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Spasmolytic A29
A29 is a spasmolytic drug. It not used by itself but is co-administered with ketobemidone in a formulation sold as Ketogan. It is an analog of both amitriptyline and diphenhydramine Diphenhydramine, sold under the brand name Benadryl among others, is an antihistamine and sedative. Although generally considered sedating, diphenhydramine can cause paradoxical central nervous system stimulation in some individuals, particula .... See also * BW247 * DPH-362 References {{Analgesic-stub NMDA receptor antagonists Pain Analgesics Antispasmodics ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antispasmodic
An antispasmodic (synonym: spasmolytic) is a pharmaceutical drug or other agent that suppresses muscle spasms. Smooth muscle spasm One type of antispasmodics is used for smooth muscle relaxation, especially in tubular organs of the gastrointestinal tract. The effect is to prevent spasms of the stomach, intestine or urinary bladder. Both dicyclomine and hyoscyamine are antispasmodic due to their anticholinergic action. Both of these drugs have side effects common to anticholinergics and can worsen gastroesophageal reflux disease (GERD). Papaverine is an opium alkaloid used to treat visceral spasms, particularly those of the intestines. Mebeverine is a papaverine analog and spasmolytic with a strong and selective action on the smooth muscles of the gastrointestinal tract, particularly of the colon. Despite being anticholinergic, it does not have the systemic anticholinergic side effects seen in other such drugs. Peppermint oil has been traditionally used as an antispasmodic, and a r ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ketobemidone
Ketobemidone, sold under the brand name Ketogan (a mixture of ketobemidone and Spasmolytic A29) among others, is a powerful synthetic opioid painkiller. Its effectiveness against pain is in the same range as morphine, and it also has some NMDA-antagonist properties imparted, in part, by its metabolite norketobemidone. This may make it useful for some types of pain that do not respond well to other opioids. It is marketed in Denmark, Iceland, Norway. Until 2024 it was available in, but is now withdrawn in Sweden. It is used for severe pain. History Ketobemidone was first synthesized in 1942 by Eisleb and colleagues, at the laboratory of I.G. Farbenindustrie at Hoechst during the Second World War. The first study of it in humans was published in 1946, and it was introduced in clinical medicine shortly after. It was not in clinical use in the United States when the Controlled Substances Act 1970 was promulgated and was assigned to Schedule I with an ACSCN of 9628. As of 2013, no ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ketogan
Ketobemidone, sold under the brand name Ketogan (a mixture of ketobemidone and Spasmolytic A29) among others, is a powerful synthetic opioid painkiller. Its effectiveness against pain is in the same range as morphine, and it also has some NMDA-antagonist properties imparted, in part, by its metabolite norketobemidone. This may make it useful for some types of pain that do not respond well to other opioids. It is marketed in Denmark, Iceland, Norway. Until 2024 it was available in, but is now withdrawn in Sweden. It is used for severe pain. History Ketobemidone was first synthesized in 1942 by Eisleb and colleagues, at the laboratory of I.G. Farbenindustrie at Hoechst during the Second World War. The first study of it in humans was published in 1946, and it was introduced in clinical medicine shortly after. It was not in clinical use in the United States when the Controlled Substances Act 1970 was promulgated and was assigned to Schedule I with an ACSCN of 9628. As of 2013, no a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Structural Analog
A structural analog, also known as a chemical analog or simply an analog, is a chemical compound, compound having a chemical structure, structure similar to that of another compound, but differing from it in respect to a certain component. It can differ in one or more atoms, functional groups, or substructures, which are replaced with other atoms, groups, or substructures. A structural analog can be imagined to be formed, at least theoretically, from the other compound. Structural analogs are often isoelectronicity, isoelectronic. Despite a high chemical similarity, structural analogs are not necessarily functional analog (chemistry), functional analogs and can have very different physical, chemical, biochemical, or pharmacological properties. In drug discovery, either a large series of structural analogs of an initial lead compound are created and tested as part of a structure–activity relationship study or a database is virtual screening, screened for structural analogs of a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Amitriptyline
