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Clinician’s Corner: SERMs

As we move through the month of October, we are discussing women’s health issues.  The first three units we discussed breast cancer. Last week we discussed raloxifene and tamoxifen, which are SERMS (selective estrogen receptor modifiers).  Estrogen receptors are present throughout the body. SERMs can block or stimulate various estrogen tissue receptors, including breast, bone, endometrium, hypothalamus and coagulation system.  We will discuss in detail the three other SERMS, not associated with breast cancer prevention.

  • Nolvadex® (tamoxifen): (BREAST CANCER PREVENTION) is considered first line therapy of estrogen receptor positive breast cancer. Both for pre-menopausal and post-menopausal (No effect on vaginal tissue)
  • Evista® (raloxifene): (BREAST CANCER PREVENTION/OSTEOPOROSIS) is for reduction in risk of invasive breast cancer in postmenopausal women with osteoporosis OR if at high risk for invasive breast cancer. (No effect on vaginal tissue)

Osphena (ospemifene) (DYSPARUNIA) 60mg tablets

Dose: take (1) tablet daily

Mechanism: estrogen agonist on vaginal tissue. Minimal effect in uterine tissue and serves as an estrogen antagonist in breast tissue. Ospemifene may have a positive effect on bone tissue. Up to 45% of postmenopausal women can experience vulvovaginal atrophy due to estrogen loss.

Indications: approved by the FDA to treat moderate to severe painful intercourse, due to estrogen deficiency of menopause.

Watch for: May make hot flashes worse.  Watch for drug interactions.

NOTES: expect about 45% of postmenopausal women to experience vulvovaginal atrophy (VVA) due to declining estrogen levels. Symptoms of VVA may include dryness, itching, irritation, and painful intercourse.

Diagnosis of VVA is based on symptoms as well as various laboratory findings. Vaginal lubrication decreases and vaginal pH increases. One of the best indicators of VVA is a pH of 5 or higher. Changes can also be seen on a cellular level

USE: being promoted for its estrogenic effect on vaginal symptoms.

Duavee®:  (conjugated estrogens/ bazedoxifene)  (MENOPAUSAL SYMPTOMS)

Use: moderate to severe hot flashes and preventing osteoporosis.

Estrogen is used for menopausal symptoms & osteoporosis.

Bazedoxifene (SERM) is added to inhibit estrogen’s effects on the uterus.  Blocking estrogen in the uterus decreases the chances of cancer.

BEST USE:   women who want to use estrogen for menopausal symptoms but need an alternative to a progestin.

Clomiphene (Clomid):  (FERTILITY) is a nonsteroidal estrogen receptor modulator (SERM).  It works in the brain to cause an increase in release of FSH (follicle stimulating hormone) and LH (luteinizing hormone). This promotes growth and maturation of a woman’s eggs.  It increases the chances of conception.

Dosage: 50mg daily beginning day 5 of the cycle.