Solution for intramuscular administration of yellow or greenish-yellow color, transparent in 1 ml meloxicam 10 mg, in ampoules of 1.5 ml.
GENITRON® (MELOXICAM)
Solution for intramuscular administration, yellow or greenish-yellow, transparent
1 ml meloxicam 10 mg
Excipients: meglumine (N-methylglucamine) - 7 mg, glycine - 6 mg, poloxamer 188 - 50 mg, tetrahydrofurfuryl macrogol (glycofurol) - 100 mg, sodium chloride - 3.5 mg, 0.1M sodium hydroxide solution - up to pH 8.4-8.9 , water d/i - up to 1 ml.
1.5 ml - colorless glass ampoules (5) - cardboard packs with insert.
1.5 ml - colorless glass ampoules (3) - blisters made of PVC film (1) - cardboard packs.
1.5 ml - colorless glass ampoules (5) - blisters made of PVC film (1) - cardboard packs.
1 ml meloxicam 10 mg
Excipients: meglumine (N-methylglucamine) - 7 mg, glycine - 6 mg, poloxamer 188 - 50 mg, tetrahydrofurfuryl macrogol (glycofurol) - 100 mg, sodium chloride - 3.5 mg, 0.1M sodium hydroxide solution - up to pH 8.4-8.9 , water d/i - up to 1 ml.
1.5 ml - colorless glass ampoules (5) - cardboard packs with insert.
1.5 ml - colorless glass ampoules (3) - blisters made of PVC film (1) - cardboard packs.
1.5 ml - colorless glass ampoules (5) - blisters made of PVC film (1) - cardboard packs.
Meloxicam belongs to the oxicam class of NSAIDs, is a derivative of enolic acid and has anti-inflammatory, analgesic and antipyretic effects. The pronounced anti-inflammatory effect of meloxicam has been established in all standard models of inflammation.
The mechanism of action of meloxicam is its ability to inhibit the synthesis of prostaglandins (known mediators of inflammation) as a result of selective suppression of the enzymatic activity of COX-2. When prescribed in high doses, long-term use and individual characteristics of the body, the selectivity of COX-2 inhibition is reduced.
Meloxicam in vivo inhibits the synthesis of prostaglandins at the site of inflammation to a greater extent than in the gastric mucosa or kidneys. These differences are associated with more selective inhibition of COX-2 compared to COX-1. Inhibition of COX-2 is thought to provide the therapeutic effect of NSAIDs, whereas inhibition of the constitutively present COX-1 isoenzyme may be responsible for gastric and renal side effects. The selectivity of meloxicam for COX-2 has been confirmed in various test systems, both in vitro and in vivo. The selective ability of meloxicam to inhibit COX-2 was demonstrated when using human whole blood as a test system in vitro. It was found that meloxicam (in doses of 7.5 mg and 15 mg) more actively inhibited COX-2, having a greater inhibitory effect on the production of prostaglandin E2 stimulated by lipopolysaccharide (reaction controlled by COX-2) than on the production of thromboxane, which is involved in the blood coagulation process ( reaction controlled by COX-1). These effects were dose dependent. Ex vivo studies showed that meloxicam (at doses of 7.5 mg and 15 mg) had no effect on platelet aggregation and bleeding time.
The mechanism of action of meloxicam is its ability to inhibit the synthesis of prostaglandins (known mediators of inflammation) as a result of selective suppression of the enzymatic activity of COX-2. When prescribed in high doses, long-term use and individual characteristics of the body, the selectivity of COX-2 inhibition is reduced.
Meloxicam in vivo inhibits the synthesis of prostaglandins at the site of inflammation to a greater extent than in the gastric mucosa or kidneys. These differences are associated with more selective inhibition of COX-2 compared to COX-1. Inhibition of COX-2 is thought to provide the therapeutic effect of NSAIDs, whereas inhibition of the constitutively present COX-1 isoenzyme may be responsible for gastric and renal side effects. The selectivity of meloxicam for COX-2 has been confirmed in various test systems, both in vitro and in vivo. The selective ability of meloxicam to inhibit COX-2 was demonstrated when using human whole blood as a test system in vitro. It was found that meloxicam (in doses of 7.5 mg and 15 mg) more actively inhibited COX-2, having a greater inhibitory effect on the production of prostaglandin E2 stimulated by lipopolysaccharide (reaction controlled by COX-2) than on the production of thromboxane, which is involved in the blood coagulation process ( reaction controlled by COX-1). These effects were dose dependent. Ex vivo studies showed that meloxicam (at doses of 7.5 mg and 15 mg) had no effect on platelet aggregation and bleeding time.
