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

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Showing 31 - 40 of 144 results

Suloctidil is considered to be calcium antagonist. In addition to its vascular antispasmodic activity, suloctidil affects blood platelets and enhances brain energy metabolism. Suloctidil was being evaluated in many clinical trials for use in dementia and thrombotic disorders. Suloctidil induces hepatotoxicity.
Status:
Possibly Marketed Outside US
Source:
ZANIDIP by Corsini, A.|Bonfatti, M.|Quarato, P.|Accomazzo, M.R.|Raiteri, M.|Sartani, A.|Testa, R.|Nicosia, S.|Paoletti, R.|Fumagalli, R.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



(R)-Lercanidipine is enantiomer of antihypertensive drugs Lercanidipine, that acts by blocking L-type calcium channels, allowing relaxation and opening of blood vessels. The dihydropyridine calcium antagonists promote systemic vasodilatation by a reversible blockade of voltagedependent Ca2+ influx through L-type channels in the cell membrane. (S)-Lercanidipine has 100- to 200-fold greater affinity than the (R)-enantiomer for the L-type calcium channel. The pharmacokinectics of (S)- Lercanidipine has been evaluated in healthy volunteers, in elderly and non-elderly patients with hypertension, and in patients with renal or hepatic impairment. Patients from these studies were investigated after receiving a single 10 or 20 mgdose of [14C]-labeled rac-Lercanidipine as a solution. The maximum plasma concentrations of (S)-Lercanidipine were reached within 2–3 h and the area under the plasma concentration–time curves were not linearly related to the dose, indicating a saturable first-pass metabolism. The absorption of (S)-LER increases after the ingestion of a highfat meal. Lercanidipine is highly bound to plasma protein (>98%) in humans. Its volume of distribution of 2–2.5 L/kg was determined in healthy volunteers after intravenous infusion of 2 mg. Lercanidipine is extensively metabolized by CYP 3A4 to inactive pyridine derivatives. A crossover study involving a single administration of either 10 mg of (R)- or (S)-LER or 20 mg of rac-LER as a solution demonstrated no in vivo enantiomer interconversion
Status:
Possibly Marketed Outside US
Source:
ZANIDIP by Corsini, A.|Bonfatti, M.|Quarato, P.|Accomazzo, M.R.|Raiteri, M.|Sartani, A.|Testa, R.|Nicosia, S.|Paoletti, R.|Fumagalli, R.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



