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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:
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)
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:
First approved in 1948
Class (Stereo):
CHEMICAL (EPIMERIC)
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:
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:
THALAMYD by SCHERING
(1961)
Source URL:
First approved in 1948
Class (Stereo):
CHEMICAL (ACHIRAL)
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:
First approved in 1948
Class (Stereo):
CHEMICAL (ACHIRAL)
Chlorothen citrate (trade name Tagathen) is an antihistamine and a first generation H1 receptor antagonist, that have been used for the treatment of asthma, bronchitis, and bronchoconstriction.‘-5. Chlorothen is synthesized by condensation of 5-chloro-2-thienylchloride and N,N-dimethyl-N-(2-pyridinyl)ethylenediamine in the presence of sodium or potassium amide
Status:
US Previously Marketed
Source:
KECTIL DIHYDROSTREPTOMYCIN SULFATE by BRISTOL LABS
(1961)
Source URL:
First approved in 1948
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Dihydrostreptomycin is an antibiotic compound derived from streptomycin by reduction with hydrogen. The primary mechanism of action of the antibiotic dihydrostreptomycin is binding to and modifying the function of the bacterial ribosome, thus leading to decreased and aberrant translation of proteins, in addition it binds mechanosensitive channel of large conductance (MscL) and modifies its conformation, thus allowing the passage of K+ and glutamate out of, and dihydrostreptomycin into, the cell. It has about the same degree of antibacterial activity as streptomycin, but it is less effective against some gram-negative microorganisms. Because it has a higher risk of irreversible deafness, and its effectiveness is no greater that that of streptomycin, dihydrostreptomycin is no longer used clinically. To date dihydrostreptomycin is approved for veterinary use to treat bacterial infections.
Status:
US Previously Marketed
First approved in 1948
Class (Stereo):
CHEMICAL (ACHIRAL)
Pentaquine is an 8-aminoquinoline that was used in the 1950s to treat malaria and trypanosomiasis. Pentaquine showed no significant sporontocidal activity against P. gallinaceum in Aedes aegypti. In the experimental animals, the antimalarial effect of pentaquine, its pharmacology and toxicology have been investigated (1, 2). Activity, 80 to 128 times that of quinine and two to eight times that of pamaquin in avian malaria. It has adverse effects very similar to those of primaquine. In mammals it is rapidly absorbed from the gastro-intestinal tract. In acute, and in short term chronic toxicity studies, pentaquine was from one-fourth to one-half as toxic as pamaquin. In the dog, pamaquin in large doses produces severe anorexia, emaciation and ocular paralysis due to central impairment of the sympathetic innervation of the eye. In high dosages pamaquin produces leukopenia, neutropenia, anemia, methemoglobinemia, emaciation, depression, and liver damage in the monkey, effects which are not produced with pentaquine in this species.