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Status:
US Previously Marketed
Source:
AKINETON by ABBVIE
(1961)
Source URL:
First approved in 1959
Source:
AKINETON by ABBVIE
Source URL:
Class (Stereo):
CHEMICAL (UNKNOWN)
Conditions:
Biperiden, sold under the brandname Akineton was used as an adjunct in the therapy of all forms of parkinsonism (postencephalitic, arteriosclerotic and idiopathic). Was also useful in the control of extrapyramidal disorders due to central nervous system drugs such as phenothiazines and other groups of psychotropics. Biperiden is a weak peripheral anticholinergic agent. It has, therefore, some antisecretory, antispasmodic and mydriatic effects. In addition, biperiden possesses nicotinolytic activity. Parkinsonism is thought to result from an imbalance between the excitatory (cholinergic) and inhibitory (dopaminergic) systems in the corpus striatum. The mechanism of action of centrally active anticholinergic drugs such as biperiden is considered to relate to competitive antagonism of acetylcholine at cholinergic receptors in the corpus striatum, which then restores the balance. Atropine-like side effects such as dry mouth; blurred vision; drowsiness; euphoria or disorientation; urinary retention; postural hypotension; constipation; agitation; disturbed behavior may been seen. Only limited pharmacokinetic studies of biperiden in humans are available.
Status:
US Previously Marketed
Source:
SULFINPYRAZONE by PAR PHARM
(1985)
Source URL:
First approved in 1959
Source:
ANTURANE by NOVARTIS
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Sulfinpyrazone was approved by the U.S. Food and Drug Administration (FDA) on May 13, 1959. It was developed and marketed as Anturane® by Novartis. Sulfinpyrazone is an oral uricosuric agent (pyrazolone derivative) used to treat chronic or intermittent gouty arthritis. Sulfinpyrazone competitively inhibits the reabsorption of uric acid at the proximal convoluted tubule, thereby facilitating urinary excretion of uric acid and decreasing plasma urate concentrations. This is likely done through inhibition of the urate anion transporter (hURAT1) as well as the human organic anion transporter 4 (hOAT4). Sulfinpyrazone is not intended for the treatment of acute attacks because it lacks therapeutically useful analgesic and anti-inflammatory effects. Sulfinpyrazone and its sulfide metabolite possess COX inhibitory effects. Sulfinpyrazone has also been shown to be a UDP-glucuronsyltransferase inhibitor and a very potent CYP2C9 inhibitor. Sulfinpyrazone is also known to be a cystic fibrosis transmembrane conductance regulator (CFTR) inhibitor as well as an inhibitor of several multridrug resistance proteins (MRPs). Branded and generic forms of sulfinpyrazone have been discontinued in the US.
Status:
US Previously Marketed
Source:
TRIMEPRAZINE TARTRATE by MORTON GROVE
(1985)
Source URL:
First approved in 1959
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Trimeprazine (also known as Alimemazine), a phenothiazine used as antipsychotic drug. This drug is used in Russia under brand name TERALIGEN and has anti-histamine, sedative, and anti-emetic (anti-nausea) effects. Teraligen is used to treat neurosis, depression and anxiety of different origins. It prevents and relieves allergic conditions, which cause pruritus and urticaria by blocking histamine produced by the body during an allergic reaction. Trimeprazine competes with free histamine for binding at HA-receptor sites. This antagonizes the effects of histamine on HA-receptors, leading to a reduction of the negative symptoms brought on by histamine HA-receptor binding. Trimeprazine is not approved for use in humans in the United States. Nevertheless, combination of alimemazine and prednisolone (commonly sold under the brand name Temaril-P) is licensed as an antipruritic and antitussive in dogs.
Status:
US Previously Marketed
First approved in 1959
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Chlorphenoxamine is an antihistamine and anticholinergic used as an antipruritic and was formerly used in the sympathomimetic treatment of parkinsonism. Histamine receptor H1 antagonist. Chlorphenoxamine is used to treat Allergic conditions, it is reported as an ingredient of Systral in Germany, Malta, Portugal, Thailand, Turkey.
