Severe vasomotor symptoms

DrugDrug NameDrug Description
DB06401BazedoxifeneBazedoxifene is a third generation selective estrogen receptor modulator (SERM), developed by Pfizer following the completion of their takeover of Wyeth Pharmaceuticals. In late 2013, Pfizer received approval for bazedoxifene as part of the combination drug DUAVEE in the prevention (not treatment) of postmenopausal osteoporosis. It is approved in the European Union (marketed in Italy and Spain) and Japan as monotherapy. In 2013, the combination product containing conjugated estrogens and bazedoxifene was approved by the FDA for the treatment of moderate to severe vasomotor symptoms associated with menopause, as well as the prevention of postmenopausal osteoporosis in women.
DB09381Estrogens, esterifiedEsterified estrogens contain a mixture of estrogenic substances; the principle component is estrone. Preparations contain 75% to 85% sodium estrone sulfate and 6% to 15% sodium equilin sulfate such that the total is not <90%. Esterified estrogens are a man-made mixture of estrogens that are used to treat symptoms of menopause such as hot flashes, vaginal dryness, vaginal burning or irritation, or other hormonal changes in the vagina. It is being also for the prevention and treatment of osteoporosis.
DB04574Estrone sulfateEstrone sulfate (as estropipate) is a form of estrogen. It has several uses such as: alleviate symptoms of menopause as hormone replacement therapy, treatment some types of infertility, treatment of some conditions leading to underdevelopment of female sexual characteristics, treatment of vaginal atrophy, treatment of some types of breast cancer (particularly in men and postmenopausal women), treatment of prostate cancer and prevention of osteoporosis.
DB00977EthinylestradiolA semisynthetic alkylated estradiol with a 17-alpha-ethinyl substitution. It has high estrogenic potency when administered orally and is often used as the estrogenic component in oral contraceptives. Ethinyl estradiol is marketed mostly as a combination oral contraceptive under several brand names such as Alesse, Tri-Cyclen, Triphasil, and Yasmin. The FDA label includes a black box warning that states that combination oral contraceptives should not be used in women over 35 years old who smoke due to the increased risk of serious cardiovascular side effects.
DB00367LevonorgestrelLevonorgestrel (LNG) is a synthetic progestogen similar to [Progesterone] used in contraception and hormone therapy.[A181988,T659] Also known as Plan B, it is used as a single agent in emergency contraception, and as a hormonal contraceptive released from an intrauterine device, commonly referred to as an IUD. Some of these devices are known as Jaydess, Kyleena, and Mirena. A subdermal implant of levonorgestrel that slowly releases the hormone over a long-term period is also available.[L7823] In addition to the above uses, levonorgestrel is used as a component of long-term combination contraceptives.[A181991,L7760,L7778] Globally, levonorgestrel is the most commonly used emergency contraceptive. It was initially granted FDA approval in 1982 and was the first emergency contraceptive containing only progesterone, showing high levels of efficacy and a lack of estrogenic adverse effects when compared to older emergency contraceptive regimens.[A181976,A181994,L7760]
DB00957NorgestimateNorgestimate is a form of progesterone, which is a female hormone important for the regulation of ovulation and menstruation. Norgestimate is used with estradiol to treat the symptoms of menopause.
