Meloxicam pills 7.5mg, 20pcs

Composition

One ampoule contains:

Active ingredient-meloxicam 7.5 mg,

excipients: meglumin, glycofural, poloxamer, glycine, sodium chloride, sodium hydroxide, water for injection.

Pharmacological action

Pharmacotherapeutic group: Nonsteroidal anti-inflammatory drugs. Oxycams. Meloxicam.

ATX code: M 01 AC 06

Pharmacological properties

Pharmacokinetics

Meloxicam is completely absorbed after intramuscular use. The relative bioavailability compared to oral bioavailability is almost 100%. Therefore, when switching from injectable to oral forms, no dose adjustment is required. After use of 15 mg of the drug intramuscularly, the peak plasma concentration of 1.6-1.8 mcg / ml is reached in 60-90 minutes.

Meloxicam binds intensively to plasma proteins (especially albumins – – 99%. Passes through histohematic barriers, penetrates synovial fluid. The synovial fluid concentration is 50% of the plasma concentration. It is metabolized in the liver to inactive metabolites. It is excreted through the intestines and kidneys (in approximately equal proportions), unchanged-5% of the daily dose (through the intestines). The elimination half-life varies from 13 to 25 hours after use. Total plasma clearance is 7-12 ml / min

. Pharmacokinetics in specific patient populations

Hepatic insufficiency, as well as mild renal insufficiency, do not significantly affect the pharmacokinetics of meloxicam. Patients with moderate renal insufficiency have a higher plasma clearance.

Reduced protein binding of meloxicam is observed in patients with end-stage renal failure.

Older men have pharmacokinetic parameters similar to those of younger men.

Older women have higher AUC values and a longer elimination half-life compared to younger patients.

Pharmacodynamics

Meloxicam is a nonsteroidal anti-inflammatory drug (NSAID) from the enolic acid class, which has anti-inflammatory, analgesic and antipyretic effects. The mechanism of the above effects is the ability of Meloxicam to inhibit the biosynthesis of prostaglandins, which are inflammatory mediators.

The mechanism of action is mainly associated with selective inhibition of cyclooxygenase-2 ( COX-2), a specific enzyme involved in the development of inflammatory processes. It is believed that COX-2 inhibition provides a therapeutic effect of NSAIDs, while inhibition of the constantly present COX-1 isoenzyme can cause side effects from the stomach and kidneys.

The selectivity of meloxicam for COX-2 was confirmed in various test systems, both in vitro and in vivo.

The frequency of perforations in the upper gastrointestinal tract, ulcers and bleeding associated with the use of meloxicam was low and depended on the dose of the drug.

Indications

Meloxicam is intended for initial and short-term (short-term) symptomatic treatment of inflammatory and degenerative joint diseases accompanied by pain, including

-rheumatoid arthritis

-osteoarthritis

-ankylosing spondylitis (Ankylosing spondylitis)

Use during pregnancy and lactation

Teratogenic effects. Meloxicam increased the incidence of cardiac septal defects (a rare complication) when using an oral dose of 60 mg / kg / day (64.5 times higher than the 15 mg/day dose for an adult weighing 50 kg in terms of body surface area) and embryoletality at oral doses ≥5 mg/kg / day (5.4 times higher than the human dose as described above) in rabbits treated with meloxicam during organogenesis. Meloxicam showed no teratogenicity in rats at oral doses of 4 mg / kg / day (approximately 2.2 times higher than the human dose as described above) during organogenesis. An increase in the stillbirth rate was observed in rats at oral doses ≥1 mg / kg / day during organogenesis.

Non-teratogenic effects. Meloxicam caused a decrease in such indicators as fertility index, live birth rate, neonatal survival at oral doses ≥0.125 mg/kg/day (approximately 0.07 times the human dose as described above) in rats during pregnancy and lactation.

Meloxicam passes through the placental barrier. No adequate and strictly controlled studies have been conducted in pregnant women. Use during pregnancy is possible if the expected effect of therapy exceeds the potential risk to the fetus.

Studies evaluating the effect of meloxicam on arterial duct closure in humans have not been conducted. The use of meloxicam in the third trimester of pregnancy should be excluded.

Childbirth and delivery. Studies in rats have shown that meloxicam, like other agents that inhibit PG synthesis, increases the number of stillbirths, causes delayed delivery and delivery at oral doses of ≥1 mg / kg / day (approximately 0.5 times the human dose as described above), and reduces the number of surviving pups at oral doses of 4 mg/kg/day (approximately 2.1 times the human dose as described above) during organogenesis. Similar observations were observed in rats receiving oral doses ≥0.125 mg / kg / day (approximately 0.07 times the human dose as described above) during pregnancy and lactation.

