Mesipol
Mesipol: 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:
ATX code:
Active substance:
Manufacturer:
Description and photo updated: 20.11.2018
Mesipol is a drug with analgesic, antipyretic and anti-inflammatory effects, used for the symptomatic treatment of inflammatory and degenerative diseases of the joints.
Release form and composition
Dosage forms of Mesipol release:
- solution for intramuscular injection: transparent, yellow or greenish-yellow, has a characteristic odor (in a cardboard box 3 or 5 ampoules of 1.5 ml);
- tablets: with a flat surface, round, yellow, on one side with a line (in a cardboard box 1 or 2 blisters of 10 pcs.).
Composition of 10 ml of Mesipol solution:
- active substance: meloxicam - 100 mg;
- additional components: glycofurol - 1000 mg; glycine - 50 mg; meglumine - 62.5 mg; poloxamer 188 - 500 mg; sodium hydroxide - 1.52 mg; sodium chloride - 30 mg; water for injection - up to 10 ml.
Composition of 1 tablet Mesipol:
- active substance: meloxicam - 7.5 or 15 mg;
- additional components: microcrystalline cellulose, lactose monohydrate, corn starch, sodium citrate, pregelatinized starch, colloidal silicon dioxide, magnesium stearate.
Pharmacological properties
Pharmacodynamics
Mesipol is one of the NSAIDs (non-steroidal anti-inflammatory drugs).
It has analgesic, antipyretic and anti-inflammatory effects. The anti-inflammatory effect of the drug is associated with inhibition of the enzymatic activity of COX-2 (cyclooxygenase), which in the area of inflammation takes part in the biosynthesis of prostaglandins. The impact on COX-1 is carried out to a lesser extent.
Pharmacokinetics
Injection solution
After intramuscular administration of Mesipol, meloxicam is completely absorbed. Possesses high bioavailability (almost 100%). C max (maximum concentration of the substance) in plasma after intramuscular administration of 15 mg of meloxicam is 0.001 62 mg / ml, the time to reach it is about 60 minutes.
To a large extent (about 99%) it binds to plasma proteins (mainly albumin). Penetrates into synovial fluid, passes through histohematogenous barriers. The concentration in the synovial fluid is approximately 50% of the plasma concentration of the drug. V d (volume of distribution) –11 l.
Meloxicam is metabolized in the liver almost completely with the formation of four metabolites (pharmacologically inactive). An important role in metabolic conversion is played by the CYP2C9 isoenzyme; the participation of the CYP3A4 isoenzyme and peroxidase is less significant.
The significant intestinal-hepatic circulation characteristic of meloxicam has no effect on the elimination of the drug. The substance is excreted mainly in the form of metabolites equally by the intestines and kidneys. Up to 5% of meloxicam is excreted unchanged by the intestine; only trace amounts of unchanged Mesipol are determined in the urine.
The average T 1/2 (half-life) of meloxicam is 20 hours. Plasma clearance averages 8 ml / min.
Pills
Meloxicam is well absorbed from the gastrointestinal tract, its absolute bioavailability is 89%. Taking the drug simultaneously with food does not affect absorption.
The concentration of Mesipol is proportional to the dose received. The time to reach equilibrium concentrations is 3-5 days. With prolonged use (longer than 12 months), the concentrations of meloxicam are similar to those observed after the first achievement of a steady state of pharmacokinetic parameters.
Plasma protein binding - from 99%. The range of differences between the highest and basal concentrations of Mesipol after taking it once a day is relatively small and is 0.000 4-0.001 or 0.000 8-0.002 mg / ml (when using a dose of 7.5 or 15 mg, respectively). The substance penetrates the histohematogenous barriers.
It is excreted mainly in the form of metabolites in equal measure with urine and feces. In unchanged form, less than 5% of the daily dose is excreted in the feces, the drug is found in unchanged form in the urine only in trace amounts. T 1/2 - 15–20 hours. Plasma clearance averages 8 ml / min. The clearance of the drug in the elderly is reduced.
Hepatic / renal failure of moderate severity does not significantly affect the pharmacokinetic processes of meloxicam.
Indications for use
According to the instructions, Mesipol is prescribed for the symptomatic treatment of the following diseases:
- rheumatoid arthritis;
- ankylosing spondylitis (ankylosing spondylitis);
- osteoarthritis;
- other inflammatory and degenerative diseases of the joints, occurring with pain.