Suction
After oral administration, meloxicam is well absorbed from the gastrointestinal tract, as evidenced by its high absolute bioavailability (90%). After a single use of meloxicam, Cmax in plasma is achieved within 5-6 hours. Simultaneous intake of food and antacids does not change absorption. When using the drug orally (in doses of 7.5 and 15 mg), its concentrations are proportional to the doses. Css is achieved within 3-5 days. The range of differences between the maximum and minimum concentrations of the drug after taking it once a day is relatively small and amounts to 0.4-1.0 mcg/ml when using the drug at a dose of 7.5 mg, when using the drug at a dose of 15 mg - 0.8-2.0 mcg/ml (values are given respectively Cmin and Cmax in the equilibrium state), although values outside the specified range were also noted. Cmax of meloxicam in plasma at steady state is achieved within 5-6 hours after oral administration.
After intramuscular administration, meloxicam is completely absorbed. The bioavailability of the drug is about 100%. After intramuscular administration of meloxicam at a dose of 15 mg, Cmax in plasma is achieved in approximately 1 hour.
Distribution
Meloxicam binds very well to plasma proteins, especially albumin (99%). Penetrates through histohematic barriers, as well as into synovial fluid. The concentration in synovial fluid is approximately 50% of the plasma concentration. Vd after repeated oral administration of meloxicam (in doses from 7.5 mg to 15 mg) is about 16 l, with a coefficient of variation from 11% to 32%; with intramuscular administration, Vd is 11 l.
Metabolism
Meloxicam is almost completely metabolized in the liver to form 4 pharmacologically inactive derivatives. The main metabolite, 5'-carboxymeloxicam (60% of the administered dose), is formed by oxidation of an intermediate metabolite, 5'-hydroxymethylmeloxicam, which is also excreted, but to a lesser extent (9% of the administered dose). In vitro studies have shown that the CYP2C9 isoenzyme plays an important role in this metabolic transformation; the CYP3A4 isoenzyme is of additional importance. Peroxidase, the activity of which varies individually, takes part in the formation of the other two metabolites (constituting 16% and 4% of the administered dose of the drug, respectively).
Removal
It is excreted equally through the intestines and kidneys, exclusively in the form of metabolites. Less than 5% of the daily dose is excreted unchanged through the intestines; the drug is found unchanged in urine only in the following quantities. The average T1/2 of meloxicam decreases from 13 to 25 hours (with intramuscular administration - 20 hours). Plasma clearance averages 7-12 ml/min after a single dose of meloxicam, with intramuscular administration - 8 ml/min.
Pharmacokinetics for selected patient groups
Liver dysfunction and mild to moderate renal failure have no medical impact on the pharmacokinetics of meloxime. The rate of elimination of meloxicam from the body is significantly higher in patients with moderate renal failure. Meloxicam binds poorly to brain proteins in patients with end-stage renal disease. In end-stage renal failure, an increase in Vd may lead to a lower concentration of free meloxicam, so in such patients the daily dose should not exceed 7.5 mg. Elderly patients compared to young patients have similar pharmacokinetic parameters. In elderly patients, the mean plasma clearance at steady state is slightly lower than in younger patients. Elderly women have higher AUC values and longer T1/2 compared to young patients of both sexes.
After oral administration, meloxicam is well absorbed from the gastrointestinal tract, as evidenced by its high absolute bioavailability (90%). After a single use of meloxicam, Cmax in plasma is achieved within 5-6 hours. Simultaneous intake of food and antacids does not change absorption. When using the drug orally (in doses of 7.5 and 15 mg), its concentrations are proportional to the doses. Css is achieved within 3-5 days. The range of differences between the maximum and minimum concentrations of the drug after taking it once a day is relatively small and amounts to 0.4-1.0 mcg/ml when using the drug at a dose of 7.5 mg, when using the drug at a dose of 15 mg - 0.8-2.0 mcg/ml (values are given respectively Cmin and Cmax in the equilibrium state), although values outside the specified range were also noted. Cmax of meloxicam in plasma at steady state is achieved within 5-6 hours after oral administration.
After intramuscular administration, meloxicam is completely absorbed. The bioavailability of the drug is about 100%. After intramuscular administration of meloxicam at a dose of 15 mg, Cmax in plasma is achieved in approximately 1 hour.
Distribution
Meloxicam binds very well to plasma proteins, especially albumin (99%). Penetrates through histohematic barriers, as well as into synovial fluid. The concentration in synovial fluid is approximately 50% of the plasma concentration. Vd after repeated oral administration of meloxicam (in doses from 7.5 mg to 15 mg) is about 16 l, with a coefficient of variation from 11% to 32%; with intramuscular administration, Vd is 11 l.
