How Do Estrogen Derivatives Work?

Estrogen derivatives are medications used in the prevention and treatment of menopausal symptoms and various conditions associated with menopause, such as vaginal dryness and bone loss (osteoporosis). Estrogen derivatives are also used in the treatment of breast and prostate cancers.

Estrogens are a group of natural endogenous hormones in women and are present in smaller quantities in men. Estrogens are the primary hormones responsible for the development and maintenance of the female reproductive system and secondary sexual characteristics. Estrogens also play an important role in male sexual function.

Estrogen derivatives supplement the deficiency in natural estrogens which get depleted with menopause in women. Estrogen derivatives relieve menopausal symptoms, prevent bone loss, and reduce the risk of cardiovascular disease in menopausal women.

Endogenous estrogens are of three major types, estradiol, estriol, and estrone. Estrogen derivatives are purified formulations of different types of estrogens derived from natural estrogens from pregnant mares or synthetic estrogen preparations. Estrogen derivatives bind to estrogen receptors in cells and have effects similar to estrogen.

Estrogen derivatives work by reducing elevated levels of reproductive hormones in postmenopausal women, which include gonadotropin-releasing hormone (GnRH) from the hypothalamus, and follicular stimulating hormone (FSH), and luteinizing hormone (LH) from the pituitary gland.

Estrogen derivatives may be combined with another class of medication known as selective estrogen receptor modulator (SERM). SERMs have estrogen-like effects on bone, increasing its density, but have antiestrogenic effects in the breast and uterus, which reduces the risk of endometrial hyperplasia (thickening) that estrogen can cause.

Estrogen derivatives may be administered through various routes including:

Oral tablets:

• Intravenous (IV) injections into the vein
• Intramuscular (IM) injections into the muscle
• Vaginal creams, tablets, inserts, and rings
• Transdermal skin patches
• Topical emulsions or gels applied to the skin
• The uses of estrogen derivatives include:

FDA-approved:

• Menopausal vasomotor symptoms (hot flashes)
• Prevention and treatment of postmenopausal osteoporosis
• Vulvar and vaginal atrophy in menopause
• Atrophic vaginitis and kraurosis vulvae (inflammatory conditions caused by postmenopausal atrophy of vagina and vulva)
• Moderate to severe dyspareunia (painful sexual intercourse due to perimenopausal vaginal dryness)
• Female hypogonadism (inadequate functioning of ovaries and sex hormone deficiency)
• Primary ovarian failure
• Removal of ovaries
• Hypoestrogenism (low estrogen levels)
• Abnormal uterine bleeding
• Breast cancer
• Metastatic inoperable breast cancer in men and women (palliative)
• Advanced androgen-dependent prostate carcinoma (palliative)

Off-label uses:

• Uremic bleeding (bleeding due to high levels of blood urea)

Orphan designation:

• Estrogen replacement in Turner syndrome

Side effects of estrogen derivatives may include the following:

• Headache
• Abdominal pain and cramping
• Back pain
• Arthralgia (joint pain)
• Breast enlargement
• Breast tenderness and pain
• Pharyngitis (throat inflammation)
• Sinusitis (inflammation of the sinuses)
• Oropharyngeal pain (oral and throat pain)
• Increased cough
• Diarrhea
• Dyspepsia (indigestion)
• Nausea
• Vomiting
• Bloating
• Flatulence
• Abdominal distention and discomfort
• Increased incidence of gallbladder disease
• Dry mouth
• Polydipsia (extreme thirst)
• Toothache
• Peripheral edema (swelling)
• Melasma/chloasma (facial skin pigmentation disorder)
• Alopecia (hair loss)
• Hirsutism (inappropriate male-pattern hair growth in women)
• Hypersensitivity reactions include:
  • Pruritus (itching)
  • Rash
  • Urticaria (hives)
  • Swelling
• Skin irritation and redness at the transdermal application site
• Exacerbation of asthma
• Upper respiratory tract infection
• Nasopharyngitis (nose and throat inflammation)
• Pelvic pain
• Neck pain
• Muscle spasms and cramps
• Leg cramps
• Pain in extremities
• Asthenia (weakness)
• Fatigue
• Malaise
• Feeling abnormal
• Dizziness
• Onset or aggravation of migraine
• Syncope (fainting)
• Depression
• Nervousness
• Anxiety
• Mood disturbances
• Irritability
• Insomnia
• Dementia
• Vasodilation
• Vaginitis (inflammation of the vagina)
• Leukorrhea (whitish vaginal discharge)
• Amenorrhea (absence of menstruation)
• Breakthrough bleeding
• Abnormal bleeding or spotting
• Metrorrhagia (vaginal bleeding between periods)
• Dysmenorrhea (painful menstruation)
• Vaginal hemorrhage
• Vaginal candidiasis (Candida yeast infection)
• Vulvovaginal mycotic (fungal) infection
• Vulvovaginal itching
• Ovarian cyst
• Increase in size of uterine leiomyomata (fibroids)
• Change in cervical secretion
• Endometrial hyperplasia
• Endometrial cancer
• Breast secretions
• Fibrocystic breast changes
• Breast cancer
• Gynecomastia (breast tissue growth in males)
• Delayed ejaculation
• Impotence
• Changes in libido
• Cystitis-like syndrome
• Dysuria (painful urination)
• Urinary urgency
• Fluid retention
• Weight changes
• Glucose intolerance
• Increased triglycerides in the blood
• Increased estrogen levels in the blood
• With vaginal rings and inserts:
• Vulvovaginal discomfort, pain, or burning
• Vaginal erosion
• Vaginal ulceration
• Vulvovaginal rash, swelling, and pruritus
• Adhesion of ring to the vaginal wall
• Vaginismus (involuntary tightening of vaginal muscles)
• Corneal curvation change
• Intolerance to contact lenses
• Retinal vascular thrombosis and occlusion
• Chest discomfort
• Hypertension (high blood pressure)
• Palpitations
• Increase in heart rate
• Ventricular extrasystoles (extra heartbeat)
• Deep vein thrombosis (blood clot)
• Pulmonary embolism
• Myocardial infarction (heart attack)
• Stroke
• Tremor
• Drug interactions

Information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with your doctor or pharmacist to make sure these drugs do not cause any harm when you take them along with travel medicines. Never stop taking your medication and never change your dose or frequency without consulting your doctor.

Generic and brand names of estrogen derivative drugs include:

• Alora
• bazedoxifene/conjugated estrogens
• Cenestin DSC
• Climara
• conjugated estrogens
• conjugated estrogens, vaginal
• Delestrogen
• DepoEstradiol
• Divigel
• Duavee
• Elestrin
• Enjuvia DSC
• Estrace
• Estrace Cream
• Estrace Vaginal
• Estraderm Transdermal
• estradiol
• estradiol intravaginal
• estradiol topical
• estradiol vaginal
• Estradot
• Estrasorb
• Estring
• Estrogel
• estrogens conjugated synthetic
• estrogens esterified
• Estrogens, Esterified
• estropipate
• Evamist
• Femring
• Femtrace
• Imvexxy
• Menest
• Menostar
• Minivelle
• Ogen 0.625
• Ogen 1.25
• Ogen 2.5
• Ogen 5
• Ortho Est
• Premarin
• Premarin Vaginal Cream
• Vagifem
• Vivelle
• Vivelle-Dot
• Yuvafem