Meloxicam DS
Meloxicam DS: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Meloxicam DS
ATX code: M01AC06
Active ingredient: meloxicam (Meloxicam)
Producers: Mekophar Chemical-Pharmaceutical, Joint Stock Company (Vietnam); Zhangjiakou Kaivei Pharmaceutical Co. Ltd. (Zhangjiakou Kaiwei Pharmaceutical, Co. Ltd.) (China)
Description and photo update: 2020-19-08
Prices in pharmacies: from 60 rubles.
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Meloxicam DS is a non-steroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic action.
Release form and composition
Dosage forms of Meloxicam DS:
- tablets: pale yellow; dosage 7.5 mg - round, on one side with a concave line and engraving "7.5" on each side of the line, on the other side - engraved "^"; dosage 15 mg - hexagonal, on one side convex, engraved "15", on the other side - with a concave line (10 pcs. in a blister, in a cardboard box 1 or 2 blisters; 20, 30 or 50 pcs. in plastic bottle with a polyethylene lid; in a cardboard box 1 bottle);
- solution for intramuscular (i / m) administration: transparent liquid, yellow with a green tint (1.5 ml in a glass ampoule, 3 ampoules in a plastic contoured pallet, 1 pallet in a cardboard box).
Each pack also contains instructions for the use of Meloxicam DS.
1 tablet contains:
- active substance: meloxicam - 7.5 or 15 mg;
- additional components: corn starch, lactose monohydrate, croscarmellose sodium, povidone, magnesium stearate, crospovidone.
15 ml of solution (1 ampoule) contains:
- active substance: meloxicam - 15 mg;
- additional components: poloxamer 188, ethanol, glycine, sodium hydroxide, sodium chloride, meglumine, water for injection.
Pharmacological properties
Pharmacodynamics
Meloxicam DS is an NSAID, the anti-inflammatory effect of which is due to the selective blocking of the activity of the enzyme cyclooxygenase-2 (COX-2), which is responsible for the biosynthesis of prostaglandins (Pg) in the area of the inflammatory process. At the same time, the drug has little effect on cyclooxygenase-1 (COX-1), which plays an important role in the production of Pg, which takes part in the regulation of blood flow in the kidneys and protects the mucous membrane of the gastrointestinal tract (GIT).
Pharmacokinetics
The relative bioavailability of meloxicam when administered intramuscularly is almost 100%. After an i / m injection at a dose of 5 mg, the maximum concentration (C max) of meloxicam in blood plasma is reached within about 60 minutes and is equal to 1.62 μg / ml.
After oral administration, the active substance is actively absorbed from the gastrointestinal tract, which is confirmed by its high absolute bioavailability - 90%. As a result of a single oral administration of meloxicam, its C max in plasma is achieved within 5–6 hours. Simultaneous administration of Meloxicam DS with food and inorganic antacids does not affect its absorption.
When taken orally and intravenously, meloxicam in doses of 7.5-15 mg, plasma levels of its content are proportional to the doses. Against the background of a course admission, the stationary state of pharmacokinetics is recorded within 3-5 days. After oral administration of the drug 1 time / day at a dose of 7.5 mg, the range of differences between its minimum concentration (C min) and C max is 0.4-1 μg / ml, and after taking at a dose of 15 mg - 0.8-2 μg / ml (respectively, the Cmin and Cmax values are indicated at the equilibrium state of pharmacokinetics), however, values outside this range were also noted. In the period of steady state pharmacokinetics, C max of meloxicam is observed in plasma 5-6 hours after oral administration.
When the drug is used for more than 1 year, its concentrations are similar to those observed after the first reaching steady-state concentrations (C ss).
Meloxicam binds to plasma proteins (mainly albumin) by 99%. It overcomes histohematogenous barriers, including it is detected in the synovial fluid, in which its content is approximately 50% of the plasma level. The volume of distribution (V d) is low, with intramuscular administration it is approximately 11 liters, with oral multiple doses (at doses of 7.5–15 mg) - approximately 16 liters, with a variation coefficient of 30–40% and 11–32%, respectively.
