Identification

Name
Meloxicam
Accession Number
DB00814  (APRD00529)
Type
Small Molecule
Groups
Approved, Vet approved
Description

Meloxicam is a nonsteroidal anti-inflammatory drug (NSAID) used to relieve the symptoms of arthritis, primary dysmenorrhea, fever; and as an analgesic, especially where there is an inflammatory component. It is closely related to piroxicam. In Europe it is marketed under the brand names Movalis, Melox, and Recoxa. In North America it is generally marketed under the brand name Mobic. In Latin America, the drug is marketed as Tenaron.

Structure
Thumb
Synonyms
  • Méloxicam
  • Meloxicam
  • Meloxicamum
External IDs
N-1539 / N1539 / UH-AC 62XX / UH-AC-62 XX / UH-AC62
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act MeloxicamTablet15 mgOralTeva2004-08-12Not applicableCanada
Act MeloxicamTablet7.5 mgOralTeva2004-08-12Not applicableCanada
MeloxicamTablet15 mgOralSanis Health Inc2010-07-26Not applicableCanada
MeloxicamTablet7.5 mg/1OralCaraco Pharmaceutical Laboratories, Ltd.2008-11-12Not applicableUs
MeloxicamTablet15 mg/1OralDr Reddy's Laboratories2007-01-01Not applicableUs
MeloxicamTablet7.5 mg/1OralMylan Pharmaceuticals Inc.2007-01-162007-01-16Us
MeloxicamTablet15 mg/1OralRanbaxy Inc.2007-05-23Not applicableUs
MeloxicamTablet7.5 mgOralPro Doc Limitee2009-06-10Not applicableCanada
MeloxicamTablet7.5 mgOralSanis Health Inc2010-07-26Not applicableCanada
MeloxicamTablet15 mg/1OralWatson Laboratories Inc.2007-03-30Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-meloxicamTablet15 mgOralApotex Corporation2004-02-13Not applicableCanada
Apo-meloxicamTablet7.5 mgOralApotex Corporation2004-02-13Not applicableCanada
Auro-meloxicamTablet7.5 mgOralAuro Pharma Inc2012-10-19Not applicableCanada
Auro-meloxicamTablet15 mgOralAuro Pharma Inc2012-10-18Not applicableCanada
Ava-meloxicamTablet15.0 mgOralAvanstra Inc2011-08-112014-08-21Canada
Ava-meloxicamTablet7.5 mgOralAvanstra Inc2011-11-082014-08-21Canada
Comfort Pac with MeloxicamKit15 mg/1Pd Rx Pharmaceuticals, Inc.2010-06-30Not applicableUs
Comfort Pac with MeloxicamKit15 mg/1Pd Rx Pharmaceuticals, Inc.2013-07-092018-07-13Us
Dom-meloxicamTablet15 mgOralDominion Pharmacal2004-02-06Not applicableCanada
Dom-meloxicamTablet7.5 mgOralDominion Pharmacal2004-02-06Not applicableCanada
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
NuDroxiPAK M-15Meloxicam (15 mg/1) + Capsaicin (0.25 mg/1mL) + Menthol (60 mg/1mL) + Methyl salicylate (250 mg/1mL)KitNuCare pharmceuticals,Inc.2007-03-07Not applicableUs
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Trepoxicam-7.5Meloxicam (7.5 mg/1) + Histidine (50 mg/1)KitPhysician Therapeutics Llc2011-01-31Not applicableUs
International/Other Brands
Achefree (Achefree) / Acticam (Acromax Dominicana) / Aflamid (Anchor) / Afloxx (Lusa) / Aglan (Zentiva) / Ainecox (Cheminter) / Aldoron (Ivax) / Alentum (Lafrancol) / Algiflex (Biogen) / Aliviodol (Centrum) / Anaxicam (Caferma) / Anposel (Medipharm) / Antrend (Labormed) / Aponip (Pharmatec) / Areloger (Gerard) / Aremil (Magma) / Armex (Qintar Pharma) / Arrox (Xepa-Soul Pattinson) / Arsitec (Arsmedendi) / Artex (Pharmedic) / Arthrobic (Mekophar) / Arthrox (Pharmanel) / Articam (Standpharm) / Artipro (Helix) / Artriclox (Garmisch) / Artrifilm (G&R) / Artriflam (Sherfarma) / Artrilom (Pro.Med.CS) / Artrilox (Combiphar) / Artrox (PharmaBrand) / Aspicam (Biofarm) / Atiflam (Doctor Andreu) / Atrozan (Pharmstandard) / Auroxicam (Aurora) / Axius (Hersil) / Mobic
Categories
UNII
VG2QF83CGL
CAS number
71125-38-7
Weight
Average: 351.401
Monoisotopic: 351.034747299
Chemical Formula
C14H13N3O4S2
InChI Key
ZRVUJXDFFKFLMG-UHFFFAOYSA-N
InChI
InChI=1S/C14H13N3O4S2/c1-8-7-15-14(22-8)16-13(19)11-12(18)9-5-3-4-6-10(9)23(20,21)17(11)2/h3-7,18H,1-2H3,(H,15,16,19)
IUPAC Name
4-hydroxy-2-methyl-N-(5-methyl-1,3-thiazol-2-yl)-1,1-dioxo-2H-1λ⁶,2-benzothiazine-3-carboxamide
SMILES
CN1C(C(=O)NC2=NC=C(C)S2)=C(O)C2=C(C=CC=C2)S1(=O)=O

