| Route | Dose (mg) |
Time measured |
Δ
E2 levels (pg/mL) |
Δ
E1 levels (pg/mL) |
E2:E1 ratio |
Ref | |||
|---|---|---|---|---|---|---|---|---|---|
|
Oral |
1 2 4 |
12 h 3 h 6 h |
+25 +40 +50 |
+150 +250 +500 |
0.15 0.16 0.10 |
[1] [1] [1] | |||
|
Sublingual |
1 0.5 0.5 0.5 |
1 h 1 h 1 h 1 h |
+450 +250 +750 +75 |
+160 +85 +250 +24 |
3 3 3 3 |
[2] [2] [3] [4] | |||
| Intranasal | 1 | 1 h | +110 | +110 | 1.0 | [5] | |||
|
Topical (
gel) |
3 3/d 3/2 d |
5 h 12–20 h 12 h 36 h |
+70 +45–279 +300–1310 +20–179 |
+50 +31–230 +24–110 +120–500 |
0.4 1 1 1 |
[6] [7] [7] [7] | |||
| Vaginal ( cream) | 0.5 1.0 |
3 h 3 h |
+830 +800 |
+150 +150 |
5.0 5.0 |
[8] [5] | |||
| Rectal | 1 | 3 h | +620 | +120 | 5.0 | [9] | |||
|
Intramuscular inj. ( oil soln.) |
EB: 5 EV: 5 EC: 5 EU: 100 PEP: 320 |
1.8, 2.4 da 2.2, 2.7 da 3.9, 5.1 da 1 d 16, 25 da |
940b 667b 338b 500b 270b |
343b 324b 145b ND 1000b |
2.7 2.1 2.3 ND 0.27 |
[10] [10] [10] [11] [12] | |||
| Intravenous inj. | 0.3 | 5 min | 8321b | 960b | 8.7 | [13] | |||
| Footnotes: a = Tmax for E2, E1 levels. b = Actual levels (not change). Sources: Main: [14] | |||||||||
See also
References
- ^ a b c Dada OA, Laumas V, Landgren BM, Cekan SZ, Diczfalusy E (1978). "Effect of graded oral doses of oestradiol on circulating hormonal levels". Acta Endocrinol. 88 (4): 754–67. doi: 10.1530/acta.0.0880754. PMID 581116.
- ^ a b Price TM, Blauer KL, Hansen M, Stanczyk F, Lobo R, Bates GW (March 1997). "Single-dose pharmacokinetics of sublingual versus oral administration of micronized 17 beta-estradiol". Obstet Gynecol. 89 (3): 340–5. doi: 10.1016/S0029-7844(96)00513-3. PMID 9052581.
- ^ Burnier AM, Martin PL, Yen SS, Brooks P (May 1981). "Sublingual absorption of micronized 17beta-estradiol". Am. J. Obstet. Gynecol. 140 (2): 146–50. doi: 10.1016/0002-9378(81)90101-0. PMID 6786097.
- ^ Fiet J, Hermano M, Witte J, Villette JM, Haimart M, Gourmel B, Tabuteau F, Rouffy J, Dreux C (September 1982). "Post-menopausal concentrations of plasma oestradiol, oestrone, FSH and LH and of total urinary oestradiol and oestrone after a single sublingual dose of oestradiol-17 beta". Acta Endocrinol. 101 (1): 93–7. doi: 10.1530/acta.0.1010093. PMID 6812348.
- ^ a b Rigg LA, Milanes B, Villanueva B, Yen SS (1977). "Efficacy of intravaginal and intranasal administration of micronized estradiol-17beta". J. Clin. Endocrinol. Metab. 45 (6): 1261–4. doi: 10.1210/jcem-45-6-1261. PMID 591620.
- ^ Strecker JR, Lauritzen C, Goessens L (1979). "Plasma concentrations of unconjugated and conjugated estrogens and gonadotrophins following application of various estrogen preparations after oophorectomy and in the menopause". Maturitas. 1 (3): 183–90. PMID 228157.
- ^ a b c Whitehead MI, Townsend PT, Kitchin Y, Dyer G, Iqbal MJ, Mansfield MD, et al. (1980). "Plasma steroid and protein hormone profiles in postmenopausal women following topical administration of oestradiol 17β". In Mauvais-Jarvis P (ed.). Percutaneous Absorption of Steroids. Academic Press. p. 231.
