Non-steroidal anti-inflammatory drug, derivative of phenylacetic acid; has anti-inflammatory analgesic and antipyretic effects. By indiscriminate inhibiting cyclooxygenase 1 and cyclooxygenase 2 it disrupts arachidonic acid metabolism, decreases quantity of prostaglandins in inflammation focus.
It is most effective for pain of inflammatory nature. Like all non-steroidal anti-inflammatory drugs it has anti-aggregate activity.
The maximum concentration in blood plasma is created after 30-40 minutes and is in linear dependence on the dose used. No changes in pharmacokinetics of diclofenac against the background of repeated administration are observed. Binding with plasma proteins – not more than 99 % (most of it is bound with albumin).
It penetrates into synovial fluid. Maximal concentration in synovial fluid is observed 2-4 hours later than in plasma. Half-life period of synovial fluid is 3-6 hours (concentration of active substance in synovial fluid is higher 4-6 hours after drug administration than in plasma and stays higher during 12 hours). The relationship between the concentration of the drug in the synovial fluid and the clinical efficacy of the drug is not clear.
Metabolism occurs as a result of multiple or single hydroxylation and conjugation with glucuronic acid. The P450 enzyme system CYP2C9 is involved in metabolism of the drug. Pharmacological activity of metabolites is lower than that of diclofenac.
Systemic clearance is 350 ml/min distribution volume is 550 ml/kg. Plasma elimination half-life is 2 hours. 65% of the administered dose is excreted as metabolites by kidneys; less than 1% is excreted unchanged, the rest of the dose is excreted as metabolites with bile.
In patients with severe renal insufficiency (creatinine clearance less than 10 ml/min) excretion of metabolites with bile is increased, while increase of their concentration in blood is not observed.
In patients with chronic hepatitis or compensated liver cirrhosis pharmacokinetic parameters of diclofenac are not changed. Diclofenac penetrates into breast milk.
Symptomatic treatment of diseases of the musculoskeletal system (rheumatoid arthritis psoriatic arthritis ankylosing spondylitis; gouty arthritis rheumatic soft tissue osteoarthritis of peripheral joints and spine including with radicular syndrome tendovaginitis bursitis).
The drug is intended to be used for symptomatic therapy to reduce pain and inflammation at the moment of use and has no effect on disease progression.
Pain syndrome of mild to moderate severity: neuralgia myalgia lumbo-ischialgia post-traumatic pain syndrome accompanied by inflammation postoperative pain headache migraine algodysmenorrhea adnexitis toothache.
One suppository contains:
diclofenac sodium – 50 mg or 100 mg
The suppository base: solid fat, type A – enough to obtain a suppository weight of 1.25 g or 2.0 g.
How to take, the dosage
Rectally in adults the initial dose is 100-150 mg/day divided into 2-3 doses; in mild cases and in long-term therapy – 50-100 mg/day; in addition to oral administration the total daily dose (rectally and orally) should not exceed 150 mg.
In algodysmenorrhea (at the appearance of the first symptoms) the initial dose is 50-100 mg/day, which may be increased during several menstrual cycles up to 150 mg, if necessary. Migraine attack – 100 mg at the first sign of an attack.
If necessary – 100 mg again. If it is necessary to continue treatment on subsequent days, the daily dose should not exceed 150 mg in several injections. In adolescents over 15 years of age, only suppositories of 50 mg are used with a single dose of not more than 1 suppository.
Increases plasma concentration of digoxin methotrexate lithium drugs and cyclosporine.
Reduces the effect of diuretics against potassium-saving diuretics increases the risk of hyperkalemia; against anticoagulants thrombolytic agents (alteplase streptokinase urokinase) – risk of bleeding (often from the gastrointestinal tract). Reduces the effects of hypotensive and sleeping pills.
Increases the likelihood of side effects of other non-steroidal anti-inflammatory drugs and glucocorticosteroids (bleeding in the gastrointestinal tract) methotrexate toxicity and cyclosporine nephrotoxicity. Acetylsalicylic acid reduces the blood concentration of diclofenac. Concomitant use with paracetamol increases the risk of nephrotoxic effects of diclofenac.
Cefamandol cefoperazone cefotetan valproic acid and plikamycin increase the incidence of hypoprothrombinemia.
Cyclosporine and gold drugs increase the effect of diclofenac on prostaglandin synthesis in the kidneys which increases nephrotoxicity.
Simultaneous administration with ethanol colchicine corticotropin serotonin reuptake inhibitors and preparations of St. John’s wort increases the risk of gastrointestinal bleeding.
