Mezavant - Instructions For Use, Analogues, Reviews, Price Of Tablets

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Mezavant

Mezavant: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Drug interactions
14. 14. Analogs
15. 15. Terms and conditions of storage
16. 16. Terms of dispensing from pharmacies
17. 17. Reviews
18. 18. Price in pharmacies

Latin name: Mezavant

ATX code: A07EC02

Active ingredient: mesalazine (Mesalazine)

Manufacturer: Cosmo S.p. A. (Cosmo, SpA) (Italy)

Description and photo update: 2019-08-10

Prices in pharmacies: from 3366 rubles.

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Mesavant is a drug with antimicrobial and local anti-inflammatory action.

Release form and composition

The drug is available in the form of enteric-coated tablets of prolonged action: biconvex, oblong, red-brown in color, engraved with "8476" on one side; the cross section shows a white or almost white core (12 pcs. in blisters, 5 blisters in a cardboard box and instructions for using Mezavant).

Composition for one tablet:

• active substance: mesalazine - 1200 mg;
• auxiliary components of the tablet core: stearic acid, talc, sodium carmellose (7MF and 7HXF), magnesium stearate, carnauba wax, sodium carboxymethyl starch (type A), colloidal silicon dioxide;
• enteric coating: copolymer of methyl methacrylate and methacrylic acid (1: 1), titanium dioxide, copolymer of methyl methacrylate and methacrylic acid (2: 1), macrogol 6000, talc, triethyl citrate, iron oxide red dye.

Pharmacological properties

Pharmacodynamics

Mesalazine is a derivative of 5-aminosalicylic acid. The exact mechanism of action of the drug is not fully understood, however, it is known that it has local anti-inflammatory activity against the intestinal epithelium. In chronic inflammatory bowel diseases in its mucous membrane, the formation of metabolites of arachidonic acid by lipoxygenase and cyclooxygenase pathways is enhanced. It is assumed that mesalazine attenuates the inflammatory process by inhibiting the synthesis of prostaglandins and inhibiting cyclooxygenases in the large intestine. It can suppress the activation of NF-kB (nuclear factor kappa-B) and, as a result, the production of major pro-inflammatory cytokines. Not so long ago, a hypothesis was put forward that the development of ulcerative colitis may be due to the lack of nuclear PPAR-γ receptors (γ-receptors,activated by the peroxisome proliferator). PPAR-γ receptor agonists have been shown to be effective in patients with ulcerative colitis. The data available to date indicate that the effect of mesalazine may be related to its effect on PPAR-γ receptors.

Pharmacokinetics

Mezavant tablets are coated with an enteric coating of methacrylic acid copolymers, and inside there is a core that contains mesalazine. The casing is designed in such a way that the release of the active substance begins only at a pH above 7.

After taking the drug inside, mesalazine quickly passes through the upper gastrointestinal tract (gastrointestinal tract) unchanged. Traces of the active substance are detected throughout the colon. Complete disintegration and release of mesalazine occurs after about 17.4 hours. The absorption of mesalazine after a single dose of Mezavant at a dose of 2.4 or 4.8 g for two weeks is equal to 21-22% of the dose taken orally. In blood plasma, mesalazine is determined 2 hours after taking on an empty stomach, and the maximum concentration is reached after 9-12 hours.

The pharmacokinetics of the drug show wide variability. The AUC indicator (area under the concentration-time curve) is directly proportional to the dose taken (in the dose range of 1.2–4.8 g). The maximum plasma concentration in the dose range of 1.2–2.4 g increased almost in direct proportion, and in the dose range of 2.4–4.8 g it increased less than proportionally to the dose taken.

After taking Mezavant with ordinary food (once and repeatedly in doses of 2.4 and 4.8 g), mesalazine is found in plasma after about 4 hours, and the maximum concentration is reached after 8 hours. Fatty foods slows down the absorption phase (when taken at a dose of 4, 8 g of mesalazine is detected in plasma only after 6 hours), however, this increases the systemic exposure of mesalazine.

The volume of distribution of the drug is relatively small and is about 18 liters. The connection of mesalazine with plasma proteins (if its concentration in plasma does not exceed 2.5 μg / ml) is not more than 43%.

The only important metabolite of the drug is inactive N-acetyl-5-aminosalicylic acid, which is formed in the cytosol of colon mucosa cells and liver cells under the action of the enzyme N-acetyltransferase-1.

The excretion of Mesavant is carried out mainly through the kidneys (excreted as a metabolite and in an unchanged form). Of 21-22% of absorbed mesalazine, less than 8% is excreted unchanged in the urine within 24 hours, and about 13% is excreted in the form of N-acetyl-5-aminosalicylic acid within 4 hours. The half-life of the drug after taking doses of 2.4 and 4.8 g averages 7-9 and 8-13 hours, respectively.

