Composition, structure and packing
The tablets from light yellow to yellow, ploskotsilindricheskie, with beveled and risk tolerance of marbling.
1 tab. Meloxicam 7.5 mg - - 15 mg.
Excipients: potato starch, lactose monohydrate, povidone, trisodium citrate, magnesium stearate, colloidal silicon dioxide.
Clinico-pharmacological group: NSAID. Selective COX-2 inhibitor.
Pharmacological action
NSAIDs. Has anti-inflammatory, analgesic and antipyretic effect. Anti-inflammatory effect associated with inhibition of COX-2 - specific enzyme involved in the biosynthesis of prostaglandins in inflammation. To a lesser extent Meloxicam blocks the COX-1 involved in the synthesis of prostaglandin that protects the mucous membrane of the gastrointestinal tract and taking part in the regulation of blood flow in the kidneys.
Pharmacokinetics
Absorption
It is well absorbed from the gastrointestinal tract. The absolute bioavailability of meloxicam - 89%. Simultaneous ingestion does not alter absorption. When using the drug inside at doses 7.5 mg and 15 mg doses are proportional to its concentration.
Distribution
Css achieved in techenie3-5 days. With long-term use (more than 1 year) concentrations are similar to those that have been observed after the first reach a steady state pharmacokinetics. Binding to plasma proteins - more than 99%.
The vast differences between the maximum and basal concentrations of the drug after receiving a once a day is relatively small and at a dose of 7.5 mg of 0.4-1 mg / ml, a dose of 15 mg - 0.8-2 mg / ml. Meloxicam penetrates histohematogenous barriers, concentration in the synovial fluid reaches 50% Cmax plasma.
Metabolism
Meloxicam is almost completely metabolized in the liver with the formation of four pharmacologically inactive metabolites. The major metabolite, 5'-karboksimeloksikam (60% of the dose), formed by oxidation of the intermediate metabolite - 5'-gidroksimetilmeloksikama (9% of the dose).
In in vitro studies revealed that biotransformation occurs with the participation CYP2S9, the added value is isoenzyme CYP3A4. In the formation of two other metabolites (representing respectively 16% and 4% of the dose) is involved peroxidase activity which is likely to vary individually.
Withdrawal
We derive equally from the feces and urine, mostly as metabolites. With the feces as unchanged output of less than 5% of the daily dose in the urine as unchanged drug is found only in trace amounts. T1 / 2 - 15-20 h. The plasma clearance is approximately 8 ml / min.
Pharmacokinetics in special clinical situations
In the elderly clearance of the drug decreases. Vd is low and amounts to an average of 11 liters. In patients with hepatic or renal insufficiency moderately pharmacokinetics of meloxicam did not significantly change.
Statement
Cimptomaticheskaya therapy:
osteoarthritis;
rheumatoid arthritis;
ankylosing spondyloarthritis (Bechterew's disease);
other inflammatory and degenerative diseases associated with pain syndrome.
Dosage regimen
In rheumatoid arthritis the recommended dose is 15 mg / day, and after a therapeutic effect the dose can be reduced to 7.5 mg / day. In osteoarthrosis the drug administered in a dose of 7.5 mg / day, with no effect of the dose can be increased to 15 mg / day.
In ankylosing spondylitis daily dose is 15 mg. The maximum daily dose should not exceed 15 mg. Drugs are taken by mouth 1 time per day during meals.
In patients with increased risk of side effects, as well as in patients with severe impaired renal function who are on hemodialysis, the dose should not exceed 7.5 mg / day. Patients with impaired renal function (CC> 25 ml / min), dosage regimen adjustment is not required.
Side effect
On the part of the digestive system: nausea, vomiting, abdominal pain, diarrhea, constipation, flatulence, erosive and ulcerative lesions gastrointestinal tract, perforation of stomach or intestinal bleeding from the gastrointestinal tract (implicit or explicit), increase in liver enzymes, hepatitis, colitis, stomatitis, dry mouth, esophagitis.
Since the cardiovascular system: tachycardia, increased blood pressure, feeling the tides.
On the part of the respiratory system: exacerbation of bronchial asthma, cough.
From the CNS: headache, dizziness, tinnitus, disorientation, confusion of thoughts, sleep disturbance.
