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Mobic
CLINICAL PHARMACOLOGY
Mobic
Mechanism of Action
Meloxicam is a nonsteroidal anti-inflammatory drug (NSAID) that exhibits antiinflammatory, analgesic, and antipyretic activities in animal models. The mechanism of action of meloxicam, like that of other NSAIDs, may be related to prostaglandin synthetase (cyclo-oxygenase) inhibition.
Pharmacokinetics
Absorption
The absolute bioavailability of meloxicam capsules was 89% following a single oral dose of 30 mg compared with 30 mg IV bolus injection. Following single intravenous doses, dose-proportional pharmacokinetics were shown in the range of 5 mg to 60 mg. After multiple oral doses the pharmacokinetics of meloxicam capsules were dose-proportional over the range of 7.5 mg to 15 mg. Mean Cmax was achieved within four to five hours after a 7.5 mg meloxicam tablet was taken under fasted conditions, indicating a prolonged drug absorption. With multiple dosing, steady state concentrations were reached by Day 5. A second meloxicam concentration peak occurs around 12 to 14 hours post-dose suggesting biliary recycling.
Meloxicam oral suspension doses of 7.5 mg/5 mL and 15 mg/10 mL have been found to be bioequivalent to meloxicam 7.5 mg and 15 mg capsules, respectively. Meloxicam capsules have been shown to be bioequivalent to Mobic® (meloxicam) tablets.
Table 1: Single Dose and Steady State Pharmacokinetic Parameters
for Oral 7.5 mg and 15 mg Meloxicam (Mean and % CV)1
| Pharmacokinetic Parameters (%CV) |
Steady State | Single Dose | |||
| Healthy male adults (Fed)2 |
Elderly males (Fed)2 |
Elderly females (Fed)2 |
Renal failure (Fasted) |
Hepatic insufficiency (Fasted) |
|
| 7.5 mg³ tablets | 15 mg capsules | 15mg capsules | 15mg capsules | 15 mg capsules | |
| N | 18 | 5 | 8 | 12 | 12 |
| Cmax[μg/mL] | 1.05 (20) | 2.3 (59) | 3.2(24) | 0.59(36) | 0.84 (29) |
| tmax[h] | 4.9 (8) | 5 (12) | 6(27) | 4(65) | 10 (87) |
| t½[h] | 20.1 (29) | 21 (34) | 24(34) | 18(46) | 16 (29) |
| CL/f[mL/min] | 8.8 (29) | 9.9 (76) | 5.1(22) | 19(43) | 11 (44) |
| Vz/f4[L] | 14.7 (32) | 15 (42) | 10(30) | 26(44) | 14 (29) |
| 1The parameter values in the
Table are from various studies 2not under high fat conditions 3MOBIC tablets 4 Vz/f =Dose/(AUC•Kel) |
|||||
Food and Antacid Effects
Generic Name: Meloxicam
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