Centchroman (Ormeloxifene)

Centchroman is a contraceptive agent belonging to the pharmacology class of Selective Estrogen Receptor Modulators.

Centchroman is also known as Ormeloxifene. It is not FDA-approved. It is, however, used in some countries as a non-hormonal oral contraceptive and for the management of dysfunctional uterine bleeding.

Centchroman effectively absorbs from the gastrointestinal tract, achieving peak serum levels within about 4 hours. It widely distributes across tissues, showing minimal affinity to plasma proteins. The drug's elimination process results in an extended terminal half-life of approximately 170 hours.

The common side effects of Centchroman include nausea, headache, and mild gastrointestinal discomfort.

Centchroman is available in tablet form.

The molecule is available in India.

Centchroman is a contraceptive agent belonging to the pharmacology class of Selective Estrogen Receptor Modulators.

Centchroman is available in Tablets.

Tablets: To be swallowed whole with water/liquid. Do not chew, crush or break it.

As the physician recommends, take it twice a week after meals.

• Dysfunctional uterine bleeding (DUB)
• Contraception

Dysfunctional uterine bleeding (DUB): Centchroman regulates menstrual cycles, reduces excessive bleeding, and modulates estrogen activity. It offers family planning benefits with minimal impact on endometrial thickness, making it suitable for women intolerant to or preferring to avoid traditional hormonal interventions for managing DUB.

Contraception: Centchroman, a valuable choice for individuals seeking family planning options with a different profile than traditional hormonal contraceptives, regulates menstrual cycles and minimizes hormonal impact, providing contraception benefits with fewer side effects.

Centchroman is utilized in the following clinical indications:

• Contraception: Used as a non-hormonal oral contraceptive for birth control.
• Management of Dysfunctional Uterine Bleeding (DUB): Helps regulate menstrual cycles, reducing excessive bleeding and providing therapeutic benefits in cases of abnormal uterine bleeding.

Orally: Administer Centchroman orally as tablets, ingesting with water. Coordinate timing with meals to enhance absorption. Adhere to the prescribed dosage and administration schedule diligently. Healthcare providers determine the appropriate dose based on individual factors. Promptly communicate any concerns or adverse reactions to facilitate necessary adjustments to the treatment plan.

Tablets: 30mg, 60mg

Tablets

Dose adjustment in adults

For treating dysfunctional uterine bleeding, Take 60 mg twice weekly for the first 12 weeks and then 60 mg once weekly for the remaining 12 weeks.

For contraception: Take one tablet (30 mg) twice a week for the first twelve weeks, and then one tablet (30 mg) once a week starting on the thirteenth week. On the first day of your menstrual cycle, take the first pill. Follow the dose irrespective of menstrual periods.

While taking the drug, consume a diet abundant in whole grains, fruits, veggies, and low-fat dairy products. Lower the risk of complications by quitting smoking and avoiding alcohol. Incorporate heart-healthy omega-three fatty acid-containing foods into your daily diet. Use low-fat cooking oils like olive, soybean, canola, and coconut oil to reduce elevated blood pressure.

Polycystic ovarian disease, hypertrophy of the cervical cavity, jaundice or hepatic impairment in the recent past, severe allergic reactions, tuberculosis, and renal impairment. Lactation and pregnancy.

Centchroman use may increase cardiovascular risk; evaluate individuals, especially those with heart disease or risk factors.

Assess thromboembolic risk, particularly in those with a history of thromboembolism, as centroman use is associated with such events.

This medicine may cause irregular periods in some women.

Evaluate liver function before and during Centchroman treatment; discontinue if significant increases in liver enzymes are observed.

Regular gynecologic assessments are recommended due to the potential risk of endometrial cancer associated with Centchroman use.

Monitor for visual disturbances, and if blurred vision occurs, discontinue Centchroman, conducting a comprehensive eye examination. Alcohol Warning

There is no sufficient scientific evidence traceable regarding the use and safety of Centchroman in concurrent use with alcohol.

Not recommended during breastfeeding.