Pharmacology

Indication

For symptomatic treatment of arthritis and osteoarthritis.

Associated Conditions
Pharmacodynamics

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.

TargetActionsOrganism
AProstaglandin G/H synthase 2
inhibitor
Human
UProstaglandin G/H synthase 1
inhibitor
Human
Absorption

Absolute bioavailability = 89%

Volume of distribution
  • 10 L
Protein binding

99.4% bound, primarily to albumin

Metabolism

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
Pathways
PathwayCategory
Meloxicam Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe risk or severity of gastrointestinal bleeding can be increased when Meloxicam is combined with (R)-warfarin.
(S)-WarfarinThe risk or severity of gastrointestinal bleeding can be increased when Meloxicam is combined with (S)-Warfarin.
3,5-diiodothyropropionic acidThe metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Meloxicam.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be decreased when combined with Meloxicam.
5-androstenedioneThe metabolism of 5-androstenedione can be decreased when combined with Meloxicam.
6-Deoxyerythronolide BThe metabolism of Meloxicam can be decreased when combined with 6-Deoxyerythronolide B.
6-O-benzylguanineThe metabolism of 6-O-benzylguanine can be decreased when combined with Meloxicam.
AbacavirMeloxicam may decrease the excretion rate of Abacavir which could result in a higher serum level.
AbciximabThe risk or severity of bleeding and hemorrhage can be increased when Meloxicam is combined with Abciximab.
AbemaciclibThe metabolism of Abemaciclib can be decreased when combined with Meloxicam.
Food Interactions
  • Take without regard to meals.

References

Synthesis Reference

Laura Coppi, "Crystalline forms of meloxicam and processes for their preparation and interconversion." U.S. Patent US20030109701, issued June 12, 2003.

