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

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Showing 8201 - 8210 of 8504 results

Status:
Possibly Marketed Outside US
Source:
Unknown by Topchiev, A.V.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Hydrocotarnine is a crystalline alkaloid, obtained from opium and also formed by the reduction of cotarnine. It is a non-narcotic opium alkaloid. Hydrocotarnine is supposed to potentiate the analgesic effect of oxycodone with unknown mechanism.
Garenoxacin is an antibacterial agent active against a range of aerobic Gram-positive and Gram-negative bacteria. It exerts its action by inhibiting bacterial DNA gyrase and topoisomerase IV. The drug was withdrawn from the market in Europe and was never approved in the USA. Garenoxacin is still marketed in Japan under the name Geninax.
Status:
Possibly Marketed Outside US
Source:
NCT00994461: Phase 4 Interventional Completed Healthy Volunteers
(2009)
Source URL:

Class (Stereo):
CHEMICAL (MIXED)



Loxoprofen (INN) is a non-steroidal anti-inflammatory drug in the propionic acid derivatives group. It is marketed in Brazil, Mexico and Japan by Sankyo as its sodium salt, loxoprofen sodium, under the trade name Loxonin, Argentina as Oxeno and in India as Loxomac. It is available in these countries for oral administration, and a transdermal preparation was approved for sale in Japan on January 2006. It is usually used to treat rheumatoid arthritis and osteoarthritis. It is also used to reduce pain and inflammation after surgery, wounds and tooth removal, as well as to bring down fever or ease pain induced by acute inflammation of upper respiratory tract Loxoprofen is a prodrug. When administered orally, loxoprofen sodium hydrate is absorbed from the gastrointestinal tract as an unchanged compound with only a modest gastric-mucosal irritation. It is then rapidly biotransformed into the active metabolite trans-OH form (SRS coordination) with a potent inhibitory effect on prostaglandin biosynthesis to exert its pharmacologic effects. Inhibition of prostaglandin biosynthesis constitutes the mechanism of action of this drug, the site of action being cyclooxygenase.
Status:
Possibly Marketed Outside US
Source:
Japan:Alilusem Potassium
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Alilusem (M17055) is under development as a novel loop diuretic for oral administration. M17055 has a potent diuretic effect and can be categorized as a loop diuretic that inhibits both the cotransport of Na+, K+, and 2Cl- at the thick ascending Henle’s loop and the reabsorption of Na+ at the distal tubule cells in the kidney. Structure of M17055 is different from those of other loop diuretics; M17055, which has a sulfate group in its structure is soluble and well absorbed, and its bioavailability in humans is 42-60% (unpublished observation). Considering that the pKa of M17055 is 2.39, almost of M17055 would be in ionized form at physiological pH in the small intestine. In humans, the major elimination route of M17055 is renal excretion, 59-72% of the dose being recovered in unchanged form in urine; the remainder is thought to be metabolized by both CYP3A4 and CYP2C9.
Status:
Possibly Marketed Outside US
Source:
NCT01876628: Phase 4 Interventional Completed Cellulitis
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Flucloxacillin is an isoxazolyl penicillin of the β-lactam group of antibiotics, which exerts a bactericidal effect upon many Gram-positive organisms including β-lactamase-producing staphylococci and streptococci. While no longer used in the United States, Flucloxacillin is supplied under a variety of trade names in other countries, including Floxapen, Flopen, Staphylex. Floxapen is indicated for the treatment of infections due to sensitive Gram-positive organisms, including β-lactamase-producing staphylococci and streptococci. Typical indications including, skin and soft tissue infections; respiratory tract infections; other infections caused by floxapen-sensitive organisms, like example, osteomyelitis, urinary tract infection, septicaemia, endocarditis. Floxapen is also indicated for use as a prophylactic agent during major surgical procedures when appropriate; for example cardiothoracic and orthopaedic surgery. Flucloxacillin, by its action on the synthesis of the bacterial wall, exerts a bactericidal effect on streptococci except those of group D (Enterococcus faecalis) staphylococci. It is not active against methicillin-resistant staphylococci. There is evidence that the risk of flucloxacillin induced liver injury is increased in subjects carrying the HLA-B*5701 allele. Despite this strong association, only 1 in 500-1000 carriers will develop liver injury. Consequently, the positive predictive value of testing the HLA-B*5701 allele for liver injury is very low (0.12%) and routine screening for this allele is not recommended. Flucloxacillin diffuses well into most tissue. Specifically, active concentrations of flucloxacillin have been recovered in bones: 11.6 mg/L (compact bone) and 15.6 mg/L (spongy bone), with a mean serum level of 8.9 mg/L. Flucloxacillin diffuses in only small proportion into the cerebrospinal fluid of subjects whose meninges are not inflamed. It is also excreted in small quantities in mother's milk. In normal subjects approximately 10% of the flucloxacillin administered is metabolised to penicilloic acid. The elimination half-life of flucloxacillin is in the order of 53 minutes.
Aescin, the major active principle from Aesculus hippocastanum (Hippocastanaceae) the horse chestnut tree, has shown satisfactory evidence for a clinically significant activity in chronic venous insufficiency (CVI), haemorrhoids and post-operative oedema. In one controlled trial aescin was shown to be as effective as compression therapy as an alternative to medical treatment for CVI. The therapeutic benefit is well supported by a number of experimental investigations in different animal models, indicative of clearcut anti-oedematous, anti-inflammatory and venotonic properties, mainly related to the molecular mechanism of the agent, allowing improved entry of ions into channels, thus raising venous tension in both in vitro and in vivo conditions. Other mechanisms, i.e. release of PGF2 from veins, antagonism to 5-HT and histamine, reduced catabolism of tissue mucopolysaccharides, further underline the wide ranging mechanisms of the therapeutic activity of aescin. Aescin exists in two forms, α and β. β-aescin (b-escin) appears to be the active component of the mixture and is the molecular form present in major available pharmaceutical products. Beta-aescin has cytotoxic activity toward human colon adenocarcinoma cell lines.
Aescin, the major active principle from Aesculus hippocastanum (Hippocastanaceae) the horse chestnut tree, has shown satisfactory evidence for a clinically significant activity in chronic venous insufficiency (CVI), haemorrhoids and post-operative oedema. In one controlled trial aescin was shown to be as effective as compression therapy as an alternative to medical treatment for CVI. The therapeutic benefit is well supported by a number of experimental investigations in different animal models, indicative of clearcut anti-oedematous, anti-inflammatory and venotonic properties, mainly related to the molecular mechanism of the agent, allowing improved entry of ions into channels, thus raising venous tension in both in vitro and in vivo conditions. Other mechanisms, i.e. release of PGF2 from veins, antagonism to 5-HT and histamine, reduced catabolism of tissue mucopolysaccharides, further underline the wide ranging mechanisms of the therapeutic activity of aescin. Aescin exists in two forms, α and β. β-aescin (b-escin) appears to be the active component of the mixture and is the molecular form present in major available pharmaceutical products. Beta-aescin has cytotoxic activity toward human colon adenocarcinoma cell lines.
Status:
Possibly Marketed Outside US
Source:
Unknown by Eykman, J.F.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



