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Progestogen Esters
A progestogen ester is an ester of a progestogen or progestin (a synthetic progestogen). 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 (though not all) steroid esters function as prodrugs. Esterification is particularly salient in the case of progesterone because progesterone itself shows very poor oral pharmacokinetics and is thus ineffective when taken orally. Unmodified, it has an elimination half-life of only 5 minutes, and is almost completely inactivated by the liver during first-pass metabolism. Micronization, however, has allowed for progesterone to be effective orally, although oral micronized progesterone was not developed until ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Progesterone
Progesterone (P4) is an endogenous steroid and progestogen sex hormone involved in the menstrual cycle, pregnancy, and embryogenesis of humans and other species. It belongs to a group of steroid hormones called the progestogens and is the major progestogen in the body. Progesterone has a variety of important functions in the body. It is also a crucial metabolic intermediate in the production of other endogenous steroids, including the sex hormones and the corticosteroids, and plays an important role in brain function as a neurosteroid. In addition to its role as a natural hormone, progesterone is also used as a medication, such as in combination with estrogen for contraception, to reduce the risk of uterine or cervical cancer, in hormone replacement therapy, and in feminizing hormone therapy. It was first prescribed in 1934. Biological activity Progesterone is the most important progestogen in the body. As a potent agonist of the nuclear progesterone receptor (nPR) ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
First-pass Metabolism
The first pass effect (also known as first-pass metabolism or presystemic metabolism) is a phenomenon of drug metabolism whereby the concentration of a drug, specifically when administered orally, is greatly reduced before it reaches the systemic circulation. It is the fraction of drug lost during the process of absorption which is generally related to the liver and gut wall. Notable drugs that experience a significant first-pass effect are buprenorphine, chlorpromazine, cimetidine, diazepam, ethanol (drinking alcohol), imipramine, insulin, lidocaine, midazolam, morphine, pethidine, propranolol, and tetrahydrocannabinol (THC). First pass metabolism may occur in the liver (for propranolol, lidocaine, clomethiazole, and NTG) or in the gut (for benzylpenicillin and insulin). After a drug is swallowed, it is absorbed by the digestive system and enters the hepatic portal system. It is carried through the portal vein into the liver before it reaches the rest of the body. The liver ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hydroxyprogesterone Caproate
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.https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021945s012lbl.pdf It has also been formulated in combination with estrogens for various indications (brand names Gravibinon and Primosiston) and as a form of long-lasting injectable birth control (brand name Chinese Injectable No. 1). 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. OHPC is generally well tolerated and produces few side effects. Injection site reactions such as pain and swelling are the most common side effect of OHPC. The medication may increase the risk of gestational diabetes when used in pregnant women. OHPC is a progestin, or a synthetic progestog ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Norethisterone Enanthate
Norethisterone enanthate (NETE), also known as norethindrone enanthate, is a form of hormonal birth control which is used to prevent pregnancy in women. It is used both as a form of progestogen-only injectable birth control and in combined injectable birth control formulations. It may be used following childbirth, miscarriage, or abortion. The failure rate per year in preventing pregnancy for the progestogen-only formulation is 2 per 100 women. Each dose of this form lasts two months with only up to two doses typically recommended. Side effects include breast pain, headaches, depression, irregular menstrual periods, and pain at the site of injection. Use in those with liver disease is not recommended as is use during pregnancy due to risk of birth defects. Use appears to be okay during breastfeeding. It does not protect against sexually transmitted infections. NETE is an ester and prodrug of norethisterone, through which it works. It works as a method of birth control by s ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Norethisterone Acetate
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. Side effects of NETA include menstrual irregularities, headaches, nausea, breast tenderness, mood changes, acne, increased hair growth, and others.https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/018405s023lbl.pdf NETA is a progestin, or a synthetic progestogen, and hence is an agonist of the progesterone receptor, the biological target of progestogens like progesterone. It has weak androgenic and estrogenic activity and no other important hormonal activity. The medication is a prodrug of norethisterone in the body. NETA was patented in 1957 and was introduced for ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
19-nortestosterone