The effects of meloxicam on labor and delivery in humans are unknown.

Category of action on the fetus according to the FDA-C.

The use of meloxicam, as well as other drugs that block the synthesis of PG, can affect fertility, so it is not recommended for women who want to become pregnant.

Meloxicam is excreted in the milk of lactating rats, with milk concentrations exceeding plasma concentrations. It is not known whether meloxicam passes into the breast milk of women, so you should stop breastfeeding during treatment or avoid using meloxicam during breastfeeding.

Contraindications

• hypersensitivity to meloxicam or any other component of the drug

• hypersensitivity to acetylsalicylic acid and other nonsteroidal anti-inflammatory drugs. Meloxicam should not be administered to patients who have history after the use of aspirin or other NSAIDs was observed symptoms of asthma, nasal polyps, angioneurotic edema, hives

• should not be given to patients receiving anticoagulants because of possible risk of intramuscular hematoma

• erosive and ulcerative changes of the gastric mucosa and duodenal ulcer

• ulcerative colitis in the acute phase, Crohn’s disease

• severe hepatic insufficiency, liver disease in the acute stage

• gastrointestinal bleeding, recently developed cerebrovascular bleeding or other hemorrhagic disease

• progressive disease of the kidneys, severe renal insufficiency (if not possible, dialysis), creatinine clearance less than 30 ml/min

• decompensated heart failure

• postoperative pain after coronary artery bypass grafting (overlay of bypass anastomosis)

• children under 18 years of age

• pregnancy and lactation

Side effects

Often (≥1/100 to <1/10)

– headache, dizziness

-decreased appetite, stomatitis

-nausea, vomiting, abdominal pain, diarrhea, constipation, flatulence, diarrhea

-pruritus, rash

-leukopenia, thrombocytopenia, anemia

– edema, swelling at the injection site, pain at the injection site

Infrequently (≥1/1000 to

– disorientation, tinnitus, vertigo, drowsiness

-palpitations, increased blood pressure, a feeling of rush of blood to the face

– erosive and ulcerative changes in the gastric and duodenal mucosa / perforation in the acute phase or recently transferred

– urticaria

– transient changes in liver function indicators (increased transaminase or bilirubin activity)

– changes in renal function indicators (increased serum creatinine and/or urea, albuminuria, hematuria), difficulty urinating, including acute urinary retention

Rarely (from ≥1/10,000 to

anaphylactic shock, anaphylactoid reactions and other hypersensitivity reactions of immediate type

– confusion, emotional lability, insomnia, nightmares

– visual disturbances, including blurred vision

– the patients predisposed to acute bronchial asthma,

gastritis, colitis, perforation of the gastrointestinal tract

– hepatitis

– toxic epidermal necrolysis, and Stevens-Johnson syndrome, angioedema, bullous dermatitis, polymorphic erythema, photosensitivity

, acute renal failure, interstitial nephritis.

Interaction

• when used concomitantly with other nonsteroidal anti-inflammatory drugs (as well as with acetylsalicylic acid), the risk of erosive and ulcerative lesions and gastrointestinal bleeding increases

• with antihypertensive drugs, the effectiveness of the latter may decrease

• with lithium preparations, lithium accumulation and an increase in its toxic effect may develop (monitoring of lithium concentration in the blood is recommended)

• with methotrexate, the side effect of the latter on the hematopoietic system increases (the risk of anemia and leukopenia, periodic monitoring of the general blood test is indicated)

• with diuretics, the risk of acute renal failure increases in patients with dehydration. Patients receiving Meloxicam in combination with diuretics, should receive a sufficient amount of fluid before therapy with Meloxicam is necessary to investigate the renal function

• concomitant use of NSAIDs and antagonists of receptors of angiotensin II (as well as ACE inhibitors) increases the effect of reduction of glomerular filtration, which may in patients with impaired renal function lead to the development of acute renal failure

• intrauterine contraceptives may reduce the effectiveness of the latter

• with anticoagulants (heparin, tiklopidin, warfarin), as well as with thrombolytic drugs (streptokinase, fibrinolysin) increases the risk of bleeding (requires periodic monitoring of indicators of blood coagulation)

• with cholestyramine, as a result of meloxicam binding, its excretion through the gastrointestinal

• tract cyclosporins increases: NSAIDs can indirectly increase the nephrotoxicity of cyclosporins through renal prostaglandins. Co-use of these drugs requires monitoring of renal function

• with selective serotonin reuptake inhibitors, which increases the risk of gastrointestinal bleeding;

• NSAIDs can cause sodium, potassium, and fluid retention and weaken the effect of saluretics. As a result, in predisposed patients, the use of NSAIDs can lead to the progression of heart failure and hypertension.

