Cyclofenil

Medical use

Cyclofenil is used to treat menstrual disturbances and anovulatory infertility caused by insufficiency of the hypothalamic–pituitary–gonadal axis in women. It has also been used to treat menopausal symptoms. The medication is generally used at a dosage of 400 to 600 mg per day.

Available forms

Cyclofenil has been available in the form of 100, 200, and 400 mg oral tablets.

Non-medical use

Cyclofenil has been used by male athletes to increase testosterone levels. It is not effective for this purpose in women.

Contraindications

Cyclofenil is contraindicated during pregnancy and in those with severe liver disease and unexplained uterine bleeding.

Side effects

Cyclofenil is associated with a relatively high incidence of hepatotoxicity. Biochemical signs of undesirable liver changes have been observed in 35% or more of individuals and 1% of individuals experience overt hepatitis.

Pharmacology

Pharmacodynamics

Cyclofenil is a SERM, or a mixed agonist and antagonist of the estrogen receptors (ERs). It is described as a relatively weak/mild SERM. The medication is generally less effective than other SERMs. The medication is an "impeded estrogen" and is thought to work as a progonadotropin by blocking the actions of estrogens in the pituitary gland and hypothalamus, thereby disinhibiting release of the gonadotropins luteinizing hormone and follicle-stimulating hormone. In men, cyclofenil can increase testosterone levels due its progonadotropic effects.

Pharmacokinetics

In terms of distribution, cyclofenil acts both centrally and peripherally. The elimination half-life of cyclofenil after a single 200 mg dose is 18 to 29 hours.

Chemistry

Cyclofenil is a nonsteroidal SERM and is closely related structurally to triphenylethylene SERMs like clomifene and tamoxifen. It has been referred to as a diphenylethylene derivative, differing from triphenylethylenes only by the replacement of one of the phenyl rings with a cyclohexane ring.

History

Cyclofenil was first introduced for medical use in 1970 under the brand name Ondogyne in France. Subsequently, it was introduced throughout the world under a variety of other brand names, including its most well-known brand name Sexovid.

Society and culture

Generic names

Cyclofenil is the English generic name of the drug and its , , and .

Brand names

Cyclofenil has been marketed under a variety of brand names including Ciclifen, Fertodur, Gyneuro, Klofenil, Menoferil, Menopax, Neoclym, Oginex, Ondonid, Ondogyne, Rehibin, Sexadieno, Sexovar, and Sexovid.

Availability

Cyclofenil remains available today only in Brazil, Italy, and Japan. In the past, it has also been available in France, Germany, Mexico, Sweden, Switzerland, Turkey, and the United Kingdom.

Regulation

Cyclofenil is included on the World Anti-Doping Agency list of illegal doping agents in sport.

Research

Cyclofenil was investigated as a possible treatment for scleroderma in the 1980s, but was found to be ineffective. Later study of its efficacy in treating Raynaud's phenomenon in people with scleroderma also found no significant benefit.

References

References

1. (14 November 2014). "The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies". Springer.
2. (January 2000). "Index Nominum 2000: International Drug Directory". Taylor & Francis.
3. "List of 7 Menopausal Disorders Medications Compared". Drugs.com.
4. (6 December 2012). "Drug Dosage in Renal Insufficiency". Springer Science & Business Media.
5. (31 July 1997). "A Handbook of Intrauterine Insemination". Cambridge University Press.
6. (15 October 2003). "Handbook of Drug Interactions: A Clinical and Forensic Guide". Springer Science & Business Media.
7. (1995). "Drug Actions: Basic Principles and Therapeutic Aspects". CRC Press.
8. (6 December 2012). "Drug-Induced Hepatotoxicity". Springer Science & Business Media.
9. (6 December 2012). "Problems in Gynaecology". Springer Science & Business Media.
10. (January 1993). "Infertility: Male and Female". Churchill Livingstone.
11. (1 July 1986). "Ovulation Induction and in Vitro Fertilization". Year Book Medical Publishers.
12. (6 December 2012). "Ovarian Function and its Disorders: Diagnosis and Therapy". Springer Science & Business Media.
13. (22 October 2013). "Physiology". Elsevier Science.
14. William Andrew Publishing. (22 October 2013). "Pharmaceutical Manufacturing Encyclopedia". Elsevier.
15. (2001). "Organic-chemical drugs and their synonyms: (an international survey)". Wiley-VCH.
16. "IBM Watson Health Products".
17. (2009). "Martindale: The Complete Drug Reference". Pharmaceutical Press.
18. (13 November 2014). "Drugs in Sport". Routledge.
19. Ed The Emtree Editorial Team. (1 January 2004). "Doping Search Guide 2004: Over 10,000 Substance Names in Reference to the 2004 WADA (World Anti-Doping Agency) List of Prohibited Substances and Methods". Elsevier.
20. (February 1990). "Treatment of generalized systemic sclerosis". Rheum Dis Clin North Am.
21. (2000). "Cyclofenil for Raynaud's phenomenon in progressive systemic sclerosis". [[Cochrane collaboration.