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Status:
US Previously Marketed
First approved in 1952
Source:
CYCLAINE by MERCK
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Hexylcaine hydrochloride, a benzoic acid ester, is a local anaesthetic that has been used for surface anaesthesia of mucous membranes. Local anesthetics produce a transient block of nerve conduction by interfering with sodium channels. This effect of the anesthetic interferes with the development of an action potential across the nerve.
Status:
US Previously Marketed
First approved in 1949
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
ALPHAPRODINE is an opioid analgesic. It was used in obstetrics, as pre-operative medication, and for minor surgical procedures. In addition, this drug was used in the dentistry setting to help effectively manage pain associated with dental procedures.
Status:
US Previously Marketed
Source:
Transentine by Ciba
(1937)
Source URL:
First marketed in 1937
Source:
Transentine by Ciba
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Adiphenine is a ternary amino ligand. It is used as a local anesthetic that reduces the frequency of acetylcholine-induced single-channel currents. It was originally introduced as a spasmolytic agent. Adiphenine reduced the muscle tone of the gastrointestinal tract, bile duct and gallbladder, bronchi, bladder. It affects the tone of the muscles of the eye, causing the pupil dilated (mydriasis), increased intraocular pressure, and paralysis of accommodation. Influences on the cardiovascular system, causing tachycardia and improving AV-conduction. Adiphenine side effects are: nausea, vomiting, heartburn, dizziness, headache. Adiphenine has not been widely used clinically.
Status:
US Previously Marketed
Source:
PENTOTHAL by ABBOTT
(1959)
Source URL:
First marketed in 1934
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Sodium thiopental (also known as Sodium Pentothal, thiopental) was discovered in 1930s by investigators working for Abbott Laboratories. Thiopental sodium was used for the induction of general anesthesia and is used as an adjunct to provide hypnosis during balanced anesthesia with other anesthetic agents, including analgesics and muscle relaxants. Thiopental sodium was also used as an adjunct for control of convulsive disorders of various etiology, including those caused by local anesthetics. Finally, thiopental sodium had been used to reduce the intracranial pressure in patients with increased intracranial pressure, if controlled ventilation is provided. Nevertheless, these prescriptions of drug were discontinued. In addition, this drug was banned for use in US executions. Thiopental sodium acts through the CNS with particular activity in the mesencephalic reticular activating system. It was shown, that mechanism of action of sodium thiopental via GABAA receptor. Thiopental 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.
Status:
US Previously Marketed
First marketed in 1933
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Hexobarbital or hexobarbitone, (sold both in acid and sodium salt, brand name Evipan, and Tobinal), is a barbiturate derivative having hypnotic and sedative effects. It was used in the 1940s and 1950s as an agent for inducing anesthesia for surgery, as well as a rapid-acting, short-lasting hypnotic for general use, and has a relatively fast onset of effects and short duration of action. It was also used to murder women prisoners at Ravensbruck Concentration Camp. Modern barbiturates (such as Thiopental) has largely supplanted the use of hexobarbital as an anesthetic, as they allow for better control of the depth of anesthesia. Hexobarbital is still used in some scientific research. Hexobarbital binds at a distinct binding site associated with a Cl- ionophore at the GABA-A receptor, increasing the duration of time for which the Cl- ionophore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged.
Status:
US Previously Marketed
First marketed in 1921
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Fructose, or fruit sugar, is a simple ketonic monosaccharide found in many plants, where it is often bonded to glucose to form the disaccharide sucrose. At a commercial scale, fructose is often derived from sugar cane, sugar beets, and maize. Fructose is one of the three dietary monosaccharides, along with glucose and galactose, that are absorbed directly into the bloodstream. A growing body of research suggests that diet high in fructose may be contributing to incidences of obesity, insulin resistance, and diabetes.
Status:
US Previously Marketed
First marketed in 1921
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Fructose, or fruit sugar, is a simple ketonic monosaccharide found in many plants, where it is often bonded to glucose to form the disaccharide sucrose. At a commercial scale, fructose is often derived from sugar cane, sugar beets, and maize. Fructose is one of the three dietary monosaccharides, along with glucose and galactose, that are absorbed directly into the bloodstream. A growing body of research suggests that diet high in fructose may be contributing to incidences of obesity, insulin resistance, and diabetes.
Status:
US Previously Marketed
Source:
Hydrated Chloral U.S.P.
