Template:Potencies and durations of natural estrogens by intramuscular injection
(Redirected from Template:Parenteral potencies and durations of steroidal estrogens)
| Estrogen | Form | Dose (mg) | Duration by dose (mg) | Refs | |
|---|---|---|---|---|---|
| EPD | CICD | ||||
| Estradiol | Aq. soln. | ? | – | <1 d | [1] |
| Oil soln. | 40–60 | – | 1–2 ≈ 1–2 d | [2][3] | |
| Aq. susp. | ? | 3.5 | 0.5–2 ≈ 2–7 d; 3.5 ≈ >5 d | [2][4][5][6][7] | |
| Microsph. | ? | – | 1 ≈ 30 d | [8][9] | |
| Estradiol benzoate | Oil soln. | 25–35 | – | 1.66 ≈ 2–3 d; 5 ≈ 3–6 d | [10][11] |
| Aq. susp. | 20 | – | 10 ≈ 16–21 d | [12][13][14] | |
| Emulsion | ? | – | 10 ≈ 14–21 d | [14][15] | |
| Estradiol dipropionate | Oil soln. | 25–30 | – | 5 ≈ 5–8 d | [10] |
| Estradiol valerate | Oil soln. | 20–30 | 5 | 5 ≈ 7–8 d; 10 ≈ 10–14 d; 40 ≈ 14–21 d; 100 ≈ 21–28 d |
[11][16] |
| Estradiol benz. butyrate | Oil soln. | ? | 10 | 10 ≈ 21 d | [17][18] |
| Estradiol cypionate | Oil soln. | 20–30 | – | 5 ≈ 11–14 d | [11] |
| Aq. susp. | ? | 5 | 5 ≈ 14–24 d | [19][20][21] | |
| Estradiol enanthate | Oil soln. | ? | 5–10 | 10 ≈ 20–30 d | [22][23][24] |
| Estradiol dienanthate | Oil soln. | ? | – | 7.5 ≈ >40 d | [25][26] |
| Estradiol undecylate | Oil soln. | ? | – | 10–20 ≈ 40–60 d; 25–50 ≈ 60–120 d |
[27][28] |
| Polyestradiol phosphate | Aq. soln. | 40–60 | – | 40 ≈ 30 d; 80 ≈ 60 d; 160 ≈ 120 d |
[29][30] |
| Estrone | Oil soln. | ? | – | 1–2 ≈ 2–3 d | [3][31] |
| Aq. susp. | ? | – | 0.1–2 ≈ 2–7 d | [32] | |
| Estriol | Oil soln. | ? | – | 1–2 ≈ 1–4 d | [3][33] |
| Polyestriol phosphate | Aq. soln. | ? | – | 50 ≈ 30 d; 80 ≈ 60 d | |
Notes and sources
Notes: All aqueous suspensions are of microcrystalline particle size. Estradiol production during the menstrual cycle is 30–640 µg/d (6.4–8.6 mg total per month or cycle). The vaginal epithelium maturation dosage of estradiol benzoate or estradiol valerate has been reported as 5 to 7 mg/week. An effective ovulation-inhibiting dose of estradiol undecylate is 20–30 mg/month. Sources: Main/General: [34][35][36][37][38][39][40][41][42] Miscellaneous: [43][44][45] | |||||
Template documentationSee also
- Template:Parenteral potencies and durations of nonsteroidal estrogens
- Template:Oral potencies of estrogens
- Template:Parenteral potencies and durations of progestogens
- Template:Parenteral durations of androgens/anabolic steroids
- Template:Structural properties of selected estradiol esters
- Pharmacokinetics of estradiol § Intramuscular injection
References
- ^ Davis ME, Wiener M, Jacobson HI, Jensen EV (December 1963). "Estradiol metabolism in pregnant and nonpregnant women". American Journal of Obstetrics and Gynecology. 87 (8): 979–990. doi:10.1016/0002-9378(63)90091-7. PMID 14089314.
- ^ a b Howard ME (1949). Modern Drug Encyclopedia and Therapeutic Index. Drug Publications. p. 322.
Supply: ALPHA ESTRADIOL, U.S.P. IN SESAME OIL—For intramuscular injection, 0.14 mg per cc, 0.28 mg per cc, and 0.7 mg per cc. Ampuls—1 cc—Boxes of 12, 25, 100. Vials, 30 cc—Boxes of 1, 6. (Chicago Pharmacal). ALPHA-ESTRADIOL, U.S.P. IN SUSPENSION—0.14 mg per cc, 0.28 mg per cc, and 0.7 mg per cc. Vials, 30 cc—Boxes of 1, 6. (Chicago Pharmacal).
