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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.
Status:
US Previously Marketed
Source:
Flexin by McNeil
(1956)
Source URL:
First approved in 1956
Source:
Flexin by McNeil
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Zoxazolamine is a centrally acting muscle relaxant. It decreased striatal dopamine metabolism without affecting striatal dopamine concentrations. More specifically, Zoxazolamine was shown to decrease striatal dopamine turnover without directly affecting dopamine synthesis, catabolism, reuptake, or release. It is the IK(Ca) channel opener. It was approved for the relief of muscle spasm in conditions such as musculoskeletal disorders and neurological diseases. Later, it was submitted for the drug's use as a uricosuric agent to treat gout. It was withdrawn from the market due to hepatotoxicity.
Status:
US Previously Marketed
First approved in 1956
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
US Previously Marketed
Source:
SUL-SPANSION by SKF
(1961)
Source URL:
First approved in 1956
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Sulfaethidole is an antibacterial agent, indicated for the treatment of urinary tract infection.
Status:
First approved in 1956
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Oleandomycin is a macrolide antibiotic, which was first described under the designation P.A.105 by Sobin, English, and Celmer (1954-5). Later it appeared on the market under three names and in two forms: as pure oleandomycin ("matromycin," Pfizer; "romicil," Hoffmann-La Roche) and as a mixture with twice its weight of tetracycline ("sigmamycin," Pfizer). Oleandomycin can be employed to inhibit the activities of bacteria responsible for causing infections in the upper respiratory tract much like Erythromycin can. Both can affect staphylococcus and enterococcus genera. Oleoandomycin is reported to inhibit most gram-positive bacteria, but has only a slight inhibiting effect on gram-negative bacteria, rickettsiae, and larger viruses. The spectrum of activity on micro-organisms is therefore wider than that of penicillin and streptomycin, but narrower than that of chloramphenicol and the tetracyclines. Oleandomycin is approved as a veterinary antibiotic in some countries. It has been approved as a swine and poultry antibiotic in the United States. However, it is currently only approved in the United States for production uses. Oleandomycin is a bacteriostatic agent. Like erythromycin, oleandomycin binds to the 50s subunit of bacterial ribosomes, inhibiting the completion of proteins vital to survival and replication. It interferes with translational activity but also with 50s subunit formation. However, unlike erythromycin and its effective synthetic derivatives, it lacks a 12-hydroxyl group and a 3-methoxy group. This change in structure may adversely affect its interactions with 50S structures and explain why it is a less powerful antibiotic.
Status:
US Previously Marketed
Source:
ACETAMINOPHEN, CAFFEINE, AND DIHYDROCODEINE BITARTRATE by MIKART
(1997)
Source URL:
First approved in 1956
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Dihydrocodeine is an opioid analgesic used as an alternative or adjunct to codeine to treat moderate to severe pain, severe dyspnea, and cough. It is semi-synthetic, and was developed in Germany in 1908 during an international search to find a more effective antitussive agent to help reduce the spread of airborne infectious diseases such as tuburculosis. It was marketed in 1911. Dihydrocodeine is metabolized to dihydromorphine -- a highly active metabolite with a high affinity for mu opioid receptors. Dihydrocodeine is used for the treatment of moderate to severe pain, including post-operative and dental pain. It can also be used to treat chronic pain, breathlessness and coughing. In heroin addicts, dihydrocodeine has been used as a substitute drug, in doses up to 2500mg/day to treat addiction.
Status:
US Previously Marketed
First approved in 1956
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Thenalidine is an antihistamine with anticholinergic properties used as an antipruritic drug. It was withdrawn from the US, Canadian, and UK markets due to a risk of neutropenia. Thenalidine is an antagonist of the H1-receptor.
Status:
First approved in 1956
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
METHITURAL (as sodium salt) is a barbiturate derivative which was used as an ultrashort-acting intravenous anesthetic.
Status:
US Previously Marketed
First approved in 1956
Class (Stereo):
CHEMICAL (MIXED)
Conditions:
Docusate, also known as docusate salts or dioctyl sulfosuccinate, prevents/relieves dry hard stool and thus is used to treat constipation. Results usually occurs 1 to 3 days after the first dose. In North America, docusate and a stimulant laxative such as sennosides are commonly used in bowel treatment protocols associated with institutionalized elderly and oncology treatments. A paucity of evidence is available to support the use of the stool softener docusate yet it continues to be prescribed in everyday clinical practice for the aforementioned populations. While the actual cost of docusate is low, additional costs associated with its administration (i.e. nursing time) and its widespread use can be significant. Docusate is absorbed into the bloodstream and excreted via the gallbladder after undergoing extensive metabolism. The effect of docusate may not necessarily be all due to its surfactant properties. Perfusion studies suggest that docusate inhibits fluid absorption or stimulates secretion in the portion of the small intestine known as the jejunum
Status:
US Previously Marketed
First approved in 1956
Class (Stereo):
CHEMICAL (MIXED)
Conditions:
Docusate, also known as docusate salts or dioctyl sulfosuccinate, prevents/relieves dry hard stool and thus is used to treat constipation. Results usually occurs 1 to 3 days after the first dose. In North America, docusate and a stimulant laxative such as sennosides are commonly used in bowel treatment protocols associated with institutionalized elderly and oncology treatments. A paucity of evidence is available to support the use of the stool softener docusate yet it continues to be prescribed in everyday clinical practice for the aforementioned populations. While the actual cost of docusate is low, additional costs associated with its administration (i.e. nursing time) and its widespread use can be significant. Docusate is absorbed into the bloodstream and excreted via the gallbladder after undergoing extensive metabolism. The effect of docusate may not necessarily be all due to its surfactant properties. Perfusion studies suggest that docusate inhibits fluid absorption or stimulates secretion in the portion of the small intestine known as the jejunum