Inflamin rectal suppositories 0.015 g. №10

Description

Inflamin rectal Composition
active substance: meloxicam;

1 suppository contains meloxicam 15 mg;

excipient: solid fat.

Inflamin rectal  Dosage form
Rectal suppositories.

Basic physical and chemical properties: suppositories of light yellow color with a greenish tinge, bullet-shaped. The presence of plaque on the surface of the suppository is allowed.

Inflamin rectal  Pharmacotherapeutic group
Non-steroidal anti-inflammatory and antirheumatic drugs. ATX code M01A C06.

Pharmachologic effect
Inflamine is a non-steroidal anti-inflammatory drug of the enolic acid class that has anti-inflammatory, analgesic and antipyretic effects. Inflamine has high anti-inflammatory activity in all standard models of inflammation. The general mechanism of these effects may lie in the ability of Inflamine to inhibit the biosynthesis of prostaglandins – inflammatory mediators.

Inflamine’s safe mechanism of action is associated with selective inhibition of cyclooxygenase-2 (COX-2) compared to cyclooxygenase-1 (COX-1). The therapeutic effect of NSAIDs is associated with inhibition of COX-2 synthesis, while inhibition of COX-1 leads to side effects from the stomach and kidneys.

The selectivity of COX-2 inhibition by meloxicam has been confirmed by many researchers both in vitro and ex vivo. Inflamine (15 mg) preferentially inhibits COX-2 ex vivo, as evidenced by the greater inhibition of PGE2 production in response to lipopolysaccharide stimulation compared to the production of thromboxane in coagulated blood (COX-1). These effects are dose-dependent. Inflamine does not affect platelet aggregation or bleeding time at recommended doses ex vivo, whereas indomethacin, diclofenac, ibuprofen, and naproxen significantly inhibit platelet aggregation and prolong bleeding.

Clinical studies have established a low incidence of gastrointestinal side effects (perforation, ulceration and bleeding) when used in the recommended doses of meloxicam compared to standard doses of other NSAIDs.

Pharmacokinetics
Meloxicam is well absorbed from the digestive tract, which is reflected in a high absolute bioavailability (89%).

Bioequivalence of suppositories to capsules has been demonstrated. When using one suppository, the maximum concentration of meloxicam in the blood plasma is achieved after 5-6 hours.

Stable concentrations are achieved on the 3-5th day.

A single intake of a daily dose determines the concentration of the drug in the blood plasma with relatively small fluctuations between its peak and low point in the range from 0.8-2 μg / ml for a dosage of 15 mg (Cmin and Cmax at a stable equilibrium concentration).

The maximum stable equilibrium concentration in blood plasma after the use of suppositories is reached after about 5 hours.

Continuous treatment for a long period (for example, 6 months) did not lead to changes in pharmacokinetic parameters compared to parameters after 2 weeks of using meloxicam 15 mg per day. Any changes are also unlikely if the duration of treatment is more than 6 months.

Distribution. In plasma, more than 99% binds to blood plasma proteins (mainly albumin). Meloxicam penetrates into the synovial fluid at a concentration of about half that in the blood plasma.