(S)-Lercanidipine is enantiomer of antihypertensive drugs Lercanidipine, that acts by blocking L-type calcium channels, allowing relaxation and opening of blood vessels. The dihydropyridine calcium antagonists promote systemic vasodilatation by a reversible blockade of voltage-dependent Ca2+ influx through L-type channels in the cell membrane. (S)-Lercanidipine has 100- to 200-fold greater affinity than the (R)-enantiomer for the L-type calcium channel. The pharmacokinetics of (S)- Lercanidipine has been evaluated in healthy volunteers, in elderly and non-elderly patients with hypertension, and in patients with renal or hepatic impairment. Patients from these studies were investigated after receiving a single 10 or 20 mg dose of [14C]-labeled rac-Lercanidipine as a solution. The maximum plasma concentrations of (S)-Lercanidipine were reached within 2–3 h and the area under the plasma concentration-time curves were not linearly related to the dose, indicating a saturable first-pass metabolism. The absorption of (S)-LER increases after the ingestion of a high-fat meal. Lercanidipine is highly bound to plasma protein (>98%) in humans. Its volume of distribution of 2–2.5 L/kg was determined in healthy volunteers after intravenous infusion of 2 mg. Lercanidipine is extensively metabolized by CYP 3A4 to inactive pyridine derivatives. A crossover study involving a single administration of either 10 mg of (R)- or (S)-LER or 20 mg of rac-LER as a solution demonstrated no in vivo enantiomer interconversion
Potassium Glycerophosphate is a source of potassium. It is used in the treatment of nutritional deficiencies. Potassium supplements can be an important part of the recovery from or prevention of many different ailments and diseases. The most common of these include helping lower blood pressure and serving as a stroke preventative. Potassium can also be used to lower levels of calcium, to help with certain diseases including Alzheimer’s and Meniere’s. It may also help with some more common issues such as a common allergy, migraines, heavy acne, alcohol abuse, dizziness and confusion, extreme fatigue, recurring constipation, insomnia, anger and aggression, irregular heartbeat and stress. Potassium can either be taken as a supplement by mouth or it can be given intravenously to certain patients who require a faster dosing of the mineral or cannot take it orally.
Watanidipine (AE0047) had been NDA filed for the treatment of hypertension in Japan. Watanidipine (as Calbren®) was awaiting registration with Mitsubishi Pharma Corporation in Japan. However, Mitsubishi Pharma Corporation has discontinued the development of this drug. Watanidipine had also been in phase II clinical trials for the treatment of stroke and preclinical trials for atherosclerosis. However, no recent development has been reported. Watanidipine (AE0047) has being shown to be a calcium antagonist with protective effects against cerebral ischaemia and the occurrence of stroke in several animal models.
Status:
Possibly Marketed Outside US
Source:
Japan:Cilnidipine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Cilnidipine (FRC-8653) is a dihydropyridine (DHP) type of calcium channel antagonist. The L-type Ca2+ channel blockade by cilnidipine affects predominantly vascular smooth muscle, thereby producing vasodilation of peripheral resistance vessels and coronary arteries. The blockade of N-type Ca2+ channels affects predominantly peripheral nerve endings of sympathetic neurons, thereby dilating blood vessels by lowering plasma catecholamine levels. Furthermore, renoprotective and neuroprotective effects as well as cardioprotective action of cilnidipine have been demonstrated in clinical practice or animal examinations. Cilnidipine was originated by Fuji & Rebio Pharmaceutical Co., Ltd. and developed jointly with Ajinomoto for the treatment of hypertension. Cilnidipine has been launched in Japan.
Ximelagatran (Exanta or Exarta, H 376/95) is an anticoagulant that has been investigated extensively as a replacement for warfarin that would overcome the problematic dietary, drug interaction, and monitoring issues associated with warfarin therapy. In 2006, its manufacturer AstraZeneca announced that it would withdraw pending applications for marketing approval after reports of hepatotoxicity (liver damage) during trials, and discontinue its distribution in countries where the drug had been approved (Germany, Portugal, Sweden, Finland, Norway, Iceland, Austria, Denmark, France, Switzerland, Argentina and Brazil). Ximelagatran is a prodrug that is rapidly converted after oral administration to the active compound melagatran. Melagatran is able to inhibit thrombin activity directly and quickly. The melagatran molecule binds to the arginine side pocket of thrombin, inactivating the thrombin. Following oral administration of ximelagatran, oral bioavailability (measured as melagatran) is 18% to 25%. Peak melagatran levels after a ximelagatran dose of 48 mg twice daily are achieved within approximately 2 hours. Ximelagatran is rapidly and extensively converted to melagatran in the liver and other tissues. This conversion is achieved by ester hydrolysis and reduction via two intermediate metabolites, hydroxymelagatran, and ethylmelagatran. The predominant compound in plasma is the active drug, melagatran. The elimination half-life of melagatran after an oral dose of ximelagatran is 2.5 to 4.3 hours.
Status:
Possibly Marketed Outside US
Source:
Japan:Arundic Acid
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



ARUNDIC ACID (ONO-2506) is an enantiomeric, three carbon atom homolog of valproic acid under development by ONO Pharmaceutical for the potential treatment of stroke, as well as Amyotrophic Lateral Sclerosis and Parkinson's disease. The injectable formulation (Proglia) is finished phase III trials for acute-phase cerebral infarction, and the oral formulation (Cereact) is finished phase II trials in the UK for Alzheimer's disease (AD) and Parkinson's disease (PD). ARUNDIC ACID restores normal astrocyte functions after brain damage by preventing reactive astrocytosis, by activating astrocytic GABAA receptors and suppressing GABA transferase. ARUNDIC ACID inhibits S-100β synthesis in activated cultured astrocytes. This agent has additional antiglutamate and antiinflammatory COX-2 inhibitor properties
Gastrodin is the main bioactive component of Gastrodia elata Blume (G. elata). Tian Ma Su Zhu She Ye (contains Gastrodin) It is an extensively used in the clinical practice of traditional Chinese medicine, to treat neurasthenia, neurasthenia syndrome, angioneurotic headache disorder, traumatic brain syndrome, vertigo meniere disease, medicinal with dizziness, vertigo, sudden deafness, vestibular neuronitis, vertebral basilar artery blood supply deficiency, etc. Apart from traditional claims, scientific reports support the antioxidative, anticonvulsive, antiinflammatory, antiepileptic, antiobesity, anxiolytic, and learning and memory improvements in activities of gastrodin
Losartan is a selective, competitive angiotensin II receptor type 1 (AT1) antagonist. Losartant is recommended as one of several preferred agents for the initial management of hypertension. Administration of losartan reduces the risk of stroke in patients with hypertension and left ventricular hypertrophy. Losartan is indicated for the treatment of diabetic nephropathy with an elevated serum creatinine and proteinuria in patients with type 2 diabetes and a history of hypertension.