- ^ a b c Brown JB (December 1957). "The relationship between urinary oestrogens and oestrogens produced in the body". The Journal of Endocrinology. 16 (2): 202–212. doi:10.1677/joe.0.0160202. PMID 13491750.
- ^ Osol A, Pratt R (1973). The United States dispensatory. Lippincott. p. 498. ISBN 978-0-397-55901-5.
The following dosages for estradiol in the form of aqueous suspension injected intramuscularly, or pellets implanted subcutaneously, are recommended by a leading maunfacturer: Menopausal syndrome.—In average cases, 1 mg. intramuscularly 2 or 3 times weekly for 2 or 3 weeks; in more severe cases, 1 to 1.5 mg. Thereafter dosage is reduced to the minimum requirement, usually within the range of 0.5 to 1 mg. of estradiol twice weekly.
- ^ Newman GT (September 1950). "Estrogen therapy by implantation of estradiol crystals". American Journal of Obstetrics and Gynecology. 60 (3): 661–664. doi:10.1016/0002-9378(50)90438-8. PMID 14771156.
- ^ Jones TM, Fang VS, Landau RL, Rosenfield R (December 1978). "Direct inhibition of Leydig cell function by estradiol". The Journal of Clinical Endocrinology and Metabolism. 47 (6): 1368–1373. doi:10.1210/jcem-47-6-1368. PMID 122429.
- ^ Yan Y, Pan J, Zhang Y, Kang J (1987). "The effect of monthly injectable contraceptive megestrol acetate compound on pituitary-ovarian function". Journal of Shanghai Second Medical University (2): 7–12. ISSN 1001-6686.
- ^ "Juvenum E (estradiol) – Medicamentos PLM". Medicamentos PLM. Archived from the original on 18 September 2018. Retrieved 17 September 2018.
- ^ Espino y Sosa S, Cortés Fuentes M, Alejandro Gómez Rico J, Cortés Bonilla M (2019). "Non-polymeric Microspheres for the Therapeutic Use of Estrogens: An Innovative Technology". In Khan WA (ed.). Estrogen. ISBN 978-1-83880-867-9.
- ^ a b Reifenstein EC (1944). "Endocrinology: A Synopsis of Normal and Pathologic Physiology, Diagnostic Procedures, and Therapy". Medical Clinics of North America. 28 (5): 1232–1276. doi:10.1016/S0025-7125(16)36180-6. ISSN 0025-7125.
- ^ 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): 415–424. doi:10.1016/S0010-7824(80)80018-7. PMID 7389356.
- ^ Kaiser R (September 1961). "[Estrogen excretion during the cycle and after injection of estradiol esters. A contribution to therapy with depot estrogens]" [Estrogen excretion during the cycle and after injection of estradiol esters. A contribution to therapy with depot estrogens]. Geburtshilfe und Frauenheilkunde (in German). 21: 868–878. PMID 13750804.
- ^ Kaiser R (1962). "Über die Oestrogenausscheidung nach Injektion von Oestradiolestern" [Estrogen excretion after injection of estradiol esters]. Gewebs-und Neurohormone: Physiologie des Melanophorenhormons [Tissue and Neurohormones: Physiology of the Melanophore Hormone] (in German). Springer, Berlin, Heidelberg. pp. 227–232. doi:10.1007/978-3-642-86860-3_24. ISBN 978-3-540-02909-0.
- ^ a b Kahr H (8 March 2013). Konservative Therapie der Frauenkrankheiten: Anzeigen, Grenzen und Methoden Einschliesslich der Rezeptur. Springer-Verlag. pp. 20–. ISBN 978-3-7091-5694-0.
- ^ Ferin J (January 1952). "Relative duration of action of natural and synthetic estrogens administered parenterally in women with estrogen deficiency". The Journal of Clinical Endocrinology and Metabolism. 12 (1): 28–35. doi:10.1210/jcem-12-1-28. PMID 14907837.
- ^ Schneider HG. Über Aufbau-und Erhaltungsdosis von Östradiolvalerianat [About Build-Up and Maintenance Dose of Estradiol Valerate] (Thesis) (in German). Berlin, Germany: Humboldt-Universität [Humboldt University]. OCLC 831117167.
- ^ Toppozada M (June 1977). "The clinical use of monthly injectable contraceptive preparations". Obstetrical & Gynecological Survey. 32 (6): 335–347. doi:10.1097/00006254-197706000-00001. PMID 865726.
- ^ Toppozada MK (1983). "Monthly Injectable Contraceptives". In Goldsmith A, Toppozada M (eds.). Long-Acting Contraception. pp. 93–103. OCLC 35018604.