From the urinary system: edema, interstitial nephritis, renal medullary necrosis, urinary tract infection, proteinuria, hematuria, renal insufficiency.
From the side of the organ of vision: conjunctivitis, blurred vision.
Dermatological reactions: increased photosensitivity.
On the part of the hemopoietic system: anemia, leukopenia, thrombocytopenia. Allergic reactions: anaphylactoid reactions (including anaphylactic shock), swelling of the lips and tongue, allergic vasculitis, erythema multiforme exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), itching, skin rash or urticaria.
Other: fever.
Contraindications
stomach ulcer and duodenal ulcer exacerbation;
renal failure, severe (without dialysis);
severe hepatic insufficiency,
"Aspirin" bronchial asthma;
Children under 15 years
Pregnancy
Lactation (breastfeeding);
Hypersensitivity to the drug's components.
Precautions should be used drug in the elderly and in patients with erosive-ulcerative lesions of the gastrointestinal tract in history.
Pregnancy and lactation
The drug is contraindicated in pregnancy. If necessary, the appointment during lactation should resolve the issue of termination of breastfeeding.
Application for violations of liver function
Patients with hepatic insufficiency moderately pharmacokinetics of meloxicam did not significantly change. Should exercise caution and monitor indicators of renal function in the application of the drug in patients with cirrhosis.
Application for violations of renal function
In patients with renal insufficiency moderately pharmacokinetics of meloxicam did not significantly change. in patients with severe impaired renal function who are on hemodialysis, the dose should not exceed 7.5 mg / day. Patients with impaired renal function (spacecraft more than 25 ml / min), dosage regimen adjustment is not required.
Should exercise caution and monitor indicators of kidney function in the application of the drug in elderly patients, patients with chronic heart failure in patients with cirrhosis, as well as in patients with hypovolemia in surgical care.
Cautions
Caution must be exercised when applying the drug in patients with a history of ulcers of the stomach and duodenum, and patients receiving anticoagulant therapy. In these patients at increased risk of erosive and ulcerative lesions of the gastrointestinal tract.
Should exercise caution and monitor indicators of kidney function in the application of the drug in elderly patients, patients with chronic heart failure in patients with cirrhosis, as well as in patients with hypovolemia in surgical care.
Patients taking both diuretics and meloxicam, should receive plenty of fluids. Patients should be informed that, in allergic reactions (including itching, skin rash, urticaria, photosensitivity) should seek medical advice to address the issue of stopping.
Effects on ability to drive vehicles and management mechanisms
Use of the drug can cause the development of undesirable effects (including headaches, dizziness, drowsiness). Therefore should be abandoned vehicle management and maintenance arrangements that require concentration.
Overdose
Symptoms: impaired consciousness, nausea, vomiting, epigastric pain, bleeding from the gastrointestinal tract, acute renal failure, liver failure, respiratory arrest, asystole.
Treatment: gastric lavage, activated charcoal method (within 1 h after drug administration), if necessary, carry symptomatically. Kolestiramin accelerates the elimination of meloxicam from the body. Forced diuresis, alkalization of urine, hemodialysis is ineffective because of the high degree of binding of meloxicam with blood proteins. No specific antidote.
Drug Interactions
With simultaneous use of other NSAIDs (including with acetylsalicylic acid) increases the risk of erosive-ulcerative lesions and bleeding from the gastrointestinal tract. With the simultaneous use of antihypertensive drugs may reduce the effectiveness of the latter.
When applied simultaneously with the preparations of lithium may develop accumulation of lithium and increase its toxic action (recommended monitoring the concentration of lithium in the blood).
When applied simultaneously with methotrexate increases the risk of anemia and leukopenia (shown periodically, an overall analysis of blood). At simultaneous application with diuretics and cyclosporine increases the risk of renal failure.
With the simultaneous use of intrauterine contraceptive devices may reduce the effectiveness of the latter.
With the simultaneous use of anticoagulants (including those with heparin, ticlopidine, warfarin), as well as with thrombolytic drugs (including with streptokinase, fibrinolysin), an increased risk of bleeding (requires periodic monitoring of indicators of blood coagulation).
At simultaneous application with kolestiraminom increased excretion of meloxicam in the gastrointestinal tract.
Terms and Conditions of storage
The drug should be stored out of reach of children, dry, dark place. Shelf life - 2 years.