Metabolism
Meloxicam is almost completely metabolized in the liver to form 4 pharmacologically inactive derivatives. The main metabolite, 5'-carboxymeloxicam (60% of the administered dose), is formed by oxidation of an intermediate metabolite, 5'-hydroxymethylmeloxicam, which is also excreted, but to a lesser extent (9% of the administered dose). In vitro studies have shown that the CYP2C9 isoenzyme plays an important role in this metabolic transformation; the CYP3A4 isoenzyme is of additional importance. Peroxidase, the activity of which varies individually, takes part in the formation of the other two metabolites (constituting 16% and 4% of the administered dose of the drug, respectively).
Removal
It is excreted equally through the intestines and kidneys, exclusively in the form of metabolites. Less than 5% of the daily dose is excreted unchanged through the intestines; the drug is found unchanged in urine only in the following quantities. The average T1/2 of meloxicam decreases from 13 to 25 hours (with intramuscular administration - 20 hours). Plasma clearance averages 7-12 ml/min after a single dose of meloxicam, with intramuscular administration - 8 ml/min.
Pharmacokinetics for selected patient groups
Liver dysfunction and mild to moderate renal failure have no medical impact on the pharmacokinetics of meloxime. The rate of elimination of meloxicam from the body is significantly higher in patients with moderate renal failure. Meloxicam binds poorly to brain proteins in patients with end-stage renal disease. In end-stage renal failure, an increase in Vd may lead to a lower concentration of free meloxicam, so in such patients the daily dose should not exceed 7.5 mg. Elderly patients compared to young patients have similar pharmacokinetic parameters. In elderly patients, the mean plasma clearance at steady state is slightly lower than in younger patients. Elderly women have higher AUC values and longer T1/2 compared to young patients of both sexes.
Short-term symptomatic therapy for:
osteoarthritis (arthrosis, degenerative joint diseases), incl. with a pain component; rheumatoid arthritis; ankylosing spondylitis (Bechterew's disease). The causes of pain and exacerbation during use, the progression of the disease is not affected.
osteoarthritis (arthrosis, degenerative joint diseases), incl. with a pain component; rheumatoid arthritis; ankylosing spondylitis (Bechterew's disease). The causes of pain and exacerbation during use, the progression of the disease is not affected.
Solution for intramuscular administration
The drug is administered deep intramuscularly. The drug cannot be administered intravenously.
The recommended dose is 7.5 mg (0.75 ml) or 15 mg (1.5 ml) 1 time / day, depending on the intensity of pain and the severity of the inflammatory process. The maximum recommended daily dose is 15 mg (1.5 ml).
In patients with severe renal failure on hemodialysis and patients with an increased risk of adverse reactions, the dose should not exceed 7.5 mg (0.75 ml) / day. For patients with mild or moderate renal failure (creatinine clearance more than 30 ml/min), no dose adjustment is required.
The drug should not be used simultaneously with other NSAIDs.
The total daily dose of meloxicam, used in the form of tablets, suppositories, oral suspension and injections, should not exceed 15 mg.
Due to possible incompatibility, meloxicam should not be mixed in the same syringe with other drugs.
The drug is administered deep intramuscularly. The drug cannot be administered intravenously.
The recommended dose is 7.5 mg (0.75 ml) or 15 mg (1.5 ml) 1 time / day, depending on the intensity of pain and the severity of the inflammatory process. The maximum recommended daily dose is 15 mg (1.5 ml).
In patients with severe renal failure on hemodialysis and patients with an increased risk of adverse reactions, the dose should not exceed 7.5 mg (0.75 ml) / day. For patients with mild or moderate renal failure (creatinine clearance more than 30 ml/min), no dose adjustment is required.
The drug should not be used simultaneously with other NSAIDs.
The total daily dose of meloxicam, used in the form of tablets, suppositories, oral suspension and injections, should not exceed 15 mg.
Due to possible incompatibility, meloxicam should not be mixed in the same syringe with other drugs.
The adverse events presented below are listed depending on the anatomical and physiological classification and frequency of occurrence. The frequency of occurrence is determined by WHO and has the following gradation: very often (>10%); often (>1% and <10%); uncommon (>0.1% and <1%); rare (>0.01% and <0.1%); very rare (less than 0.01%, including isolated cases).
From the hematopoietic system: infrequently - anemia; rarely - changes in the number of blood cells, including changes in the leukocyte formula, leukopenia, thrombocytopenia.
From the immune system: not established - anaphylactic shock, anaphylactoid/anaphylactic conditions, other hypersensitivity reactions.
From the nervous system: often - headache; infrequently - dizziness, drowsiness.
Mental disorders: often - emotional lability; not established - confusion, disorientation.
From the angle of view: rarely - conjunctivitis, visual impairment, including blurred vision.
