Exen-Sanovel - instructions for use, dose, side effects, contraindications

Composition:Composition 1 tablet contains:
Active substance: meloxicam 7.5 mg, 15 mg.
Excipients: lactose monohydrate, sodium citrate dihydrate, microcrystalline cellulose, povidone, silicon dioxide colloid, crospovidone, magnesium stearate.

Description:Description 7.5 mg: Round biconvex tablets with a light yellow color with a greenish hue sided risk.
15 mg: oval biconvex light yellow to greenish in color with two-way risk.

Pharmacotherapeutic group:nonsteroidal anti-inflammatory drug

ATX: & nbsp

M.01.A.C.06 Meloksikam

M.01.A.C Oksikamy

Pharmacodynamics:Eksen-sanovel - a non-steroidal anti-inflammatory drug having analgesic, antiinflammatory and antipyretic action. The mechanism of action is associated with the inhibition of the synthesis of prostaglandins as a result of selective suppression of the enzymatic activity of cyclooxygenase-2 (COX-2), involved in the biosynthesis of prostaglandins in the inflammatory region. When the appointment in high doses, long-term use and individual features of the organism, COG-2, the selectivity decreases. Suppresses the synthesis of prostaglandins in the inflammation region to a greater extent than in the gastric mucosa or kidneys, which is associated with a relatively selective inhibition of COX-2. Less often causes erosive and ulcerative diseases of the gastrointestinal tract (GIT). Less meloxicam acts on cyclooxygenase-1 (COX-1), involved in the synthesis of prostaglandins, protecting the mucous membrane of the gastrointestinal tract and taking part in the regulation of blood flow in the kidneys.

Pharmacokinetics:It is well absorbed from the gastrointestinal tract, the absolute bioavailability of meloxicam is 89%. Simultaneous food intake does not change the intake. When using the drug inside at doses of 7.5 and 15 mg, its concentrations are proportional to the doses. Equilibrium concentrations are reached within. 3-5 days. With prolonged use of the drug (more than 1 year), the concentrations are similar to those observed after the first achievement of a steady state of pharmacokinetics.
Binding to plasma proteins is more than 99%. The range of differences between the maximum and basal concentrations of the drug after its administration once a day is relatively small and amounts to using a dose of 7.5 mg 0.4-1.0 μg / ml, and when a dose of 15 mg is 0.8-2, 0 μg / ml, (Cmin and Stach, respectively). Meloksikam penetrates through the histohematological barriers, the concentration in the synovial fluid reaches 50% of the maximum concentration of the drug in the plasma.Almost completely metabolized in the liver with the formation of four pharmacologically inactive derivatives. The main metabolite, 5'-carboxymeloxicam (60% of the dose value), is formed by oxidation of the intermediate metabolite, 5'-hydroxymethylmeloxicam, which is also excreted, but to a lesser degree (9% of the dose value). In vitro studies have shown that CYP 2C9 plays an important role in this metabolic transformation, the CYP isoenzyme ZA4 is of additional importance. In the formation of two other metabolites (which, respectively, account for 16% and 4% of the dose), peroxidase takes part, the activity of which probably varies individually.
It is excreted equally through the intestines and kidneys, mainly in the form of metabolites. Through the intestine unchanged output of less than 5% of the daily dose in the urine as unchanged drug is detected only in trace amounts. The half-life period (T1 / 2) of meloxicam is 15-20 hours. Plasma clearance is an average of 8 ml / min. In elderly people, the clearance of the drug is reduced. The volume of distribution is low, and averages 11 liters.
Hepatic or renal failure of moderate severity does not significantly affect the pharmacokinetics of meloxicam.

Indications:- Symptomatic treatment of osteoarthritis;
- Symptomatic treatment of rheumatoid arthritis;
- Symptomatic treatment of ankylosing spondylitis (Bekhterev's disease).

