Clomiphene Citrate / Anastrozole

Capsule

22 mg / 0.25 mg  |  45 mg / 0.25 mg

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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.

Anastrozole  Description4

Anastrozole is a selective non-steroidal aromatase inhibitor. It is used in postmenopausal women with hormone receptor-positive breast cancer.

Clomiphene Mechanism of Action1,2,3

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.

Anastrozole Mechanism of Action4,5,6

In postmenopausal women, estrogens are mainly derived from the action of the aromatase enzyme, which converts adrenal androgens (primarily androstenedione and testosterone) to estrone and estradiol. Suppression of estrogen biosynthesis in peripheral tissues and in cancer cells can be achieved by specifically inhibiting the aromatase enzyme. Therapeutically, this inhibition results in decreased systemic estrogen levels and increased systemic testosterone levels, which is therapeutic in estrogen-dependent breast cancers and in disease states where increased testosterone is important.

Clomiphene Adverse Reactions1,2

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

Anastrozole Adverse Reactions4

Common

  • Hot flashes
  • Gastrointestinal (nausea, vomiting, abdominal pain)
  • Headache
  • Weight gain
  • Osteopenia
  • Insomnia

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.

 

Anastrozole Contraindications & Precautions4,6

Contraindications

  • Known hypersensitivity to anastrozole or any component of the formulation.

Precautions:

  • Use with caution in patients with pre-existing hypercholesterolemia.
  • Use with caution in patients with pre-existing osteoporosis; consider bone mineral density (BMD) monitoring in patients treated with anastrozole.
  • Not recommended in patients who are pregnant.
  • Use with caution in patients with pre-existing ischemic cardiac disease.
  • 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. Clinical Pharmacology anastrozole clinical monograph 2025 https://www.clinicalkey.com/pharmacology/
  5. de Ronde W, de Jong FH. Aromatase inhibitors in men: effects and therapeutic options. Reprod Biol Endocrinol. 2011 Jun 21;9:93.
  6. Anastrozole (Ascend Laboratories, LLC): FDA Package Insert. https://medlibrary.org/lib/rx/meds/anstrozole-15/. Anastrozole package insert. Revised 03/11 Accessed May 20, 2025

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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