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Restrict the search for
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Status:
US Previously Marketed
Source:
HUMORSOL by MERCK
(1959)
Source URL:
First approved in 1959
Source:
HUMORSOL by MERCK
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Demecarium (HUMORSOL®) is an indirect-acting parasympathomimetic agent, also known as a cholinesterase inhibitor and anticholinesterase. Cholinesterase inhibitors prolong the effect of acetylcholine, which is released at the neuroeffector junction of parasympathetic postganglion nerves, by inactivating the cholinesterases that break it down. Application of demecarium (HUMORSOL®) to the eye produces intense miosis and ciliary muscle contraction due to inhibition of cholinesterase, allowing acetylcholine to accumulate at sites of cholinergic transmission. These effects are accompanied by increased capillary permeability of the ciliary body and iris, increased permeability of the blood-aqueous barrier, and vasodilation. Myopia may be induced or, if present, may be augmented by the increased refractive power of the lens that results from the accommodative effect of the drug. Demecarium (HUMORSOL®) indirectly produces some of the muscarinic and nicotinic effects of acetylcholine as quantities of the latter accumulate.
Status:
US Previously Marketed
Source:
COMBID ISOPROPAMIDE by SKF
(1961)
Source URL:
First approved in 1957
Source:
DARBID by GLAXOSMITHKLINE
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Isopropamide is a quaternary ammonium antimuscarinic with peripheral effects similar to those of atropine. It has been used as an adjunct in the treatment of peptic ulcer disease, in the relief of gastro-intestinal and urinary tract disorders associated with smooth muscle spasm, in rhinitis, and the relief of symptoms of cold.
Status:
US Previously Marketed
Source:
CAMOFORM by PD
(1961)
Source URL:
First approved in 1956
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
BIALAMICOL is a hydroxybiphenyl antiprotozoal used for the treatment of acute and chronic amoebiasis.
Status:
US Previously Marketed
Source:
CENTRINE/PHENOBARBITAL AMINOPENTAMIDE HYDROGEN SULFATE by BRISTOL LABS
(1961)
Source URL:
First approved in 1953
Class (Stereo):
CHEMICAL (UNKNOWN)
Conditions:
Aminopentamide is a potent antispasmodic agent. As a cholinergic blocking agent for smooth muscle, its action is similar to atropine. Aminopentamide hydrogen sulfate is marketed under the brand name Centrine indicated in the treatment of acute abdominal visceral spasm, pylorospasm or hypertrophic gastritis and associated nausea, vomiting and/or diarrhea of the dogs and cats. Centrine effectively reduces the tone and amplitude of colonic contractions to a greater degree and for a more extended period than does atropine. Centrine effects a reduction in gastric secretion, a decrease in gastric acidity and a marked decrease in gastric motility. Aminopentamide is a nonselective muscarinic cholinergic .
Status:
US Previously Marketed
Source:
QUERTINE by ABBOTT
(1961)
Source URL:
First approved in 1953
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Quercetin is a unique bioflavonoid that has been extensively studied by researchers over the past 30 years. Quercetin, the most abundant of the flavonoids (the name comes from the Latin –quercetum, meaning oak forest, quercus oak) consists of 3 rings and 5 hydroxyl groups. Quercetin is a member of the class of flavonoids called flavonoles and forms the backbone for many other flavonoids including the citrus flavonoids like rutin, hesperidins, Naringenin and tangeritin. It is widely distributed in the plant kingdom in rinds and barks. The best described property of Quercetin is its ability to act as antioxidant. Quercetin seems to be the most powerful flavonoids for protecting the body against reactive oxygen species, produced during the normal oxygen metabolism or are induced by exogenous damage [9, 10]. One of the most important mechanisms and the sequence of events by which free radicals interfere with the cellular functions seem to be the lipid peroxidation leading eventually the cell death. To protect this cellular death to happen from reactive oxygen species, living organisms have developed antioxidant line of defense systems [11]. These include enzymatic and non-enzymatic antioxidants that keep in check ROS/RNS level and repair oxidative cellular damage. The major enzymes, constituting the first line of defence, directly involved in the neutralization of ROS/RNS are: superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GPx) The second line of defence is represented by radical scavenging antioxidants such as vitamin C, vitamin A and plant phytochemicals including quercetin that inhibit the oxidation chain initiation and prevent chain propagation. This may also include the termination of a chain by the reaction of two radicals. The repair and de novo enzymes act as the third line of defence by repairing damage and reconstituting membranes. These include lipases, proteases, DNA repair enzymes and transferases. Quercetin is a specific quinone reductase 2 (QR2) inhibitor, an enzyme (along with the human QR1 homolog) which catalyzes metabolism of toxic quinolines. Inhibition of QR2 in plasmodium may potentially cause lethal oxidative stress. The inhibition of antioxidant activity in plasmodium may contribute to killing the malaria causing parasites.
