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Raloxifene
Raloxifene, sold under the brand name Evista among others, is a medication used to prevent and treat osteoporosis in postmenopausal women and those on glucocorticoids. For osteoporosis it is less preferred than bisphosphonates. It is also used to reduce the risk of breast cancer in those at high risk. It is taken by mouth. Common side effects include hot flashes, leg cramps, swelling, and joint pain. Severe side effects may include blood clots and stroke. Use during pregnancy may harm the baby. The medication may worsen menstrual symptoms. Raloxifene is a selective estrogen receptor modulator (SERM) and therefore a mixed agonist–antagonist of the estrogen receptor (ER). It has estrogenic effects in bone and antiestrogenic effects in the breasts and uterus. Raloxifene was approved for medical use in the United States in 1997. It is available as a generic medication. In 2020, it was the 292nd most commonly prescribed medication in the United States, with more than 1millio ...
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Selective Estrogen Receptor Modulator
Selective estrogen receptor modulators (SERMs), also known as estrogen receptor agonists/antagonists (ERAAs), are a class of drugs that act on estrogen receptors (ERs). Compared to pure ER agonists–antagonists (e.g., full agonists and silent antagonists), SERMs are more tissue-specific, allowing them to selectively inhibit or stimulate estrogen-like action in various tissues. Medical uses SERMs are used for various estrogen-related diseases, including treatment of ovulatory dysfunction in the management of infertility treatment, prevention of postmenopausal osteoporosis, treatment and risk reduction of breast cancer, and treatment of dyspareunia due to menopause. SERMs are also used in combination with conjugated estrogens indicated for the management of estrogen deficiency symptoms and of vasomotor symptoms associated with menopause. SERMs are also being explored for gender-affirming hormone therapy in some non-binary transgender individuals that were assigned male a ...
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Estrogen Receptor
Estrogen receptors (ERs) are proteins found in cell (biology), cells that function as receptor (biochemistry), receptors for the hormone estrogen (17β-estradiol). There are two main classes of ERs. The first includes the intracellular estrogen receptors, namely ERα and ERβ, which belong to the nuclear receptor family. The second class consists of membrane estrogen receptors (mERs), such as GPER (GPR30), ER-X, and Gq-mER, Gq-mER, which are primarily G protein-coupled receptors. This article focuses on the nuclear estrogen receptors (ERα and ERβ). Upon activation by estrogen, intracellular ERs undergo protein targeting, translocation to the nucleus where they bind to specific DNA sequences. As DNA-binding transcription factors, they regulate the activity of various genes. However, ERs also exhibit functions that are independent of their DNA-binding capacity. These non-genomic actions contribute to the diverse effects of estrogen signaling in cells. Estrogen receptors (ERs) b ...
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Menopause
Menopause, also known as the climacteric, is the time when Menstruation, menstrual periods permanently stop, marking the end of the Human reproduction, reproductive stage for the female human. It typically occurs between the ages of 45 and 55, although the exact timing can vary. Menopause is usually a natural change related to a decrease in circulating blood estrogen levels. It can occur earlier in those who smoke tobacco. Other causes include surgery that removes both ovaries, some types of chemotherapy, or anything that leads to a decrease in hormone levels. At the physiological level, menopause happens because of a decrease in the ovaries' production of the hormones estrogen and progesterone. While typically not needed, measuring hormone levels in the blood or urine can confirm a diagnosis. Menopause is the opposite of menarche, the time when periods start. In the years before menopause, a woman's periods typically become irregular, which means that periods may be longer ...
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Osteoporosis
Osteoporosis is a systemic skeletal disorder characterized by low bone mass, micro-architectural deterioration of bone tissue leading to more porous bone, and consequent increase in Bone fracture, fracture risk. It is the most common reason for a broken bone among the Old age, elderly. Bones that commonly break include the vertebrae in the Vertebral column, spine, the bones of the forearm, the wrist, and the hip. Until a broken bone occurs there are typically no symptoms. Bones may weaken to such a degree that a break may occur with minor stress or spontaneously. After the broken bone heals, some people may have chronic pain and a decreased ability to carry out normal activities. Osteoporosis may be due to lower-than-normal peak bone mass, maximum bone mass and greater-than-normal bone loss. Bone loss increases after menopause in women due to lower levels of estrogen, and after andropause in older men due to lower levels of testosterone. Osteoporosis may also occur due to a ...
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Bisphosphonates
Bisphosphonates are a class of drugs that prevent the loss of bone density, used to treat osteoporosis and similar diseases. They are the most commonly prescribed to treat osteoporosis. Evidence shows that they reduce the risk of fracture in post-menopausal women with osteoporosis. Bone tissue undergoes constant remodeling and is kept in balance (homeostasis) by osteoblasts creating bone and osteoclasts destroying bone. Bisphosphonates inhibit the digestion of bone by encouraging osteoclasts to undergo apoptosis, or cell death, thereby slowing bone loss. The uses of bisphosphonates include the prevention and treatment of osteoporosis, Paget's disease of bone, bone metastasis (with or without hypercalcemia), multiple myeloma, primary hyperparathyroidism, osteogenesis imperfecta, fibrous dysplasia, and other conditions that exhibit bone fragility. Chemical structure and mechanistic aspects The term bisphosphonate refers to the presence two phosphonate () groups. They are als ...
