Meloxicam – a non-steroidal anti-inflammatory drug with analgesic, anti-inflammatory and antipyretic activity. The anti-inflammatory action due to inhibition of the enzymatic activity of cyclooxygenase-2 (COX-2) involved in the biosynthesis of prostaglandins in inflammation. To a lesser extent Meloxicam acts on cyclooxygenase-1 (COX-1) participating in the synthesis of prostaglandins deca durabolin dosage which protect the mucosa of the gastrointestinal tract, and taking part in the regulation of blood flow in the kidney.
Relative bioavailability is nearly 100%. After the / m administration at a dose of 5 mg the maximum concentration (Cmax) was 1.62 g / ml and is attained within about 60 minutes. Meloxicam is well bound to plasma proteins, especially to albumin (99%). Penetrates into the synovial fluid, synovial fluid concentration is about 50% of plasma concentrations. The volume of distribution is low, on average 11 l. Interindividual differences constitute 30-40%.
Meloxicam is almost completely metabolized in the liver with the formation of 4 pharmacologically inactive derivatives. The main metabolite, 5′-karboksimeloksikam (60% of the dose), formed by oxidation of an intermediate metabolite 5′-gidroksimetilmeloksikama which is also excreted, but to a lesser extent (9% of the dose). Studies in vitro have shown that the metabolic conversion of isozyme plays an important role CYP 2C9, additional importance ZA4 CYP isozyme. The formation of two other metabolites (components, respectively, 16% and 4% of the dose) participates peroxidase, which activity is likely to vary individually.
Deduced equally with feces and urine, mainly as metabolites. Unchanged in the feces appears less than 5% of the daily dose in the urine as unchanged drug is found only in trace amounts. The average half-life of meloxicam is 20 hours. Plasma clearance is in average 8 mL / min.
Meloxicam demonstrates linear pharmacokinetics at doses of 7.5-15 mg when administered intramuscularly.
Hepatic or renal insufficiency of moderate severity has no significant effect on the pharmacokinetics of meloxicam.
- Symptomatic treatment of osteoarthritis;
- Symptomatic treatment of rheumatoid arthritis;
- 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;
- contraindicated in the post-coronary artery bypass surgery;
- decompensated heart failure;
- 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 gastric mucosa and 12 duodenal ulcer, active gastrointestinal bleeding;
- inflammatory bowel disease (ulcerative colitis, Crohn’s disease);
- 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 renal disease including confirmed by hyperkalemia;
- pregnancy, breast-feeding;
- Children up to age 18 years.
Ischemic heart disease, cerebrovascular disease, chronic heart failure, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, creatinine clearance 30-60 ml / min. A history of the development of ulcerative lesions gastrointestinal tract, the presence of infection Helicobacter pylori, old age, long-term use of NSAIDs, frequent alcohol consumption, severe somatic diseases, concomitant therapy following medications:
- Anticoagulants (eg, warfarin)
- antiplatelet agents (eg, aspirin, clopidogrel)
- oral steroids (e.g., prednisolone)
- selective serotonin reuptake inhibitor (such as citalopram, fluoxetine, paroxetine, sertraline)
To reduce the risk of adverse effects on the gastrointestinal tract to use the minimum effective dose as low as possible short course.
Use during pregnancy and during breastfeeding
Meloxicam is contraindicated during pregnancy. Inhibition of prostaglandin synthesis may have an adverse effect on pregnancy and fetal development. Data from epidemiological studies suggest an increased risk of spontaneous abortion and fetal heart defects after application of prostaglandin synthesis inhibitors during pregnancy. The absolute risk of developing heart disease increased from less than 1% to 1.5%. This risk increases with the dose and duration of therapy.
In the III trimester of pregnancy the use of prostaglandin synthesis inhibitors can cause the following violations of the fetus:
- premature closure of the ductus arteriosus and pulmonary hypertension as a result of toxic effects on the cardio-pulmonary system;
- renal dysfunction, with the further development of renal failure from reducing the amount of amniotic fluid.
