Hypnotic, or soporific drugs, commonly known as sleeping pills, are a class of psychoactive drugs whose primary function is to induce sleep and to treat insomnia (sleeplessness).
Glutethimide is a hypnotic sedative that was introduced by Ciba in 1954 as a safe alternative to barbiturates to treat insomnia. Before long, however, it had become clear that glutethimide was just as likely to cause addiction and caused similar withdrawal symptoms. Doriden was the brand-name version. Current production levels in the United States point to its use only in small-scale research. Manufacturing of the drug was discontinued in the US in 1993 and discontinued in several eastern European countries in 2006.
Flurazepam is a drug which is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, hypnotic, sedative and skeletal muscle relaxant properties. It produces a metabolite with a long half-life, which may stay in the bloodstream for days. Flurazepam was patented in 1968 and came into medical use the same year. Flurazepam, developed by Roche Pharmaceuticals was one of the first benzo hypnotics to be marketed.
Butabarbital is a prescription barbiturate sleep aid and anxiety medication. Butabarbital has a particularly fast onset of effects and short duration of action compared to other barbiturates, which makes it useful for certain applications such as treating severe insomnia, relieving general anxiety and relieving anxiety before surgical procedures; however it is also relatively dangerous particularly when combined with alcohol, and so is now rarely used, although it is still prescribed in some Eastern European and South American countries. Its intermediate duration of action gives butabarbital an abuse potential slightly lower than secobarbital. Butabarbital can be hydrolyzed to Valnoctamide.
Clomethiazole is a sedative and hypnotic originally developed by Hoffmann-La Roche in the 1930s. The drug is used in treating and preventing symptoms of acute alcohol withdrawal.
Phenprobamate is a centrally acting skeletal muscle relaxant, with additional sedative and anticonvulsant effects. Overdose is similar to barbiturates. Its mechanism of action is probably similar to meprobamate. Phenprobamate has been used in humans as an anxiolytic, and is still sometimes used in general anesthesia and for treating muscle cramps and spasticity. Phenprobamate is still used in some European countries, but it has generally been replaced by newer drugs. Phenprobamate is metabolized by oxidative degradation of the carbamate group and ortho-hydroxylation of the benzene ring, and is eliminated in urine by the kidneys.
Methyprylon(Noludar) was a sedative of the piperidinedione derivative family developed by Hoffmann-La Roche. This medicine was used for treating insomnia, but is now rarely used as it has been replaced by newer drugs with fewer side effects, such as benzodiazepines. Methyprylon was withdrawn from the US market in June 1975 and the Canadian market in September 1990. Some other trade names are Noctan and Dimerin.
Aprobarbital, sold as Oramon, Somnifaine, and Allonal, is a barbiturate derivative invented in the 1920s by Ernst Preiswerk. It has sedative, hypnotic and anticonvulsant properties, and was used primarily for the treatment of insomnia. Aprobarbital was never as widely used as more common barbiturate derivatives such as phenobarbital and is now rarely prescribed as it has been replaced by newer drugs with a better safety margin.
Alphenal, also known as 5-allyl-5-phenylbarbituric acid, is a barbiturate derivative developed in the 1920s. It has primarily anticonvulsant properties, and was used occasionally for the treatment of epilepsy or convulsions, although not as commonly as better known barbiturates such as phenobarbital.
Butallylonal is a barbiturate derivative invented in the 1920s. It has sedative properties, and was used primarily as an anaesthetic in veterinary medicine. Butallylonal is considered similar in effects to pentobarbital but is longer in action, being considered an intermediate-acting barbiturate rather than short-acting.
Cyclopentobarbital sodium is a barbiturate derivative invented in the 1940s. It has sedative and anticonvulsant properties, and was used primarily as an anaesthetic in veterinary medicine. Cyclopal is considered similar in effects to phenobarbital but lasts almost three times as long, and is considered a long-acting barbiturate with a fairly slow onset of action.
Rolicyclidine (PCPy) is a dissociative anesthetic drug with hallucinogenic and sedative effects. It is similar in effects to phencyclidine but is slightly less potent and has less stimulant effects instead producing a sedative effect described as being somewhat similar to a barbiturate, but with additional PCP-like dissociative, anaesthetic and hallucinogenic effects. Due to its similarity in effects to PCP, PCPy was placed into the Schedule I list of illegal drugs in the 1970s, although it has never been widely abused and is now little known.
Narcobarbital (Pronarcon) is a barbiturate derivative developed in 1932 by Carl Heinrich Friedrich Boedecker and Heinrich Gruber Schoneberg, assignors to the firm J. D. Riedel-E. de Haën AG, Berlin, Germany. Later, in 1937, may, was patented in United States. It is an N-methylated derivative of propallylonal and has similar sedative effects. It is still used in veterinary medicine for inducing surgical anaesthesia.
Mebutamate is an anxiolytic and sedative drug with antihypertensive effects of the carbamate class. It has effects comparable to those of barbiturates such as secobarbital, but is only around 1/3 the potency of secobarbital as a sedative. Side effects include dizziness and headaches.
Pyrithyldione 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%.
Meclonazepam was discovered by a team at Hoffmann-La Roche in the 1970s and is a drug which is a benzodiazepine derivative similar in structure to clonazepam. It has sedative and anxiolytic actions like those of other benzodiazepines, and also has anti-parasitic effects against the parasitic worm Schistosoma mansoni.
Enallylpropymal (Narconumal) is a barbiturate derivative developed by Hoffman la Roche in the 1930s. It has sedative and hypnotic effects and is considered to have a moderate abuse potential.
A barbiturate is a drug that acts as a central nervous system depressant. Barbiturates are effective as anxiolytics, hypnotics, and anticonvulsants, but have physical and psychological addiction potential as well as overdose potential among other possible adverse effects. They have largely been replaced by benzodiazepines and nonbenzodiazepines ("Z-drugs") in routine medical practice, particularly in the treatment of anxiety and insomnia, due to the significantly lower risk of addiction and overdose and the lack of an antidote for barbiturate overdose. Despite this, barbiturates are still in use for various purposes: in general anesthesia, epilepsy, treatment of acute migraines or cluster headaches, acute tension headaches, euthanasia, capital punishment, and assisted suicide.
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.
Ro09-9212 is a thienodiazepine derivative with sedative and anxiolytic effects, which has been sold as a designer drug.
