Prolactin Releasers
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Prolactin Releasers
A prolactin modulator is a drug which affects the hypothalamic–pituitary–prolactin axis (HPP axis) by modulating the secretion of the pituitary hormone prolactin from the anterior pituitary, anterior pituitary gland. ''Prolactin inhibitors'' suppress and ''prolactin releasers'' induce the secretion of prolactin, respectively. Prolactin inhibitors Prolactin inhibitors are mainly used to treat hyperprolactinemia (high prolactin levels). Agonists of the dopamine D2 receptor, D2 receptor such as bromocriptine and cabergoline are able to strongly suppress pituitary prolactin secretion and thereby decrease circulating prolactin levels, and so are most commonly used as prolactin inhibitors. D2 receptor agonists that are described as prolactin inhibitors include the approved medications bromocriptine, cabergoline, lisuride, metergoline, pergolide, quinagolide, and terguride and the never-marketed agent lergotrile. Other dopamine agonists and dopaminergic agents, for instance levodopa ...
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Bromocriptine
Bromocriptine, originally marketed as Parlodel and subsequently under many brand names, is an ergoline derivative and dopamine agonist that is used in the treatment of pituitary tumors, Parkinson's disease, hyperprolactinaemia, neuroleptic malignant syndrome, and, as an adjunct, Diabetes mellitus type 2, type 2 diabetes. It was patented in 1968 and approved for medical use in 1975. Medical uses Bromocriptine is used to treat acromegaly and conditions associated with hyperprolactinemia like amenorrhea, infertility, hypogonadism, and prolactin-secreting adenomas. It is also used to prevent ovarian hyperstimulation syndrome For label updates seFDA index page for NDA 017962 and to treat Parkinson's disease. Since the late 1980s it has been used, off-label, to reduce the symptoms of cocaine withdrawal but the evidence for this use is poor. Bromocriptine has been successfully used in cases of galactorrhea precipitated by dopamine antagonists like risperidone. A quick-release formul ...
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Pergolide
Pergolide, sold under the brand name Permax and Prascend (veterinary) among others, is an ergoline-based dopamine receptor agonist used in some countries for the treatment of Parkinson's disease. Parkinson's disease is associated with reduced dopamine synthesis in the substantia nigra of the brain. Pergolide acts on many of the same receptors as dopamine to increase receptor activity. It was patented in 1978 and approved for medical use in 1989. In 2007, pergolide was withdrawn from the U.S. market for human use after several published studies revealed a link between the drug and increased rates of valvular heart disease. However, a veterinary form of pergolide, marketed under the trade name Prascend, is permitted for the treatment of pituitary pars intermedia dysfunction (PPID) also known as equine Cushing's syndrome (ECS) in horses. Medical uses Pergolide is no longer available for use by humans in the United States, however, it is still used in various other countries, wher ...
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Mammoplasia
Mammoplasia is the normal or spontaneous enlargement of human breasts. Mammoplasia occurs normally during puberty and pregnancy in women, as well as during certain periods of the menstrual cycle. When it occurs in males, it is called gynecomastia and is considered to be pathological. When it occurs in females and is extremely excessive, it is called macromastia (also known as gigantomastia or breast hypertrophy) and is similarly considered to be pathological. Mammoplasia may be due to breast engorgement, which is temporary enlargement of the breasts caused by the production and storage of breast milk in association with lactation and/or galactorrhea (excessive or inappropriate production of milk). Mastodynia (breast tenderness/pain) frequently co-occurs with mammoplasia. During the luteal phase (latter half) of the menstrual cycle, due to increased mammary blood flow and/or premenstrual fluid retention caused by high circulating concentrations of estrogen and/or progesterone ...
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Side Effect
In medicine, a side effect is an effect of the use of a medicinal drug or other treatment, usually adverse but sometimes beneficial, that is unintended. Herbal and traditional medicines also have side effects. A drug or procedure usually used for a specific effect may be used specifically because of a beneficial side-effect; this is termed " off-label use" until such use is approved. For instance, X-rays have long been used as an imaging technique; the discovery of their oncolytic capability led to their use in radiotherapy for ablation of malignant tumours. Frequency of side effects The World Health Organization and other health organisations characterise the probability of experiencing side effects as: * Very common, ≥ 1⁄10 * Common (frequent), 1⁄10 to 1⁄100 * Uncommon (infrequent), 1⁄100 to 1⁄1000 * Rare, 1⁄1000 to 1⁄10000 * Very rare, < 110000 The

Hypoprolactinemia
Hypoprolactinemia is a medical condition characterized by a deficiency in the serum levels of the hypothalamic-pituitary hormone prolactin. Signs and symptoms Hypoprolactinemia is associated with ovarian dysfunction in women, and, in men, metabolic syndrome, anxiety symptoms, arteriogenic erectile dysfunction, premature ejaculation, oligozoospermia (low concentration of sperm in semen), asthenospermia (reduced sperm motility), hypofunction of seminal vesicles, and hypoandrogenism. In one study, normal sperm characteristics were restored when prolactin levels were brought up to normal values in men with hypoprolactinemia. Hypoprolactinemia can be a cause of lactation failure after childbirth. Causes Hypoprolactinemia can result from autoimmune disease, hypopituitarism, growth hormone deficiency, hypothyroidism, excessive dopamine action in the tuberoinfundibular pathway and/or the anterior pituitary, and ingestion of drugs that activate the D2 receptor, such as direct D2 r ...
