GnRH Antagonists
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GnRH Antagonists
Gonadotropin-releasing hormone antagonists (GnRH antagonists) are a class of medications that antagonize the gonadotropin-releasing hormone receptor (GnRH receptor) and thus the action of gonadotropin-releasing hormone (GnRH). They are used in the treatment of prostate cancer, endometriosis, uterine fibroids, female infertility in assisted reproduction, and for other indications. Some GnRH antagonists, such as cetrorelix, are similar in structure to natural GnRH (a hormone made by neurons in the hypothalamus) but that have an antagonistic effect, while other GnRH antagonists, such as elagolix and relugolix, are non-peptide and small-molecule compounds. GnRH antagonists compete with natural GnRH for binding to GnRH receptors, thus decreasing or blocking GnRH action in the body. Medical uses Prostate cancer Testosterone promotes growth of many prostate tumors and therefore reducing circulating testosterone to very low (castration) levels is often the treatment goal in the man ...
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Cetrorelix
Cetrorelix (, ), or cetrorelix acetate (, ), sold under the brand name Cetrotide, is an injectable gonadotropin-releasing hormone (GnRH) gonadotropin-releasing hormone antagonist, antagonist. A synthetic compound, synthetic decapeptide, it is used in assisted reproduction to inhibit premature luteinizing hormone surges The drug works by blocking the action of GnRH upon the pituitary, thus rapidly suppressing the production and action of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). In addition, cetrorelix can be used to treat hormone-sensitive cancers of the prostate and breast (in pre-/perimenopausal women) and some benign gynaecological disorders (endometriosis, uterine fibroids and endometrial thinning). It is administered as either multiple 0.25 mg daily subcutaneous injections or as a single-dose 3 mg subcutaneous injection. The duration of the 3 mg single dose is four days; if human chorionic gonadotropin (hCG) is not administered within fou ...
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Female Infertility
Female infertility refers to infertility in women, which is the inability to Fertilisation, conceive after sexual intercourse. It affects an estimated 48 million women, globally. Female infertility varies widely by region. The highest rates of female infertility are found in Eastern Europe and South Central Asia, followed by South Asia, Sub-Saharan Africa, and Middle East and North Africa. Female infertility rates are lowest in East Asia and Latin America. Fertility is affected by a variety of factors, including hormone, hormones, nutritional status, disease, and malformations of the uterus. Infertility affects women from around the world, and the social stigmas affecting infertile women may vary from region to region. Cause Causes or factors of female infertility can basically be classified regarding whether they are Acquired disorder, acquired or genetic, or strictly by location. Although factors of female infertility can be classified as either acquired or genetic, female i ...
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Urethral Obstruction
Urinary tract obstruction is a urologic disease consisting of a decrease in the free passage of urine through one or both ureters and/or the urethra. It is a cause of urinary retention. Complete obstruction of the urinary tract requires prompt treatment for renal preservation.Chowdhury SH, Cozma AI, Chowdhury JH. Urinary Tract Obstruction. Essentials for the Canadian Medical Licensing Exam: Review and Prep for MCCQE Part I. 2nd edition. Wolters Kluwer. Hong Kong. 2017. Any sign of infection, such as fever and chills, in the context of obstruction to urine flow constitutes a urologic emergency. Causes Causes of urinary tract obstruction include: * Bladder stone and renal stone * Benign prostatic hyperplasia * Obstruction as a congenital disorder. * Foreign object such as a bullet or pellet. Congenital urinary tract obstruction Urinary tract obstruction as a congenital disorder results in oligohydramnios which in turn can lead to the Potter sequence of atypical physical appearance. P ...
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Bone Pain
Bone pain (also known medically by several other names) is pain coming from a bone, and is caused by damaging stimuli. It occurs as a result of a wide range of diseases or physical conditions or both, and may severely impair the quality of life.Luger, N. Mach, D. Sevcik, M. Mantyh, P. (2005). Bone cancer pain: From mechanism to model to therapy. ''Journal of Pain and Symptom Management''. 29(5): 32-46. Bone pain belongs to the class of deep somatic pain, often experienced as a dull pain that cannot be localized accurately by the patient. This is in contrast with the pain which is mediated by superficial receptors in, e.g., the skin. Bone pain can have several possible causes ranging from extensive physical stress to serious diseases such as cancer.Zwas, T. Elkanovitch, R. George, F. (1987). Interpretation and Classification of Bone Scintigraphic Findings in Stress Fractures. ''Journal of Nuclear Medicine''. 28: 452-457.Mantyh, P. Clohisy, D. Koltzenburg, M. Hunt, S. (2002). Mole ...