- ^ Schiff I, Tulchinsky D, Ryan KJ (1977). "Vaginal absorption of estrone and 17beta-estradiol". Fertil. Steril. 28 (10): 1063–6. doi: 10.1016/S0015-0282(16)42855-4. PMID 908445.
- ^ Lauritzen C (December 1986). "Die Behandlung der klimakterischen Beschwerden durch vaginale, rektale und transdermale Ostrogensubstitution" [Treatment of disorders of the climacteric by vaginal, rectal and transdermal estrogen substitution]. Gynakologe (in German). 19 (4): 248–53. ISSN 0017-5994. PMID 3817597.
- ^ a b c Oriowo MA, Landgren BM, Stenström B, Diczfalusy E (April 1980). "A comparison of the pharmacokinetic properties of three estradiol esters". Contraception. 21 (4): 415–24. doi: 10.1016/S0010-7824(80)80018-7. PMID 7389356.
- ^ Vermeulen A (1975). "Longacting steroid preparations". Acta Clin Belg. 30 (1): 48–55. doi: 10.1080/17843286.1975.11716973. PMID 1231448.
- ^ Stege R, Gunnarsson PO, Johansson CJ, Olsson P, Pousette A, Carlström K (May 1996). "Pharmacokinetics and testosterone suppression of a single dose of polyestradiol phosphate (Estradurin) in prostatic cancer patients". Prostate. 28 (5): 307–10. doi: 10.1002/(SICI)1097-0045(199605)28:5<307::AID-PROS6>3.0.CO;2-8. PMID 8610057.
- ^ Kuhnz W, Gansau C, Mahler M (September 1993). "Pharmacokinetics of estradiol, free and total estrone, in young women following single intravenous and oral administration of 17β-estradiol". Arzneimittelforschung. 43 (9): 966–73. ISSN 0004-4172. PMID 8240460.
- ^ Nichols KC, Schenkel L, Benson H (1984). "17 beta-estradiol for postmenopausal estrogen replacement therapy". Obstet Gynecol Surv. 39 (4): 230–45. doi: 10.1097/00006254-198404000-00022. PMID 6717863.
| Route | Dose (mg) |
Time measured |
Δ
E2 levels (pg/mL) |
Δ
E1 levels (pg/mL) |
E2:E1 ratio |
Ref | |||
|---|---|---|---|---|---|---|---|---|---|
|
Oral |
1 2 4 |
12 h 3 h 6 h |
+25 +40 +50 |
+150 +250 +500 |
0.15 0.16 0.10 |
[1] [1] [1] | |||
|
Sublingual |
1 0.5 0.5 0.5 |
1 h 1 h 1 h 1 h |
+450 +250 +750 +75 |
+160 +85 +250 +24 |
3 3 3 3 |
[2] [2] [3] [4] | |||
| Intranasal | 1 | 1 h | +110 | +110 | 1.0 | [5] | |||
|
Topical (
gel) |
3 3/d 3/2 d |
5 h 12–20 h 12 h 36 h |
+70 +45–279 +300–1310 +20–179 |
+50 +31–230 +24–110 +120–500 |
0.4 1 1 1 |
[6] [7] [7] [7] | |||
| Vaginal ( cream) | 0.5 1.0 |
3 h 3 h |
+830 +800 |
+150 +150 |
5.0 5.0 |
[8] [5] | |||
| Rectal | 1 | 3 h | +620 | +120 | 5.0 | [9] | |||
|
Intramuscular inj. ( oil soln.) |
EB: 5 EV: 5 EC: 5 EU: 100 PEP: 320 |
1.8, 2.4 da 2.2, 2.7 da 3.9, 5.1 da 1 d 16, 25 da |
940b 667b 338b 500b 270b |
343b 324b 145b ND 1000b |
2.7 2.1 2.3 ND 0.27 |
[10] [10] [10] [11] [12] | |||
| Intravenous inj. | 0.3 | 5 min | 8321b | 960b | 8.7 | [13] | |||
| Footnotes: a = Tmax for E2, E1 levels. b = Actual levels (not change). Sources: Main: [14] | |||||||||
See also
References
- ^ a b c Dada OA, Laumas V, Landgren BM, Cekan SZ, Diczfalusy E (1978). "Effect of graded oral doses of oestradiol on circulating hormonal levels". Acta Endocrinol. 88 (4): 754–67. doi: 10.1530/acta.0.0880754. PMID 581116.
