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Conestoral

Conestoral - General Information

Conjugated estrogens, a mixture of the water-soluble salts of sulfate esters from estrone, equilin, 17 α-dihydroequilin, and other related steroids, may be derived from pregnant equine urine or yam and soy plants. Estrogens are important in the development and maintenance of the female reproductive system and secondary sex characteristics.

 

Pharmacology of Conestoral

Conjugated estrogens, a mixture of the water soluble salts of sulfate esters from estrone, equilin, 17 α-dihydroequilin, and other related steroids, may be derived from pregnant equine urine or yam and soy plants. Estrogens are important in the development and maintenance of the female reproductive system and secondary sex characteristics. They promote growth and development of the vagina, uterus, and fallopian tubes, and enlargement of the breasts. Indirectly, they contribute to the shaping of the skeleton, maintenance of tone and elasticity of urogenital structures, changes in the epiphyses of the long bones that allow for the pubertal growth spurt and its termination, growth of axillary and pubic hair, and pigmentation of the nipples and genitals. Decline of estrogenic activity at the end of the menstrual cycle can bring on menstruation, although the cessation of progesterone secretion is the most important factor in the mature ovulatory cycle. However, in the preovulatory or nonovulatory cycle, estrogen is the primary determinant in the onset of menstruation. Estrogens also affect the release of pituitary gonadotropins. The pharmacologic effects of conjugated estrogens are similar to those of endogenous estrogens.

 

Conestoral for patients

(Updated June 28, 2004)

ENJUVIA™

(synthetic conjugated estrogens, B) Tablets

Read this patient information before you start taking ENJUVIA, and read what you get each time you refill ENJUVIA. There may be new information. This information does not take the place of talking to your healthcare provider about your medical condition or your treatment.

WHAT IS THE MOST IMPORTANT INFORMATION I SHOULD KNOW ABOUT ENJUVIA (AN ESTROGEN HORMONE)?

· Estrogens increase the chances of getting cancer of the uterus.

Report any unusual vaginal bleeding right away while you are taking estrogens. Vaginal bleeding after menopause may be a warning sign of cancer of the uterus (womb). Your healthcare provider should check any unusual vaginal bleeding to find out the cause.

· Do not use estrogens with or without progestins to prevent heart disease, heart attacks, or strokes.

Using estrogens with or without progestins may increase your chances of getting heart attacks, strokes, breast cancer, and blood clots. Using estrogens with progestins may increase your risk of dementia. You and your healthcare provider should talk regularly to determine whether you still need treatment with ENJUVIA.

What is ENJUVIA?

ENJUVIA is a medicine that contains estrogen hormones.

What is ENJUVIA used for?

ENJUVIA is used after menopause to reduce moderate to severe hot flashes. Estrogens are hormones made by a woman's ovaries. The ovaries normally stop making estrogens when a woman is between 45 and 55 years old. This drop in body estrogen levels causes the "change of life" or menopause (the end of monthly menstrual periods). Sometimes, both ovaries are removed during an operation before natural menopause takes place. The sudden drop in estrogen levels causes "surgical menopause."

When the estrogen levels begin dropping, some women develop very uncomfortable symptoms, such as feelings of warmth in the face, neck, and chest, or sudden strong feelings of heat and sweating ("hot flashes" or "hot flushes"). In some women, the symptoms are mild, and they will not need estrogens. In other women, symptoms can be more severe. You and your healthcare provider should talk regularly about whether you still need treatment with ENJUVIA.

Who should not take ENJUVIA?

Do not start taking ENJUVIA if you:

  • have unusual vaginal bleeding
  • currently have or have had certain cancers - estrogens may increase the chances of getting certain types of cancers, including cancer of the breast or uterus. If you have or had cancer, talk with your healthcare provider about whether you should take ENJUVIA.
  • had a stroke or heart attack in the past year
  • currently have or have had blood clots
  • currently have or have had liver problems
  • are allergic to ENJUVIA or any of its ingredients - see the end of this leaflet for a list of ingredients in ENJUVIA.
  • think you may be pregnant

Tell your healthcare provider:

  • if you are breastfeeding - the hormones in ENJUVIA can pass into your milk.
  • about all of your medical problems - your healthcare provider may need to check you more carefully if you have certain conditions, such as asthma (wheezing), epilepsy (seizures), migraine, endometriosis, lupus, or problems with your heart, liver, thyroid, kidneys, or have high calcium levels in your blood.
  • about all the medicines you take - this includes prescription and nonprescription medicines, vitamins, and herbal supplements. Some medicines may affect how ENJUVIA works. ENJUVIA may also affect how your other medicines work.
  • if you are going to have surgery or will be on bedrest - you may need to stop taking estrogens.

