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17α-hydroxyprogesterone Acetate
Hydroxyprogesterone acetate (OHPA), sold under the brand name Prodox, is an oral administration, orally active progestin related to hydroxyprogesterone caproate (OHPC) which has been used in clinical medicine, clinical and veterinary medicine. It has reportedly also been used in birth control pills. OHPA is a progestin, or a synthetic compound, synthetic progestogen (medication), progestogen, and hence is an agonist of the progesterone receptor, the biological target of progestogens like progesterone. OHPA was discovered in 1953 and was introduced for medical use in 1956. Medical uses OHPA has been used in the treatment of a variety of gynecological disorders, including secondary amenorrhea, functional uterine bleeding, infertility, habitual abortion, dysmenorrhea, and premenstrual syndrome. OHPA (100 mg) was reportedly marketed in combination with mestranol (80 μg) as a sequential combined birth control pill under the brand name Hormolidin. The preparation was av ...
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Oral Administration
Oral administration is a route of administration where a substance is taken through the mouth. Per os abbreviated to P.O. is sometimes used as a direction for medication to be taken orally. Many medications are taken orally because they are intended to have a systemic effect, reaching different parts of the body via the bloodstream, for example. Oral administration can be easier and less painful than other routes, such as injection. However, the onset of action is relatively low, and the effectiveness is reduced if it is not absorbed properly in the digestive system, or if it is broken down by digestive enzymes before it can reach the bloodstream. Some medications may cause gastrointestinal side effects, such as nausea or vomiting, when taken orally. Oral administration can also only be applied to conscious patients, and patients willing and able to swallow. Terminology ''Per os'' (; ''P.O.'') is an adverbial phrase meaning literally from Latin "through the mouth" or "by mouth ...
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Secondary Amenorrhea
Amenorrhea is the absence of a menstrual period in a woman of reproductive age. Physiological states of amenorrhoea are seen, most commonly, during pregnancy and lactation ( breastfeeding). Outside the reproductive years, there is absence of menses during childhood and after menopause. Amenorrhoea is a symptom with many potential causes. Primary amenorrhea is defined as an absence of secondary sexual characteristics by age 13 with no menarche or normal secondary sexual characteristics but no menarche by 15 years of age. It may be caused by developmental problems, such as the congenital absence of the uterus, failure of the ovary to receive or maintain egg cells, or delay in pubertal development. Secondary amenorrhoea, ceasing of menstrual cycles after menarche, is defined as the absence of menses for three months in a woman with previously normal menstruation, or six months for women with a history of oligomenorrhoea. It is often caused by hormonal disturbances from the hypot ...
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Progesterone (medication)
Progesterone (P4) is a medication and naturally occurring steroid hormone. It is a progestogen and is used in combination with estrogens mainly in hormone therapy for menopausal symptoms and low sex hormone levels in women. It is also used in women to support pregnancy and fertility and to treat gynecological disorders. Progesterone can be taken by mouth, in through the vagina, and by injection into muscle or fat, among other routes. A progesterone vaginal ring and progesterone intrauterine device used for birth control also exist in some areas of the world. Progesterone is well tolerated and often produces few or no side effects. However, a number of side effects are possible, for instance mood changes. If progesterone is taken by mouth or at high doses, certain central side effects including sedation, sleepiness, and cognitive impairment can also occur. The medication is a naturally occurring progestogen and hence is an agonist of the progesterone receptor (PR), t ...
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17α-hydroxyprogesterone
17α-Hydroxyprogesterone (17α-OHP), also known as 17-OH progesterone (17-OHP), or hydroxyprogesterone (OHP), is an endogenous progestogen steroid hormone related to progesterone. It is also a chemical intermediate in the biosynthesis of many other endogenous steroids, including androgens, estrogens, glucocorticoids, and mineralocorticoids, as well as neurosteroids. Biological activity 17α-OHP is an agonist of the progesterone receptor (PR) similarly to progesterone, albeit weakly in comparison. In addition, it is an antagonist of the mineralocorticoid receptor (MR) as well as a partial agonist of the glucocorticoid receptor (GR), albeit with very low potency ( EC50 >100-fold less relative to cortisol) at the latter site, also similarly to progesterone. Biochemistry Biosynthesis 17α-OHP is derived from progesterone via 17α-hydroxylase (encoded by CYP17A1) 17α-OHP increases in the third trimester of pregnancy primarily due to fetal adrenal production. This steroid is ...
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IC50
The half maximal inhibitory concentration (IC50) is a measure of the potency of a substance in inhibiting a specific biological or biochemical function. IC50 is a quantitative measure that indicates how much of a particular inhibitory substance (e.g. drug) is needed to inhibit, ''in vitro'', a given biological process or biological component by 50%. The biological component could be an enzyme, cell, cell receptor or microorganism. IC50 values are typically expressed as molar concentration. IC50 is commonly used as a measure of antagonist drug potency in pharmacological research. IC50 is comparable to other measures of potency, such as EC50 for excitatory drugs. EC50 represents the dose or plasma concentration required for obtaining 50% of a maximum effect ''in vivo''. IC50 can be determined with functional assays or with competition binding assays. Sometimes, IC50 values are converted to the pIC50 scale. :\ce = -\log_ \ce Due to the minus sign, higher values of pIC50 indica ...
