Meloxicam is a non-steroidal anti-inflammatory drug with analgesic and antipyretic effects. It is used as injections (deep intramuscular), tablets (orally) and suppositories (rectally). The medicine is affordable and gives a quick effect. Used only in consultation with a doctor, dispensed from pharmacies with a prescription.
"Meloxicam" is a drug with the active ingredient of the same name. It is a non-steroidal anti-inflammatory drug. It has antipyretic, analgesic and analgesic effects.
Available in 3 dosage forms:
- solution in ampoules;
- pills;
- suppositories (candles).
The active component of Meloxicam is a derivative of organic enolic acid. It inhibits the activity of the enzyme cyclooxygenase-2 and slows down the formation of prostaglandins. As a result, inflammatory processes are stopped, the lesion is reduced, resulting in an analgesic effect.
The drug is released only with a prescription. It can be stored at room temperature (no more than 25 degrees) out of the reach of children. The shelf life is 2 years from the date of production.
Contraindications and side effects
The drug should not be used if there are such contraindications:
- intolerance to pyrazolone and its derivatives;
- allergic reactions, hypersensitivity to acetylsalicylic acid;
- recurrent nasal polyposis;
- severe kidney damage;
- peptic ulcers of the gastrointestinal tract;
- bronchial asthma;
- period of pregnancy, as well as lactation (at any stage);
- older people take the drug with caution.
Meloxicam suppositories are not allowed to be used in the presence of diseases of the rectum, anal region, if they are chronic. Other contraindications are possible, so be sure to consult a doctor before starting use.
In some cases, side effects are observed:
- exacerbation of stomach and intestinal ulcers;
- vomiting, nausea;
- belching;
- bloating;
- constipation;
- diarrhea syndrome;
- headaches;
- dizziness;
- drowsy state;
- leukopenia;
- anemia;
- increased blood pressure;
- skin rashes, itching, other forms of allergies;
- swelling;
- high urea level;
- blood rush to the chest, face, neck.
Meloxicam solution for intramuscular administration 10 mg/ml 1.5 ml ampoule, 3 pcs (B-Pharm)
Registration Certificate Holder
B-PHARM (Russia)
Dosage form
Medicine - Meloxicam
Description
Solution for intramuscular administration
in the form of a transparent or slightly opalescent liquid of yellow color with a greenish tint.
1 ml
meloxicam 10 mg
Excipients
: meglumine - 6.25 mg, tetrahydrofurfuryl macrogol - 100 mg, poloxamer 188 - 50 mg, sodium chloride - 3 mg, glycine - 5 mg, sodium hydroxide solution 1M - to pH 8.2-8.9, water for injection - up to 1 ml.
1.5 ml - ampoules (3) - contour cell packaging (1) - cardboard packs. 1.5 ml - ampoules (5) - contour cell packaging (1) - cardboard packs. 1.5 ml - ampoules (5) - contour cell packaging (2) - cardboard packs.
Indications
Symptomatic treatment: osteoarthritis (arthrosis, degenerative joint diseases), incl. with a pain component; rheumatoid arthritis; ankylosing spondylitis; other inflammatory and degenerative diseases of the musculoskeletal system, such as arthropathy, dorsopathies (for example, sciatica, low back pain, shoulder periarthritis), accompanied by pain.
Parenterally used as initial therapy and short-term symptomatic treatment.
Contraindications for use
Hypersensitivity to meloxicam; hypersensitivity (including to other NSAIDs); complete or incomplete combination of bronchial asthma, recurrent nasal polyposis or paranasal sinuses, angioedema or urticaria caused by intolerance to acetylsalicylic acid or other NSAIDs due to the existing likelihood of cross-sensitivity (including a history); erosive and ulcerative lesions 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 and heart failure; severe renal failure (if hemodialysis is not performed, creatinine clearance <30 ml/min, and also with confirmed hyperkalemia); active liver disease; active gastrointestinal bleeding, recent cerebrovascular bleeding or established diagnosis of diseases of the blood coagulation system; concomitant therapy with anticoagulants, because there is a risk of intramuscular hematoma formation; therapy of perioperative pain during coronary artery bypass grafting; pregnancy; lactation period (breastfeeding); children and adolescents up to 18 years of age.
Carefully
History of gastrointestinal diseases (presence of Helicobacter pylori infection); congestive heart failure; renal failure (creatinine clearance 30-60 ml/min); IHD; cerebrovascular diseases; dyslipidemia/hyperlipidemia; diabetes; concomitant therapy with the following drugs: anticoagulants, oral corticosteroids, antiplatelet agents, selective serotonin reuptake inhibitors; peripheral arterial disease; elderly age; long-term use of NSAIDs; smoking; frequent drinking of alcohol.
pharmachologic effect
NSAIDs, a derivative of enolic acid, have anti-inflammatory, analgesic and antipyretic effects.