How should I take ENJUVIA?

  • Take one ENJUVIA tablet by mouth at the same time each day.
  • Start at the lowest dose and talk to your healthcare provider about how well that dose is working for you.
  • Estrogens should be used at the lowest dose possible for your treatment only as long as needed. You and your healthcare provider should talk regularly (for example, every 3 to 6 months) about whether you still need treatment with ENJUVIA.
  • ENJUVIA may be taken with or without food.

What are the possible side effects of estrogens?

Less common but serious side effects include:

  • Breast cancer
  • Cancer of the uterus
  • Stroke
  • Heart attack
  • Blood clots
  • Dementia
  • Gallbladder disease
  • Ovarian cancer

These are some of the warning signs of serious side effects:

  • Breast lumps
  • Unusual vaginal bleeding
  • Dizziness and faintness
  • Changes in speech
  • Severe headaches
  • Chest pain
  • Shortness of breath
  • Pains in your legs
  • Changes in vision
  • Vomiting
Call your healthcare provider right away if you get any of these warning signs, or any other symptoms that concern you.

Common side effects include:

  • Headache
  • Breast pain
  • Irregular vaginal bleeding or spotting
  • Stomach/abdominal cramps, bloating
  • Nausea and vomiting
  • Hair loss

Other side effects include:

  • High blood pressure
  • Liver problems
  • High blood sugar
  • Fluid retention
  • Enlargement of benign tumors of the uterus ("fibroids")
  • Vaginal yeast infection

These are not all the possible side effects of ENJUVIA. For more information, ask your health-care provider or pharmacist.

What can I do to lower my chances of a serious side effect with ENJUVIA?

  • Talk with your healthcare provider regularly about whether you should continue taking ENJUVIA.
  • If you have a uterus, talk to your healthcare provider about whether the addition of a progestin is right for you.
  • See your healthcare provider right away if you get vaginal bleeding while taking ENJUVIA.
  • Have a breast exam and mammogram (breast X-ray) every year unless your healthcare provider tells you something else. If members of your family have had breast cancer or if you have ever had breast lumps or an abnormal mammogram, you may need to have breast exams more often.
  • If you have high blood pressure, high cholesterol (fat in the blood), diabetes, are overweight, or if you use tobacco, you may have higher chances for getting heart disease. Ask your healthcare provider for ways to lower your chances of getting heart disease.

General information about safe and effective use of ENJUVIA.

Medicines are sometimes prescribed for conditions that are not mentioned in patient information leaflets. Do not take ENJUVIA for conditions for which it is not prescribed. Do not give ENJUVIA to other people, even if they have the same symptoms you have. It may harm them.

Keep ENJUVIA out of the reach of children.

This leaflet provides a summary of the most important information about ENJUVIA. If you would like more information, talk with your healthcare provider or pharmacist. You can ask for information about ENJUVIA that is written

What are the ingredients in ENJUVIA?

ENJUVIA tablets for oral administration are available in 0.3 mg, 0.45 mg, 0.625 mg and 1.25 mg strengths of synthetic conjugated estrogens, B. These tablets contain the following inactive ingredients: ascorbyl palmitate, butylated hydroxyanisole, colloidal silicon dioxide, edetate disodium dehydrate, plasticized ethylcellulose, hypromellose, lactose monohydrate, magnesium stearate, purified water, iron oxide red, titanium dioxide, polyethylene glycol, polysorbate 80, triacetate and triacetin/glycerol. In addition, the 0.45 mg tablets contain iron oxide black and iron oxide yellow and the 1.25 mg tablets contain iron oxide yellow.

 

Conestoral Interactions

DRUG/LABORATORY TEST INTERACTIONS

1. Accelerated prothrombin time, partial thromboplastin time, and platelet aggregation time; increased platelet count; increased factors II, VII antigen, VIII antigen, VIII coagulant activity, IX, X, XII, VII-X complex, II-VII-X complex, and beta-thromboglobulin; decreased levels of anti-factor Xa and antithrombin III, decreased antithrombin III activity; increased levels of fibrinogen and fibrinogen activity; increased plasminogen antigen and activity.

2. Increased thyroid-binding globulin (TBG) levels leading to increased circulating total thyroid hormone levels as measured by protein-bound iodine (PBI), T4 levels (by column or by radioimmunoassay) or T3 levels by radioimmunoassay. T3 resin uptake is decreased, reflecting the elevated TBG. Free T4 and free T3 concentrations are unaltered. Patients on thyroid replacement therapy may require higher doses of thyroid hormone.

3. Other binding proteins may be elevated in serum, (i.e., corticosteroid binding globulin (CBG), sex hormone binding globulin (SHBG)) leading to increased total circulating corticosteroids and sex steroids, respectively. Free hormone concentrations may be decreased. Other plasma proteins may be increased (angiotensinogen/renin substrate, alpha-1-antitrypsin, ceruloplasmin).