From the organ of hearing: infrequently - vertigo; rarely - tinnitus.
From the digestive system: often - abdominal pain, dyspepsia, diarrhea, nausea, vomiting; uncommon - hidden or obvious gastrointestinal bleeding, gastritis, stomatitis, constipation, bloating, belching; rarely - gastroduodenal ulcers, colitis, esophagitis; very rarely - perforation of the gastrointestinal tract.
From the liver and biliary tract: infrequently - transient changes in liver function indicators (for example, increased activity of transaminases or bilirubin); very rarely - hepatitis.
From the skin and subcutaneous tissues: infrequently - angioedema, itching, skin rash; rarely - urticaria, toxic epidermal necrolysis, Stevens-Johnson syndrome; very rarely - bullous dermatitis, erythema multiforme; not established - photosensitivity.
From the respiratory system: rarely - bronchial asthma in patients with allergies to acetylsalicylic acid or other NSAIDs.
From the cardiovascular system: infrequently - increased blood pressure, a feeling of a “rush” of blood to the face; rarely - a feeling of palpitations.
From the urinary system: infrequently - changes in kidney function indicators (increased concentrations of creatinine and/or urea in the blood serum), urinary disorders, including acute urinary retention; very rarely - acute renal failure.
Other: often - peripheral edema, swelling and pain at the injection site (solution for intramuscular administration).
Concomitant use with drugs that suppress bone marrow (for example, methotrexate) may cause cytopenia.
Gastrointestinal bleeding, ulceration, or perforation can be fatal.
As with other NSAIDs, the possibility of interstitial nephritis, glomerulonephritis, renal medullary necrosis, and nephrotic syndrome cannot be ruled out.
From the hematopoietic system: infrequently - anemia; rarely - changes in the number of blood cells, including changes in the leukocyte formula, leukopenia, thrombocytopenia.
From the immune system: not established - anaphylactic shock, anaphylactoid/anaphylactic conditions, other hypersensitivity reactions.
From the nervous system: often - headache; infrequently - dizziness, drowsiness.
Mental disorders: often - emotional lability; not established - confusion, disorientation.
From the angle of view: rarely - conjunctivitis, visual impairment, including blurred vision.
From the organ of hearing: infrequently - vertigo; rarely - tinnitus.
From the digestive system: often - abdominal pain, dyspepsia, diarrhea, nausea, vomiting; uncommon - hidden or obvious gastrointestinal bleeding, gastritis, stomatitis, constipation, bloating, belching; rarely - gastroduodenal ulcers, colitis, esophagitis; very rarely - perforation of the gastrointestinal tract.
From the liver and biliary tract: infrequently - transient changes in liver function indicators (for example, increased activity of transaminases or bilirubin); very rarely - hepatitis.
From the skin and subcutaneous tissues: infrequently - angioedema, itching, skin rash; rarely - urticaria, toxic epidermal necrolysis, Stevens-Johnson syndrome; very rarely - bullous dermatitis, erythema multiforme; not established - photosensitivity.
From the respiratory system: rarely - bronchial asthma in patients with allergies to acetylsalicylic acid or other NSAIDs.
From the cardiovascular system: infrequently - increased blood pressure, a feeling of a “rush” of blood to the face; rarely - a feeling of palpitations.
From the urinary system: infrequently - changes in kidney function indicators (increased concentrations of creatinine and/or urea in the blood serum), urinary disorders, including acute urinary retention; very rarely - acute renal failure.
Other: often - peripheral edema, swelling and pain at the injection site (solution for intramuscular administration).
Concomitant use with drugs that suppress bone marrow (for example, methotrexate) may cause cytopenia.
Gastrointestinal bleeding, ulceration, or perforation can be fatal.
As with other NSAIDs, the possibility of interstitial nephritis, glomerulonephritis, renal medullary necrosis, and nephrotic syndrome cannot be ruled out.
Complete or incomplete combination of bronchial asthma, angioedema or urticaria, recurrent polyposis of the nose and paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (including a history); erosive and ulcerative lesions of the mucous membrane of the stomach and duodenum in the acute stage or recently suffered; inflammatory bowel diseases (Crohn's disease or ulcerative colitis in the acute stage); severe liver failure or active liver disease; severe renal failure with CC less than 30 ml/min (in patients not undergoing hemodialysis with confirmed hyperkalemia); progressive kidney disease; active gastrointestinal bleeding; recent cerebrovascular bleeding or a confirmed diagnosis of diseases of the blood coagulation system; thyroid diseases (for tablets); decompensated heart failure; acute myocardial infarction; period after coronary artery bypass surgery; pregnancy; lactation period (breastfeeding); children under 12 years of age (for tablets); children and adolescents up to 18 years of age (for solution for intramuscular administration); hereditary lactose intolerance, impaired absorption of glucose and galactose, lactase deficiency (for tablets); hypersensitivity to the active substance or auxiliary components of the drug (including other NSAIDs).