There are no data on the use of mesalazine in patients with impaired liver function. The systemic exposure of the drug in elderly patients after a single dose of 4.8 g was almost 2 times higher than in younger patients. The value of systemic exposure to mesalazine is inversely proportional to renal function (assessed by creatinine clearance). This fact must be taken into account when prescribing Mezavant to patients over 65 years old.

In case of impaired renal function, a decrease in the rate of excretion and an increase in the plasma concentration of mesalazine are possible, which increases the risk of unwanted side effects from the urinary system.

In women, the area under the AUC curve is 2 times higher than in males.

Indications for use

Mesavant is used to induce remission by endoscopic and clinical parameters in patients with ulcerative colitis of mild or moderate severity.

The drug is also prescribed for patients with ulcerative colitis to maintain remission.

Contraindications

Absolute:

• severe renal dysfunction (glomerular filtration rate less than 30 ml / min);
• severe liver dysfunction;
• children and adolescents up to 18 years old;
• increased individual sensitivity to salicylates (including mesalazine) or auxiliary ingredients of the drug.

Relative (Mezavant tablets are used with caution):

• mild to moderate renal / liver dysfunction;
• diseases that predispose to the development of pericarditis or myocarditis;
• chronic impairment of lung function (including bronchial asthma);
• allergy to sulfasalazine (since cross-hypersensitivity to mesalazine is possible);
• the period of pregnancy and breastfeeding. alicylates, including sensitivity to mesalazine and other salicylates, as well as ients

Mezavant, instructions for use: method and dosage

Mezavant tablets are taken orally, during meals, without chewing, not breaking or crushing, but swallowing whole.

Adults, including elderly patients (over the age of 65), in order to induce remission, are prescribed 2-4 tablets (2.4-4.8 g) of Mezavant once a day. If the patient is not sensitive to the minimum dose, it is recommended to use the drug in the maximum daily dose, which is 4 tablets (4.8 g). The effect of treatment when taking the maximum daily dose should be assessed no earlier than after 8 weeks.

To maintain remission, Mezavant is prescribed 2 tablets (2.4 g) once a day.

Side effects

Unwanted disorders that occur when taking Mezavant (the following classification of frequency of occurrence is used: very often - ≥ 1/10, often - ≥ 1/100 and <1/10, infrequently - ≥ 1/1000 and <1/100, rarely - ≥ 1 / 10,000 and <1/1000, very rarely - <1/10 000, with an unknown frequency - it is not possible to determine the frequency of side effects):

• digestive system: often - dyspeptic disorders, nausea, abdominal pain, vomiting, bloating, diarrhea, flatulence, abnormal liver function tests; infrequently - pancreatitis, colitis, rectal polyp; with an unknown frequency - cholelithiasis, hepatitis;
• respiratory system: infrequently - pain in the larynx and / or pharynx; with an unknown frequency - bronchospasm;
• cardiovascular system: often - increased blood pressure; infrequently - hypotension, tachycardia; with an unknown frequency - pericarditis, myocarditis;
• central nervous system: often - headache; infrequently - tremors, drowsiness, dizziness; with an unknown frequency - neuropathy;
• lymphatic system and blood: infrequently - a decrease in the number of platelets; rarely - agranulocytosis; with an unknown frequency - a decrease in the number of leukocytes (including neutrophils), aplastic anemia, a deficiency of erythrocytes, leukocytes and platelets;
• musculoskeletal system: often - back pain, arthralgia; infrequently - myalgia;
• urinary system: rarely - renal failure; with an unknown frequency - interstitial nephritis;
• skin and subcutaneous fat: often - skin rash, itching; infrequently - pathological baldness, acne;
• immune system: infrequently - nettle rash; with an unknown frequency - angioedema, pneumonitis (including eosinophilic and interstitial, as well as allergic alveolitis), anaphylactic reactions, DRESS syndrome;
• other reactions: often - fever, asthenia; infrequently - weakness, swelling of the face.

Overdose

Mesavant belongs to aminosalicylates, therefore the signs of drug poisoning are similar to the symptoms of intoxication with other salicylates. In particular, the patient experiences the following reactions: headache, drowsiness, tinnitus, hyperthermia, vertigo, hyperventilation, vomiting, diarrhea, increased sweating (against which dehydration is possible), pulmonary edema, hypoglycemia, impaired pH and electrolyte balance of the blood, confusion of consciousness.

Treatment methods for salicylate intoxication are standard. Therapy includes correction of fluid and electrolyte imbalance and hypoglycemia, as well as maintaining adequate renal function.

special instructions

Before starting treatment with Mezavant, as well as at least 2 times a year during treatment with the drug, it is necessary to examine kidney function.