- ^ Thurman A, Kimble T, Hall P, Schwartz JL, Archer DF (June 2013). "Medroxyprogesterone acetate and estradiol cypionate injectable suspension (Cyclofem) monthly contraceptive injection: steady-state pharmacokinetics". Contraception. 87 (6): 738–743. doi:10.1016/j.contraception.2012.11.010. PMID 23265980.
- ^ Rahimy MH, Ryan K, Hopkins NK (1999). "Lunelle™ monthly contraceptive injection (medroxyprogesterone acetate and estradiol cypionate injectable suspension): steady-state pharmacokinetics of MPA and E2 in surgically sterile women". Contraception. 60 (4): 209–214. doi:10.1016/S0010-7824(99)00086-4. ISSN 0010-7824. PMID 10640167.
- ^ Martins RS, Antunes NJ, Comerlatti G, Caraccio G, Moreno RA, Frecentese F, et al. (June 2019). "Quantification of estradiol cypionate in plasma by liquid chromatography coupled with tandem mass spectrometry: Application in a pharmacokinetic study in healthy female volunteers". Journal of Pharmaceutical and Biomedical Analysis. 170: 273–278. doi:10.1016/j.jpba.2019.03.053. PMID 30947128. S2CID 96433789.
- ^ Wiemeyer JC, Fernandez M, Moguilevsky JA, Sagasta CL (November 1986). "Pharmacokinetic studies of estradiol enantate in menopausic women". Arzneimittel-Forschung. 36 (11): 1674–1677. PMID 3814225.
- ^ Recio R, Garza-Flores J, Schiavon R, Reyes A, Diaz-Sanchez V, Valles V, et al. (June 1986). "Pharmacodynamic assessment of dihydroxyprogesterone acetophenide plus estradiol enanthate as a monthly injectable contraceptive". Contraception. 33 (6): 579–589. doi:10.1016/0010-7824(86)90046-6. PMID 3769482.
- ^ Gual C, Pérez-Palacios G, Perez AE, Ruiz MR, Solis J, Cervantes A, et al. (1973). "Metabolic fate of a long-acting injectable estrogen-progestogen contraceptive 1,2". Contraception. 7 (4): 271–287. doi:10.1016/0010-7824(73)90145-5. ISSN 0010-7824.
- ^ Saygin D, Tabib T, Bittar HE, Valenzi E, Sembrat J, Chan SY, et al. (1987). "Transcriptional profiling of lung cell populations in idiopathic pulmonary arterial hypertension". Pulmonary Circulation. 10 (1): 121–131. doi:10.3109/01674828709016773. PMC 7052475. PMID 32166015.
- ^ Sherwin BB, Gelfand MM, Schucher R, Gabor J (February 1987). "Postmenopausal estrogen and androgen replacement and lipoprotein lipid concentrations". American Journal of Obstetrics and Gynecology. 156 (2): 414–419. doi:10.1016/0002-9378(87)90295-X. PMID 3826177.
- ^ Wied GL (January 1954). "[Estradiol valerate and estradiol undecylate, two new estrogens with prolonged action; comparison with estradiol benzoate]" [Estradiol valerate and estradiol undecylate, two new estrogens with prolonged action; comparison with estradiol benzoate]. Geburtshilfe und Frauenheilkunde (in German). 14 (1): 45–52. PMID 13142295.
- ^ Gouygou C, Gueritee N, Pye A (1956). "[A fat-soluble, delayed estrogen : the estradiol undecylate]" [A fat-soluble, delayed estrogen: the estradiol undecylate]. Therapie (in French). 11 (5): 909–917. PMID 13391788.
- ^ Saygin D, Tabib T, Bittar HE, Valenzi E, Sembrat J, Chan SY, et al. (1961). "Transcriptional profiling of lung cell populations in idiopathic pulmonary arterial hypertension". Pulmonary Circulation. 10 (1): 115–118. doi:10.1177/2045894020908782. PMC 7052475. PMID 32166015.
- ^ 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". The Prostate. 28 (5): 307–310. doi:10.1002/(SICI)1097-0045(199605)28:5<307::AID-PROS6>3.0.CO;2-8. PMID 8610057. S2CID 33548251.
- ^ Saygin D, Tabib T, Bittar HE, Valenzi E, Sembrat J, Chan SY, et al. (1942). "Transcriptional profiling of lung cell populations in idiopathic pulmonary arterial hypertension". Pulmonary Circulation. 10 (1): 628–632. doi:10.1210/jcem-2-11-628. PMC 7052475. PMID 32166015.
- ^ Micromedex (1 January 2003). USP DI 2003: Drug Information for Healthcare Professionals. Thomson Micromedex. p. 1246. ISBN 978-1-56363-429-1.
