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 | |
UNII |
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]
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.
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 | |
UNII |
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]
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.