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Nequinate
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DB11433 |
[Nequinate is an antiprotozoan used as a coccidiostat for poultry and rabbits. Nequinate belongs to the family of Hydroquinolones. These are compounds containing an hydrogenated quinoline bearing a ketone group.] |
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Narasin
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DB11432 |
[Narasin is an agent with coccidiostatic and antibacterial properties.] |
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GW-493838
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DB12760 |
[GW493838 has been used in trials studying the treatment of Neuropathic Pain.] |
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Timcodar
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DB12761 |
[Timcodar has been used in trials studying the treatment of Unspecified Adult Solid Tumor, Protocol Specific.] |
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Moxidectin
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DB11431 |
[Moxidectin is a potent, broad-spectrum endectocide (antiparasitic that is active against endo- and ecto-parasites) with activity against nematodes, insects, and acari. It was first used in cattle followed by an approved use in general animals. It is a semi-synthetic methoxine derivative of nemadectin which is a 16-member pentacyclic lactone of the milbemycin class. Moxidectin differs by the absence of a disaccharide moiety on carbon 13, a substituted olefinic side chain at carbon 25 and a unique methoxime moiety at carbon 23. Due to these modifications, moxidectin is classified as a second generation macrocyclic lactone.[A33385] Moxidectin was developed by Medicines Development for Global Health and FDA approved in June 13, 2018.[L2970]] |
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Naproxen
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DB00788 |
[Naproxen is classified as a nonsteroidal anti-inflammatory dug (NSAID) and was initially approved for prescription use in 1976 and then for over-the-counter (OTC) use in 1994.[A178975] It can effectively manage acute pain as well as pain related to rheumatic diseases, and has a well studied adverse effect profile.[A179098] Given it's overall tolerability and effectiveness, naproxen can be considered a first line treatment for a variety of clinical situations requiring analgesia.[A179098] Naproxen is available in both immediate and delayed release formulations, in combination with sumatriptan to treat migraines, and in combination with esomeprazole to lower the risk of developing gastric ulcers.[L6582][L6583][L7309][L7312]] |
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Acyclovir
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DB00787 |
[Acyclovir is a nucleotide analog antiviral used to treat herpes simplex, _Varicella zoster_, herpes zoster, herpes labialis, and acute herpetic keratitis[L7303,L7315,L7318,L7321,L7324,L7327]. Acyclovir is generally used first line in the treatment of these viruses and some products are indicated for patients as young as 6 years old.[L7321]
Acyclovir was granted FDA approval on 29 March 1982.[L7318]] |
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Gadopentetic acid
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DB00789 |
[A complex of gadolinium with a chelating agent, diethylenetriamine penta-acetic acid (DTPA see pentetic acid), that is given to enhance the image in cranial and spinal MRIs. (From Martindale, The Extra Pharmacopoeia, 30th ed, p706)] |
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Coenzyme M
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DB09110 |
[Coenzyme M (commonly known by its salt form, Mesna) is a synthetic sulfhydryl (thiol) compound and is used for prophylaxis of Ifosfamide and cyclophosphamide induced hemorrhagic cystitis.[A18572]] |
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Mefenamic acid
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DB00784 |
[A non-steroidal anti-inflammatory agent with analgesic, anti-inflammatory, and antipyretic properties. It is an inhibitor of cyclooxygenase.] |
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Estradiol
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DB00783 |
[Estradiol (also known as E2 or 17β-estradiol) is a naturally occurring hormone that circulates endogenously within the human body. It is the most potent form of mammalian estrogenic steroids and acts as the major female sex hormone. As such, estradiol plays an essential role in the regulation of the menstrual cycle, in the development of puberty and secondary female sex characteristics, as well as in ageing and several hormonally-mediated disease states. Estrogen mediates its effects across the body through potent agonism of the Estrogen Receptor (ER), which is located in various tissues including in the breasts, uterus, ovaries, skin, prostate, bone, fat, and brain. Estradiol binds to both subtypes of the Estrogen Receptor: Estrogen Receptor Alpha (ERα) and Estrogen Receptor Beta (ERβ). Estradiol also acts as a potent agonist of G Protein-coupled Estrogen Receptor (GPER), which has recently been recognized as a major mediator of estradiol's rapid cellular effects [A31620].
Estradiol is commercially available in several hormone therapy products for managing conditions associated with reduced estrogen production such as menopausal and peri-menopausal symptoms as well as hypoestrogenism. It is also used in transgender hormone therapy, as a component of oral contraceptive pills for preventing pregnancy (most commonly as [DB00977], a synthetic form of estradiol), and is sometimes used for the palliative treatment of some hormone-sensitive cancers like breast and prostate cancer. Estradiol is available in a number of formulations including oral, transdermal, and injectable.
The primary source of estrogen in normally cycling adult women is the ovarian follicle, which secretes 70 to 500 mcg of estradiol daily, depending on the phase of the menstrual cycle. However, after menopause, most endogenous estrogen is produced by conversion of androstenedione, secreted by the adrenal cortex, to estrone by peripheral tissues. Thus, estrone and the sulphate conjugated form, estrone sulphate, are the most abundant circulating estrogens in postmenopausal women [FDA Label]. Although circulating estrogens exist in a dynamic equilibrium of metabolic interconversions, estradiol is the principal intracellular human estrogen and is substantially more potent than its metabolites, estrone and estriol at the receptor level. Because of the difference in potency between estradiol and estrone, menopause (and a change in primary hormone from estradiol to estrone) is associated with a number of symptoms associated with this reduction in potency and in estrogenic effects. These include hot flashes, vaginal dryness, mood changes, irregular menses, chills, and sleeping problems.