The mechanism of the anti-inflammatory effect of meloxicam is its ability to inhibit the synthesis of prostaglandins, known mediators of inflammation.
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 mediate the therapeutic effects of NSAIDs, whereas inhibition of the constitutively present isoenzyme COX-1 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 have shown that meloxicam (at doses of 7.5 mg and 15 mg) has no effect on platelet aggregation and bleeding time.
In clinical studies, gastrointestinal side effects generally occurred less frequently with meloxicam 7.5 and 15 mg doses than with other comparable NSAIDs. This difference in the frequency of side effects from the gastrointestinal tract is mainly due to the fact that when taking meloxicam, such phenomena as dyspepsia, vomiting, nausea, and abdominal pain were observed less frequently. The incidence of upper gastrointestinal perforation, ulceration, and bleeding associated with meloxicam use was low and dose-related.
Drug interactions
Other inhibitors of prostaglandin synthesis, including glucocorticoids and salicylates - concomitant use with meloxicam increases the risk of ulceration in the gastrointestinal tract and gastrointestinal bleeding (due to synergistic action). Concomitant use with other NSAIDs is not recommended.
Anticoagulants for oral administration, heparin for systemic use, thrombolytic agents - simultaneous use with meloxicam increases the risk of bleeding. In case of simultaneous use, careful monitoring of the blood coagulation system is necessary.
Antiplatelet drugs, serotonin reuptake inhibitors - simultaneous use with meloxicam increases the risk of bleeding due to inhibition of platelet function. In case of simultaneous use, careful monitoring of the blood coagulation system is necessary.
Lithium preparations - NSAIDs increase plasma lithium levels by reducing its excretion by the kidneys. The simultaneous use of meloxicam with lithium preparations is not recommended. If simultaneous use is necessary, careful monitoring of plasma lithium concentrations is recommended throughout the course of lithium use.
Methotrexate - NSAIDs reduce the secretion of methotrexate by the kidneys, thereby increasing its plasma concentration. The simultaneous use of meloxicam and methotrexate (at a dose of more than 15 mg per week) is not recommended. In case of simultaneous use, careful monitoring of renal function and blood count is necessary. Meloxicam may increase the hematological toxicity of methotrexate, especially in patients with impaired renal function.
Diuretics - the use of NSAIDs while taking diuretics in case of dehydration of patients is accompanied by a risk of developing acute renal failure.
Antihypertensive drugs (beta-blockers, ACE inhibitors, vasodilators, diuretics). NSAIDs reduce the effect of antihypertensive drugs due to inhibition of prostaglandins, which have vasodilating properties.
Angiotensin II receptor antagonists, as well as ACE inhibitors, when used together with NSAIDs, increase the decrease in glomerular filtration, which can thereby lead to the development of acute renal failure, especially in patients with impaired renal function.
Cholestyramine, by binding meloxicam in the gastrointestinal tract, leads to its faster elimination.
Pemetrexed - with the simultaneous use of meloxicam and pemetrexed in patients with CC from 45 to 79 ml/min, the use of meloxicam should be discontinued 5 days before starting pemetrexed and can be resumed 2 days after the end of treatment. If there is a need for concomitant use of meloxicam and pemetrexed, patients should be carefully monitored, especially for myelosuppression and the occurrence of gastrointestinal side effects. In patients with creatinine clearance <45 ml/min, the use of meloxicam with pemetrexed is not recommended.
NSAIDs, by acting on renal prostaglandins, may enhance the nephrotoxicity of cyclosporine.
When co-administering medicinal products with meloxicam that have a known ability to inhibit CYP2C9 and/or CYP3A4 (or are metabolized by these enzymes), such as sulfonylurea derivatives or probenecid, the possibility of pharmacokinetic interaction should be taken into account.
When used concomitantly with oral hypoglycemic agents (eg, sulfonylureas, nateglinide), a CYP2C9-mediated interaction is possible, which may lead to increased blood concentrations of both the hypoglycemic agents and meloxicam. Patients taking meloxicam concomitantly with a sulfonylurea or nateglinide should carefully monitor blood glucose concentrations due to the potential for hypoglycemia.
Dosage regimen
They are installed individually, depending on the intensity of pain and the severity of the inflammatory process. Prescribed IM at a dose of 7.5 mg or 15 mg 1 time/day.
