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

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Showing 1681 - 1690 of 3134 results

Status:
Possibly Marketed Outside US
Source:
NCT00422318: Phase 4 Interventional Completed Heart Failure
(2004)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Benzbromarone (INN) is a uricosuric agent and non-competitive inhibitor of xanthine oxidase used in the treatment of gout, especially when the first line treatment, allopurinol, fails or produces intolerable adverse effects. It is structurally related to the antiarrhythmic amiodarone. Benzbromarone was introduced in the 1970s and was viewed as having few associated serious adverse reactions. It was registered in about 20 countries throughout Asia, South America and Europe. In 2003, the drug was withdrawn by Sanofi-Synthélabo, after reports of serious hepatotoxicity, although it is still marketed in several countries by other drug companies. The withdrawal has greatly limited its availability around the world and increased difficulty in accessing it in other countries where it has never been available. Standard dosages of benzbromarone (100 mg/day) tend to produce greater hypouricaemic effects than standard doses of allopourinol (300 mg/day) or probenecid (1000 mg/day). Adverse effects associated with benzbromarone are relatively infrequent but potentially severe. Four cases of benzbromarone-induced hepatotoxicity were identified from primary literature, and eleven cases have been reported by Sanofi-Synthélabo but details are not available in the public domain. Only one of the four publicly published cases demonstrated a clear relationship between the drug and liver injury as demonstrated by rechallenge. The other three cases lacked incontrovertible evidence to support a diagnosis of benzbromarone-induced hepatotoxicity. If all the reported cases are assumed to be due to benzbromarone, the estimated risk of hepatotoxicity in Europe was approximately 1 in 17 000 patients but may be higher in Japan. Benzbromarone is a very potent inhibitor of CYP2C9. The mechanism of benzbromarone hepatotoxicity is believed to be due to its hepatic metabolism by CYP2C9 and possible effects of the parent compound or its metabolites on mitochondrial function. Benzbromarone is a benzofuran and shares structural similarities with benzarone and amiodarone, all three of which affect mitochondrial function.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Trimethyldiphenylpropylamine (Recipavrin) is a methadon analog with antispasmodic properties. It exerts both musculotropic (antibarium) and anticholinergic action, relieves smooth muscle spasms, e.g. dysmenorrhea and pains associated with gallstones. It was marketed in Sweden in the 1960s as a spasmolytic drug under tradename Recipavrin.
Status:
Possibly Marketed Outside US
Source:
NCT04254731: Phase 4 Interventional Active, not recruiting Adverse Drug Effect
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Conditions:

levomethadone, or R-(−)-methadone, is the active enantiomer of methadone; having approximately 50x the potency of the S-(+)-enantiomer as well as greater μ-opioid receptor selectivity.
Status:
Possibly Marketed Outside US
Source:
NCT01908465: Phase 4 Interventional Completed Irritable Bowel Syndrome (IBS)
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Ebastine is an antihistamine which blocks H1-receptors through its carboxylic acid metabolite. Ebastine is indicated for the treatment of allergic rhinitis and chronic idiopathic urticaria.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Se-75 norcholesterol is radiopharmaceutical derivative of cholesterol, a natural precursor in the synthesis of adrenocortical steroid hormones. Se-75 is a radioactive isotope of selenium, it has half-life period of 120 days, and emits gamma-rays upon decay. Se-75 norcholesterol was used under tradename Scintadren to diagnose a wide range of adrenal pathologies, including Cushing syndrome, Cushing's disease, carcinoma, adrenal insufficiency, and phaeochromocytoma. The drug was withdrawn in the early 2000s in favor of I-131 norcholesterol.
Phenibut (beta-phenyl-gamma-aminobutyric acid or 4-amino-3-phenylbutyric acid) is a neuropsychotropic drug that was discovered and introduced into clinical practice in Russia in the 1960s. It has anxiolytic and nootropic (cognition enhancing) effects. It acts as a GABA-mimetic, primarily at GABA(B) receptors. Pharmacological activity of racemic phenibut relies on R-phenibut and this correlates to the binding affinity of enantiomers of phenibut to the GABAB receptor. In addition R-phenibut binds to the α2-δ subunit of voltage-dependent calcium channels. It is highly effective in treating anxiety, post-traumatic stress disorder, depression, asthenia, insomnia, alcoholism, stuttering, and vestibular disorders. It also improves mental performance (attention, memory, speed and accuracy of sensory-motor reactions), physical performance, reduces sleep disorders as well as movement and speech disorders.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Iprindole under the brand name Prondol was used as an antidepressant but now is no longer marketed. It possesses the beta-adrenergic properties and has an indirect beta 2-mimetic effect.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Nicotinyl methylamide (N-methylnicotinamide) is an experimental drug with no approved indication or marketed formulation. Nicotinyl methylamide is a metabolite of niacin (or nicotinamide) and is commonly found in human urine. However low levels of urinary excretion of N-methylnicotinamide indicates niacin deficiency. In patients with liver cirrhosis nicotinamide methylation is increased leading to a rise in urinary N-methylnicotinamide. The hyperfunction of this methylating pathway might play a protective role against the toxic effect of intracellular accumulation of nicotinamide deriving from the catabolic state of cirrhosis. N-methylnicotinamide is known to inhibit choline transport and reduce choline clearance out of the brain. N-methylnicotinamide has been found to be a microbial metabolite. N-methylnicotinamide inhibits arterial thrombosis in hypertensive rats. N-methylnicotinamide via production/release of prostacyclin inhibits arterial thrombosis development. The antithrombotic effect of N-methylnicotinamide is accompanied by platelet inhibition and enhanced fibrinolysis, due to the decrease production of plasminogen activator inhibitor -1.
Pyriproxyfen is a broad-spectrum insect growth regulator with insecticidal activity against public health insect pests: houseflies, mosquitoes and cockroaches. In agriculture and horticulture, pyriproxyfen has registered uses for the control of scale, whitefly, bollworm, jassids, aphids and cutworms. Pyriproxyfen is used on citrus fruit in Israel, South Africa, Spain and Italy. Pyriproxyfen is one of several insecticides used for the control of the red imported fire ant (Solenopsis invicta) in California, USA. Pyriproxyfen has also been considered by WHO for vector control under its Pesticides Evaluation Scheme. It is a potent suppressor of embryogenesis and adult formation of the sweetpotato whitefly, Bemisia tabaci (Gennadius), and the greenhouse whitefly, Trialeurodes vaporariorum (Westwood). Dipping of cotton or tomato seedlings infested with 0 to 1-day-old eggs in 0.1 mg litre−1 resulted in over 90% suppression of egg hatch of both B. tabaci and T. vaporariorum. Pyriproxyfen is registered in the U.S. for flea and tick control in the home and on pets, as well as indoor and outdoor ant and roach control. Formulas include carpet powders, foggers, aerosols, shampoos, bait, and pet collars.
Status:
Possibly Marketed Outside US
Source:
Unknown by Bayer
Source URL:

Class (Stereo):
CHEMICAL (MIXED)



Flumethrin is a type II synthetic pyrethroid insecticide used externally in veterinary medicine against parasitic insects and ticks on cattle, sheep, goats, horses, and dogs, and the treatment of parasitic mites in honeybee colonies. In veterinary medicine, it is applied topically to sheep, cattle, and goats, as a 1% w/v pour-on or as a plunge dip for the control of ticks, lice, and mites. The pour-on is applied at a rate of 2 mg/kg BW. The plunge dip is diluted at a rate of 1-litre product in 900 liters water. For control of scab, the sheep must be dipped for one minute. Plastic strips impregnated with 3.6 mg Flumethrin are hung in beehives for the diagnosis and treatment of varroatosis in honeybees. Four strips per hive are used for mature colonies and 2 per hive for immature colonies. Flumethrin causes a long-lasting prolongation of the normally transient increase in sodium permeability of the nerve membrane during excitation, resulting in long-lasting trains of repetitive firing. The cyano group on the phenoxy-fluorobenzyl alcohol moiety is considered to be responsible for the long-lasting prolongation of sodium permeability. The type II pyrethroids produce a distinct poisoning syndrome which is characterized by choreoathetosis (sinuous writhing of the whole body) and salvation. Flumethrin on the membrane of nerve cells blocking the closure of the ion gates of the sodium channel during re-polarization. This strongly disrupts the transmission of nervous impulses, causing spontaneous depolarization of the membranes or repetitive discharges. At low concentrations insects and other arthropods suffer from hyperactivity. At high concentrations, they are paralyzed and die. Sensory and nervous cells are particularly sensitive. Flumethrin is a complex mixture of stereoisomers. The molecule contains three asymmetric carbon atoms, there is cis-trans isomerism at the cyclopropane ring and cis-trans isomerism at the carbon-carbon double bond of the alkene. So there are 16 different isomers. Commercial Flumethrin typically contains 92% of the trans isomers on the cyclopropane ring and the cis-configuration at the olefinic carbon-carbon double bond and 8% of the isomer with cis geometry on the cyclopropane ring and the cis-configuration at the olefinic carbon-carbon double bond.

Showing 1681 - 1690 of 3134 results