Meloxicam is almost completely biotransformed in the liver, resulting in the formation of 4 pharmacologically inactive derivatives. The main metabolite (60% of the administered dose) is 5'-carboxymeloxicam, formed by oxidation of the intermediate metabolite 5'-hydroxymethylmeloxicam, which is also excreted, but in a smaller amount (9% of the administered dose). In the process of in vitro studies, it was demonstrated that an important role in this metabolic transformation is played by the isoenzyme CYP2C9, as well as a less significant role by the isoenzyme CYP3A4. For the formation of two other metabolites, which make up 16 and 4% of the used dose of the drug, the enzyme peroxidase is responsible, the activity of which, presumably, varies individually.
The drug is excreted mostly in the form of metabolites equally through the intestines and kidneys. In unchanged form, no more than 5% of the daily dose is excreted with feces; in the urine, the drug in unchanged form is detected only in trace amounts. When administered intramuscularly, the average half-life (T 1/2) is 20 hours, and the plasma clearance is 8 ml / min. When taken orally, T 1/2 is 13-25 hours, and plasma clearance after a single use is approximately 7-12 ml / min.
Indications for use
Meloxicam DS is recommended for the symptomatic treatment of the following diseases:
- rheumatoid arthritis;
- osteoarthritis, for tablets - including degenerative joint lesions, arthrosis, including with a pain component;
- ankylosing spondylitis (ankylosing spondylitis).
The use of the drug allows to reduce the inflammatory process and pain syndrome at the time of application, and does not affect the progression of the underlying disease.
Contraindications
Absolute:
- decompensated heart failure, for pills - severe;
- the period after the operation of coronary artery bypass grafting;
- cerebrovascular or other bleeding - for solution;
- active gastrointestinal bleeding, a diagnosed disease of the blood coagulation system, recent cerebrovascular bleeding - for tablets;
- period of exacerbation of inflammatory bowel diseases, including Crohn's disease and ulcerative colitis;
- erosive and ulcerative defects of the gastric mucosa and duodenal ulcer, for tablets - in the acute phase or recently transferred, including perforation of the stomach and duodenum 12;
- severe renal failure in patients not receiving dialysis treatment with creatinine clearance (CC) <30 ml / min; progressive kidney disease, including proven hyperkalemia;
- active liver disease or severe hepatic impairment;
- partial or complete combination of bronchial asthma, recurrent polyposis rhinosinusitis and intolerance to acetylsalicylic acid and any other NSAIDs, including COX-2 inhibitors (including indications in history);
- glucose-galactose malabsorption or lactase deficiency, rare hereditary galactose intolerance - for tablets;
- age up to 18 years - for solution and up to 12 years - for tablets;
- pregnancy and the period of breastfeeding;
- hypersensitivity to any component of Meloxicam DS.
Relative (it is recommended to use the drug with caution):
- ischemic heart disease (CHD), chronic heart failure (CHF);
- cerebrovascular diseases;
- peripheral arterial lesions;
- presence of Helicobacter pylori infection; a history of indications of the development of ulcerative lesions of the gastrointestinal tract, additionally for tablets - a history of liver disease;
- diabetes;
- dyslipidemia / hyperlipidemia;
- moderate renal failure (CC 30-60 ml / min);
- severe somatic diseases;
- elderly age;
- frequent alcohol consumption, smoking;
- long-term treatment with NSAIDs;
- combination therapy with the following drugs: antiplatelet agents (clopidogrel, acetylsalicylic acid), oral glucocorticosteroids (GCS) (prednisolone), anticoagulants (warfarin), selective serotonin reuptake inhibitors (SSRIs) (sertraline, paroxetine, citaloprametine.
In order to reduce the risk of adverse reactions from the gastrointestinal tract, it is necessary to use Meloxicam DS in the lowest effective dose for the shortest possible course.
Meloxicam DSV, instructions for use: method and dosage
Solution for i / m administration
Meloxicam DS solution should be injected deep into the / m, intravenous administration should not be performed.
The drug is administered 1 time / day at 7.5 mg (½ ampoule) or 15 mg (1 ampoule), choosing the dose taking into account the severity of the inflammation and the intensity of the pain syndrome. The maximum daily dose should not exceed 15 mg.
Parenteral use of Meloxicam DS in the form of a solution for intravenous administration is indicated only during the first 2-3 days of treatment; in the future, the patient must be transferred to the oral form (tablets).
When using various dosage forms of meloxicam, its total daily dose should not exceed 15 mg.
