Women's Health

Estradiol is the principal intracellular human estrogen and is substantially more active than its metabolites, estrone and estriol, at the cellular level. Estradiol can be obtained from natural sources or prepared synthetically. There is no evidence that ‘natural’ estrogens are more or less efficacious or safe than ‘synthetic’ estrogens. Due to almost complete first-pass metabolism, estradiol must be given in a micronized oral dosage form to ensure the therapeutic effect. Esterification of estradiol to estradiol cypionate or valerate increases the parenteral duration of action of estradiol to allow for parenteral intramuscular administration. Estradiol is primarily used to prevent osteoporosis and relieve vasomotor and genitourinary symptoms associated with menopause (natural or surgical), for postmenopausal osteoporosis prevention, and is also used to treat female hypogonadism and other abnormalities of female gonadotropin dysfunction. Various estrogen products have been marketed in the U.S. since 1938. Estradiol is available in many dosage forms, including oral tablets, transdermal systems, topical emulsions, topical gels, topical sprays, vaginal creams, vaginal rings, and parenteral depot injections. Vaginal therapies are preferred in postmenopausal women with exclusive genitourinary symptoms, due to lower systemic absorption/exposure with most of these dosage forms. Many estradiol products have been FDA-approved since the 1990’s, in accordance with the FDA’s guidance to provide efficacious low-dose estrogen therapies in alternate drug delivery systems.

Estradiol is the principal intracellular human estrogen and is substantially more active than its metabolites, estrone, and estriol, at the cellular level. Estradiol can be obtained from natural sources or prepared synthetically. There is no evidence that ‘natural’ estrogens are more or less efficacious or safe than ‘synthetic’ estrogens. Due to almost complete first-pass metabolism, estradiol must be given in a micronized oral dosage form to ensure the therapeutic effect. Esterification of estradiol to estradiol cypionate or valerate increases the parenteral duration of action of estradiol to allow for parenteral intramuscular administration. Estradiol is primarily used to prevent osteoporosis and relieve vasomotor and genitourinary symptoms associated with menopause (natural or surgical), for postmenopausal osteoporosis prevention, and is also used to treat female hypogonadism and other abnormalities of female gonadotropin dysfunction. Various estrogen products have been marketed in the U.S. since 1938. Estradiol is available in many dosage forms, including oral tablets, transdermal systems, topical emulsions, topical gels, topical sprays, vaginal creams, vaginal rings, and parenteral depot injections. Vaginal therapies are preferred in postmenopausal women with exclusive genitourinary symptoms, due to lower systemic absorption/exposure with most of these dosage forms. Many estradiol products have been FDA-approved since the 1990’s, in accordance with the FDA’s guidance to provide efficacious low-dose estrogen therapies in alternate drug delivery systems.

Progesterone is one of several primary hormones in women that play a key role in the maintenance of pregnancy. After the rupture of the ovarian follicle and release of the ovum within the female ovary, progesterone is secreted by mature granulosa cells known as the corpus luteum. The released progesterone causes a thickening of the endometrial wall of the uterus, preparing it for the implantation of a fertilized ovum. If fertilization and implantation do not occur, the corpus luteum eventually atrophies and the serum progesterone levels fall. However, if implantation does occur, the serum progesterone levels remain elevated throughout the duration of the pregnancy as the placenta takes over the role of progesterone production.

Testosterone is the primary androgen found in the body. Endogenous testosterone is synthesized by cells in the testis, ovary, and adrenal cortex. Therapeutically, testosterone is used in the management of hypogonadism, either congenital or acquired. Testosterone is also the most effective exogenous androgen for the palliative treatment of carcinoma of the breast in postmenopausal women. Testosterone was in use in 1938 and approved by the FDA in 1939. Anabolic steroids, derivatives of testosterone, have been used illicitly and are now controlled substances. Testosterone, like many anabolic steroids, was classified as a controlled substance in 1991. Developed in the United States by Uniumed Pharmaceuticals as AndroGel, testosterone cream was FDA approved in 2000 for the treatment of testosterone deficiency, which often results in a variety of hypogonadic conditions from mood and energy to sexual dysfunctions, as well as a treatment for several injury-related conditions like those experienced by severe burn and accident victims. A very popular form of testosterone, AndroGel is sold around the world under a couple of less popular brand/trade names most notably Testogel (manufactured in the UK by Laboratoires Besins and distributed by Bayer), Testim (manufactured in the U.S. by Auxilium Pharmaceuticals, Inc.), and various generic versions often sold under the name testosterone cream or gel.

The transdermal delivery system of testosterone cream targets the same, or at least very similar bodily regions as injections and other forms of testosterone. More specifically, maximum absorption of testosterone cream is achieved when (as with injectable testosterone) it’s administered to densely muscled bodily regions. Since greater amounts of muscle at the point of application equates to a higher number of testosterone absorbing capillaries, testosterone can be more rapidly shuttled into the bloodstream.

Testosterone is the primary androgen found in the body. Endogenous testosterone is synthesized by cells in the testis, ovary, and adrenal cortex. Therapeutically, testosterone is used in the management of hypogonadism, either congenital or acquired. Testosterone is also the most effective exogenous androgen for the palliative treatment of carcinoma of the breast in postmenopausal women. Testosterone was in use in 1938 and approved by the FDA in 1939. Anabolic steroids, derivatives of testosterone, have been used illicitly and are now controlled substances. Testosterone, like many anabolic steroids, was classified as a controlled substance in 1991. Developed in the United States by Uniumed Pharmaceuticals as AndroGel, testosterone cream was FDA approved in 2000 for the treatment of testosterone deficiency, which often results in a variety of hypogonadic conditions from mood and energy to sexual dysfunctions, as well as a treatment for several injury-related conditions like those experienced by severe burn and accident victims. A very popular form of testosterone, AndroGel is sold around the world under a couple of less popular brand/trade names most notably Testogel (manufactured in the UK by Laboratoires Besins and distributed by Bayer), Testim (manufactured in the U.S. by Auxilium Pharmaceuticals, Inc.), and various generic versions often sold under the name testosterone cream or gel.

