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Clomiphene

Hormone Management
ClomidClomifeneSerophene

Overview

Clomiphene, also known as Clomid, Clomifene, or Serophene, is a synthetic non-steroidal compound that belongs to the triphenylethylene group. It is not an endogenous hormone but is used in hormone management, primarily in reproductive medicine. Clomiphene is produced synthetically and is classified as a selective estrogen receptor modulator (SERM). Researchers have extensively studied its role in fertility treatments. Clomiphene's primary physiological role is to induce ovulation in women who are anovulatory or oligo-ovulatory. It has been a subject of research in areas such as polycystic ovary syndrome (PCOS) and male infertility. Researchers have found that clomiphene can also be used to treat certain cases of male hypogonadism. The mechanism of action of clomiphene involves its interaction with estrogen receptors in the hypothalamus. By binding to these receptors, clomiphene inhibits the negative feedback of estrogen on the gonadotropin-releasing hormone (GnRH) secretion, leading to an increase in the release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH), which stimulates ovulation. Clomiphene is primarily administered orally. Researchers have observed that it has a variable half-life, with an average of 5 to 7 days, due to its enterohepatic recirculation and high lipid solubility. It is metabolized in the liver and excreted primarily through feces. Clomiphene is clinically used to treat female infertility due to ovulatory dysfunction. It is approved by regulatory agencies such as the FDA for this purpose. Researchers have found that it is generally well-tolerated, though it may cause side effects such as hot flashes and ovarian hyperstimulation syndrome. Clomiphene is not a controlled substance but requires a prescription for use.

Mechanism of Action

Clomiphene acts on estrogen receptors in the hypothalamus, blocking the negative feedback of estrogen on GnRH secretion. This leads to increased secretion of FSH and LH, promoting ovulation and increasing fertility potential.

Molecular Data

FormulaC26H28ClNO
Molecular Weight406 g/mol
CAS Number911-45-5
PubChem CID2800

Half-Life & Pharmacokinetics

OralHalf-life is approximately 5 to 7 days due to enterohepatic recirculation.

Clomiphene's long half-life is attributed to its high lipid solubility and enterohepatic recirculation.

Storage

Temperature

Store at room temperature (15-30°C)

Light

Protect from light

Form

Stable in tablet form for extended periods

Notes

Keep in a dry place to prevent degradation.

Solubility

Clomiphene is poorly soluble in water but soluble in ethanol and organic solvents.

Legal Status

🇩🇪DE

Clomiphene is a prescription-only medication (verschreibungspflichtig) in Germany.

🇺🇸US

Clomiphene is FDA-approved for the treatment of female infertility and requires a prescription.

🇦🇺AU

In Australia, clomiphene is classified as a Schedule 4 (S4) prescription-only medicine.

🇬🇧UK

Clomiphene is a prescription-only medicine (POM) in the UK, regulated by the MHRA.

Legal status information is provided for general reference only and may not reflect the most current regulatory changes. Always verify with official government sources before making any decisions.

6 Research Publications

Safety and efficacy of enclomiphene and clomiphene for hypogonadal men.

Human

Translational andrology and urology · 2024

Researchers found that enclomiphene, compared to clomiphene, significantly increased testosterone levels in men with low testosterone while also having fewer reported side effects. This suggests that enclomiphene may be a safer and effective treatment option for hypogonadal men. Further studies are needed to confirm these results and understand the long-term effects.

  • Enclomiphene increased testosterone levels by a median of 166.
  • Enclomiphene had a lower rate of adverse effects compared to clomiphene.
  • The study supports enclomiphene as a viable treatment for hypogonadism.
PubMed

[Medical treatments for male infertility].

Review

Progres en urologie : journal de l'Association francaise d'urologie et de la Societe francaise d'urologie · 2023

Researchers observed that certain medical treatments can improve male fertility by stimulating sperm production and reducing oxidative stress. They found that hormonal treatments are beneficial for specific conditions like oligoasthenozoospermia, while antioxidant supplements may enhance sperm quality and increase chances of pregnancy. This review aims to help urologists develop tailored treatment strategies for patients and couples seeking to improve fertility outcomes.

  • Hormonal treatments can stimulate sperm production in men with oligoasthenozoospermia.
  • The effectiveness of treatments for non-obstructive azoospermia depends on hormone levels.
  • Antioxidant supplements may improve sperm quality and increase live birth rates.
PubMed

Comparing efficacy and safety of stair step protocols for clomiphene citrate and letrozole in ovulation induction for women with polycystic ovary syndrome (PCOS): a randomized controlled clinical trial.

Human

Journal of medicine and life · 2023

Researchers observed that letrozole may be more effective than clomiphene citrate for inducing ovulation in women with polycystic ovary syndrome (PCOS), with an ovulation rate of 86% compared to 72%. The pregnancy rate was also slightly higher in the letrozole group at 22%. However, the differences in ovulation rates were not statistically significant.

  • Letrozole had a higher ovulation rate (86%) compared to clomiphene citrate (72%).
  • The pregnancy rate was slightly higher in the letrozole group (22%).
  • Both medications were tested using a stair step protocol over three cycles.
PubMed

Long-Term Safety and Efficacy of Clomiphene Citrate for the Treatment of Hypogonadism.

Human

The Journal of urology · 2019

Researchers found that clomiphene citrate can be a safe and effective long-term treatment for men with low testosterone levels, with 88% achieving normal testosterone levels after more than three years of use. They observed that most patients reported symptom improvements and experienced minimal side effects.

  • 88% of men treated for more than 3 years achieved normal testosterone levels.
  • 77% reported improvements in symptoms.
  • Only 8% experienced side effects, which were generally mild.
PubMed

Gonadotrophins versus clomifene citrate with or without intrauterine insemination in women with normogonadotropic anovulation and clomifene failure (M-OVIN): a randomised, two-by-two factorial trial.

Human

Lancet (London, England) · 2018

Researchers found that women with irregular ovulation who switched from clomifene citrate to gonadotrophins had a higher chance of having a live birth. However, adding intrauterine insemination did not significantly improve the chances of conception compared to regular intercourse.

  • Switching to gonadotrophins increased livebirth rates compared to continuing clomifene citrate.
  • Intrauterine insemination did not lead to more livebirths than intercourse.
  • Multiple pregnancy rates were low and similar across treatment groups.
PubMed

Management strategies for ovulation induction in women with polycystic ovary syndrome and known clomifene citrate resistance.

Review

Current opinion in obstetrics & gynecology · 2009

Researchers observed that clomifene citrate is commonly used to help women with polycystic ovary syndrome (PCOS) ovulate, but some women do not respond to this treatment. For those resistant to clomifene citrate, combining it with metformin or considering surgical options like laparoscopic ovarian drilling may be effective. New drug options, such as aromatase inhibitors, also show promise, but further studies are needed to confirm their effectiveness.

  • 60-85% of women with PCOS respond to clomifene citrate for ovulation induction.
  • Combining clomifene citrate with metformin is a valid strategy for those resistant to clomifene.
  • New treatments like aromatase inhibitors show potential but require more research.
PubMed

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This page is for informational and research purposes only. All information is based on published scientific literature. Nothing on this page constitutes medical advice or replaces consultation with a qualified healthcare professional.