Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Monoisotopic mass
273.05565634
InChI
InChI=1S/C15H12ClNO2/c1-8(15(18)19)9-2-4-11-12-7-10(16)3-5-13(12)17-14(11)6-9/h2-8,17H,1H3,(H,18,19)
InChI Key
InChIKey=PUXBGTOOZJQSKH-UHFFFAOYSA-N
IUPAC Name
2-(6-chloro-9H-carbazol-2-yl)propanoic acid
Traditional IUPAC Name
carprofen
SMILES
CC(C(O)=O)C1=CC2=C(C=C1)C1=C(N2)C=CC(Cl)=C1
Độ hòa tan
Practically insoluble at 25 °C
pKa (strongest acidic)
4.42
Refractivity
74.16 m3·mol-1
Dược Lực Học :
Carprofen is a non-steroidal anti-inflammatory drug (NSAID) of the propionic acid class that includes ibuprofen, naproxen, and ketoprofen. It is no longer used in the clinical setting, but is approved for use in dogs. Carprofen is non-narcotic and has characteristic analgesic and antipyretic activity approximately equipotent to indomethacin in animal models.
Cơ Chế Tác Dụng :
Carprofen is a non-steroidal anti-inflammatory drug (NSAID) that is used by veterinarians as a supportive treatment for the relief of arthritic symptoms in geriatric dogs. Carprofen was previously used in human medicine for over 10 years (1985-1995). It was generally well tolerated, with the majority of adverse effects being mild, such as gastro-intestinal pain and nausea, similar to those recorded with aspirin and other non-steroidal anti-inflammatory drugs. It is no longer marketed for human usage, after being withdrawn on commercial grounds. [Wikipedia]
The mechanism of action of carprofen, like that of other NSAIDs, is believed to be associated with the inhibition of cyclooxygenase activity. Two unique cyclooxygenases have been described in mammals. The constitutive cyclooxygenase, COX-1, synthesizes prostaglandins necessary for normal gastrointestinal and renal function. The inducible cyclooxygenase, COX-2, generates prostaglandins involved in inflammation. Inhibition of COX-1 is thought to be associated with gastrointestinal and renal toxicity while inhibition of COX-2 provides anti-inflammatory activity. In an in vitro study using canine cell cultures, carprofen demonstrated selective inhibition of COX-2 versus COX-1.
Dược Động Học :
▧ Absorption :
Rapidly and nearly completely absorbed (more than 90% bioavailable) when administered orally.
▧ Protein binding :
High (99%)
▧ Metabolism :
Hepatic.
▧ Half Life :
Approximately 8 hours (range 4.5–9.8 hours) in dogs.
Độc Tính :
Symptoms of NSAID overdose include dizziness and nystagmus. Oral LD50 in mouse and rat is 282 mg/kg and 149 mg/kg, respectively.
Chỉ Định :
For use as a pain reliever in the treatment of joint pain and post-surgical pain.
Liều Lượng & Cách Dùng :
Tablet - Oral
Dữ Kiện Thương Mại
Nhà Sản Xuất
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Sản phẩm biệt dược : lmadyl
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Sản phẩm biệt dược : lmafen
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Sản phẩm biệt dược : Rimadyt