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Castration
Castration is any action, surgery, surgical, chemical substance, chemical, or otherwise, by which a male loses use of the testicles: the male gonad. Surgical castration is bilateral orchiectomy (excision of both testicles), while chemical castration uses pharmaceutical drugs to deactivate the testes. Some forms of castration cause sterilization (medicine), sterilization (permanently preventing the castrated person or animal from reproduction, reproducing); it also greatly reduces the production of hormones, such as testosterone and estrogen. Surgical castration in animals is often called neutering. #Other animals, Castration of animals is intended to favor a desired development of the animal or of its habits, as an anaphrodisiac or to prevent overpopulation. The parallel of castration for female animals is spaying. Castration may also refer medically to oophorectomy in female humans and animals. The term ''castration'' may also be sometimes used to refer to emasculation where ...
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Tumor
A neoplasm () is a type of abnormal and excessive growth of tissue. The process that occurs to form or produce a neoplasm is called neoplasia. The growth of a neoplasm is uncoordinated with that of the normal surrounding tissue, and persists in growing abnormally, even if the original trigger is removed. This abnormal growth usually forms a mass, which may be called a tumour or tumor.'' ICD-10 classifies neoplasms into four main groups: benign neoplasms, in situ neoplasms, malignant neoplasms, and neoplasms of uncertain or unknown behavior. Malignant neoplasms are also simply known as cancers and are the focus of oncology. Prior to the abnormal growth of tissue, such as neoplasia, cells often undergo an abnormal pattern of growth, such as metaplasia or dysplasia. However, metaplasia or dysplasia does not always progress to neoplasia and can occur in other conditions as well. The word neoplasm is from Ancient Greek 'new' and 'formation, creation'. Types A neopla ...
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Competitive Inhibition
Competitive inhibition is interruption of a chemistry, chemical pathway owing to one chemical substance inhibiting the effect of another by competing with it for molecular binding, binding or chemical bond, bonding. Any metabolism, metabolic or chemical messenger (other), chemical messenger system can potentially be affected by this principle, but several classes of competitive inhibition are especially important in biochemistry and medicine, including the competitive form of enzyme inhibitor, enzyme inhibition, the competitive form of receptor antagonist, receptor antagonism, the competitive form of antimetabolite activity, and the competitive form of poisoning (which can include any of the aforementioned types). Enzyme inhibition type In competitive inhibition of enzyme catalysis, binding of an inhibitor prevents binding of the target molecule of the enzyme, also known as the substrate. This is accomplished by blocking the binding site of the substrate – the active si ...
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Small-molecule
In molecular biology and pharmacology, a small molecule or micromolecule is a low molecular weight (≤ 1000 daltons) organic compound that may regulate a biological process, with a size on the order of 1 nm. Many drugs are small molecules; the terms are equivalent in the literature. Larger structures such as nucleic acids and proteins, and many polysaccharides are not small molecules, although their constituent monomers (ribo- or deoxyribonucleotides, amino acids, and monosaccharides, respectively) are often considered small molecules. Small molecules may be used as research tools to probe biological function as well as leads in the development of new therapeutic agents. Some can inhibit a specific function of a protein or disrupt protein–protein interactions. Pharmacology usually restricts the term "small molecule" to molecules that bind specific biological macromolecules and act as an effector, altering the activity or function of the target. Small molecules can have ...
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Relugolix
Relugolix, sold under the brand names Orgovyx and Relumina among others, is a gonadotropin-releasing hormone antagonist (GnRH receptor antagonist) medication which is used in the treatment of prostate cancer, uterine fibroids and endometriosis. It is taken oral administration, by mouth. Side effects of relugolix include menstrual abnormalities, hot flashes, hyperhidrosis, excessive sweating, headache, and Osteoporosis, decreased bone mineral density. Relugolix is a GnRH antagonist, or an receptor antagonist, antagonist of the gonadotropin-releasing hormone receptor. Unlike most other GnRH modulators, but similarly to elagolix (brand name Orilissa), relugolix is a non-peptide, small-molecule chemical compound, compound and is oral administration, orally active. It suppresses sex hormone levels to the menopause, postmenopausal or castration, castrate range in both women and men. Medical uses Relugolix is approved in the United States, Canada and the United Kingdom for the treatm ...
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Elagolix
Elagolix, sold under the brand name Orilissa, is a gonadotropin-releasing hormone antagonist (GnRH antagonist) medication which is used in the treatment of pain associated with endometriosis in women. It is also under development for the treatment of uterine fibroids and menorrhagia, heavy menstrual bleeding in women. The medication was under investigation for the treatment of prostate cancer and benign prostatic hyperplasia, enlarged prostate in men as well, but development for these conditions was discontinued. Elagolix is taken oral administration, by mouth once or twice per day. It can be taken for up to 6 to 24 months, depending on the dosage. Side effects of elagolix include menopausal symptoms, menopausal-like symptoms such as hot flashes, night sweats, insomnia, amenorrhea, mood (psychology), mood changes, anxiety, and decreased bone mineral density, bone density, among others. Elagolix is a GnRH antagonist, or an receptor antagonist, antagonist of the gonadotropin- ...
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