Contraindications:- hypersensitivity to meloxicam or auxiliary components of the drug; lactose is included, so patients with rare hereditary diseases such as galactose intolerance, lactase deficiency or glucose-galactose malabsorption should not take the drug;
- condition after aortocoronary shunting;
uncompensated heart failure;
- anamnestic data on an attack of bronchial obstruction, rhinitis,
- urticaria after taking acetylsalicylic acid or other NSAIDs (complete or incomplete acetylsalicylic acid intolerance syndrome - rhinosinusitis, urticaria, polyps of the nasal mucosa, asthma);
- erosive and ulcerative changes in the mucous membrane of the stomach or duodenum, active gastrointestinal bleeding;
- Inflammatory bowel disease (ulcerative colitis, Crohn's disease);
- cerebrovascular bleeding or other bleeding;
- severe hepatic impairment or active liver disease;
- chronic renal insufficiency in patients not undergoing dialysis (creatinine clearance less than 30 ml / min), progressive kidney diseases incl. confirmed hyperkalemia;
- pregnancy, the period of breastfeeding;
- Children under 15 years.

Carefully:Ischemic heart disease, cerebrovascular disease, congestive heart failure, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, creatinine clearance less than 60 ml / min.
Anamnestic data on the development of gastrointestinal ulcer, the presence of Helicobacter pylori infection, advanced age, prolonged use of NSAIDs, frequent alcohol consumption, severe physical illness, concomitant therapy with the following drugs:
- anticoagulants (for example, warfarin)
- antiaggregants (for example, acetylsalicylic acid, clopidogrel)
- oral glucocorticosteroids (for example, prednisolone)
- selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline)
To reduce the risk of developing adverse events on the part of the gastrointestinal tract, a minimum effective dose should be used with the minimum possible short course.

Pregnancy and lactation:Contraindicated in pregnancy and lactation.

Dosing and Administration:The drug is taken orally during meals at a daily dose of 7.5 - 15 mg.
Recommended dosing regimen:
- Rheumatoid arthritis: 15 mg per day. Depending on the therapeutic effect, the dose can be reduced to 7.5 mg per day.
- Osteoarthritis: 7.5 mg per day. If the dose is ineffective, it can be increased to 15 mg per day.
- Ankylosing spondylitis: 15 mg per day.
The maximum daily dose should not exceed 15 mg.
In patients with an increased risk of side effects, as well as in patients with severe renal failure who are on hemodialysis, the dose should not exceed 7.5 mg per day.

Side effects:From the digestive system: more than 1% - dyspepsia, incl. nausea, vomiting, abdominal pain, constipation, flatulence, diarrhea; 0.1-1% - a transient increase in the activity of "liver" transaminases, hyperbilirubinemia, belching, esophagitis, gastroduodenal ulcer, bleeding from the gastrointestinal tract (incl.latent), stomatitis; less than 0.1% - perforation of the gastrointestinal tract, colitis, hepatitis, gastritis.
On the part of the organs of hematopoiesis: more than 1% - anemia; 0.1-1% change in the blood formula, incl. leukopenia, tamocytopenia.
From the skin: more than 1% - itching, skin rash; 0,1-1% - urticaria; less than 0.1% - photosensitivity, bullous eruptions, erythema multiforme, incl. Stevens-Johnson syndrome, toxic epidermal necrolysis.
On the part of the respiratory system: less than 0.1% - bronchospasm.
From the nervous system: more than 1% - dizziness, headache; 0,1-1% - vertigo, tinnitus, drowsiness; less than 0,1% - confusion, disorientation, emotional lability.
From the cardiovascular system: more than 1% - peripheral edema; 0.1-1% - increased blood pressure, palpitations, "tides" of blood to the skin of the face. From the side of the urinary system: 0.1-1% - hypercreatininaemia and / or increased urea in the blood serum; less than 0.1% - acute renal failure; connection with the reception of meloxicam is not established - interstitial nephritis, albuminuria, hematuria.
From the sense organs: less than 0.1% - conjunctivitis, visual impairment, incl. blurred vision.
Allergic reactions: less than 0.1% - angioedema, anaphylactoid / anaphylactic reactions.