US20030109701
General References
Not Available
External Links
Human Metabolome Database
HMDB0014952
KEGG Drug
D00969
KEGG Compound
C08169
PubChem Compound
54677470
PubChem Substance
46506624
ChemSpider
10442740
BindingDB
50056998
ChEBI
6741
ChEMBL
CHEMBL599
Therapeutic Targets Database
DAP000971
PharmGKB
PA450353
HET
MXM
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Meloxicam
ATC Codes
M01AC56 — Meloxicam, combinationsM01AC06 — Meloxicam
AHFS Codes
  • 28:08.04.92 — Other Nonsteroidal Antiimflammatory Agents
PDB Entries
4m11 / 4o1z
FDA label
Download (45.4 KB)
MSDS
Download (35.7 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1Active Not RecruitingNot AvailableSystemic Lupus Erythematosus (SLE)1
1CompletedNot AvailableHealthy Volunteers4
1CompletedTreatmentHealthy Volunteers8
1RecruitingPreventionContraception1
1RecruitingTreatmentHealthy Volunteers1
2CompletedNot AvailableRheumatoid Arthritis1
2CompletedTreatmentDental Pain1
2CompletedTreatmentDysmenorrhea1
2CompletedTreatmentHysterectomy1
2CompletedTreatmentPain NOS1
2CompletedTreatmentPharyngitis1
2CompletedTreatmentPost-Operative Pain1
2RecruitingTreatmentAcute Myeloid Leukemia Arising From Previous Myelodysplastic Syndrome / Chronic Myelogenous Leukemia, BCR-ABL1 Positive / Chronic Myelomonocytic Leukemia / Leukemia Acute Myeloid Leukemia (AML) / Myelodysplastic Syndrome / Myelodysplastic/Myeloproliferative Neoplasms / Secondary Acute Myeloid Leukemia (Secondary AML, sAML)1
2RecruitingTreatmentAnkylosing Spondylitis (AS)1
2RecruitingTreatmentHematopoietic Stem Cells / Lymphoma, Hodgkins / Multiple Myeloma (MM) / Non-Hodgkin's Lymphoma (NHL)1
2RecruitingTreatmentMultiple Myeloma (MM) / Non-Hodgkin's Lymphoma (NHL)1
2Unknown StatusPreventionRupture; Graafian Follicle1
2WithdrawnTreatmentOsteoarthritis (OA)1
2, 3RecruitingTreatmentDysmenorrhea1
3CompletedNot AvailableRheumatoid Arthritis1
3CompletedTreatmentAnkylosing Spondylitis (AS)1
3CompletedTreatmentBack Pain Lower Back1
3CompletedTreatmentLumbar Sciatic Pain1
3CompletedTreatmentOsteoarthritis (OA)2
3CompletedTreatmentPost-Operative Pain3
3CompletedTreatmentPostpartum1
3CompletedTreatmentProstatic Neoplasms1
3CompletedTreatmentRheumatoid Arthritis1
3CompletedTreatmentRheumatoid Arthritis, Juvenile2
3Not Yet RecruitingTreatmentOsteoarthritis (OA)1
3RecruitingTreatmentOpioids Use / Shoulder Pain1
3RecruitingTreatmentPostoperative pain2
3TerminatedTreatmentSurgery, Laparoscopic1
4CompletedPreventionOsteoarthritis (OA) / Rheumatoid Arthritis1
4CompletedTreatmentBiliary Atresia, Kasai Portoenterostomy Status1
4CompletedTreatmentOsteoarthritis (OA)3
4CompletedTreatmentPharyngitis1
4RecruitingTreatmentAnkylosing Spondylitis (AS) / Spondyloarthritis, Axial1
Not AvailableCompletedNot AvailableAcute Gouty Arthritis / Arthritis / Headaches / Migraines / Muscle Spasms / Radicular syndrome / Synovitis / Tendonitis1
Not AvailableCompletedNot AvailableKnee Osteoarthritis (Knee OA)1
Not AvailableCompletedNot AvailableRheumatoid Arthritis4
Not AvailableCompletedTreatmentInflammatory Reaction2
Not AvailableCompletedTreatmentKnee Osteoarthritis (Knee OA)1