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Antiestrogen
Antiestrogens, also known as estrogen antagonists or estrogen blockers, are a class of drugs which prevent estrogens like estradiol from mediating their biological effects in the body. They act by blocking the estrogen receptor (ER) and/or inhibiting or suppressing estrogen production., Antiestrogens are one of three types of sex hormone antagonists, the others being antiandrogens and antiprogestogens. Antiestrogens are commonly used to stop steroid hormones, estrogen, from binding to the estrogen receptors leading to the decrease of estrogen levels. Decreased levels of estrogen can lead to complications in sexual development. Types and examples Antiestrogens include selective estrogen receptor modulators (SERMs) like tamoxifen, clomifene, and raloxifene, the ER silent antagonist and selective estrogen receptor degrader (SERD) fulvestrant, aromatase inhibitors (AIs) like anastrozole, and antigonadotropins including androgens/anabolic steroids, progestogens, and GnRH an ...
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Breast Cancer
Breast cancer is a cancer that develops from breast tissue. Signs of breast cancer may include a Breast lump, lump in the breast, a change in breast shape, dimpling of the skin, Milk-rejection sign, milk rejection, fluid coming from the nipple, a newly inverted nipple, or a red or scaly patch of skin. In those with Metastatic breast cancer, distant spread of the disease, there may be bone pain, swollen lymph nodes, shortness of breath, or yellow skin. Risk factors for developing breast cancer include obesity, a Sedentary lifestyle, lack of physical exercise, alcohol consumption, hormone replacement therapy during menopause, ionizing radiation, an early age at Menarche, first menstruation, having children late in life (or not at all), older age, having a prior history of breast cancer, and a family history of breast cancer. About five to ten percent of cases are the result of an inherited genetic predisposition, including BRCA mutation, ''BRCA'' mutations among others. Breast ...
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Pregnancy
Pregnancy is the time during which one or more offspring gestation, gestates inside a woman's uterus. A multiple birth, multiple pregnancy involves more than one offspring, such as with twins. Conception (biology), Conception usually occurs following sexual intercourse, vaginal intercourse, but can also occur through assisted reproductive technology procedures. A pregnancy may end in a Live birth (human), live birth, a miscarriage, an Abortion#Induced, induced abortion, or a stillbirth. Childbirth typically occurs around 40 weeks from the start of the Menstruation#Onset and frequency, last menstrual period (LMP), a span known as the Gestational age (obstetrics), ''gestational age''; this is just over nine months. Counting by Human fertilization#Fertilization age, ''fertilization age'', the length is about 38 weeks. Implantation (embryology), Implantation occurs on average 8–9 days after Human fertilization, fertilization. An ''embryo'' is the term for the deve ...
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Menstrual Symptoms
Menstruation (also known as a period, among other colloquial terms) is the regular discharge of blood and mucosal tissue from the inner lining of the uterus through the vagina. The menstrual cycle is characterized by the rise and fall of hormones. Menstruation is triggered by falling progesterone levels, and is a sign that pregnancy has not occurred. Women use feminine hygiene products to maintain hygiene during menses. The first period, a point in time known as menarche, usually begins during puberty, between the ages of 11 and 13. However, menstruation starting as young as 8 years would still be considered normal. The average age of the first period is generally later in the developing world, and earlier in the developed world. The typical length of time between the first day of one period and the first day of the next is 21 to 45 days in young women; in adults, the range is between 21 and 35 days with the average often cited as 28 days. In the biggest study of menstrual app ...
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Oral Administration
Oral administration is a route of administration whereby a substance is taken through the Human mouth, mouth, swallowed, and then processed via the digestive system. This is a common route of administration for many medications. Oral administration can be easier and less painful than other routes of administration, such as Injection (medicine), 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 able to swallow. Terminology ''Per os'' (; ''P.O.'') is an adverbial phrase meaning literally from Latin "through the mouth" or "by mouth". The expression is used in medicine to describe a treatment that is taken orally (but not ...
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Agonist
An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an Receptor antagonist, antagonist blocks the action of the agonist, while an inverse agonist causes an action opposite to that of the agonist. Etymology The word originates from the Ancient Greek, Greek word (''agōnistēs''), "contestant; champion; rival" < (''agōn''), "contest, combat; exertion, struggle" < (''agō''), "I lead, lead towards, conduct; drive."


Types of agonists

Receptor (biochemistry), Receptors can be activated by either endogenous agonists (such as hormones and neurotransmitters) or exogenous agonists (such as medication, drugs), resulting in a biological response. A physiological agonism an ...
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