4. Increased plasma HDL and HDL2 cholesterol subfraction concentrations, reduced LDL cholesterol concentration, increased triglyceride levels.

5. Impaired glucose tolerance.

6. Reduced response to metyrapone test.

 

Conestoral Contraindications

ENJUVIA tablets should not be used in individuals with any of the following conditions:

1. Undiagnosed abnormal genital bleeding.

2. Known, suspected, or history of cancer of the breast.

3. Known or suspected estrogen-dependent neoplasia.

4. Active deep vein thrombosis, pulmonary embolism or a history of these conditions.

5. Active or recent (e.g., within the past year) arterial thromboembolic disease (e.g., stroke, myocardial infarction).

6. Liver dysfunction or disease.

7. ENJUVIA tablets should not be used in patients with known hypersensitivity to its ingredients.

8. Known or suspected pregnancy. There is no indication for ENJUVIA in pregnancy. There appears to be little or no increased risk of birth defects in children born to women who have used estrogens and progestins from oral contraceptives inadvertently during early pregnancy.

 

Additional information about Conestoral

Conestoral Indication: For the treatment of moderate to severe vasomotor symptoms associated with the menopause, atrophic vaginitis, osteoporosis, hypoestrogenism due to hypogonadism, castration, primary ovarian failure, breast cancer (for palliation only), and Advanced androgen-dependent carcinoma of the prostate (for palliation only)
Mechanism Of Action: Estrogens enter the cells of responsive tissues (e.g., female organs, breasts, hypothalamus, pituitary) where they interact with a protein receptor, subsequently increasing the rate of synthesis of DNA, RNA, and some proteins. Estrogens decrease the secretion of gonadotropin-releasing hormone by the hypothalamus, reducing the secretion of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) from the pituitary.
Drug Interactions: Amobarbital The enzyme inducer decreases the effect of hormones
Aprobarbital The enzyme inducer decreases the effect of hormones
Butabarbital The enzyme inducer decreases the effect of hormones
Butalbital The enzyme inducer decreases the effect of hormones
Butethal The enzyme inducer decreases the effect of hormones
Ethotoin The enzyme inducer decreases the effect of hormones
Fosphenytoin The enzyme inducer decreases the effect of hormones
Griseofulvin The enzyme inducer decreases the effect of hormones
Heptabarbital The enzyme inducer decreases the effect of hormones
Hexobarbital The enzyme inducer decreases the effect of hormones
Mephenytoin The enzyme inducer decreases the effect of hormones
Methohexital The enzyme inducer decreases the effect of hormones
Methylphenobarbital The enzyme inducer decreases the effect of hormones
Pentobarbital The enzyme inducer decreases the effect of hormones
Phenobarbital The enzyme inducer decreases the effect of hormones
Phenytoin The enzyme inducer decreases the effect of hormones
Prednisolone The estrogenic agent increases the effect of corticosteroid
Prednisone The estrogenic agent increases the effect of corticosteroid
Primidone The enzyme inducer decreases the effect of hormones
Raloxifene Association not recommended
Secobarbital The enzyme inducer decreases the effect of hormones
Talbutal The enzyme inducer decreases the effect of hormones
Ursodeoxycholic acid Estrogens decreases the effect of ursodiol
Food Interactions: Avoid alcohol.
Take with food to reduce nausea.
Avoid excessive quantities of coffee or tea (Caffeine).
Generic Name: Conjugated Estrogens
Synonyms: Estrone Estrone Hydrogen Sulfate; Estrogens; Estrone-sulfate; Estrone Sulphate; Estrone Sulfate Sodium; Estrone Sulfate; Estrone Sodium Sulfate; Estrone Hydrogen Sulfate; Oestrone Sulphate; Sodium Estrone Sulfate
Drug Category: Estrogens
Drug Type: Small Molecule; Approved

Other Brand Names containing Conjugated Estrogens: Conestoral; Evex; Hyhorin; Morestin; Par Estro; Premarin; Prempro/Premphase;
Absorption: Well absorbed
Toxicity (Overdose): Nausea and vomiting
Protein Binding: 90% bound to plasma proteins
Biotransformation: Hepatic
Half Life: 7.4 hours
Dosage Forms of Conestoral: Powder, for solution Intravenous
Tablet Oral
Cream Topical
Chemical IUPAC Name: sodium [(8R,9S,13S,14S)-13-methyl-17-oxo-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-3-yl] sulfate
Chemical Formula: C18H21NaO5S
Conjugated Estrogens on Wikipedia: Not Available
Organisms Affected: Humans and other mammals