Pharmacoeconomics

Manufacturers
  • Boehringer ingelheim pharmaceuticals inc
  • Actavis totowa llc
  • Apotex inc etobicoke site
  • Aurobindo pharma ltd
  • Beijing double crane pharmaceutical co ltd
  • Beijing yabao biopharmaceutical co ltd
  • Breckenridge pharmaceutical inc
  • Caraco pharmaceutical laboratories ltd
  • Carlsbad technology inc
  • Corepharma llc
  • Dr reddys laboratories inc
  • Genpharm inc
  • Glenmark generics ltd
  • Lupin pharmaceuticals inc
  • Mutual pharmaceutical co inc
  • Mylan pharmaceuticals inc
  • Roxane laboratories inc
  • Strides arcolab ltd
  • Taro pharmaceutical industries ltd
  • Teva pharmaceuticals usa
  • Unichem laboratories ltd
  • Watson laboratories inc
  • Zydus pharmaceuticals usa inc
Packagers
  • 4uOrtho LLC
  • Advanced Pharmaceutical Services Inc.
  • Aidarex Pharmacuticals LLC
  • Apotex Inc.
  • Apotheca Inc.
  • A-S Medication Solutions LLC
  • Aurobindo Pharma Ltd.
  • Blenheim Pharmacal
  • Boehringer Ingelheim Ltd.
  • Breckenridge Pharmaceuticals
  • Bryant Ranch Prepack
  • Cadila Healthcare Ltd.
  • Cadista Pharmaceuticals Inc.
  • Caraco Pharmaceutical Labs
  • Carlsbad Technology Inc.
  • Cipla Ltd.
  • Corepharma LLC
  • Dispensing Solutions
  • Diversified Healthcare Services Inc.
  • Doctor Reddys Laboratories Ltd.
  • Dorx LLC
  • Genpharm LP
  • Glenmark Generics Ltd.
  • H.J. Harkins Co. Inc.
  • Innoviant Pharmacy Inc.
  • International Laboratories Inc.
  • Keltman Pharmaceuticals Inc.
  • Lake Erie Medical and Surgical Supply
  • Lannett Co. Inc.
  • Lupin Pharmaceuticals Inc.
  • Mallinckrodt Inc.
  • Medisca Inc.
  • Murfreesboro Pharmaceutical Nursing Supply
  • Mylan
  • Nucare Pharmaceuticals Inc.
  • Palmetto Pharmaceuticals Inc.
  • PD-Rx Pharmaceuticals Inc.
  • Physicians Total Care Inc.
  • Preferred Pharmaceuticals Inc.
  • Prepak Systems Inc.
  • Rebel Distributors Corp.
  • Remedy Repack
  • Resource Optimization and Innovation LLC
  • Roxane Labs
  • Sandoz
  • Southwood Pharmaceuticals
  • St Mary's Medical Park Pharmacy
  • Stat Rx Usa
  • Strides Arcolab Limited
  • Taro Pharmaceuticals USA
  • Teva Pharmaceutical Industries Ltd.
  • UDL Laboratories
  • Unichem Laboratories Ltd.
  • Vangard Labs Inc.
  • Yung Shin Pharmaceutical Industry Ltd.
  • Zydus Pharmaceuticals
Dosage forms
FormRouteStrength
TabletOral15.0 mg
Kit15 mg/1
Tablet7.5 mg/1
TabletOral15 mg/1
TabletOral7.5 mg/1
SuspensionOral7.5 mg/5mL
TabletOral15 mg
TabletOral7.5 mg
Kit
CapsuleOral10 mg/1
CapsuleOral5 mg/1
Prices
Unit descriptionCostUnit
Meloxicam 7.5 mg/5ml Suspension 100ml Bottle86.99USD bottle
Meloxicam bp powder56.61USD g
Mobic 15 mg tablet7.37USD tablet
Meloxicam 15 mg tablet4.94USD tablet
Mobic 7.5 mg tablet4.74USD tablet
Meloxicam 7.5 mg tablet3.23USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6184220Yes1999-09-252019-09-25Us
US9649318No2015-03-312035-03-31Us
US9526734No2013-03-312033-03-31Us
US9808468No2015-03-312035-03-31Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)254 dec °CPhysProp
water solubility7.15 mg/LNot Available
logP3.43AVDEEF,A (1997)
Caco2 permeability-4.71ADME Research, USCD
pKa4.08MERCK INDEX (1996)
Predicted Properties
PropertyValueSource
Water Solubility0.154 mg/mLALOGPS
logP2.28ALOGPS
logP1.6ChemAxon
logS-3.4ALOGPS
pKa (Strongest Acidic)4.47ChemAxon
pKa (Strongest Basic)0.47ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area99.6 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity88.62 m3·mol-1ChemAxon
Polarizability34.25 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9156
Blood Brain Barrier-0.9811
Caco-2 permeable+0.8484
P-glycoprotein substrateSubstrate0.5181
P-glycoprotein inhibitor INon-inhibitor0.7516
P-glycoprotein inhibitor IINon-inhibitor0.7491
Renal organic cation transporterNon-inhibitor0.9275
CYP450 2C9 substrateSubstrate0.5637
CYP450 2D6 substrateNon-substrate0.9117
CYP450 3A4 substrateNon-substrate0.6649
CYP450 1A2 substrateNon-inhibitor0.9271
CYP450 2C9 inhibitorInhibitor0.5511
CYP450 2D6 inhibitorNon-inhibitor0.9322
CYP450 2C19 inhibitorNon-inhibitor0.8948
CYP450 3A4 inhibitorNon-inhibitor0.8191
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7316
Ames testNon AMES toxic0.8576
CarcinogenicityNon-carcinogens0.7052
BiodegradationNot ready biodegradable0.9312
Rat acute toxicity3.4619 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9579
hERG inhibition (predictor II)Non-inhibitor0.7999
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0udi-0009000000-d860614369de32fc5b55
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-00kf-0901000000-0d362af6b48e1604f3c0
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0006-0900000000-f79d2bd45c77067c33bf
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0006-0900000000-385da9c2b565923f3591
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0006-0900000000-24d8592c133da8552647
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0uxr-0905000000-155a653652a8dc132b5c
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0uxu-2905000000-a1d5ee29626527977b8e
MS/MS Spectrum - , positiveLC-MS/MSsplash10-014l-3900000000-835e2ce927e75b3bb1fb
MS/MS Spectrum - , positiveLC-MS/MSsplash10-014l-3910000000-cf38e48efa983293e01f

