www.ijbcp.com International Journal of Basic & Clinical Pharmacology | August 2018 | Vol 7 | Issue 8 Page 1437 IJBCP International Journal of Basic & Clinical Pharmacology Print ISSN: 2319-2003 | Online ISSN: 2279-0780 Review Article Clomiphene citrate: the changing landscape Mahesh C. Gupta, Jyoti Khanna* INTRODUCTION Ovulatory dysfunction is one of the leading causes of female infertility. Among all the drugs currently available, clomiphene citrate (CC) remains the most commonly prescribed ovulation-inducing medication and is probably the most appropriate initial choice in the majority of anovulatory infertile women. 1 Clomiphene citrate has emerged as a boon in the induction of ovulation in the human female. This wonder drug, however, was discovered as an antifertility and antiovulatory drug in laboratory animals. The adverse effects observed in the clinical use of this compound have not yet been studied well. One of the worst side effects of this compound is abortion associated with its use in clinical practice. Considerable knowledge gaps still exist regarding the mode of action of this compound and the effects of this compound in the female reproduction. This aspect is further complicated by the fact that clomiphene citrate is a non-racemic mixture of two isomers, zuclomiphene and enclomiphene, having individual and opposite biological actions. 2 This article highlights the brief historical perspective, describes the pharmacology with respect to its isomers, their mode of action, and indications for use and a discussion on the risks and side effects of CC treatment. ABSTRACT Ovulatory dysfunction is one of the leading causes of female infertility. Clomiphene citrate has emerged as a boon in the induction of ovulation in the human female. Clomiphene results in many adverse effects some of which are documented, and some reported spontaneously. Clomiphene citrate is a non- racemic mixture of two isomers, zuclomiphene and enclomiphene, having individual and opposite biological actions. It is accepted that cis isomer (zuclomiphene) is estrogenic and trans isomer (enclomiphene) is anti-estrogenic. Zuclomiphene does not have any ovulation-induction property but gets accumulated for a longer time in the human body and it has more agonistic activity than enclomiphene. Thus, Zuclomiphene may be responsible for the adverse effects by clomiphene citrate. Enclomiphene is being explored for its potential use in male as well as female infertility. Trails are underway to explore its effectiveness and safety in various disorders. This article highlights the pharmacology of Clomiphene with respect to its isomers and the potential uses of enclomiphene based on evidences available. Keywords: Clomiphene, Enclomiphene, Infertility, Zuclomiphene DOI: http://dx.doi.org/10.18203/2319-2003.ijbcp20183011 Department of Pharmacology, Pandit Bhagwat Dayal Sharma, Post Graduate Institute of Medical Sciences (PGIMS), Rohtak, Haryana, India Received: 29 May 2018 Accepted: 26 June 2018 *Correspondence to: Dr. Jyoti Khanna, Email: jk.jyotikhanna1@ gmail.com Copyright: © the author(s), publisher and licensee Medip Academy. This is an open- access article distributed under the terms of the Creative Commons Attribution Non- Commercial License, which permits unrestricted non- commercial use, distribution, and reproduction in any medium, provided the original work is properly cited.