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Mifepristone
drug data and news
Mifepristone drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Mifepristone | ||
| Brand Names/Synonyms | HSDB 6841; Mifegyne; Mifeprex; Mifepriston; Mifepristona [Spanish]; Mifepristone; Mifepristone [Usan:Ban:Inn]; Mifepristonum [Latin]; RU 486; RU-486; RU-486, MIFEPRISTONE | ||
| Indication | For induced abortion | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Mifepristone is a synthetic steroid with antiprogestational effects indicated for the medical termination of intrauterine pregnancy through 49 days' pregnancy. Doses of 1 mg/kg or greater of mifepristone have been shown to antagonize the endometrial and myometrial effects of progesterone in women. During pregnancy, the compound sensitizes the myometrium to the contraction-inducing activity of prostaglandins. Mifepristone also exhibits antiglucocorticoid and weak antiandrogenic activity. The activity of the glucocorticoid dexamethasone in rats was inhibited following doses of 10 to 25 mg/kg of mifepristone. Doses of 4.5 mg/kg or greater in human beings resulted in a compensatory elevation of adrenocorticotropic hormone (ACTH) and cortisol. | ||
| Mechanism Of Action | The anti-progestational activity of mifepristone results from competitive interaction with progesterone at progesterone-receptor sites. Based on studies with various oral doses in several animal species (mouse, rat, rabbit and monkey), the compound inhibits the activity of endogenous or exogenous progesterone. The termination of pregnancy results. | ||
| Mifepristone News (When available) |
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| Dosage Forms | Tablet | ||
| Drug_Category | Menstruation-Inducing Agents; Luteolytic Agents; Contraceptives, Oral, Synthetic; Contraceptives, Postcoital, Synthetic; Hormone Antagonists; Abortifacient Agents, Steroidal ATC:G03XB01 | ||
| Absorption | The absolute bioavailability of a 20 mg oral dose is 69% | ||
| Interactions |
Interactions for Mifepristone: Although specific drug or food interactions with mifepristone have not been studied, on the basis of this drugís metabolism by CYP 3A4, it is possible that ketoconazole, itraconazole, erythromycin, and grapefruit juice may inhibit its metabolism (increasing serum levels of mifepristone). Furthermore, rifampin, dexamethasone, St. Johnís Wort, and certain anticonvulsants (phenytoin, phenobarbital, carbamazepine) may induce mifepristone metabolism (lowering serum levels of mifepristone). Based on in vitro inhibition information, coadministration of mifepristone may lead to an increase in serum levels of drugs that are CYP 3A4 substrates. Due to the slow elimination of mifepristone from the body, such interaction may be observed for a prolonged period after its administration. Therefore, caution should be exercised when mifepristone is administered with drugs that are CYP 3A4 substrates and have narrow therapeutic range, including some agents used during general anesthesia. | ||
| Toxicity | Nearly all of the women who receive Mifeprex and misoprostol will report adverse reactions, and many can be expected to report more than one such reaction. About 90% of patients report adverse reactions following administration of misoprostol on day three of the treatment procedure. Side effects include more heavy bleeding than a heavy manstrual period, abdominal pain, uterine cramping, nausea, vomiting, diarrhea, | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | 11-(4-dimethylaminophenyl)-17-hydroxy-13-methyl-17-prop-1-ynyl-1,2,6,7,8,11,12,13,14,15,16,17-dodecahydrocyclopenta[a]phenanthren-3-one | ||
| Chemical Formula | C29H35NO2 | ||
| Molecular Weight | 429.594 g/mol | ||
| Smiles String | CC#CC1(CCC2C1(CC(C3=C4CCC(=O)C=C4CCC23)C5=CC=C(C=C5)N(C)C)C)O | ||
| Melting Point | 191-196 °C | ||
| Water Solubility | poorly soluble | ||
| State | Solid | ||
| LogP/Hphobicity | 4.368 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Hepatic | ||
| Half Life | 18 hours | ||
| Protein Binding [%] | 98% (bound to plasma proteins, albumin and a 1-acid glycoprotein) | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Mifepristone.html http://www.rxlist.com/cgi/generic3/mifeprist.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00432 | ||
| CAS Registry Number | 84371-65-3 | ||
| KEGG Compound ID | C07652 | ||
| PubChem ID | SID:65375 | ||
| PharmGKB ID | PA450500 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | Not Available |
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