Meloksikam solution

General characteristics. Structure:

Active agents: to meloksika of 10,00 mg/ml
excipients: glycine (aminoacetic acid), a macrogoal (polyethyleneglycol 400), меглумин (N - methyl - D - glyukamin), povidon-K 17 (пласдон S-15 or коллидон 17 F), 1,2 - propylene glycol, sodium hydroxide, water for injections.

Description:
Transparent liquid from color, yellow to yellow with a greenish shade.

Pharmacological properties:

Pharmacodynamics. Non-steroidal anti-inflammatory drug (NPVP), possesses antiinflammatory, febrifugal, analgetic action. Belongs to the class of oksikam; derivative enoliyevy acid. The action mechanism - inhibition of synthesis of prostaglandins (Pg) as a result of selective suppression of enzymatic activity of cyclooxygenase 2 (TsOG2). At appointment in high doses, prolonged use and specific features of an organism of TsOG2 selectivity decreases. Suppresses synthesis of Pg in the field of an inflammation more than in a mucous membrane of a stomach or kidneys that is connected with rather selective inhibition of TsOG2. Causes erosive and ulcer diseases of the digestive tract (DT) less often.

Pharmacokinetics. Meloksikam is completely absorbed after intramuscular introduction. Relative bioavailability in comparison with bioavailability at intake makes nearly 100%. After intramuscular administration of drug in a dose of 5 mg the maximum concentration in blood makes 1,62 mkg/ml and is reached within about 60 minutes.
Meloksikam well contacts proteins of a blood plasma, especially albumine (99%). Gets into synovial fluid. Concentration in synovial fluid makes about 50% of concentration in plasma. Distribution volume - on average 11 l. Interindividual deviations make 30-40%.
Meloksikam is almost completely metabolized to 4 pharmacological inert metabolites. The main metabolite, to 5-karboksimeloksika (60% of a dose), is formed by oxidation of an intermediate metabolite of a 5-gidroksimetilmeloksikam. The researches in vitro showed that in this metabolic transformation an important role is played by CYP2C9 isoenzyme, additional value has CYP3A4 isoenzyme. Peroxidase which activity can individually vary takes part in formation of two other metabolites (components respectively 16 and 4% of drug dose size).
Excretion of a meloksikam, it is preferential in the form of metabolites, it is carried out in identical quantity with urine and a stake. In not changed view with a stake less than 5% of the size of a daily dose are removed. In urine in not changed look drug is found only in trace quantities. The average elimination half-life makes about 20 h. Plasma clearance - on average 8 ml/min.
Meloksikam shows linear pharmacokinetics in doses of 7,5-15 mg at intramuscular introduction.

Indications to use:

Pseudorheumatism; osteoarthrosis; an ankylosing spondylarthritis (Bekhterev's disease) both the other inflammatory and degenerative diseases of joints which are followed by a pain syndrome. It is intended for symptomatic therapy, reduction of pain and an inflammation at the time of use; does not render on progressing of a disease of influence.

Route of administration and doses:

Intramuscular introduction of Meloksikam is reasonable during the first 2-3 days of treatment. Further it is necessary to pass to administration of drug inside.
The recommended Meloksikam's dose for injections makes 7,5 mg or 15 mg/days depending on intensity of a pain syndrome and expressiveness of inflammatory process. The maximum recommended daily dose should not exceed 15 mg.

At the patients with a chronic renal failure of heavy degree who are on a hemodialysis, Meloksikam's dose should not exceed 7,5 mg/days.
Considering that the dose mode for children and teenagers aged up to 15 years is not established, Meloksikam is appointed only to adults and teenagers 15 years are more senior.
Meloksikam it is necessary to enter by a deep intramuscular injection. It is not necessary to apply intravenously.

Features of use:

At emergence of round ulcers or gastrointestinal bleeding, development of side effects from skin and mucous membranes drug should be cancelled.
At patients with the reduced volume of the circulating blood (VCB) and reduced glomerular filtering (dehydration, HSN, cirrhosis, a nephrotic syndrome, clinically expressed diseases of kidneys, reception of diuretics, dehydration after big surgeries) emergence of clinically expressed HPN which is completely reversible after drug withdrawal (at such patients in an initiation of treatment it is necessary to monitorirovat a daily urine and function of kidneys) is possible. At permanent and essential increase in transaminases and change of other indicators of function of a liver drug should be cancelled and carried out control tests. At patients with the increased risk of side effects treatment begin 7,5 mg with a dose. In HPN end-stage at the patients who are on dialysis, the dose should not exceed 7,5 mg/days. During treatment it is necessary to be careful during the driving of motor transport and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions (at emergence of dizzinesses and drowsiness). For decrease in risk of development of the undesirable phenomena from a GIT it is necessary to use minimum effective dose minimum possible short course.