Carefully:history of gastrointestinal diseases (peptic ulcer of the stomach and duodenum, liver disease), the presence of Helicobacter pylori infection; IHD, chronic heart failure; cerebrovascular diseases; moderate renal failure (creatinine clearance 30-60 ml/min); dyslipidemia/hyperlipidemia; diabetes; simultaneous use of oral corticosteroids (including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline); severe somatic diseases; peripheral arterial disease; elderly age; long-term use of NSAIDs; smoking; frequent drinking of alcohol; severe somatic diseases; bronchial asthma; tuberculosis; severe osteoporosis. To reduce the risk of developing adverse events from the gastrointestinal tract, the minimum effective dose should be used for the shortest possible short course. It is known that NSAIDs pass into breast milk, so the use of the drug during breastfeeding is contraindicated.
As a drug that inhibits COX/prostaglandin synthesis, Genitron® may affect fertility and is therefore not recommended for women planning pregnancy. Meloxicam may delay ovulation. In this regard, in women who have problems conceiving and are undergoing examination for such problems, it is recommended to discontinue taking the drug Genitron®.
Use for liver dysfunction
The use of the drug is contraindicated in severe liver failure or active liver disease.
In patients with liver cirrhosis (compensated), no dose adjustment is required.
Use for renal impairment
The use of the drug is contraindicated in severe renal failure with CC less than 30 ml/min (in patients not undergoing hemodialysis with confirmed hyperkalemia), progressive kidney diseases.
In patients with moderate renal failure (creatinine clearance 30-60 ml/min), the drug should be prescribed with caution.
Use in children
The drug is contraindicated for use in children under 12 years of age (tablets), and in children under 18 years of age (solution for intramuscular administration).
Use in elderly patients
The drug should be prescribed with caution to elderly patients.
Carefully:history of gastrointestinal diseases (peptic ulcer of the stomach and duodenum, liver disease), the presence of Helicobacter pylori infection; IHD, chronic heart failure; cerebrovascular diseases; moderate renal failure (creatinine clearance 30-60 ml/min); dyslipidemia/hyperlipidemia; diabetes; simultaneous use of oral corticosteroids (including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline); severe somatic diseases; peripheral arterial disease; elderly age; long-term use of NSAIDs; smoking; frequent drinking of alcohol; severe somatic diseases; bronchial asthma; tuberculosis; severe osteoporosis. To reduce the risk of developing adverse events from the gastrointestinal tract, the minimum effective dose should be used for the shortest possible short course. It is known that NSAIDs pass into breast milk, so the use of the drug during breastfeeding is contraindicated.
As a drug that inhibits COX/prostaglandin synthesis, Genitron® may affect fertility and is therefore not recommended for women planning pregnancy. Meloxicam may delay ovulation. In this regard, in women who have problems conceiving and are undergoing examination for such problems, it is recommended to discontinue taking the drug Genitron®.
Use for liver dysfunction
The use of the drug is contraindicated in severe liver failure or active liver disease.
In patients with liver cirrhosis (compensated), no dose adjustment is required.
Use for renal impairment
The use of the drug is contraindicated in severe renal failure with CC less than 30 ml/min (in patients not undergoing hemodialysis with confirmed hyperkalemia), progressive kidney diseases.
In patients with moderate renal failure (creatinine clearance 30-60 ml/min), the drug should be prescribed with caution.
Use in children
The drug is contraindicated for use in children under 12 years of age (tablets), and in children under 18 years of age (solution for intramuscular administration).
Use in elderly patients
The drug should be prescribed with caution to elderly patients.
Because The potential risk of adverse reactions depends on the dose and duration of treatment, the minimum effective dose should be used for the shortest possible short course.
The duration of treatment is determined individually depending on the course of the disease and the effectiveness of the therapy.
Patients with gastrointestinal diseases should undergo regular examination when using the drug Genitron®. The drug should not be prescribed to patients with peptic ulcers or gastrointestinal bleeding. At any time during treatment, with or without previous symptoms or a history of serious gastrointestinal disease, potentially fatal gastrointestinal bleeding, ulceration, or perforation may occur. If ulcerative lesions of the gastrointestinal tract or gastrointestinal bleeding occur, the drug must be discontinued. The most serious effects were observed in older people.
In patients with cardiovascular diseases or with risk factors for the development of such diseases, NSAIDs can increase the risk of serious cardiovascular thrombotic events, myocardial infarction, angina attack and stroke, which can be fatal. With an increase in the duration of treatment, this risk may increase.
