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Category

Hypnotics

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bentazepam
Bentazepam (also known as Thiadipone, Tiadipona) is a thienodiazepine which is a benzodiazepine analog.
daridorexant
niaprazine
Niaprazine (INN; brand name Nopron) is a sedative-hypnotic drug of the phenylpiperazine group. It has been used in the treatment of sleep disturbances since the early 1970s in several European countries including France, Italy, and Luxembourg. It is commonly used with children and adolescents on account of its favorable safety and tolerability profile and lack of abuse potential.
deschloroetizolam
Deschloroetizolam (also known as Etizolam-2) is a thienotriazolodiazepine that is the dechlorinated analog of the closely related etizolam. The compound has been sold as a designer drug.
doxefazepam
Doxefazepam (marketed under brand name Doxans) is a benzodiazepine medication. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. It is used therapeutically as a hypnotic. According to Babbini and colleagues in 1975, this derivative of flurazepam was between 2 and 4 times more potent than the latter while at the same time being half as toxic in laboratory animals.
embutramide
Embutramide (INN, USAN, BAN; brand name Embutane) is a potent sedative drug that is structurally related to GHB. It was developed by Hoechst A.G. in 1958 and was investigated as a general anesthetic agent, but was found to have a very narrow therapeutic window, with a 50 mg/kg dose producing effective sedation and a 75 mg/kg dose being fatal. Along with strong sedative effects, embutramide also produces respiratory depression and ventricular arrhythmia. Because of these properties, it was never adopted for medical use as an anesthetic as it was considered too dangerous for this purpo
ethallobarbital
Ethallobarbital (brand names Dormin, Dumex, Dormitiv, Dorval), also known as ethallymal and 5-allyl-5-ethylbarbituric acid, is an allyl-substituted barbiturate described as a sedative/hypnotic. It was first synthesized in 1927.
apronal
Apronal (brand name Sedormid), or apronalide, also known as allylisopropylacetylurea or allylisopropylacetylcarbamide, is a hypnotic/sedative drug of the ureide (acylurea) group synthesized in 1926 by Hoffmann-La Roche. Though it is not a barbiturate, apronal is similar in structure to the barbiturates (being an open-chain carbamide instead of having a heterocyclic ring). In accordance, it is similar in action to the barbiturates, although considerably milder in comparison (formerly used as a daytime sedative at doses of 1 to 2 grams every 3 to 4 hours). Upon the finding that it caused patient
propylbarbital
Propylbarbital (Propal, Propanal, Proponal), also known as 5,5-dipropylbarbituric acid, is a barbiturate derivative used as a hypnotic drug.
propiomazine
Propiomazine, sold under the brand name Propavan among others, is an antihistamine which is used to treat insomnia and to produce sedation and relieve anxiety before or during surgery or other procedures and in combination with analgesics as well as during labor. Propiomazine is a phenothiazine, but is not used therapeutically as a neuroleptic because it does not block dopamine receptors well.
evoxine
Evoxine (haploperine) is a furoquinoline alkaloid with hypnotic and sedative effects. It is found naturally in a variety of Australian and African plants including Evodia xanthoxyloides and Teclea gerrardii.
alcohol
active ingredient in alcoholic beverages
crotarbital
Crotylbarbital (Mepertan, Kalipnon, Barotal), also known as crotarbital, is a barbiturate derivative developed by Eli Lilly in the 1930s. It has sedative and hypnotic effects, and was used for the treatment of insomnia until it was replaced by newer alternative drugs with fewer side effects and lower risk of overdose.
prothipendyl
Prothipendyl (brand names Dominal, Timovan, Tolnate), also known as azapromazine or phrenotropin, is an anxiolytic, antiemetic, and antihistamine of the azaphenothiazine group which is marketed in Europe and is used to treat anxiety and agitation in psychotic syndromes. It differs from promazine only by the replacement of one carbon atom with a nitrogen atom in the tricyclic ring system. Prothipendyl is said to not possess antipsychotic effects, and in accordance, appears to be a weaker dopamine receptor antagonist than other phenothiazines.
etodroxizine
Etodroxizine (INN; brand names Vesparax, Drimyl, Indunox, and Isonox) is a first-generation antihistamine of the diphenylmethylpiperazine group which is used as a sedative/hypnotic drug in Europe and South Africa.
