Contra-Indications:
Polycystic ovarian disease Cervical hyperplasia Recentb history of jaundice or hepatic impairment Severe allergic states TB Renal impairment Prgnancy Lactation
Special precautions-
Women who desire to be preegnant should disconitinue taking this drug
Dosages/ Overdosage Etc:
Indications:
Dysfunctional uterine bleeding
Dosage-
120mg twice a week, every Sunday/Wednesday for the first 12 weeks and then 60mg on following Sunday/Wednesday for 12 weeks.
Pharmacology/ Pharmacokinetics:
Pharmacology:
Omeloxifene has a week estrogenic and a potent anti-estrogenic profile. It is expected to exert a contrceptive effect and normalize the bleeding from uterine cavity by regularising the expression of estrogen receptors on the endometrium. Ormiloxifene prevents proliferatin of endometrium and does not affect the cornification of vaginal and cervical epithelium.
Both of these processes are estrogen dependent.
Ormeloxifene comptete with estradiol E2 for binding with cystosol receptors It not only blocks cytol receptors but also causes their prolonged depletion and therefore its action lasts long after the drug has been withdrawn, unlike the other drug in use so far.
Pharmacokinetics:
After a 60mg oral administration, a peak plasma concentration of 125 ng/ml was acheived in 4 hours. The terminal disposition half life of the drug was calculated to be 170 hours.