Sedatives

Vinylbital, also known as butylvinal, is a sedative hypnotic drug which is a barbiturate derivative. It was developed by Aktiebolaget Pharmacia in the 1950s.

Heptabarb (INN; Eudan, Medapan, Medomin, Noctyn), also known as heptabarbitone (BAN) or heptabarbital, is a sedative and hypnotic drug of the barbiturate family. It was used in Europe for the treatment of insomnia from the 1950s onwards, but has since been discontinued.

Oxomemazine is an antihistamine and anticholinergic of the phenothiazine chemical class for the treatment of cough.

Chloralose (also known as α-chloralose) is an avicide, and a rodenticide used to kill mice in temperatures below 15 °C. It is also widely used in neuroscience and veterinary medicine as an anesthetic and sedative. Either alone or in combination, such as with urethane, it is used for long-lasting, but light anesthesia. It has been used with oral administration to sedate wild Canada geese for translocation in Nevada.

Vinbarbital is a hypnotic drug which is a barbiturate derivative. It was developed by Sharp and Dohme in 1939.

chemical compound

Opipramol, sold under the brand name Insidon among others, is an anxiolytic and tricyclic antidepressant that is used throughout Europe. Despite chemically being a tricyclic dibenzazepine (iminostilbene) derivative similar to imipramine, opipramol is not a monoamine reuptake inhibitor like most other tricyclic antidepressants, and instead acts primarily as a sigma-1 receptor agonist. It was developed by Schindler and Blattner in 1961.

Barbexaclone (Maliasin) is a salt compound of phenobarbital and levopropylhexedrine. It was introduced in 1965. It has been reported to be as effective as phenobarbital but better tolerated; however, as of 2004, these "promising results" had not yet been confirmed nor denied in controlled trials.

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.

Ganaxolone, sold under the brand name Ztalmy, is a medication used to treat seizures in people with cyclin-dependent kinase-like 5 (CDKL5) deficiency disorder. Ganaxolone is a neuroactive steroid gamma-aminobutyric acid (GABA) A receptor positive modulator.

Kavain is the principal kavalactone found in the roots of the kava plant (Piper methysticum), where it contributes significantly to the plant's psychoactive and anxiolytic effects.

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 (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.

Triclofos (brand names Triclos, Pedicloryl) is a sedative drug used rarely for treating insomnia.

Lactucarium is the milky fluid secreted by several species of lettuce, especially Lactuca virosa, usually from the base of the stems. It is known as lettuce opium because of its sedative and analgesic properties. It has also been reported to promote a mild sensation of euphoria. Because it is a latex, lactucarium physically resembles opium, in that it is excreted as a white fluid and can be reduced to a thick smokable solid.

300px|thumb|right|The general structure of the kavalactones, without the R1-R2 -O-CH2-O- bridge and with all possible C=C double bonds shown. Kavalactones are a class of lactone compounds found in kava roots and Alpinia zerumbet (shell ginger) and in several Gymnopilus, Phellinus and Inonotus fungi. Some kavalactones are bioactive. They are responsible for the psychoactive, analgesic, euphoric and sedative effects of kava.

Fospropofol (INN), often used as the disodium salt (trade name Lusedra), is an intravenous sedative-hypnotic agent. It is currently approved for use in sedation of adult patients undergoing diagnostic or therapeutic procedures such as endoscopy.

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.

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

Isovaleramide is an organic compound with the formula (CH3)2CHCH2C(O)NH2. The amide derived from isovaleric acid, it is a colourless solid.

Detomidine is an imidazole derivative and α2-adrenergic receptor agonist, used as a large animal sedative, primarily used in horses. It is usually available as the salt detomidine hydrochloride. It is a prescription medication available to veterinarians sold under various trade names.

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.

Nitromethaqualone is an analogue of methaqualone that has similar sedative and hypnotic properties. It is significantly more potent (10×) compared to the parent compound; the typical dose is approximately 25 mg.

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.

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.