NSAIDs can increase sodium, potassium and water retention and reduce the natriuretic effects of diuretics. As a consequence, predisposed patients may experience or increase heart failure or hypertension. Clinical monitoring is recommended for such patients, and adequate hydration should be maintained. Before starting treatment, it is necessary to study kidney function. In the case of combination therapy, renal function should also be monitored.
In patients with reduced renal blood flow, the use of NSAIDs (NSAIDs inhibit the synthesis of renal prostaglandin, which plays an important role in maintaining renal blood flow) can cause renal failure, which occurs when anti-inflammatory therapy with nonsteroidal drugs is discontinued. The greatest risk of such a reaction occurs in elderly patients, with dehydration, with chronic heart failure, cirrhosis of the liver, nephrotic syndrome, chronic kidney disease, who receive concomitant therapy with diuretic drugs, ACE inhibitors or angiotensin II receptor antagonists, or after extensive surgical interventions that led to hypovolemia. Such patients need to monitor diuresis and renal function at the beginning of therapy. In isolated cases, NSAIDs can lead to interstitial nephritis, glomerulonephritis, renal medular necrosis or the development of nephrotic syndrome.
In the treatment of NSAIDs, individual cases of increased activity of transaminases or other indicators of liver function have been described, which in most cases were insignificant and temporary. In case of persistent and significant deviation from the norm, treatment with Genitron® should be discontinued and control tests should be performed. In clinically stable patients with cirrhosis of the liver, there is no need to reduce the dose of Genitron®, it is necessary to monitor the detected laboratory changes.
Weakened patients need more careful monitoring, since their side effects are more severe. As with the treatment of other NSAIDs, the drug should be prescribed with caution to elderly patients who are more likely to have a decrease in kidney, liver and heart function.
The drug Genitron®, like any other NSAID, can mask the symptoms of the underlying infectious disease.
In very rare cases, serious skin reactions (some of them fatal) have been observed with the use of NSAIDs, including exfoliative dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis. A high risk of such reactions is observed at the beginning of treatment, while in most cases such reactions appeared during the first month of treatment. At the first appearance of skin rashes, lesions of the mucous membranes or other signs of hypersensitivity, it is necessary to stop using the drug Genitron®. Due to the possible occurrence of side effects with localization on the skin and mucous membranes, special attention should be paid to the appearance of appropriate symptoms. If side effects occur, treatment with the drug should be discontinued.
Influence on the ability to drive vehicles and manage mechanisms
During the treatment period, it is possible to reduce the speed of mental and motor reactions, therefore it is necessary to refrain from driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.
Overdose
Symptoms: drowsiness, impaired consciousness, nausea, vomiting, epigastric pain, gastrointestinal bleeding, acute renal failure, liver failure, arterial hypertension, arterial hypotension, respiratory arrest, asystole.
Treatment: there is no specific antidote. In case of an overdose of the drug, symptomatic therapy is carried out; in case of an overdose of the drug in the form of tablets, gastric lavage, taking activated charcoal. Forced diuresis, urine alkalinization, hemodialysis are ineffective due to the high degree of binding of the drug to blood proteins.
Drug interaction
When used concomitantly with other prostaglandin synthesis inhibitors, including GCS and salicylates, meloxicam may increase the risk of gastrointestinal mucosal ulcers and gastrointestinal bleeding due to their synergism.
The co-administration of meloxicam and other NSAIDs is not recommended.
Together with anticoagulants, heparin for systemic use, and thrombolytic agents, meloxicam increases the risk of bleeding. If it is impossible to avoid their simultaneous use, it is necessary to monitor the indicators of the blood coagulation system.
Simultaneous administration with meloxicam of antiplatelet drugs, serotonin reuptake inhibitors increases the risk of bleeding due to inhibition of platelet function. In the case of simultaneous use, careful monitoring of the blood coagulation system is necessary.
Meloxicam can reduce the renal excretion of lithium, which leads to an increase in its concentration in blood plasma to a toxic level. Simultaneous use of meloxicam with lithium preparations is not recommended. If simultaneous use is necessary, careful monitoring of the concentration of lithium in plasma is recommended throughout the course of the use of lithium preparations.
NSAIDs reduce the excretion of methotrexate by the kidneys, thereby increasing its concentration in plasma. Simultaneous use of meloxicam and methotrexate (at a dose of more than 15 mg per week) is not recommended. The risk of interaction between NSAIDs and methotrexate may also occur in patients using methotrexate in low doses, especially in patients with impaired renal function. In case of simultaneous use, careful monitoring of kidney function and blood formula is necessary. Meloxicam may increase the hematological toxicity of methotrexate, especially in patients with impaired renal function. When meloxicam and methotrexate are used together for 3 days, the risk of increased toxicity of the latter increases.