Overdose:Symptoms: impaired consciousness, nausea, vomiting, epigastric pain, gastrointestinal bleeding, acute renal failure, hepatic insufficiency, respiratory arrest, asystole.
Treatment: there is no specific antidote; When overdosing the drug should be washed stomach, taking activated charcoal (within the next hour, symptomatic therapy, forced diuresis, alkalinization of urine, hemodialysis - ineffective due to the high connection of the drug with blood proteins.

Interaction:- With simultaneous use with other non-steroidal anti-inflammatory drugs (as well as with acetylsalicylic acid), the risk of erosive and ulcerative lesions and bleeding of the gastrointestinal tract increases;
- With simultaneous use with antihypertensive drugs, it is possible to reduce the effectiveness of the latter;
- With simultaneous use with lithium preparations, development of cumulation of lithium and increase of its toxic effect (it is recommended to control the concentration of lithium in the blood);
- With simultaneous use with methotrexate, the side effect of the latter on the hematopoietic system is increased (the risk of anemia and leukopenia, periodic monitoring of the general blood test is shown);
- With simultaneous use with diuretics and with cyclosporine, the risk of developing kidney failure increases;
- With simultaneous use with intrauterine contraceptives, the effectiveness of the latter may be reduced;
- With simultaneous use with anticoagulants (heparin, ticlopidine, warfarin), as well as with thrombolytic drugs (streptokinase, fibrinolysin), the risk of bleeding increases (periodic monitoring of blood coagulability indices is necessary).
- With simultaneous application with colestyramine, the excretion of the drug from the body is accelerated.
- With simultaneous application with selective serotonin reuptake inhibitors, the risk of developing gastrointestinal bleeding increases.

Special instructions:- Care should be taken when using the drug in patients who have a history of peptic ulcer and duodenal ulcer, as well as patients who are on anticoagulation therapy. In such patients, the risk of erosive and ulcerative diseases of the gastrointestinal tract is increased.
- Care should be taken to monitor kidney function in elderly patients, patients with chronic heart failure with circulatory failure, in patients with cirrhosis, as well as in patients with hypovolemia as a result of surgical interventions.
- Patients with a slight or moderate decrease in renal function (creatinine clearance more than 25 ml / min) do not require correction of the dosing regimen.
- Patients taking both diuretics and meloxicam, should take a sufficient amount of fluid.
- If in the course of treatment there were allergic reactions (itching, skin rash, urticaria, photosensitivity) it is necessary to see a doctor with the purpose of resolving the issue of stopping the drug.
- Meloksikam, as well as other NSAIDs, can mask the symptoms of infectious diseases.
- The use of meloxicam, as well as other drugs that block the synthesis of prostaglandins, can affect fertility, so it is not recommended for women who want to become pregnant.

Effect on the ability to drive transp. cf. and fur:The use of the drug can cause the emergence of unwanted effects in the form of headaches and dizziness, drowsiness. It should abandon the management of vehicles and maintenance of machines and mechanisms that require concentration of attention.

Form release / dosage:Tablets of 7.5 mg and 15 mg.
For 10 tablets in a blister of PVC-aluminum foil. For 3 blisters in a cardboard pack together with instructions for use.

Packaging:

(10) - packings, cellular, outline (3) - packs, cardboard

Storage conditions:List B
In a dry place, at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:Tablets with a dosage of 7.5 mg - 4 years, tablets with a dosage of 15 mg - 3 years.
Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-005804/09

Date of registration:17.07.2009

The owner of the registration certificate:Sanovel Pharmaco-industrial trading companySanovel Pharmaco-industrial trading company Turkey

Information update date: & nbsp16.08.2015

Illustrated instructions

Instructions

Exen-Sanovel (Exen-Sanovel)