α-Asarone is a phytochemical compound with neuroprotective, anti-oxidative, anticonvulsive and cognitive enhancing action, isolated from the Chinese medicinal herb Acorus tatarinowii. Numerous clinical studies in China had indicated the effectiveness of α-asarone against respiratory disorders and epilepsy. Asarone tablets have been clinically used as bronchial asthma and bronchitis prescription drug in China. Unfortunately, toxic and genotoxic studies of a-asarone have indicated that this compound may pose a risk to human health, including embryotoxicity and maternal toxicity in rats, hepatotoxicity in rat-cultivated hepatocytes, and in vivo and in vitro genotoxic damage in mammalian cells.
Status:
Possibly Marketed Outside US
Source:
NCT00994461: Phase 4 Interventional Completed Healthy Volunteers
(2009)
Source URL:

Class (Stereo):
CHEMICAL (MIXED)



Loxoprofen (INN) is a non-steroidal anti-inflammatory drug in the propionic acid derivatives group. It is marketed in Brazil, Mexico and Japan by Sankyo as its sodium salt, loxoprofen sodium, under the trade name Loxonin, Argentina as Oxeno and in India as Loxomac. It is available in these countries for oral administration, and a transdermal preparation was approved for sale in Japan on January 2006. It is usually used to treat rheumatoid arthritis and osteoarthritis. It is also used to reduce pain and inflammation after surgery, wounds and tooth removal, as well as to bring down fever or ease pain induced by acute inflammation of upper respiratory tract Loxoprofen is a prodrug. When administered orally, loxoprofen sodium hydrate is absorbed from the gastrointestinal tract as an unchanged compound with only a modest gastric-mucosal irritation. It is then rapidly biotransformed into the active metabolite trans-OH form (SRS coordination) with a potent inhibitory effect on prostaglandin biosynthesis to exert its pharmacologic effects. Inhibition of prostaglandin biosynthesis constitutes the mechanism of action of this drug, the site of action being cyclooxygenase.
Status:
Possibly Marketed Outside US
Source:
ANCYLOL by American Cyanamid
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Disophenol is a drug used in veterinary medicine recommended for use in the treatment of dogs infested with hook worms (Ancylostoma caninum, A. braziliense and Uncinuriu stenocephala) and cats infested with the hookworm A. tubaeforme.

Showing 8201 - 8210 of 8504 results