DB09317Synthetic Conjugated Estrogens, ASynthetic conjugated estrogens A are composed of a blend of the following nine synthetic estrogenic substances: estrone sulfate, sodium equilin sulfate, sodium 17α-dihydroequilin sulfate, sodium 17α-estradiol sulfate, sodium 17β­ dihydroequilin sulfate, sodium 17α-dihydroequilenin sulfate, sodium 17β-dihydroequilenin sulfate, sodium equilenin sulfate, and sodium 17β-estradiol sulfate. This blend of nine estrogen derivatives are plant-derived forms of endogenous estrogens and contain many of the same compounds as the Conjugated Equine Estrogens (CEEs), although they are not considered to be equivalent. Available as the product Enjuvia (FDA), this combination of plant-derived estrogenic compounds is indicated for the treatment of moderate to severe vasomotor symptoms and vulvovaginal atrophy associated with menopause. All estrogen products mimic the effects of endogenous estrogens in the body which are responsible for the development and maintenance of the female reproductive system and secondary sexual characteristics. Estrogens act by binding to estrogen receptors on a wide variety of tissues in the body and modulating the pituitary secretion of the gonadotropins, luteinizing hormone (LH) and follicle stimulating hormone (FSH) through a negative feedback mechanism. Prior to menopause, the primary source of estrogen is the ovarian follicle, which secretes 70-500 micrograms of estradiol daily, depending on the phase of the menstrual cycle. However, once a woman stops ovulating there is a sharp decline in the production of progesterone and estradiol by the ovaries and a consequent fluctuation in LH and FSH due to a lack of feedback control. This shift in hormone production is largely responsible for many of the symptoms experienced during and after menopause and includes hot flashes and other vasomotor symptoms, painful intercourse, vaginal dryness, and vulvovaginal atrophy. These symptoms are able to be reduced by replacing many of the hormones lost during and following menopause with synthetic or naturally occurring forms, in a therapy known as Hormone Replacement Therapy (HRT). Pharmacologic estrogen products are available in a variety of formats. Although many of them contain several compounds in common (such as the estrogen derivatives sodium estrone sulfate and sodium equilin sulfate), they vary by their original source (such as horse-, human-, or plant-derived), and the remaining mixture of estrogenic derivatives. Conjugated Equine Estrogens (CEEs) are derived from the urine of pregnant mares and contain a blend of at least 10 estrogen derivatives. Marketed under the brand name Premarin, CEEs are the most frequently used form of conjugated estrogens. There is currently no generic form of CEEs available as a detailed analytical characterization of the active ingredients or of their estrogenic activity is not available at this time. Conjugated estrogens are also available in a plant-derived synthetic form that replicates the naturally occurring, horse-derived forms. Available as either "Synthetic Conjugated Estrogens, A" containing 9 estrogen derivatives (available as Cenestin) or as "Synthetic Conjugated Estrogens, B" containing 10 estrogen derivatives (available as Enjuvia), these products are isolated as precursors from yam or soy plants and then chemically modified to mimic the products available in their naturally occurring form.
DB09318Synthetic Conjugated Estrogens, BSynthetic conjugated estrogens, B tablets contain a blend of ten synthetic estrogenic substances. The estrogenic substances are: sodium estrone sulfate, sodium equilin sulfate, sodium 17α-dihydroequilin sulfate, sodium 17α-estradiol sulfate, sodium 17β­ dihydroequilin sulfate, sodium 17α-dihydroequilenin sulfate, sodium 17β-dihydroequilenin sulfate, sodium equilenin sulfate, sodium 17β-estradiol sulfate, and sodium Δ8,9-dehydroestrone sulfate. This blend of ten estrogen derivatives are plant-derived forms of endogenous estrogens and contain many of the same compounds as the Conjugated Equine Estrogens (CEEs), although they are not considered to be equivalent. Available as the product Cenestin (FDA), this combination of plant-derived estrogenic compounds is indicated for the treatment of moderate to severe vasomotor symptoms, vulvovaginal atrophy, vaginal dryness, and paint with intercourse associated with menopause. All estrogen products mimic the effects of endogenous estrogens in the body which are responsible for the development and maintenance of the female reproductive system and secondary sexual characteristics. Estrogens act by binding to estrogen receptors on a wide variety of tissues in the body and modulating the pituitary secretion of the gonadotropins, luteinizing hormone (LH) and follicle stimulating hormone (FSH) through a negative feedback mechanism. Prior to menopause, the primary source of estrogen is the ovarian follicle, which secretes 70-500 micrograms of estradiol daily, depending on the phase of the menstrual cycle. However, once a woman stops ovulating there is a sharp decline in the production of progesterone and estradiol by the ovaries and a consequent fluctuation in LH and FSH due to a lack of feedback control. This shift in hormone production is largely responsible for many of the symptoms experienced during and after menopause and includes hot flashes and other vasomotor symptoms, painful intercourse, vaginal dryness, and vulvovaginal atrophy. These symptoms are able to be reduced by replacing many of the hormones lost during and following menopause with synthetic or naturally occurring forms, in a therapy known as Hormone Replacement Therapy (HRT). Pharmacologic estrogen products are available in a variety of formats. Although many of them contain several compounds in common (such as the estrogen derivatives sodium estrone sulfate and sodium equilin sulfate), they vary by their original source (such as horse-, human-, or plant-derived), and the remaining mixture of estrogenic derivatives. Conjugated Equine Estrogens (CEEs) are derived from the urine of pregnant mares and contain a blend of at least 10 estrogen derivatives. Marketed under the brand name Premarin, CEEs are the most frequently used form of conjugated estrogens. There is currently no generic form of CEEs available as a detailed analytical characterization of the active ingredients or of their estrogenic activity is not available at this time. Conjugated estrogens are also available in a plant-derived synthetic form that replicates the naturally occurring, horse-derived forms. Available as either "Synthetic Conjugated Estrogens, A" containing 9 estrogen derivatives (available as Cenestin) or as "Synthetic Conjugated Estrogens, B" containing 10 estrogen derivatives (available as Enjuvia), these products are isolated as precursors from yam or soy plants and then chemically modified to mimic the products available in their naturally occurring form.
