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QuickView for meloxicam (compound)


PubChem
Name: meloxicam
PubChem Compound ID: 4052
Molecular formula: C14H13N3O4S2
Molecular weight: 351.403 g/mol
DrugBank
Identification
Name: meloxicam
Name (isomeric): DB00814
Drug Type: small molecule
Synonyms:
Meloxicamum [latin]
Brand: PHL-meloxicam, Metacam, Ratio-meloxicam, Gen-meloxicam, Mobic, Apo-meloxicam, Novo-meloxicam, Co Meloxicam, Movatec, PMS-meloxicam, Parocin, Tenaron, Dom-meloxicam, Movalis, Mobicox
Category: Antineoplastic Agents, Cyclooxygenase Inhibitors, Antiemetics, Growth Inhibitors, Analgesics, Nonsteroidal Anti-inflammatory Agents (NSAIAs)
CAS number: 71125-38-7
Pharmacology
Indication: For symptomatic treatment of arthritis and osteoarthritis.
Pharmacology: Meloxicam is an nonsteroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic properties. Prostaglandins are substances that contribute to inflammation of joints. Meloxicam inhibits prostaglandin synthetase (cylooxygenase 1 and 2) and leads to a decrease of the synthesis of prostaglandins, therefore, inflammation is reduced.
Mechanism of Action: Anti-inflammatory effects of meloxicam are believed to be due to inhibition of prostaglandin synthetase (cylooxygenase), leading to the inhibition of prostaglandin synthesis. As prostaglandins sensitize pain receptors, inhibition of their synthesis may be associated with the analgesic and antipyretic effects of meloxicam.
Absorption: Absolute bioavailability = 89%
Protein binding: 99.4% bound, primarily to albumin
Biotransformation: Meloxicam is almost completely metabolized into inactive metabolites by the cytochrome P450 (CYP450) isozymes. CYP2C9 is primarily responsible for metabolism of meloxicam while CYP3A4 plays a minor role. An intermediate metabolite, 5'-hydroxymethyl meloxicam, is further metabolized to 5'-carboxy meloxicam, the major metabolite. Peroxidase activity is thought to produce the two other inactive metabolites of meloxicam.
Route of elimination: Meloxicam is almost completely metabolized to four pharmacologically inactive metabolites. Meloxicam excretion is predominantly in the form of metabolites, and occurs to equal extents in the urine and feces. Only traces of the unchanged parent compound are excreted in the urine (0.2%) and feces (1.6%). The extent of the urinary excretion was confirmed for unlabeled multiple 7.5 mg doses: 0.5%, 6% and 13% of the dose were found in urine in the form of meloxicam, and the 5'-hydroxymethyl and 5'-carboxy metabolites, respectively.
Half Life: 15-20 hours
Clearance: 8.8 mL/min [Healthy Male Adults (Fed) oral 7.5 mg tablets] 9.9 mL/min [Eldery Male (Fed) oral 15 mg capsules] 5.1 mL/min [Eldery Female (Fed) oral 15 mg capsules] 19 mL/min [Renal Failure (Fasted) oral 15 mg capsules] 11 mL/min [Hepatic Insufficiency (Fasted) oral 15 mg capsules]
Toxicity: LD50, Acute: 84 mg/kg (Rat); Oral 470 mg/kg (Mouse); Oral 320 mg/kg (Rabbit)
Affected organisms: Humans and other mammals
Interactions
Food interaction:
Take without regard to meals.
Drug interaction:
WarfarinThe antiplatelet effects of meloxicam may increase the bleed risk associated with warfarin. Consider alternate therapy or monitor for signs and symptoms of bleeding during concomitant therapy.
DicumarolMeloxicam may increase the anticoagulant effect of dicumarol.
AnisindioneMeloxicam may increase the anticoagulant effect of anisindione.
LithiumMeloxicam increases serum levels of lithium
VoriconazoleVoriconazole may increase the serum concentration of meloxicam by decreasing its metabolism via CYP2C9 and CYP3A4. Monitor for changes in the therapeutic and adverse effects of meloxicam if voriconazole is initiated, discontinued or dose changed.
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