3-hydroxyphenazepam
3-Hydroxyphenazepam is a benzodiazepine with hypnotic, sedative, anxiolytic, and anticonvulsant properties. It is an active metabolite of phenazepam, as well as the active metabolite of the benzodiazepine prodrug cinazepam. Relative to phenazepam, 3-hydroxyphenazepam has diminished myorelaxant properties, but is about equivalent in most other regards. Like other benzodiazepines, 3-hydroxyphenazepam behaves as a positive allosteric modulator of the benzodiazepine site of the GABAA receptor with an EC50 value of 10.3 nM. It has been sold as a designer drug.
tetrabarbital
Tetrabarbital (INN; Butysal, Butysedal, Tetramal) is a barbiturate derivative used as a hypnotic.
pyrithyldione
Pyrithyldione (Presidon, Persedon) is a psychoactive drug invented in 1949. An improved method of manufacture was patented by Roche in 1959. It was used as a hypnotic or sedative and presumed to be less toxic than barbiturates. Today, this substance is no longer used. Agranulocytosis was sometimes reported as adverse effect. Pyrithyldione is also a CYP2D6 inducer but is not as potent as glutethimide. In studies, it increased the O-demethylation of codeine by 20%.
cinazepam
Nalobrazepam (), also known as cinazepam or BD-798 and sold under the brand name Levana, is an atypical benzodiazepine derivative.
gaboxadol
Gaboxadol, also known as 4,5,6,7-tetrahydroisoxazolo(5,4-c)pyridin-3-ol (THIP) and by its former developmental code names Lu-2-030, MK-0928, and OV101, is a GABAA receptor agonist related to muscimol which was investigated for the treatment of insomnia and other conditions like Angelman syndrome but was never marketed. At lower doses, the drug has sedative and hypnotic effects, and at higher doses, it produces hallucinogenic effects. It is taken orally.
desmethyletizolam
Metizolam (also known as desmethyletizolam) is a thienotriazolodiazepine that is the demethylated analogue of the closely related etizolam.
sulfonethylmethane
Trional (Methylsulfonal) is a sedative-hypnotic and anesthetic drug with GABAergic actions. It has similar effects to sulfonal, except it is faster acting.
Fenadiazole
Fenadiazole (), also known as phénadiazole () and sold under the brand names Hypnazol, Eudormil, and Viodor, is a hypnotic and sedative medication which has been used to treat insomnia but is no longer marketed. It is described as a non-barbiturate hypnotic with marked or profound hypnotic and sedative properties in animals, variable hypnotic effects in humans (rapidly inducing sleep for 6 to 8hours), additional anticonvulsant, antithermal, and spasmolytic effects, and a generally well-tolerated profile in humans (at an average dosage of 200mg/day). The drug was synthesized, pharmacologically
acecarbromal
Acecarbromal (INN) (brand names Sedamyl, Abasin, Carbased, Paxarel, Sedacetyl, numerous others), also known as acetylcarbromal and acetyladalin, is a hypnotic and sedative drug of the ureide (acylurea) group discovered by Bayer in 1917 that was formerly marketed in the United States and Europe. It is also used in combination with extract of quebracho and vitamin E as a treatment for erectile dysfunction under the brand name Afrodor in Europe. Acecarbromal is structurally related to the barbiturates, which are basically cyclized ureas. Prolonged use is not recommended as it can cause bromine po
sulfonmethane
Sulfonmethane (sulfonomethane, sulfonal, acetone diethyl sulfone) is a chemical compound first synthesized by Eugen Baumann in 1888 and introduced as a hypnotic drug by Alfred Kast later on, but now superseded by newer and safer sedatives. Its appearance is either in colorless crystalline or powdered form. In United States, it is scheduled as a Schedule III drug in the Controlled Substances Act.
QH-II-66
QH-II-66 (QH-ii-066) is a sedative drug which is a benzodiazepine derivative. It produces some of the same effects as other benzodiazepines, but is much more selective than most other drugs of this class and so produces somewhat less sedation and ataxia than other related drugs such as diazepam and triazolam, although it still retains anticonvulsant effects.
acebrochol
Acebrochol (INN), also known as cholesteryl acetate dibromide or 5α,6β-dibromocholestan-3β-ol acetate, is a neuroactive steroid which was described as a sedative and hypnotic but was never marketed.
chlorhexadol
Chloralodol (Chlorhexadol) is a hypnotic/sedative. It is a Schedule III drug in the United States; however, it is not currently marketed in the US so it is no longer prescribed.
