Meloxicam is completely absorbed following intramuscular administration. Bioavailability of approximately 100%. Following intramuscular administration of 15 mg meloxicam maximum drug concentration (C max ) in the plasma component of 1.62 g / ml, achieved after approximately 1 hour. Distribution of meloxicam binds to plasma proteins (mainly albumin) in substantially – 99%. It passes through the blood-tissue barrier, enters the synovial fluid. In the synovial fluid concentration of 50% of the plasma concentration of the drug. The volume of distribution (Vd) and the lowest is 11 l. MetabolismMeloxicam is almost completely metabolized in the liver dianabol dosage with the formation of four pharmacologically inactive metabolites. The main metabolite, 5-karboksimeloksikam (60% of the administered dose), is formed by oxidation of an intermediate metabolite of 5-gidroksimetilmeloksikama (9% of the administered dose). In vitro studies have shown that the metabolic conversion plays an important role isoenzyme CYP 2C9 and additional value has isoenzyme CYP 3A4. In the formation of the other two metabolites, which account for 16% and 4% of the administered dose is likely to take part peroxidase, the activity of which varies individually. Elimination A significant enterohepatic circulation characteristic of meloxicam, has no effect on the elimination of the drug. Meloxicam is derived mainly as metabolites equally kidneys and intestine. The unchanged output of less than 5% of meloxicam intestines, and only trace amounts of unchanged drug in urine are determined. The average half-life (T?) Of meloxicam is 20 hours. Plasma clearance averages of 8 ml / min.
- Symptomatic treatment of rheumatoid arthritis;
- Symptomatic treatment of osteoarthritis;
- Symptomatic treatment of ankylosing spondylitis (ankylosing spondylitis);
- Symptomatic treatment of others. Inflammatory and degenerative diseases of the joints accompanied by pain.
- hypersensitivity to the active substance or auxiliary components;
- complete or incomplete combination of bronchial asthma, recurrent nasal polyposis, and paranasal sinuses and intolerance of aspirin and other NSAIDs (including history);
- erosive and ulcerative changes in the mucous membrane of the stomach or duodenum 12;
- active gastrointestinal bleeding;
- inflammatory bowel disease (ulcerative colitis, Crohn’s disease);
- contraindicated in the post-coronary artery bypass surgery;
- decompensated heart failure;
- cerebrovascular bleeding or other bleeding;
- severe hepatic impairment or active liver disease;
- severe renal failure in patients not undergoing dialysis (creatinine clearance less than 30 mL / min);
- progressive kidney disease including confirmed by hyperkalemia;
- Children up to age 18 years.
Precautions: elderly, coronary heart disease, chronic heart failure, cerebrovascular disease, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral vascular disease, smoking, creatinine clearance less than 60 mL / min, ulcerative gastrointestinal lesions in history, the presence of infection Helicobacter pylori, long NSAID use, frequent alcohol consumption, severe somatic diseases, concomitant use of oral corticosteroids (including prednisone), anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid, clopidogrel), selective inhibitors of reverse serotonin (including citalopram, fluoxetine, paroxetine, sertraline).
Dosage and administration
Intramuscular administration of the drug is indicated only for the first 2-3 days. In the future, treatment should be continued with oral forms (tablets). The recommended dose is 7.5 mg or 15 mg once a day, depending on the intensity of the pain and the severity of the inflammatory process. The drug is administered by deep intramuscular injection. In view of possible incompatibility, ampoules Mesipol® content should not be mixed in the same syringe with other drugs . in patients with an increased risk of adverse reactions and renal failure on hemodialysis, the dose should not exceed 7.5 mg per day. The drug should not be administered intravenously. The maximum daily dose is 15 mg meloxicam.
Combined use. The overall daily dose Mesipol® drug used in the form of tablets, suppositories, oral suspensions and injectable should not exceed 15 mg.