When used for oral or IM administration, estradiol is commonly synthesized as a pro-drug ester (such as [DB13952], [DB13953], [DB13954], [DB13955], and [DB13956]). It is commonly produced with an ester side-chain as endogenous estradiol has very low oral bioavailability on its own (2-10%). First-pass metabolism by the gut and the liver quickly degrades the estradiol molecule before it gets a chance to enter the systemic circulation and exert its estrogenic effects [A12102]. Esterification of estradiol aims to improve absorption after oral administration (such as with Estradiol valerate) or to sustain release from intramuscular depot injections (such as with Estradiol Cypionate) through improved lipophilicity [T84]. Following absorption, the esters are cleaved, resulting in the release of endogenous estradiol, or 17β-estradiol.
Recommendations for treatment of menopausal symptoms changed drastically following the release of results and early termination of the Women's Health Initiative (WHI) studies in 2002 as a number of concerns were raised regarding the use of estrogen [A31626]. Specifically, the combined estrogen–progestin arm was discontinued after approximately five years of follow up due to a statistically significant increase in invasive breast cancer and in cardiovascular events [A31627]. Following extensive critique of the WHI results in the years following its release, Hormone Replacement Therapy (HRT) is now recommended to be used only for a short period (for 3-5 years post-menopause) in low doses, and in women without a history of breast cancer or at increased risk of cardiovascular or thromboembolic disease [A31628]. Notably, use of estrogen for menopausal symptoms should always be accompanied by a progestin component due to estrogen's effects on the endometrium; in women with an intact uterus, unopposed estrogen has been shown to promote the growth of the endometrium which can lead to endometrial hyperplasia and possibly cancer in the long-term.
[DB00977] (EE) is a synthetic form of estradiol commonly used as the estrogenic component of most combination Oral Contraceptive Pills (OCPs). Ethinyl Estradiol differs from Estradiol in that it has improved biovailability and greater resistance to metabolism, making it more suitable for oral administration.] |
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Nitrous acid
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DB09112 |
[Nitrous acid (as sodium nitrite) is used as part of an intravenous mixture with sodium thiosulfate to treat cyanide poisoning. It is on the World Health Organization's List of Essential Medicines, a list of the most important medications needed in a basic health system. There is also research to investigate its applicability towards treatments for heart attacks, brain aneurysms, pulmonary hypertension in infants, and Pseudomonas aeruginosa infections.] |
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Marimastat
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DB00786 |
[Used in the treatment of cancer, Marmiastat is an angiogenesis and metastasis inhibitor. As an angiogenesis inhibitor it limits the growth and production of blood vessels. As an antimetatstatic agent it prevents malignant cells from breaching the basement membranes.] |
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Pentastarch
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DB09111 |
[Pentastarch is an artificial colloid (hydroxyethyl starch derivative). Pentastarch is characterized by presenting five hydroxyethyl groups, which signifies an approximate 50% hydroxyethylation. It is sold under the name Pentaspan by Bristol-Myers Squibb and is used for fluid resuscitation. When administered, pentastarch remains mainly in the circulatory system and hence, it is considered a plasma expander.] |
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Cryptenamine
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DB00785 |
[Cryptenamine is a mixture of closely related hypotensive alkaloids from Veratrum album (Liliaceae). It has been used in the treatment of hypertension but has largely been replaced by drugs with fewer adverse effects. Cryptenamine has a marked and re-producible depressor effect when given intravenously to hypertensive patients, however the mechanism of action is not known.] |
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Colfosceril palmitate
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DB09114 |
[Colfosceril palmitate is a synthetic pulmonary surfactant administered in infants with respiratory distress syndrome.[A31510] It was part of the first generation of commercially available artificial surfactants.[T70] It was developed by Burroughs Wellcome and it was FDA approved on August 6, 1990.[L1109] Nowadays colfosceril palmitate is under the state of canceled post-marketing.] |
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Phenelzine
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DB00780 |
[Phenelzine, with the formula β-phenylethylhydrazine, is a monoamine oxidase inhibiting antidepressant that is effective in the treatment of panic disorder and social anxiety disorder.[A15753] It was developed by Parke Davis and originally FDA approved on June 9th, 1961. It is currently approved under prescription by the name of Nardil.] |
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Poractant alfa
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DB09113 |
[Poractant alfa is a pulmonary surfactant marketed as Curosurf in the United States and Canada. It is used to treat Respiratory Distress Syndrome (RDS) in premature infants with an endogenous pulmonary surfactant deficiency. Poractant alfa is an extract of natural porcine lung surfactant consisting of 99% polar lipids (mainly phospholipids) and 1% hydrophobic low molecular weight proteins (surfactant associated proteins SP-B and SP-C). The phospholipid content of the extract consists primarily of phosphatidylcholine and dipaImitoylphosphatidylcholine. Poractant alfa is a creamy white suspension of this extract in 0.9% sodium chloride solution. It contains no preservatives.] |
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Propantheline
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DB00782 |
[A muscarinic antagonist used as an antispasmodic, in rhinitis, in urinary incontinence, and in the treatment of ulcers. At high doses it has nicotinic effects resulting in neuromuscular blocking.] |
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Calcium carbimide
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DB09116 |
[Calcium carbimide, sold as the citrate salt, is an alcohol-sensitizing agent. Its effects are similar to the drug disulfiram (Antabuse) in that it interferes with the normal metabolism of alcohol by preventing the breakdown of the metabolic product acetaldehyde. Calcium carbimide was conceived as an alternative for the treatment of alcoholism with a reduced side effect profile either when it is consumed accompanied by alcohol or without it.[A31516] This drug was developed by Lederle Cyanamid Canada Inc and approved for marketing in Canada in 1959. The current status of calcium carbimide is cancelled post marketing.[L1113]] |