No pharmacokinetic drug interactions were detected with the simultaneous use of meloxicam and antacids, cimetidine, digoxin, furosemide.

How to take, course of use and dosage

Intramuscular use of the drug can only be used for 3-5 days (depending on the severity of the condition). In the future, treatment is continued with the use of oral forms (tablets) or rectal suppositories.

The recommended dose is 7.5 mg or 15 mg once a day, depending on the intensity of pain and the severity of the inflammatory process.

The drug is administered by deep intramuscular injection.

In patients with an increased risk of adverse reactions and with severe renal insufficiency, who are on hemodialysis, the dose should not exceed 7.5 mg per day. If there is a slight or moderate decrease in renal function (creatinine clearance is reduced by no more than 25 ml/min from normal), as well as with cirrhosis of the liver in remission, no dose adjustment is required.

The drug should not be administered intravenously.

The maximum daily dose of meloxicam is 15 mg.

Combined use. The total daily dose of the drug Meloxicam, used in the form of tablets, suppositories, suspension for oral use and injection, should not exceed 15 mg.

Due to possible incompatibilities, the contents of Meloxicam ampoules should not be mixed in the same syringe with other medications.

Overdose

Symptoms: nausea, vomiting, abdominal pain, increased other side effects of the drug.

Treatment: symptomatic. There are no specific antidotes. During clinical trials, cholestyramine was shown to accelerate the elimination of meloxicam.

Special instructions

Meloxicam in ampoules is not intended for intravenous use!

As with other NSAIDs, Meloxicam should be used with caution in patients with diseases of the upper gastrointestinal tract, as well as in patients receiving anticoagulant therapy. If peptic ulcer or gastrointestinal bleeding occurs, Meloxicam should be discontinued.

When Meloxicam is prescribed, gastrointestinal bleeding, ulceration or perforation may develop with or without prior symptoms and episodes of similar gastrointestinal complications in the past. In the elderly, there is a more severe course of these complications.

Special attention should be paid to patients who have experienced undesirable effects from the skin and mucous membranes, in such cases, discontinuation of Meloxicam should be considered.

NSAIDs, including Meloxicam, inhibit the synthesis of renal prostaglandins, which are involved in maintaining sufficient levels of renal blood flow. The use of NSAIDs in patients with reduced renal blood flow and circulating blood volume may accelerate renal decompensation, however, after discontinuation of NSAID therapy, renal function usually returns to its previous level. The risk of developing such reactions is particularly high in patients with dehydration, patients with congestive heart failure, cirrhosis of the liver, nephrotic syndrome and severe kidney diseases, in patients receiving diuretics, as well as those who have undergone significant surgery that led to hypovolemia. In such patients, diuresis and renal function should be carefully monitored from the very beginning of treatment.

In rare cases, Meloxicam, like other NSAIDs, can cause interstitial nephritis, glomerulonephritis, renal medulla necrosis, or nephrotic syndrome.

In rare cases, an increase in serum transaminases or changes in other indicators of liver function have been reported. In most cases, deviations from the norm were insignificant, transient.

If deviations from the norm are expressed or are permanent, you should stop taking Meloxicam and conduct control laboratory tests.

No dose reduction is required in patients with clinically non-progressive cirrhosis of the liver. Weakened and emaciated patients may suffer more severe side effects, and such patients should be carefully monitored. As with other NSAIDs, Meloxicam should be used with caution in elderly patients who are more likely to have impaired renal, liver, or heart function.

Meloxicam may promote sodium, potassium, and water retention and weaken the natriuretic effects of diuretics. As a result, in the presence of predisposing factors, the use of NSAIDs can lead to the progression of heart failure and hypertension. Therefore, clinical monitoring should be performed in patients at risk.

Like other NSAIDs, MOVALIS can mask the symptoms of infectious diseases.

Fertility

The use of meloxicam, as well as other drugs that inhibit cyclooxygenase/prostaglandin synthesis, may reduce fertility, and is not recommended for women planning pregnancy. Meloxicam may delay ovulation. Therefore, women with difficulty getting pregnant, as well as women undergoing infertility testing, should stop taking meloxicam.

Features of the drug’s effect on the ability to drive a vehicle or potentially dangerous mechanisms

If you experience side effects such as impaired visual acuity, dizziness or drowsiness, it is recommended to stop such activities as driving a car or working with machinery.

Form of production

Tablets

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C.

Keep out of reach of children!

Shelf life

1 year

Do not use after the expiration date.

Active ingredient

Meloxicam

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

Children as prescribed by a doctor, Adults as prescribed by a doctor

Indications

Osteochondrosis, Osteoarthritis and Arthritis, Osteoarthritis, Sciatica, Periarthritis, Sciatica, Rheumatoid Arthritis, Lumbago