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

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Showing 11 - 20 of 32 results

Status:
US Approved OTC
Source:
21 CFR 358.710(b)(4) dandruff:seborrheic dermatitis salicylic acid
Source URL:
First marketed in 1860
Source:
sodium salicylate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Methyl salicylate (or methyl 2-hydroxybenzoate), also known as wintergreen oil, is a natural product and is present in white wine, tea, porcini mushroom Boletus edulis, Bourbon vanilla, clary sage, red sage and fruits including cherry, apple, raspberry, papaya and plum. Methyl salicylate is topically used in combination with methanol and under brand name SALONPAS to temporarily relieves mild to moderate aches and pains of muscles and joints associated with: strains, sprains, simple backache, arthritis, bruises. The precise mechanism of action of methyl salicylate is not known, but there is suggested, that it cause dilation of the capillaries thereby increasing blood flow to the area.
Tolazoline, also known as priscoline, was used in treatment of persistent pulmonary hypertension of the newborn. But that prescription was discontinued. Priscoline given intravenously produces vasodilatation, primarily due to a direct effect on vascular smooth muscle, and cardiac stimulation; the blood pressure response depends on the relative contributions of the two effects. Priscoline usually reduces pulmonary arterial pressure and vascular resistance. The mechanisms of its therapeutic effects are not clear, but is known, that tolazoline is a non-selective competitive α-adrenergic receptor antagonist and it possesses histamine agonist activity.
Status:
Possibly Marketed Outside US
First approved in 2018

Class (Stereo):
CHEMICAL (ACHIRAL)



Felbinac, an active metabolite of fenbufen, is two times more potent than the parent drug. Felbinac is used topically to alleviate pain in the joints and muscles caused by injury or inflammation (Trixam 3% gel or foam). The drug is believed to exert its action by inhibiting COX-2 protein.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Etofenamate is a non-steroidal anti-inflammatory drug (NSAID) used for the treatment of joint and muscular pain.
Bufexamac is a nonsteroidal antiinflammatory drug (NSAID) used in topical formulations to treat dermatological diseases (eczema and dermatitis) and proctological conditions (haemorrhoids and anal fissure). Bufexamac-containing medicines have been available in EU Member States since the 1970s. In 2010 European Medicines Agency recommends revocation of marketing authorisations for bufexamac due to high risk of contact allergies. The phenolic bufexamac decomposition products could be the reason for its eczema-provoking properties frequently described in the literature. Bufexamac is a class IIb histone deacetylase (HDAC6, HDAC10) inhibitor. Bufexamac also triggered an HDAC6-independent, hypoxia-like response by stabilizing Hypoxia-inducible factor 1-alpha, providing a possible mechanistic explanation of its adverse, pro-inflammatory effects. Bufexamac was capable of specifically inhibiting leukotriene A4 hydrolase and attenuating lung inflammation in acute lung injury mouse model.
Status:
Possibly Marketed Outside US
Source:
NCT02229747: Phase 4 Interventional Completed Pharyngitis
(2001)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Nimesulide is a relatively COX-2 selective, non-steroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic properties. Its approved indications are the second line treatment of acute pain and primary dysmenorrhoea. Due to concerns about the risk of hepatotoxicity, nimesulide has been withdrawn from market in many countries.
Status:
Possibly Marketed Outside US
Source:
Japan:Feprazone
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Feprazone is an anti-inflammatory compound developed for the treatment of such conditions as osteoarthritis, rheumatoid arthritis, rheumatic fever and gouty arthritis. The drug was tested in phase III of clinical trials, however its further faith is unknown.
Niflumic acid belongs to the group of nonsteroidal anti-inflammatory drugs (NSAIDs) and used in the treatment of rheumatoid arthritis, and joint and muscular pain. Its mechanism of action is believed to be based on selective inhibition of cycloxygenases-2 that results in antipyretic, analgesic, and anti-inflammatory effects. In addition to these effects on prostaglandin synthesis, it has been shown to act as a positive allosteric modulator on α1β2γ2 and as a negative modulator on α6β2 and α6β2γ2 (and α1β2) GABAA receptors. In addition, was reported, that niflumic acid blocked T-type calcium channels. It is available for clinical use in several European countries.
Status:
Possibly Marketed Outside US
Source:
Mydocalm by Richter, G.
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Tolperisone is a centrally acting muscle relaxant first synthesized in 1956 and used in clinical practice since the 1960’s. Tolperisone is an aryl alkyl β-aminoketone with an asymmetric carbon atom α to the carbonyl group. The dextrorotatory enantiomer was reported less effective, however, no detailed analyses of the enantiomers are available. The precise mechanism of action of tolperisone is not fully known. The most prominent effect of tolperisone is its inhibitory action on pathways of spinal reflexes. It suppresses the mono and polysynaptic reflex transmission by both pre-synaptic and post-synaptic mechanisms.
Status:
Possibly Marketed Outside US
Source:
Danilon
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



In 2012, two newly developed active pharmaceutical ingredients for horses and food producing animals were released on the German market for veterinary drug products. Those are the parenterally applicable first generation cephalosporin Cefalonium (Cepravin) and the nonsteroidal anti-inflammatory drug Suxibuzone (Danilon). Suxibuzone is a d drug for treatment of pain and inflammation associated with musculoskeletal conditions in the horse eg. osteoarthritic conditions, bursitis, laminitis and soft tissue inflammation. It is a prodrug of the phenylbutazone, which inactivates prostaglandin H synthase and prostacyclin synthase

Showing 11 - 20 of 32 results