Composition
Meloxicam 15 mg
Pharmacological action
Pharmaceutical Group:
NSAIDs.
Pharmaceutical action:
NSAIDs have anti-inflammatory, antipyretic, and analgesic effects. Belongs to the class of oxycams; a derivative of enolic acid.
The mechanism of action is inhibition of Pg synthesis as a result of selective suppression of COX-2 enzymatic activity. When prescribed in high doses, long-term use and individual characteristics of the body, COX 2 selectivity decreases. Inhibits Pg synthesis in the inflammatory region to a greater extent than in the gastric mucosa or kidneys, which is associated with a relatively selective inhibition of COX-2.
It is less likely to cause erosive and ulcerative diseases
of the gastrointestinal tract. :
Absorption from the gastrointestinal tract after oral or rectal use is 89%; tablets and suppositories are bioequivalent. Food intake does not affect absorption. The plasma concentration is dose-dependent. TCmax – 5-6 hours. Css is created in 3-5 days.
Binding to plasma proteins is 99%. Passes through histohematic barriers, penetrates synovial fluid. The synovial fluid concentration is 50% of the plasma concentration. Metabolism in the liver – to inactive metabolites.
It is excreted through the intestines and kidneys (in approximately equal proportions), unchanged – 5% of the daily dose (through the intestines). T1 / 2-20 hours Plasma clearance is on average 8 ml / min (decreases in the elderly).
Indications
Rheumatoid arthritis; osteoarthritis; ankylosing spondylitis (Ankylosing spondylitis), etc. inflammatory and degenerative joint diseases accompanied by pain syndrome.
It is intended for symptomatic therapy, reducing pain and inflammation at the time of use, and does not affect the progression of the disease.
Contraindications
Hypersensitivity (including to NSAIDs etc. ), and a combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance of ask and drugs pirazolona range;
gastric ulcer and 12 duodenal ulcer (in the phase of exacerbation), severe liver failure, chronic renal failure in patients not undergoing dialysis (KK less than 30 ml/min), active gastrointestinal bleeding;
progressive kidney disease, severe liver failure or active liver disease status after conducting coronary artery bypass surgery, confirmed hyperkalemia, inflammatory bowel disease, children’s age (under 12 years), pregnancy, lactation.
With caution. Advanced age, CHD, CHF, cerebrovascular diseases, dyslipidemia/hyperlipidemia, diabetes mellitus, peripheral arterial diseases, smoking, CRF (creatinine clearance 30-60 ml/min), a history of gastrointestinal ulcers, the presence of H. pulori infection, long-term use of NSAIDs, alcoholism, severe somatic diseases, simultaneous use of oral corticosteroids (including prednisone), anticoagulants (including prednisone). warfarin), antiplatelet agents (including clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline).
Side effects
Frequency: often-more than 1%; infrequently-0.1-1%; rarely-0.01-0.1%; very rarely-less than 0.01%.
From the digestive system: often-dyspepsia, including nausea, vomiting, abdominal pain, constipation, flatulence, diarrhea; infrequently-transient increase in the activity of “liver” transaminases, hyperbilirubinemia, belching, esophagitis, gastroduodenal ulcer, gastrointestinal bleeding (including hidden), stomatitis; rarely-gastrointestinal perforation, colitis, hepatitis, gastritis.
From the hematopoietic organs: often-anemia; infrequently-changes in the blood formula, including leukopenia, tromocytopenia.
From the skin: often-pruritus, skin rash; infrequently-urticaria; rarely-photosensitization, bullous rashes, erythema multiforme, including Stevens-Johnson syndrome, toxic epidermal necrolysis.
From the respiratory system: rarely-bronchospasm.
From the nervous system: often – dizziness, headache; infrequently-vertigo, tinnitus, drowsiness; rarely-confusion, disorientation, emotional lability.
From the cardiovascular system: often-peripheral edema; infrequently-increased blood pressure, palpitations, “flushes” of blood to the skin of the face.
From the urinary system: infrequently-hypercreatininemia and / or increased serum urea concentration; rarely – acute renal failure; association with meloxicam intake has not been established – interstitial nephritis, albuminuria, hematuria.
From the sensory organs: rarely-conjunctivitis, visual impairment, including blurred vision.
Allergic reactions: rarely-angioedema, anaphylactoid / anaphylactic reactions.
Interaction
When taken concomitantly with other NSAIDs, the risk of developing ulcerative lesions of the gastrointestinal tract and gastrointestinal bleeding increases. ; increases the concentration of Li+ in plasma when used concomitantly with Li+drugs;
reduces the effectiveness of IUDs, antihypertensive drugs;
indirect anticoagulants, ticlopidine, heparin, thrombolytics increase the risk of bleeding;
methotrexate increases the myelodepressive effect;
diuretics increase the risk of renal dysfunction;
cyclosporine increases the nephrotoxic effect; colestyramine accelerates excretion.
Myelotoxic drugs increase the manifestations of hematotoxicity of the drug.
How to take, course of use and dosage
Inside, with meals, in a daily dose of 7.5-15 mg.
The maximum daily dose is 15 mg, in patients with severe renal insufficiency who are on hemodialysis – 7.5 mg. With a slight or moderate decrease in renal function (creatinine clearance more than 25 ml/min), as well as with cirrhosis of the liver in a stable clinical condition, no dose adjustment is required. The initial dose in patients with an increased risk of side effects is 7.5 mg / day.
Rectally – 15 mg (one candle) 1 time a day.
Overdose
Symptoms: impaired consciousness, nausea, vomiting, epigastric pain, gastrointestinal bleeding, acute renal failure, acute liver failure, respiratory arrest, asystole.
Treatment: gastric lavage, taking activated charcoal, symptomatic therapy. Forced diuresis, urine alkalinization, and hemodialysis are ineffective due to the high degree of meloxicam binding to plasma proteins. There is no specific antidote.
Special instructions
In case of peptic ulcers or gastrointestinal bleeding, the development of side effects from the skin and mucous membranes, the drug should be discontinued.
Patients with reduced BCC and reduced glomerular filtration rate (dehydration, CHF, cirrhosis of the liver, nephrotic syndrome, clinically expressed kidney diseases, diuretics, dehydration after major surgical operations) may develop clinically expressed CRF, which is completely reversible after discontinuation of the drug (in such patients, daily diuresis and renal function should be monitored at the beginning of treatment). With a persistent and significant increase in transaminases and changes in other parameters. For liver function indicators, the drug should be discontinued and follow-up tests should be performed.
In patients with an increased risk of side effects, treatment begins with a dose of 7.5 mg. In end-stage CRF in patients undergoing dialysis, the dose should not exceed 7.5 mg / day. During the treatment period, care should be taken when driving vehicles and doing other activities. potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions (when dizziness and drowsiness occur). To reduce the risk of gastrointestinal adverse events, the minimum effective dose should be used in the shortest possible course.
Form of production
Pills.
Active ingredient
Meloxicam
Conditions of release from pharmacies
By prescription
Dosage form
Tablets
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