Taxonomy

Description
This compound belongs to the class of organic compounds known as benzothiazines. These are organic compounds containing a benzene fused to a thiazine ring (a six-membered ring with four carbon atoms, one nitrogen atom and one sulfur atom).
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Benzothiazines
Sub Class
Not Available
Direct Parent
Benzothiazines
Alternative Parents
Alpha amino acids and derivatives / N-arylamides / 2,5-disubstituted thiazoles / Organosulfonamides / Benzenoids / 1,2-thiazines / Vinylogous acids / Heteroaromatic compounds / Secondary carboxylic acid amides / Azacyclic compounds
show 4 more
Substituents
Alpha-amino acid or derivatives / Benzothiazine / N-arylamide / 2,5-disubstituted 1,3-thiazole / Ortho-thiazine / Benzenoid / Organosulfonic acid amide / Azole / Heteroaromatic compound / Vinylogous acid
show 16 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
monocarboxylic acid amide, 1,3-thiazole, benzothiazine (CHEBI:6741)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Prostaglandin-endoperoxide synthase activity
Specific Function
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Constitutively expressed in some tissues in physiological conditions, such as the endothelium, kidney and...
Gene Name
PTGS2
Uniprot ID
P35354
Uniprot Name
Prostaglandin G/H synthase 2
Molecular Weight
68995.625 Da
References
  1. Poulsen Nautrup B, Horstermann D: [Pharmacodynamic and pharmacokinetic aspects of the non-inflammatory non-steroidal agent meloxicam in dogs]. Dtsch Tierarztl Wochenschr. 1999 Mar;106(3):94-100. [PubMed:10220944]
  2. Tegeder I, Lotsch J, Krebs S, Muth-Selbach U, Brune K, Geisslinger G: Comparison of inhibitory effects of meloxicam and diclofenac on human thromboxane biosynthesis after single doses and at steady state. Clin Pharmacol Ther. 1999 May;65(5):533-44. [PubMed:10340919]
  3. Blanco FJ, Guitian R, Moreno J, de Toro FJ, Galdo F: Effect of antiinflammatory drugs on COX-1 and COX-2 activity in human articular chondrocytes. J Rheumatol. 1999 Jun;26(6):1366-73. [PubMed:10381057]
  4. Panara MR, Renda G, Sciulli MG, Santini G, Di Giamberardino M, Rotondo MT, Tacconelli S, Seta F, Patrono C, Patrignani P: Dose-dependent inhibition of platelet cyclooxygenase-1 and monocyte cyclooxygenase-2 by meloxicam in healthy subjects. J Pharmacol Exp Ther. 1999 Jul;290(1):276-80. [PubMed:10381787]
  5. Gross JM, Dwyer JE, Knox FG: Natriuretic response to increased pressure is preserved with COX-2 inhibitors. Hypertension. 1999 Nov;34(5):1163-7. [PubMed:10567199]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Prostaglandin-endoperoxide synthase activity
Specific Function
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Involved in the constitutive production of prostanoids in particular in the stomach and platelets. In gas...
Gene Name
PTGS1
Uniprot ID
P23219
Uniprot Name
Prostaglandin G/H synthase 1
Molecular Weight
68685.82 Da
References
  1. Blanco FJ, Guitian R, Moreno J, de Toro FJ, Galdo F: Effect of antiinflammatory drugs on COX-1 and COX-2 activity in human articular chondrocytes. J Rheumatol. 1999 Jun;26(6):1366-73. [PubMed:10381057]