Not recommended for use during pregnancy.

Adopt a diet with whole grains, fruits, and veggies; quit smoking.

The adverse reactions related to Centchroman can be categorized as

• Common Adverse Effects: Gastrointestinal discomfort and nausea.
• Less Common Adverse Effects: Headaches and visual disturbances.
• Rare Adverse effects: Severe psychiatric symptoms, thromboembolic events, significant liver enzyme increases, fluid retention, and cardiovascular effects.

Centchroman may interact with antibiotics like tetracycline and amoxicillin, potentially affecting their efficacy. These interactions could impact the overall effectiveness of both Centchroman and the antibiotics. Consult healthcare providers to ensure proper management and to avoid potential complications or reduced therapeutic benefits.

The most common side effects of Centchroman include

Delayed periods

Abdominal pain

Headache

Depression

• Pregnancy and Lactation

Because of the possible significant harmful effects on the unborn child, it is not advised that pregnant women use this medicine. It should be utilised only when life is in danger and the advantages exceed the hazards.

If breastfeeding mothers do not require this medication, they should not take it. It is best to examine the advantages and disadvantages of this medication with your doctor before using it.

• Paediatrics Use

As per the FDA, Centchroman is not recommended for pediatric patients.

Dose Adjustment in Kidney Impairment Patients:

It should be used with caution in those with pre-existing kidney disease. There are no specific dosage adjustments provided.

Dose Adjustment in Hepatic Impairment Patients:

It is probably unsafe to use in patients with liver disease and should be avoided.

Symptoms: Nausea, vomiting, abdominal pain, headaches and visual disturbances

Management: There is no specific antidote. Management of Centchroman overdosage involves supportive care and symptomatic treatment. Management of Centchroman overdosage involves supportive care and symptomatic therapy.

Pharmacodynamics:

With contraceptive properties, ormeloxifene is a selective estrogen receptor modulator (SERM). It is also thought to have potential benefits in the management of endometriosis, uterine fibroids, osteoporosis, dermatitis, restenosis, and breast cancer.

Pharmacokinetics:

Absorption: Centchroman exhibits excellent absorption from the gastrointestinal tract, demonstrating peak serum levels within approximately 4 hours post-administration.

Distribution: The drug showcases extensive distribution across various tissues, penetrating effectively due to its favourable pharmacokinetic profile. Centchroman displays minimal affinity to plasma proteins, contributing to its broad tissue distribution.

Excretion: Centchroman's elimination follows a protracted course, with a terminal half-life of approximately 170 hours. This prolonged half-life underscores the sustained presence of the drug in the body, influencing dosing frequency and overall therapeutic considerations.

• Kamboj VP, Ray S, Anand N. Centchroman: A safe reversible postcoital contraceptive with curative and prophylactic activity in many disorders. Front Biosci (Elite Ed). 2018 Jan 1;10(1):1-14. doi: 10.2741/e807. PMID: 28930603.
• Singh MM. Centchroman, a selective estrogen receptor modulator, as a contraceptive and for the management of hormone-related clinical disorders. Med Res Rev. 2001 Jul;21(4):302-47. doi: 10.1002/med.1011. PMID: 11410933.
• Sarkar A, Wadhawan I, Raj A, Nagabhushana P, Singh P. Improving the Acceptance Rate of Centchroman As a Postpartum Contraceptive Through a Quality Improvement Initiative. Cureus. 2022 Sep 17;14(9):e29277. doi: 10.7759/cureus.29277. PMID: 36277560; PMCID: PMC9580608.
• Misra NC, Nigam PK, Gupta R, Agarwal AK, Kamboj VP. Centchroman--a non-steroidal anti-cancer agent for advanced breast cancer: phase-II study. Int J Cancer. 1989 May 15;43(5):781-3. doi: 10.1002/ijc.2910430506. PMID: 2714882.

• https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4030721/
• https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5367218/
• https://nhm.gov.in/images/pdf/programmes/family-planing/guidelines/
• https://pdf.usaid.gov/pdf_docs/PA00W89Z.pdf