Pills
Meloxicam DS tablets are taken orally with meals 1 time / day with a sufficient amount of liquid.
Recommended daily doses:
- osteoarthritis: 7.5 mg each, if the therapeutic effect is insufficient, the dose can be increased to 15 mg;
- rheumatoid arthritis; ankylosing spondylitis: 15 mg each, depending on the observed effect, the dose can be reduced to 7.5 mg.
The maximum daily dose is 15 mg. In adolescents 12-18 years old, the maximum dose is set at the rate of 0.25 mg / kg / day, but not more than 15 mg / day.
Side effects
The use of Meloxicam DS can cause the development of the following side effects on the part of systems and organs:
- immune system: infrequently (for tablets) - other immediate-type hypersensitivity reactions; with an unknown frequency - anaphylactoid / anaphylactic reactions, for tablets - anaphylactic shock;
- blood and lymphatic system: infrequently - anemia; rarely - a change in the number of blood cells, including a change in the leukocyte formula; leukopenia, thrombocytopenia; extremely rare (for tablets) - agranulocytosis;
- nervous system: often - headache; infrequently - drowsiness, dizziness;
- mental disorders: often - mood changes; rarely - emotional lability; with an unknown frequency - disorientation, confusion;
- Gastrointestinal tract: often - dyspepsia, abdominal pain, nausea, vomiting, diarrhea; infrequently - flatulence, constipation, belching, stomatitis, gastritis, bleeding from the gastrointestinal tract (including hidden); rarely - colitis, esophagitis, gastroduodenal ulcers; extremely rare - perforation of the digestive tract;
- liver and biliary tract: infrequently - transient increase in the activity of hepatic transaminases or bilirubin content (if these changes are significant or do not weaken over time, it is necessary to stop taking Meloxicam DS); extremely rare - hepatitis;
- respiratory system, chest and mediastinal organs: rarely - bronchial asthma (if you are allergic to other NSAIDs or acetylsalicylic acid), bronchospasm;
- skin and subcutaneous tissues: infrequently - skin rash, itching, angioedema; rarely - urticaria, toxic epidermal necrolysis, Stevens-Johnson syndrome; extremely rarely - erythema multiforme, bullous dermatitis (the occurrence of such reactions is noted mainly during the first month of the course, with the development of the initial signs of a skin rash or changes in the mucous membranes, you need to consult a doctor); with an unspecified frequency - photosensitivity;
- cardiovascular system: infrequently - rush of blood to the skin of the face, increased blood pressure (BP); rarely - palpitations;
- urinary system: increased serum blood urea and / or hypercreatininemia; for tablets - urinary disorders, including acute urinary retention; extremely rare - acute renal failure;
- sense organs: infrequently - vertigo; rarely - visual impairment, including blurred vision, conjunctivitis, tinnitus;
- genitals and mammary gland (for tablets): infrequently - late ovulation; with an unknown frequency - infertility in women;
- others: often - edema, including edema of the lower extremities;
- local reactions: often - swelling at the injection site; infrequently - soreness at the injection site.
An ulcer or perforation of the gastrointestinal tract, or gastrointestinal bleeding, which occurred during therapy with Meloxicam DS, can be fatal.
The simultaneous use of Meloxicam DS and drugs that depress the bone marrow (including methotrexate) can cause cytopenia. There are reports of isolated cases of agranulocytosis in the combined treatment with meloxicam and other myelotoxic agents.
When carrying out drug therapy, as well as when using other NSAIDs, one cannot exclude the possibility of developing glomerulonephritis, interstitial nephritis, renal medullary necrosis, proteinuria, hematuria, and nephrotic syndrome.
Overdose
The main symptoms of a meloxicam overdose may include nausea, vomiting, impaired consciousness, gastrointestinal bleeding, epigastric pain, liver failure, acute renal failure, decreased blood pressure, asystole, respiratory arrest.
The specific antidote is unknown, with established intoxication, symptomatic treatment is performed. In the case of oral administration of the drug for 1 hour after receiving an excessive dose, gastric lavage and intake of activated charcoal are recommended. According to research data, cholestyramine, by binding meloxicam in the gastrointestinal tract, ensures its faster excretion.
