Follestrine - General Information

An aromatized C18 steroid with a 3-hydroxyl group and a 17-ketone, a major mammalian estrogen. It is converted from androstenedione directly, or from testosterone via estradiol. In humans, it is produced primarily by the cyclic ovaries, placenta, and the adipose tissue of men and postmenopausal women. [PubChem]


Pharmacology of Follestrine

Follestrine, a synthetically prepared or naturally occurring steroidal estrogen obtained from pregnant equine urine, is the primary circulating estrogen after menopause. Follestrine is naturally derived from the peripheral conversion of androstenedione by an aromatase enzyme found in adipose tissues and is converted to estradiol in peripheral tissues. Estropipate is piperazine-stabilized estrone sulfate. Follestrine, and estropipate are used to treat abnormalities related to gonadotropin hormone dysfunction, vasomotor symptoms, atrophic vaginitis, and vulvar atrophy associated with menopause, and for the prevention of osteoporosis due to estrogen deficiency.


Follestrine for patients


This medicine is a combination of estrogen and progesterone use to treat menopause symptoms. Your doctor may prescribe this medicine for other conditions as well.

General Information

This information is for educational purposes only. Not every known side effect, adverse effect, or drug interaction is in this database. If you have questions about your medicines, talk to your healthcare provider.

Proper use of this medicine

Follow the directions provided to you by your doctor or pharmacy. This medicine may come with a patient information leaflet. This medicine can be taken with food or on an empty stomach. Take this medicine at the same time every day.

Missed Dose

Take your next dose as soon as you remember. If it is time for your next dose, skip the missed dose and go back to your regular schedule. Do not double doses.


Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat and moisture (not in the bathroom). Throw away any medication that is outdated or no longer needed.

Possible Side Effects

nausea, vomiting, diarrhea
rash, itching
loss of scalp hair
change in libido
back pain
dizziness, lightheadedness
stomach upset, bloating or nausea
Notify your doctor if you experience any of the following:
severe depression
calf pain
sudden severe headache
chest pain
shortness of breath
lumps in the breast
weakness or tingling in the arms or legs
changes in vaginal bleeding
nausea, loss of appetite, bloating
breast tenderness
breakthrough bleeding, spotting, missed periods
If you experience weight changes, depression, swelling of the ankles or fingers, check with your doctor as soon as possible.
Contact your doctor if you experience any of the following:
sudden or severe headache
loss of coordination
sudden loss of vision, slurred speech
severe chest pain, or weakness or numbness in the arms or legs


Follestrine Interactions

Drug Interactions

This medicine may be affected by the drug cholestyramine and should not be taken with any form of estrogen therapy. Talk to your pharmacist for more information.
Drugs that may decrease the effects of this medicine include:
phenytoin (Dilantin)
carbamazepine (Tegretol)
Estrogens may decrease the effects of benzodiazepines (lorezepam
temezepam). If you are taking these medicines together or you have further questions about drug interactions
talk to your doctor or pharmacist.
Consult your doctor or pharmacist if you are taking any of the following:
seizure medications
medications to help you sleep


Follestrine Contraindications

Estrogens/ estradiol/ estrones should not be used:

During Pregnancy: Vaginal Cream, Oral Tablets, Transdermal. If you think you may be pregnant, do not use any form of estrogen-containing drug. Using estrogens while you are pregnant may cause your unborn child to have birth defects. Estrogens do not prevent miscarriage.
If You Have Unusual Vaginal Bleeding Which Has not Been Evaluated by Your Doctor: Vaginal Cream, Oral Tablets, Transdermal. Unusual vaginal bleeding can be a warning sign of cancer of the uterus, especially if it happens after menopause. Your doctor must find out the cause of the bleeding so that he or she can recommend the proper treatment. Taking estrogens without visiting your doctor can cause you serious harm if your vaginal bleeding is caused by cancer of the uterus.
If You Have Had Cancer: Since estrogens increase the risk of certain types of cancer, you should not use estrogens if you have ever had cancer of the breast or uterus, unless your doctor recommends that the drug may help in cancer treatment. (For certain patients with breast or prostate cancer, estrogens may help.)
If You Have any Circulation Problems: Estrogen drugs should not be used except in unusually special situations in which your doctor judges that you need estrogen therapy so much that the risks are acceptable. Men and women with abnormal blood clotting conditions should avoid estrogen use (see Dangers of Estrogens).
When They do not Work: During menopause, some women develop nervous symptoms or depression. Estrogens do not relieve these symptoms. You may have heard that taking estrogens for years after menopause will keep your skin soft and supple and keep you feeling young. There is no evidence for these claims and such long-term estrogen use may have serious risks.
After Childbirth or When Breastfeeding a Baby: Estrogens should not be used to try to stop the breasts from filling with milk after a baby is born. Such treatment may increase the risk of developing blood clots (see Dangers of Estrogens).
If you are breastfeeding, you should avoid using any drugs because many drugs pass through to the baby in the milk. While nursing a baby, you should take drugs only on the advice of your health care provider.


Additional information about Follestrine

Follestrine Indication: For management of Menopausal and postmenopausal disorders
Mechanism Of Action: Estrogens enter the cells of responsive tissues (e.g., female organs, breasts, hypothalamus, pituitary) where they interact with a protein receptor, estrogen receptors, subsequently increasing the rate of synthesis of DNA, RNA, and some proteins. 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: Not Available
Food Interactions: Not Available
Generic Name: Estrone
Synonyms: Not Available
Drug Category: Antineoplastic Agents; Osteoporosis Prophylactic; Anti-menopausal Agents; Estrogens
Drug Type: Small Molecule; Approved

Other Brand Names containing Estrone: Aquacrine; Crinovaryl; Cristallovar; Crystogen; Destrone; Disynformon; Endofolliculina; Esterone; Estrin; Estrogenic Substance; Estrol; Estron; Estrona; Estrona [Inn-Spanish]; Estrona [Spanish]; Estrone [Usan-Inn]; Estrone-A; Estronum [Inn-Latin]; Estrovarin; Estrugenone; Estrusol; Femestrone Inj.; Femestrone Injection; Femidyn; Fermidyn; Folikrin; Folipex; Folisan; Follestrine; Follestrol; Follicular Hormone; Folliculin; Folliculine; Folliculine Benzoate; Follicunodis; Follidrin; GSS 33; Glandubolin; Hiestrone; Hormestrin; Hormofollin; Hormovarine; Kestrone; Ketodestrin; Ketohydroxy-Estratriene; Ketohydroxyestrin; Ketohydroxyoestrin; Ketophydroxyestrin; Kolpon; Menagen; Menformon; Menformon A; Mestronaq; OVEX; Oestrin; Oestroform; Oestrone; Oestrone [Steroidal Oestrogens]; Oestronum; Oestroperos; Ovifollin; Penncap M; Perlatan; Sinafid M-48; Solliculin; Theelin; Thelestrin; Thelykinin; Thynestron; Tokokin; Unden; Wynestron; Wynestronpencap M;
Absorption: 43%
Toxicity (Overdose): Symptoms of overdose include nausea and vomiting. Withdrawal bleeding may occur in females.
Protein Binding: >95%
Biotransformation: Hepatic.
Half Life: 19 hours
Dosage Forms of Follestrine: Solution / drops Oral
Liquid Oral
Cream Intravaginal
Chemical IUPAC Name: (8R,9S,13S,14S)-3-hydroxy-13-methyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-17-one
Chemical Formula: C18H22O2
Estrone on Wikipedia:
Organisms Affected: Humans and other mammals