U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 591 - 600 of 623 results

Status:
US Previously Marketed
First approved in 1960

Class (Stereo):
CHEMICAL (RACEMIC)



Oxyphenbutazone is a non-steroidal anti-inflammatory drug, cyclooxygenase (prostaglandin synthetase) inhibitors which was marked under brand name tandearil for the treatment rheumatic disorders such as ankylosing spondylitis, osteoarthritis, and rheumatoid arthritis. But this drug was withdrawn from markets due to bone marrow suppression.
Status:
US Previously Marketed
Source:
Leritine by Merck Sharp & Dohme
(1957)
Source URL:
First approved in 1957
Source:
Leritine by Merck Sharp & Dohme
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Aniledrine is a narcotic pain reliver. The drug was prescribed as an analgesic in anaesthesia (Leritine brand name), however, it is no longer available on the market. Although the exact mechanism is not fully understood, aniledrine appears to elicit its action by binding to endorphine receptors in CNS.
Status:
US Previously Marketed
Source:
PROPOXYPHENE HYDROCHLORIDE by ALRA
(1982)
Source URL:
First approved in 1957

Class (Stereo):
CHEMICAL (ABSOLUTE)



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:
Leritine by Merck Sharp & Dohme
(1957)
Source URL:
First approved in 1957
Source:
Leritine by Merck Sharp & Dohme
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Aniledrine is a narcotic pain reliver. The drug was prescribed as an analgesic in anaesthesia (Leritine brand name), however, it is no longer available on the market. Although the exact mechanism is not fully understood, aniledrine appears to elicit its action by binding to endorphine receptors in CNS.
Status:
US Previously Marketed
First approved in 1952

Class (Stereo):
CHEMICAL (ACHIRAL)



Phenylbutazone is an anti-inflammatory drug, which binds to and inactivates cyclooxygenases and prostacyclin synthase through peroxide (H2O2) mediated deactivation. The reduced production of prostaglandin leads to reduced inflammation of the surrounding tissues. Phenylbutazone was marked under the brand name butazolidin for the treatment rheumatoid arthritis and gout, but then this usage was discontinued. In addition, phenylbutazone is used in UK for the treatment of ankylosing spondylitis, but only in those cases, when other therapies are unsuitable.
Status:
US Previously Marketed
Source:
ALLONAL AMINOPHENAZONE by ROCHE
(1961)
Source URL:
First marketed in 1897
Source:
Pyramidon
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Aminophenazone is a phenyl-pyrazolone derivative with potent analgesic and antipyretic properties. Aminophenazone has been used as salt or complexes, including topically as the salicylate. It was recommended for the treatment of a fever, neuralgia, myositis, acute rheumatism, arthritis, chorea. In 1999 the FDA suspended aminophenazone. The drug caused agranulocytosis. Some of the cases of agranulocytosis were fatal. Another reason for suspending this drug from the market was its ability to react with nitrite-containing food, thus forming carcinogenic nitrosamines. A breath test with 13C-labeled aminopyrine has been used as a non-invasive measure of cytochrome P-450 metabolic activity in liver function tests.
Status:
Possibly Marketed Outside US
Source:
CFR:21 CFR 310.201
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Gentisic acid is an active metabolite of salicylic acid degradation, which possesses a broad spectrum of biological activity, such as anti-inflammatory, antirheumatic and antioxidant properties. The antioxidant activity and radioprotective properties of gentisic acid are exerted by its phenoxyl group. It is also used in cosmetics as a skin-whitening agent for the treatment of skin pigmentary disorders by influencing the synthesis of melanin through inhibition of melanosomal tyrosinase activity Gentisic acid is also a biomarker of Renal Cell Carcinoma.
Flunixin meglumine is a potent, non-narcotic, non-steroidal, analgesic agent with anti-inflammatory and anti-pyretic activity was approved to use in horses, cattle and pigs. In horses it is recommended for the alleviation of inflammation and pain associated with musculoskeletal disorders. It is also recommended for the alleviation of visceral pain associated with colic. In the cattle: it is indicated for the control of pyrexia associated with bovine respiratory disease, endotoxemia and acute bovine mastitis. It is also indicated for the control of inflammation in endotoxemia. Flunixin persists in inflammatory tissues and is associated with anti-inflammatory properties which extend well beyond the period associated with detectable plasma drug concentration. Flunixin meglumine is classified as a carboxylic acid. Its mechanism of action is believed to be primarily via the inhibition of cyclooxygenase (COX) enzymes. This inhibition results in decreased formation of cyclooxygenase-derived eicosanoids involved in the pathophysiology of inflammation, such as thromboxanes and prostaglandins.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Oxolamine under brand names Symphocal, Perebron is used in some countries as a cough suppressant for the treatment of pharyngitis, tracheitis, bronchitis, bronchiectasis, pertussis. Oxolamine possesses anti-inflammatory activity, which causes a reduction in the irritation of the nervous receptors of the respiratory tract.
Status:
Possibly Marketed Outside US
Source:
Schmerz. Apr 2003;17(2):110-6.: Phase 4 Human clinical trial Completed Pain, Postoperative
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

TILIDINE is a low to medium potency opioid analgesic. It is metabolized to its active metabolites, nortilidine and bisnortilidine. Its analgesic activity is largely exerted through nortilidine which is a potent agonist at Mu opioid receptors.

Showing 591 - 600 of 623 results