There is evidence that meloxicam can reduce the effectiveness of intrauterine contraceptives, but this has not been proven.
When using meloxicam together with diuretics, there may be a risk of acute renal failure, therefore, kidney function should be monitored and an adequate level of hydration should be maintained.
Meloxicam reduces the effect of antihypertensive agents (beta-blockers, ACE inhibitors, vasodilators, diuretics) due to inhibition of prostaglandins with vasodilating properties.
Meloxicam and angiotensin II receptor antagonists, as well as ACE inhibitors, have a synergistic effect on reducing glomerular filtration. In patients with existing renal dysfunction, this can lead to acute renal failure.
Colestyramine, binding meloxicam in the gastrointestinal tract, leads to its faster excretion.
Meloxicam, affecting renal prostaglandins, enhances the nephrotoxicity of cyclosporine, which requires enhanced monitoring of kidney function with simultaneous use of drugs.
Meloxicam is almost completely destroyed by hepatic metabolism, approximately 2/3 of which are carried out with the participation of cytochrome (CYP) P450 and 1/3 - by peroxidase oxidation. Pharmacokinetic interaction of meloxicam and other drugs at the stage of metabolism is possible due to their effect on SUR2C9 and / or SUR3A4.
When used simultaneously with hypoglycemic agents for oral administration, meloxicam may enhance their effect, thereby contributing to the risk of hypoglycemia.
Meloxicam can weaken the effect of digoxin, cortisone, diuretics.
With simultaneous administration of meloxicam with antacids, cimetidine, digoxin and furosemide, interaction at the pharmacokinetic level was not revealed.
The duration of treatment is determined individually depending on the course of the disease and the effectiveness of the therapy.
Patients with gastrointestinal diseases should undergo regular examination when using the drug Genitron®. The drug should not be prescribed to patients with peptic ulcers or gastrointestinal bleeding. At any time during treatment, with or without previous symptoms or a history of serious gastrointestinal disease, potentially fatal gastrointestinal bleeding, ulceration, or perforation may occur. If ulcerative lesions of the gastrointestinal tract or gastrointestinal bleeding occur, the drug must be discontinued. The most serious effects were observed in older people.
In patients with cardiovascular diseases or with risk factors for the development of such diseases, NSAIDs can increase the risk of serious cardiovascular thrombotic events, myocardial infarction, angina attack and stroke, which can be fatal. With an increase in the duration of treatment, this risk may increase.
NSAIDs can increase sodium, potassium and water retention and reduce the natriuretic effects of diuretics. As a consequence, predisposed patients may experience or increase heart failure or hypertension. Clinical monitoring is recommended for such patients, and adequate hydration should be maintained. Before starting treatment, it is necessary to study kidney function. In the case of combination therapy, renal function should also be monitored.
In patients with reduced renal blood flow, the use of NSAIDs (NSAIDs inhibit the synthesis of renal prostaglandin, which plays an important role in maintaining renal blood flow) can cause renal failure, which occurs when anti-inflammatory therapy with nonsteroidal drugs is discontinued. The greatest risk of such a reaction occurs in elderly patients, with dehydration, with chronic heart failure, cirrhosis of the liver, nephrotic syndrome, chronic kidney disease, who receive concomitant therapy with diuretic drugs, ACE inhibitors or angiotensin II receptor antagonists, or after extensive surgical interventions that led to hypovolemia. Such patients need to monitor diuresis and renal function at the beginning of therapy. In isolated cases, NSAIDs can lead to interstitial nephritis, glomerulonephritis, renal medular necrosis or the development of nephrotic syndrome.
In the treatment of NSAIDs, individual cases of increased activity of transaminases or other indicators of liver function have been described, which in most cases were insignificant and temporary. In case of persistent and significant deviation from the norm, treatment with Genitron® should be discontinued and control tests should be performed. In clinically stable patients with cirrhosis of the liver, there is no need to reduce the dose of Genitron®, it is necessary to monitor the detected laboratory changes.
Weakened patients need more careful monitoring, since their side effects are more severe. As with the treatment of other NSAIDs, the drug should be prescribed with caution to elderly patients who are more likely to have a decrease in kidney, liver and heart function.
The drug Genitron®, like any other NSAID, can mask the symptoms of the underlying infectious disease.
In very rare cases, serious skin reactions (some of them fatal) have been observed with the use of NSAIDs, including exfoliative dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis. A high risk of such reactions is observed at the beginning of treatment, while in most cases such reactions appeared during the first month of treatment. At the first appearance of skin rashes, lesions of the mucous membranes or other signs of hypersensitivity, it is necessary to stop using the drug Genitron®. Due to the possible occurrence of side effects with localization on the skin and mucous membranes, special attention should be paid to the appearance of appropriate symptoms. If side effects occur, treatment with the drug should be discontinued.
