Meloxicam belongs to the NSAIDs class of oxicams is derived analboy acid
and has anti-inflammatory, analgesic and antipyretic effect. Expressed
anti-inflammatory effect maximumcontrolled on all standard models of inflammation.
The mechanism of action of meloxicam is gospodaresti to inhibit the synthesis of prostaglandins (known mediators of inflammation) by the selective suppression of fermentativnogo COX-2. When administered in wysokiego, long-term use and individuallydecorated body selectivity of inhibition of COX-2 decreases.
Meloxicam invivo inhibits the synthesis of prostaglandins at the site of inflammation to a greater extent, chemv the gastric mucosa or the kidney. These differences are associated with a selective ingibirovanie-2in comparison with COX-1. It is believed tongebirge COX-2 provides the therapeutic effect of NSAIDs, while ingibirovaniya the presence of the isoenzyme COX-1It may be the reason for side effects stomach and kidneys.
Selectivity of meloxicam in relation to COX-2 confirmed in various test systems in vitro and invivo. Selective sposobnostyami to inhibit COX-2 displayed when using as a test system cannonrosi human invitro. It was found that Malossi
Kam (at doses 7.5 mg and 15 mg) more ingibirovannoj-2, exerting a greater inhibitory influence the production of prostaglandin E2, stimuliresponsive (reaction, kontroliruemykh-2), than thromboxane production,involved in blood clotting(reaction, controlled by COX-1). These effects depended on the dose. In the exvivo studies shown that meloxicam (at doses 7.5 MMI 15 mg) had no effect on platelet aggregation and bleeding time.
After intake of meloxicam is well absorbed from the gastrointestinal tract, as evidenced by high
the absolute bioavailability (90%). After a single application meloxicamum in plasma
is achieved within 5-6 h. Odnovremennom food or antacids does not alter the absorption.
In applying the drug inside (in doses 7.5 and 15 mg), its concentration is proportional to
doses. Css is achieved within 3-5 days. The range of differences between the maximum and minimalistichnaya of the drug after it take 1 time/day is relatively small and consists of 0.4-1.0 mcg/ml when using the drug in dose of 7.5 mg, when used in a dose of 15 mg –0.8-2.0 µg/ml (shown, respectively, values of Cmin and Cmax at steady state), GoToMeeting and values beyond ukazannye. Smokelocke in plasma at steady state is achieved within 5-6 h of polarama inside.
After the/m introduction meloxicam is completely absorbed. The bioavailability of the drug is
approximately 100%. After the/m introduction, meloxicam a dose of 15 mg of Smahv priblizitelno plasma achieved through 1 h.
Meloxicam is very well associated with alkamides, especially albumin (99%). Predicament gistogematicalkie barriers, as well as in synovial fluid. The concentration in synovial fluid is approximately 50% of plasma concentration. Vd posledovatelnostyakh inside of meloxicam (at doses 7.5, 15 mg mgda) is about 16 l of coeficientului from 11% to 32%, when the/m introduction Vdсоставляет 11 l
Meloxicam is almost completely metaboliziruetsa the liver with the formation of 4 pharmacologically
inactive derivatives. The main metabolite,5′-carboxymethoxy (60% imposed dose),
is formed by oxidation of promezhutochnaya, 5′-hydroxymethyluracil, which-
that was also excreted, but to a lesser extent(9% of the administered dose). Studies invitro have shown that this metabolic prevrascheniya the role of the CYP2C9 isoenzyme, additional important isoenzyme CYP3A4.
The formation of two other metabolites (components, respectively, 16% and 4% of the administered dose
drug) participating peroxidase, activity which individually varies.
Excreted equally via the intestines to the kidneys, mainly as metabolites.
Unchanged through the intestines vvoditsya 5% of the magnitude of the daily dose, in the urine in an unmodified form the drug is detected in only trace amounts. The average T1/2 maximumvalue from 13 to 25 h (with the/m introduction – 20 hours).
Plasma clearance is in average 7-12 ml/min after a single dose of meloxicam, in the/m introduction – 8 ml/min.
Pharmacokinetics in special patient groups
The liver and pocetnastrana easy and moderate severity
significant impact on farmakokineticheskimi has not. The rate of excretion
of meloxicam from the body significantly, Viseu patients with renal insufficiency average
severity. Meloxicam worse, svyazyvaetsya plasma proteins in patients with end
renal failure. When terminologicheskii failure, the increase in Vd may
to result in higher free meloxicam concentrations, and therefore in such patients
daily dose should not exceed 7.5 mg.