The tablets from light yellow to yellow, ploskotsilindricheskie, with beveled and risk tolerance of marbling.
1 tab. Meloxicam 7.5 mg - - 15 mg.
Excipients: potato starch, lactose monohydrate, povidone, trisodium citrate, magnesium stearate, colloidal silicon dioxide.
Clinico-pharmacological group: NSAID. Selective COX-2 inhibitor.
Pharmacological action
NSAIDs. Has anti-inflammatory, analgesic and antipyretic effect. Anti-inflammatory effect associated with inhibition of COX-2 - specific enzyme involved in the biosynthesis of prostaglandins in inflammation. To a lesser extent Meloxicam blocks the COX-1 involved in the synthesis of prostaglandin that protects the mucous membrane of the gastrointestinal tract and taking part in the regulation of blood flow in the kidneys.
Pharmacokinetics
Absorption
It is well absorbed from the gastrointestinal tract. The absolute bioavailability of meloxicam - 89%. Simultaneous ingestion does not alter absorption. When using the drug inside at doses 7.5 mg and 15 mg doses are proportional to its concentration.
Distribution
Css achieved in techenie3-5 days. With long-term use (more than 1 year) concentrations are similar to those that have been observed after the first reach a steady state pharmacokinetics. Binding to plasma proteins - more than 99%.
The vast differences between the maximum and basal concentrations of the drug after receiving a once a day is relatively small and at a dose of 7.5 mg of 0.4-1 mg / ml, a dose of 15 mg - 0.8-2 mg / ml. Meloxicam penetrates histohematogenous barriers, concentration in the synovial fluid reaches 50% Cmax plasma.
Metabolism
Meloxicam is almost completely metabolized in the liver with the formation of four pharmacologically inactive metabolites. The major metabolite, 5'-karboksimeloksikam (60% of the dose), formed by oxidation of the intermediate metabolite - 5'-gidroksimetilmeloksikama (9% of the dose).
In in vitro studies revealed that biotransformation occurs with the participation CYP2S9, the added value is isoenzyme CYP3A4. In the formation of two other metabolites (representing respectively 16% and 4% of the dose) is involved peroxidase activity which is likely to vary individually.
Withdrawal
We derive equally from the feces and urine, mostly as metabolites. With the feces as unchanged output of less than 5% of the daily dose in the urine as unchanged drug is found only in trace amounts. T1 / 2 - 15-20 h. The plasma clearance is approximately 8 ml / min.
Pharmacokinetics in special clinical situations
In the elderly clearance of the drug decreases. Vd is low and amounts to an average of 11 liters. In patients with hepatic or renal insufficiency moderately pharmacokinetics of meloxicam did not significantly change.
Statement
Cimptomaticheskaya therapy:
osteoarthritis;
rheumatoid arthritis;
ankylosing spondyloarthritis (Bechterew's disease);
other inflammatory and degenerative diseases associated with pain syndrome.
Dosage regimen
In rheumatoid arthritis the recommended dose is 15 mg / day, and after a therapeutic effect the dose can be reduced to 7.5 mg / day. In osteoarthrosis the drug administered in a dose of 7.5 mg / day, with no effect of the dose can be increased to 15 mg / day.
In ankylosing spondylitis daily dose is 15 mg. The maximum daily dose should not exceed 15 mg. Drugs are taken by mouth 1 time per day during meals.
In patients with increased risk of side effects, as well as in patients with severe impaired renal function who are on hemodialysis, the dose should not exceed 7.5 mg / day. Patients with impaired renal function (CC> 25 ml / min), dosage regimen adjustment is not required.
Side effect
On the part of the digestive system: nausea, vomiting, abdominal pain, diarrhea, constipation, flatulence, erosive and ulcerative lesions gastrointestinal tract, perforation of stomach or intestinal bleeding from the gastrointestinal tract (implicit or explicit), increase in liver enzymes, hepatitis, colitis, stomatitis, dry mouth, esophagitis.
Since the cardiovascular system: tachycardia, increased blood pressure, feeling the tides.
On the part of the respiratory system: exacerbation of bronchial asthma, cough.
From the CNS: headache, dizziness, tinnitus, disorientation, confusion of thoughts, sleep disturbance.
