Selective Estrogen Receptor Modulators
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Selective Estrogen Receptor Modulators
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–Receptor antagonist, 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, ovulatory dysfunction in the management of infertility treatment, prevention of Osteoporosis, 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 Hypoestrogenism, estrogen deficiency symptoms and of vasomotor symptoms associated with menopause. SERMs are also being explored for gender-affirming hormone therapy ...
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Tamoxifen
Tamoxifen, sold under the brand name Nolvadex among others, is a selective estrogen receptor modulator used to prevent breast cancer in women and men. It is also being studied for other types of cancer. It has been used for Albright syndrome. Tamoxifen is typically taken daily by mouth for five years for breast cancer. Serious side effects include a small increased risk of uterine cancer, stroke, vision problems, and pulmonary embolism. Common side effects include irregular periods, weight loss, and hot flashes. It may cause harm to the baby if taken during pregnancy or breastfeeding. It is a selective estrogen-receptor modulator (SERM) and works by decreasing the growth of breast cancer cells. It is a member of the triphenylethylene group of compounds. Tamoxifen was initially made in 1962, by chemist Dora Richardson. It is on the World Health Organization's List of Essential Medicines. Tamoxifen is available as a generic medication. In 2020, it was the 317th mos ...
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Receptor Antagonist
A receptor antagonist is a type of receptor ligand or drug that blocks or dampens a biological response by binding to and blocking a receptor rather than activating it like an agonist. Antagonist drugs interfere in the natural operation of receptor proteins.Pharmacology Guide: In vitro pharmacology: concentration-response curves
." '' GlaxoWellcome.'' Retrieved on December 6, 2007.
They are sometimes called blockers; examples include alpha blockers, beta b ...
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Secondary Sex Characteristic
A secondary sex characteristic is a physical characteristic of an organism that is related to or derived from its sex, but not directly part of its reproductive system. In humans, these characteristics typically start to appear during puberty—and include enlarged breasts and widened hips of females, facial hair and Adam's apples on males, and pubic hair on both. In non-human animals, they can start to appear at sexual maturity—and include, for example, the manes of male lions, the bright facial and rump coloration of male mandrills, and horns in many goats and antelopes. Secondary sex characteristics are particularly evident in the sexually dimorphic phenotypic traits that distinguish the sexes of a species. In evolution, secondary sex characteristics are the product of sexual selection for traits that show fitness, giving an organism an advantage over its rivals in courtship and in aggressive interactions. Many characteristics are believed to have been establishe ...
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Estradiol (medication)
Estradiol (E2) is a medication and naturally occurring steroid hormone. It is an estrogen and is used mainly in menopausal hormone therapy and to treat hypogonadism, low sex hormone levels in women. It is also used in hormonal contraception, hormonal birth control for women, in feminizing hormone therapy for transgender women and some Non-binary gender, non-binary individuals, and in the treatment of hormone-sensitive cancers like prostate cancer in men and breast cancer in women, among other uses. Estradiol can be taken oral administration, by mouth, sublingual administration, held and dissolved under the tongue, as a gel or transdermal patch, patch that is transdermal, applied to the skin, intravaginal administration, in through the vagina, by intramuscular injection, injection into muscle or subcutaneous injection, fat, or through the use of an subcutaneous implant, implant that is placed into fat, among other route of administration, routes. Side effects of estradiol in ...
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Non-binary Gender
Non-binary or genderqueer gender identities are those that are outside the male/female gender binary. Non-binary identities often fall under the transgender umbrella since non-binary people typically identify with a gender that is different from the sex assigned to them at birth, although some non-binary people do not consider themselves transgender. Non-binary people may identify as an intermediate or separate third gender, identify with more than one gender or no gender, or have a fluctuating gender identity. Gender identity is separate from sexual or romantic orientation; non-binary people have various sexual orientations. Non-binary people as a group vary in their gender expressions, and some may reject gender identity altogether. Some non-binary people receive gender-affirming care to reduce the mental distress caused by gender dysphoria, such as gender-affirming surgery or hormone replacement therapy. Terms and definitions The term "genderqueer" first app ...
