Combination of | |
---|---|
Estradiol benzoate | Estrogen |
Estradiol phenylpropionate | Estrogen |
Clinical data | |
Trade names | Dimenformon Prolongatum |
Other names | EB/EPP; Org 369-2 |
Routes of administration | Intramuscular injection |
Identifiers | |
CAS Number | |
PubChem CID | |
ChemSpider | |
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Estradiol benzoate/estradiol phenylpropionate (EB/EPP), sold under the brand name Dimenformon Prolongatum, is an injectable combination formulation of estradiol benzoate (EB), a shorter-acting estrogen, and estradiol phenylpropionate (EPP), a longer-acting estrogen, which has been used in menopausal hormone therapy for women in Europe but appears to no longer be available. [1] [2] [3] [4] It has also been used to suppress lactation in women and has been used in feminizing hormone therapy for transgender women. [5] [6] It has been provided in the form of 1 mL ampoules containing 2.5 mg EB and 10 mg EPP in oil solution and is administered by intramuscular injection at regular intervals. [2]
The pharmacokinetics of this formulation and its constituent components have been studied. [7] [8] [9] [10] [11] [12]
A combination of 12.5 mg EB and 10 mg EPP (developmental code name Org 369–2) has been studied for use in women as a postcoital contraceptive within 48 hours of unprotected sex. [13] [9] [14] [15] [16]
Estradiol valerate (EV), sold for use by mouth under the brand name Progynova and for use by injection under the brand names Delestrogen and Progynon Depot among others, is an estrogen medication. It is used in hormone therapy for menopausal symptoms and low estrogen levels, hormone therapy for transgender people, and in hormonal birth control. It is also used in the treatment of prostate cancer. The medication is taken by mouth or by injection into muscle or fat once every 1 to 4 weeks.
Norethisterone acetate (NETA), also known as norethindrone acetate and sold under the brand name Primolut-Nor among others, is a progestin medication which is used in birth control pills, menopausal hormone therapy, and for the treatment of gynecological disorders. The medication available in low-dose and high-dose formulations and is used alone or in combination with an estrogen. It is ingested orally.
Estradiol benzoate (EB), sold under the brand name Progynon-B among others, is an estrogen medication which is used in hormone therapy for menopausal symptoms and low estrogen levels in women, in hormone therapy for transgender women, and in the treatment of gynecological disorders. It is also used in the treatment of prostate cancer in men. Estradiol benzoate is used in veterinary medicine as well. When used clinically, the medication is given by injection into muscle usually two to three times per week.
Estradiol cypionate (EC), sold under the brand name Depo-Estradiol among others, is an estrogen medication which is used in hormone therapy for menopausal symptoms and low estrogen levels in women, in hormone therapy for trans women, and in hormonal birth control for women. It is given by injection into muscle once every 1 to 4 weeks.
Estradiol undecylate, also known as estradiol undecanoate and formerly sold under the brand names Delestrec and Progynon Depot 100 among others, is an estrogen medication which has been used in the treatment of prostate cancer in men. It has also been used as a part of hormone therapy for transgender women. Although estradiol undecylate has been used in the past, it was discontinued .The medication has been given by injection into muscle usually once a month.
Estradiol dipropionate (EDP), sold under the brand names Agofollin, Di-Ovocylin, and Progynon DP among others, is an estrogen medication which has been used in hormone therapy for menopausal symptoms and low estrogen levels in women and in the treatment of gynecological disorders. It has also been used in feminizing hormone therapy for transgender women and in the treatment of prostate cancer in men. Although widely used in the past, estradiol dipropionate has largely been discontinued and is mostly no longer available today. It appears to remain in use only in Japan, Macedonia, and Australia. Estradiol dipropionate is given by injection into muscle at intervals ranging from once or twice a week to once every week and a half to two weeks.
