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

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Showing 371 - 380 of 525 results

Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Flumedroxone is a progestative agent. It is a pregnane derivative substituted at C-6 by a trifluoromethyl group. It was tested whether flumedroxone had prophylactic value in migraine. No benefit was found in males, or in females with no history of menstrual exacerbation of migraine. In women whose migraine was worse around the time of menstruation flumedroxone resulted in statistically fewer headaches of less severity. With the dose used in this trial side-effects were frequent, the commonest being polymenorrhagia, which occurred in half the women of reproductive age.
Status:
Possibly Marketed Outside US
Source:
Japan:Nizofenone Fumarate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Nizofenone (Ekonal, Midafenone) is a neuroprotective drug which protects neurons from death following cerebral anoxia (interruption of oxygen supply to the brain). It might thus be useful in the treatment of acute neurological conditions such as stroke. Nizofenone ameliorates various pathophysiologic events during ischemia, such as ATP depletion, lactate accumulation, glutamate release, free fatty acid liberation, edema, and neuronal degeneration; in particular, ischemia-induced excessive glutamate release has been completely blocked by this drug. This drug has also radical-scavenging action, comparable to vitamin E, and inhibits oxygen radical-induced lipid peroxidation. The potent cerebroprotective effect of nizofenone has been demonstrated in various experimental models of cerebral hypoxia, ischemia (focal and global), ischemia-reperfusion, and infarction. The clinical efficacy of nizofenone has been proved by pioneering double-blind studies in acute subarachnoid hemorrhage patients. Nizofenone is clinically used for preventing the delayed ischemic neurologic deficits due to late vasospasm following subarachnoid hemorrhage.
Status:
Possibly Marketed Outside US
Source:
NCT02307396: Phase 4 Interventional Completed Schizophrenia
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Perazine (Taxilan) is a moderate-potency typical antipsychotic of the phenothiazine class. Perazine is an older antipsychotic drug first introduced in the 1950s. It is suggested to have a low level of side effects (especially for movement disorders). Its use is regional and restricted to countries like Germany, Poland, the Netherlands and the former Yugoslavia. Perazine has being shown to be a potent inhibitor of human CYP1A2. It acts as a dopamine antagonist.
Etifoxine (etafenoxine, StresamⓇ) is a non-benzodiazepine anxiolytic with an anticonvulsant effect. It was developed in the 1960s for anxiety disorders and is currently being studied for its ability to promote peripheral nerve healing and to treat chemotherapy-induced pain. In addition to being mediated by GABA-A2 receptors like benzodiazepines, etifoxine appears to produce anxiolytic effects directly by binding to 2 or 3 subunits of the GABAA receptor complex. It also modulates GABAA receptors indirectly via stimulation of neurosteroid production after etifoxine binds to the 18 kDa translocator protein (TSPO) of the outer mitochondrial membrane in the central and peripheral nervous systems, previously known as the peripheral benzodiazepine receptor (PBR). Therefore, the effects of etifoxine are not completely reversed by the benzodiazepine antagonist flumazenil. Etifoxine is used for various emotional and bodily reactions followed by anxiety. It is contraindicated in situations such as shock, severely impaired liver or kidney function, and severe respiratory failure. The average dosage is 150 mg per day for no more than 12 weeks. The most common adverse effect is drowsiness at the initial stage. It does not usually cause any withdrawal syndromes. In conclusion, etifoxine shows less adverse effects of anterograde amnesia, sedation, impaired psychomotor performance, and withdrawal syndromes than those of benzodiazepines.
Status:
Possibly Marketed Outside US
Source:
Japan:Xaliproden Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Xaliproden is an orally active 5HT1-A receptor antagonist that was being developed by Sanofi. It has been evaluated for the treatment of Alzheimer's disease and amyotrophic lateral sclerosis (ALS), and protection against peripheral neurotoxicity associated with certain cancer chemotherapies. Two large, 18-month, clinical trials of xaliproden (monotherapy or adjunctive therapy, respectively) in patients with mild to moderate AD (MMSE, 16–26, inclusive) were completed in 2007. Failure to demonstrate sufficient efficacy in both trials resulted in cancelation of the xaliproden development program for AD in September 2007.
Status:
Possibly Marketed Outside US
Source:
NCT01363648: Phase 4 Interventional Completed Cognitive Impairment
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Choline alfoscerate (alpha-Glycerylphosphorylcholine or Alpha-GPC) is a nootropic choline-containing phospholipid. Choline alphoscerate increases the release of acetylcholine in rat hippocampus, facilitates learning and memory in experimental animals, improves brain transduction mechanisms and decreases age-dependent structural changes occurring in rat brain areas involved in learning and memory. The compound exerts neuroprotective effects in models of altered cholinergic neurotransmission and of brain vascular injury. In clinical studies choline alphoscerate improved memory and attention impairment, as well as affective and somatic symptoms in dementia disorders. In Europe alpha-GPC is a prescription medication for the treatment of Alzheimer's disease. It is available in two forms; one is taken by mouth, and the other is given as a shot. In the United States alpha-GPC is only available as a dietary supplement, mostly in products promoted to improve memory. Other uses for alpha-GPC include treatment of various kinds of dementia, stroke, and "mini-stroke" (transient ischemic attack, TIA). Alpha-GPC is also used for improving memory, thinking skills, and learning.
Flunarizine is a selective calcium entry blocker with calmodulin binding properties and histamine H1 / dopamine D2 blocking activity. It is not available in the US but marketed in other countries for prophylaxis of a migraine, occlusive peripheral vascular disease, the vertigo of central and peripheral origin, motion sickness and as an adjuvant in the therapy of epilepsy. The drug is also investigated for the treatment of schizophrenia.
Status:
Possibly Marketed Outside US
Source:
Japan:Mosapramine Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Mosapramine (Cremin) is used to treat chronic schizophrenia in Japan. It is a potent dopamine antagonist with high affinity to the dopamine receptor subtypes 2, 3 and 4, and with moderate affinity for the 5-HT2 receptors
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Propacetamol is a bioprecursor of paracetamol. It is rapidly hydrolyzed by plasma esterases and releases its constituent paracetamol by the end of its intravenous or intramuscular administration. Its metabolism is identical to that of paracetamol. It is used in post-operative care and is delivered by I.V. It is given if the patient is unable to take oral or rectally delivered paracetamol and non-steroidal anti-inflammatory drugs are contraindicated. The onset of analgaesia from propacetamol is more rapid than paracetamol given orally. 2 g of propacetamol are equivalent to 1g of paracetamol.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

1,6-Dimethyl-3-carbethoxy-4-oxo-6,7,8,9-tetrahydro-homopyrimidazol (rimazolium, MZ-144) is an analgesic (non-narcotic). It proved to be effective in all the analgesic assays used (independently of the nociceptive stimulus applied) (hot plate, tail flick, writhing tests, Randall-Selitto test, tail clip, surgical pain) differing in this respect from the nonsteroidal antiinflammatory analgetics. Rimazolium lacks the capacity of producing opiate-like physiological dependence. Also rimazolium fails to show any indication of narcotic-like abuse liability by any of clinical assessments. Rimazolium is registered in Hungary under the brand name Probon. In Hungary among analgesics Probon is the first of choice especially in case of chronic pain accompanying chronic respiratory tract diseases.

Showing 371 - 380 of 525 results