Meloksikam of a candle 0,015 No. 10

General characteristics. Structure:

International and chemical names: meloxicam; 4-gidroksi-2-metil-N-(5-methyl-2-тиазолил) - 2H-1,2-petrolthiazin-3-karboksamid 1,1 dioxide; main physical and chemical properties: suppositories of color, light yellow with a greenish shade. On the surface of suppository existence of a plaque is allowed. structure: 1 suppository contains a meloksikam of 15 mg; excipients: solid fat.

Pharmacological properties:

Pharmacodynamics. Antiinflammatory, analgetic, antipyretic. The mechanism of action is caused preferential by the selection inhibition of cyclooxygenase-2 that leads to oppression of biosynthesis of antiinflammatory prostaglandins in the inflammation center. Thanks to low affinity to cyclooxygenase-1, drug in therapeutic doses does not exert a negative impact on biosynthesis of the cytoprotective prostaglandins in digestive tract and kidneys, and also does not suppress functional activity of thrombocytes. Is hondroneytralny drug, does not influence proteoglycan synthesis by chondrocytes of a joint cartilage.

Pharmacokinetics. At rectal use to meloksika it is well adsorbed in a system blood stream, bioavailability makes 89%. Stable therapeutic concentration in blood is reached in 3-5 days after an initiation of treatment. Linkng with proteins of plasma makes more than 99%. Is exposed to biotransformation in a liver, it is preferential by oxidation with formation of 4 inactive metabolites. The main role in metabolism of a meloksikam is played by CYP2CP and CYP3A4 enzymes, and also peroxidase. Drug distribution volume low – on average 11 l, plasma clearance - 8 ml/min. The elimination half-life makes about 20 hours that allows to accept it 1 time a day. Removal from an organism happens kidneys and intestines in equal proportions; 5% of a daily dose are excreted in not changed look by intestines. Drug passes through gis-togematichesky barriers, well gets into synovial fluid where its concentration makes 50% of level in a blood plasma.
At elderly people only insignificant increase in the period of poluvy-maintaining drug and decrease in plasma clearance is observed (especially at women).
Essential change of pharmacokinetics of a meloksikam and increase in risk of development of side effects at purpose of drug by the patient with a liver or moderate renal failure (clearance of creatinine of 20-40 ml/min.) is noted.

Indications to use:

Inflammatory and degenerative diseases of joints (arthroses, osteoarthritis), the pseudorheumatism ankylosing a spondylarthritis.

Route of administration and doses:

To adults and teenagers 15 years are more senior appoint on 1 suppository rektalno 1 time a day. Suppositories of a meloksikam are intended for use during short time (5-7 days) then it is necessary to pass to use of a meloksikam in the form of tablets.

Features of use:

With care appoint to the patients having a peptic ulcer of a stomach or duodenum in the anamnesis and also the patients receiving anticoagulating therapy. In case of a round ulcer or gastrointestinal bleeding drug should be cancelled.
With care patients of advanced age should appoint drug with abnormal liver functions, kidneys and heart, and also the exhausted and weakened patient.
At emergence of changes of indicators of function of a liver treatment meloksikamy it is necessary to stop and conduct control laboratory researches.
Non-steroidal anti-inflammatory drugs inhibit synthesis of the renal prostaglandins participating in maintenance of normal level of a renal blood-groove. Therefore at purpose of non-steroidal anti-inflammatory drugs to patients with a reduced renal blood-groove or volume of the circulating blood there is a risk of development
decompensations of kidneys. In rare instances drugs of this group can cause intersticial nephrite, a glomerulonephritis, a necrosis of marrow of kidneys or a nephrotic syndrome. Patients need to consider possible negative influence of non-steroidal anti-inflammatory drugs on kidneys at purpose of a meloksikam with dehydration, congestive heart failure, cirrhosis, a nephrotic syndrome, heavy renal failures, and also to the patients who are accepting diuretics, transferred the operative measure which led to a hypovolemia. At patients of these categories from an initiation of treatment meloksikamy it is necessary to control a diuresis and function of kidneys.
At emergence of by-effects from the central nervous system (drowsiness, etc.), an organ of sight to patients it is necessary to refuse control of vehicles or work with mechanisms.

