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

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Showing 61 - 70 of 94 results

Status:
Possibly Marketed Outside US
Source:
NCT00380523: Phase 4 Interventional Completed Pain
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Etoricoxib is a selective COX-2 inhibitor, which is approved in Europe for the treatment of inflammatory disorders such as osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, acute pain conditions, gout and postoperative dental surgery pain.
Status:
Possibly Marketed Outside US
Source:
NCT02682524: Phase 4 Interventional Completed Osteoarthritis of Knee
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Aceclofenac is a non-steroidal anti-inflammatory drug (NSAID) analog of Diclofenac. It is used for the relief of pain and inflammation in rheumatoid arthritis, osteoarthritis and ankylosing spondylitis. The dose is 100 mg twice daily, and should not be given to people with porphyria or breastfeeding mothers and is not recommended for children. Aceclofenac is a cytokine inhibitor. Aceclofenac works by blocking the action of a substance in the body called cyclo-oxygenase. Cyclo-oxygenase is involved in the production of prostaglandins (chemicals in the body which cause pain, swelling and inflammation). Aceclofenac is the glycolic acid ester of diclofenac. The incidence of gastric ulcerogenicity of aceclofenac has been reported to be significantly lower than that of other frequently prescribed NSAIDs: for instance, 2-fold less than naproxen, 4-fold less than diclofenac, and 7-fold less than indomethacin. Aceclofenac is metabolized in human hepatocytes and human microsomes to form [2-(2',6'-dichloro-4'-hydroxy- phenylamino)phenyl] acetoxyacetic acid as the major metabolite, which is then further conjugated.
Lonazolac is a nonsteroidal anti-inflammatory drug. The mononuclear cell response to a synovial stimulus can be abolished by very low concentrations of lonazolac. This blockade can be completely released by the addition of prostaglandin E2. Lonazolac appears therefore as an agent able in addition to modulate the immune response. The release of histamine from human basophils was significantly decreased after preincubation of the cells with lonazolac Ca. Preincubation of human polymorphonuclear leukocytes with lonazolac Ca led to an inhibition of leukotriene generation induced by either the Ca ionophore or opsonized zymosan. Lonazolac Ca affected different enzymes of the platelet activating factor metabolism. After pre- and post-treatment with lonazolac-Ca, the numbers of animals with lung metastases and the score of metastases significantly decreased. Lonazolac-Ca is indicated for the treatment of painful inflammatory rheumatic diseases of the joints and the spine. Acute irritation in osteoarthritis and spondylosis. Soft tissue rheumatism. Post-traumatic and postoperative pain and swelling states.
Status:
Possibly Marketed Outside US
Source:
NORVEDAN
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Fentiazac is a non-steroidal anti-inflammatory agent developed for the treatment of pain disorders. The drug was marketed under the name Norvedan, however, its current marketing status is unknown and supposed to be "discontinued".
Status:
Possibly Marketed Outside US
Source:
Trocoxil by Searle
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Mavacoxib (trade name Trocoxil) is a veterinary drug used to treat pain and inflammation in dogs with the degenerative joint disease. Mavacoxib is a non-steroidal anti-inflammatory drug (NSAID) of the coxib class. Mavacoxib acts by preferential inhibition of COX-2-mediated prostaglandin synthesis. It, therefore, possesses analgesic and anti-inflammatory properties. The products of COX-2 metabolism are also involved in ovulation, implantation, and closure of the ductus arteriosus. Mavacoxib is well absorbed after oral administration; bioavailability was 87% in fed dogs and 46 % in fasted conditions and the recommended dose is based on administration with food. Therapeutic concentrations in fed dogs are reached rapidly and peak concentrations are obtained in less than 24 hours after administering a dose. Mavacoxib is approximately 98% bound to plasma proteins. It is extensively distributed throughout the body and almost all the mavacoxib-related residues in plasma comprise parent drug. The rate of body clearance of mavacoxib is slow and the major route of elimination is by biliary excretion of the parent drug. Adverse reactions of the digestive tract such as vomiting and diarrhea were commonly reported, loss of appetite, hemorrhagic diarrhea, and melaena have been reported in uncommon cases. Gastrointestinal ulceration was reported in rare cases. Apathy, degradation of renal biochemistry parameters and impaired renal function have been reported in uncommon cases. In rare cases, these adverse reactions may be fatal.