Tìm theo
Meloxicam
Các tên gọi khác (6 ) :
  • Meloxicam
  • Méloxicam
  • Meloxicam
  • Meloxicamum
  • Mobic
  • UNII-vg2qf83cgl
Thuốc giảm đau, hạ sốt, chống viêm không steroid, điều trị Gút và các bệnh xương khớp
Thuốc Gốc
Small Molecule
CAS: 71125-38-7
ATC: M01AC06
ĐG : 4uOrtho LLC , http://www.4udr.com
CTHH: C14H13N3O4S2
PTK: 351.401
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. [Wikipedia]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C14H13N3O4S2
Phân tử khối
351.401
Monoisotopic mass
351.034747299
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)
InChI Key
InChIKey=ZRVUJXDFFKFLMG-UHFFFAOYSA-N
IUPAC Name
4-hydroxy-2-methyl-N-(5-methyl-1,3-thiazol-2-yl)-1,1-dioxo-2H-1$l^{6},2-benzothiazine-3-carboxamide
Traditional IUPAC Name
meloxicam
SMILES
CN1C(C(=O)NC2=NC=C(C)S2)=C(O)C2=C(C=CC=C2)S1(=O)=O
Độ tan chảy
254 dec °C
Độ hòa tan
7.15 mg/L
logP
3.43
logS
-3.4
pKa (strongest acidic)
4.47
pKa (Strongest Basic)
0.47
PSA
99.6 Å2
Refractivity
88.62 m3·mol-1
Polarizability
34.25 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
5
H Bond Donor Count
2
Physiological Charge
-1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
caco2 Permeability
-4.71
pKa
4.08
Dược Lực Học : 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.
Cơ Chế Tác Dụng : 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. [Wikipedia] 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.
Dược Động Học :
▧ 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]
Độc Tính : LD50, Acute: 84 mg/kg (Rat); Oral 470 mg/kg (Mouse); Oral 320 mg/kg (Rabbit)
Chỉ Định : For symptomatic treatment of arthritis and osteoarthritis.
Tương Tác Thuốc :
  • Acenocoumarol Meloxicam may increase the anticoagulant effect of acenocoumarol.
  • Anisindione Meloxicam may increase the anticoagulant effect of anisindione.
  • Azilsartan medoxomil Increases toxicity of each. May deteriorate renal function, particularly in volume depleted or elderly patients. Decreases effects of azilsartan by antagonism.
  • Colesevelam Bile acid sequestrants may decrease the absorption of Nonsteroidal Anti-Inflammatory Agents. Monitor for decreased serum concentrations/therapeutic effects of nonsteroidal anti-inflammatory agents (NSAID) if coadministered with bile acid sequestrants. Separating the administration of doses by 2 or more hours may reduce (but not eliminate) the risk of interaction. The manufacturer of colesevelam recommends that drugs should be administered at least 1 hour before or 4 hours after colesevelam.
  • Dicoumarol Meloxicam may increase the anticoagulant effect of dicumarol.
  • Eltrombopag Increases levels of Meloxicam via metabolism decrease. UDP-glucuronosyltransferase inhibition with unclear significance.
  • Ginkgo biloba Additive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided.
  • Lithium Meloxicam increases serum levels of lithium
  • Pralatrexate NSAIDs increase the risk of toxicity due to impairment of renal clearance of pralatrexate thus increasing exposure. Monitor for adverse effects or adjust dose of pralatrexate.
  • Telmisartan Concomitant use of Telmisartan and Meloxicam may increase the risk of acute renal failure and hyperkalemia. Monitor renal function at the beginning and during treatment.
  • Timolol The NSAID, Meloxicam, may antagonize the antihypertensive effect of Timolol.
  • Trandolapril The NSAID, Meloxicam, may reduce the antihypertensive effect of Trandolapril. Consider alternate therapy or monitor for changes in Trandolapril efficacy if Meloxicam is initiated, discontinued or dose changed.
  • Treprostinil The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Meloxicam. Monitor for increased bleeding during concomitant thearpy.
  • Voriconazole Voriconazole 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.
  • Warfarin The 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.
Liều Lượng & Cách Dùng : Suspension - Oral - 7.5 mg/5 ml
Tablet - Oral - 15 mg
Tablet - Oral - 7.5 mg
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Achefree
    Sản phẩm biệt dược : Achefree
  • Sản phẩm biệt dược : Acticam
  • Công ty : Anchor
    Sản phẩm biệt dược : Aflamid
  • Công ty : Lusa
    Sản phẩm biệt dược : Afloxx
  • Công ty : Zentiva
    Sản phẩm biệt dược : Aglan
  • Công ty : Cheminter
    Sản phẩm biệt dược : Ainecox
  • Công ty : Ivax
    Sản phẩm biệt dược : Aldoron
  • Công ty : Lafrancol
    Sản phẩm biệt dược : Alentum
  • Công ty : Biogen
    Sản phẩm biệt dược : Algiflex
  • Công ty : Centrum
    Sản phẩm biệt dược : Aliviodol
  • Công ty : Caferma
    Sản phẩm biệt dược : Anaxicam
  • Công ty : Medipharm
    Sản phẩm biệt dược : Anposel
  • Công ty : Labormed
    Sản phẩm biệt dược : Antrend
  • Công ty : Pharmatec
    Sản phẩm biệt dược : Aponip
  • Công ty : Gerard
    Sản phẩm biệt dược : Areloger
  • Công ty : Magma
    Sản phẩm biệt dược : Aremil
  • Công ty : Qintar Pharma
    Sản phẩm biệt dược : Armex
  • Sản phẩm biệt dược : Arrox
  • Công ty : Arsmedendi
    Sản phẩm biệt dược : Arsitec
  • Công ty : Pharmedic
    Sản phẩm biệt dược : Artex
  • Công ty : Mekophar
    Sản phẩm biệt dược : Arthrobic
  • Công ty : Pharmanel
    Sản phẩm biệt dược : Arthrox
  • Công ty : Standpharm
    Sản phẩm biệt dược : Articam
  • Công ty : Helix
    Sản phẩm biệt dược : Artipro
  • Công ty : Garmisch
    Sản phẩm biệt dược : Artriclox
  • Công ty : G&R
    Sản phẩm biệt dược : Artrifilm
  • Công ty : Sherfarma
    Sản phẩm biệt dược : Artriflam
  • Công ty : Pro.Med.CS
    Sản phẩm biệt dược : Artrilom
  • Công ty : Combiphar
    Sản phẩm biệt dược : Artrilox
  • Công ty : PharmaBrand
    Sản phẩm biệt dược : Artrox
  • Công ty : Biofarm
    Sản phẩm biệt dược : Aspicam
  • Công ty : Doctor Andreu
    Sản phẩm biệt dược : Atiflam
  • Công ty : Pharmstandard
    Sản phẩm biệt dược : Atrozan
  • Công ty : Aurora
    Sản phẩm biệt dược : Auroxicam
  • Công ty : Hersil
    Sản phẩm biệt dược : Axius
  • Sản phẩm biệt dược : Mobic
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00814
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5281106
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506624
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C08169
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00969
ChemSpider
http://www.chemspider.com/Chemical-Structure.4444553.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50056998
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0378-1066-01
PharmGKB
http://www.pharmgkb.org/drug/PA450353
Wikipedia
http://en.wikipedia.org/wiki/Meloxicam
RxList
http://www.rxlist.com/cgi/generic/mobic.htm
Drugs.com
http://www.drugs.com/cdi/meloxicam.html
... loading
... loading