ormeloxifene

Action and Spectrum

Actions and Spectrum 

• Contraception: Used by women to prevent pregnancy by inhibiting ovulation and altering cervical mucus. 
• Emergency Contraception: Can be used within 72 hours of unprotected intercourse. 
• Management of Abnormal Uterine Bleeding: Helps regulate menstrual cycles and reduce heavy or irregular bleeding. 
• Potential Breast Cancer Prevention: Investigated for its potential to reduce breast cancer risk. 
• Bone Health: May preserve bone density and be considered in postmenopausal women to reduce osteoporosis risk. 
• Endometrial Protection: Offers protection for the uterine lining, especially in women on hormone therapy. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Delayed Menstruation 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindications: 

• Hypersensitivity 
• Pregnancy 
• Breastfeeding 
• Severe Liver Disease 

Cautions: 

• Mild to moderate liver disease 
• Thromboembolic disorders 
• Hypertension 
• Diabetes 
• Ocular disorders 
• Smoking 

Pregnancy / Lactation

Pregnancy consideration:  

The drug is not indicated during lactation.  

Breastfeeding warnings:  

It is unknown whether the drug is excreted in breast milk. 

Pregnancy category: 

Category A: Well-controlled and satisfactory studies show no risk to the fetus in the initial or later trimester. 

<b>Category B: There was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: There was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence, these categories of drugs need to be avoided by pregnant women.    

Category N: No data is available for the drug under this category. 

Pharmacology

Pharmacology:  

ormeloxifene exerts its pharmacological effects by interacting with estrogen receptors in the body. It is considered a SERM because it can act as an agonist and antagonist of estrogen receptors, depending on the tissue type and circumstances. 

ormeloxifene’s contraceptive effect primarily results from its antagonistic action on estrogen receptors in the hypothalamus and pituitary gland. This inhibits the release of gonadotropin-releasing hormone (GnRH) and follicle-stimulating hormone (FSH), which, in turn, suppresses ovulation. 

Pharmacodynamics: 

ormeloxifene’s ability to modulate estrogen receptors leads to changes in hormonal levels in the body, particularly affecting the menstrual cycle and hormone secretion. 

Its estrogenic action in the endometrium can protect against endometrial hyperplasia or cancer, making it useful in hormone replacement therapy. 

Pharmacokinetics: 

Absorption 

ormeloxifene is typically administered orally in the form of tablets. After oral administration, it is absorbed through the gastrointestinal tract and enters the bloodstream. 

Distribution 

Once in the bloodstream, ormeloxifene is distributed throughout the body. It may bind to plasma proteins, influencing its availability for pharmacological action. The drug can also cross the blood-brain barrier and enter various tissues. 

Metabolism 

ormeloxifene undergoes metabolism in the liver. It is primarily metabolized by the cytochrome P450 (CYP) enzyme system, particularly the CYP3A4 enzyme. Metabolism can lead to the formation of metabolites, some of which may contribute to the drug’s pharmacological effects. 

Elimination and Excretion 

Eliminating ormeloxifene and its metabolites occurs primarily through the feces and urine. The drug and its metabolites are excreted from the body over time. 

Adminstartion

Administration: 

• Daily Dosage: ormeloxifene is taken orally as a daily tablet. It is often recommended to take one tablet daily, preferably at the same time each day, for contraception. 
• Start Date: It’s important to begin taking ormeloxifene on the prescribed start date, typically on the first day of the menstrual cycle or as directed by a healthcare provider. This ensures its effectiveness as a contraceptive. 
• Continuous Use: Continue taking the tablet daily without interruption.

Patient Information Leaflet

Patient information leaflet 

Generic Name: ormeloxifene 

Pronounced as: or-me-loks-i-feen 

Why do we use ormeloxifene? 

• Contraception: To prevent pregnancy by inhibiting ovulation and altering cervical mucus. 
• Emergency Contraception: In higher doses within 72 hours of unprotected intercourse. 
• Management of Abnormal Uterine Bleeding: For conditions like heavy or irregular menstrual bleeding. 
• Endometrial Protection: To safeguard the uterine lining, often in hormone replacement therapy. 
• Potential Breast Cancer Prevention: Investigated for reducing breast cancer risk. 
• Bone Health: May help maintain bone density and reduce the risk of osteoporosis.