Microdiol - General Information:Generally refers to the 17-beta-isomer of estradiol, an aromatized C18 steroid with hydroxyl group at 3-beta- and 17-beta-position. Microdiol-17-beta is the most potent form of mammalian estrogenic steroids. In humans, it is produced primarily by the cyclic ovaries and the placenta. It is also produced by the adipose tissue of men and postmenopausal women. The 17-alpha-isomer of estradiol binds weakly to estrogen receptors (receptors, estrogen) and exhibits little estrogenic activity in estrogen-responsive tissues. Various isomers can be synthesized. [PubChem]
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Pharmacology:Microdiol, the principal intracellular human estrogen, is substantially more active than its metabolites, estrone and estriol, at the cellular level.
Microdiol for patients
Read this PATIENT INFORMATION before you start taking EstroGel and read the patient information each time you refill your EstroGel prescription. 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 EstroGel (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 attack, strokes, breast cancer, and blood clots. You and your healthcare provider should talk regularly about whether you still need treatment with EstroGel.
What is EstroGel?
EstroGel is a clear, colorless gel medicine that contains an estrogen hormone (estradiol) which is absorbed through the skin into the bloodstream. The estrogen hormone in EstroGel is a synthetic estrogen made from a plant source.
What is EstroGel used for?
EstroGel is used after menopause to:
· reduce moderate to severe hot flashes
Estrogens are hormones made by a womanís 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 get very uncomfortable symptoms, such as feelings of warmth in the face, neck, and chest, or sudden intense episodes 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 EstroGel.
· treat moderate to severe dryness, itching, and burning in and around your vagina
You and your healthcare provider should talk regularly about whether you still need treatment with EstroGel to control these problems. If you use EstroGel only to treat your dryness, itching, and burning in and around your vagina, talk with your healthcare provider about whether a topical vaginal product would be better for you.
Who should not use EstroGel?
Do not start using EstroGel if you:
· have unusual vaginal bleeding
· currently have or have had certain cancers
Estrogens may increase the chances of getting certain types of cancer, including cancer of the breast or uterus. If you have or have had cancer, talk with your healthcare provider about whether you should use EstroGel.
· 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 EstroGel or any of its ingredients
See the end of this leaflet for a list of ingredients in EstroGel.
· think you may be pregnant
Tell your healthcare provider:
· if you are breastfeeding
The hormone in EstroGel can pass into your breast milk.
· about all 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 EstroGel works. EstroGel may also affect how your other medicines work.
· if you are going to have surgery or will be on bed rest
You may need to stop taking estrogens.
How is EstroGel supplied?
EstroGel is available in a metered dose pump that delivers 1.25 grams (g) of a gel containing 0.75 milligrams (mg) of estradiol each time the pump is depressed.
Please refer to the chart below to determine the number of full pump depressions required for the daily dose prescribed by your healthcare provider:
Prescribed Daily Dose
Number of Pump
Amount of estradiol
How should I use the EstroGel pump?
It is important that you read and follow these directions on how to use the EstroGel pump properly.
1. Before using the pump for the first time, it must be primed. Remove the large pump cover and fully depress the pump twice. Discard the unused gel by thoroughly rinsing down the sink or placing it in the household trash in a manner that avoids accidental exposure or ingestion by household members or pets. After priming, the pump is ready to use, and one complete pump depression will dispense the same amount of EstroGel each time.
2. Apply EstroGel at the same time each day. You should apply your daily dose of gel to clean, dry, unbroken skin. If you take a bath or shower or use a sauna, apply your EstroGel dose after your bath, shower, or sauna. If you go swimming, try to leave as much time as possible between applying your EstroGel dose and going swimming.
3. Be sure your skin is completely dry before applying EstroGel.
4. To apply the dose, collect the gel into the palm of your hand by pressing the pump firmly and fully with one fluid motion without hesitation.
5. Apply the gel to one arm using your hand. Spread the gel as thinly as possible over the entire area on the inside and outside of your arm from wrist to shoulder.