(1921)
Source URL:
First marketed in 1921
Source:
Hydrated Chloral U.S.P.
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Chloral is a chlorinated aldehyde that found extensive use, beginning in the 1940s, as a precursor in the production of the insecticide DDT and, to a lesser extent, of other insecticides and pharmaceuticals. This use of chloral has declined steadily since the 1960s, especially in those countries where the use of DDT has been restricted. Chloral is readily converted to chloral hydrate in the presence of water. Chloral hydrate is used as a sedative before medical procedures and to reduce anxiety related to withdrawal from drugs. Wider exposure to chloral hydrate occurs at microgram-per-liter levels in drinking water and swimming pools as a result of chlorination. Chloral hydrate is a well-established aneuploidogenic agent that also has some mutagenic activity. In human cells in vitro, chloral hydrate induced aneuploidy, micronuclei and gene mutations. Chloral hydrate clearly induced micronuclei in Chinese hamster cells, whereas findings in mouse lymphoma cells were conflicting. Induction of somatic mutation (but not sex-linked mutation) by chloral hydrate was demonstrated in insects. Chloral hydrate is metabolized in vivo to trichloroethanol, which is responsible for its physiological and psychological effects. The metabolite of chloral hydrate exerts its pharmacological properties via enhancing the GABA receptor complex and therefore is similar in action to benzodiazepines, nonbenzodiazepines, and barbiturates. In clinical studies, oral chloral hydrate appears to have a lower sedation failure rate when compared with oral promethazine for children undergoing pediatric neurodiagnostic procedures. The sedation failure was similar for other comparisons such as oral dexmedetomidine, oral hydroxyzine hydrochloride, and oral midazolam. When compared with intravenous pentobarbital and music therapy, oral chloral hydrate had a higher sedation failure rate. Compared to dexmedetomidine, chloral hydrate was associated with a higher risk of nausea and vomiting.
Status:
US Previously Marketed
Source:
Hydrated Chloral U.S.P.
(1921)
Source URL:
First marketed in 1921
Source:
Hydrated Chloral U.S.P.
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Chloral is a chlorinated aldehyde that found extensive use, beginning in the 1940s, as a precursor in the production of the insecticide DDT and, to a lesser extent, of other insecticides and pharmaceuticals. This use of chloral has declined steadily since the 1960s, especially in those countries where the use of DDT has been restricted. Chloral is readily converted to chloral hydrate in the presence of water. Chloral hydrate is used as a sedative before medical procedures and to reduce anxiety related to withdrawal from drugs. Wider exposure to chloral hydrate occurs at microgram-per-liter levels in drinking water and swimming pools as a result of chlorination. Chloral hydrate is a well-established aneuploidogenic agent that also has some mutagenic activity. In human cells in vitro, chloral hydrate induced aneuploidy, micronuclei and gene mutations. Chloral hydrate clearly induced micronuclei in Chinese hamster cells, whereas findings in mouse lymphoma cells were conflicting. Induction of somatic mutation (but not sex-linked mutation) by chloral hydrate was demonstrated in insects. Chloral hydrate is metabolized in vivo to trichloroethanol, which is responsible for its physiological and psychological effects. The metabolite of chloral hydrate exerts its pharmacological properties via enhancing the GABA receptor complex and therefore is similar in action to benzodiazepines, nonbenzodiazepines, and barbiturates. In clinical studies, oral chloral hydrate appears to have a lower sedation failure rate when compared with oral promethazine for children undergoing pediatric neurodiagnostic procedures. The sedation failure was similar for other comparisons such as oral dexmedetomidine, oral hydroxyzine hydrochloride, and oral midazolam. When compared with intravenous pentobarbital and music therapy, oral chloral hydrate had a higher sedation failure rate. Compared to dexmedetomidine, chloral hydrate was associated with a higher risk of nausea and vomiting.
Status:
US Previously Marketed
Source:
Chloretone by Parke-Davis
(1911)
Source URL:
First marketed in 1911
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Chlorobutanol, or trichloro-2-methyl-2-propanol, is an analgesic and sedative hypnotic in man, and an experimental general anesthetic. It has antibacterial and antifungal properties. It is also used chemical preservative for parenteral drugs. It was found, that chlorobutanol inhibited mammalian Nav 1.2 channels at concentrations less than those used to preserve parenteral solutions. Its mechanism of inhibiting Na channels differs from that of local anesthetics in that it does not show use dependent or state dependent inhibition.