DrugDrug NameTargetType
DB06401BazedoxifeneEstrogen receptor alphatarget
DB06401BazedoxifeneUDP-glucuronosyltransferase 1-4enzyme
DB06401BazedoxifeneEstrogen receptor betatarget
DB06401BazedoxifeneUDP-glucuronosyltransferase 1-8enzyme
DB06401BazedoxifeneUDP-glucuronosyltransferase 1-10enzyme
DB09381Estrogens, esterifiedCytochrome P450 3A4enzyme
DB09381Estrogens, esterifiedThyroxine-binding globulincarrier
DB04574Estrone sulfateCytochrome P450 1A2enzyme
DB04574Estrone sulfateCytochrome P450 3A4enzyme
DB04574Estrone sulfateEstrogen receptor alphatarget
DB04574Estrone sulfateEstrogen receptor betatarget
DB04574Estrone sulfateSex hormone-binding globulincarrier
DB04574Estrone sulfateSerum albumincarrier
DB04574Estrone sulfateCytochrome P450 2C9enzyme
DB04574Estrone sulfateMultidrug and toxin extrusion protein 1transporter
DB04574Estrone sulfateMultidrug and toxin extrusion protein 2transporter
DB00977EthinylestradiolEstrogen receptor alphatarget
DB00977EthinylestradiolNuclear receptor subfamily 1 group I member 2target
DB00977EthinylestradiolCytochrome P450 3A4enzyme
DB00977EthinylestradiolCytochrome P450 2C8enzyme
DB00977EthinylestradiolBile salt export pumptransporter
DB00977EthinylestradiolSodium/bile acid cotransportertransporter
DB00977EthinylestradiolCanalicular multispecific organic anion transporter 1transporter
DB00977EthinylestradiolP-glycoprotein 1transporter
DB00977EthinylestradiolSex hormone-binding globulintarget
DB00977EthinylestradiolUDP-glucuronosyltransferase 1-1enzyme
DB00977EthinylestradiolCytochrome P450 2C19enzyme
DB00367LevonorgestrelProgesterone receptortarget
DB00367LevonorgestrelEstrogen receptor alphatarget
DB00367Levonorgestrel3-oxo-5-alpha-steroid 4-dehydrogenase 1target
DB00367LevonorgestrelCytochrome P450 3A4enzyme
DB00367LevonorgestrelAndrogen receptortarget
DB00367LevonorgestrelSex hormone-binding globulintarget
DB00367LevonorgestrelGlucocorticoid receptortarget
DB00367LevonorgestrelCytochrome P450 3A5enzyme
DB00957NorgestimateProgesterone receptortarget
DB00957NorgestimateEstrogen receptor alphatarget
DB00957NorgestimateCanalicular multispecific organic anion transporter 1transporter
DB00957NorgestimateCytochrome P450 3A4enzyme
DB00957NorgestimateAndrogen receptortarget
DB09317Synthetic Conjugated Estrogens, ACytochrome P450 3A4enzyme
DB09317Synthetic Conjugated Estrogens, AEstrogen receptor alphatarget
DB09317Synthetic Conjugated Estrogens, AThyroxine-binding globulincarrier
DB09318Synthetic Conjugated Estrogens, BEstrogen receptor alphatarget
DB09318Synthetic Conjugated Estrogens, BCytochrome P450 3A4enzyme
DB09318Synthetic Conjugated Estrogens, BThyroxine-binding globulincarrier
DrugDrug NamePhaseStatusCount