Rofecoxib CAS 162011-90-7 Light yellow crystalline powder Treatment of osteoarthritis
1. Product title:Rofecoxib
2. Product parameter table:
|Appearance||Light yellow crystalline powder||CAS No||162011-90-7|
|Brand Name||Kan Ying||Store-method||Cool Dry Place|
|Shelf Life||2 Years When
3. Product Description:Rofecoxib is used for the treatment of osteoarthritis, rheumatoid arthritis, adult acute pain and primary dysmenorrhea, and acute treatment of migraine attacks with or without aura. Rofecoxib is a solid. This compound belongs to stilbene. These are organic compounds containing 1,2-diphenylethylene moieties. Stilbene (C6-C2-C6) is derived from the common phenylpropene (C6-C3) skeleton structural unit. The introduction of one or more hydroxyl groups into the benzene ring produces stilbenes. Rofecoxib has a half-life of 17 hours, and its average oral bioavailability is approximately 93% at the therapeutic recommended doses of 125, 25, and 50 mg. The proteins targeted by rofecoxib include elastin and prostaglandin G/H synthase2. Cytochrome P450 1A2, cytochrome P450 3A4, cytochrome P450 2C9, cytochrome P450 2C8, known prostaglandin G/H synthase 1 metabolize rofecoxib. On September 30, 2004, Merck voluntarily withdrew rofecoxib from the market because of concerns that long-term, high-dose use would increase the risk of heart attack and stroke.
Rofecoxib is a potent and oral COX-2 specific inhibitor. The IC50 values of human COX-2 in human osteosarcoma cells and Chinese hamster ovary cells are 26 and 18 nM, respectively; Rofecoxib is effective against COX-2 The selectivity is 1000 times that of human COX-1. In U937 cells and Chinese hamster ovary cells, IC50 values are >50 μM and >15 μM, respectively.
6. Adverse reactions:1. The blood system
Can cause aplastic anemia, white blood cells, blood cells, blood cell reduction.
2. Cardiovascular system
Oedema, hypertension, palpitations, and congestive heart failure may occur.
3. Central nervous system
Visible headache, dizziness, dizziness, anxiety, depression, insomnia, worsening epilepsy, etc.
4. Digestive system
(1) This drug can cause nausea, heartburn, diarrhea and other adverse reactions. Compared with non-selective cyclooxygenase inhibitors, it causes less indigestion, gastric acid reflux, upper abdominal discomfort, vomiting, and upper gastrointestinal perforation. , Ulcers or bleeding. Patients with a history of upper gastrointestinal bleeding and those older than 65 have a higher incidence of upper gastrointestinal bleeding, but this has nothing to do with treatment.
(2) Reports of rare oral ulcers.
(3) It has been reported that this drug can cause ALT (alanine aminotransferase) and/or AST (aspartate aminotransferase) values to increase, which can be about 3 times higher than the upper limit of normal, and can The incidence of symptoms that cause liver insufficiency is similar to that of ibuprofen, but significantly lower than that of diclofenac. After continuing treatment, about half of the increase in these test values can be eliminated.
5. Urinary/reproductive system
Renal prostaglandins may play a compensatory role in maintaining renal perfusion. Therefore, administration of this drug in the case of impaired renal perfusion may lead to a decrease in prostaglandin production, resulting in further reduction of renal blood flow and impairing renal function. Patients with obvious renal dysfunction, insufficient cardiac compensation and liver cirrhosis are at greater risk for the above reactions. Consideration should be given to monitoring the renal function of these patients. Stop using this medicine to restore the patient's renal function to the state before treatment.
6. Respiratory system
There are reports of upper respiratory tract infection and bronchitis in foreign countries, and the incidence is greater than that of the placebo group.
7. Musculoskeletal system
There are reports of back pain, weakness and fatigue in foreign countries, and the incidence is greater than that of the placebo group.
7. Precautions:People who are allergic to this medicine and its ingredients should not be used. Patients with advanced kidney disease and severe liver insufficiency are contraindicated. People with high blood pressure, urinary retention, heart failure, gastrointestinal bleeding, smoking and alcohol addiction should be used with caution.