The elderly patients compared to younger patients have similar pharmacokinetic parameters. Older patientswere plasma clearance at steady state are slightly lower than younger patients.
Uzenmunaigas age higher AUC values and prolonged T1/2 compared to the young patients of both sexes.
Short-term symptomatic therapy for:
Designed to reduce pain and inflammation at the time of use, progressiverelease not affected.
The drug is taken orally, during meals, without chewing.
In osteoarthritis, the daily dose is 7.5 mg,if necessary, may be increased
up to 15 mg/day.
In rheumatoid arthritis the drug naznachayut 15 mg/day, in achieving positive
therapeutic effect the dose may be reduced to 7.5 mg/day.
In ankylosing spondylitis the drug is administered at 15 mg/day, in achieving a positive therapeutic effect the dose may bitsyura to 7.5 mg/day.
In patients with an increased risk of pomocniczy initial dose is 7.5 mg/day.
In patients with severe renal insufficiency,on hemodialysis, dose should not exceed 7.5 mg/day. In patients with renal insufficiency mild to moderate severity (QC above than 30 ml/min) dose adjustment is not required.
In patients with liver cirrhosis (compensated)dose adjustment is not required.
The solution for the on/m introduction
The/m introduction the drug is indicated only teenieporn 2-3 days. Further treatment continues with the use of oral forms (tablets).The drug is injected deep into the/m. the Drug can be.
The recommended dose is 7.5 mg (0.75 ml) or 15 mg (1.5 ml) 1 times/day, depending on the intensity of the pain and the severity of the inflammatory process. The maximum recommended stockades – 15 mg (1.5 ml).
Given the possible incompatibility, meloxicam should not be mixed in the same syringe with other-
In patients with severe renal insufficiency,hemodialysis, and patients with an increased risk of adverse reactions dose not dorinaprivate 7.5 mg (0.75 ml)/day. For patients renal insufficiency mild or moderate (QC over 30 ml/min) correction desyne required.You should not use the drug odnovremenno other NSAIDs.
The total daily dose of meloxicam used in the form of tablets, suppositories, suspension for
ingestion and injection should not rise than 15 mg.
Adverse events below lists depending on the anatomical and physiological-
iceconnectionnumber occurrence.The frequency of occurrence is determined by who
and has the following gradation: very often (>10%);often (>1% and <10%); infrequently (>0.1% and <1%); rare(>0.01% and <0.1%); very rare (less than 0.01%, including isolated cases).
With the hematopoietic system: rarely – anemia; rare – change in the number of blood cells, including changes in leukocyte, leukopenia, thrombocytopenia.
The immune system: not known –anaphylactic shock, anaphylactoid/Ana-
vention of the reaction, other hypersensitivity reactions.
From the nervous system: often – Golovnaya; infrequently – dizziness, drowsiness.
Mental disorders: common – emotionallntelligence; not established – confusion, disorientation.
From the body of the vision: rarely – conjunctivitis,visual disturbances including blurred vision.
On the part of the organ of hearing: infrequent–vertigo; rarely–tinnitus.
From the digestive system: often–bolw stomach, indigestion, diarrhea, nausea, vomiting; infrequently – implicit or explicit gastro-kishechnorastvorimye, gastritis, stomatitis, constipation, vzdumaite, belching; rarely gastroduodenalis, colitis, esophagitis; very rarely – perforated.
The liver and biliary tract: rarely – transient changes of liver function parameters (e.g., increasing activesteering or bilirubin) very rare –
The skin and subcutaneous tissue: rare –angioneurotic edema, pruritus, rash;
rarely, urticaria, toxic epidermolysis, Stevens-Johnson syndrome; very
rarely bullous dermatitis, erythema multiforme; was found in the photosensitivity.
The respiratory system: rarely – bronchial asthma in patients allergic to acetylsalicylic acid or other NSAIDs.
From the side of cardiovascular system: rarely – increased blood pressure, a sense of “tide” of blood
to a person; rare – palpitations.
From the urinary system: infrequently –changing indicators of renal function (increase in creatinine concentration and/or mocheviny serum), urination disorders,including acute urinary retention; very rarely –acute renal failure.
Other: often – peripheral edema, edema, and bolw the site of drug injection (solution for the on/m introduction).
The combined use of drugs depressing the bone marrow (e.g.,
methotrexate) may cause cytopenia.
Gastrointestinal bleeding, ulcer or perforation can result in death.
As with other NSAIDs, do not rule out the possibility of interstitial nephritis, Glo-
maroneia, renal medullary necrosis,nephrotic syndrome.
|The purpose of the medication||Oxicams|