, tenosynovitis. The drug is intended for symptomatic therapy, reduce pain and inflammation at the time of use, does not affect the progression of the disease.
Pain: headache (including migraine) and toothache, lumbago, sciatica, ossalgia, neuralgia, myalgia, arthralgia, sciatica, for cancer, post-traumatic and postoperative pain syndrome, accompanied by inflammation.
Algodismenorea: inflammatory processes in the pelvis, including adnexitis.
Infectious and inflammatory diseases of the ENT – organs with severe pain syndrome (as part of complex therapy): pharyngitis, tonsillitis, otitis media.
Contraindications
Hypersensitivity (including other NSAIDs), a complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance to acetylsalicylic acid (ASA) or other history of gastric ulcer and duodenal ulcer, active gastrointestinal bleeding, inflammatory bowel disease, severe hepatic and heart failure period after coronary artery bypass grafting, severe renal failure inactivity (creatinine clearance (CC) less than 30 ml / min), progressive kidney disease, active liver disease, confirmed hyperkalemia, pregnancy (III trimester), lactation, childhood (up to 6 years – for enteric-coated tablets 25 mg) .
Hereditary lactose intolerance, malabsorption of glucose-galactose, lactase deficiency.
Caution. Stomach ulcer and duodenal ulcer, ulcerative colitis, Crohn’s disease, a history of liver disease, liver porphyria, chronic heart failure, hypertension, a significant decrease in circulating blood volume (BCC) (including after extensive surgery), elderly patients (including those receiving diuretics, debilitated patients and patients with low body weight), bronchial asthma, concomitant use of GCS (including prednisone), anticoagulants (including warfarin), antiplatelet agents ( including ASA, clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline), ischemic heart disease, cerebrovascular disease, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral artery disease, smoking, chronic renal failure (CC 30-60 ml / min), the presence of Helicobacter pylori infection, prolonged use of NSAIDs, alcoholism, severe somatic diseases.
Use during pregnancy and lactation
Contraindicated in the third trimester of pregnancy. In the I and II trimester of pregnancy should be used according to strict indications and at the lowest dosage.
Diclofenac passes into breast milk. If necessary, the appointment of the drug during lactation, breastfeeding should be discontinued.
Composition
1 tab. contains:
Active substances: diclofenac sodium 25 mg
Dosage and Administration
Inside.
To achieve the fast desired therapeutic effect, take 30 minutes before a meal. In other cases, take before, during or after a meal, not chewed, washed down with a sufficient amount of water. Adults and adolescents from 15 years old – 25-50 mg 2-3 times a day. Upon reaching the optimal therapeutic effect, the dose is gradually reduced and transferred to maintenance treatment at a dose of 50 mg / day. The maximum daily dose is 150 mg.
In juvenile rheumatoid arthritis, the daily dose may be increased to 3 mg / kg body weight.
The indicative use of the drug is presented in the table:
Age (body weight, kg) Single dose (number of tablets) Daily dose (number of tablets)
6-7 years (20-24) 1 [25] 1 [25]
8-11 years (25-37) 1 [25] 2-3 [ 50-75]
12-14 years old (38-50) 1-2 [25-50] 3-4 [75-100]
Older than 15 and adults 1-2 [25-50] 2-6 [50-150 ]
Side effects of the
From the gastrointestinal tract: more than 1% – abdominal pain or spasm, bloating, diarrhea, nausea, constipation, flatulence, increased activity of hepatic tranaminases, peptic ulcer with possible complications (bleeding, perforation), gastrointestinal bleeding without ulcers less than 1% – vomiting, jaundice, melena, blood in the stool, damage to the esophagus, aphthous stomatitis, dry mucous membranes (including the oral cavity), hepatitis (possibly fulminant), liver necrosis , cirrhosis, hepatorenal syndrome, changes in appetite, pancreatitis (including concomitant hepatitis), cholecystopancreatitis, colitis.
From the nervous system: more often 1% – headache, dizziness less than 1% – sleep disturbance, drowsiness, depression, irritability, aseptic meningitis (more often in patients with systemic lupus erythematosus and other systemic diseases of the connective tissue), cramps, general weakness, disorientation , nightmares, a sense of fear.
From the sensory organs: often 1% – tinnitus less than 1% – blurred visual perception, diplopia, taste disorder, reversible or irreversible hearing loss, scotoma.
From the skin: more than 1% – itching, skin rash less than 1% – alopecia, urticaria, eczema, toxic dermatitis, erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell syndrome), increased photosensitivity, small hemorrhages.
From the genitourinary system: more often 1% – fluid retention less than 1% – nephrotic syndrome, proteinuria, oliguria, hematuria, interstitial nephritis, papillary necrosis, acute renal failure, azotemia.
From the hemopoietic organs and the immune system: less 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 necrotic fasciitis).
From the respiratory system: 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.
Drug Interaction
Increases plasma concentrations of digoxin, methotrexate, lithium and cyclosporine.
Reduces the effect of diuretics, against the background of potassium-sparing diuretics increases the risk of hyperkalemia on the background of anticoagulants, thrombolytic agents (alteplase, streptokinase, urokinase) – the risk of bleeding (more often from the gastrointestinal tract).
Reduces the effects of hypotensive and sleeping pills.
Increases the likelihood of side effects of other NSAIDs and glucocorticosteroid agents (bleeding in the gastrointestinal tract), toxicity of methotrexate and nephrotoxicity of cyclosporine. Acetylsalicylic acid lowers 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 the synthesis of prostaglandins in the kidneys, which increases nephrotoxicity.
Co-administration with ethanol, colchicine, corticotropin and St. John’s wort increases the risk of bleeding in the gastrointestinal tract.
Diclofenac enhances the effect of photosensitization drugs. Drugs that block tubular secretion increase the plasma concentration of diclofenac, thereby increasing its toxicity.
Quinolone antibacterials are a risk of seizures.
Overdose
Symptoms: vomiting, dizziness, headache, shortness of breath, obscuration of consciousness, in children – myoclonic cramps, nausea, vomiting, abdominal pain, bleeding, impaired liver and kidney function.
Treatment: gastric lavage, administration of activated charcoal, symptomatic therapy, aimed at eliminating the increase in blood pressure, impaired renal function, convulsions, irritation of the gastrointestinal tract, respiratory depression. Forced diuresis, hemodialysis are ineffective.
Storage conditions
Store the drug in a dry, dark place, out of the reach of children, at a temperature not exceeding 25 ° C.
Expiration
3 years.
Active ingredient
Diclofenac
Formulation
Dosage form
tablets
Tatkhimpharmpreparaty, Russia
