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

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Showing 301 - 310 of 525 results

Status:
Possibly Marketed Outside US
Source:
NCT00000300: Phase 4 Interventional Completed Opioid-Related Disorders
(1995)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Levomethadyl acetate (LAAM) is a synthetic opioid agonist with actions qualitatively similar to morphine (a prototypic mu agonist) and affecting the central nervous system (CNS) and smooth muscle. Principal actions include analgesia and sedation. Tolerance to these effects develops with repeated use. An abstinence syndrome generally occurs upon cessation of chronic administration similar to that observed with other opiates, but with slower onset, more prolonged course, and less severe symptoms. LAAM exerts its clinical effects in the treatment of opiate abuse through two mechanisms. First, LAAM cross-substitutes for opiates of the morphinetype, suppressing symptoms of withdrawal in opiate-dependent individuals. Second, chronic oral administration of LAAM can produce sufficient tolerance to block the subjective “high” of usual doses of parenterally administered opiates. Since the introduction of levomethadyl in 1995, the manufacturer has received increasing reports of severe cardiac-related adverse events, including QT interval prolongation, Torsades de Pointes and cardiac arrest. Other cardiac-related adverse events have also been reported, including arrhythmias, syncope, and angina. These events led to the removal of levomethadyl from the European market in March 2001. A very small number of patients may benefit from levomethadyl, but the risk of continued distribution and use no longer outweighs the overall benefits.
Propanidid (Epontol) is an analgetically potent and shortterm anesthetic, widely used in the 1960s. It was originally introduced by Bayer in 1963. Epontol, an injectable emulsion formulation of propanidid, provided by Bayer, was withdrawn from the market in Great Britain in 1983 because of concern over anaphylactoid reactions. Thus, in spite of the fact that propanidid provides shorter and more predictable recovery times than propofol, it has not been accepted widely as an injectable anesthetic. Even though Cremophor EL has been shown to cause anaphylactic reactions in humans in several cases (both when given intravenously and orally), it is still debated whether or not propanidid itself may have contributed to the reactions. It has been argued that the toxic effects or reactions to propanidid (and Althesin) were due to the drugs themselves. Several cases of negative reactions have been recorded for different drugs using Cremophor EL as solubilizer. This suggest that the negative reactions were mainly caused by Cremophor and not by the drug substances themselves. Propanidid is presumed to work as a GABA receptor agonist.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Chlorproethazine (Neuriplege) is a neuroleptic, antipsychotic and muscle relaxant. Neuriplege® cream was available as a non‐prescription medication in France until its withdrawal from the market by regulatory authorities in January 2007. Neuriplege caused phototoxicity and photocontact allergy.
Status:
Possibly Marketed Outside US
Source:
Operidine by Janssen Pharmaceutica
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Conditions:

PHENOPERIDINE is an opioid analgesic partly metabolized to meperidine in the liver. It is derived from pethidine by replacing the N methyl by a phenyl propanol chain. It is reputed to be a typical morphine-like analgesic characterized by its high potency, rapid onset of action, the intensity of its peak effect and the short duration of its pharmacological effects. It is used in general anesthesia.
Status:
Possibly Marketed Outside US
Source:
NCT04249596: Phase 4 Interventional Recruiting Treatment Resistant Depression
(2020)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


TIANEPTINE, a tricyclic antidepressant, is a drug used for the treatment of the major depressive disorder. It was discovered by The French Society of Medical Research in the 1980s. Unlike other tricyclic antidepressants, TIANEPTINE is a selective serotonin reuptake enhancer with minimal effects on norepinephrine and dopamine uptake. Also, it is a full agonist at the mu-opioid and delta-opioid receptors with no effect at the kappa-opioid receptors. Selective mu-opioid agonists typically induce euphoria, which may contribute to TIANEPTINE's antidepressant effect. It is marketed as Coaxil/Stablon in many European countries, but it is not available in the US.
Medazepam is a benzodiazepine drug with anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. It is known by the following brand names: Azepamid, Nobrium, Tranquirax (mixed with bevonium), Rudotel, Raporan, Ansilan and Mezapam. Marketed in Russia. Indicated for the treatment of neurotic disorders and states, accompanied with sense of fear, anxiety, intension, raised irritability, insomnia, vegetative lability.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Benzoctamine (Tacitin), a psychotropic drug, known to exert in man an anti-anxiety effect. Its action also was studied when given as a hypnotic or sedative in patients with respiratory failure. Benzoctamine decreases 5-HT turnover in the brain and this action may play a role in the anti-anxiety effect of the drug.
Status:
Possibly Marketed Outside US
Source:
NCT02307396: Phase 4 Interventional Completed Schizophrenia
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Sertindole (brand names: "Serdolect" and "Serlect") is an antipsychotic medication. Sertindole was developed by the Danish pharmaceutical company Lundbeck and marketed under license by Abbott Labs. Like other atypical antipsychotics, it has activity at dopamine and serotonin receptors in the brain. It is used in the treatment of schizophrenia. Sertindole is not approved for use in the United States and was discontinued in Australia in January 2014. In Europe, sertindole was approved and marketed in 19 countries from 1996, but its marketing authorization was suspended by the European Medicines Agency in 1998 and the drug was withdrawn from the market. In 2002, based on new data, the EMA's CHMP suggested that Sertindole could be reintroduced for restricted use in clinical trials, with strong safeguards including extensive contraindications and warnings for patients at risk of cardiac dysrhythmias, a recommended reduction in maximum dose from 24 mg to 20 mg in all but exceptional cases, and extensive ECG monitoring requirement before and during treatment.
Status:
Possibly Marketed Outside US
Source:
PIPORTIL L4 by Puech, A.J.|Chermat, R.|Malatray, J.|Simon, P.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Pipotiazine (Piportil), also known as Pipothiazine, is a typical antipsychotic of the phenothiazine class used in the United Kingdom and other countries for the treatment of schizophrenia. Its properties are similar to those of chlorpromazine. Piportil® L4 (pipotiazine palmitate) is the palmitic ester of pipotiazine, a piperidine phenothiazine with antipsychotic properties and weak sedative activity. The esterification of pipotiazine is responsible for its prolonged duration of action. The onset of action appears usually within the first 2 to 3 days after injection and the effects of the drug on psychotic symptoms are significant within one week. Improvement in symptomatology lasts from 3 to 6 weeks, but adequate control may frequently be maintained with one injection every 4 weeks. However, in view of the variations in individual response, careful supervision is required throughout treatment. Piportil L4 has actions similar to those of other phenothiazines. Among the different phenothiazine derivatives, Piportil L4 appears to be less sedating and to have a weak propensity for causing hypotension or potentiating the effects of CNS depressants and anesthetics. However, it produces a high incidence of extrapyramidal reactions.
Trifluperidol is an antipsychotic butyrophenone derivative. It is a high-affinity sigma receptor blocker and it was strongly selective for NR1a/2B receptors. It exhibit pharmacological effects and a mechanism of action very similar to that of phenothiazines and thioxanthenes in that it blocks dopaminergic receptors. It is more selective with respect to D2 receptors. Trifluperidol is indicated for the treatment of acute and chronic schizophrenia, mania and hypomania, organic psychoses, childhood behavioral disorders, agitation in psychotic illness and motor tics. Trifluperidol has been suspected as a cause of cataract in Japan. Patients receiving trifluperidol treatment may develop a parkinsonian-like syndrome which responds to withdrawal of the drug or concurrent administration of an anti-parkinsonian drug. Acute dystonias and akathisia are other acute extrapyramidal effects; tardive dyskinesia may supervene after longer periods of treatment.

Showing 301 - 310 of 525 results