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Isoform
A protein isoform, or "protein variant", is a member of a set of highly similar proteins that originate from a single gene or gene family and are the result of genetic differences. While many perform the same or similar biological roles, some isoforms have unique functions. A set of protein isoforms may be formed from alternative splicings, variable promoter usage, or other post-transcriptional modifications of a single gene; post-translational modifications are generally not considered. (For that, see Proteoforms.) Through RNA splicing mechanisms, mRNA has the ability to select different protein-coding segments ( exons) of a gene, or even different parts of exons from RNA to form different mRNA sequences. Each unique sequence produces a specific form of a protein. The discovery of isoforms could explain the discrepancy between the small number of protein coding regions genes revealed by the human genome project and the large diversity of proteins seen in an organism: different ...
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Progesterone Receptor
The progesterone receptor (PR), also known as NR3C3 or nuclear receptor subfamily 3, group C, member 3, is a protein found inside cells. It is activated by the steroid hormone progesterone. In humans, PR is encoded by a single ''PGR'' gene residing on chromosome 11q22, it has two isoforms, PR-A and PR-B, that differ in their molecular weight. The PR-B is the positive regulator of the effects of progesterone, while PR-A serve to antagonize the effects of PR-B. Mechanism Progesterone is necessary to induce the progesterone receptors. When no binding hormone is present the carboxyl terminal inhibits transcription. Binding to a hormone induces a structural change that removes the inhibitory action. Progesterone antagonists prevent the structural reconfiguration. After progesterone binds to the receptor, restructuring with dimerization follows and the complex enters the nucleus and binds to DNA. There transcription takes place, resulting in formation of messenger RNA that is tra ...
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Argentina
Argentina (), officially the Argentine Republic ( es, link=no, República Argentina), is a country in the southern half of South America. Argentina covers an area of , making it the second-largest country in South America after Brazil, the fourth-largest country in the Americas, and the eighth-largest country in the world. It shares the bulk of the Southern Cone with Chile to the west, and is also bordered by Bolivia and Paraguay to the north, Brazil to the northeast, Uruguay and the South Atlantic Ocean to the east, and the Drake Passage to the south. Argentina is a federal state subdivided into twenty-three provinces, and one autonomous city, which is the federal capital and largest city of the nation, Buenos Aires. The provinces and the capital have their own constitutions, but exist under a federal system. Argentina claims sovereignty over the Falkland Islands, South Georgia and the South Sandwich Islands, and a part of Antarctica. The earliest recorded human prese ...
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Combined Birth Control Pill
The combined oral contraceptive pill (COCP), often referred to as the birth control pill or colloquially as "the pill", is a type of birth control that is designed to be taken orally by women. The pill contains two important hormones: progestin (a synthetic form of the hormone progestogen/progesterone) and estrogen (usually ethinylestradiol and 17β estradiol). When taken correctly, it alters the menstrual cycle to eliminate ovulation and prevent pregnancy. COCPs were first approved for contraceptive use in the United States in 1960, and are a very popular form of birth control. They are used by more than 100 million women worldwide and by about 9 million women in the United States. From 2015 to 2017, 12.6% of women aged 15–49 in the US reported using COCPs, making it the second most common method of contraception in this age range (female sterilization is the most common method). Use of COCPs, however, varies widely by country, age, education, and marital status. For examp ...
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Mestranol
Mestranol, sold under the brand names Enovid, Norinyl, and Ortho-Novum among others, is an estrogen medication which has been used in birth control pills, menopausal hormone therapy, and the treatment of menstrual disorders. It is formulated in combination with a progestin and is not available alone. It is taken by mouth. Side effects of mestranol include nausea, breast tension, edema, and breakthrough bleeding among others. It is an estrogen, or an agonist of the estrogen receptors, the biological target of estrogens like estradiol. Mestranol is a prodrug of ethinylestradiol in the body. Mestranol was discovered in 1956 and was introduced for medical use in 1957. It was the estrogen component in the first birth control pill. In 1969, mestranol was replaced by ethinylestradiol in most birth control pills, although mestranol continues to be used in a few birth control pills even today. Mestranol remains available only in a few countries, including the United States, United Kingd ...
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Premenstrual Syndrome
Premenstrual syndrome (PMS) refers to emotional and physical symptoms that regularly occur in the one to two weeks before the start of each menstrual period. Symptoms resolve around the time menstrual bleeding begins. Different women experience different symptoms. Premenstrual syndrome is commonly noted by at least one physical, emotional, or behavioral symptom, that resolves with menses. The range of symptoms is wide, and most commonly are breast tenderness, bloating, headache, mood swings, depression, anxiety, anger, and irritability. They must interfere with daily living, during two menstrual cycles of prospective recording. These symptoms are nonspecific and may be seen in women without PMS. Often PMS-related symptoms are present for about six days. An individual's pattern of symptoms may change over time. Symptoms do not occur during pregnancy or following menopause.> Diagnosis requires a consistent pattern of emotional and physical symptoms occurring after ovulation and ...
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Dysmenorrhea
Dysmenorrhea, also known as period pain, painful periods or menstrual cramps, is pain during menstruation. Its usual onset occurs around the time that menstruation begins. Symptoms typically last less than three days. The pain is usually in the pelvis or lower abdomen. Other symptoms may include back pain, diarrhea or nausea. Dysmenorrhea can occur without an underlying problem. Underlying issues that can cause dysmenorrhea include uterine fibroids, adenomyosis, and most commonly, endometriosis. It is more common among those with heavy periods, irregular periods, those whose periods started before twelve years of age and those who have a low body weight. A pelvic exam and ultrasound in individuals who are sexually active may be useful for diagnosis. Conditions that should be ruled out include ectopic pregnancy, pelvic inflammatory disease, interstitial cystitis and chronic pelvic pain. Dysmenorrhea occurs less often in those who exercise regularly and those who have childre ...
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