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Status:
US Previously Marketed
Source:
PARADIONE by ABBVIE
(1949)
Source URL:
First approved in 1949
Source:
PARADIONE by ABBVIE
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Paramethadione is an anticonvulsant in the oxazolidinedione class developed by the Abbott Laboratories, approved by the Food and Drug Administration in 1949 for the treatment of absence seizures, also called partial seizures. Paramethadione acts to reduce T-type calcium currents in thalamic neurons which has been proposed to underlie the 3-Hz spike-and-wave discharge seen on electroencephalogram (EEG) during absence seizures.
Status:
First approved in 1949
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Caramiphen is a muscarinic M1 acetylcholine receptor antagonist, which was used for the treatment of Parkinson Disease and cough, but then there using were discontinued. Caramiphen is also used in local anesthesia, and effect could be achieved through the suppression of voltage-gated Na⁺ currents.
Status:
US Previously Marketed
Source:
TRIPELENNAMINE HYDROCHLORIDE by WATSON LABS
(1973)
Source URL:
First approved in 1948
Source:
PBZ by NOVARTIS
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Tripelennamine (sold as Pyribenzamine by Novartis) is a drug that is used as an antipruritic and first-generation antihistamine. Histamine acting on H1-receptors produces vasodilatation, hypotension, flushing, headache, tachycardia, and bronchoconstriction. Histamine also increases vascular permeability and potentiates pain. Tripelennamine can be used in the treatment of asthma, hay fever, rhinitis, and urticaria, but is now less common as newer antihistamines have replaced it.
Status:
US Previously Marketed
Source:
PRISCOLINE by NOVARTIS
(1948)
Source URL:
First approved in 1948
Source:
PRISCOLINE by NOVARTIS
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Tolazoline, also known as priscoline, was used in treatment of persistent pulmonary hypertension of the newborn. But that prescription was discontinued. Priscoline given intravenously produces vasodilatation, primarily due to a direct effect on vascular smooth muscle, and cardiac stimulation; the blood pressure response depends on the relative contributions of the two effects. Priscoline usually reduces pulmonary arterial pressure and vascular resistance. The mechanisms of its therapeutic effects are not clear, but is known, that tolazoline is a non-selective competitive α-adrenergic receptor antagonist and it possesses histamine agonist activity.
Status:
First approved in 1948
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Isometheptene (usually as isometheptene mucate) is a sympathomimetic amine sometimes used in the treatment of migraines and tension headaches due to its vasoconstricting properties. Isometheptene's vasoconstricting properties arise through activation of the sympathetic nervous system via epinephrine and norepinephrine. These compounds elicit smooth muscle activation leading to vasoconstriction by interacting with cell surface adrenergic receptors.
Status:
US Previously Marketed
Source:
SULFISOXAZOLE by HEATHER
(1982)
Source URL:
First approved in 1948
Source:
GANTRISIN by ROCHE
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Sulfisoxazole is a sulfonamide antibacterial antibiotic. The sulfonamides are synthetic bacteriostatic antibiotics with a wide spectrum against most gram-positive and many gram-negative organisms. However, many strains of an individual species may be resistant. Sulfisoxazole acetyl in combination with erythromycin ethylsuccinate is used for treatment of ACUTE OTITIS MEDIA in children that is caused by susceptible strains of Haemophilus influenzae. Sulfisoxazole acetyl is a prodrug of sulfisoxazole. Acetyl group is added to make the drug poorly water soluble, and is hydrolyzed in vivo to the active drug. Sulfisoxazole and its acetylated metabolites are excreted primarily by the kidneys through glomerular filtration. Sulfisoxazole is a competitive inhibitor of the enzyme dihydropteroate synthetase. It inhibits bacterial synthesis of dihydrofolic acid by preventing the condensation of the pteridine with para-aminobenzoic acid (PABA), a substrate of the enzyme dihydropteroate synthetase. The inhibited reaction is necessary in these organisms for the synthesis of folic acid
Status:
US Previously Marketed
Source:
VASOCON-A by NOVARTIS
(1990)
Source URL:
First approved in 1948
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Antazoline is an antagonist of histamine H1 receptors. It selectively bind to but does not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine. Antazoline in combination with naphazoline (VASOCON-A®) is indicated to relieve the symptoms of allergic conjunctivitis.
Status:
First approved in 1948
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Mephenesin is a centrally acting muscle relaxant. This medication is prescribed for muscle spasm. It can be used as an antidote for strychnine poisoning. Most common side effects are: lassitude, drowsiness, weakness, loss of appetite, nausea and vomiting, hypersensitivity reactions. Its clinical usefulness is considered to be limited by its brief duration of action.
Status:
First approved in 1947
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Alverine is a smooth muscle relaxant used for the treatment irritable bowel syndrome. Alverine may increase calcium influx during action potentials due to inhibition of the inactivation of L-type calcium channels, but may also suppress evoked activity by inhibiting the sensitivity of contractile proteins to calcium.
Status:
US Previously Marketed
Source:
DIASONE SODIUM by ABBVIE
(1947)
Source URL:
First approved in 1947
Source:
DIASONE SODIUM by ABBVIE
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Sulfoxone is a water-soluble sulfone and is a competitive inhibitor of the bacterial enzyme dihydropteroate synthetase. Sulfoxone under the brand name Diasone was used as an antileprosy drug, for treatment of dermatitis herpetiformis, and to treat pulmonary tuberculosis. Presently, usage of diasone has been discontinued.