Action and Spectrum

Actions and Spectrum: 

The actions of conjugated estrogens are like those of endogenous estrogens, which include: 

• Promoting the development and maintenance of female reproductive structures, such as the uterus, vagina, and fallopian tubes. 
• Maintaining bone density and reducing the risk of osteoporosis. 
• Regulating cholesterol levels in the blood. 
• Maintaining the health of the skin and mucous membranes. 
• Regulating the menstrual cycle. 
• Reducing the frequency and severity of hot flashes and other symptoms of menopause. 

The spectrum of activity of conjugated estrogens depends on the dose and route of administration. At lower doses, they are used for hormone replacement therapy (HRT) to relieve symptoms of menopause and prevent osteoporosis. At higher doses, they may be used to treat certain types of breast and prostate cancers, and to suppress ovulation in women with certain medical conditions. However, the use of conjugated estrogens at high doses is associated with an increased risk of breast cancer, blood clots, and other serious side effects. Therefore, their use should be carefully considered and monitored by a healthcare provider. 

Drug Interaction

Adverse Reaction

Frequency Defined 

>10% 

Abdominal pain  

Breast enlargement 

Breast tenderness  

Back pain  

Pharyngitis  

Sinusitis  

Diarrhea  

Headache  

rthralgia  

1-10% 

Depression  

Flatulence  

Vaginitis 

Dizziness  

Nervousness  

Increased cough  

Pruritus  

Leukorrhea  

Leg cramps  

Frequency not Defined 

Amenorrhea 

Melasma 

Breakthrough bleeding 

Corneal curvation change 

Weight changes 

Vaginal moniliasis 

Spotting 

Black Box Warning

Black Box Warning: 

Estrogens increase the risk of breast cancer, endometrial cancer, cardiovascular issues, and dementia.  

Contraindication / Caution

Contraindication/Caution: 

• Pregnancy: conjugated estrogens should not be used during pregnancy as they can cause fetal harm. 
• Breast cancer: conjugated estrogens should not be used in women with a history of breast cancer, as they may promote the growth of breast cancer cells. 
• Abnormal vaginal bleeding: conjugated estrogens should not be used in women with abnormal vaginal bleeding, as this may be a sign of a more serious condition. 
• Liver disease: conjugated estrogens should be used with caution in women with liver disease, as they may increase the risk of liver damage. 
• Blood clots: conjugated estrogens can increase the risk of blood clots, especially in women who have a history of blood clots or who are at high risk for blood clots. 
• Cardiovascular disease: conjugated estrogens may increase the risk of cardiovascular disease, especially in women who have a history of heart disease, high blood pressure, or high cholesterol. 
• Gallbladder disease: conjugated estrogens may increase the risk of gallbladder disease. 
• Endometriosis: conjugated estrogens should be used with caution in women with endometriosis, as they may worsen symptoms. 

Pregnancy / Lactation

Pregnancy consideration:  

Category X 

Breastfeeding warnings:  

Conjugated estrogens are excreted in breast milk and should be taken cautiously. 

Pregnancy category: 

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester. 
• Category B: No evidence of risk to the fetus is found in animal reproduction studies, and there are not enough studies on pregnant women. 
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for a human product; Pregnant women must take care of the potential risks. 
• Category D: There is adequate data with sufficient evidence of human fetal risk from various platforms. However, despite potential dangers may be used only in emergencies for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. The drug is not for pregnant women. 
• Category N: No data is available for the drug under this category. 

Pharmacology

Pharmacology: 

Once absorbed into the bloodstream, conjugated estrogens bind to estrogen receptors in various tissues and organs throughout the body. This results in a range of physiological effects, including: 

• Stimulation of the growth and development of female reproductive tissues, such as the uterus, vagina, and fallopian tubes. 
• Maintenance of bone density by inhibiting bone resorption and stimulating bone formation. 
• Regulation of cholesterol metabolism by decreasing LDL (bad) cholesterol levels and increasing HDL (good) cholesterol levels. 
• Maintenance of the health of the skin and mucous membranes. 
• Regulation of the menstrual cycle. 
• Reduction of menopausal symptoms, such as hot flashes, vaginal dryness, and mood changes.  

Pharmacodynamics: 

The pharmacodynamics of conjugated estrogens refers to the way in which they produce their effects in the body. Conjugated estrogens are a mixture of estrogen hormones that bind to estrogen receptors in various tissues and organs throughout the body. 

Pharmacokinetics: 

Absorption 

conjugated estrogens are readily absorbed from gastrointestinal tract 

The onset of action takes place in 2-4 weeks (PO-menopause) 

The peak plasma concentration is achieved in 7 hours 

Distribution 

The protein bound is 80% 

Metabolism 

The drug is metabolized in liver to form inactive sulfates and glucuronides 

The metabolites formed are Estradiol, estriol and estrone 

Elimination and Excretion 

The drug is mainly excreted in urine 

Adminstartion

Administration: 

conjugated estrogens are available in different formulations and can be administered orally, parenterally (by injection), or vaginally. 

• Oral tablets: conjugated estrogens are available in tablet form to be taken orally with or without food. The dosage and frequency of administration depend on the medical condition being treated and the individual patient’s response to treatment. 
• Parenteral injection: conjugated estrogens can be administered by injection either intravenously (into a vein) or intramuscularly (into a muscle). This method is generally used for short-term treatment or in emergency situations. 
• Vaginal cream: conjugated estrogens can also be administered as a cream applied vaginally. This method is typically used to treat vaginal dryness, itching, or discomfort associated with menopause. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: conjugated estrogens 

Pronounced: con-juh-gah-ted es-troh-gens  

Why do we use conjugated estrogens? 

conjugated estrogens are used for a variety of medical conditions related to hormonal imbalance. They are commonly used to treat symptoms of menopause, such as hot flashes, vaginal dryness, and mood changes. They may also be used to prevent bone loss and reduce the risk of osteoporosis in postmenopausal women. 

In addition to menopausal symptoms, conjugated estrogens may also be used to treat conditions such as hypoestrogenism (low levels of estrogen), ovarian failure, and female hypogonadism. They may also be used in the treatment of certain types of breast and prostate cancers, and to suppress ovulation in women with certain medical conditions.