Nandrolone, also known as 19-nortestosterone, is an androgen and anabolic steroid (AAS) which is used in the form of esters such as nandrolone decanoate (brand name Deca-Durabolin) and nandrolone phenylpropionate (brand name Durabolin). Nandrolone esters are used in the treatment of anemias, cachexia (muscle wasting syndrome), osteoporosis, breast cancer, and for other indications. They are not used by mouth and instead are given by injection into muscle or fat. Side effects of nandrolone esters include symptoms of masculinization like acne, increased hair growth, voice changes, and decreased sexual desire due to its ability to suppress endogenous testosterone synthesis while not being a sufficient androgen itself. They are synthetic androgens and anabolic steroids and hence are agonists of the androgen receptor (AR), the biological target of androgens like testosterone and dihydrotestosterone (DHT). Nandrolone has strong anabolic effects and weak androgenic effects, which giv ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nomegestrol Acetate
Nomegestrol acetate (NOMAC), sold under the brand names Lutenyl and Zoely among others, is a progestin medication which is used in birth control pills, menopausal hormone therapy, and for the treatment of gynecological disorders.http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Public_assessment_report/human/002068/WC500120841.pdf https://www.tga.gov.au/sites/default/files/auspar-zoely.pdf It is available both alone and in combination with an estrogen. NOMAC is taken by mouth. A birth control implant for placement under the skin was also developed but ultimately was not marketed. Side effects of NOMAC include menstrual irregularities, headaches, nausea, breast tenderness, and others. NOMAC is a progestin, or a synthetic progestogen, and hence is an agonist of the progesterone receptor, the biological target of progestogens like progesterone. It has some antiandrogenic activity and no other important hormonal activity. Nomegestrol, a related compound, was patented ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hydroxyprogesterone Caproate
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.https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021945s012lbl.pdf It has also been formulated in combination with estrogens for various indications (brand names Gravibinon and Primosiston) and as a form of long-lasting injectable birth control (brand name Chinese Injectable No. 1). 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. OHPC is generally well tolerated and produces few side effects. Injection site reactions such as pain and swelling are the most common side effect of OHPC. The medication may increase the risk of gestational diabetes when used in pregnant women. OHPC is a progestin, or a synthetic progestog ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cyproterone Acetate
Cyproterone acetate (CPA), sold alone under the brand name Androcur or Ethinylestradiol/cyproterone acetate, with ethinylestradiol under the brand names Diane or Diane-35 among others, is an antiandrogen and progestin medication used in the treatment of androgen-dependent conditions such as acne, hirsutism, excessive body hair growth, precocious puberty, early puberty, and prostate cancer, as a component of feminizing hormone therapy for transgender women, and in oral contraceptive, birth control pills. It is formulated and used both alone and in combination with an estrogen (medication), estrogen. CPA is taken Oral administration, by mouth one to three times per day. Common side effects of high-dose CPA in men include gynecomastia (breast development) and feminization (biology), feminization. In both men and women, possible side effects of CPA include hypogonadism, low sex hormone levels, reversible infertility, sexual dysfunction, fatigue (medical), fatigue, depression (mood), ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Megestrol Acetate
Megestrol acetate (MGA), sold under the brand name Megace among others, is a progestin medication which is used mainly as an appetite stimulant to treat wasting syndromes such as cachexia.https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021778s018lbl.pdf It is also used to treat breast cancer and endometrial cancer, and has been used in birth control. MGA is generally formulated alone, although it has been combined with estrogens in birth control formulations. It is usually taken by mouth. Side effects of MGA include increased appetite, weight gain, vaginal bleeding, nausea, edema, low sex hormone levels, sexual dysfunction, osteoporosis, cardiovascular complications, glucocorticoid effects, and others. MGA is a progestin, or a synthetic progestogen, and hence is an agonist of the progesterone receptor, the biological target of progestogens like progesterone. It has weak partial androgenic activity, weak glucocorticoid activity, and no other important hormonal activit ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Medroxyprogesterone Acetate
Medroxyprogesterone acetate (MPA), also known as depot medroxyprogesterone acetate (DMPA) in injectable form and sold under the brand name Depo-Provera among others, is a hormonal medication of the progestin type. It is used as a method of birth control and as a part of menopausal hormone therapy. It is also used to treat endometriosis, abnormal uterine bleeding, abnormal sexuality in males, and certain types of cancer. The medication is available both alone and in combination with an estrogen. It is taken by mouth, used under the tongue, or by injection into a muscle or fat. Common side effects include menstrual disturbances such as absence of periods, abdominal pain, and headaches. More serious side effects include bone loss, blood clots, allergic reactions, and liver problems. Use is not recommended during pregnancy as it may harm the baby. MPA is an artificial progestogen, and as such activates the progesterone receptor, the biological target of progesterone. It ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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