  2. Panara MR, Renda G, Sciulli MG, Santini G, Di Giamberardino M, Rotondo MT, Tacconelli S, Seta F, Patrono C, Patrignani P: Dose-dependent inhibition of platelet cyclooxygenase-1 and monocyte cyclooxygenase-2 by meloxicam in healthy subjects. J Pharmacol Exp Ther. 1999 Jul;290(1):276-80. [PubMed:10381787]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Chesne C, Guyomard C, Guillouzo A, Schmid J, Ludwig E, Sauter T: Metabolism of Meloxicam in human liver involves cytochromes P4502C9 and 3A4. Xenobiotica. 1998 Jan;28(1):1-13. [PubMed:9493314]
  2. Ludwig E, Schmid J, Beschke K, Ebner T: Activation of human cytochrome P-450 3A4-catalyzed meloxicam 5'-methylhydroxylation by quinidine and hydroquinidine in vitro. J Pharmacol Exp Ther. 1999 Jul;290(1):1-8. [PubMed:10381752]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
  4. Meloxicam FDA label [File]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Chesne C, Guyomard C, Guillouzo A, Schmid J, Ludwig E, Sauter T: Metabolism of Meloxicam in human liver involves cytochromes P4502C9 and 3A4. Xenobiotica. 1998 Jan;28(1):1-13. [PubMed:9493314]
  2. Ludwig E, Schmid J, Beschke K, Ebner T: Activation of human cytochrome P-450 3A4-catalyzed meloxicam 5'-methylhydroxylation by quinidine and hydroquinidine in vitro. J Pharmacol Exp Ther. 1999 Jul;290(1):1-8. [PubMed:10381752]
  3. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Phosphogluconate dehydrogenase (decarboxylating) activity
Specific Function
Catalyzes the oxidative decarboxylation of 6-phosphogluconate to ribulose 5-phosphate and CO(2), with concomitant reduction of NADP to NADPH.
Gene Name
PGD
Uniprot ID
P52209
Uniprot Name
6-phosphogluconate dehydrogenase, decarboxylating
Molecular Weight
53139.56 Da
References
  1. Akkemik E, Budak H, Ciftci M: Effects of some drugs on human erythrocyte 6-phosphogluconate dehydrogenase: an in vitro study. J Enzyme Inhib Med Chem. 2010 Aug;25(4):476-9. doi: 10.3109/14756360903257900. [PubMed:20235752]
  2. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. Agundez JA, Garcia-Martin E, Martinez C: Genetically based impairment in CYP2C8- and CYP2C9-dependent NSAID metabolism as a risk factor for gastrointestinal bleeding: is a combination of pharmacogenomics and metabolomics required to improve personalized medicine? Expert Opin Drug Metab Toxicol. 2009 Jun;5(6):607-20. doi: 10.1517/17425250902970998 . [PubMed:19422321]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Atpase activity, coupled to transmembrane movement of substances
Specific Function
May be an organic anion pump relevant to cellular detoxification.
Gene Name
ABCC4
Uniprot ID
O15439
Uniprot Name
Multidrug resistance-associated protein 4
Molecular Weight
149525.33 Da
References
  1. Uchida Y, Kamiie J, Ohtsuki S, Terasaki T: Multichannel liquid chromatography-tandem mass spectrometry cocktail method for comprehensive substrate characterization of multidrug resistance-associated protein 4 transporter. Pharm Res. 2007 Dec;24(12):2281-96. Epub 2007 Oct 16. [PubMed:17939016]

Drug created on June 13, 2005 07:24 / Updated on November 12, 2018 07:22