Mecloqualone (Nubarene, Casfen) is a quinazolinone-class GABAergic and is an analogue of methaqualone that was first made in 1960 and marketed mainly in France and some other European countries. It has sedative, hypnotic, and anxiolytic properties caused by its agonist activity at the β subtype of the GABAa receptor, and was used for the treatment of insomnia. Mecloqualone is faster-acting but shorter-lasting than methaqualone and so was used only as a sleeping pill, in contrast to methaqualone, which was used as a general-purpose anxiolytic as well. Mecloqualone was never as widely used as me

active ingredient in alcoholic beverages

Febarbamate (INN; Solium, Tymium), also known as phenobamate, is an anxiolytic and tranquilizer of the barbiturate and carbamate families which is used in Europe by itself and as part of a combination drug formulation called tetrabamate.

Cloroqualone is a quinazolinone-class GABAergic and is an analogue of methaqualone developed in the 1980s and marketed mainly in France and some other European countries. It has sedative and antitussive properties resulting from its agonist activity at the β subtype of the GABAa receptor and sigma-1 receptor, and was sold either alone or in combination with other ingredients as a cough medicine. Cloroqualone has weaker sedative properties than methaqualone and was sold for its useful cough-suppressing effects, but was withdrawn from the French market in 1994 because of concerns about its poten

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.

Captodiame (INN), also known as captodiamine, is an antihistamine sold under the trade names Covatine, Covatix, and Suvren which is used as a sedative and anxiolytic. The structure is related to diphenhydramine.

chemical compound

Methylmethaqualone (MMQ) is a quinazolinone and an analogue of methaqualone that has similar sedative and hypnotic properties to its parent compound (resulting from its agonist activity at the β subtype of the GABAA receptor) and is around 3 times as potent in animal models. Methylmethaqualone differs from methaqualone by 4-methylation on the phenyl ring. It was made illegal in Germany in 1999 and listed by the DEA as a "drug of forensic interest" at about the same time, but little other information is available. It would appear that this compound was sold on the black market in Germany as a d

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.

Alfaxalone, also known as alphaxalone or alphaxolone and sold under the brand name Alfaxan and Faxone, is a neuroactive steroid and general anesthetic which is used currently in veterinary practice as an induction agent for anesthesia and as an injectable anesthetic. The most common side effect seen in current veterinary practice is respiratory depression when Alfaxan is administered concurrently with other sedative and anesthetic drugs; when premedications are not given, veterinary patients also become agitated and hypersensitive when waking up.

Afloqualone (Arofuto) is a quinazolinone family GABAergic drug and is an analogue of methaqualone developed in the 1970s by a team at Tanabe Seiyaku. It has sedative and muscle-relaxant effects resulting from its agonist activity at the β subtype of the GABAa receptor and has had some clinical use, although it causes photosensitization as a side-effect that can cause skin problems such as dermatitis.

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

SL-164, also known as dicloqualone or DCQ, is an analogue of methaqualone developed in the late 1960s by a team at Sumitomo. SL-164 has similar sedative, hypnotic and properties to the parent compound, but was never marketed for clinical use, due to higher risk of convulsions. Like other 4-substituted analogues, such as methylmethaqualone, SL-164 may cause seizures.

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

Methapyrilene is an antihistamine and anticholinergic of the pyridine chemical class which was developed in the early 1950s. It was sold under the trade names Co-Pyronil and Histadyl EC in the UK. It has relatively strong sedative effects, to the extent that its primary use was as a medication for insomnia rather than for its antihistamine action. Together with scopolamine, it was the main ingredient in Sominex, Nytol, and Sleep-Eze. It also provided the sedative component of Excedrin PM. All of these products were reformulated in the late 1970s when methapyrilene was demonstrated to cause liv

Romifidine is a drug that is used in veterinary medicine as a sedative mainly in large animals such as horses, although it may be used in a wide variety of species. It is not used in humans, but is closely related in structure to the commonly used drug clonidine.

