Lornoxicam, lyophilizate 8 mg 5 pcs

Pharmacodynamics

Lornoxicam is a non-steroidal anti-inflammatory agent, has pronounced analgesic and anti-inflammatory effect, belongs to the class of oxycams.

The mechanism of action is the inhibition of prostaglandin synthesis (inhibition of cyclooxygenase enzyme), leading to suppression of inflammation.

Lornoxicam has no effect on key body parameters: body temperature, heart rate (HR), blood pressure (BP), electrocardiogram (ECG), spirometry.

The analgesic effect of lornoxicam is not associated with narcotic action.

Lornoxicam does not have an opiate-like effect on the central nervous system (CNS). Unlike narcotic analgesics it does not suppress respiration and does not cause drug addiction.

Due to the local irritating effect on the gastrointestinal tract (GIT) and systemic ulcerogenic effect associated with inhibition of prostaglandin synthesis, GIT complications are common undesirable effects during treatment with non-steroidal anti-inflammatory drugs.

Pharmokinetics

Absorption

Maximum concentration (Cmax) of lornoxicam in blood plasma during intramuscular (v/m) injection is reached after about 0.4 hours. Absolute bioavailability (calculated by AUC – area under the curve “concentration-time”) after intramuscular administration is 97%.

Distribution

Lornoxicam is found in plasma unchanged and as a hydroxylated metabolite. The degree of binding of lornoxicam with plasma proteins is about 99% and does not depend on the concentration. Biotransformation Lornoxicam is largely metabolized in the liver, mainly through hydroxylation to inactive 5-hydroxylornoxicam.

Biotransformation of lornoxicam is performed via CYP2C9 isoenzyme. Due to the polymorphism of the gene encoding this enzyme, there are people with slow and fast metabolism of the drug, which can lead to a significant increase in plasma levels of lornoxicam in those with slow metabolism. Hydroxylated metabolite has no pharmacological activity. Lornoxicam is completely metabolized: about 2/3 of the drug is excreted by the liver, and 1/3 – by the kidneys as an inactive metabolite.

Excretion

Half-life (T1/2) of lornoxicam on average is 3 to 4 hours. The drug clearance is decreased by 30-40 % in elderly patients (over 65 years). No significant changes in lornoxicam kinetics are observed in patients with hepatic or renal dysfunction, except for cumulation in patients with chronic liver disease after 7 days of treatment at a daily dose of 12 mg or 16 mg.

Indications

Active ingredient

Composition

How to take, the dosage

When administered orally, 4 mg 2-3 times/day or 8 mg 2 times/day.

The initial dose is 8-16 mg by IV or IM. If the analgesic effect is insufficient, a dose of 8 mg may be reintroduced with another 8 mg.

The maximum daily dose: when given orally, 16 mg; in concomitant gastrointestinal disorders, renal or hepatic disorders, elderly patients (over 65), patients with a body weight less than 50 kg, or after an extensive surgical intervention, 12 mg in 3 doses.

Interaction

Special Instructions

Contraindications

Side effects

Overdose

Similarities