From the urinary system: edema, interstitial nephritis, renal medullary necrosis, urinary tract infection, proteinuria, hematuria, renal insufficiency.
From the side of the organ of vision: conjunctivitis, blurred vision.
Dermatological reactions: increased photosensitivity.
On the part of the hemopoietic system: anemia, leukopenia, thrombocytopenia. Allergic reactions: anaphylactoid reactions (including anaphylactic shock), swelling of the lips and tongue, allergic vasculitis, erythema multiforme exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), itching, skin rash or urticaria.
Other: fever.
Contraindications
stomach ulcer and duodenal ulcer exacerbation;
renal failure, severe (without dialysis);
severe hepatic insufficiency,
"Aspirin" bronchial asthma;
Children under 15 years
Pregnancy
Lactation (breastfeeding);
Hypersensitivity to the drug's components.
Precautions should be used drug in the elderly and in patients with erosive-ulcerative lesions of the gastrointestinal tract in history.
Pregnancy and lactation
The drug is contraindicated in pregnancy. If necessary, the appointment during lactation should resolve the issue of termination of breastfeeding.
Application for violations of liver function
Patients with hepatic insufficiency moderately pharmacokinetics of meloxicam did not significantly change. Should exercise caution and monitor indicators of renal function in the application of the drug in patients with cirrhosis.
Application for violations of renal function
In patients with renal insufficiency moderately pharmacokinetics of meloxicam did not significantly change. in patients with severe impaired renal function who are on hemodialysis, the dose should not exceed 7.5 mg / day. Patients with impaired renal function (spacecraft more than 25 ml / min), dosage regimen adjustment is not required.
Should exercise caution and monitor indicators of kidney function in the application of the drug in elderly patients, patients with chronic heart failure in patients with cirrhosis, as well as in patients with hypovolemia in surgical care.
Cautions
Caution must be exercised when applying the drug in patients with a history of ulcers of the stomach and duodenum, and patients receiving anticoagulant therapy. In these patients at increased risk of erosive and ulcerative lesions of the gastrointestinal tract.
Should exercise caution and monitor indicators of kidney function in the application of the drug in elderly patients, patients with chronic heart failure in patients with cirrhosis, as well as in patients with hypovolemia in surgical care.
Patients taking both diuretics and meloxicam, should receive plenty of fluids. Patients should be informed that, in allergic reactions (including itching, skin rash, urticaria, photosensitivity) should seek medical advice to address the issue of stopping.
Effects on ability to drive vehicles and management mechanisms
Use of the drug can cause the development of undesirable effects (including headaches, dizziness, drowsiness). Therefore should be abandoned vehicle management and maintenance arrangements that require concentration.
Overdose
Symptoms: impaired consciousness, nausea, vomiting, epigastric pain, bleeding from the gastrointestinal tract, acute renal failure, liver failure, respiratory arrest, asystole.
Treatment: gastric lavage, activated charcoal method (within 1 h after drug administration), if necessary, carry symptomatically. Kolestiramin accelerates the elimination of meloxicam from the body. Forced diuresis, alkalization of urine, hemodialysis is ineffective because of the high degree of binding of meloxicam with blood proteins. No specific antidote.
Drug Interactions
With simultaneous use of other NSAIDs (including with acetylsalicylic acid) increases the risk of erosive-ulcerative lesions and bleeding from the gastrointestinal tract. With the simultaneous use of antihypertensive drugs may reduce the effectiveness of the latter.
When applied simultaneously with the preparations of lithium may develop accumulation of lithium and increase its toxic action (recommended monitoring the concentration of lithium in the blood).
When applied simultaneously with methotrexate increases the risk of anemia and leukopenia (shown periodically, an overall analysis of blood). At simultaneous application with diuretics and cyclosporine increases the risk of renal failure.
With the simultaneous use of intrauterine contraceptive devices may reduce the effectiveness of the latter.
With the simultaneous use of anticoagulants (including those with heparin, ticlopidine, warfarin), as well as with thrombolytic drugs (including with streptokinase, fibrinolysin), an increased risk of bleeding (requires periodic monitoring of indicators of blood coagulation).
At simultaneous application with kolestiraminom increased excretion of meloxicam in the gastrointestinal tract.
Terms and Conditions of storage
The drug should be stored out of reach of children, dry, dark place. Shelf life - 2 years.
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