The mother during birth may increase the duration of bleeding and to decrease uterine capacity and, as a consequence, increase the time of delivery. It is known that NSAIDs penetrate into breast milk, so Meloxicam is not recommended during lactation.
Dosing and Administration
Intramuscular injection 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 1 to 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. Given the possible compatibility of the contents of the ampoules Melbek ® should not be mixed in the same syringe with other drugs.
In patients with an increased risk of side effects, as well as in patients with severe renal impairment on hemodialysis, the dose should not exceed 7.5 mg day.
The drug should not be administered intravenously. Dosage Melbek preparation for intramuscular injection in children and adolescents has not been determined, this dosage form may only be used in adult patients.
The maximum daily dose should not exceed 15 mg. The combined use of overall daily dose Melbek drug ® , used in the form of pills and injections, should not exceed 15 mg.
very often – more than 1/10, often – more than 1/100 and less than 1/10, rarely – more than 1/1000 and less than 1/100, rarely – more than 1/10000 and less than 1/1000, very rare – less . 1/10000 From the side of hematopoiesis : rarely – anemia; rarely – changes in blood counts, including leukopenia, thrombocytopenia. From the digestive system : very often – indigestion, including nausea, vomiting, abdominal pain, constipation, flatulence, diarrhea; rarely – transient increase in activity of “liver” transaminases, hyperbilirubinemia, deca durabolin dosage belching, bleeding from the gastrointestinal tract (including hidden), stomatitis, gastritis; rarely – esophagitis, gastroduodenal ulcer, colitis, gastritis; very rarely – gastrointestinal perforation, hepatitis. For the skin : rarely – angioneurotic edema, pruritus, skin rash; -krapivnitsa rarely, toxic epidermal necrolysis, Stevens-Johnson syndrome; . very rare – bullous rash, erythema multiforme part of the respiratory system : rarely – in predisposed patients after administration of aspirin or other NSAIDs, reported the development of acute asthma. From the nervous system : often – headache; rarely – drowsiness, dizziness; . rare – mood swings, nightmares, Cardio-vascular system : Infrequent – increased blood pressure, “tides” of blood to the skin of the face; . rare – palpitation From the urinary system : rarely – hyperkalemia, hypercreatininemia and / or an increase in urea in blood serum; very rarely – acute renal failure. From the sensory organs : rarely – vertigo, rarely – visual impairment, including blurred vision, conjunctivitis, tinnitus. Allergic reactions : rare – anaphylactoid / anaphylactic reactions.Local reactions : possible burning and pain at the injection site.
Symptoms .: Impaired consciousness, nausea, vomiting, epigastric pain, gastrointestinal-bleeding, acute renal failure, liver failure, respiratory arrest, asystole Treatment : No specific antidote; symptomatic therapy. Forced diuresis, alkalization of urine, hemodialysis – are ineffective because of the high regard of the drug to blood proteins.
Interaction with other drugs With simultaneous use with other non-steroidal 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 preparations possible development of lithium accumulation and increase its toxic effect (recommended monitoring the concentration of lithium in the blood). In an application with methotrexate increases the side effects of the latter on the hematopoietic system (risk of anemia and leukopenia, shows periodic blood count control). While the use of diuretics and cyclosporine increases the risk of renal failure. While the use of intrauterine contraceptive devices may decrease 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 blood clotting). in an application with kolestiraminom, as a result of binding of meloxicam , increasing its excretion via the gastrointestinal tract. with simultaneous use with selective serotonin reuptake inhibitors increase the risk of gastrointestinal bleeding.
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. In these patients, increased risk of erosive and ulcerative diseases of the gastrointestinal tract. Use caution and monitor renal function when using the drug in elderly patients, patients with chronic heart failure with clinical manifestations in patients with cirrhosis, and in patients with hypovolemia due to surgical interventions.
Patients with renal insufficiency, if the clearance creatinine more than 30 ml / min do not require a correction mode.
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 in the course of 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 prostaglandin deca durabolin dosage synthesis, may affect fertility, so it is not recommended to appoint women planning to become pregnant.
Effects on ability to drive vehicles and mechanisms for
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.