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

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Showing 51 - 60 of 68 results

Status:
Possibly Marketed Outside US
Source:
NCT02022592: Phase 4 Interventional Completed Sedation in Intensive Care Unit Patients
(2014)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Lormetazepam (or methyl-lorazepam), possesses hypnotic, anxiolytic, sedative and skeletal muscle relaxant properties. Lormetazepam is not approved for sale in the United States or Canada, though it is licensed in the Netherlands as 1 and 2 mg tablets, under the brand names Loramet and Noctamid and as generic, available from several different manufacturers. Lormetazepam is a short-acting benzodiazepine and is sometimes used in patients who have difficulty in maintaining sleep or falling asleep. Lormetazepam binds to the benzodiazepine receptor which in turn enhances the effect of the GABAA receptor producing its therapeutic effects as well as adverse effects. Lormetazepam appears to be more selective in the type of benzodiazepine receptor it binds to showing a higher affinity for the omega 1 receptor which is responsible for sedation. Changes in electroencephalography can therefore be used to measure the sedative sleep promoting properties of lormetazepam.
Status:
Possibly Marketed Outside US
Source:
Bromisoval by Knoll
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Bromisoval (INN; aka bromvalerylurea) is a hypnotic and sedative compound of the bromoureide group discovered by Knoll in 1907 and patented in 1909. It is marketed over the counter in Asia under various trade names (such as Brovarin) usually in combination with non-steroidal anti-inflammatory drugs. Chronic use of bromisoval has been associated with bromine poisoning. Bromovisal can be prepared by bromination of isovaleric acid by the Hell-Volhard-Zelinsky reaction followed by reaction with urea. Bromvalerylurea (BU) can suppress expression of many kinds of pro- and anti-inflammatory mediators in LPS- or interferon-γ activated alveolar and peritoneal macrophages. Bromisoval was found to ameliorate sepsis in rats. It also prevents elevated serum-IL-6 level as well as IL-6 mRNA expression in septic rats. Bromisoval was also found useful for inflammatory skin disorders. The compound is able to suppress the TLR ligands-induced proinflammatory response similar to the steroid DEX without the side effects often associated with the steroid usage.
Status:
Possibly Marketed Outside US
Source:
Lendormin by Takeda Pharmaceutical
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Brotizolam (marketed under brand name Lendormin) is a sedative-hypnotic thienotriazolodiazepine drug which is a benzodiazepine analog. It possesses anxiolytic, anticonvulsant, hypnotic, sedative and skeletal muscle relaxant properties, and is considered to be similar in effect to short-acting benzodiazepines such as triazolam. It is used in the short-term treatment of severe or debilitating insomnia and in a dose of 0.25 mg can be used as a premedication prior to surgery, this dose was found to be comparable in efficacy to 2 mg flunitrazepam as a premedicant prior to surgery. The drug was developed by a team led by T Nishiyama while working for Takeda Chemical Industries in 1976 in Japan. Brotizolam is not approved for sale in the UK, United States or Canada. It is approved for sale in the Netherlands, Germany, Spain, Belgium, Luxembourg, Austria, Portugal, Israel, Italy, Taiwan and Japan. Insomnia. Brotizolam is prescribed for the short-term treatment, 2–4 weeks only of severe or debilitating insomnia. Insomnia can be described as a difficulty falling asleep, frequent awakening, early awakenings or a combination of each. Brotizolam inhibits the hypothalamus and cerebral limbic system controlling emotion through GABA, a typical inhibitory transmitter of central nervous system. As a result, unnecessary stimulation from the autonomic nervous system and other sites is blocked, demonstrating central nervous action including hypnosis, sedation and anti-anxiety
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Allobarbital (5,5-diallylbarbituric acid) is a medium to long-acting barbiturate. It is under international control according to the UN Convention on Psychotropic Substances (Schedule IV). It is used as a sedative and hypnotic and in combination with acetaminophen and codeine as an analgesic. Allobarbital exerts anticonvulsive activity through GABA-ergic mechanisms. Sulfuric derivatives of allobarbital may exert anti-inflammatory activity.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Cyclobarbital (5-cyclohexenyl-5-ethyl-barbituric acid) is a short-acting barbiturate exerting sedative-hypnotic properties. Cyclobarbital is metabolized to inactive ketocyclobarbital. The convention on psychotropic substances, which was signed in Vienna in 1971, today regulates cyclobarbital as a schedule III barbiturate. Cyclobarbital is used in combination with diazepam tranquilizer (Reladorm).
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Hexapropymate, a hypnotic/sedative drug that was available without prescription in Belgium under the trade name Merinax for the treatment of insomnia. Poisoning with hexapropymate was a serious condition that required symptomatic treatment in the intensive care unit. As a result, the drug was substituted by newer agents with improved safety profiles.
Status:
Possibly Marketed Outside US
Source:
Heminevrin by Hoffman-La Roche
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Chlormethiazole has sedative, hypnotic, anticonvulsant and neuroprotective properties. This drug is approved in different counties under the different brand name (e.g., Heminevrin) and is used for the management of restlessness and agitation in the elderly, short-term treatment of severe insomnia in the elderly and treatment of alcohol withdrawal symptoms. Clomethiazole interacts with the picrotoxin/barbiturate site of the GABAA-receptor-chloride channel complex. Clomethiazole is pharmacologically distinct from both the benzodiazepines and the barbiturates. Given alone its effects on respiration are slight and the therapeutic index high.
structurally diverse
Status:
US Previously Marketed
Source:
Valerian U.S.P.
(1921)
Source URL:
First marketed in 1921
Source:
Valerian U.S.P.
Source URL:

Class:
STRUCTURALLY DIVERSE

Status:
First marketed in 1921
Source:
calcium pentobarbital
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Pentobarbital belongs to the class of a short-acting barbiturate is used as sedatives, hypnotics, for the short-term treatment of insomnia, since they appear to lose their effectiveness for sleep induction and sleep maintenance after 2 weeks; preanesthetics and anticonvulsant, in anesthetic doses, in the emergency control of certain acute convulsive episodes, e.g., those associated with status epilepticus, cholera, eclampsia, meningitis, tetanus, and toxic reactions to strychnine or local anesthetics. Pentobarbital binds at a distinct binding site associated with a Cl- ionopore at the GABAA receptor, increasing the duration of time for which the Cl- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged. All of these effects are associated with marked decreases in GABA-sensitive neuronal calcium conductance (gCa). The net result of barbiturate action is acute potentiation of inhibitory GABAergic tone. Barbiturates also act through potent (if less well characterized) and direct inhibition of excitatory AMPA-type glutamate receptors, resulting in a profound suppression of glutamatergic neurotransmission.
Status:
First marketed in 1921
Source:
Potassium Acetate U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Potassium is needed to maintain good health. When potassium level falls below 3.5 mmol/L, Hypokalemia is diagnosed. In case of extremely low level of potassium (lower than 2.5 mmol/L) the following symptoms are appeared: malaise and fatigue. This low level of potassium can lead to severe muscle weakness and paralysis; respiratory failure; intermittent muscle spasms. It is known, foods that are good sources of potassium and low in sodium may reduce the risk of high blood pressure and stroke. Potassium supplementation is also recommended as an adjuvant antihypertensive agent for patients with essential hypertension.