Patients with asthma are especially at risk of developing hypersensitivity reactions, so they should be monitored.

In rare cases, during treatment with the drug, a severe violation of the blood composition develops. If the patient has unexplained bleeding, bruising or purpura, fever and sore throat, blood should be taken for analysis. If you suspect a change in the cellular composition of the blood, mesalazine therapy should be discontinued.

Mesavant can cause acute intolerance syndrome, which is often difficult to distinguish from an exacerbation of the inflammatory process in the intestine. The frequency of this phenomenon is not exactly known, but in controlled trials of sulfasalazine and mesalazine, it was up to 3%. The main symptoms of the syndrome are: acute abdominal pain, intestinal cramps, bloody diarrhea, sometimes rash, headache and fever. In case of any suspicion of acute intolerance syndrome, Mezavant should be canceled and no longer used.

Obstruction of the upper gastrointestinal tract (functional or organic) can inhibit the onset of the therapeutic effect.

Mesalazine may falsely increase urinary normetanephrine levels when tested by liquid chromatography, since the chromatograms of normetanephrine and N-acetyl-5-aminosalicylic acid (the main metabolite of mesalazine) are similar. An alternative method is recommended to determine the concentration of normetanephrine.

Influence on the ability to drive vehicles and complex mechanisms

It is believed that Mezavant does not affect the ability to drive vehicles and work with other potentially dangerous and complex mechanisms, however, no special studies have been conducted on this topic.

Application during pregnancy and lactation

Data on the use of Mezavant during pregnancy are limited. Mesalazine passes through the placenta to the fetus, but its concentration in fetal tissues is significantly lower than therapeutic concentrations. Animal studies have not revealed any adverse effects of mesalazine on the fetus, pregnancy, childbirth and further development of the offspring. In humans, the use of Mezavant during pregnancy is possible after assessing the expected benefit to the mother and the potential risk to the fetus. Care should be taken when prescribing large doses of the drug to pregnant women.

A certain amount of mesalazine is secreted in breast milk. The concentration of the metabolite in breast milk is slightly higher. The drug is used with caution during lactation, taking into account the ratio of benefits to the mother and risks to the child. Cases of sporadic diarrhea have been reported in breastfed babies whose mothers took mesalazine.

According to available data, Mezavant does not affect the ability of male patients to conceive.

Pediatric use

It is not recommended to prescribe mezavant to persons under 18 years of age, since there is no data on the efficacy and safety of mesalazine in children and adolescents under 18 years of age.

With impaired renal function

Patients with mild or moderate impairment of renal function should be careful when taking Mezavant.

The drug is contraindicated in patients with severely impaired renal function (at a glomerular filtration rate of less than 30 ml / min).

For violations of liver function

Since during treatment with mesalazine, there have been cases of increased activity of liver enzymes, Mezavant should be prescribed with caution in case of mild or moderate hepatic dysfunction.

For patients with severely impaired liver function, Mezavant is contraindicated.

Drug interactions

Mesalazine does not interact with the four most commonly used antimicrobial agents in medical practice (metronidazole, amoxicillin, sulfamethoxazole, and ciprofloxacin).

Mesavant should be used with caution in conjunction with nephrotoxic agents, including azathioprine and non-steroidal anti-inflammatory drugs, as the risk of unwanted side effects from the kidneys increases.

Mesalazine can inhibit the activity of the enzyme thiopurine methyltransferase, therefore it is used with caution in conjunction with mercaptopurine and azathioprine (due to the risk of a violation of the cellular composition of the blood).

Mesavant can reduce the activity of coumarin anticoagulants. If the use of this combination is necessary, the prothrombin time should be monitored regularly.

Analogs

Mezavant's analogs are: Mesakol, Kansalazin, Salofalk, Pentasa, Asakol and Ulcolfri.

Terms and conditions of storage

Keep out of the reach of children at a temperature not exceeding 25 ° C.

The shelf life of the tablets is 2 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Mezavant

According to reviews, Mezavant is a very good drug for the treatment of ulcerative colitis. Patients note that it is more effective than other mesalazine-containing drugs. The drug rarely causes side effects.

The main disadvantage is the price of the tablets, which is significantly higher than the average. Mezavant is not always available in pharmacies.

The price of Mezavant in pharmacies

The price of Mezavant in the form of enteric-coated tablets of prolonged action (60 pcs. Per pack) is 3990–4120 rubles.

Mezavant: prices in online pharmacies

Drug name Price Pharmacy

Mezavant 1200 mg enteric-coated tablets of prolonged action 60 pcs. 3366 RUB Buy

Mezavant tablets p.p. prolonged action 1200mg 60 pcs. 4034 RUB Buy

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!