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Meloxicam for humans





Metabolism of Meloxicam in human liver involves cytochromes

7/9/2014
12:35 | Author: Kate Thompson

Morbid
Metabolism of Meloxicam in human liver involves cytochromes

The metabolism of Meloxicam (ME) and the cytochrome(s) P450 (CYPs) involved were analysed by using primary human hepatocytes, human liver microsomes.

2. 3. The metabolism of Meloxicam (ME) and the cytochrome(s) P450 (CYPs) involved were analysed by using primary human hepatocytes, human liver microsomes and microsomes from recombinant human B-lymphoblastoid cell lines. The kinetics of the formation of M7 by human liver microsomes were biphasic with Km = 13.6 +/- 9.5 and 381 +/- 55.2 microM respectively. The involvement of 3A4 was shown by inhibition of ME metabolism by ketoconazole, correlation between ME metabolism and nifedipine oxidase activity and metabolism of ME by recombinant 3A4. The involvement of 2C9 was demonstrated by inhibition of tolbutamide hydroxylase activity in the presence of ME, inhibition of ME metabolism by sulphaphenazole, correlation between ME metabolism and tolbutamide hydroxylase activity and active metabolism of ME by recombinant 2C9. 1. The corresponding Vmax were 33.7 +/- 24.2 and 143 +/- 83.9 pmol/min/mg protein respectively. Kinetics of the formation of M7 by the individual enzymes resulted in a Km = 9.6 microM and Vmax = 8.4 pmol/min/mg protein for 2C9 and a Km = 475 microM and Vmax = 23 pmol/min/mg protein for 3A4. CYP2C9 and, to a much lesser extent, CYP3A4 were found to convert ME to M7. While human hepatocytes were capable of converting ME to a 5-hydroxymethyl metabolite (M7) and then to a 5-carboxyderivative (M5), human liver microsomes formed mostly only the 5-hydroxymethylderivative.

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Pharmacokinetics of meloxicam in animals and the relevance to

5/8/2014
02:30 | Author: Caitlin White

Morbid
Pharmacokinetics of meloxicam in animals and the relevance to

Drug Metab Dispos. 1998 Jun;26(6):576-84. Pharmacokinetics of meloxicam in animals and the relevance to humans. Busch U, Schmid J, Heinzel G, Schmaus.

The pharmacokinetic profile of meloxicam in rats most closely resembles that in humans; therefore, reliable clinical predictions can be made from studies in this rodent species. The percentage of meloxicam binding to protein was higher in rats and humans (>99%) than in other species. The main metabolites in rats, mini-pigs, and humans were a 5'-hydroxymethyl derivative (AF-UH 1 SE) and a 5'-carboxy metabolite (UH-AC 110 SE). The excretion balance in mini-pigs resembled that in humans, with almost equal concentrations being eliminated in the urine and the feces. In contrast, low concentrations of meloxicam were found in the central nervous system, compared with those in plasma. The pharmacokinetic profile of the new nonsteroidal anti-inflammatory drug meloxicam was investigated in a number of animal species, including mice, rats, dogs, mini-pigs, and baboons, after administration of meloxicam. The plasma concentration-time profiles for meloxicam in rats and dogs were comparable to that in humans, whereas there were marked differences between humans and mice, mini-pigs, and baboons. As in humans, meloxicam circulated mainly in the form of the parent compound in the plasma of mice, rats, dogs, mini-pigs, and baboons. The highest tissue concentrations of meloxicam in rats and mini-pigs were seen in the liver and kidneys.

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National Library of Medicine 8600 Rockville Pike, Bethesda MD, 20894 USA. National Center for Biotechnology Information, U.S.

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What Is Meloxicam Used For? - eMedTV.com

3/7/2014
04:45 | Author: Kate Thompson

Meloxicam drug information
What Is Meloxicam Used For? - eMedTV.com

As this eMedTV Web page explains, meloxicam treats several conditions related to pain, inflammation, swelling, or stiffness (for example, osteoarthritis).

Mobic. Ridgefield, CT: Boehringer Ingelheim Pharmaceuticals, Inc.;2012 March.

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Meloxicam -1 - European Medicines Agency

11/16/2014
04:20 | Author: Caitlin White

Morbid
Meloxicam -1 - European Medicines Agency

Primary pharmacological in several species including humans, probably due to inhibition of inducible cyclooxygenase. Water-soluble forms of meloxicam.

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01 Meloxicam (Metacam) - - a VIN company!

9/15/2014
02:35 | Author: Kate Thompson

Morbid
01 Meloxicam (Metacam) - - a VIN company!

(For veterinary information only). Brand name: Metacam, Mobic, Mobicox. Available in 7.5 and 15 mg tablets (human formulations) and two.

Date Published : 11/1/2004 10:46:00 AM Date Reviewed/Revised: 03/05/2011.

The hepatopathy reaction usually occurs in the first 3 weeks after starting carprofen but could theoretically occur later.

The veterinary formulations of meloxicam are oral liquids (either 1.5mg/ml or 0.5 mg/ml). It is important not to use human medications on pets unless your veterinarian has provided detailed dosing instructions. In general, human strength pills will be too strong except in very large dogs. It is important to compare these sizes to the human tabletsthat are available in much higher strengths.

There is currently a newer formulation at one third the strength of the original, which can be dosed more accuray with the included syringe.

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