Clomiphene Citrate / Anastrozole

Available Dosage Strengths

22 mg / 0.25 mg  |  45 mg / 0.25 mg

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Product Overview

Clomiphene (Clomid®) Description1,2,3

Clomiphene was originally marketed under the brand name Clomid®. It is a fertility medication that induces ovulation in infrequently ovulating or anovulatory women. The drug that produces ovulation in patients with an intact hypothalamic-pituitary-ovarian axis and with ovaries that are capable of functioning normally. For women, clomiphene leads to the release of pituitary gonadotropins that initiates steroidogenesis and folliculogenesis, resulting in growth of the ovarian follicle and an increase in the circulating level of estradiol. For men, the drug increases testosterone through increased LH and FSH production who have low testosterone levels.

Anastrozole  Description4

Anastrozole is a selective non-steroidal aromatase inhibitor. Anastrozole is used in postmenopausal women with hormone receptor-positive breast cancer.4

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 Action 4,5,6

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 & Precautions 4,6

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 tablets at controlled room temperature 59-86°F (15-30°C). Protect from heat, light, and excessive humidity, and store in closed containers.

  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

This sheet is a summary. It may not cover all possible drug information about this product. Call your doctor for medical advice and/or about side effects. You may report side effects to the FDA at 1-800-FDA-1088.  A Wells Pharmacy Network pharmacist will be happy to answer any questions. For consultation, please call 1-800-622-4510.

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