6. Always place the small protective cap back on the tip of the pump, and the large pump cover over the top of the pump after each use.
7. Wash your hands with soap and water after applying the gel to reduce the chance that the medicine will spread from your hands to other people.
8. It is not necessary to massage or rub in EstroGel. Simply allow the gel to dry for up to five minutes before dressing.
9. Alcohol based gels are flammable. Avoid fire, flame or smoking until the gel has dried.
10. Once dry, EstroGel is odorless.
11. Never apply EstroGel directly to the breast. Do not allow others to apply the gel for you.
12. The EstroGel pump contains enough product to allow for initial priming of the pump twice and to deliver 64 daily doses. After you have initially primed the pump twice and dispensed 64 doses, you will need to discard the pump.
What should I do if someone else is exposed to EstroGel?
If someone else is exposed to EstroGel by direct contact with the gel, that person should wash the area of contact with soap and water as soon as possible. The longer the gel is in contact with the skin before washing, the greater is the chance that the other person will absorb some of the estrogen hormone. This is especially important for men and children.
What should I do if I get EstroGel in my eyes?
If you get EstroGel in your eyes, rinse your eyes right away with warm clean water to flush out any EstroGel. Seek medical attention if needed.
What should I do if I miss a dose?
If you miss a dose, do not double the dose on the next day to catch up. If your next dose is less than 12 hours away, it is best just to wait and apply your normal dose the next day. If it is more than 12 hours until the next dose, apply the dose you missed and resume your normal dosing the next day.
What should I avoid while using EstroGel?
It is important that you do not spread the medicine to others, especially men and children. Be sure to wash your hands after applying EstroGel. Do not allow others to make contact with the area of skin where you applied the gel for at least one hour after application. Alcohol based gels are flammable. Avoid fire, flame or smoking until the gel has dried.
What are the possible side effects of estrogens?
Less common but serious side effects include:
· Breast cancer
· Cancer of the uterus
· Heart attack
· Blood clots
· 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
Call your healthcare provider right away if you get any of these warning signs, or any other unusual symptoms that concerns you.
Common side effects include:
· 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 EstroGel. For more information, ask your healthcare provider or pharmacist.
What can I do to lower my chances of getting a serious side effect with EstroGel?
Talk with your healthcare provider regularly about whether you should continue using EstroGel. If you have a uterus, talk with 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 using EstroGel. 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 of getting heart disease. Ask your healthcare provider for ways to lower your chances of getting heart disease.
General information about the safe and effective use of EstroGel
Medicines are sometimes prescribed for conditions that are not mentioned in patient information leaflets. Do not use EstroGel for conditions for which it was not prescribed. Do not give EstroGel to other people, even if they have the same symptoms you have. It may harm them.
Keep EstroGel out of the reach of children.
This leaflet provides a summary of the most important information about EstroGel. If you would like more information, talk with your healthcare provider or pharmacist. You can ask for information about EstroGel that is written for health professionals. You can get more information by calling the toll free number 800-241-1643.
What are the ingredients of EstroGel?
EstroGel contains estradiol, purified water, alcohol, triethanolamine, and carbomer 934P.
EstroGel should be stored with the cap on securely. Store at 20° to 25°C (68° to 77°F); excursions permitted to 15° to 30°C (59° to 86°F) [See USP Controlled Room Temperature]. Do not freeze. The gel should not be used after the date printed on the end of the metered-dose pump after the term "Exp." (expiry date).
Manufactured for: Unimed Pharmaceuticals, Inc., A Solvay Pharmaceuticals, Inc. company Marietta, GA 30062 By Laboratoires Besins International Montrouge, France 500123 3E Rev 3/2004, © 2004 Solvay Pharmaceuticals, Inc.
D. Drug and 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) 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 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.
Estrogens 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 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. EstroGel therapy should not be used in patients with known hypersensitivity to its ingredients.
8. Known or suspected pregnancy. There is no indication for EstroGel 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 MicrodiolMicrodiol Indication: For the treatment of urogenital symptoms associated with post-menopausal atrophy of the vagina (such as dryness, burning, pruritus and dyspareunia) and/or the lower urinary tract (urinary urgency and dysuria).