Influence on the ability to drive vehicles and manage mechanisms
During the treatment period, it is possible to reduce the speed of mental and motor reactions, therefore it is necessary to refrain from driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.
Overdose
Symptoms: drowsiness, impaired consciousness, nausea, vomiting, epigastric pain, gastrointestinal bleeding, acute renal failure, liver failure, arterial hypertension, arterial hypotension, respiratory arrest, asystole.
Treatment: there is no specific antidote. In case of an overdose of the drug, symptomatic therapy is carried out; in case of an overdose of the drug in the form of tablets, gastric lavage, taking activated charcoal. Forced diuresis, urine alkalinization, hemodialysis are ineffective due to the high degree of binding of the drug to blood proteins.
Drug interaction
When used concomitantly with other prostaglandin synthesis inhibitors, including GCS and salicylates, meloxicam may increase the risk of gastrointestinal mucosal ulcers and gastrointestinal bleeding due to their synergism.
The co-administration of meloxicam and other NSAIDs is not recommended.
Together with anticoagulants, heparin for systemic use, and thrombolytic agents, meloxicam increases the risk of bleeding. If it is impossible to avoid their simultaneous use, it is necessary to monitor the indicators of the blood coagulation system.
Simultaneous administration with meloxicam of antiplatelet drugs, serotonin reuptake inhibitors increases the risk of bleeding due to inhibition of platelet function. In the case of simultaneous use, careful monitoring of the blood coagulation system is necessary.
Meloxicam can reduce the renal excretion of lithium, which leads to an increase in its concentration in blood plasma to a toxic level. Simultaneous use of meloxicam with lithium preparations is not recommended. If simultaneous use is necessary, careful monitoring of the concentration of lithium in plasma is recommended throughout the course of the use of lithium preparations.
NSAIDs reduce the excretion of methotrexate by the kidneys, thereby increasing its concentration in plasma. Simultaneous use of meloxicam and methotrexate (at a dose of more than 15 mg per week) is not recommended. The risk of interaction between NSAIDs and methotrexate may also occur in patients using methotrexate in low doses, especially in patients with impaired renal function. In case of simultaneous use, careful monitoring of kidney function and blood formula is necessary. Meloxicam may increase the hematological toxicity of methotrexate, especially in patients with impaired renal function. When meloxicam and methotrexate are used together for 3 days, the risk of increased toxicity of the latter increases.
There is evidence that meloxicam can reduce the effectiveness of intrauterine contraceptives, but this has not been proven.
When using meloxicam together with diuretics, there may be a risk of acute renal failure, therefore, kidney function should be monitored and an adequate level of hydration should be maintained.
Meloxicam reduces the effect of antihypertensive agents (beta-blockers, ACE inhibitors, vasodilators, diuretics) due to inhibition of prostaglandins with vasodilating properties.
Meloxicam and angiotensin II receptor antagonists, as well as ACE inhibitors, have a synergistic effect on reducing glomerular filtration. In patients with existing renal dysfunction, this can lead to acute renal failure.
Colestyramine, binding meloxicam in the gastrointestinal tract, leads to its faster excretion.
Meloxicam, affecting renal prostaglandins, enhances the nephrotoxicity of cyclosporine, which requires enhanced monitoring of kidney function with simultaneous use of drugs.
Meloxicam is almost completely destroyed by hepatic metabolism, approximately 2/3 of which are carried out with the participation of cytochrome (CYP) P450 and 1/3 - by peroxidase oxidation. Pharmacokinetic interaction of meloxicam and other drugs at the stage of metabolism is possible due to their effect on SUR2C9 and / or SUR3A4.
When used simultaneously with hypoglycemic agents for oral administration, meloxicam may enhance their effect, thereby contributing to the risk of hypoglycemia.
Meloxicam can weaken the effect of digoxin, cortisone, diuretics.
With simultaneous administration of meloxicam with antacids, cimetidine, digoxin and furosemide, interaction at the pharmacokinetic level was not revealed.
The drug should be stored out of the reach of children, protected from light at a temperature not exceeding 25°C. Shelf life - 5 years. Do not use after the expiration date stated on the package.
Conditions for dispensing from pharmacies
The drug is available with a prescription.
Conditions for dispensing from pharmacies
The drug is available with a prescription.
Any questions?Please contact us, we look forward to receiving your message!
Ⓒ 2023 Systema Plus
Contact
Our adress
127030, Moscow, ext. ter. Tverskoy Municipal District, st. Sushchevskaya, building 21, floor 4, room/office I/429
Сообщение об успешной отправке!