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

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Showing 31 - 40 of 85 results

Status:
US Previously Marketed
Source:
21 CFR 310.545(a)(23)(i) internal analgesic salsalate
Source URL:
First approved in 1995
Source:
Salsalate by Caraco Pharmaceutical Laboratories, Ltd.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Salsalate is a dimer of salicylic acid. Upon administration, it is metabolically hydrolyzed to salicylic acid. Salsalate is is a nonsteroidal anti-inflammatory agent for oral administration for treatment of rheumatoid arthritis, osteoarthritis and related rheumatoid disorders. In addition, salsalate is investigated for treatment of type 2 diabetes.
Status:
US Previously Marketed
First approved in 1989

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Dezocine was discovered and patented by American Home Products Corp. in 1978. Dezocine is a partial opiate drug and was used for pain management under brand name Dalgan. But then usage of this drug was discontinued in US. Dezocine acts as a partial μ-receptor agonist, a κ-receptor antagonist, and a norepinephrine and serotonin reuptake inhibitor (via norepinephrine transporter and serotonin transporter). Dezocine shares the CNS depressant and respiratory depressant effects of opioid analgesics. Dezocine has not been shown to produce clinically significant cardiovascular adverse effects.
Methysergide is an oral, synthetic ergot alkaloid, structurally related to the oxytocic agent methylergonovine and to the potent hallucinogen LSD. Methysergide is used prophylactically to reduce the frequency and intensity of severe vascular headaches. Although methysergide is an ergot alkaloid, it is a weak vasoconstrictor and oxytocic. Methysergide is a more potent antagonist of peripheral serotonin receptors than other ergot alkaloids. Methysergide is not just a 5HT2 antagonist, it is also a 5HT1 agonist. Although methysergide and sumatriptan both stimulate serotonin receptors centrally, methysergide is intended for prophylaxis while sumatriptan is indicated for treatment of an acute attack. Methysergide was approved by the FDA in 1962. Methysergide was formerly used for prophylaxis of cluster headaches/migraine headaches, but is no longer recommended due to retroperitoneal/retropulmonary fibrosis.
Status:
US Previously Marketed
First approved in 1962

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Methoxyflurane is an inhalation anesthetic. Methoxyflurane was used for surgical, obstetric, or dental anesthesia, but was withdrawn from US market due to safety concerns, but is still in use in Australia and other countries. Methoxyflurane induces muscle relaxation and reduces pains sensitivity by altering tissue excitability by decreasing the extent of gap junction mediated cell-cell coupling and altering the activity of the channels that underlie the action potential.
Status:
US Previously Marketed
Source:
PRINADOL by SKF
(1961)
Source URL:
First approved in 1959
Source:
Prinadol by Smith Kline & French
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

(-)-Phenazocine is an opioid analgesic drug, which is related to pentazocine and has a similar profile of effects. (-)-Phenazocine is a potent mu opioid receptor agonist. In addition, (−)-phenazocine is also known to bind to δ opioid receptors (DOR) and κ opioid receptors (KOR). Regarding their analgesic potency, (−)-phenazocine was twenty times more potent than morphine in the hot plate test and sixty times more potent than its dextro enantiomer when it was subcutaneously (s.c.) administered
Status:
US Previously Marketed
Source:
ACETAMINOPHEN, CAFFEINE, AND DIHYDROCODEINE BITARTRATE by MIKART
(1997)
Source URL:
First approved in 1956
Source:
Rapacodin by Knoll
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


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
Source:
STRASCOGESIC SALICYLAMIDE by STRASENBURGH
(1961)
Source URL:
First approved in 1943
Source:
Salicylamide by Various Mfrs.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Salicylamide is a non-prescription drug with analgesic and antipyretic properties (NSAID). It is used in combination with aspirin and caffeine in the over-the-counter pain remedies (such as EXAPRIN). Salicylamide can produce sedation and sleep in humans and animals. Has been used as model drug in pharmacokinetic and metabolic studies as a dophamine 2 receptor ligand. Salicylamide is a white or light pink crystals or powder. Organic compound it is a carboxamide derivative of salicylic acid.
Status:
US Previously Marketed
Source:
PABALATE HC POTASSIUM SALICYLATE by ROBINS
(1961)
Source URL:
First marketed in 1921
Source:
potassium salicylate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Potassium salicylate is the potassium salt of salicylic acid. Potassium Salicylate is a cosmetic biocide and preservative, not currently in use. Potassium salicylate was used for the treatment of melasma. Potassium salicylate is considered safe as used when formulated to avoid irritation and when formulated to avoid increasing sun sensitivity, or, when increased sun sensitivity would be expected, directions for use include the daily use of sun protection.
Status:
US Previously Marketed
Source:
Acetphenetidin U.S.P.
(1921)
Source URL:
First marketed in 1887
Source:
Phenacetin by Bayer
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Phenacetin was used as an analgesic and fever-reducing drug in both human and veterinary medicine for many years. Since a major portion of a dose of phenacetin is rapidly metabolised to paracetamol, it seems possible that phenacetin owes some of its therapeutic activity to its main metabolite, paracetamol, whereas its most troublesome side effect (methaemoglobinaemia) is due to another metabolite, p-phenetidine. Phenacetin was shown to inhibit cyclooxygenase (COX)-3, a cyclooxygenase-1 variant while p-phenetidine potently inhibits both COX-1 and COX-2. There is sufficient evidence in humans for the carcinogenicity of analgesic mixtures containing phenacetin. Analgesic mixtures containing phenacetin cause cancer of the renal pelvis, and of the ureter. Phenacetin was withdrawn from many analgesic mixtures long before the legal ban in several countries.
Antipyrine is an analgesic and antipyretic that has been given by mouth and as ear drops. It is often used in testing the effects of other drugs or diseases on drug-metabolizing enzymes in the liver. It inhibits cyclooxygenases and shows little anti-inflammatory activity. Like many old and approved substances after almost 100 years of use, antipyrine has been associated with some serious side effects, namely agranulocytosis and shock reactions.