Status:
US Previously Marketed
First approved in 1959
Class (Stereo):
CHEMICAL (UNKNOWN)
Targets:
Conditions:
Protokylol, a sympathomimetic drug has been utilized in general clinical practice as a bronchodilator. Protokylol (brand names Caytine, Ventaire) is a β-adrenergic receptor agonist which was used as a bronchodilator in Europe and the United States.
Status:
US Previously Marketed
Source:
TACE 25 MG ERGONOVINE by MERRELL
(1959)
Source URL:
First approved in 1959
Source:
TACE 25 MG ERGONOVINE by MERRELL
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Ergonovine (also known as ergometrine) is the active water soluble component of ergot of rye. Ergonovine is being used as a maleate salt to prevent or treate postpartum haemorrhage and postabortion haemorrhage. Ergonovine stimulates alpha-adrenergic and serotonin receptors, thus activating contractions of uterine and vascular smooth muscle. Ergonovine may have depressant effect on CNS system as it binds to dopamine receptors.
Status:
First approved in 1958
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Troleandomycin (also known Triacetyl-oleandomycin and having brand name Tao) is a macrolide antibiotic which used to for the treat of infections of the upper and lower respiratory tract: such as tonsillitis, bronchitis, sinusitis, and pneumonia. However, the brand name Tao was discontinued. Troleandomycin acts by penetrating the bacterial cell membrane and reversibly binding to the 50 S subunit of bacterial ribosomes or near the "P" or donor site so that binding of tRNA (transfer RNA) to the donor site is blocked. Translocation of peptides from the "A" or acceptor site to the "P" or donor site is prevented, and subsequent protein synthesis is inhibited.
Status:
US Previously Marketed
Source:
CHLORPROPAMIDE by PAR PHARM
(1984)
Source URL:
First approved in 1958
Source:
DIABINESE by PFIZER
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Chlorpropamide (DIABINESE®), is a sulfonylurea hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. It appears to lower the blood glucose acutely by stimulating the release of insulin from the pancreas, an effect dependent upon functioning beta cells in the pancreatic islets. The mechanism by which chlorpropamide (DIABINESE®) lowers blood glucose during long-term administration has not been clearly established. Extra-pancreatic effects may play a part in the mechanism of action of oral sulfonylurea hypoglycemic drugs. While chlorpropamide is a sulfonamide derivative, it is devoid of antibacterial activity. Chlorpropamide (DIABINESE®) may also prove effective in controlling certain patients who have experienced primary or secondary failure to other sulfonylurea agent.
Status:
US Previously Marketed
Source:
SINGOSERP by CIBA
(1961)
Source URL:
First approved in 1958
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Syrosingopine, a drug derived from reserpine, which was investigated for the treatment of essential hypertension. The combination of syrosingopine and a mitochondrial inhibitor for the treatment of cancer and for achieving immunosuppression was patented. This invention also relates to a fluorescence-based method for predicting syrosingopine sensitivity of a cancer cell.
Status:
US Previously Marketed
Source:
HALOTHANE by BH
(1976)
Source URL:
First approved in 1958
Source:
FLUOTHANE by WYETH AYERST
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Halothane, USP is an inhalation anesthetic chemically designated 2-Bromo-2-chloro-1,1,1-trifluoroethane. Halothane, sold under the brand name Fluothane among others, is a general anesthetic. It can be used to start or maintain anesthesia. One of its benefits is that it does not increase the production of saliva which can be particularly useful in those who are difficult to intubate. Side effects include an irregular heartbeat, decreased effort to breath (respiratory depression), and liver problems. It should not be used in people with porphyria or a history of malignant hyperthermia either in themselves or their family members. It is unclear whether use during pregnancy is harmful to the baby, and it is not generally recommended for use during a cesarean section. Fluothane is no longer commercially available in the United States.