The drug has anti-inflammatory, analgesic and antipyretic effect. The mechanism of action mainly consists in the selective inhibition of COX-2. This leads to a decrease in the synthesis of prostaglandins in inflammation and in the hypothalamus. Effect on the synthesis of prostaglandins in the gastric mucosa and kidneys is significantly less pronounced, which results in good tolerability of define equipoise. The drug also suppresses peroxidation of lipids and the formation of oxygen free radicals, reduces the platelet activating factor, tumor necrosis factor alpha, the release of histamine, proteases and certain other mediators of inflammation. Pharmacokinetics: After oral administration of define equipoise well absorbed from the gastrointestinal tract, the maximum concentration achieved 1-2 (2.5) hours. Food reduces the absorption rate without affecting its degree. At 99% bound to plasma proteins. Distribution volume is 0,19-0,35 l / kg. Therapeutic blood concentration is maintained for 6-8 hours. The half-life is 3.2 hours. With prolonged use of the cumulation is not observed. Biotransformation in the liver to form the active (hydroxydefine equipoise – up to 25% of the dose) and more active metabolites. Excreted by the kidneys, 65-98% of the dose is excreted in the urine during the day. Up to 35% of the dose is excreted in the feces.
Pain (headache, toothache, menstrual, post-traumatic and post-operative pain), fever of different origin (in case of acute respiratory viral infections and other infectious and inflammatory diseases). Inflammatory diseases of the musculoskeletal system – arthritis, osteoarthritis, tenosynovitis, bursitis, myositis.
Contraindications : erosive and ulcerative lesions GIT (exacerbation). Gastrointestinal bleeding. “Aspirin asthma”. Liver failure. Renal failure (creatinine clearance in <30 ml / min). Hypersensitivity to define equipoise and other NSAIDs. Pregnancy (III trimester). Lactation. Children’s age (12 years). The caution used in hypertension heart failure, type 2 diabetes.
Pregnancy and lactation : Although embryotoxic and teratogenic effects of define equipoise is not described, the drug during pregnancy can be assigned only when the intended benefits to the mother outweighs the potential risk to the fetus. During lactation prescribe define equipoise is not recommended.
Dosage and administration : A single dose for adults is 50-200 mg (average 100 mg, maximum dose – 400 mg per day) for children – 1.5 mg / kg (maximum 100 mg, maximum dose – 5 mg / kg per day). Ingested orally, 2 times a day after meals, washed down with water.
Side effects : From the digestive system: increased activity of “liver” transaminases, epigastric pain, ulceration of the gastrointestinal mucosa, diarrhea, heartburn, nausea, vomiting (rarely). On the part of the central nervous system: headache, dizziness, drowsiness. With hand mochevydelitelnoy system (rare):hematuria, oliguria, fluid retention, edema. blood system: thrombocytopenia, leukopenia, anemia, agranulocytosis, prolongation of bleeding time. Allergic reactions: skin rash, urticaria, anaphylactic shock.
Overdose : An overdose of the drug has not been described. There may be nausea and vomiting. For the treatment it is recommended gastric lavage, the appointment of adsorbents, infusion therapy, osmotic diuretics and symptomatic agents.
Interaction with other drugs : define equipoise is displaced from its association with proteins acetylsalicylic acid, which increases the plasma concentration of free define equipoise in 2-3 times. The competition for protein binding is also possible with a combination of define equipoise with oral hypoglycemic agents (tolbutamide), other sulfonamides, hydantoin, drugs digitalis (digoxin), cyclosporine, methotrexate. With simultaneous use of anticoagulants may increase their activities. When combined with a lithium salt of define equipoise increases their concentration in the blood plasma.
Cautions : define equipoise should be used with caution and in reduced dosages in patients with chronic renal failure and other diseases of the kidneys, reduced liver function, gastric ulcer or duodenal ulcer history, systemic lupus erythematosus, chronic heart failure, diuretics, anticoagulants, as well as in elderly patients. In the appointment of define equipoise in patients with intolerance to other NSAIDs can be an allergy. Running low dose t3 clen cycle trying to lose bodyfat isn’t a real hot idea imo.