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Status:
First approved in 1960
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
PROTHIPENDYL is a neuroleptic azaphenothiazine used to treat anxiety and agitation in psychotic syndromes. It also shows strong antihistamine and anti-emetic actions.
Status:
First approved in 1960
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Clemizole is a drug in clinical development for the treatment of hepatitis C virus (HCV) infection. Clemizole is a novel inhibitor of TRPC5 channels. Clemizole is an H1 antagonist. Clemizole, an antihistamine drug that was once widely used for treatment of allergic disease, was recently discovered to be a potent inhibitor (IC50, 24 nM) of the interaction between an HCV protein (NS4B) and HCV RNA. Although clemizole was widely used during the 1950s and 1960s, this was before contemporary regulatory requirements were established for new drug development, and there is very minimal information about its pharmacokinetics and metabolism.
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:
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:
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:
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.
Status:
US Previously Marketed
Source:
LIQUAMAR by ORGANON USA INC
(1957)
Source URL:
First approved in 1957
Source:
LIQUAMAR by ORGANON USA INC
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Phenprocoumon is the dominant anticoagulant in clinical use in several continental European countries. It used for the prevention and treatment of thromboembolic disease including venous thrombosis, thromboembolism, and pulmonary embolism as well as for the prevention of ischemic stroke in patients with atrial fibrillation. Phenprocoumon inhibits vitamin K reductase, resulting in depletion of the reduced form of vitamin K (vitamin KH2). Bleedings are the most important side -effects of oral anticoagulants. The gastrointestinal and the urinary tract are often affected; the most dangerous are intracerebral hemorrhages. A great number of drugs increase the risk of bleeding of oral anticoagulants. Enzyme inhibitors (e.g. allopurinol, androgens, cimetidine, ciprofloxacin, co-trimoxazole, certain anti-inflammatory agents, fibrates, imidazoles, macrolide antibiotics, etc.) reinforce, and enzyme inducers (e.g. barbiturates, rifampicin) and oral contraceptives reduce, the anticoagulant action.
Status:
US Previously Marketed
Source:
TRIAMCINOLONE by PUREPAC PHARM
(1982)
Source URL:
First approved in 1957
Source:
ARISTOCORT by ASTELLAS
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Triamcinolone is a long-acting synthetic corticosteroid primarily used for their anti-inflammatory effects in disorders of many organ systems. Triamcinolone diacetate injectable suspension is indicated for intramuscular use as follows: Allergic States Control of severe or incapacitating allergic conditions intractable to adequate trials of conventional treatment in asthma, atopic dermatitis, contact dermatitis, drug hypersensitivity reactions, perennial or seasonal allergic rhinitis, serum sickness, transfusion reactions. Bullous dermatitis herpetiformis, exfoliative erythroderma, mycosis fungoides, pemphigus, severe erythema multiform (Stevens-Johnson syndrome). Endocrine Disorders Primary or secondary adrenocortical insufficiency, congenital adrenal hyperplasia, hypercalcemia associated with cancer, nonsuppurative thyroiditis. To tide the patient over a critical period of the disease in regional enteritis and ulcerative colitis. Hematologic Disorders Acquired (autoimmune) hemolytic anemia, Diamond-Blackfan anemia, pure red cell aplasia, selected cases of secondary thrombocytopenia. Trichinosis with neurologic or myocardial involvement, tuberculous meningitis with subarachnoid block or impending block when used with appropriate ant tuberculous chemotherapy. For palliative management of leukemia’s and lymphomas. Nervous System Acute exacerbations of multiple sclerosis; cerebral edema associated with primary or metastatic brain tumor, or craniotomy. Sympathetic ophthalmia, uveitis and ocular inflammatory conditions unresponsive to topical corticosteroids. To induce diuresis or remission of proteinuria in idiopathic nephrotic syndrome or that due to lupus erythematosus. Berylliosis, fulminating or disseminated pulmonary tuberculosis when used concurrently with appropriate ant tuberculous chemotherapy, idiopathic eosinophilic pneumonias, symptomatic sarcoidosis. As adjunctive therapy for short-term administration in acute gouty arthritis; acute rheumatic carditis. The anti-inflammatory actions of corticosteroids are thought to involve lipocortins, phospholipase A2 inhibitory proteins that, through inhibition of arachidonic acid, control the biosynthesis of prostaglandins and leukotrienes. Firstly, however, these glucocorticoids bind to the glucocorticoid receptors, which translocate into the nucleus, bind DNA (GRE), and change genetic expression both positively and negatively. The immune system is suppressed by corticosteroids due to a decrease in the function of the lymphatic system, a reduction in immunoglobulin and complement concentrations, the precipitation of lymphocytopenia, and interference with antigen-antibody binding.
Status:
US Previously Marketed
Source:
PEGANONE by RECORDATI RARE
(1957)
Source URL:
First approved in 1957
Source:
PEGANONE by RECORDATI RARE
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Ethotoin is a hydantoin derivative and anticonvulsant. Ethotoin exerts an antiepileptic effect without causing general central nervous system depression. The mechanism of action is probably very similar to that of phenytoin. The latter drug appears to stabilize rather than to raise the normal seizure threshold, and to prevent the spread of seizure activity rather than to abolish the primary focus of seizure discharges. Ethotoin inhibits nerve impulses in the motor cortex by lowering sodium ion influx, limiting tetanic stimulation. Ethotoin is used for the control of tonic-clonic (grand mal) and complex partial (psychomotor) seizures. Ethotoin is marketed as Peganone by Ovation.
Status:
US Previously Marketed
Source:
PROPOXYPHENE HYDROCHLORIDE by ALRA
(1982)
Source URL:
First approved in 1957
Source:
DARVON by XANODYNE PHARM
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Propoxyphene is a centrally acting opiate analgesic. Propoxyphene is an odorless, freely soluble in water, white crystalline powder with a bitter taste. In vitro studies demonstrated propoxyphene and the metabolite norpropoxyphene inhibit sodium channels (local anesthetic effect) with norpropoxyphene being approximately 2 fold more potent than propoxyphene and propoxyphene approximately 10 fold more potent than lidocaine. Propoxyphene and norpropoxyphene inhibit the voltage-gated potassium current carried by cardiac rapidly activating delayed rectifier (hERG) channels with approximately equal potency. It is unclear if the effects on ion channels occur within therapeutic dose range. Propoxyphene is indicated for the relief of mild to moderate pain.