Side effects:

From digestive tract: dyspepsia, nausea, vomiting, abdominal pains, lock, meteorism, diarrhea; seldom – an esophagitis, stomatitis, an eructation, digestive tract erosive cankers, the latent or macroscopically visible gastrointestinal bleeding, tranzitorny changes of function of a liver (increase in level of hepatic transaminases or bilirubin); in some cases – perforation of intestines, colitis.
From the central and peripheral nervous system: headache; seldom – dizziness, a sonitus, drowsiness; in some cases change of mood, orientation disturbance, sleeplessness, nightmares.
From cardiovascular system: hypostases, it is rare – increase in arterial pressure, tachycardia.
From an urinary system: seldom – changes of laboratory indicators of function of kidneys (increase in level of creatinine and/or urea in blood); in some cases – an acute renal failure.
From system of a hemopoiesis: seldom – anemia, a leukopenia, thrombocytopenia.
Dermatological reactions: itch, rash; seldom – a small tortoiseshell; in some cases – a photosensitization, violent reactions, a multiformny erythema, Stephens-Johnson's syndrome, a toxic epidermal necrolysis.
Allergic reactions: in some cases – a Quincke's disease, reactions of immediate hypersensitivity (including anaphylactic and anaphylactoid).
Others: reactions of local irritation (burning, an itch in anorectal area), in some cases - conjunctivitis, vision disorders are possible (including an illegibility).

Interaction with other medicines:

At simultaneous use of a meloksikam with other non-steroidal anti-inflammatory drugs took away-ivayetsya risk of development of erosive cankers and bleedings in digestive tract.
It is necessary to avoid the combined use of drug with anticoagulants, trombolitika, antiagregant in connection with increase in risk of development of bleedings.
At simultaneous use with diuretics the risk of development of an acute renal failure in patients with dehydration in this connection the patients receiving to meloksika in combination with diuretics have to receive enough liquid increases. This category of patients before therapy meloksikamy needs to investigate function of kidneys.
Meloksikam can cause a delay of sodium, potassium, liquid therefore at predisposed patients the risk of progressing of heart failure and arterial hypertension increases.
Meloksikam reduces efficiency of beta adrenoblockers, inhibitors of an angiotensin-converting enzyme, vasodilators, diuretics, intrauterine contraceptives.
Meloksikam can strengthen a methotrexate gematotoksichnost in this connection at their simultaneous use laboratory control of peripheral blood is necessary. Meloksikam increases nephrotoxicity of cyclosporine therefore at their simultaneous use it is necessary to control function of kidneys.
At simultaneous use of a meloksikam with drugs of lithium increase in level of lithium in a blood plasma is noted. Holestiramin accelerates removal of a meloksikam.
Perhaps pharmacokinetic interaction of a meloksikam with hypoglycemic drugs, and also the means modifying activity or which are metabolized by means of cytochrome 2C9 or cytochrome 3A4.
Clinically significant interaction with antacids, Cimetidinum, digoxin and furosemide is not revealed.

Contraindications:

Inflammatory diseases of a rectum, rectal or proctal bleeding (including in the anamnesis), a peptic ulcer of a stomach or duodenum in an aggravation phase, the expressed abnormal liver functions, a renal failure (without carrying out a hemodialysis), the increased individual sensitivity to a meloksikam and other non-steroidal anti-inflammatory drugs and/or components of drug, pregnancy, the breastfeeding period, age up to 15 years.

Overdose:

Symptoms of acute overdose are the lethargy, drowsiness, nausea, vomiting, pain in epigastric area, gastrointestinal bleedings are possible. The serious poisoning can lead to arterial hypertension, an acute renal failure, liver dysfunction, a coma, a cardiac standstill. The phenomena described in the section "Side effect" are possible. Treatment: drug withdrawal, washing of a rectum, symptomatic therapy. There is no specific antidote.

Storage conditions:

In the place protected from light, at a temperature from +8 °C to + 15 °C. To store in the place, unavailable to children.  A period of validity – 2 years.

Issue conditions:

According to the recipe

Packaging:

On 5 suppositories in a blister strip packaging.