Contraindications
Injection solution
Absolute:
- complete or partial combination of bronchial asthma, recurrent nasal / paranasal sinus polyposis with intolerance to acetylsalicylic acid and other NSAIDs (including a burdened history);
- active gastrointestinal bleeding;
- kidney disease of a progressive nature, including confirmed hyperkalemia;
- severe renal failure in patients who have not undergone dialysis (with creatinine clearance less than 30 ml / min);
- intestinal diseases of an inflammatory nature (nonspecific ulcerative colitis, granulomatous enteritis);
- severe liver failure or active liver disease;
- erosive and ulcerative changes in the mucous membrane of the stomach or duodenum;
- heart failure in the stage of decompensation;
- period after coronary artery bypass grafting;
- cerebrovascular or other bleeding;
- age up to 18 years;
- pregnancy and the period of breastfeeding;
- individual intolerance to the components of the drug.
Relative (Mesipol is prescribed under medical supervision):
- the presence of an infection with Helicobacter pylori (Helicobacter pylori);
- long-term use of NSAIDs;
- cardiac ischemia;
- cerebrovascular diseases;
- chronic heart failure;
- hyperlipoproteinemia;
- diabetes;
- impaired renal function with creatinine clearance less than 60 ml / min;
- peripheral arterial disease;
- a history of indications of ulcerative lesions of the gastrointestinal tract;
- frequent use of alcoholic beverages;
- smoking;
- severe somatic diseases;
- combined use with oral glucocorticosteroids (prednisolone), anticoagulants (warfarin), antiplatelet agents (acetylsalicylic acid, clopidogrel), third-generation antidepressants (citalopram, fluoxetine, paroxetine, sertraline);
- elderly age.
Pills
Absolute:
- aspirin bronchial asthma;
- exacerbation of gastric ulcer and duodenal ulcer;
- renal / hepatic impairment in severe course;
- active gastrointestinal bleeding;
- pregnancy and the period of breastfeeding;
- age up to 15 years;
- individual intolerance to the components of the drug.
Relative (Mesipol is prescribed under medical supervision):
- burdened history of erosive and ulcerative lesions of the gastrointestinal tract;
- elderly age.
Instructions for the use of Mesipol: method and dosage
With the combined use of different dosage forms of Mesipol, the total dose should not exceed 15 mg per day.
In cases of increased risk of adverse reactions, as well as severe renal failure in patients on hemodialysis, the maximum daily dose is 7.5 mg.
Injection solution
Mesipol is administered intramuscularly (deep intramuscular injection). The solution cannot be administered intravenously.
Injection administration is indicated only during the first two to three days of therapy, then patients are transferred to take the drug inside.
The recommended daily dose of Mesipol is 7.5 or 15 mg once (the dose is determined by the intensity of pain and the severity of the inflammatory process).
Do not mix Mesipol in the same syringe with other drugs / substances.
Pills
Mesipol is taken orally once a day, preferably with meals.
Recommended daily intake:
- osteoarthritis: 7.5 mg, possibly doubled;
- rheumatoid arthritis: 15 mg, possibly halving;
- ankylosing spondylitis: 15 mg.
Side effects
Mesipol therapy can lead to the development of the following disorders (> 10% - very often;> 1% and 0.1% and 0.01% and <0.1% - rarely; <0.01% - very rarely):
- skin: often - skin rash, itching; infrequently - urticaria; rarely - bullous rashes, increased sensitivity to the action of ultraviolet / visible radiation, erythema multiforme, including Stevens-Johnson syndrome, toxic epidermal necrolysis;
- allergic reactions: rarely - anaphylactic / anaphylactoid reactions, Quincke's edema;
- digestive system: often - dyspepsia, including nausea, vomiting, abdominal pain, flatulence, constipation, diarrhea; infrequently - increased activity of transient hepatic transaminases, latent / overt bleeding from the gastrointestinal tract, hyperbilirubinemia, esophagitis, belching, erosive and ulcerative lesions of the gastrointestinal tract, stomatitis; rarely - gastritis, perforation of the gastrointestinal tract, hepatitis, colitis;
- cardiovascular system: often - peripheral edema; infrequently - increased blood pressure, flushing of the skin of the face, palpitations;
- hematopoietic system: often - anemia; infrequently - a change in the blood count, including leukopenia, thrombocytopenia;
- central nervous system: often - headache, dizziness; infrequently - tinnitus, vertigo, drowsiness; rarely - emotional lability, disorientation, confusion;
- urinary system: infrequently - hypercreatininemia / increased serum urea; rarely - renal failure in acute course; with the reception of meloxicam, the connection has not been confirmed - proteinuria, interstitial nephritis, hematuria;
- sense organs: rarely - conjunctivitis, visual impairment (including blurred vision);
- respiratory system: rarely - bronchospasm;
- local reactions (intramuscular solution): burning / pain at the injection site.
