Vaginal estrogen

Short description: Estrogen administered intervaginally

Vaginal estrogen is a form of estrogen that is delivered by intravaginal administration. Vaginally administered estrogens are thereby exerting their effects mainly in the nearby tissue, with more limited systemic effects compared to orally administered estrogens.[1] It will not protect against osteoporosis.[2] With perhaps the exception of the Femring,[3] it also will not alleviate the hot flashes and hormonal imbalance caused by menopause.[2]

## Contents

* 1 Indications
* 2 Forms
* 3 Side effects
* 4 Contraindications
* 4.1 Pregnant women
* 4.2 Breastfeeding
* 5 Alternatives
* 6 See also
* 7 References

## Indications

Vaginally administered estrogen are usually used to treat some menopausal symptoms that are isolated to the vagina, vulva, and urethra.[4]

* Atrophic vaginitis, with presentations such as dryness and soreness in the vagina and dyspareunia (pain during sexual intercourse)[1]
* Itching, redness, or soreness of the vulva[1]
* Urinary urgency (feeling an urge to urinate more often than is needed), or dysuria (experiencing pain while urinating)[5]

## Forms

* Vaginal tablets, including Vagifem which contains estradiol[6]
* Vaginal creams, including Premarin which is a compound cream[7] consisting primarily of conjugated estrogens isolated from mare's urine. Another vaginal cream is Ovesterin, which contains estriol.
* Vaginal rings (such as Oestring), which are polymeric drug delivery devices designed to provide controlled release of drugs to the vagina over extended periods of time. Although the Femring might be able to ease hot flashes,[3] this does not appear to be the case for other vaginal estrogen rings or vaginal creams.[8]

## Side effects

Most of the vaginally administered estrogens are synthetic and therefore cause the following side effects[9]

Serious side effects:

* chest pain or heavy feeling, pain spreading to the arm or shoulder, nausea, sweating, general ill feeling;
* sudden numbness or weakness, especially on one side of the body;
* sudden severe headache, confusion, problems with vision, speech, or balance;
* pain, swelling, warmth, or redness in one or both legs;
* abnormal vaginal bleeding;
* migraine headache;
* pain, swelling, or tenderness in the stomach;
* confusion, problems with memory or concentration;
* jaundice (yellowing of the skin or eyes);
* swelling in the hands, ankles, or feet; or
* a breast lump.

Less serious side effects may include:[10]

* mild nausea, vomiting, bloating, stomach cramps;
* breast pain, tenderness, or swelling;
* freckles or darkening of facial skin;
* increased hair growth, loss of scalp hair;
* changes in weight or appetite;
* problems with contact lenses;
* vaginal itching or discharge;
* changes in the menstrual periods, decreased sex drive; or
* headache, nervousness, dizziness, tired feeling.

## Contraindications

Estrogen administered vaginally should not be given to persons who are:

### Pregnant women

Estrogen should not be used while pregnant as it could cause serious birth defects.

### Breastfeeding

Estrogen passes into the breast milk and will cause a decrease in the production and quality of breast milk.

## Alternatives

To effectively alleviate the symptoms of menopause, it is best to take oral estrogen instead of topical estrogen since the results are systemic and it will rejuvenate the entire reproductive system and not just the perineal area.[11][additional citation(s) needed]

Phytoestrogens are plant derived compounds found in a wide variety of foods. Several health benefits including a lowered risk of osteoporosis, heart disease, breast cancer, and menopausal symptoms are frequently attributed to phytoestrogens but many are also considered to have the potential to cause adverse health effects.[12] Plants such as Kacip Fatimah have been found to contain phytoestrogens that could alleviate some symptoms of menopause.[13]

## See also

* Pharmacokinetics of estradiol § Vaginal administration

## References

1. ↑ 1.0 1.1 1.2 Estrogen (Vaginal Route) from Mayo Clinic / Thomson Healthcare Inc. Portions of this document last updated: Nov. 1, 2011
2. ↑ 2.0 2.1 "Estrogen (Vaginal Route) Before Using - Mayo Clinic". http://www.mayoclinic.org/drugs-supplements/estrogen-vaginal-route/before-using/drg-20069459.
3. ↑ 3.0 3.1 Pharmacology for Nurses. Jones & Bartlett Publishers. 2014. p. 80. ISBN 978-1449689407. https://books.google.com/books?id=7P-9BQAAQBAJ&pg=PA80.
4. ↑ "Estrogen (Vaginal route)". Mmddic/DDIC602127 (National Center for Biotechnology Information). 2015-10-01. https://www.ncbi.nlm.nih.gov/books/PMH0045756/.
5. ↑ "Estrogen Vaginal Advanced Patient Information - Drugs.com". https://www.drugs.com/cons/estrogen-vaginal.html.
6. ↑ Vagifem - Manufacturer's website
7. ↑ Premarin (conjugated estrogens) Vaginal Cream - Detailed View: Safety Labeling Changes Approved By FDA Center for Drug Evaluation and Research (CDER) -- November 2008
8. ↑ Pharmacology for Pharmacy Technicians - E-Book. Elsevier Health Sciences. 2014. p. 573. ISBN 978-0323292658. https://books.google.com/books?id=ZtHsAwAAQBAJ&pg=PA573.
9. ↑ "Side Effects of Premarin Vaginal Cream (Conjugated Estrogens Vaginal Cream) Drug Center - RxList". http://www.rxlist.com/premarin-vaginal-cream-side-effects-drug-center.htm.
10. ↑ "Estrogen Vaginal: MedlinePlus Drug Information". https://www.medlineplus.gov/druginfo/meds/a606005.html.
11. ↑ "Hormone Replacement Therapy". http://www.drmarinajohnson.com/articles/hormone-replacement-therapy/.
12. ↑ Patisaul, Heather B.; Jefferson, Wendy (2010-10-01). "The pros and cons of phytoestrogens". Frontiers in Neuroendocrinology 31 (4): 400–419. doi:10.1016/j.yfrne.2010.03.003. ISSN 0091-3022. PMID 20347861.
13. ↑ Nadia, M. E.; Nazrun, A. S.; Norazlina, M.; Isa, N. M.; Norliza, M.; Ima Nirwana, S. (2012). "The Anti-Inflammatory, Phytoestrogenic, and Antioxidative Role of Labisia pumilain Prevention of Postmenopausal Osteoporosis". Advances in Pharmacological Sciences 2012: 1–7. doi:10.1155/2012/706905. PMID 22611381.