Since Meloxicam DS is characterized by a high degree of urinary alkalization with blood proteins, forced diuresis and hemodialysis are ineffective.
special instructions
If there is a history of ulcerative lesions of the stomach or duodenal ulcer, as well as with concomitant anticoagulant therapy, special care is required during the period of use of Meloxicam DS due to the aggravation of the risk of developing erosive and ulcerative gastrointestinal pathologies.
Ulcers, gastrointestinal perforations or gastrointestinal bleeding (including severe) can occur during NSAID therapy at any time, regardless of the absence or presence of symptoms or a history of serious gastrointestinal lesions. The most severe consequences of these side effects are observed mainly in elderly patients.
During treatment with NSAIDs, cases of increased risk of severe cardiovascular thrombosis, angina attacks, myocardial infarction, with a possible fatal outcome were established. This threat increases against the background of long-term use of NSAIDs, as well as with a history of these diseases or a predisposition to their development.
Meloxicam DS, like other NSAIDs, inhibits the production of Pg in the kidneys, which are involved in maintaining renal perfusion. In the case of reduced renal blood flow or reduced volume of circulating blood, the use of the drug can contribute to the decompensation of latent renal failure. As a rule, after discontinuation of the drug, renal function is restored to its original level. The threat of this reaction is aggravated in the elderly, in patients with CHF, dehydration, liver cirrhosis, kidney damage or nephrotic syndrome, after severe surgical interventions that cause hypovolemia, as well as with simultaneous therapy with diuretics, angiotensin II receptor antagonists, ACE inhibitors. In patients from this risk group, kidney activity and diuresis should be monitored at the beginning of treatment.
NSAIDs, including Meloxicam DS, can mask the manifestations of infectious diseases.
Influence on the ability to drive vehicles and complex mechanisms
Due to the fact that when using meloxicam, such undesirable effects as headache, drowsiness and dizziness may occur, during the period of therapy, one should refrain from driving potentially dangerous and complex mechanisms, including vehicles.
Application during pregnancy and lactation
Treatment with Meloxicam DS during pregnancy and breastfeeding (NSAIDs are excreted in breast milk) is contraindicated.
Since the drug suppresses the production of COX / Pg, it can also affect fertility, therefore it is not recommended for use in women planning pregnancy. Meloxicam can lead to a delay in ovulation, therefore, the appointment of Meloxicam DS is contraindicated for patients with a reduced ability to conceive or undergoing examination for infertility.
Pediatric use
The drug in the form of tablets is contraindicated for the treatment of children under 12 years of age. Injections of Meloxicam DS solution are prohibited for children and adolescents under 18 years of age.
With impaired renal function
The presence of mild or moderate renal failure does not significantly affect the pharmacokinetics of the drug. Patients with moderate renal impairment have a significantly higher rate of elimination of meloxicam. In end-stage renal failure, the binding of the drug to plasma proteins worsens; due to an increase in V d, higher concentrations of free meloxicam may occur.
With severe renal failure (CC <30 ml / min), patients not undergoing dialysis, or with progressive kidney disease, including with confirmed hyperkalemia, drug therapy is contraindicated.
Patients with severe renal failure undergoing hemodialysis treatment should use Meloxicam DS in a dose not exceeding 7.5 mg. In patients with moderate functional impairment of the kidneys (CC> 30 ml / min), when the drug is taken orally, dose adjustment is not required; with intravenous injections, meloxicam should be used in a dose of not more than 7.5 mg.
For violations of liver function
The presence of liver failure does not lead to changes in the pharmacokinetics of meloxicam.
Treatment with the drug is contraindicated in patients with active liver disease or severe liver dysfunction. With small or moderate functional disorders of the liver, a dose reduction of the drug is not required.
Use in the elderly
Elderly patients are recommended to use Meloxicam DS at an initial daily dose of 7.5 mg.
