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Absorption

Lornoxicam is absorbed rapidly and almost completely from the gastrointestinal tract. Maximum plasma concentrations are
achieved after approx. 30 minutes.
The difference between Xefo standard tablets and Xefo Rapid is the fast absorption. A new formulation technique has
been used resulting in release of 90% of the active drug already in the ventricle after only 5 minutes.

Distribution
Lornoxicam is more than 99% bound to plasma proteins, almost exclusively to serum albumin. As lornoxicam is mostly
confined to the volume of distribution of serum albumin, tissue binding of this drug is far less important than its plasma
binding in determining the volume of distribution (Vd).
Vd of lornoxicam after standard tablets or intravenous administration is between 5 and 10 L in humans (0.1 to 0.2 L/kg) and
is consistent with that of the other oxicams.
Lornoxicam is found in the plasma in unchanged form and as its hydroxylated metabolite. The hydroxylated metabolite
exhibits no pharmacological activity.

Metabolism
Lornoxicam is metabolised completely, and is (like e.g. diclofenac and other oxicams) metabolised by cytochrome P450
2C9. Due to genetic polymorphism slow and extensive metabolisers exist for this enzyme, which could result in markedly
increased plasma levels of lornoxicam in slow metabolisers.
The incidence of poor metabolisers of CYP2C9 is very low. The incidence is about 2 % in Caucasians (reports vary from
0.03 to 0.008). The incidence is even lower in Asians.
Three metabolites of [14C]-lornoxicam were identified in young healthy male volunteers. After a 4 mg oral dose of [14C]-
lornoxicam in human volunteers, plasma radioactivity was represented almost entirely by lornoxicam and its 5'-hydroxy
metabolite, with low concentrations of 2 polar metabolites persisting for up to 120 hours post-dose. 1

Laboratory studies incubating lornoxicam with human liver microsomes confirmed that the principal metabolite is 5'-hydroxy-
lornoxicam. The Cmax value of 5'-hydroxy-lornoxicam, is approximately one-tenth that of the parent lornoxicam and occurs
at 3.5 hours post-dose.
When tested in animal models, lornoxicam did not induce liver enzymes. From clinical trial data there is no evidence of
accumulation of lornoxicam after repeated administrations, when given according to recommended dosage. This finding was
supported by drug monitoring data from 1 year studies.

Elimination
Only negligible amounts of intact lornoxicam are excreted unchanged in the urine, with radioactivity being limited to 5'-
hydroxy-lornoxicam and two minor metabolites. Almost all radioactivity was accounted for, with 42% of isotope being
recovered from the urine and 51% from faeces.
Approximately 2/3 is eliminated via the liver and 1/3 via the kidneys as inactive substance.

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