Estradiol hexahydrobenzoate (EHHB), sold under a number of brand names including Benzo-Ginoestril A.P., BenzoGynoestryl Retard, Ginestryl-15-Depot, Menodin, and Tardoginestryl, is an estrogen medication which was previously used for indications such as menopausal hormone therapy and gynecological disorders. EHHB is given by injection into muscle at regular intervals, for instance once every few weeks.
Estradiol phenylpropionate (EPP), also known as estradiol 17β-phenylpropionate and sold under the brand name Menformon Prolongatum, is an estrogen which is no longer marketed. It is an estrogen ester, specifically the C17β phenylpropionate ester of estradiol.
Estradiol dienanthate (EDE), sold under the brand names Climacteron among others, is a long-acting estrogen medication which was previously used in menopausal hormone therapy for women and to suppress lactation in women. It was formulated in combination with estradiol benzoate (EB), a short-acting estrogen, and testosterone enanthate benzilic acid hydrazone (TEBH), a long-acting androgen/anabolic steroid. EDE has not been made available for medical use alone. The medication, in combination with EB and TEBH, was given by injection into muscle once or at regular intervals, for instance once every 6 weeks.
Estradiol benzoate butyrate (EBB), sold under the brand names Neolutin N, Redimen, Soluna, and Unijab and formerly known under the developmental code name Unimens, is an estrogen medication which is used in hormonal birth control for women. It is formulated in combination with dihydroxyprogesterone acetophenide, a progestin, and is used specifically as a combined injectable contraceptive. EBB is not available for medical use alone. The medication, in combination with DHPA, is given by injection into muscle once a month.
Estradiol (E2) is a medication and naturally occurring steroid hormone. It is an estrogen and is used mainly in menopausal hormone therapy and to treat low sex hormone levels in women. It is also used in hormonal birth control for women, in feminizing hormone therapy for transgender women, and in the treatment of hormone-sensitive cancers like prostate cancer in men and breast cancer in women, among other uses. Estradiol can be taken by mouth, held and dissolved under the tongue, as a gel or patch that is applied to the skin, in through the vagina, by injection into muscle or fat, or through the use of an implant that is placed into fat, among other routes.
The pharmacology of estradiol, an estrogen medication and naturally occurring steroid hormone, concerns its pharmacodynamics, pharmacokinetics, and various routes of administration.
The pharmacology of estradiol, an estrogen medication and naturally occurring steroid hormone, concerns its pharmacodynamics, pharmacokinetics, and various routes of administration.
Estradiol benzoate/progesterone (EB/P4), sold under the brand names Duogynon and Sistocyclin among others, is a combination medication of estradiol benzoate (EB), an estrogen, and progesterone (P4), a progestogen. It has been formulated both as short-acting oil solutions and long-acting microcrystalline aqueous suspensions and is given by injection into muscle either once or continuously at regular intervals.
Estradiol benzoate/testosterone isobutyrate (EB/TiB), sold under the brand names Femandren M and Folivirin, is an injectable combination medication of estradiol benzoate (EB), an estrogen, and testosterone isobutyrate (TiB), an androgen/anabolic steroid, which is used in menopausal hormone therapy for women. It is provided in the form of 1 mL ampoules containing 2.5 mg estradiol benzoate and 25 mg testosterone isobutyrate in a microcrystalline aqueous suspension and is administered by intramuscular injection once every 4 to 6 weeks. EB/TiB reportedly has a duration of about 14 to 21 days.
Estradiol benzoate/estradiol dienanthate/testosterone enanthate benzilic acid hydrazone (EB/EDE/TEBH), sold under the brand names Climacteron, Lactimex, Lactostat, and Amenose, is an injectable combination medication of estradiol benzoate (EB), an estrogen, estradiol dienanthate (EDE), an estrogen, and testosterone enanthate benzilic acid hydrazone (TEBH), an androgen/anabolic steroid, which is used in menopausal hormone therapy for peri- and postmenopausal women and to suppress lactation in postpartum women. Clinical studies have assessed this formulation.