Side effects:

From the alimentary system: more than 1% - dyspepsia, including nausea, vomiting, abdominal pains, a lock, a meteorism, diarrhea; 0.1-1% - passing increase in activity of "hepatic" transaminases, a hyperbilirubinemia, an eructation, an esophagitis, a gastroduodenal ulcer, bleeding from a GIT (including hidden), stomatitis; less than 0.1% - perforation of a GIT, colitis, hepatitis, gastritis.
From bodies of a hemopoiesis: more than 1% - anemia; 0.1-1% - change of a blood count, including a leukopenia, thrombocytopenia.
From integuments: more than 1% - an itch, skin rash; 0.1-1% - a small tortoiseshell; less than 0.1% - a photosensitization, violent rashes, a multiformny erythema, including Stephens-Johnson's syndrome, a toxic epidermal necrolysis.
From respiratory system: less than 0.1% - a bronchospasm.
From a nervous system: more than 1% - dizziness, a headache; 0.1-1% - вертиго, a sonitus, drowsiness; less than 0.1% - confusion of consciousness, a disorientation, emotional lability.
From outside warmly - vascular system: more than 1% - peripheral hypostases; 0.1-1% - increase in the arterial pressure (AP), heartbeat, "inflows" of blood to face skin.
From an urinary system: 0.1-1% - a giperkreatininemiya and/or increase in urea in blood serum; less than 0.1% - an acute renal failure; connection with reception of a meloksikam is not established - intersticial nephrite, an albuminuria, a hamaturia.
From sense bodys: less than 0.1% - conjunctivitis, a vision disorder, including a sight illegibility.
Allergic reactions: less than 0.1% - a Quincke's disease, anaphylactoid/anaphylactic reactions.

Interaction with other medicines:

At a concomitant use with other NPVP the risk of development of cankers of a GIT and gastrointestinal bleeding increases.
At simultaneous use of NPVP with drugs of lithium concentration of ions of lithium in a blood plasma due to decrease in renal excretion of lithium increases. In case of need such combination therapy is recommended to exercise control of the level of ions of lithium in a blood plasma in an initiation of treatment, at selection of a dose and cancellation of a meloksikam.
Meloksikam reduces efficiency of intrauterine contraceptives (VMK), hypotensive medicines. Indirect anticoagulants, тиклопидин, heparin, trombolitik increase risk of bleedings. The methotrexate strengthens miyelodepressivny action; diuretics increase risk of development of renal failures; cyclosporine strengthens nephrotoxic action; Colestyraminum accelerates removal. Myelotoxic medicines strengthen manifestations of a gematotoksichnost of drug.

Contraindications:

Hypersensitivity (including to NPVP of other groups), a combination of bronchial asthma, the nose recuring a polypose and okolonosovy bosoms and intolerance of acetylsalicylic acid (ASK) and medicines of a pyrazolon row; a peptic ulcer of a stomach and a 12-perstny gut (in an aggravation phase), a heavy liver failure, the chronic renal failure (CRF) at the patients who are not exposed to dialysis (the clearance of creatinine (CC) less than 30 ml/min.), active gastrointestinal bleeding; the progressing diseases of kidneys, a heavy liver failure or an active disease of a liver, a state after performing aortocoronary shunting, the confirmed hyperpotassemia, inflammatory diseases of intestines, children's age (up to 15 years), pregnancy, the lactation period.

With care:
Advanced age, the coronary heart disease (CHD), the chronic heart failure (CHF), cerebrovascular diseases, дислипидемия / a lipidemia, a diabetes mellitus, diseases of peripheral arteries, smoking, KK less than 60 ml/min., GIT cankers in the anamnesis, existence of an infection of N. of pylori, long use NPVP, alcoholism, heavy somatopathies, a concomitant use of peroral glucocorticoid means (GKS) (including Prednisolonum), anticoagulants (including warfarin), antiagregant (including клопидогреля), selective serotonin reuptake inhibitors (including a tsitaloprama, fluoxetine, a paroksetin, sertraline).

Overdose:

Symptoms: consciousness disturbance, bleeding from digestive tract, an acute renal failure.
Treatment: there are no specific antidotes; symptomatic therapy is shown.

Storage conditions:

List B. In the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity: 3 years. Not to apply after a period of validity.

Issue conditions:

According to the recipe

Packaging:

Solution for intramuscular introduction of 10 mg/ml.
On 1,5 ml in the ampoules from glass of the 1st hydrolytic class of brown color having system of a break. On 3, 5 or 10 ampoules place in a blister strip packaging from a film polyvinyl chloride. On 1 or 2 blister strip packagings together with the application instruction place in a pack from a cardboard.