2010/12/17

Bi-Xikam

Release form, composition and packing Bi-Xikam 
 
Pill light yellow, Valium. 1 tab. meloxicam 7.5 mg. Excipients: sodium citrate dihydrate, anhydrous lactose, microcrystalline cellulose, povidone (Kollidon, polyvinylpyrrolidone 25 000), colloidal silicon dioxide (Aerosil), crospovidone (poliplasdon VIC EL-10), magnesium stearate.

Pill light yellow, Valium. 1 tab. meloxicam 15 mg. Excipients: sodium citrate dihydrate, anhydrous lactose, microcrystalline cellulose, povidone (Kollidon, polyvinylpyrrolidone 25 000), colloidal silicon dioxide (Aerosil), crospovidone (poliplasdon VIC EL-10), magnesium stearate. Clinico-pharmacological group: NSAID. Selective COX-2 inhibitor.

Pharmacological action

NSAIDs. Has anti-inflammatory, analgesic and antipyretic effect. The mechanism of action is selective inhibition of enzymatic activity of COX-2 involved in the biosynthesis of prostaglandins in inflammation. In appointing the high-dose, long-term use and individual characteristics of the organism of COX-2 selectivity may be reduced. Inhibits the synthesis of prostaglandins in inflammation to a greater extent than in the mucosa of the gastrointestinal tract and kidneys.

Pharmacokinetics

Suction

After oral administration, is well absorbed from the gastrointestinal tract. The absolute bioavailability of meloxicam - 89%. Simultaneous ingestion does not alter absorption. While taking the drug orally at doses of 7.5 mg and 15 mg meloxicam concentration in plasma is proportional to dose. The vast differences between the Cmax and Cmin in plasma after a single dose is relatively small and at a dose of 7.5 mg of 0.4-1 mg / ml, a dose of 15 mg - 0.8-2 mg / ml, (presented, respectively, values and Cmin and Cmax ).

Distribution

Css achieved within 3-5 days. With prolonged use of the drug (more than 1 year) concentrations are similar to those that have been reported after first reaching an equilibrium state. Plasma protein binding of more than 99%. Vd is small and amounts to an average of 11 liters. Meloxicam crosses gistogematicheskie barriers, the concentration in the synovial fluid reaches 50% Cmax of the drug in blood plasma.

Metabolism

Meloxicam is almost completely metabolized in the liver with the formation of four pharmacologically inactive metabolites.

Breeding

T1 / 2 of meloxicam is 15-20 hours is derived equally from feces and urine, mostly as metabolites. With the feces as unchanged output of less than 5% of the daily dose in the urine as unchanged drug is found only in trace amounts. Plasma clearance is an average of 8 ml / min.

Pharmacokinetics in special clinical situations

In the elderly clearance of the drug decreases. Hepatic or renal failure of moderate severity did not significantly affect the pharmacokinetics of meloxicam.

Statement

Inflammatory and degenerative diseases of joints, accompanied by pain syndrome:
rheumatoid arthritis;
osteoarthritis;
Ankylosing spondylitis (ankylosing spondylitis).

Dosing regimen

The drug is taken orally during a meal one time per day. In rheumatoid arthritis the recommended dose is 15 mg / day. Depending on the therapeutic effect of the dose can be reduced to 7.5 mg / day. Osteoarthritis: The recommended dose - 7.5 mg / day. With the ineffectiveness of the dose may be increased to 15 mg / day.

If ankylosing spondylitis dose is 15 mg / day. The maximum daily dose should not exceed 15 mg. In patients with increased risk of side effects, as well as in patients with severe renal insufficiency on hemodialysis, the dose should not exceed 7.5 mg / day.

Side effect
From the digestive system: nausea, vomiting, abdominal pain, diarrhea, constipation, flatulence, erosive and ulcerative lesions of the gastrointestinal tract, perforation of stomach or intestinal ulcers, gastrointestinal bleeding (implicit or explicit), elevated liver enzymes, hepatitis, colitis, stomatitis , dry mouth, esophagitis, hyperbilirubinemia, belching.
Cardio-vascular system: tachycardia, increased blood pressure, feeling the tides.
With the respiratory system: exacerbation of bronchial asthma, cough.
CNS: headache, dizziness, tinnitus, disorientation, confusion, thoughts, sleep disturbance, drowsiness, emotional lability.
With the urinary system: edema, interstitial nephritis, renal medullary necrosis, urinary tract infection, proteinurniya, hematuria, renal failure, hypercreatininemia and / or an increase of urea in the blood serum.
On the part of the vision: conjunctivitis, blurred vision.
From the hemopoietic system: anemia, leukopenia, thrombocytopenia.
Dermatological reactions: itching, skin rash, increased photosensitivity.

Allergic reactions: urticaria, anaphylactoid reactions (including anaphylactic shock), angioedema, allergic vasculitis, erythema multiforme eksudativnaya (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome).

Other: fever.

Contraindications
"Aspirin" asthma;
gastric ulcer and duodenal ulcer in acute phase;
gastrointestinal, cerebrovascular or other bleeding;
severe renal insufficiency (unless hemodialysis);
severe hepatic impairment;
severe congestive heart failure;
Children up to age 15 years;
pregnancy;
Lactation (breastfeeding);
hypersensitivity to the drug.

Caution should be used on patients of advanced age, with erosive and ulcerative lesions of the gastrointestinal tract in history.

Pregnancy and lactation

The drug is contraindicated during pregnancy and lactation.

Use in hepatic dysfunction

Contraindicated in severe liver failure.

Use in renal impairment

In renal failure, if the spacecraft more than 25 ml / min correction dosing regimen is not required. In patients with increased risk of side effects, as well as in patients with severe renal insufficiency on hemodialysis, the dose should not exceed 7.5 mg / day. Contraindicated in severe renal failure if left hemodialysis.

Cautions

It should be used with caution on patients with an indication of a history of peptic ulcer of the stomach and duodenum, as well as in patients receiving anticoagulation therapy. In these patients at increased risk of erosive and ulcerative lesions of the gastrointestinal tract.

With care and control of indicators of kidney function should use the drug in elderly patients, patients with chronic heart failure with signs of circulatory failure in patients with cirrhosis and in patients with hypovolemia due to surgical interventions.

In renal failure, if CC> 25 ml / min correction dosing regimen is not required.

In patients on dialysis, the maximum dose is 7.5 mg / day.

Patients taking both diuretics and meloxicam, should get plenty of fluids.

If in the course of treatment have an allergic reaction (including itching, skin rash, urticaria) and photosensitivity, the patient should consult a doctor to solve the issue of termination of treatment.

Effects on ability to drive vehicles and management mechanisms

Use of the drug may cause unwanted effects in the form of headaches and dizziness, sleepiness. If you experience these phenomena should be abandoned vehicle, maintenance of machines and mechanisms.

Overdose

Symptoms: increased side effects.

Treatment: gastric lavage, activated charcoal reception (during the next hours after admission), the holding of symptomatic therapy. Kolestiramin accelerates the removal of meloxicam from the body. A specific antidote does not exist.

Drug Interactions

In an application with other NSAIDs (as well as of acetylsalicylic acid) and increased risk of erosive and ulcerative lesions and bleeding from the gastrointestinal tract. In an application with antihypertensive drugs may reduce the effectiveness of the latter.

In an application with lithium therapy may develop accumulation of lithium and increase its toxicity (recommended to control the concentration of lithium in the blood).

In an application with methotrexate increases the side effects of the latter on the hematopoietic system (risk of anemia and leukopenia, shows a periodic monitoring of blood count).