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Gender-affirming Hormone Therapy
Gender-affirming hormone therapy (GAHT), also called hormone replacement therapy (HRT) or transgender hormone therapy, is a form of hormone therapy in which sex hormones and other sex-hormonal agent, hormonal medications are administered to transgender or gender nonconforming individuals for the purpose of more closely aligning their secondary sexual characteristics with their gender identity. This form of hormone therapy is given as one of two types, based on whether the goal of treatment is masculinization or feminization (biology), feminization: * Masculinizing hormone therapy – for Trans man, transgender men or transmasculine people; consists of androgens and occasionally antiestrogens. * Feminizing hormone therapy – for Trans woman, transgender women or transfeminine people; consists of estrogen (medication), estrogens with or without antiandrogens. Eligibility for GAHT may require an assessment for gender dysphoria or persistent gender incongruence; Many medical instituti ...
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Vasomotor
Vasomotor refers to actions upon a blood vessel which alter its diameter. More specifically, it can refer to vasodilator action and vasoconstrictor action. Control Sympathetic innervation Sympathetic nerve fibers travel around the tunica media of the artery, secrete neurotransmitters such as norepinephrine into the extracellular fluid surrounding the smooth muscle (tunica media) from the terminal knob of the axon. The smooth muscle cell membranes have α and β-adrenergic receptors for these neurotransmitters. Activation of α-adrenergic receptors promotes vasoconstriction, while the activation of β-adrenergic receptors mediates the relaxation of muscle cells, resulting in vasodilation. Normally, α-adrenergic receptors predominate in smooth muscle of resistance vessels.Robert C. Ward et al. (2002). In Foundations for osteopathic medicine'. Lippincott Williams & Wilkins. 2nd edition. p. 98. . Google Book Search. Retrieved on 5 December 2010. Endothelium derived chemicals En ...
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Hypoestrogenism
Hypoestrogenism, or estrogen deficiency, refers to a lower than normal level of estrogen. It is an umbrella term used to describe estrogen deficiency in various conditions. Estrogen deficiency is also associated with an increased risk of cardiovascular disease, and has been linked to diseases like urinary tract infections and osteoporosis. In women, low levels of estrogen may cause symptoms such as hot flashes, sleeping disturbances, decreased bone health, and changes in the genitourinary system. Hypoestrogenism is most commonly found in women who are postmenopausal, have primary ovarian insufficiency (POI), or are presenting with amenorrhea (absence of menstrual periods). Hypoestrogenism includes primarily genitourinary effects, including thinning of the vaginal tissue layers and an increase in vaginal pH. With normal levels of estrogen, the environment of the vagina is protected against inflammation, infections, and sexually transmitted infections. Hypoestrogenism c ...
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Conjugated Estrogens
Conjugated estrogens (CEs), or conjugated equine estrogens (CEEs), sold under the brand name Premarin among others, is an estrogen medication which is used in menopausal hormone therapy and for various other indications. It is a mixture of the sodium salts of estrogen conjugates found in horses, such as estrone sulfate and equilin sulfate. CEEs are available in the form of both natural preparations manufactured from the urine of pregnant mares and fully synthetic replications of the natural preparations. They are formulated both alone and in combination with progestins such as medroxyprogesterone acetate. CEEs are usually taken by mouth, but can also be given by application to the skin or vagina as a cream or by injection into a blood vessel or muscle. Side effects of CEEs include breast tenderness and enlargement, headache, fluid retention, and nausea among others. It may increase the risk of endometrial hyperplasia and endometrial cancer in women with an intact uter ...
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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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Ovulatory Dysfunction
Ovulation is an important part of the menstrual cycle in female vertebrates where the egg cells are released from the ovaries as part of the ovarian cycle. In female humans ovulation typically occurs near the midpoint in the menstrual cycle and after the follicular phase. Ovulation is stimulated by an increase in luteinizing hormone (LH). The ovarian follicles rupture and release the secondary oocyte ovarian cells. After ovulation, during the luteal phase, the egg will be available to be fertilized by sperm. If it is not, it will break down in less than a day. Meanwhile, the uterine lining (endometrium) continues to thicken to be able to receive a fertilized egg. If no conception occurs, the uterine lining will eventually break down and be shed from the body via the vagina during menstruation. Some people choose to track ovulation in order to improve or aid becoming pregnant by timing intercourse with their ovulation. The signs of ovulation may include cervical mucus changes ...
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