ESTRONE Parenteral Dosage Forms ESTRONE INJECTABLE SUSPENSION USP Usual adult dose Atrophic vaginitis or Menopausal (vasomotor) symptoms or Vulvar atrophy—Intramuscular, 100 to 500 mcg (0.1 to 0.5 mg) two or three times a week, cyclically or continuously as appropriate. Estrogen deficiency, due to ovariectomy or Female hypogonadism or Primary ovarian failure—Intramuscular, 100 mcg (0.1 mg) to 1 mg a week, administered as a single dose or in divided doses, cyclically or continuously. A few patients may need doses of up to 2 mg a week.
- ^ Heithecker R, Aedo AR, Landgren BM, Cekan SZ (1991). "Plasma estriol levels after intramuscular injection of estriol and two of its esters". Hormone Research. 35 (6): 234–238. doi:10.1159/000181911. PMID 1819548.
- ^ Lauritzen C (1988). "Natürliche und Synthetische Sexualhormone – Biologische Grundlagen und Behandlungsprinzipien" [Natural and Synthetic Sexual Hormones – Biological Basis and Medical Treatment Principles]. In Schneider HP, Lauritzen C, Nieschlag E (eds.). Grundlagen und Klinik der Menschlichen Fortpflanzung [Foundations and Clinic of Human Reproduction] (in German). Walter de Gruyter. pp. 229–306. ISBN 978-3110109689. OCLC 35483492.
- ^ Knörr K, Knörr-Gärtner H, Beller FK, Lauritzen C (1982). Lehrbuch der Geburtshilfe und Gynäkologie: Physiologie und Pathologie der Reproduktion [Textbook of Obstetrics and Gynecology: Physiology and Pathology of Reproduction]. Springer-Verlag. pp. 508–. ISBN 978-3-662-00526-2.
- ^ Knörr K, Beller FK, Lauritzen C (1972). Lehrbuch der Gynäkologie [Textbook of Gynecology]. Springer-Verlag. pp. 212–213. ISBN 978-3-662-00942-0.
- ^ Labhart A (1974). Clinical Endocrinology: Theory and Practice. Springer Science & Business Media. pp. 551–553. ISBN 978-3-642-96158-8.
- ^ Horský J, Presl J (1981). "Hormonal Treatment of Disorders of the Menstrual Cycle". In Horsky J, Presl J (eds.). Ovarian Function and its Disorders: Diagnosis and Therapy. Springer Science & Business Media. pp. 309–332. doi:10.1007/978-94-009-8195-9_11. ISBN 978-94-009-8195-9.
- ^ Ufer J (1 January 1978). "Zur Therapeutischen Anwendung der Hormone" [For the Therapeutic Use of Hormones]. Hormontherapie in der Frauenheilkunde: Grundlagen und Praxis [Hormonal Therapy in Gynecology: Principles and Practice] (in German) (5th ed.). Walter de Gruyter. pp. 93–113. doi:10.1515/9783110837131-013. ISBN 978-3110066647. OCLC 924728827.
- ^ Ufer J (1969). The Principles and Practice of Hormone Therapy in Gynaecology and Obstetrics. de Gruyter. pp. 44, 138.
Table: Composition: Oestradiol valerate. Preparation: Primogyn Depot. Form of application: i.m. Proliferation dose in mg: 20–30. Estimated duration of action following a single application in days: 12–14.
- ^ Willibald Pschyrembel (1968). Praktische Gynäkologie: für Studierende und Ärzte [Practical Gynecology: for Students and Doctors]. Walter de Gruyter. pp. 598–599, 601. ISBN 978-3-11-150424-7.
- ^ Garza-Flores J (April 1994). "Pharmacokinetics of once-a-month injectable contraceptives". Contraception. 49 (4): 347–359. doi:10.1016/0010-7824(94)90032-9. PMID 8013219.
- ^ Nichols KC, Schenkel L, Benson H (April 1984). "17 beta-estradiol for postmenopausal estrogen replacement therapy". Obstetrical & Gynecological Survey. 39 (4): 230–245. doi:10.1097/00006254-198404000-00022. PMID 6717863.
- ^ Kaiser R (July 1993). "[Gestagen-estrogen combinations in gynecology. On the history, dosage and use of a hormone principle]" [Gestagen-Oestrogen Combinations in Gynaecology. History, Dosage and Use of a Hormonal Principle]. Geburtshilfe und Frauenheilkunde. 53 (7): 503–513. doi:10.1055/s-2007-1022924. PMID 8370495.
- ^ el-Mahgoub S, Karim M (February 1972). "Depot estrogen as a monthly contraceptive in nulliparous women with mild uterine hypoplasia". American Journal of Obstetrics and Gynecology. 112 (4): 575–576. doi:10.1016/0002-9378(72)90319-5. PMID 5008627.