Drug information of Dienestrol

Dienestrol

Drug group: Hormone

Dienestrol is a synthetic, non-steroidal estrogen. It is an estrogen receptor agonist. Estrogens work partly by increasing a normal clear discharge from the vagina and making the vulva and urethra healthy. Using or applying an estrogen relieves or lessens: dryness and soreness in the vagina, itching, redness, or soreness of the vulva. Conditions that are treated with vaginal estrogens include a genital skin condition (vulvar atrophy), inflammation of the vagina (atrophic vaginitis), and inflammation of the urethra (atrophic urethritis).

Mechanism of effect

Dienestrol is a synthetic, non-steroidal estrogen. Estrogens passively diffuse into target cells of responsive tissues, complex with the estrogen receptors, and enter the cell's nucleus to initiate or enhance gene transcription of protein synthesis after binding to DNA.

Pharmacodynamic

Estrogens diffuse into their target cells and interact with a protein receptor. Target cells include the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. 

Pharmacokinetics

Drug Concentration Levels
A) Time to Peak Concentration
Vaginal, Cream: 3 to 4 hours
Vaginal estrogen preparations are readily absorbed, producing higher blood levels than those obtained when the same quantity of drug is given orally
Absorption
A) Bioavailability
Systemic absorption and mode of action of dienestrol are unquantified but is often sufficient enough to cause systemic effects
Metabolism
A) Metabolism Sites and Kinetics
The inactivation of estrogen in the body is carried out in the liver; however, topical therapy results initially in a bypass of the hepatic circulation

Drug indications

For use in the treatment of atrophic vaginitis and kraurosis vulvae.

Dosage

    For estrone
    For vaginal dosage form (cream):
        For treating a genital skin condition (vulvar atrophy) and inflammation of the vagina (atrophic vaginitis) in postmenopausal women:
            Adults—2 to 4 milligrams (mg) of estrone (two to four grams of cream) inserted into the vagina once a day or as directed by your doctor.
    For vaginal dosage form (suppository):
        For treating a genital skin condition (vulvar atrophy) and inflammation of the vagina (atrophic vaginitis) in postmenopausal women:
            Adults—250 to 500 micrograms (mcg) inserted into the vagina once a day or as directed by your doctor.

Drug contraindications

A) cancer of the breast
B) estrogen-dependent neoplasia
C) genital bleeding, undiagnosed abnormal
D) history of thrombophlebitis, thrombosis, or thromboembolic disorders associated with previous estrogen use
E) pregnancy
F) thrombophlebitis or thromboembolic disorders, activethrombophlebitis or thromboembolic disordeactive

Side effects

Less common
  • Breast pain
  • enlarged breasts
  • itching of the vagina or genitals
  • headache
  • nausea
  • stinging or redness of the genital area
  • thick, white vaginal discharge without odor or with a mild odor
Rare
  • Feeling of vaginal pressure (with estradiol vaginal insert or ring)
  • unusual or unexpected uterine bleeding or spotting
  • vaginal burning or pain (with estradiol vaginal insert or ring)
 
Incidence not known
  • Diarrhea
  • dizziness
  • fast heartbeat
  • feeling faint
  • fever
  • hives
  • hoarseness
  • itching
  • joint pain, stiffness, or swelling
  • muscle pain
  • rash
  • shortness of breath
  • skin redness
  • swelling of eyelids, face, lips, hands, or feet
  • tightness in the chest
  • trouble with breathing or swallowing
  • vomiting
  • wheezing
Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:
Less common
  • Abdominal or back pain
  • clear vaginal discharge (usually means the medicine is working)
Incidence not known
  • Acne
  • enlargement of penis or testes
  • growth of pubic hair
  • rapid increase in height
  • swelling of the breasts or breast soreness in males

Using medicines in this class with any of the following medicines is not recommended. Your doctor may decide not to treat you with a medication in this class or change some of the other medicines you take.
  • Dasabuvir
  • Ombitasvir
  • Paritaprevir
  • Ritonavir
  • Tranexamic Acid
  • Using medicines in this class with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.
    • Amifampridine
    • Apalutamide
    • Aprepitant
    • Armodafinil
    • Artemether
    • Bexarotene
    • Boceprevir
    • Bosentan
    • Brigatinib
    • Bupropion
    • Carbamazepine
    • Cenobamate
    • Ceritinib
    • Clobazam
    • Conivaptan
    • Dabrafenib
    • Darunavir
    • Dexamethasone
    • Dicloxacillin
    • Donepezil
    • Doxycycline
    • Efavirenz
    • Elvitegravir
    • Encorafenib
    • Enzalutamide
    • Eslicarbazepine Acetate
    • Etravirine
    • Fosaprepitant
    • Fosnetupitant
    • Fosphenytoin
    • Griseofulvin
    • Isotretinoin
    • Ivosidenib
    • Lesinurad
    • Lixisenatide
    • Lorlatinib
    • Lumacaftor
    • Minocycline
    • Mitotane
    • Modafinil
    • Mycophenolic Acid
    • Nafcillin
    • Netupitant
    • Nevirapine
    • Oxcarbazepine
    • Phenobarbital
    • Phenylbutazone
    • Phenytoin
    • Pitolisant
    • Pixantrone
    • Prednisone
    • Primidone
    • Red Clover
    • Rifabutin
    • Rifampin
    • Rifapentine
    • Rufinamide
    • Secobarbital
    • St John's Wort
    • Sugammadex
    • Tazemetostat
    • Telaprevir
    • Theophylline
    • Topiramate
    • Ulipristal
    • Valproic Acid

Alerts

It is not yet known whether the use of vaginal estrogens increases the risk of breast cancer in women. It is very important that you check your breasts on a regular basis for any unusual lumps or discharge. Report any problems to your doctor. You should also have a mammogram (x-ray picture of the breasts) done if your doctor recommends it.
It is important that you have a regular pelvic exam (pap smear). Your doctor will tell you how often this exam should be done.
Talk to your doctor if you have high blood pressure, high cholesterol (fats in the blood), or diabetes, use tobacco, or are overweight. You may have a higher risk for getting heart disease.
Although the chance is low, use of estrogen may increase your chance of getting cancer of the ovary or uterus (womb). Regular visits to your health professional can help identify these serious side effects early.

Points of recommendation

Avoid using latex condoms, diaphragms, or cervical caps for up to 72 hours after using estrogen vaginal creams. Certain estrogen products may contain oils in the creams that can weaken latex (rubber) products and cause condoms to break or leak, or cervical caps or diaphragms to wear out sooner. Check with your health care professional to make sure the vaginal estrogen product you are using can be used with latex devices.
This medicine is often used at bedtime to increase effectiveness through better absorption.
Vaginal creams or suppositories will melt and leak out of the vagina. A minipad or sanitary napkin will protect your clothing. Do not use tampons (like those used for menstrual periods) since they may soak up the medicine and make the medicine less effective.
Avoid exposing your male sexual partner to your vaginal estrogen cream or suppository by not having sexual intercourse right after using these medicines. Your male partner might absorb the medicine through his penis if it comes in contact with the medicine.

Pregnancy level

Estrogens should not be used during pregnancy, since an estrogen called diethylstilbestrol (DES) that is no longer taken for hormone replacement has caused serious birth defects in humans and animals.

Breast feeding warning

Use of this medicine is not recommended in nursing mothers. Estrogens pass into the breast milk and may decrease the amount and quality of breast milk. Caution should be exercised in mothers who are using estrogen and breast-feeding.

Drug forms

Estrace Estring Femring Imvexxy Ortho Dienestrol Premarin Premarin Vaginal Vagifem

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