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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
Source:
TRIMEPRAZINE TARTRATE by MORTON GROVE
(1985)
Source URL:
First approved in 1959
Class (Stereo):
CHEMICAL (EPIMERIC)
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:
First approved in 1957
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Acenocoumarol is mono-coumarin derivative with racemic mixture of R (+) and S (-) enantiomers. Acenocoumarol is structurally similar to vitamin K and is competitively able to inhibit the enzyme vitamin K-epoxide reductase. It exerts anticoagulant action by preventing the regeneration of reduced vitamin K by interfering with action of vitamin K epoxide reductase. Acenocoumarol is prescribed as the anticoagulant in various thromboembolic disorders.
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 (ABSOLUTE)
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.
Status:
US Previously Marketed
Source:
TOLBUTAMIDE by ASCOT
(1983)
Source URL:
First approved in 1957
Source:
ORINASE by PHARMACIA AND UPJOHN
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Tolbutamide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). It is structurally similar to acetohexamide, chlorpropamide and tolazamide and belongs to the sulfonylurea class of insulin secretagogues, which act by stimulating β cells of the pancreas to release insulin. Sulfonylureas lower blood glucose in patients with NIDDM by directly stimulating the acute release of insulin from functioning beta cells of pancreatic islet tissue by an unknown process that involves a sulfonylurea receptor (receptor 1) on the beta cell. Sulfonylureas inhibit the ATP-potassium channels on the beta cell membrane and potassium efflux, which results in depolarization and calcium influx, calcium-calmodulin binding, kinase activation, and release of insulin-containing granules by exocytosis, an effect similar to that of glucose.
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 (ABSOLUTE)
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.
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 (ABSOLUTE)
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.
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 (ABSOLUTE)
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.
Status:
US Previously Marketed
Source:
DEPROL BENACTYZINE by WALLACE
(1961)
Source URL:
First approved in 1957
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Benactyzine, an anticholinergic drug, had been used as an antidepressant in the treatment of depression and associated anxiety. It is no longer used in medicine due to its ineffectiveness but is widely used in scientific research. Benactyzine is a muscarinic antagonist which also inhibits the nicotinic acetylcholine receptor.
Status:
US Previously Marketed
Source:
SPARINE by WYETH AYERST
(1957)
Source URL:
First approved in 1956
Source:
SPARINE by HIKMA
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Promazine (Sparine) is a phenothiazine neuroleptic used for short-term management of moderate to severe psychomotor agitation and treatment of agitation and restlessness in the elderly. Promazine is an antagonist at types 1, 2, and 4 dopamine receptors, 5-HT receptor types 2A and 2C, muscarinic receptors 1 through 5, alpha(1)-receptors, and histamine H1-receptors. Promazine's antipsychotic effect is due to antagonism at dopamine and serotonin type 2 receptors, with greater activity at serotonin 5-HT2 receptors than at dopamine type-2 receptors. This may explain the lack of extrapyramidal effects. Promazine does not appear to block dopamine within the tuberoinfundibular tract, explaining the lower incidence of hyperprolactinemia than with typical antipsychotic agents or risperidone. Antagonism at muscarinic receptors, H1-receptors, and alpha(1)-receptors also occurs with promazine. Promazine is not approved for human use in the United States. It is available in the US for veterinary use under the names Promazine and Tranquazine.