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Morniflumate is a non-steroidal anti-inflammatory drug and represent as a beta-morpholinoethyl ester of niflumic acid, which is rapidly hydrolyzed in the plasma, releasing the free acidic form, the molecule responsible for the pharmacological effects. It was shown, that morniflumate was effective in the treatment of chronic recurring bronchitis and inhibited cyclooxygenase-1, 2 (COX-1, 2). Morniflumate has a 30-year history of clinical use, particularly for the treatment of pain associated with pediatric ear-nose-throat (ENT) infection. In addition, it appears to be a valid and well-tolerated alternative to other NSAIDs, or to antibiotics, for the treatment of pain and other symptoms of soft tissue inflammation.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Naproxcinod is the first in the class of CINODs and has been evaluated in preclinical and clinical studies. It is metabolized to naproxen and has been shown to donate nitric oxide in vitro and in vivo. It stimulated the expression of heme oxygenase-mRNA in endothelial cells in vitro, a crucial mediator of antioxidant and tissue-protective actions. In preclinical studies, Naproxcinod has been shown to be analgesic and anti-inflammatory. Naproxcinod dose-dependently displayed a noticeable and significant anti-ischemic effect in reperfused ischemic rabbit hearts and did not exhibit the hypertensive effects of naproxen. In a proof of concept study in 31 healthy volunteers with GI tolerance as the primary endpoint, Naproxcinod caused fewer gastric erosions in both the stomach and the duodenum than naproxen, while 0.2 erosions were found with placebo. Naproxcinod caused less of an adverse effect in intestinal permeability than naproxen and was similar to placebo.
Status:
Possibly Marketed Outside US
Source:
ZUBRIN by Ortho-McNeil
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Tepoxalin is a nonsteroidal anti-inflammatory drug approved for veterinary use in the United States and many other countries. Marketed under the brand name Zubrin, Tepoxalin is indicated for the control of pain and inflammation associated with osteoarthritis in dogs. Tepoxalin has an unique property as an NSAIDs that suppresses both cyclooxygenase and lipoxygenase.
Status:
Possibly Marketed Outside US
Source:
NCT01066676: Phase 4 Interventional Completed Osteoarthritis of the Hip or Knee
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Dexibuprofen, S(+)-ibuprofen, is a non-steroidal anti-inflammatory drug and active dextrorotatory enantiomer of ibuprofen. Pharmacotherapeutic effects of dexibuprofen are more potent with lesser side effects than that of the racemic mixture of both isomers. In the acute and chronic treatment of osteoarthritis, it exhibits equivalent efficacy and tolerability as that of celecoxib. Dexibuprofen is a non-selective inhibitor of cyclooxygenase (COX), which is an enzyme involved in prostaglandin (mediators of pain and fever) and thromboxane (stimulators of blood clotting) synthesis via the arachidonic acid pathway. Dexibuprofen is a non-selective cyclooxygenase inhibitor and hence, it inhibits the activity of both COX-1 and COX-2. The inhibition of COX-2 activity decreases the synthesis of prostaglandins involved in mediating inflammation, pain, fever, and swelling while the inhibition of COX-1 is thought to cause some of the side effects of Dexibuprofen including GI ulceration. The major disadvantage of dexibuprofen is its low bioavailability, the account of its low solubility in physiological media.
Status:
Possibly Marketed Outside US
Source:
SURGAM by Roussel-Uclaf
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Tiaprofenic acid is a non-steroidal, anti-inflammatory, analgesic compound, which nonselectively inhibits cyclooxygenase protein. Tiaprofenic acid was approved in Europe for the symptomatic relief of arthritis, ankylosing spondylitis and other inflammatory-rheumatic disorders as well as the painful conditions after injury.

Showing 61 - 70 of 94 results