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Metoclopramide
Metoclopramide is a medication used to treat nausea, vomiting, gastroparesis, and gastroesophageal reflux disease. It is also used to treat migraine headaches. Common side effects include feeling tired, diarrhea, akathisia, and tardive dyskinesia. More serious side effects include neuroleptic malignant syndrome and depression. It is thus rarely recommended that people take the medication for longer than twelve weeks. No evidence of harm has been found after being taken by many pregnant women. It belongs to the group of medications known as dopamine-receptor antagonists and works as a prokinetic. In 2012, metoclopramide was one of the top 100 most prescribed medications in the United States. It is available as a generic medication. It is on the WHO Model List of Essential Medicines, World Health Organization's List of Essential Medicines. In 2022, it was the 245th most commonly prescribed medication in the United States, with more than 1million prescriptions. Medical uses ...
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Domperidone
Domperidone, sold under the brand name Motilium among others, is a dopamine antagonist medication which is used to treat nausea and vomiting and certain gastrointestinal problems like gastroparesis (delayed gastric emptying). It raises the level of prolactin in the human body and is used off label to induce and promote breast milk production. It may be taken by mouth or rectally. Side effects may include headache, anxiety, dry mouth, abdominal cramps, diarrhea, and elevated prolactin levels. Secondary to increased prolactin levels, breast changes, milk outflow, menstrual irregularities, and hypogonadism can occur. Domperidone may also cause QT prolongation and has rarely been associated with serious cardiac complications such as sudden cardiac death. However, the risks are small and occur more with high doses. Domperidone acts as a peripherally selective antagonist of the dopamine D2 and D3 receptors. Due to its low entry into the brain, the side effects of ...
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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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GnRH Analogue
A GnRH modulator, or GnRH receptor modulator, also known as an LHRH modulator or LHRH receptor modulator, is a type of medication which modulates the GnRH receptor, the biological target of the hypothalamic hormone gonadotropin-releasing hormone (GnRH; also known as luteinizing-releasing hormone, or LHRH). They include GnRH agonists and GnRH antagonists. These medications may be GnRH analogues like leuprorelin and cetrorelix – peptides that are structurally related to GnRH – or small-molecules like elagolix and relugolix, which are structurally distinct from and unrelated to GnRH analogues. GnRH modulators affect the secretion of the gonadotropins, luteinizing hormone (LH) and follicle-stimulating hormone (FSH), which in turn affects the gonads, influencing their function and hence fertility as well as the production of sex steroids, including that of estradiol and progesterone in women and of testosterone in men. As such, GnRH modulators can also be described a ...
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Aromatase Inhibitor
Aromatase inhibitors (AIs) are a class of drugs used in the treatment of breast cancer in postmenopausal women and in men, and gynecomastia in men. They may also be used off-label to reduce estrogen conversion when supplementing testosterone exogenously. They may also be used for chemoprevention in women at high risk for breast cancer. Aromatase is the enzyme that catalyzes a key aromatization step in the synthesis of estrogen. It converts the enone ring of androgen precursors such as testosterone, to a phenol, completing the synthesis of estrogen. As such, AIs are estrogen synthesis inhibitors. Because hormone-positive breast and ovarian cancers are dependent on estrogen for growth, AIs are taken to either block the production of estrogen or block the action of estrogen on receptors. Medical uses Cancer In contrast to premenopausal women, in whom most of the estrogen is produced in the ovaries, in postmenopausal women estrogen is mainly produced in peripheral tissues of th ...
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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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Levodopa
Levodopa, also known as L-DOPA and sold under many brand names, is a dopaminergic medication which is used in the treatment of Parkinson's disease (PD) and certain other conditions like dopamine-responsive dystonia and restless legs syndrome. The drug is usually used and formulated in combination with a peripherally selective aromatic L-amino acid decarboxylase (AAAD) inhibitor like carbidopa or benserazide. Levodopa is taken by mouth, by inhalation, through an intestinal tube, or by administration into fat (as foslevodopa). Side effects of levodopa include nausea, the wearing-off phenomenon, dopamine dysregulation syndrome, and levodopa-induced dyskinesia, among others. The drug is a centrally permeable monoamine precursor and prodrug of dopamine and hence acts as a dopamine receptor agonist. Chemically, levodopa is an amino acid, a phenethylamine, and a catecholamine. The major reason for enhanced risks for levodopa induced dyskinesia (LID) and OFF phases durin ...
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