- ^ a b Price TM, Blauer KL, Hansen M, Stanczyk F, Lobo R, Bates GW (March 1997). "Single-dose pharmacokinetics of sublingual versus oral administration of micronized 17 beta-estradiol". Obstet Gynecol. 89 (3): 340–5. doi: 10.1016/S0029-7844(96)00513-3. PMID 9052581.
- ^ Burnier AM, Martin PL, Yen SS, Brooks P (May 1981). "Sublingual absorption of micronized 17beta-estradiol". Am. J. Obstet. Gynecol. 140 (2): 146–50. doi: 10.1016/0002-9378(81)90101-0. PMID 6786097.
- ^ Fiet J, Hermano M, Witte J, Villette JM, Haimart M, Gourmel B, Tabuteau F, Rouffy J, Dreux C (September 1982). "Post-menopausal concentrations of plasma oestradiol, oestrone, FSH and LH and of total urinary oestradiol and oestrone after a single sublingual dose of oestradiol-17 beta". Acta Endocrinol. 101 (1): 93–7. doi: 10.1530/acta.0.1010093. PMID 6812348.
- ^ a b Rigg LA, Milanes B, Villanueva B, Yen SS (1977). "Efficacy of intravaginal and intranasal administration of micronized estradiol-17beta". J. Clin. Endocrinol. Metab. 45 (6): 1261–4. doi: 10.1210/jcem-45-6-1261. PMID 591620.
- ^ Strecker JR, Lauritzen C, Goessens L (1979). "Plasma concentrations of unconjugated and conjugated estrogens and gonadotrophins following application of various estrogen preparations after oophorectomy and in the menopause". Maturitas. 1 (3): 183–90. PMID 228157.
- ^ a b c Whitehead MI, Townsend PT, Kitchin Y, Dyer G, Iqbal MJ, Mansfield MD, et al. (1980). "Plasma steroid and protein hormone profiles in postmenopausal women following topical administration of oestradiol 17β". In Mauvais-Jarvis P (ed.). Percutaneous Absorption of Steroids. Academic Press. p. 231.
- ^ Schiff I, Tulchinsky D, Ryan KJ (1977). "Vaginal absorption of estrone and 17beta-estradiol". Fertil. Steril. 28 (10): 1063–6. doi: 10.1016/S0015-0282(16)42855-4. PMID 908445.
- ^ Lauritzen C (December 1986). "Die Behandlung der klimakterischen Beschwerden durch vaginale, rektale und transdermale Ostrogensubstitution" [Treatment of disorders of the climacteric by vaginal, rectal and transdermal estrogen substitution]. Gynakologe (in German). 19 (4): 248–53. ISSN 0017-5994. PMID 3817597.
- ^ a b c Oriowo MA, Landgren BM, Stenström B, Diczfalusy E (April 1980). "A comparison of the pharmacokinetic properties of three estradiol esters". Contraception. 21 (4): 415–24. doi: 10.1016/S0010-7824(80)80018-7. PMID 7389356.
- ^ Vermeulen A (1975). "Longacting steroid preparations". Acta Clin Belg. 30 (1): 48–55. doi: 10.1080/17843286.1975.11716973. PMID 1231448.
- ^ Stege R, Gunnarsson PO, Johansson CJ, Olsson P, Pousette A, Carlström K (May 1996). "Pharmacokinetics and testosterone suppression of a single dose of polyestradiol phosphate (Estradurin) in prostatic cancer patients". Prostate. 28 (5): 307–10. doi: 10.1002/(SICI)1097-0045(199605)28:5<307::AID-PROS6>3.0.CO;2-8. PMID 8610057.
- ^ Kuhnz W, Gansau C, Mahler M (September 1993). "Pharmacokinetics of estradiol, free and total estrone, in young women following single intravenous and oral administration of 17β-estradiol". Arzneimittelforschung. 43 (9): 966–73. ISSN 0004-4172. PMID 8240460.
- ^ Nichols KC, Schenkel L, Benson H (1984). "17 beta-estradiol for postmenopausal estrogen replacement therapy". Obstet Gynecol Surv. 39 (4): 230–45. doi: 10.1097/00006254-198404000-00022. PMID 6717863.