Clomiphene Citrate / Pregnenolone

Capsule

45 mg / 20 mg

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Disclaimer: Images are for reference only; actual products may vary.

Product Overview

Clomiphene (Clomid™) Description1,2,3

Clomiphene, originally marketed as Clomid™, is a fertility medication used to induce ovulation in women who ovulate infrequently or not at all. It stimulates ovulation in patients with an intact hypothalamic-pituitary-ovarian axis and normally functioning ovaries. In women, clomiphene promotes the release of pituitary gonadotropins, initiating steroidogenesis and folliculogenesis, which leads to ovarian follicle development and increased circulating estradiol levels. In men with low testosterone, the drug can increase testosterone levels through stimulation of LH and FSH production.

Pregnenolone Description4-6
Pregnenolone is a naturally occurring endogenous steroid and a precursor in the biosynthesis of various other steroids, including progesterone, mineralocorticoids, glucocorticoids, androgens, and estrogens. It is primarily synthesized in the adrenal glands, with smaller amounts produced in the liver, gonads, brain, and skin.

Pregnenolone is a compounded preparation designed for systemic absorption through the skin, typically formulated in a lipophilic cream or gel base or taken by mouth in capsule form. It is used for supporting cognitive function, managing adrenal fatigue, improving mood, and alleviating symptoms associated with hormonal imbalances, such as those in perimenopause and andropause.

Clomiphene Mechanism of Action1-3

Clomiphene is classified as a selective-estrogen receptor-modulator due to its ability to compete with estradiol for estrogen receptors at the level of the hypothalamus. The drug blocks the normal negative feedback of circulating estradiol on the hypothalamus, preventing estrogen from lowering the output of gonadotropin releasing hormone. Gonadotropin releasing hormone pulses increases during clomiphene therapy and stimulates the pituitary gland to release more FSH and LH. For women, FSH and LH stimulate the ovaries to develop oocyte follicles. For men, it stimulates the production of testosterone.

Pregnenolone Mechanism of Action4-6

Pregnenolone functions as a neurosteroid and hormonal precursor. After absorption, it enters systemic circulation and is converted into downstream hormones depending on enzymatic activity in target tissues.

Neurosteroid effects: It modulates GABA-A receptors indirectly and can enhance cognitive performance and reduce anxiety in some settings.
Endocrine pathway: Pregnenolone is the parent molecule in the steroidogenic pathway. It undergoes enzymatic conversion to:
– Progesterone via 3β-HSD
– DHEA via 17α-hydroxylation followed by cleavage
– And further into testosterone, estradiol, cortisol, and aldosterone depending on tissue-specific enzymes

Clomiphene Adverse Reactions1,2

  • Hot flashes
  • Abdominal or pelvic discomfort
  • Breast tenderness
  • Nausea, vomiting
  • Mood swings, headaches

Pregnenolone Adverse Effects4-6
Common

  • Insomnia or altered sleep patterns
  • Irritability or mood changes
  • Acne or oily skin
  • Headaches
  • Breast tenderness or gynecomastia (in rare cases)

Less common but possible

  • Hirsutism
  • Libido changes (increased or decreased)
  • Menstrual irregularities in women
  • Fatigue

Clomiphene Contraindications & Precautions1,2

Contraindications

  • Contraindicated during pregnancy
  • Liver disease or history of hepatic dysfunction
  • Abnormal uterine bleeding of unknown cause
  • Ovarian cysts unrelated to polycystic ovary syndrome
  • Uncontrolled thyroid or adrenal dysfunction
  • Pituitary or hypothalamic tumors

Precautions

  • Visual symptoms (blurring, scotomas) may occur; discontinue if persistent
  • Increased risk of multiple births (twins, triplets)
  • Spontaneous abortion and congenital anomalies

Pregnenolone Contraindications / Precautions4-6
Contraindications

  • Known hypersensitivity to pregnenolone or cream base ingredients
  • Hormone-sensitive conditions (e.g., breast cancer, prostate cancer, endometriosis, uterine fibroids) unless under medical supervision
  • Pregnancy and lactation (safety not established)

Precautions

  • Individuals with hormone-sensitive cancers should use with caution
  • May interact with hormone replacement therapy or affect levels of other steroids
  • Use caution in pediatric or geriatric populations due to lack of safety data
  • Not recommended in active seizure disorders without medical oversight (due to neurosteroid effects)
  • Store at controlled room temperature (20°C to 25°C / 68°F to 77°F)
  • Protect from moisture and light
  • Keep in a tightly closed container
  1. Clomiphene citrate package insert Clomid Revised October 2012 Accessed June 2, 2025. https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/016131s026lbl.pdf
  2. Clinical Pharmacology clomiphene clinical monograph 2025 https://www.clinicalkey.com/pharmacology/
  3. Karen M. Wheeler, Devang Sharma, Parviz K. Kavoussi, Ryan P. Smith, Raymond Costabile, Clomiphene Citrate for the Treatment of Hypogonadism, Sexual Medicine Reviews, Volume 7, Issue 2, April 2019, Pages 272–276.
  4. Pregnenolone – Patient Handout; NatMed Pro; 2025; https://naturalmedicines-therapeuticresearch-com.lp.hscl.ufl.edu/databases/food,-herbs-supplements/patienthandout.aspx?productid=98&lang=en
  5. Pregnenolone – Professional Monograph; NatMed Pro; 2025; https://naturalmedicines-therapeuticresearch-com.lp.hscl.ufl.edu/databases/food,-herbs-supplements/professional.aspx?productid=98
  6. Pregnenolone – Drugbank ; 2025; https://go.drugbank.com/drugs/DB02789

WPPL operates as a 503A compounding pharmacy and prepares individualized prescription medications pursuant to provider direction. Compounded preparations are not reviewed, tested, or approved by the FDA.

This listing also includes commercially manufactured products for convenience; these items are not compounded by our pharmacy and are sold as provided by their manufacturers. Actual products in stock at time of dispensing may vary due to supply chain variability. Any statements regarding non-compounded products are manufacturer-supplied, have not been evaluated by the FDA, and are not intended to diagnose, treat, cure, or prevent any disease. WPPL does not verify or endorse any therapeutic claims made by manufacturers. Please refer to original labeling for complete product information.

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