{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
Status:
First approved in 1953
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
STANOLONE, also known as dihydrotestosterone, is a potent androgenic metabolite of testosterone and anabolic agent for systemic use. It may be used as a replacement of male sex steroids in men who have androgen deficiency, for example as a result of the loss of both testes, and also the treatment of certain rare forms of aplastic anemia which are or may be responsive to anabolic androgens.
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:
RAVOCAINE AND NOVOCAIN W/ LEVOPHED by EASTMAN KODAK
(1952)
Source URL:
First approved in 1952
Source:
RAVOCAINE AND NOVOCAIN W/ LEVOPHED by EASTMAN KODAK
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Propoxycaine hydrochloride is a local anesthetic of the ester type that has a rapid onset of action and a longer duration of action than procaine hydrochloride. Propoxycaine Hydrochloride is the hydrochloride salt form of propoxycaine, a para-aminobenzoic acid ester. Propoxycaine binds to and inhibits voltage-gated sodium channels, thereby inhibiting the ionic flux required for the initiation and conduction of impulses. This results in a loss of sensation.
Status:
US Previously Marketed
Source:
Hydergine by Sandoz
(1951)
Source URL:
First approved in 1951
Source:
Hydergine by Sandoz
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Dihydro-alpha-ergocryptine is an ergot alkaloid that has an agonist activity on D2 dopaminergic receptors and a partial agonist activity on D1 receptors. It also demonstrated antagonistic activity towards alpha-adrenergic receptors. The drug was approved by FDA in combination with other alkaloids (dihydroergocornine, dihydroergocristine and dihydro-beta-ergocryptine mesylate salts) under the name Hydergine for the treatment of dimentia and cerebrovascular insufficiency.
Status:
US Previously Marketed
Source:
HETRAZAN by LEDERLE
(1950)
Source URL:
First approved in 1950
Source:
HETRAZAN by LEDERLE
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Diethylcarbamazine is used in humans, dogs and cats for the treatment of parasitic infections, including pulmonary eosinophilia, loiasis, and lymphatic filariasis. The exact mechanism of its action is unknown, however some studies showed the involvment of inducible nitric-oxide synthase and the cyclooxygenase pathway. Although there is no information on whether the drug is marketed in the USA and Europe, it is currently used in India.
Status:
US Previously Marketed
Source:
CHLOROMYCETIN HYDROCORTISONE by PARKEDALE
(1953)
Source URL:
First approved in 1950
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Chloramphenicol is a broad-spectrum antibiotic that was first isolated from
Streptomyces venezuelae in 1947. The drug was subsequently chemically synthesized. It has both a bacteriostatic and bactericidal effect; in the usual therapeutic concentrations it is bacteriostatic. Chloramphenicol is used for the treatment of serious gram-negative, gram-positive, and anaerobic infections. It is especially useful in the treatment of meningitis, typhoid fever, and cystic fibrosis. It should be reserved for infections for which other drugs are ineffective or contraindicated. Chloramphenicol, a small inhibitor of bacterial protein synthesis, is active against a variety of bacteria and readily enters the CSF. It has been used extensively in the last decades for the treatment of bacterial meningitis. In industrialized countries, chloramphenicol is restricted mostly to topical uses because of the risk of induction of aplastic anemia. However, it remains a valuable reserve antibiotic for patients with allergy to β-lactam antibiotics or with CNS infections caused by multiresistant pathogens.
Status:
US Previously Marketed
First approved in 1950
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Khellin is a crystalline extract of a crude drug, which has long been used in Egypt for the treatment of ureteral colic. It is used in the management of bronchial asthma and angina pectoris. Interest in khellin as an adjunct to ultraviolet (UV) light therapy in the treatment of vitiligo is based on the structural similarity between khellin and the psoralens. Success has been reported using oral and topical khellin in clinical studies but it is not likely that khellin will be approved for the treatment of vitiligo. Unwanted side effects of khellin include dizziness, reversible cholestatic jaundice, pseudoallergic reaction, and elevated levels of liver enzymes (transaminases and gamma-glutamyltransferase).
Status:
First approved in 1948
Class (Stereo):
CHEMICAL (MIXED)
Conditions:
METHYLHEXANEAMINE, an amphetamine derivative, is also known as 1,3-dimethylamylamine (DMAA). It was introduced in 1948 as a nasal inhaler for allergic or infectious rhinitis. By the 1970s, it had been withdrawn from the market. DMAA is currently used as an ingredient in many sports performance and weight loss products. According to FDA, it is not a dietary ingredient, and DMAA-containing products marketed as dietary supplements are illegal and their marketing violates the law.
Status:
US Previously Marketed
Source:
TRIPLE SULFA by FOUGERA
(1985)
Source URL:
First approved in 1945
Source:
SULTRIN by ORTHO MCNEIL PHARM
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Sulfabenzamide is an antibacterial/antimicrobial. Often used in conjunction with sulfathiazole and sulfacetamide (trade name - Sultrin) as a topical, intravaginal antibacterial preparation against Haemophilus (Gardnerella) vaginalis bacteria. The mode of action of SULTRIN is not completely known. Indirect effects, such as lowering the vaginal pH, may be equally important mechanisms.
Status:
US Previously Marketed
Source:
TUBOCURARINE CHLORIDE by BRISTOL MYERS SQUIBB
(1945)
Source URL:
First approved in 1945
Source:
TUBOCURARINE CHLORIDE by BRISTOL MYERS SQUIBB
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Tubocurarine, a naturally occurring alkaloid, is used to treat smoking withdrawl syndrom. Tubocurarine, the chief alkaloid in tobacco products, binds stereo-selectively to nicotinic-cholinergic receptors at the autonomic ganglia, in the adrenal medulla, at neuromuscular junctions, and in the brain. Two types of central nervous system effects are believed to be the basis of Tubocurarine's positively reinforcing properties. A stimulating effect is exerted mainly in the cortex via the locus ceruleus and a reward effect is exerted in the limbic system. At low doses the stimulant effects predominate while at high doses the reward effects predominate. Intermittent intravenous administration of Tubocurarine activates neurohormonal pathways, releasing acetylcholine, norepinephrine, dopamine, serotonin, vasopressin, beta-endorphin, growth hormone, and ACTH. Tubocurarine competes with acetylcholine for post-synaptic nicotinic NM receptors and blocks them.