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

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Showing 311 - 320 of 322 results

Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Guanazodine is a new antihypertensive drug. Guanazodine caused a sustained decrease in the systemic blood pressure of spontaneously hypertensive rats, renal hypertensive dogs and normal cats. No tachyphylaxis developed when the drug was administered orally. The heart rate decreased. Guanazodine relaxed the cat nictitating membrane, attenuated the positive chronotropic response to sympathetic nerve stimulation in anesthetized dogs and in isolated rabbit aorta to transmural electrical stimulation. Guanazodine potentiated the pressor response to noradrenaline but attenuated the response to tyramine in anesthetized cats. It may be concluded that the hypotensive effect of guanazodine is related to adrenergic neuron blocking action, the noradrenaline-depleting action in peripheral tissues is similar to the effect of guanethidine and bethanidine. However, this drug is less potent than guanethidine. Toxicity and side effects appear to be less with guanazodine than with guanethidine and bethanidine.
Status:
Possibly Marketed Outside US
Source:
Pirroksan by All-Union Scientific-Research Chemical-Pharmaceutical Institute
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Proroxan is a non-selective а-adrenoblocker. Proroxan was found to prevent the development of hypertensive crises and improve cerebral bioelectrical parameters in most of hypertensive patients. Proroxan has been used as an antihypertensive and in the treatment of Ménière’s disease, motion sickness, and allergic dermatitis.
Status:
Possibly Marketed Outside US
Source:
Japan:Norfenefrine Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Norfenefrine or meta-octopamine, also known as 3,β-dihydroxyphenethylamine, is an adrenergic agent used as a sympathomimetic drug which is marketed in Europe, Japan, and Mexico. Along with its structural isomer p-octopamine and the tyramines, norfenefrine is a naturally occurring, endogenous trace amine and plays a role as a minor neurotransmitter in the brain. Norfenefrine controls blood pressure in acute hypotensive states eg pheochromocytomectomy, sympathectomy, poliomyelitis, spinal anesth, MI, septicemia, blood transfusion and drug reactions. Adjunct in treatment of cardiac arrest and hypotension.
Status:
Possibly Marketed Outside US
Source:
UK NHS:Tramazoline hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Tramazoline is a sympathomimetic drug that is used in the form of tramazoline hydrochloride in nasal decongestant preparations. Tramazoline is an α-adrenergic receptor agonist that inhibits secretion of nasal mucus.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Trimazosin was originated by Pfizer and was licensed to Bristol-Myers Squibb worldwide except for Canada, Mexico and the USA. Trimazosin is a quinazoline antihypertensive agent structurally related to the selective alpha 1-adrenoceptor blocker prazosin. Trimazosin is an alpha adrenergic receptor antagonist. Compared with prazosin, trimazosin was a less potent but more efficacious hypotensive agent. At doses which caused equal or even greater hypotensive effects than those caused by prazosin, trimazosin caused less inhibition of pressor responses to phenylephrine. When administered during a maximum hypotensive response to prazosin, trimazosin caused an additional fall in pressure. Trimazosin is an effective antihypertensive when given by itself or in combination with a diuretic. Its ability to induce vasodilation without concomitant sodium retention or stimulation of the renin axis may be an important factor in its effectiveness. Trimazosin has the potential to cause sustained improvement in left ventricular function, both at rest and during exercise, in patients with chronic congestive heart failure (CHF).
Alpha-ketoglutarate (AKG), an endogenous intermediary metabolite in the Krebs cycle, is a molecule involved in multiple metabolic and cellular pathways. As an intermediate of the tricarboxylic acid cycle, AKG is essential for the oxidation of fatty acids, amino acids, and glucose. Extracellular AKG is a significant source of energy for cells of the gastrointestinal tract. As a precursor for the synthesis of glutamate and glutamine in multiple tissues (including liver, skeletal muscle, heart, brain, and white adipose tissue), AKG bridges carbohydrate and nitrogen metabolism for both conservation of amino acids and ammonia detoxification. Additionally, emerging evidence shows that AKG is a regulator of gene expression and cell signaling pathways (including the mammalian target of rapamycin and AMPactivated protein kinase). Thus, AKG is an attractive dietary supplement in animal and human nutrition to improve cellular energy status, immunity, and health.AKG can decrease protein catabolism and increase protein synthesis to enhance bone tissue formation in the skeletal muscles and can be used in clinical applications. In addition to these health benefits, a recent study has shown that AKG can extend the lifespan of adult Caenorhabditis elegans by inhibiting ATP synthase and TOR. Orally, AKG is used for kidney disease, gastrointestinal disorders, bacterial overgrowth, intestinal toxemia, liver dysfunction, and chronic candidiasis. It is also used for improving peak athletic performance, improving amino acid metabolism in hemodialysis patients, and cataracts. Intravenously, AKG is used for preventing ischemic injury during heart surgery, improving renal blood flow after heart surgery, and preventing muscle protein depletion after surgery or trauma.
Status:
Possibly Marketed Outside US
Source:
UK NHS:Moxisylyte hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Moxisylyte, also known as thymoxamine, is a drug used in urology for the treatment of erectile dysfunction, also was studied, that this drug may be useful to treat ocular disorders such as diabetic retinopathy. It is an alpha1-adrenergic antagonist. Was developed for self-injection therapy in France and marketed in several European countries as Icavex. In the spring 2005 the manufacturer of Icavex decided to withdraw this drug from Europe market, presumable due to its low market shares.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Debrisoquin is an antihypertensive drug having guanethidine-like properties, which inhibits monoamine oxidase (MAO) and does not enter the brain. Debrisoquine was used for the treatment of hypertension. Debrisoquine hydroxylation phenotype has been the most used test in humans to evaluate CYP2D6 activity. Two debrisoquine hydroxylation phenotypes have been described: poor and extensive metabolizers. A group with a very low debrisoquine metabolic ratio within the extensive metabolizers, named ultrarapid metabolizers, has also been distinguished. This CYP2D6 variability can be for a large part alternatively determined by genotyping, which appears to be of clinical importance given CYP2D6 involvement in the metabolism of a large number of commonly prescribed drugs.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

mixture
Status:
First approved in 1953
Source:
Hydergine by Sandoz
Source URL:

Class:
MIXTURE



Ergoloid mesylates (USAN), co-dergocrine mesilate (BAN) or dihydroergotoxine mesylate, trade name Hydergine, is a mixture of the methanesulfonate salts of three dihydrogenated ergot alkaloids (dihydroergocristine, dihydroergocornine, and alpha- and beta-dihydroergocryptine). It was developed by Albert Hofmann (the inventor of LSD) for Sandoz (now part of Novartis). Ergoloid mesylates act centrally, decreasing vascular tone and slowing the heart rate, and acts peripherally to block alpha-receptors. One other possible mechanism is the effect of ergoloid mesylates on neuronal cell metabolism, resulting in improved oxygen uptake and cerebral metabolism, thereby normalizing depressed neurotransmitter levels. Ergoloid Mesylate may increase cerebral metabolism and blood flow. The role of this medication in the therapy of dementia is controversial. A recent controlled study in patients with Alzheimer's disease found that there was no advantage to the use of ergoloid mesylates compared to placebo, suggesting that ergoloid mesylates may lower scores on some cognitive and behavioral rating scales. Further study is needed to determine the risk-benefit profile of ergoloid mesylates in the treatment of dementia.

Showing 311 - 320 of 322 results