Status:
US Previously Marketed
Source:
CENTRINE/PHENOBARBITAL AMINOPENTAMIDE HYDROGEN SULFATE by BRISTOL LABS
(1961)
Source URL:
First approved in 1953
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Aminopentamide is a potent antispasmodic agent. As a cholinergic blocking agent for smooth muscle, its action is similar to atropine. Aminopentamide hydrogen sulfate is marketed under the brand name Centrine indicated in the treatment of acute abdominal visceral spasm, pylorospasm or hypertrophic gastritis and associated nausea, vomiting and/or diarrhea of the dogs and cats. Centrine effectively reduces the tone and amplitude of colonic contractions to a greater degree and for a more extended period than does atropine. Centrine effects a reduction in gastric secretion, a decrease in gastric acidity and a marked decrease in gastric motility. Aminopentamide is a nonselective muscarinic cholinergic .
Status:
US Previously Marketed
Source:
CENTRINE/PHENOBARBITAL AMINOPENTAMIDE HYDROGEN SULFATE by BRISTOL LABS
(1961)
Source URL:
First approved in 1953
Class (Stereo):
CHEMICAL (UNKNOWN)
Conditions:
Aminopentamide is a potent antispasmodic agent. As a cholinergic blocking agent for smooth muscle, its action is similar to atropine. Aminopentamide hydrogen sulfate is marketed under the brand name Centrine indicated in the treatment of acute abdominal visceral spasm, pylorospasm or hypertrophic gastritis and associated nausea, vomiting and/or diarrhea of the dogs and cats. Centrine effectively reduces the tone and amplitude of colonic contractions to a greater degree and for a more extended period than does atropine. Centrine effects a reduction in gastric secretion, a decrease in gastric acidity and a marked decrease in gastric motility. Aminopentamide is a nonselective muscarinic cholinergic .
Status:
US Previously Marketed
Source:
CENTRINE/PHENOBARBITAL AMINOPENTAMIDE HYDROGEN SULFATE by BRISTOL LABS
(1961)
Source URL:
First approved in 1953
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Aminopentamide is a potent antispasmodic agent. As a cholinergic blocking agent for smooth muscle, its action is similar to atropine. Aminopentamide hydrogen sulfate is marketed under the brand name Centrine indicated in the treatment of acute abdominal visceral spasm, pylorospasm or hypertrophic gastritis and associated nausea, vomiting and/or diarrhea of the dogs and cats. Centrine effectively reduces the tone and amplitude of colonic contractions to a greater degree and for a more extended period than does atropine. Centrine effects a reduction in gastric secretion, a decrease in gastric acidity and a marked decrease in gastric motility. Aminopentamide is a nonselective muscarinic cholinergic .
Status:
US Previously Marketed
Source:
CENTRINE/PHENOBARBITAL AMINOPENTAMIDE HYDROGEN SULFATE by BRISTOL LABS
(1961)
Source URL:
First approved in 1953
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Aminopentamide is a potent antispasmodic agent. As a cholinergic blocking agent for smooth muscle, its action is similar to atropine. Aminopentamide hydrogen sulfate is marketed under the brand name Centrine indicated in the treatment of acute abdominal visceral spasm, pylorospasm or hypertrophic gastritis and associated nausea, vomiting and/or diarrhea of the dogs and cats. Centrine effectively reduces the tone and amplitude of colonic contractions to a greater degree and for a more extended period than does atropine. Centrine effects a reduction in gastric secretion, a decrease in gastric acidity and a marked decrease in gastric motility. Aminopentamide is a nonselective muscarinic cholinergic .
Status:
US Previously Marketed
First approved in 1952
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Aminopterin is a synthetic derivative of pterins with antineoplastic and immunosuppressive properties. As a folate analog, aminopterin competes for the folate binding site of the enzyme dihydrofolate reductase, thereby blocking tetrahydrofolate synthesis, and resulting in depletion of nucleotide precursors and inhibition of DNA, RNA and protein synthesis. Aminopterin was marketed by Lederle Laboratories (Pearl River, New York) in the United States from 1953 to 1964 for the indication of pediatric leukemia. The closely related antifolate methotrexate was simultaneously marketed by the company during the same period. Aminopterin was discontinued by Lederle Laboratories in favor of methotrexate due to manufacturing difficulties of the former. During the period Aminopterin was marketed, the agent was used off-label to safely treat over 4,000 patients with psoriasis in the United States, producing dramatic clearing of lesions. The use of aminopterin in cancer treatment was supplanted in the 1950s by methotrexate due to the latter's better therapeutic index in a rodent tumor model. Now in a more pure preparation and supported by laboratory evidence of superior tumor cell uptake in vitro, aminopterin is being investigated in clinical trials in leukemia as a potentially superior antifolate to methotrexate.