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

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Showing 101 - 110 of 171 results

Zotepine is a potent antipsychotic and antidepressive drug, which was developed in Japan and used in many countries for the treatment of schizophrenia. Zotepine has high affinity to D2, 5-HT2A, 5-HT2C, 5-HT6, 5-HT7, alpha1A, H1, and D1 receptors at therapeutically relevant concentrations and has similar affinities to 5-HT1A, alpha2A, and M1 receptors at high concentrations. In human zotepine is metabolized to a major metabolite, norzotepine, which has profile similar to that of zotepine for important neurotransmitter receptors known to be responsible for zotepine antipsychotic activity.The drug is still available in Asia.
Melperone is an antipsychotic drug which is used in Europe for the treatment of sleep disorders, agitation and confusion states. The exact mechanism of melperone action is unknown.
Status:
Possibly Marketed Outside US
Source:
Alodorm by Good, M.L.|Bryan, S.E.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Nitrazepam (trade names: Alodorm, Apodorm, Arem, Mogadon, Nitrados, Nitrazadon, Nitrosun, Ormodon, Paxadorm, Remnos, and Somnite) is a hypnotic drug of the benzodiazepine class, indicated for the short-term relief of severe, disabling anxiety and insomnia. Nitrazepam has sedative and motor-impairing properties, as well as amnestic, anticonvulsant, and skeletal muscle relaxant effects. Nitrazepam is used to treat short-term sleeping problems (insomnia), namely difficulty falling asleep, frequent awakening, early awakening, or a combination of each. Nitrazepam is sometimes tried to treat epilepsy when other medications fail. It has been found to be more effective than clonazepam in the treatment of West syndrome, which is age-dependent epilepsy, affecting the very young. In uncontrolled studies, nitrazepam has shown effectiveness in infantile spasms and is sometimes considered when other anti-seizure drugs have failed. However, drowsiness, hypotonia, and most significantly tolerance to anti-seizure effects typically develop with long-term treatment, generally limiting Nitrazepam to acute seizure management. More common side effects may include: Central nervous system depression, including somnolence, dizziness, depressed mood, rage, violence, fatigue, ataxia, headache, vertigo, impairment of memory, impairment of motor functions, hangover feeling in the morning, slurred speech, decreased physical performance, numbed emotions, reduced alertness, muscle weakness, double vision, and inattention have been reported. Unpleasant dreams and rebound insomnia have also been reported. Nitrazepam is a long-acting benzodiazepine with an elimination half-life of 15–38 hours (mean elimination half-life 26 hours).
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

2-Dipiperonylaminoethanol is tertiary amine derivative classified by the WHO as an antipsychotic and anxiolytic drug. The compound was patented as antispasmodic medication in 1948.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)


WT-161 is a potent inhibitor of histone deacetylase (HDAC). It inhibits HDAC6, HDAC1, and HDAC2 with IC50 values of 0.4 nM, 8.35 nM, and 15.4 nM. The compound has demonstrated anti-tumor activity in preclinical models of multiple myeloma and breast cancer.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Ethallobarbital (Dormin, Dumex), an oral hypnotic drug that is included in the list of Schedule III drugs of the United States Controlled Substances Act.
Status:
Possibly Marketed Outside US
Source:
Rohypnol by Hoffman-La Roche
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Flunitrazepam is an intermediate-acting benzodiazepine with general properties similar to those of diazepam. It is generally intended to be for short-term treatment for chronic or severe insomniacs who are unresponsive to other hypnotics. The main pharmacological effects of Flunitrazepam are the enhancement of GABA at the GABAA receptor. The physical effects of Flunitrazepam include sedation, muscle relaxation, decreased anxiety, and prevention of convulsions. It causes partial amnesia; individuals are unable to remember certain events that they experience while under the influence of the drug. Chronic use of Flunitrazepam can result in physical dependence and the appearance of a withdrawal syndrome when the drug is discontinued. Flunitrazepam impairs cognitive and psychomotor functions affecting reaction time and driving skill. The use of this drug in combination with alcohol is a particular concern as both central nervous system depressants potentiate each other's toxicity.
Status:
Possibly Marketed Outside US
Source:
NCT02307396: Phase 4 Interventional Completed Schizophrenia
(2015)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Sulpiride is an atypical antipsychotic drug (although some texts have referred to it as a typical antipsychotic) of the benzamide class used mainly in the treatment of psychosis associated with schizophrenia and major depressive disorder, and sometimes used in low dosage to treat anxiety and mild depression. Sulpiride is commonly used in Europe, Russia and Japan. Sulpiride is a selective antagonist at dopamine D2 and D3 receptors. This action dominates in doses exceeding 600 mg daily. In doses of 600 to 1,600 mg sulpiride shows mild sedating and antipsychotic activity. Its antipsychotic potency compared to chlorpromazine is only 0.2 (1/5). In low doses (in particular 50 to 200 mg daily) its prominent feature is antagonism of presynaptic inhibitory dopamine receptors accounting for some antidepressant activity and a stimulating effect. Therefore, it is in these doses used as a second line antidepressant. Racemic and L-sulpiride significantly decreased stimulated serum gastrin concentration, but they did not affect fasting serum gastrin or basal and stimulated gastric acidity. D-sulpiride significantly decreased gastric acid secretion, without affecting serum gastrin levels.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)


Emepronium bromide (Cetiprina) is a quarternary ammonium compound with anticholinergic effects. It is mainly used in the treatment of urinary frequency, urge and urge incontinence and is usually administered orally and occasionally intramuscularly. Emepronium bromide was introduced into Britain, after having been used in Sweden for a number of years. The drug was advocated especially for elderly patients suffering from nocturia and urgency with incontinence, when these were due to causes other than obstruction. It was also advocated for enuresis and hypertonic bladder states following surgery or radiotherapy.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Vinylbital is a barbiturate derivative. It was introduced into therapy in 1963 and used as a sedative and in the treatment of insomnia.

Showing 101 - 110 of 171 results