Side effect
From the hematopoietic system: infrequently - anemia; rarely - leukopenia, thrombocytopenia, changes in the number of blood cells, including changes in the leukocyte formula.
From the immune system: infrequently - immediate hypersensitivity reactions; frequency not established - anaphylactic shock, anaphylactoid reactions.
Mental disorders: rarely - mood changes; frequency not established - confusion, disorientation.
From the nervous system: often - headache; infrequently - dizziness, drowsiness.
From the senses: infrequently - vertigo; rarely - conjunctivitis, visual impairment, including blurred vision, tinnitus.
From the cardiovascular system: infrequently - increased blood pressure, a feeling of a “rush” of blood to the face; rarely - palpitations.
From the respiratory system: rarely - bronchial asthma in patients with allergies to acetylsalicylic acid and other NSAIDs.
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 transaminase activity or bilirubin concentration); very rarely - hepatitis.
From the skin and subcutaneous tissues: infrequently - angioedema, itching, skin rash; rarely - toxic epidermal necrolysis, Stevens-Johnson syndrome, urticaria; very rarely - bullous dermatitis, erythema multiforme; frequency not established - photosensitivity.
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.
From the reproductive system: infrequently - late ovulation; frequency not established - infertility in women.
Other: often - pain and swelling at the injection site; infrequently - swelling.
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 excluded.
special instructions
Patients with gastrointestinal diseases require regular monitoring. If ulcerative lesions of the gastrointestinal tract or gastrointestinal bleeding occur, meloxicams should be discontinued.
Gastrointestinal ulcers, perforation, or bleeding may occur at any time during the use of NSAIDs, with or without warning symptoms or a history of serious gastrointestinal complications. The consequences of these complications are generally more serious for older people.
When using meloxicam, serious skin reactions such as exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis may develop. Therefore, special attention should be paid to patients who report the development of adverse events from the skin and mucous membranes, as well as hypersensitivity reactions to the drug, especially if such reactions were observed during previous courses of treatment. The development of such reactions is observed, as a rule, during the first month of treatment. If the first signs of skin rash, changes in mucous membranes or other signs of hypersensitivity appear, discontinuation of meloxicam should be considered.
Cases have been described when taking NSAIDs to increase the risk of developing serious cardiovascular thrombosis, myocardial infarction, angina, possibly fatal. This risk increases with long-term use of the drug, as well as in patients with a history of the above diseases and predisposed to such diseases.
NSAIDs inhibit the synthesis of prostaglandins in the kidneys, which are involved in maintaining renal perfusion. The use of NSAIDs in patients with reduced renal blood flow or reduced volume may lead to decompensation of latent renal failure. After discontinuation of NSAIDs, renal function usually returns to baseline levels. Those most at risk for developing this reaction are elderly patients, patients with dehydration, congestive heart failure, liver cirrhosis, nephrotic syndrome or acute renal impairment, patients concomitantly taking diuretics, ACE inhibitors, angiotensin II receptor antagonists, and also patients who have undergone major surgical interventions that lead to hypovolemia. In such patients, diuresis and renal function should be carefully monitored when initiating therapy.
The use of NSAIDs in combination with diuretics can lead to sodium, potassium and water retention, as well as a decrease in the natriuretic effect of diuretics. As a result, predisposed patients may experience increased signs of heart failure or hypertension. Therefore, careful monitoring of the condition of such patients is necessary, as well as maintaining adequate hydration.
Before starting treatment, a kidney function test is necessary. In case of combination therapy, renal function should also be monitored.
When using meloxicam (as well as most other NSAIDs), episodic increases in serum transaminase activity or other indicators of liver function are possible. In most cases, this increase was small and transitory. If the detected changes are significant or do not decrease over time, meloxicam should be discontinued and laboratory changes observed should be monitored.
Weakened or malnourished patients may be less able to tolerate adverse events and should be monitored closely.
Like other NSAIDs, meloxicam may mask the symptoms of an underlying infectious disease.
As a COX/prostaglandin synthesis inhibitor, meloxicam may have an effect on fertility and is therefore not recommended for women who have difficulty conceiving. In women undergoing examination for this reason, discontinuation of meloxicam is recommended.
In patients with mild to moderate renal insufficiency (creatinine clearance>25 ml/min), no dose adjustment is required.
In patients with liver cirrhosis (compensated), no dose adjustment is required.
Impact on the ability to drive vehicles using machinery
When driving or operating machinery, the possibility of dizziness, drowsiness, visual impairment or other central nervous system disorders should be taken into account. During the treatment period, patients must be careful when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Use during pregnancy and breastfeeding
Restrictions during pregnancy - Contraindicated. Restrictions when breastfeeding - Contraindicated. Use during pregnancy and breastfeeding is contraindicated.