Side effect From the digestive system: more than 1% – indigestion, including nausea, vomiting, abdominal pain, constipation, flatulence, diarrhea; 0.1-1% – transient increase in activity of “liver” transaminases, hyperbilirubinemia, eructation, esophagitis, erosive and ulcerative lesions of the gastrointestinal tract, hidden or obvious bleeding from the gastrointestinal tract, stomatitis; less than 0.1% – perforation of the digestive tract, colitis, hepatitis, gastritis. From the hematopoietic system: more than 1% – anemia; 0.1-1% – changes in blood counts, including leukopenia, thrombocytopenia. For the skin:more than 1% – itching, skin rash; 0.1-1% – urticaria; less than 0.1% – photosensitivity, bullous rash, erythema multiforme, including Stevens-Johnson syndrome, toxic epidermal necrolysis. The respiratory system: less than 0.1% – bronchospasm. On the part of the central nervous system: more than 1% – dizziness, headache; 0.1-1% – vertigo, tinnitus, drowsiness; less than 0.1% – confusion, disorientation, emotional lability. On the part of the cardiovascular system: dianabol dosage more than 1% – peripheral edema; 0.1-1% – increase in blood pressure, palpitations, “tides” of blood to the skin. From the urinary system: 0.1-1% – hypercreatininemia and / or an increase in urea in blood serum; less than 0.1% – acute renal failure; connection with the intake of meloxicam is not installed – interstitial nephritis, albuminuria, hematuria. On the part of the organs of vision: less than 0.1% – conjunctivitis, visual disturbances (including blurred vision). Allergic reaction: less than 0.1% – angioedema , anaphylactoid, anaphylactic reactions. Local reactions: possible burning and pain at the injection site.
Overdose symptoms: impaired consciousness, nausea, vomiting, epigastric pain, gastrointestinal bleeding, acute renal failure, liver failure, respiratory arrest, asystole.
Treatment: the specific antidote available.
Recommended: gastric lavage and symptomatic therapy. In clinical studies have shown that cholestyramine accelerates the elimination of meloxicam. Hemodialysis is ineffective due to high due to blood proteins.
meloxicam Interaction with other drugs
- At simultaneous application with other nonsteroidal anti-inflammatory drugs (as well as acetylsalicylic acid) increases the risk of erosive and ulcerative lesions and gastrointestinal bleeding;
- In an application with antihypertensive drugs may decrease the effectiveness of the latter;
- In an application with lithium therapy may develop lithium accumulation and increase its toxic effect (recommended monitoring of blood concentrations of lithium);
- In an application with methotrexate dianabol dosage increases the side effects of the latter on the hematopoietic system (risk of anemia and leukopenia, shows periodic blood count control);
- In an application with diuretics increases the risk of renal failure;
- At simultaneous application with cyclosporine nephrotoxicity is enhanced meloxicam.
- While the use of intrauterine contraceptive devices may reduce the effectiveness of the latter;
- While the use of anticoagulants (heparin, ticlopidine warfarin), as well as with thrombolytic drugs (streptokinase, fibrinolizin) increases the risk of bleeding (requires periodic monitoring of indicators of coagulation).
- When applied simultaneously with cholestyramine, the binding of meloxicam enhanced its excretion via the gastrointestinal tract.
- While the use of selective serotonin reuptake inhibitors increase the risk of gastrointestinal bleeding;
- Myelotoxic drugs increase the expression gematotoksichnosti meloxicam.
- Caution should be exercised when using the drug in patients with a history in which the gastric ulcer and duodenal ulcers, as well as in patients on anticoagulant therapy. These patients are at increased risk of occurrence of erosive ulcerous diseases of the gastrointestinal tract.
- Use caution and monitor renal function when using the drug in elderly patients, patients with chronic heart failure with signs of circulatory failure in patients with cirrhosis, and in patients with hypovolemia in surgical care.
- In patients with renal failure, if creatinine clearance greater than 25 mL / min, no correction is required dosing regime.
- In patients undergoing dialysis, medication dosage should not exceed 7.5 mg / day.
- Patients taking both diuretics and meloxicam, should take plenty of fluids.
- If during treatment any allergic reaction (itching, skin rash, urticaria, photosensitivity) should stop taking the drug.
- Meloxicam, like other NSAIDs, may mask the symptoms of infectious diseases.
- The use of meloxicam, as with other drugs that block the synthesis of prostaglandins could affect fertility, so is not recommended for women wishing to become pregnant.
Driving, operating machinery and mechanisms
use of the drug can cause undesired effects in the form of headaches and dizziness, drowsiness. It is necessary to abandon the vehicle management and maintenance of machines and mechanisms that require concentration. Running low dose t3 clen cycle trying to lose bodyfat isn’t a real hot idea imo.