Estradiol benzoate/estradiol phenylpropionate/testosterone propionate/testosterone phenylpropionate/testosterone isocaproate (EB/EPP/TP/TPP/TiC), sold under the brand names Estandron Prolongatum, Lynandron Prolongatum, and Mixogen, was an injectable combination medication of the estrogens estradiol benzoate (EB) and estradiol phenylpropionate (EPP) and the androgens/anabolic steroids testosterone propionate (TP), testosterone phenylpropionate (TPP), and testosterone isocaproate (TiC) which was used in menopausal hormone therapy for women. It was also used to suppress lactation in postpartum women.
Estradiol/estradiol enanthate (E2/E2-EN) is an injectable combination formulation of estradiol (E2), a short-acting estrogen, and estradiol enanthate (E2-EN), a long-acting estrogen, which was developed by Boehringer around 1960 for potential medical use but was never marketed. It contained 1 mg E2 and 9 mg E2-EN in oil solution and was intended for administration by intramuscular injection.
Estradiol benzoate/estradiol valerate/norethisterone acetate/testosterone enanthate (EB/EV/NETA/TE), sold under the brand name Ablacton, is an injectable combination medication of estradiol benzoate (EB), an estrogen, estradiol valerate (EV), an estrogen, norethisterone acetate (NETA), a progestin, and testosterone enanthate (TE), an androgen/anabolic steroid, which has been used to suppress lactation in women. It contains 5 mg EB, 8 mg EV, 20 mg NETA, and 180 mg TE in oil solution and is provided in the form of ampoules. It is given as a single intramuscular injection following childbirth. The medication was manufactured by Schering and was previously marketed in Italy and Spain, but is no longer available.
Estradiol benzoate/progesterone/testosterone propionate (EB/P4/TP), sold under the brand names Lukestra, Steratrin, Trihormonal, and Trinestryl, is an injectable combination medication of estradiol benzoate (EB), an estrogen, progesterone (P4), a progestogen, and testosterone propionate (TP), an androgen/anabolic steroid. It contained 1 to 3 mg EB, 20 to 25 mg P4, and 25 mg TP, was provided in the form of ampoules, and was administered by intramuscular injection. The medication was introduced by 1949 and was marketed in the United States, the United Kingdom, and Germany among other places. It is no longer available.
Table 2.2 Guidelines on hormone therapy [...] Presurgical A.2.: Induction of designated sex characteristics [...] estradiol benzoate, estradiol phenylpropionate (25 mg/2 weeks) [...]
A combination of 12.5 mg estradiol benzoate and 10 mg estradiol phenylpropionate was used for postcoital contraception in 60 women. Treatment occurred within 48 hours of unprotected coitus in almost all cases, and generally between the 10th and 18th days of the cycle. Plasma luteinizing hormone, follicle-stimulating hormone, prolactin, estradiol, and progesterone were determined before and 8 days after treatment, and after the following menstruation. Few side effects were observed. Cycle length and duration of menstruation were not greatly changed. In 7 women plasma progesterone levels were above 5 ng/ml before treatment, while in 35 others they were below 1 ng. In about one-third of the women, plasma progesterone was below 1 ng/ml in both determinations, indicating anovulatory cycles. It is impossible to determine whether the estrogen medication was responsible for these. Since 3 pregnancies were observed in the group, the effectiveness of this treatment is questionable.
With respect to morning-after injection, 150 volunteers given 12.5 mg estradiol benzoate and 10 mg of estradiol phenylpropionate exhibited very low frequency of side effects; however, 4 pregnancies, considered to be method-failures, were observed. Endometrial biopsy and histological examination showed pronounced local epithelial proliferation in 3 cases. Recordings of post-ovulatory basal body temperature showed a consistent pattern, possibly due to the low dosage used. These results suggest immediate treatment with the indicated dosage levels after unprotected intercourse may be effective especially in emergency cases such as failure of other contraceptive methods, unexpected intercourse and rape.