Rofecoxib is used for the treatment of osteoarthritis, rheumatoid arthritis, acute pain in adults, and primary dysmenorrhea, as well as acute treatment of migraine attacks with or without auras. Rofecoxib is a solid. This compound belongs to the stilbenes. These are organic compounds containing a 1,2-diphenylethylene moiety. Stilbenes (C6-C2-C6 ) are derived from the common phenylpropene (C6-C3) skeleton building block. The introduction of one or more hydroxyl groups to a phenyl ring lead to stilbenoids. Rofecoxib has a half-life of 17 hours and its mean oral bioavailability at therapeutically recommended doses of 125, 25, and 50 mg is approximately 93%. The proteins that rofecoxib target include elastin and prostaglandin G/H synthase 2. Cytochrome P450 1A2, Cytochrome P450 3A4, Cytochrome P450 2C9, Cytochrome P450 2C8, and Prostaglandin G/H synthase 1 are known to metabolize rofecoxib. On September 30, 2004, Merck voluntarily withdrew rofecoxib from the market because of concerns about increased risk of heart attack and stroke associated with long-term, high-dosage use.
罗非昔布制备储备液:
浓度溶解体积质量
1mg
5mg
10mg
1mM
2.1032mL
10.5159mL
21.0318mL
5mM
0.4206mL
2.1032mL
4.2064mL
10mM
0.2103mL
1.0516mL
2.1032mL
50mM
0.0421mL
0.2103mL
0.4206mL
罗非昔布临床数据( 数据源于:http:// clinicaltrials.gov)
Conversion of different model animals based on BSA(Value based on data from FDA Draft Guidelines)
Animal A (mg/kg)=Animal B(mg/kg)multiplied by AnimalBm系数/AnimalAm系数 For example, to modify the dose of resveratrol uesd for a mouse(22.4mg/kg) to a dose based on the BSA for a rat, multiply 22.4mg/kg by the Km factor for a mouse and zhen divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2mg/kg