The transdermal delivery system of testosterone cream targets the same, or at least very similar bodily regions as injections and other forms of testosterone. More specifically, maximum absorption of testosterone cream is achieved when (as with injectable testosterone) it’s administered to densely muscled bodily regions. Since greater amounts of muscle at the point of application equates to a higher number of testosterone absorbing capillaries, testosterone can be more rapidly shuttled into the bloodstream.

Progesterone is a naturally occurring progestin. In the body, it is synthesized in the ovaries, testes, placenta, and adrenal cortex. Progesterone is primarily used to treat amenorrhea, abnormal uterine bleeding, or as a contraceptive. Progesterone is also used to prevent early pregnancy failure in women with corpus luteum insufficiency, including women undergoing assisted reproductive technology (ART). Additionally, the use of progesterone for preterm delivery prophylaxis is being investigated. Preliminary data indicate that progesterone may be effective in preventing preterm delivery in high-risk women, especially those with a history of preterm delivery; however, the optimal dosage and route have not been determined. The American College of Obstetricians and Gynecologists (ACOG) Committee recommends that if progesterone is to be used for the prevention of preterm delivery, it should only be used in women with a history of spontaneous birth at < 37 weeks gestation, until more data supporting its use in other high-risk women are available. A study in support of the use of vaginal progesterone in women with a short cervix has been published. Progesterone is available commercially as an intramuscular injection, an intravaginal gel, an intravaginal insert, oral capsules, or a powder for use in extemporaneous preparations (e.g., vaginal suppositories). A progesterone-releasing IUD (Progestasert®) that was inserted once yearly has been discontinued. Progesterone was approved by the FDA in 1939. In May 1998, micronized progesterone capsules for oral administration were approved for secondary amenorrhea; they received a second indication in December 1998 for the prevention of endometrial hyperplasia in postmenopausal women with an intact uterus taking estrogen replacement therapy. In May 1997, a progesterone vaginal gel (Crinone®) was approved for progesterone supplementation or replacement as part of an Assisted Reproductive Technology (ART) program for infertile women; a second intravaginal gel, Prochieve™, was released to the US market in 2002. A vaginal insert, Endometrin®, for progesterone supplementation as part of an ART program in infertile women was approved in June 2007.

Estradiol is the principal intracellular human estrogen and is substantially more active than its metabolites, estrone and estriol, at the cellular level. Estradiol can be obtained from natural sources or prepared synthetically. There is no evidence that ‘natural’ estrogens are more or less efficacious or safe than ‘synthetic’ estrogens. Due to almost complete first-pass metabolism, estradiol must be given in a micronized oral dosage form to ensure therapeutic effect. Esterification of estradiol to estradiol cypionate or valerate increases the parenteral duration of action of estradiol to allow for parenteral intramuscular administration. Estradiol is primarily used to prevent osteoporosis and relieve vasomotor and genitourinary symptoms associated with menopause (natural or surgical), for postmenopausal osteoporosis prevention, and is also used to treat female hypogonadism and other abnormalities of female gonadotropin dysfunction. Various estrogen products have been marketed in the U.S. since 1938. Estradiol is available in many dosage forms, including oral tablets, transdermal systems, topical emulsions, topical gels, topical sprays, vaginal creams, vaginal rings, and parenteral depot injections. Vaginal therapies are preferred in postmenopausal women with exclusive genitourinary symptoms, due to lower systemic absorption/exposure with most of these dosage forms. Many estradiol products have been FDA-approved since the 1990’s, in accordance with the FDA’s guidance to provide efficacious low-dose estrogen therapies in alternate drug delivery systems.

Progesterone is a naturally occurring progestin. In the body, it is synthesized in the ovaries, testes, placenta, and adrenal cortex. Progesterone is primarily used to treat amenorrhea, abnormal uterine bleeding, or as a contraceptive. Progesterone is also used to prevent early pregnancy failure in women with corpus luteum insufficiency, including women undergoing assisted reproductive technology (ART). Additionally, the use of progesterone for preterm delivery prophylaxis is being investigated. Preliminary data indicate that progesterone may be effective in preventing preterm delivery in high-risk women, especially those with a history of preterm delivery; however, the optimal dosage and route have not been determined. The American College of Obstetricians and Gynecologists (ACOG) Committee recommends that if progesterone is to be used for the prevention of preterm delivery, it should only be used in women with a history of spontaneous birth at < 37 weeks gestation, until more data supporting its use in other high-risk women are available. A study in support of the use of vaginal progesterone in women with a short cervix has been published. Progesterone is available commercially as an intramuscular injection, an intravaginal gel, an intravaginal insert, oral capsules, or a powder for use in extemporaneous preparations (e.g., vaginal suppositories). A progesterone-releasing IUD (Progestasert®) that was inserted once yearly has been discontinued. Progesterone was approved by the FDA in 1939. In May 1998, micronized progesterone capsules for oral administration were approved for secondary amenorrhea; they received a second indication in December 1998 for the prevention of endometrial hyperplasia in postmenopausal women with an intact uterus taking estrogen replacement therapy. In May 1997, a progesterone vaginal gel (Crinone®) was approved for progesterone supplementation or replacement as part of an Assisted Reproductive Technology (ART) program for infertile women; a second intravaginal gel, Prochieve™, was released to the US market in 2002. A vaginal insert, Endometrin®, for progesterone supplementation as part of an ART program in infertile women was approved in June 2007.