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Progestogens, also sometimes written progestagens or gestagens, are a class of natural or synthetic steroid hormones that bind to and activate the progesterone receptors (PR). Progesterone is the major and most important progestogen in the body. The progestogens are named for their function in maintaining pregnancy, although they are also present at other phases of the estrous and menstrual cycles.
A progestogen, also referred to as a progestagen, gestagen, or gestogen, is a type of medication which produces effects similar to those of the natural female sex hormone progesterone in the body. A progestin is a synthetic progestogen. Progestogens are used most commonly in hormonal birth control and menopausal hormone therapy. They can also be used in the treatment of gynecological conditions, to support fertility and pregnancy, to lower sex hormone levels for various purposes, and for other indications. Progestogens are used alone or in combination with estrogens. They are available in a wide variety of formulations and for use by many different routes of administration. Examples of progestogens include natural or bioidentical progesterone as well as progestins such as medroxyprogesterone acetate and norethisterone.
Ethisterone, also known as ethinyltestosterone, pregneninolone, and anhydrohydroxyprogesterone and formerly sold under the brand names Proluton C and Pranone among others, is a progestin medication which was used in the treatment of gynecological disorders but is now no longer available. It was used alone and was not formulated in combination with an estrogen. The medication is taken by mouth.
Hydroxyprogesterone caproate (OHPC), sold under the brand names Proluton and Makena among others, is a progestin medication which is used to prevent preterm birth in pregnant women with a history of the condition and to treat gynecological disorders. It has also been formulated in combination with estrogens for various indications and as a form of long-lasting injectable birth control. It is not used by mouth and is instead given by injection into muscle or fat, typically once per week to once per month depending on the indication.
Combined injectable contraceptives (CICs) are a form of hormonal birth control for women. They consist of monthly injections of combined formulations containing an estrogen and a progestin to prevent pregnancy.
Segesterone acetate (SGA), sold under the brand names Nestorone, Elcometrine, and Annovera, is a progestin medication which is used in birth control and in the treatment of endometriosis in the United States, Brazil, and other South American countries. It is available both alone and in combination with an estrogen. It is not effective by mouth and must be given by other routes, most typically as a vaginal ring or implant that is placed into fat.
Testosterone caproate (TCa), also known as testosterone hexanoate, is an androgen and anabolic steroid and a testosterone ester that is no longer marketed. It was formerly available as a component of Omnadren 250, along with testosterone isocaproate, testosterone phenylpropionate, and testosterone propionate, but this formulation has since been discontinued.
Hydroxyprogesterone heptanoate (OHPH), also known as hydroxyprogesterone enanthate (OHPE) and sold under the brand names H.O.P., Lutogil A.P., and Lutogyl A.P. among others, is a progestin medication used for progestogenic indications. It has been formulated both alone and in together with estrogens, androgens/anabolic steroids, and other progestogens in several combination preparations. OHPH is given by injection into muscle at regular intervals.
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.
A progestogen ester is an ester of a progestogen or progestin. The prototypical progestogen is progesterone, an endogenous sex hormone. Esterification is frequently employed to improve the pharmacokinetics of steroids, including oral bioavailability, lipophilicity, and elimination half-life. In addition, with intramuscular injection, steroid esters are often absorbed more slowly into the body, allowing for less frequent administration. Many steroid esters function as prodrugs.
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 dibutyrate (EDBu), or estradiol dibutanoate, is an estrogen medication and an estrogen ester – specifically, a diester of estradiol – which is no longer used. It was a component of Triormon Depositum, a combination formulation of estradiol dibutyrate, testosterone caproate, and hydroxyprogesterone heptanoate which was developed in the 1950s.
Estradiol benzoate/estradiol valerate/hydroxyprogesterone caproate (EB/EV/OHPC), sold under the brand name Sin-Ol, is a combination medication of estradiol benzoate (EB), an estrogen, estradiol valerate (EV), an estrogen, and hydroxyprogesterone caproate (OHPC), a progestin, which was reportedly used as a combined injectable contraceptive in women in the early 1970s. It contained 1 mg EB, 10 mg EV, and 250 mg OHPC in oil solution, was provided in the form of 3 mL ampoules, and was administered by intramuscular injection at regular intervals. The medication was manufactured by the pharmaceutical company Reuffer in Mexico.