Benzoctamine is a drug that possesses sedative and anxiolytic properties. Marketed as Tacitin by Ciba-Geigy, it is different from most sedative drugs because in most clinical trials it does not produce respiratory depression, but actually stimulates the respiratory system. As a result, when compared to other sedative and anxiolytic drugs such as benzodiazepines like diazepam, it is a safer form of tranquilizing. However, when co-administered with other drugs that cause respiratory depression, like morphine, it can cause increased respiratory depression.

Tetrabarbital (INN; Butysal, Butysedal, Tetramal) is a barbiturate derivative used as a hypnotic.

chemical compound

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.

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.

Difebarbamate (INN) is a tranquilizer of the barbiturate and carbamate families which is used in Europe as a component of a combination drug formulation referred to as tetrabamate (Atrium, Sevrium).

Mebroqualone (MBQ) is a quinazolinone-class GABAergic and is an analogue of mecloqualone that has similar sedative and hypnotic properties to its parent compound, resulting from its agonist activity at the β subtype of the GABAa receptor. It was originally synthesized in the 1960s Mebroqualone differs from mecloqualone by having a bromine atom instead of a chlorine on the 3-phenyl ring. It was made illegal in Germany in 1998 but little other information is available. It would appear that this compound was sold on the black market in Germany as a designer drug analogue of mecloqualone.

Necopidem is a drug in the imidazopyridine family, which is related to the better known drugs zolpidem and alpidem. It is therefore considered a nonbenzodiazepine and as such may have sedative and anxiolytic effects, given its structural similarity to other nonbenzodiazepine hypnotics.

Sigmodal (Rectidon) is a barbiturate derivative. It has sedative, hypnotic and anticonvulsant properties, and was used in surgical anaesthesia in the 1950s, and frequently appeared in drug mixtures in the 60s.

Acaprazine (INN) is an anxiolytic and "adrenolytic" drug of the phenylpiperazine group that was never marketed.

Clorotepine (; brand names Clotepin, Clopiben), also known as octoclothepin or octoclothepine, is an antipsychotic of the tricyclic group which was derived from perathiepin in 1965 and marketed in the Czech Republic by Spofa in or around 1971 for the treatment of schizophrenic psychosis.

Etaqualone (Aolan, Athinazone, Ethinazone) is a quinazolinone-class GABAergic and is an analogue of methaqualone that was developed in the 1960s. It was primarily marketed in France and other European countries, as well as later in China, where it is still used clinically as of 2022. It has sedative, hypnotic, muscle relaxant and central nervous system depressant properties resulting from its agonist activity at the β-subtype of the GABAA receptor, and was used for the treatment of insomnia.

Piperidione (trade name Sedulon) is a sedative drug, structurally related to methyprylon and pyrithyldione. It used to be marketed by Roche as a cough medicine available in liquid form. In the US, it was approved by the FDA on grounds of safety alone in 1947. After Roche failed to submit evidence of efficacy to the Drug Efficacy Study Implementation program in 1972, it was withdrawn from the US market.

Almorexant (INN), also known by its development code ACT-078573, is an orexin antagonist, acting as a competitive antagonist of the OX1 and OX2 orexin receptors, which was being developed by the pharmaceutical companies Actelion and GSK for the treatment of insomnia. Development of the drug was abandoned in January 2011 due to concerns over the hepatic safety of almorexant after transient increases in liver enzymes were observed in trials.

Probarbital (trade names Ipral, Vasalgin) is a barbiturate derivative invented in the 1920s. It has sedative, hypnotic and anticonvulsant properties.

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.

U-89843A (PNU-89843) is a sedative drug which acts as an agonist at GABAA receptors, specifically acting as a positive allosteric modulator selective for the α1, α3 and α6 subtypes. It has sedative effects in animals but without causing ataxia, and also acts as an antioxidant and may have neuroprotective effects. It was developed by a team at Upjohn in the 1990s.

Valofane is a sedative drug structurally related to the barbiturates and similar drugs such as primidone. It is metabolized once inside the body to form the barbiturate proxibarbital (proxibarbal) and is thus a prodrug.

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.