tetrahydrodeoxycorticosterone
Tetrahydrodeoxycorticosterone (abbreviated as THDOC; 3α,21-dihydroxy-5α-pregnan-20-one), also referred to as allotetrahydrocorticosterone, is an endogenous neurosteroid. It is synthesized from the adrenal hormone deoxycorticosterone by the action of two enzymes, 5α-reductase type I and 3α-hydroxysteroid dehydrogenase. THDOC is a potent positive allosteric modulator of the GABAA receptor, and has sedative, anxiolytic and anticonvulsant effects. Changes in the normal levels of this steroid particularly during pregnancy and menstruation may be involved in some types of epilepsy (catamenial epilep
3,4-dihydroxy-3-methyl-4-phenyl-1-butyne
Centalun was developed by Boehringer Ingelheim in 1962 and is a psycholeptic drug with hypnotic and sedative effects, via allosteric agonism of the GABAA receptor. It was previously used for sedation in medical procedures such as surgery, orthopedics and gynecology, although it is no longer in clinical use. Despite its history of clinical use, centalun was never incorporated into the CSA and therefore remains unregulated as a drug of abuse.
dichloralphenazone
Dichloralphenazone is a 1:2 mixture of antipyrine with chloral hydrate. In combination with paracetamol and isometheptene, it is the active ingredient of medications for migraine and tension headaches, including Epidrin and Midrin. Performance impairments are common with this drug and caution is advised, for example when driving motor vehicles. Additional uses of dichloralphenazone include sedation for the treatment of short-term insomnia, although there are probably better drug choices for the treatment of insomnia.
metomidate
Metomidate is a non-barbiturate imidazole that was discovered by Janssen Pharmaceutica in 1965 and under the names (Hypnodil, Nokemyl) is sold as a sedative-hypnotic drug used in Europe to treat humans and for veterinary purposes.
anhalonidine
Anhalonidine, also known as '''N-desmethylpellotine', a naturally occurring tetrahydroisoquinoline alkaloid which can be isolated from certain members of the cactus family, such as Lophophora''. It is structurally related to mescaline. Anhalonidine produced no hallucinogenic effects in humans at doses of up to 250mg. However, it has been reported to have a calming or sedative effect instead, with about one-fourth the potency of pellotine and with marked sedation occurring at doses of 100 to 250mg. Anhalonidine has been found to act as a potent inverse agonist of the serotonin 5-HT7 receptor.
atagabalin
Atagabalin (, ; developmental code name PD-0200390) is a drug developed by Pfizer and related to gabapentin, which similarly binds to the α2δ calcium channels (1 and 2). It was under development as a treatment for insomnia, but was discontinued following unsatisfactory trial results. The drug reached phase 2 clinical trials for this indication prior to the discontinuation of its development.
(RS)-4-hydroxyvaleric acid
group of enantiomers
ORG 20599
ORG-20599 is a synthetic neuroactive steroid, with sedative effects resulting from its action as a GABAA receptor positive allosteric modulator and, at higher concentrations, agonist. It was developed for use as an anaesthetic agent but was never marketed for this purpose, although it is still used in scientific research.
alpha-methylhistamine
α-Methylhistamine is a synthetic derivative and a selective histamine H3 receptor agonist. It decreases blood pressure and heart rate in guinea pigs. The drug also has sedative and hypnotic effects in animals.
tetronal
Tetronal is a sedative-hypnotic and anesthetic drug with GABAergic actions. It is not as effective as trional.
Eplivanserin
Eplivanserin, also known by its former developmental code names SR-46349 and SR-46615 and by its former tentative brand names Ciltyri and Sliwens, is a serotonin 5-HT2A receptor antagonist which was under development by Sanofi Aventis for the treatment of a variety of medical conditions but was never marketed. It is taken orally.
Long-term impact of alcohol on the brain
effect of alcohol consumption
Narcosynthesis
Narcosynthesis is a technique of treating post-traumatic stress disorder popularized by psychiatrists in the post-World War II era. Also called sodium amytal interview, amobarbital interview, or amytal interview, it uses free association as well as dream and during the session as a basis for uncovering relevant topics for later therapeutic discussion.
Org 21465
ORG-21465 is a synthetic neuroactive steroid, with sedative effects resulting from its action as a GABAA receptor positive allosteric modulator. It is similar to related drugs such as ORG-20599, and was similarly developed as an improved alternative to other sedative steroids such as althesin and allopregnanolone, which despite its superior properties in some respects has not proved to offer enough advantages to be accepted into clinical use.
clocental
Clocental (dolcental) is a carbamate-derived sedative hypnotic.
dimdazenil
Dimdazenil, sold under the brand name Junoenil, is a medication used in the treatment of insomnia in China. It is a benzodiazepine derivative and a partial positive allosteric modulator of the GABAA receptor with two- to four-fold higher functional affinity for the α1 subunit relative to the α2, α3, and α5 subunits.