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

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Showing 351 - 360 of 525 results

Pizotifen (INN) or pizotyline (USAN), trade name Sandomigran, is a benzocycloheptene-based drug used as a medicine, primarily as a preventative to reduce the frequency of recurrent migraine headaches. Pizotifen is a serotonin antagonist acting mainly at the 5-HT2A and 5HT2C receptors. It also has some activity as an antihistamine as well as some anticholinergic activity. The main medical use for pizotifen is for the prevention of vascular headache including migraine and cluster headache. Pizotifen is one of a range of medications used for this purpose, other options include propranolol, topiramate, valproic acid and amitriptyline. While pizotifen is reasonably effective, its use is limited by side effects, principally drowsiness and weight gain, and it is usually not the first choice medicine for preventing migraines, instead being used as an alternative when other drugs have failed to be effective. It is not effective in relieving migraine attacks once in progress. Pizotifen has also been reported as highly effective in a severe case of erythromelalgia, a rare neurovascular disease that is sometimes refractory to the other drugs named above. Side effects include sedation, dry mouth, drowsiness, increased appetite and weight gain. Occasionally it may cause nausea, headaches, or dizziness. In rare cases, anxiety, aggression and depression may also occur. Pizotifen is well absorbed from the gastro-intestinal tract, peak plasma concentrations occurring approximately 5 hours after oral administration. The absorption of pizotifen is fast (absorption half life 0.5 to 0.8 hours) and nearly complete (80%). Over 90% is bound to plasma proteins. Pizotifen undergoes extensive metabolism. Over half of a dose is excreted in the urine, chiefly as metabolites; a significant proportion is excreted in the faeces. The primary metabolite of pizotifen (N-glucuronide conjugate) has a long elimination half-life of about 23 hours.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Acetylleucine is a drug that is used for symptomatic treatment of acute vestibular vertigo and dizziness. Its pharmacodynamics are not fully understood. The hypothesis is that it restores the membrane potential, via an interaction with membrane phospholipids on the injured side of vestibular neurons mainly in the thalamus or parietal region of the cortex. Clinical trials on animals showed an improvement in locomotor balance after forced rotation or unilateral vestibular neurotomy. Acetylleucine has a marketing authorisation in France although there is no evidence of its efficacy on human. Acetylleucine neither reduced the nausea associated with this provocative stimulus, nor hastened the acquisition or retention of vestibular habituation of motion sickness and nystagmus.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Apronalide is an acyclic analog of barbiturates. It was used under tradename "Sedormid" as a sedative an hypnotic agent. In 1934 it was discovered that the drug causes thrombocytopenic purpura. Apronalide is still marketed in Japan, where it is used in combination with caffeine and ibuprofen for the treatment of headache.
Status:
Possibly Marketed Outside US
Source:
Aclimafel by Societe d'Etudes Scientifiques et Industrielles de Ile-de-France
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Veralipride (trade name Agreal, Agradil) is a benzamide neuroleptic medicine indicated in the treatment of vasomotor symptoms associated with the menopause when a contraindication or non-acceptance of hormone therapy (HT) exists. Veralipride is a dopaminergic antagonist of receptor D2, that induces prolactin secretion without any estrogenic or progestagenic effects. Veralipride is well absorbed when administered orally, achieving maximal concentrations at 2.5 hours. It is poorly metabolized and is eliminated in the urine and feces. After oral administration, the half-life is 4 hours, and 44% is excreted without any changes in urine in the first 120 hours. Most of the studies agree that the decrease of vasomotor symptoms associated with the menopause (hot flushes) with veralipride use is from 48.0% to 89.9% depending on the time of use and method of administration. One of the main secondary effects of veralipride use is hyperprolactinemia, which may or may not be accompanied by galactorrhea, and can disappear at 48 hours of treatment withdrawal. The most serious effects that have been reported with veralipride use are those extrapyramidal, such as acute dyskinesia, tardive dyskinesia, Parkinsonism, postural tremor, myoclonia, and dystonia. Many of these have been related to over-dosage and due to the lack of prescription instruction follow-up. The presentation of secondary adverse events is decreased using this medicament at a dose no greater than 100 mg/day, for short time spans, and leaving drug-free intervals between schedules. Veralipride has never gained approval in the United States. On July 2007, the EMA recommended the withdrawal of marketing authorizations for veralipride. The still in use Mexican Official Norm for the prevention and control of perimenopausal and postmenopausal diseases in women establishes that the drug can be useful in the control of vasomotor symptoms.
Toloxatone is an antidepressant launched in 1984 in France for the treatment of depression. It is a selective reversible inhibitor of MAO-A (RIMA).
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (UNKNOWN)

Dixyrazine is a typical antipsychotic of the phenothiazine group. Under a trademark Esucos, the drug was used in European countries as an antipsychotic, antiemetic and sedative with oral doses ranging from 20 to 75 mg daily. Dixyrazine has also been given by injection.
Status:
Possibly Marketed Outside US
Source:
Unknown by Janssen Pharmaceutica
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Penfluridol is a highly potent; first generation diphenylbutylpiperidine antipsychotic was developed by Janssen Pharmaceutica in 1968 and is used to treat schizophrenial and similar psychotic disorders. It is, however, like most typical antipsychotics, being increasingly replaced by the atypical antipsychotics. This drug is long-acting dopamine receptor blocker.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (MIXED)



Valnoctamide is a valproic acid derivative associated with a decreased risk for congenital abnormalities and developed by Beersheva Mental Health Center for treatment mania. Valnoctamide has been marketed as an anxiolytic and sedative in several European countries (as Nirvanil), including Italy, Holland, and Switzerland, until the year 2000 but was not actively promoted as an anticonvulsant. It was marketed in the U.S. as Axiquel by McNeil Laboratories in the 1970s. In mice, valnoctamide has been shown to be distinctly less teratogenic than valproic acid. Injection of 3 mkmol ⁄ kg at day 8 of gestation produced only 1% exencephaly (as compared to 0–1% in control mice and 53% in valproate-treated mice). Embryolethality rates showed similar results: 52% with valproate versus 5% in the controls and 2% with valnoctamide. Valnoctamide's patent is expired, and it is not the property of any major pharmaceutical company. Valnoctamide has potential as a therapy in epilepsy including status epilepticus (SE) and neuropathic pain and is currently being developed for the treatment of mania and Schizoaffective Disorder. In clinical trials, Valnoctamide was well tolerated but lacked efficacy in the treatment of symptoms in patients with acute mania.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (MIXED)

Chlorhexadol (or Chloralodol), a hypnotic compound which is included in the list of Schedule III drugs of the United States Controlled Substances Act.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (EPIMERIC)

Bornaptine is a synthetic anticholinergic drug. The compound is a nonselective M1 and M4 antagonist and was shown to inhibit the negative inotropic response to carbachol in the isolated left atrium of the rat with pA2 of 7.27. Bornaprine is used for the treatment of symptoms of Parkinson's disease. A clinical trial showed the superiority of Bornaprine over placebo in reducing parkinsonian tremor. Bornaptine demonstrated positive results in localized hyperhidrosis.

Showing 351 - 360 of 525 results