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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
Source:
Hydrated Chloral U.S.P.
(1921)
Source URL:
First marketed in 1921
Source:
Hydrated Chloral U.S.P.
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
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
First marketed in 1921
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Sucrose is a disaccharide composed of glucose and fructose, and found in many plants and plant parts. Sucrose is often extracted and refined from either sugarcane or beet sugar for human consumption. Upon ingestion, sucrose is hydrolyzed in the small intestine by by sucrase to glucose and fructose. Sucrose is used as inactive ingredients in numerous drugs. In medicine, sucrose is used for pain relief in infants.
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.
Status:
US Previously Marketed
First marketed in 1907
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Tricaine (MS-222, Tricaine-S), a water-soluble local anesthetic, is used commonly for sedation, immobilization, and anesthesia of poikilothermic animals and has been accepted as a common anesthetic for use in the cold-blooded animals. It has long been recognized as a valuable tool for the proper handling of these animals during manual spawning (fish stripping), weighing, measuring, marking, surgical operations, transport, photography, and research. Tricaine was developed by Merck as a sulfonated analog of benzocaine with high solubility in water. The main advantage of Tricaine is the short duration of action and rapid metabolism. There are many reports describing the use of Tricaine for anesthetizing poikilothermic animals because it is a safe agent for immersion anesthesia even though the other anesthetics such as ether, ethanol, thiopental, halothane, isoflurane, barbiturates also could be used. Amphibians could be anesthetized easily by immersion methods with Tricaine because the amphibian skin is extremely permeable and water is absorbed through the skin rather than ingested. Tricaine has been administered as an injectable agent also.
Status:
US Previously Marketed
First marketed in 1907
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Amylocaine (trade name Stovaine) is a local anesthetic, that was widely used for spinal anesthesia in Caesarean section. The dose used would produce anesthesia for up to 1 h. Reports of the use of spinal analgesia for abdominal and perineal surgery in infants are found from several centers during the first half of the twentieth century. However, this agent often fails to provide good maternal sensory block and currently, Amylocaine has been replaced with new anesthetics.
Status:
US Previously Marketed
Source:
PROCAINE HYDROCHLORIDE by GD SEARLE LLC
(1982)
Source URL:
First marketed in 1905
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Procaine is an anesthetic agent indicated for production of local or regional anesthesia, particularly for oral surgery. Procaine (like cocaine) has the advantage of constricting blood vessels which reduces bleeding, unlike other local anesthetics like lidocaine. Procaine is an ester anesthetic. It is metabolized in the plasma by the enzyme pseudocholinesterase through hydrolysis into para-aminobenzoic acid (PABA), which is then excreted by the kidneys into the urine. Procaine acts mainly by inhibiting sodium influx through voltage gated sodium channels in the neuronal cell membrane of peripheral nerves. When the influx of sodium is interrupted, an action potential cannot arise and signal conduction is thus inhibited. The receptor site is thought to be located at the cytoplasmic (inner) portion of the sodium channel. Procaine has also been shown to bind or antagonize the function of N-methyl-D-aspartate (NMDA) receptors as well as nicotinic acetylcholine receptors and the serotonin receptor-ion channel complex.
Status:
US Previously Marketed
Source:
Acetphenetidin U.S.P.
(1921)
Source URL:
First marketed in 1887
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Phenacetin was used as an analgesic and fever-reducing drug in both human and veterinary medicine for many years. Since a major portion of a dose of phenacetin is rapidly metabolised to paracetamol, it seems possible that phenacetin owes some of its therapeutic activity to its main metabolite, paracetamol, whereas its most troublesome side effect (methaemoglobinaemia) is due to another metabolite, p-phenetidine.
Phenacetin was shown to inhibit cyclooxygenase (COX)-3, a cyclooxygenase-1 variant while p-phenetidine potently inhibits both COX-1 and COX-2. There is sufficient evidence in humans for the carcinogenicity of analgesic mixtures containing phenacetin. Analgesic mixtures containing phenacetin cause cancer of the renal pelvis, and of the ureter. Phenacetin was withdrawn from many analgesic mixtures long before the legal ban in several countries.
Status:
US Previously Marketed
First marketed in 1885
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Antipyrine is an analgesic and antipyretic that has been given by mouth and as ear drops. It is often used in testing the effects of other drugs or diseases on drug-metabolizing enzymes in the liver. It inhibits cyclooxygenases and shows little anti-inflammatory activity. Like many old and approved substances after almost 100 years of use, antipyrine has been associated with some serious side effects, namely agranulocytosis and shock reactions.