Use for renal impairment
Restrictions for impaired renal function - With caution.
Use is contraindicated in severe renal failure (if hemodialysis is not performed, CC <30 ml/min, and also with confirmed hyperkalemia).
Use with caution in case of renal failure (creatinine clearance 30-60 ml/min).
Use for liver dysfunction
Restrictions for liver dysfunction - With caution.
Use is contraindicated in severe liver failure or active liver disease.
In patients with liver cirrhosis (compensated), no dose adjustment is required.
Use in elderly patients
Restrictions for elderly patients - Use with caution. Use with caution in elderly patients.
Use in children
Restrictions for children - Contraindicated. Use in children and adolescents under 18 years of age is contraindicated.
Instructions for use of Meloxicam tablets and suppositories
Tablets are taken once a day in an amount of 7.5-15 mg with meals. This dosage is intended for adults and adolescents. In this case, the tablets can only be used for the first few days, after which it is possible to replace them with another drug.
If the patient is on hemodialysis and has severe kidney pathologies, he can use no more than 7.5 mg per day. However, daily and single dosages of other drugs in the same series (for example, Meloxicam Prana) may differ. The norm depends on the person’s age, condition, concomitant diseases and other factors.
Suppositories are administered rectally once a day - regardless of the time of day or meal. One suppository corresponds to a daily dosage of 15 mg.
Attention!
In case of overdose, the side effects described above may occur. Immediate gastric lavage is indicated; treatment is symptomatic. A specific antidote for Meloxicam has not been developed.
Meloxicam
Meloxicam is a representative of the most popular class of non-steroidal anti-inflammatory drugs. NSAIDs today have firmly established themselves at the top of the pharmacological charts in terms of frequency of prescription by doctors and sales volumes from pharmacies. And this is absolutely justified: they allow you to achieve the desired therapeutic effect in the shortest possible time - and this is exactly what both patients and doctors themselves expect from the drug. The mechanism of action of NSAIDs is associated with the suppression of the activity of cyclooxygenase, or, as it is abbreviated in the specialized literature, COX. For reference: this is an enzyme that promotes the reproduction of prostaglandins, mediators of pain and inflammation. There are (in any case, their presence has been established for certain) two forms of COX. COX-1 saturates most organs and tissues and is in a constantly activated form. It is involved in the synthesis of normal, “non-extreme” prostaglandins, which regulate the normal routine functioning of cells, expressed in the formation of gastrointestinal mucus, suppression of the secretion of hydrochloric acid in the stomach, influence on platelet aggregation, blood supply to the kidneys and other completely ordinary, but necessary processes for the body. Another thing is COX-2: this enzyme is activated only in response to any anti-inflammatory stimuli. That is why it is believed that the unwanted side effects of NSAIDs on the digestive tract and kidneys are associated with the suppression of COX-1, and the therapeutically significant anti-inflammatory effect is associated with the inhibition of COX-2.
The effect of early generations of NSAIDs could be compared to carpet bombing: they indiscriminately “turned off” both COX-1 and COX-2. In contrast, meloxicam is a selective COX-2 inhibitor, which avoids negative reactions with a compatible or higher therapeutic effect compared to the same diclofenac or naproxen. The main purpose of meloxicam is to suppress pain and inflammatory reactions in osteoarthritis and rheumatoid arthritis, although the drug can be used to relieve pain of other origins.
Today in Russian pharmacies you can find three dosage forms of meloxicam: tablets, solution for intramuscular administration and rectal suppositories. The tablets are taken orally once a day with meals. For osteoarthritis, the recommended (also maximum) daily dose for all forms of the drug is 15 mg, for rheumatoid arthritis - 7.5 mg. Injections are made only intramuscularly, observing the required injection depth. The suppositories are inserted as deep as possible into the anus. If the patient has an increased risk of developing negative side effects, then the daily dose should be halved.
Drug interactions
Combined use with myelotoxic drugs increases the side effects of Meloxicam on the blood. If you take the drug together with non-steroidal anti-inflammatory medications, the risk of bleeding in the stomach and intestines, as well as exacerbation of ulcers, increases.
If you take Cholestyramine, the drug promotes the rapid elimination of Meloxicam. When using Heparin, Ticlopidine, drugs to lower blood pressure, and indirect anticoagulants, the risk of bleeding increases. When taken together with Cyclosporine, the likelihood of kidney-related side effects increases.