* v
* t
* e

Estrogens and antiestrogens

Estrogens|

| ER agonists|

* Steroidal: Alfatradiol
* Certain androgens/anabolic steroids (e.g., testosterone, testosterone esters, methyltestosterone, metandienone, nandrolone esters) (via estrogenic metabolites)
* Certain progestins (e.g., norethisterone, noretynodrel, etynodiol diacetate]], tibolone)
* Clomestrone
* Cloxestradiol acetate
* Conjugated estriol
* Conjugated estrogens
* Epiestriol
* Epimestrol
* Esterified estrogens
* Estetrol†
* Estradiol
* Estradiol esters (e.g., estradiol acetate, estradiol benzoate, estradiol cypionate, estradiol enanthate, estradiol undecylate, [[Chemistry:Estradiol estradiol valerate, Polyestradiol phosphate|polyestradiol phosphate]], estradiol ester mixtures (Climacteron))
* Estramustine phosphate
* Estriol
* Estriol esters (e.g., estriol succinate, polyestriol phosphate)
* Estrone
* Estrone esters
* Estrone sulfate
* Estropipate (piperazine estrone sulfate)
* Ethinylestradiol#
* Ethinylestradiol sulfonate
* Hydroxyestrone diacetate
* Mestranol
* Methylestradiol
* Moxestrol
* Nilestriol
* Prasterone (dehydroepiandrosterone; DHEA)
* Prasterone enanthate
* Prasterone sulfate
* Promestriene
* Quinestradol
* Quinestrol

* Nonsteroidal: Benzestrol
* Bifluranol
* Chlorotrianisene
* Dienestrol
* Dienestrol diacetate
* Diethylstilbestrol (stilbestrol)
* Diethylstilbestrol esters/ethers
* Dimestrol (diethylstilbestrol dimethyl ether)
* Fosfestrol (diethylstilbestrol diphosphate)
* Mestilbol (diethylstilbestrol monomethyl ether)
* Doisynoestrol (fenocycline)
* Hexestrol
* Hexestrol esters
* Methallenestril
* Methestrol dipropionate (promethestrol dipropionate)
* Paroxypropione
* Quadrosilan
* Triphenylbromoethylene
* Triphenylchloroethylene
* Zeranol

|

Progonadotropins|

* Antiandrogens (e.g., bicalutamide)
* GnRH agonists (e.g., GnRH (gonadorelin), leuprorelin)
* Gonadotropins (e.g., FSH, LH)

Antiestrogens|

| ER antagonists
(incl. SERMs/SERDs)|

* Acolbifene†
* Anordrin
* Bazedoxifene
* Broparestrol
* Clomifene#
* Cyclofenil
* Enclomifene†
* Epitiostanol
* Lasofoxifene
* Mepitiostane
* Ormeloxifene
* Ospemifene
* Raloxifene
* Tamoxifen#
* Toremifene

* Exclusively antagonistic: Fulvestrant

|

Aromatase inhibitors|

* First-generation: Aminoglutethimide
* Testolactone

* Second-generation: Fadrozole
* Formestane

* Third-generation: Anastrozole
* Exemestane
* Letrozole

Antigonadotropins|

* Androgens/Anabolic steroid|Anabolic steroid|Anabolic steroid]]]]s (e.g., testosterone, testosterone esters, nandrolone esters, oxandrolone, fluoxymesterone)
* D2 receptor antagonists (prolactin releasers) (e.g., domperidone, metoclopramide, risperidone, haloperidol, chlorpromazine, sulpiride)
* GnRH agonists (e.g., leuprorelin, goserelin)
* GnRH antagonists (e.g., cetrorelix, elagolix)
* Progestogens (e.g., chlormadinone acetate, cyproterone acetate, gestonorone caproate, hydroxyprogesterone caproate, [[Chemistry:Medroxyprogesterone medroxyprogesterone acetate, Chemistry:Megestrol acetate|megestrol acetate]])

Others|

* Mixed mechanism of action: Danazol
* Gestrinone

* Androstenedione immunogens: Androvax (androstenedione albumin)
* Ovandrotone albumin (Fecundin)

* #WHO-EM
* ‡Withdrawn from market
* Clinical trials:
* †Phase III
* §Never to phase III

See also
Estrogen receptor modulators
Androgens and antiandrogens
Progestogens and antiprogestogens
List of estrogens

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*[ER]: Estrogen receptor
*[GnRH]: gonadotropin-releasing hormone
*[FSH]: follicle-stimulating hormone
*[LH]: luteinizing hormone
*[SERMs]: selective estrogen receptor modulators
*[SERDs]: selective estrogen receptor downregulators