Drug interactions
- other NSAIDs (including acetylsalicylic acid), GCS: the threat of erosive and ulcerative defects and bleeding from the gastrointestinal tract increases as a result of synergistic action (suppression of Pg production); this combination is not recommended;
- angiotensin II receptor antagonists, ACE inhibitors: the effect of decreasing glomerular filtration increases, which can contribute to the occurrence of acute renal failure, especially in patients with impaired renal function;
- SSRIs: increases the likelihood of gastrointestinal bleeding;
- antiplatelet drugs (clopidogrel, acetylsalicylic acid), anticoagulants (warfarin, ticlopidine, heparin), fibrinolytic agents (fibrinolysin, streptokinase): the risk of bleeding is aggravated due to inhibition of platelet function; periodic monitoring of blood clotting indicators is required;
- antihypertensive drugs [β-blockers, vasodilators, diuretics, angiotensin-converting enzyme (ACE) inhibitors]: the efficacy of antihypertensive drugs is weakened due to inhibition of the production of Pg, exhibiting vasodilating properties;
- diuretics: the threat of water, potassium and sodium retention in the body is aggravated, as well as the appearance of acute renal failure in case of dehydration of patients; in predisposed patients, an aggravation of arterial hypertension or signs of heart failure is possible; against the background of this combination, it is necessary to ensure adequate hydration, and before the start of joint administration, to investigate renal function;
- cyclosporine: increased nephrotoxicity of this substance, due to the inhibitory effect on the production of Pg; it is required to control the work of the kidneys, especially in the elderly;
- pemetrexed: the threat of myelosuppression and the appearance of adverse effects from the gastrointestinal tract is aggravated; in patients with CC 45–79 ml / min, if it is necessary to use this substance 5 days before the start of its intake, the use of meloxicam should be discontinued and then resumed no earlier than 2 days after the end of pemetrexed administration; when CC is <45 ml / min, this combination is not recommended;
- methotrexate: the hematological toxicity of this substance increases (the risk of anemia and leukopenia), due to a decrease in its tubular secretion and an increase in plasma concentration, the simultaneous administration of Meloxicam DS with methotrexate at a dose above 15 mg per week is not recommended; with the simultaneous use of meloxicam and methotrexate in low doses, it is necessary to monitor the blood count and kidney function (especially in renal failure);
- lithium preparations: the risk of an increase in their toxic effect is aggravated due to a decrease in renal excretion; it is necessary to control the plasma content of lithium in the blood throughout the entire combination therapy;
- probenecid: it is required to take into account the likelihood of pharmacokinetic interaction;
- antacids, cimetidine, furosemide, digoxin: no significant pharmacokinetic interaction is observed;
- hypoglycemic agents for oral administration (sulfonylurea derivatives, nateglinide): an increase in the level of concentration in the blood of meloxicam and these drugs may be recorded; due to the possible occurrence of hypoglycemia, it is necessary to carefully monitor the concentration of glucose in the blood;
- intrauterine contraceptives: their effectiveness may decrease.
Analogs
Meloxicam DS analogs are Meloxicam, Amelotex, Movalis, Artrozan, B-xikam, GenITRON, Mataren, Liberum, Medsikam, Melbek, etc.
Terms and conditions of storage
Store in a place out of the reach of children, protected from moisture and light, at a temperature not exceeding 25 ° C.
The shelf life of both dosage forms of Meloxicam DS is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Meloxicam DS
Reviews of Meloxicam DS are ambiguous. Many patients believe that with intramuscular injections of the drug (there are no reviews of the oral form), it helps in the symptomatic treatment of osteoarthritis, arthritis, arthrosis, osteochondrosis of the cervical and thoracic spine, spondylitis, and also relieves pain in joints and muscles. Usually, a significant improvement in the condition is noted after a course of administration of a solution consisting of three injections. Meloxicam DS injections effectively relieve pain, inflammation and stiffness in movements, and at the same time the drug is cheaper than many analogues.
At the same time, many complaints are left about the numerous undesirable effects of the drug, especially from the gastrointestinal tract. Some patients were unhappy with the analgesic effect of Meloxicam DS, because after the course of treatment they did not feel any relief of symptoms.
Price for Meloxicam DS in pharmacies
The price of Meloxicam DS, in the form of a solution for intramuscular injection (10 mg / ml), can vary from 60 to 120 rubles. per package containing 3 ampoules of 1.5 ml. The price of the tablets is unknown, since at present this dosage form of the drug is not available in the pharmacy network.
Meloxicam DS: prices in online pharmacies
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Drug name Price Pharmacy |
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Meloxicam DS 10 mg / ml solution for intramuscular administration 1.5 ml 3 pcs. RUB 60 Buy |
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Meloxicam DS solution for intramuscular injection. 10mg / ml 1.5ml 3 pcs. RUB 99 Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