Mechanism Of Action: Microdiol enters target cells freely (e.g., female organs, breasts, hypothalamus, pituitary) and interacts with a target cell receptor. When the estrogen receptor has bound its ligand it can enter the nucleus of the target cell, and regulate gene transcription which leads to formation of messenger RNA. The mRNA interacts with ribosomes to produce specific proteins that express the effect of estradiol upon the target cell. Estrogens increase the hepatic synthesis of sex hormone binding globulin (SHBG), thyroid-binding globulin (TBG), and other serum proteins and suppress follicle-stimulating hormone (FSH) from the anterior 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
Secobarbital The enzyme inducer decreases the effect of hormones
Talbutal The enzyme inducer decreases the effect of hormones
Raloxifene Association not recommended
Ursodeoxycholic acid Estrogens decreases the effect of ursodiol
Food Interactions: Take with food to decrease nausea.
Generic Name: Estradiol
Synonyms: D-Estradiol; D-Oestradiol; Estradiol-17beta; Estradiol Valerate; Estradiol Cypionate; Dihydroxyestrin; Dihydroxyoestrin; Dihydroxyesterin; Dihydrofollicular Hormone; Dihydrofolliculin; Cis-Estradiol; Cis-Oestradiol; Beta-Estradiol
Drug Category: Anti-menopausal Agents; Anticholesteremic Agents; Estrogens
Drug Type: Small Molecule; Approved
Other Brand Names containing Estradiol: Aerodiol; Agofollin; Alora; Altrad; Amnestrogen; Aquadiol; Bardiol; Climaderm; Climara; Combipatch; Compudose; Compudose 200; Compudose 365; Corpagen; Delestrogen; Depo-Estradiol; Dermestril; Dihydromenformon; Dihydrotheelin; Dimenformon; Dimenformon Prolongatum; Diogyn; Diogynets; Divigel; Encore; Esclim; Estinyl; Estrace; Estraderm; Estraderm Tts; Estradurin; Estrasorb; Estreva; Estrifam; Estring; Estring Vaginal Ring; Estroclim; Estroclim 50; Estrofem 2; Estrofem Forte; Estrogel; Estrogens, Esterified; Estrovite; Evorel; Extrasorb; Femestral; Femestrol; Feminone; Femogen; Fempatch; Femring; Femtrace; Femtran; Follicyclin; Ginedisc; Ginosedol; Gynergon; Gynestrel; Gynodiol; Gynoestryl; Gynpolar; Innofem; Lamdiol; Lynoral; Macrodiol; Macrol; Menest; Menorest; Menostar; Microdiol; Nordicol; Oestergon; Oestradiol; Oestradiol R; Oestrogel; Oestroglandol; Oestrogynal; Ovahormon; Ovasterol; Ovastevol; Ovociclina; Ovocyclin; Ovocycline; Ovocylin; Perlatanol; Primofol; Profoliol; Profoliol B; Progynon; Progynon Dh; Progynon-Dh; Ricifon; Ritsifon; Sandrena Gel; Sisare Gel; Sk-Estrogens; Soldep; Sotipox; Syndiol; Systen; Tradelia; Trial Sat; Trocosone; Vagifem; Vivelle; Zerella; Zumenon; Elestrin; Evamist;
Toxicity (Overdose): Can cause nausea and vomiting, and withdrawal bleeding may occur in females.
Protein Binding: >95%
Biotransformation: Exogenous estrogens are metabolized using the same mechanism as endogenous estrogens. Estrogens are partially metabolized by cytochrome P450.
Half Life: 36 hours
Dosage Forms of Microdiol: Ring Intravaginal
Chemical IUPAC Name: (8R,9S,13S,14S,17S)-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol
Chemical Formula: C18H24O2
Estradiol on Wikipedia: http://en.wikipedia.org/wiki/Estradiol
Organisms Affected: Humans and other mammals
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