Relative bioavailability is nearly 100%. Following intramuscular administration of 5 mg maximum concentration (Cmax) was 1.62 g / ml and is attained within about 60 minutes. Testosterone propionate buy well associated plasma protein, especially albumin (99%). Penetrates into the synovial fluid, synovial fluid concentration is about 50% of plasma concentrations. The volume of distribution (Vd) is low, on average 11 l. Interindividual differences constitute 30-40%.
Is almost completely metabolized in the liver with the formation of four pharmacologically inactive derivatives. The main metabolite, 5′-karboksimeloksikam (60% of the dose), is formed by oxidation of an intermediate metabolite 5′-hydroxy-metilmeloksikama 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 CYP2C9, additional importance isoenzyme CYP3A4. 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. In unmodified form with the faeces derived at least 5% of the daily dose in the urine in an unmodified form of the drug is found only in trace amounts. The average half-life (T ½ ) is 20 hours. The plasma clearance amounts on 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 testosterone propionate buy treatment of osteoarthritis;
- Symptomatic treatment of rheumatoid arthritis;
- Symptomatic treatment of ankylosing spondylitis (ankylosing spondylitis).
- 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 polyposis, nasal mucosa and paranasal sinuses and intolerance of aspirin and other nonsteroidal anti-inflammatory drugs (NSAIDs) (including history);
- erosive and ulcerative changes in gastric mucosa and 12 duodenal ulcer, active gastrointestinal bleeding;
- exacerbation of inflammatory bowel disease (ulcerative colitis, Crohn’s disease);
- cerebrovascular bleeding or other bleeding;
- severe hepatic impairment or active liver disease;
- severe renal insufficiency in patients who are not undergoing dialysis (creatinine clearance (CC) of 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, QC 30 to 60 ml / min.
A history of the development of ulcerative lesions of the gastrointestinal tract (GIT), 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 (e.g., aspirin, clopidogrel);
- oral steroids (e.g., prednisone);
- 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.
Dosage and administration
Intramuscular. 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 15 mg 1 time / day, depending on the intensity of pain and the severity of inflammation. The drug is administered by deep intramuscular injection. Intravenous drug banned! In patients with increased risk of adverse reactions, the daily dose should not exceed 7.5 mg. In patients with end-stage renal disease on hemodialysis, the dose should not exceed 7.5 mg. In patients with low or moderate renal impairment (creatinine clearance 30 mL / min), the dose should not exceed 7.5 mg. Of the preparation The dosage regimen for intramuscular injection in children and adolescents is not defined, this dosage form may only be used in adult patients. The maximum recommended daily dose of -15 mg. In the combined application of different drug dosage forms its maximum daily dose in tablets, suppositories, and as a solution for injection of 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 “hepatic” transaminases, hyperbilirubinemia, eructation, esophagitis, gastroduodenal ulcer, bleeding from the gastrointestinal tract (including hidden), stomatitis; less than 0.1% – gastrointestinal perforation, colitis, hepatitis, gastritis. From the hematopoietic system : more than 1% – anemia; 0.1-1% – changes in blood testosterone propionate buy 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 (CNS) : 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 (CVS) : more than 1% – peripheral edema; 0.1-1% – increase in blood pressure (BP), heart rate, “tides” of blood to the skin. From the mochevydelitelnoy 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.From the senses : less than 0.1% – conjunctivitis, visual disturbances, including blurred vision. Allergic reaction : less than 0.1% – angioedema, anaphylactic / anaphylactoid reactions. Local reactions : more than 1% – swelling at the injection site; less than 1% – pain at the injection site
Overdose 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 reception with other NSAIDs (as well as acetylsalicylic acid) increases the risk of erosive and ulcerative lesions and bleeding from the gastrointestinal tract.
In an application with antihypertensive drugs may decrease the effectiveness of the latter.
In an application with lithium preparations may development of cumulation of lithium and increase its toxic effect (recommended monitoring the concentration of lithium in the blood).
When applied simultaneously 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 with cyclosporin increased risk of developing renal failure. I In an application with intrauterine contraceptives may decrease the effectiveness of the latter.
While the use of anticoagulants (heparin, ticlopidine warfarin), antiplatelet agents (aspirin, clopidogrel), as well as with fibrinolytic drugs (streptokinase, fibrinolizin) increases the risk of bleeding ( requires periodic monitoring of indicators of coagulation). While the use of selective serotonin reuptake inhibitors increase the risk of gastrointestinal bleeding.
Caution must 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 gastrointestinal disease.
Use caution and monitor renal function when using the drug in elderly patients, in patients with chronic heart failure with clinical manifestations in patients with cirrhosis, and in patients with hypovolemia as a result of surgery. In patients with renal insufficiency, if the spacecraft 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 sufficient the amount of liquid.
If in the process of treating any allergic reaction (itching, skin rash, urticaria, photosensitivity) should consult a doctor with a view to resolving the issue of the termination of reception of a preparation.
meloxicam, like other NSAIDs, may mask the symptoms of infectious diseases.
The use of meloxicam, testosterone propionate buy as the and other drugs that block prostaglandin synthesis, may affect fertility, so is not recommended for women planning pregnancy.
Driving, operating machinery and mechanisms
use of the drug can cause undesired effects in the form of headaches and dizziness, drowsiness. In the period of treatment should refrain from driving motor vehicles and activities potentially hazardous activities that require high concentration and psychomotor speed reactions.