The severity and frequency of development of disorders can vary depending on the dosage form of Mesipol.
Overdose
The main symptoms are manifested in the form of asystole, respiratory arrest, impaired consciousness, gastrointestinal bleeding, nausea, epigastric pain, vomiting, liver failure, acute renal failure.
There is no specific antidote. Shows symptomatic therapy, gastric lavage. According to clinical studies, the elimination of meloxicam is accelerated by cholestyramine. Due to the high degree of binding to blood proteins, hemodialysis is ineffective.
special instructions
Due to the increased likelihood of developing erosive and ulcerative diseases of the gastrointestinal tract, caution during therapy should be observed by patients with a burdened history of gastric ulcer and duodenal ulcer, as well as with the combined use of Mesipol with anticoagulants.
It also requires caution and control of renal function during the use of the drug in elderly patients, with chronic heart failure with symptoms of cirrhosis, liver cirrhosis, hypovolemia associated with surgical interventions.
In patients with mild to moderate renal insufficiency, correction of the Mesipol dosage regimen is not required.
Against the background of combined use with diuretics, patients should consume sufficient liquid.
When allergic reactions appear during treatment (in the form of itching, urticaria, skin rash, photosensitivity), therapy is canceled.
Like other NSAIDs, Mesipol can mask the symptoms of infectious diseases.
Influence on the ability to drive vehicles and complex mechanisms
During the period of therapy, it is recommended to refuse to drive vehicles, which is associated with the likelihood of adverse reactions (dizziness, headache, drowsiness).
Application during pregnancy and lactation
Mesipol is not prescribed for women during pregnancy / breastfeeding.
Pediatric use
Therapy with Mesipol is contraindicated:
- injection solution: up to 18 years old;
- tablets: up to 15 years.
With impaired renal function
Therapy with Mesipol is contraindicated:
- injection solution: severe renal failure in patients not undergoing dialysis (creatinine clearance less than 30 ml / min); kidney disease of a progressive nature, including confirmed hyperkalemia;
- tablets: renal failure in severe course.
For violations of liver function
Therapy with Mesipol is contraindicated:
- injection solution: severe liver failure or active liver disease;
- tablets: severe hepatic impairment.
Use in the elderly
Mesipol in all dosage forms for elderly patients should be prescribed under medical supervision.
Drug interactions
- drugs with hypotensive action: the effectiveness of their action decreases;
- other NSAIDs: the likelihood of developing erosive and ulcerative lesions and bleeding of the gastrointestinal tract increases;
- diuretics: the likelihood of impaired renal function increases;
- intrauterine contraceptives: their effectiveness decreases;
- cholestyramine: its excretion is enhanced;
- lithium preparations: accumulation of lithium develops, which leads to an increase in its toxic effect (it is recommended to control the concentration of lithium in the blood);
- methotrexate: its side effects on the hematopoietic system are enhanced (the risk of leukopenia and anemia increases; periodic monitoring of a general blood test is shown);
- cyclosporine: the toxic effect of Mesipol increases, manifested by kidney damage;
- anticoagulants (ticlopidine, heparin, warfarin), thrombolytic drugs (fibrinolysin, streptokinase): the likelihood of bleeding increases (periodic monitoring of blood clotting parameters is required);
- drugs with myelotoxic effect: the manifestations of hematotoxicity of meloxicam increase;
- antidepressants of the third generation: the likelihood of developing gastrointestinal bleeding increases.
Analogs
Analogs of Mesipol are: Movix, Medsikam, Movalis, Bi-xikam, MELBEK, M-Kam, Artrozan, Melbek Forte, Flexibon, Movasin, Oksikamoks, Meloxicam, Mirlox, Meloflam, Liberum, Amelotex, Mataren, Melox.
Terms and conditions of storage
Store in a place protected from light and moisture at temperatures up to 25 ° C. Keep out of the reach of children.
Shelf life:
- injection solution - 2 years;
- tablets - 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Mesipol
According to reviews, Mesipol is a fast-acting and effective drug used to relieve pain and inflammation in joint diseases. Of the shortcomings, they indicate the likelihood of developing adverse reactions.
The price of Mesipol in pharmacies
The approximate price for Mesipol (3 or 5 ampoules per pack) is 285–404 or 365–475 rubles.
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, 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!
