U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 621 - 630 of 1075 results

Status:
US Previously Marketed
First approved in 1954

Class (Stereo):
CHEMICAL (ABSOLUTE)



Digoxin is a cardiac glycoside derived from the purple foxglove flower. In 1785, the English chemist, botanist, and physician Sir William Withering published his findings that Digitalis purpurea could be used to treat cardiac dropsy (congestive heart failure; CHF). Digoxin has been in use for many years, but was not approved by the FDA for treatment of heart failure (HF) until the late 1990s. Another FDA indication for digoxin is atrial fibrillation (AF). Digoxin also has numerous off-label uses, such as in fetal tachycardia, supra-ventricular tachycardia, cor pulmonale, and pulmonary hypertension. Digitoxin inhibits the Na-K-ATPase membrane pump, resulting in an increase in intracellular sodium and calcium concentrations. Increased intracellular concentrations of calcium may promote activation of contractile proteins (e.g., actin, myosin). Digoxin also has Para sympathomimetic properties. By increasing vagal tone in the sinoatrial and atrioventricular (AV) nodes, it slows the heart rate and AV nodal conduction.
Status:
US Previously Marketed
Source:
Aminopterin Sodium by Lederle
(1952)
Source URL:
First approved in 1952
Source:
Aminopterin Sodium by Lederle
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



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.
Status:
US Previously Marketed
First approved in 1951

Class (Stereo):
CHEMICAL (RACEMIC)



Dyphylline is 7-(2,3-dihydroxypropyl)-theophylline, a white, extremely bitter, amorphous powder that is freely soluble in water and soluble in alcohol. Dyphylline is stable in gastrointestinal fluids over a wide range of pH. Dyphylline is a xanthine derivative with pharmacologic actions similar to theophylline and other members of this class of drugs. Its primary action is that of bronchodilation, but it also exhibits peripheral vasodilatory and other smooth muscle relaxant activity to a lesser degree. The bronchodilatory action of dyphylline, as with other xanthines, is thought to be mediated through competitive inhibition of phosphodiesterase with a resulting increase in cyclic AMP producing relaxation of the bronchial smooth muscle. Dyphylline exerts its bronchodilatory effects directly and, unlike theophylline, is excreted unchanged by the kidneys without being metabolized by the liver. Because of this, dyphylline pharmacokinetics and plasma levels are not influenced by various factors that affect liver function and hepatic enzyme activity, such as smoking, age, congestive heart failure, or concomitant use of drugs which affect liver function.
Edrophonium is a short and rapid-acting cholinergic drug. Chemically, edrophonium is ethyl (m-hydroxyphenyl) dimethylammonium. Edrophonium is used for the differential diagnosis of myasthenia gravis and as an adjunct in the evaluation of treatment requirements in this disease. It may also be used for evaluating emergency treatment in myasthenic crises. Because of its brief duration of action, it is not recommended for maintenance therapy in myasthenia gravis. It is also useful whenever a curare antagonist is needed to reverse the neuromuscular block produced by curare, tubocurarine, gallamine triethiodide or dimethyl-tubocurarine. It is not effective against decamethonium bromide and succinylcholine chloride. It may be used adjunctively in the treatment of respiratory depression caused by curare overdosage.
Status:
US Previously Marketed
Source:
Floropryl by Merck
(1949)
Source URL:
First approved in 1949
Source:
Floropryl by Merck
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Isofluorophate (diisopropyl fluorophosphate) is an irreversile acetylcholinesterase inhibitor. It was used in ophthalmology as a miotic agent in treatment of chronic glaucoma.
Status:
US Previously Marketed
Source:
Thiouracil by Lilly
(1946)
Source URL:
First approved in 1946
Source:
Thiouracil by Lilly
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Thiouracil or 2-thiouracil was introduced in 1943 as the first thionamide anti-thyroid drug. Owing to a high frequency of adverse reactions, especially agranulocytosis, use of thiouracil was abandoned in favor of other, less toxic drugs. Thiouracil is not currently used as a thyrostatic drug in humans. Thiouracil inhibits thyroid activity by blocking the enzyme thyroid peroxidase. It is also it is a highly selective inhibitor of neuronal nitric oxide synthase, by interfering with the substrate- and tetrahydrobiopterin (BH(4))-binding to the enzyme. Due to its ability selectively accumulating in de novo-synthesized melanin in overactive melanin-producing cells and thus providing a means to localize melanoma cells, thiouracil can represent a useful new tool to identify modulators of human hair pigmentation.
Status:
US Previously Marketed
Source:
Furmethide by Smith Kline & French
(1944)
Source URL:
First approved in 1944
Source:
Furmethide by Smith Kline & French
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

FURTRETHONIUM is an agonist of muscarinic acetylcholine receptors. It was used for the treatment of glaucoma.
Glycyrrhizic Acid is specific compound isolated from licorice plants. Ammonium Glycyrrhizate (also known as GLYCYRRHIZIN, AMMONIATED) is a salt, was investigated to be a safe and is used as ingredient in the formulation of makeup, fragrance, hair care, skin care, shaving, personal hygiene and suntan products.
Status:
US Previously Marketed
Source:
Physostigmine Salicylate U.S.P.
(1921)
Source URL:
First marketed in 1921
Source:
Physostigmine Salicylate U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Physostigmine (Phy) is one of the oldest drug isolated from Calabar beans and successfully used for the treatment of glaucoma in 1864. Since then, it has been widely employed for various therapeutic purposes. Recently, it has gained prominence because of its clinical trials in the treatment of Alzheimer's disease. Physostigmine was used to treat glaucoma. It can be applied topically to the conjunctiva. Phy is also considered to be a potent prophylactic antidote for organophosphate poisoning. It is a reversible cholinesterase (ChE) inhibitor and has a short duration of action. For the last 50 years, numerous authors have shown that pretreatment with Phy would rapidly improve the incapacitating effects of organophosphate intoxication in various animal species. Phy carbamylates to a portion of ChE enzyme and thus protects the enzyme from binding with organophosphate, which are irreversible ChE inhibitors. The carbamylated ChE enzyme decarbamylates to free the enzyme for normal functioning. The rates of decarbamylation of butyrylcholinesterase (BuChE) in plasma and ChE in brain and muscle are different and are related to the half-life of Phy in these tissues. In addition to ChE inhibition, Phy has a direct action on acetylcholine (ACh) receptor ionophore complex by interacting with the ACh-gated cation channels. A cholinesterase inhibitor that is rapidly absorbed through membranes. It also can cross the blood-brain barrier and is used when central nervous system effects are desired, as in the treatment of severe anticholinergic toxicity.
Status:
Possibly Marketed Outside US
Source:
NCT02812043: Phase 4 Interventional Completed Non-dermatophyte Onychomycosis
(2016)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Amorolfine (or amorolfin), is a morpholine antifungal drug with broad spectrum of activity. Its fungicidal action is based on an alteration of the fungal cell membrane targeted primarily on sterol biosynthesis. Amorolfine is administered as a nail lacquer in patients suffering from onychomycosis, as a cream in patients suffering from dermatomycosis. Amorolfine is well tolerated. The local adverse effects observed were mainly burning and itching.