Meloxicam
MELOXICAM- meloxicam tablet
Dr. Reddy’s Laboratories Limited
ATTENTION DISPENSER: Accompanying Medication Guide must be dispensed with this product.
Prescribing Information
WARNING
Cardiovascular Risk
- NSAIDs may cause an increased risk of serious cardiovascular thrombotic events, myocardial infarction, and stroke, which can be fatal. This risk may increase with duration of use. Patients with cardiovascular disease or risk factors for cardiovascular disease may be at greater risk (see WARNINGS and CLINICAL TRIALS).
- Meloxicam is contraindicated for the treatment of peri-operative pain in the setting of coronary artery bypass graft (CABG) surgery (see WARNINGS).
Gastrointestinal Risk
- NSAIDs cause an increased risk of serious gastrointestinal adverse events including bleeding, ulceration, and perforation of the stomach or intestines, which can be fatal. These events can occur at any time during use and without warning symptoms. Elderly patients are at greater risk for serious gastrointestinal events (see WARNINGS).
DESCRIPTION
Meloxicam, an oxicam derivative, is a member of the enolic acid group of nonsteroidal anti-inflammatory drugs (NSAIDs). Each pale yellow to yellow tablet contains 7.5 mg or 15 mg meloxicam for oral administration. Meloxicam is chemically designated as 4-hydroxy-2-methyl-N -(5-methyl-2-thiazolyl)-2H -1,2-benzothiazine-3-carboxamide-1,1-dioxide. The molecular weight is 351.4. Its empirical formula is C14 H13 N3 O4 S2 and it has the following structural formula.
Meloxicam is a pale yellow to yellow powder, practically insoluble in water, slightly soluble in dimethyl formamide and dimethyl sulphoxide. Meloxicam has an apparent partition coefficient (log P) app = 0.1 in n -octanol/buffer pH 7.4. Meloxicam has pKa values of 1.1 and 4.2.
Meloxicam is available as a tablet for oral administration containing 7.5 mg or 15 mg meloxicam.
The inactive ingredients in meloxicam tablets include colloidal silicon dioxide, crospovidone, lactose monohydrate, magnesium stearate, microcrystalline cellulose, povidone and sodium citrate dihydrate.
CLINICAL PHARMACOLOGY
Mechanism of Action
Meloxicam is a nonsteroidal anti-inflammatory drug (NSAID) that exhibits anti-inflammatory, 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.
| Steady State | Single Dose | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| PharmacokineticParameters(% CV) | Healthymale adults(Fed)† | Elderlymales(Fed)† | Elderlyfemales(Fed)† | Renalfailure(Fasted) | Hepaticinsufficiency(Fasted) | ||||||
| 7.5 mg ‡tablets | 15 mgcapsules | 15 mgcapsules | 15 mgcapsules | 15 mgcapsules | |||||||
| 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) |
| t1/2 | [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 /f § | [L] | 14.7 | (32) | 15 | (42) | 10 | (30) | 26 | (44) | 14 | (29) |
Food and Antacid Effects
Administration of meloxicam capsules following a high fat breakfast (75 g of fat) resulted in mean peak drug levels (i.e., Cmax ) being increased by approximately 22% while the extent of absorption (AUC) was unchanged. The time to maximum concentration (Tmax ) was achieved between 5 and 6 hours. No pharmacokinetic interaction was detected with concomitant administration of antacids. Based on these results, meloxicam can be administered without regard to timing of meals or concomitant administration of antacids.
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