Lornoxicam
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Lornoxicam
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| Systematic (IUPAC) name | |
| (3E)-6-chloro-3-[hydroxy-(pyridin-2-ylamino)methylidene]-2-methyl-1,1-dioxothieno[2,3-e]thiazin-4-one | |
| Identifiers | |
| CAS number | ? |
| ATC code | M01 |
| PubChem | |
| Chemical data | |
| Formula | C13H10ClN3O4S2 |
| Mol. mass | 371.8192 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | ? |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
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| Legal status | |
| Routes | ? |
Lornoxicam is a non-steroidal anti-inflammatory drug.
What is it used for:
- Inflammatory disease of the joints
- Osteoarthritis
- Pain following surgery
- Pain in the lower back and hip which travels down the back of the thigh into the leg (sciatica)
METABOLISM: CYP2C9 has been shown to be the primary enzyme responsible for the biotransformation of the lornoxicam to its major metabolite, 5’-hydroxylornoxicam. Recently, it was reported that lornoxicam 5’-hydroxylation by the variant CYP2C9.3 and CYP2C9.13 was markedly reduced compared with wild type, both in vitro and in vivo. We suggest lornoxicam as a good Probe for CYP2C9 activity, both In Vitro and In Vivo.
Three of the most commonly employed substrate probes for determining CYP2C9 activity in crude human tissue fractions are (S)-warfarin (7-hydroxylation), tolbutamide (methylhydroxylation), and diclofenac (4_-hydroxylation). And the best in vivo probes for CYP2C9 activity are tolbutamide and flurbiprofen. Turnover of (S)-warfarin and tolbutamide by CYP2C9 is extremely slow. Conversely, diclofenac has the advantage that CYP2C9 catalyzes its metabolism with a high turnover number, but is not a useful in vivo probe for the CYP2C9 enzyme.
We suggest lornoxicam as a good Probe for CYP2C9, both In Vitro and In Vivo. First, turnover of lornoxicam by CYP2C9 is much faster than (S)-warfarin and tolbutamide. So it is beneficial in allowing for facile, economical HPLC-UV assays to be employed for routine screening in vitro. Second, the lornoxicam poor metabolizer we found who is heterozygous for the CYP2C9*13 together with the CYP2C9*3, i.e. with the invalidated CYP2C9, has the lornoxicam half-life of about 105 h, indicating the specific biotransformation of the NSAID by CYP2C9.
Mode of action: Lornoxicam readily penetrates into synovial fluid. Lornoxicam synovial fluid: plasma AUC ratio is 0.5 after administration of 4mg twice daily.
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