Diclofenac increases the effect of drugs that cause photosensitization. Drugs that block tubular secretion increase the plasma concentration of diclofenac thereby increasing its toxicity.
Antibacterial drugs of quinolone group – the risk of seizures. Effect on the results of laboratory tests: diclofenac may affect the values of serum transaminases (if this effect is prolonged or if there are complications the treatment must be stopped) and may also cause an increase in potassium concentration.
Because of the important role of prostaglandins in maintaining renal blood flow, special caution should be exercised when prescribing to patients with cardiac or renal insufficiency as well as in the therapy of elderly patients taking diuretics and patients who for any reason have a decrease in circulating blood volume (e.g. after major surgery).
If diclofenac is administered in such cases it is recommended as a precaution to monitor renal function.
In patients with hepatic insufficiency (chronic hepatitis compensatory cirrhosis) kinetics and metabolism do not differ from those of patients with normal liver function. During long-term therapy it is necessary to monitor liver function, peripheral blood count and fecal occult blood test.
During the treatment it is possible to decrease the speed of mental and motor reactions, so it is necessary to refrain from driving motor transport and other potentially dangerous activities that require high concentration and quick psychomotor reactions.
– The period after coronary artery bypass grafting.
– III trimester of pregnancy period of breastfeeding.
– Uncompensated heart failure.
– Hypersensitivity to the active substance or auxiliary components.
– Anamnestic evidence of an attack of bronchoobstruction rhinitis urticaria after receiving acetylsalicylic acid or other NSAIDs (total or partial intolerance syndrome of acetylsalicylic acid – rhinosinusitis urticaria nasal mucosal polyps asthma).
– Erosive and ulcerative changes of the mucosa of the stomach or 12 duodenum active gastrointestinal bleeding.
– Exacerbation of inflammatory bowel diseases (non-specific ulcerative colitis Crohn’s disease).
– Cerebrovascular bleeding or other bleeding and hemostasis disorders.
– Severe hepatic insufficiency or active liver disease.
– Severe renal insufficiency (creatinine clearance less than 30 ml/min) progressive renal diseases, including confirmed hyperkalemia.
– Childhood (under 18 years for suppositories by 100 mg to 15 years for suppositories by 50 mg).
– Rectal bleeding hemorrhoids trauma or inflammation of the rectum.
Frequently, 1-10%; sometimes, 01-1%; rarely, 001-01%; very rarely, less than 0001% including individual cases.
Digestive system disorders: frequent – epigastric pain nausea vomiting diarrhea dyspepsia flatulence anorexia increased aminotransferase activity; rare – gastritis proctitis bleeding from the GI tract (vomiting with blood melena diarrhea with blood admixture) GI ulcers (with or without bleeding or perforation) hepatitis jaundice liver function disorder; very rare – stomatitis glossitis esophageal damage diaphragm-like intestinal strictures nonspecific hemorrhagic colitis exacerbation of ulcerative colitis or Crohn’s disease constipation pancreatitis fulminant hepatitis exacerbation of hemorrhoids.
Nervous system: common – headache dizziness; rare – somnolence; very rare – sensory disorders including paresthesia memory disorders tremor cramps anxiety cerebrovascular disorders aseptic meningitis disorientation depression insomnia nightmares irritability mental disorders.
Sense organs: often – vertigo; very rare – visual impairment (blurred vision diplopia) hearing impairment tinnitus impairment of the sense of taste.
Urinary system disorders: very rarely – acute renal failure hematuria proteinuria interstitial nephritis nephrotic syndrome papillary necrosis.
Hematopoietic organs: very rarely – thrombocytopenia leukopenia hemolytic and aplastic anemia agranulocytosis.
Allergic reactions: anaphylactic/anaphylactoid reactions including significant decrease in blood pressure and shock; very rare – angioedema (including facial).
Cardiovascular system disorders: very rare – palpitations chest pain increased blood pressure vasculitis heart failure myocardial infarction.
Respiratory system disorders: rare – bronchial asthma (including dyspnea); very rare – pneumonitis.
The skin: often – skin rash; rarely – urticaria; very rare – bullous rash eczema including multiforme and Stevens-Johnson syndrome Lyell syndrome exfoliative dermatitis itching hair loss photosensitization purpura including allergic.
Local reactions when rectal administration: irritation of the rectal mucosa mucous discharge with a touch of blood pain during defecation rectal bleeding.
Symptoms: dizziness headache hyperventilation pulmonary confusion in children – myoclonic convulsions nausea vomiting abdominal pain bleeding from the gastrointestinal tract liver and kidney disorders.
Treatment: activated charcoal symptomatic therapy. Forced diuresis hemodialysis is ineffective.
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