Progesterone/hydroxyprogesterone heptanoate/α-tocopherol palmitate (P4/OHPH/VE), sold under the brand name Tocogestan, is a combination medication of progesterone (P4), a short-acting progestogen, hydroxyprogesterone heptanoate (OHPH), a long-acting progestogen, and α-tocopherol palmitate, a prodrug of α-tocopherol and form of vitamin E, which was previously used in France to support pregnancy in women but is no longer available. It contained 50 mg P4, 200 mg OHPH, and 250 mg in 2 mL oil solution, was provided in the form of 2 mL ampoules, and was administered by intramuscular injection.
Estrone/progesterone/testosterone (E1/P4/T), sold under the brand name Tristeron or Tristerone, is an injectable combination medication of estrone (E1), an estrogen, progesterone (P4), a progestogen, and testosterone (T), an androgen/anabolic steroid, which was used in the treatment of functional uterine bleeding in women. It contained 6 mg estrone, 50 mg progesterone, and 25 mg testosterone in microcrystalline aqueous suspension and was administered by intramuscular injection. The medication was manufactured by Wyeth and was marketed by 1951. It is no longer available.
Estradiol diundecylate/hydroxyprogesterone heptanoate/testosterone cyclohexylpropionate (EDU/OHPH/TCHP), sold under the brand name Trioestrine Retard, is an injectable combination medication of estradiol diundecylate (EDU), an estrogen, hydroxyprogesterone heptanoate (OHPH), a progestogen, and testosterone cyclohexylpropionate (TCHP), an androgen/anabolic steroid. It contained 2.25 mg EDU, 100 mg OHPH, and 67.5 mg TCHP in oil solution, was provided as ampoules, and was administered by intramuscular injection. The medication was manufactured by Roussel and Théramex and was marketed by 1953. It is no longer available.
Estradiol hexahydrobenzoate/hydroxyprogesterone caproate/testosterone hexahydrobenzoate (EHHB/OHPC/THHB), sold under the brand name Trinestril AP, is an injectable combination medication of estradiol hexahydrobenzoate (EHHB), an estrogen, hydroxyprogesterone caproate (OHPC), a progestogen, and testosterone hexahydrobenzoate (THHB), an androgen/anabolic steroid. It contained 3 mg EHHB, 75 mg OHPC, and 100 mg THHB and was administered by intramuscular injection once per month. The medication was marketed by 1957.
Estrapronicate/hydroxyprogesterone heptanoate/nandrolone undecanoate (EPC/OHPH/NU), tentative brand name Trophobolene or Trophoboline, is an injectable combination medication of estrapronicate, an estrogen, hydroxyprogesterone heptanoate (OHPH), a progestogen, and nandrolone undecanoate (NU), an androgen/anabolic steroid, which was never marketed. It contained 1.3 mg EPC, 80 mg OHPH, and 50 mg NU in oil solution and was administered by intramuscular injection. The medication was developed by Théramex in the mid-to-late 1960s. It was studied for use for a variety of indications, including treatment of coronary insufficiency, growth deficiency, and osteoporosis, as well as hormonal disorders in gonadotropin deficiency.
References
- 1 2 3 Ermiglia G, Valli P (May 1957). "Studio sul triormon depositum nella sindrome climaterica; curve di eliminazione dei cataboliti e durata dell'effetto terapeutico" [Study of tribormone depositum in the climacteric syndrome; catabolite elimination curves and duration of the therapeutic effect]. Quaderni di Clinica Ostetrica e Ginecologica (in Italian). 12 (5): 284–93. ISSN 0033-491X. PMID 13465973.
Triormon depositum (estradiol dibutyrate 3, testosterone caprylate 50, and hydroxyprogesterone heptanoate 30 mg.), administered in castor oil-benzyl benzoate soln. or polyvinylpyrrolidone suspension to 21 women in climacteric, was followed by estradiol, pregnanediol, and 17-keto steroid urinary curves, most with a peak at the 4th day, and approaching starting values at the 8-10th day. The therapeutic efficacy of the drug was satisfactory.
- ↑ "Home". micromedexsolutions.com.
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