Amitriptyline, sold under the brand name Elavil among others, is a tricyclic antidepressant primarily used to treat major depressive disorder, and a variety of pain syndromes such as neuropathic pain, fibromyalgia, migraine and tension headaches. Due to the frequency and prominence of side effects, amitriptyline is generally considered a second-line therapy for these indications. The most common side effects are dry mouth, drowsiness, dizziness, constipation, and weight gain. Glaucoma, liver toxicity and abnormal heart rhythms are rare but serious side effects. Blood levels of amitriptyline vary significantly from one person to another, and amitriptyline interacts with many other medications potentially aggravating its side effects. Amitriptyline was discovered in the late 1950s by scientists at Merck and approved by the US Food and Drug Administration (FDA) in 1961. It is on the World Health Organization's List of Essential Medicines. It is available as a generic medicati ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Diphenhydramine
Diphenhydramine, sold under the brand name Benadryl among others, is an antihistamine and sedative. Although generally considered sedating, diphenhydramine can cause paradoxical central nervous system stimulation in some individuals, particularly at higher doses. This may manifest as agitation, anxiety, or restlessness rather than sedation. It is a H1 antagonist#First-generation (non-selective, classical), first-generation H1-antihistamine and it works by blocking certain effects of histamine, which produces its antihistamine and sedative effects. Diphenhydramine is also a potent anticholinergic. It is mainly used to treat allergy, allergies, insomnia, and symptoms of the common cold. It is also less commonly used for tremors in parkinsonism, and nausea. It is taken oral administration, by mouth, injection into a vein, injected into a vein, injection into a muscle, injected into a muscle, or topical medication, applied to the skin. Maximal effect is typically around two hours af ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
BW247
BW-247 is an antidepressant. BW-247 is a secondary amine, closely related in structure to the tricyclic antidepressants, which inhibits NA uptake in aortic strips and rat cerebral cortex slices. Unlike the tricyclic antidepressants, it is reported not to possess anticholinergic activity. See also *Spasmolytic A29 A29 is a spasmolytic drug. It not used by itself but is co-administered with ketobemidone in a formulation sold as Ketogan. It is an analog of both amitriptyline and diphenhydramine Diphenhydramine, sold under the brand name Benadryl am ... * DPH-362 References Norepinephrine reuptake inhibitors {{Medicine-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
DPH-362
DPH-362 is a simplified amitriptyline analog created by omission of the two-carbon dibenzosuberane bridge (the seven membered ring). The resulting compound still had activity in a test to explore TCA sodium channel blockers with analgesic properties. It is based on previous structures such aSpasmolytic A29(one of the active ingredients in Ketogan) and SKF-89976A. See also *Amitriptyline *γ-Butyrolactone γ-Butyrolactone (GBL) or ''gamma''-butyrolactone is an organic compound with the formula . It is a hygroscopic, colorless, water-miscible liquid with a weak characteristic odor. It is the simplest Γ-lactone, 4-carbon lactone. It is mainly used ... References Sodium channel blockers Analgesics Dimethylamino compounds Drugs with unknown mechanisms of action {{Analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
NMDA Receptor Antagonists
NMDA receptor antagonists are a class of drugs that work to antagonize, or inhibit the action of, the ''N''-Methyl-D-aspartate receptor ( NMDAR). They are commonly used as anesthetics for humans and animals; the state of anesthesia they induce is referred to as dissociative anesthesia. Several synthetic opioids function additionally as NMDAR-antagonists, such as pethidine, levorphanol, methadone, dextropropoxyphene, tramadol, and ketobemidone. Some NMDA receptor antagonists, such as ketamine, dextromethorphan (DXM), phencyclidine (PCP), methoxetamine (MXE), and nitrous oxide (N2O), are sometimes used as recreational drugs, for their dissociative, hallucinogenic, and euphoriant properties. When used recreationally, they are classified as dissociative drugs. Uses and effects NMDA receptor antagonists induce a state called dissociative anesthesia, marked by catalepsy, amnesia, and analgesia. Ketamine is a favored anesthetic for emergency patients with unknown ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pain
Pain is a distressing feeling often caused by intense or damaging Stimulus (physiology), stimuli. The International Association for the Study of Pain defines pain as "an unpleasant sense, sensory and emotional experience associated with, or resembling that associated with, actual or potential tissue damage." Pain motivates organisms to withdraw from damaging situations, to protect a damaged body part while it heals, and to avoid similar experiences in the future. Congenital insensitivity to pain may result in reduced life expectancy. Most pain resolves once the noxious stimulus is removed and the body has healed, but it may persist despite removal of the stimulus and apparent healing of the body. Sometimes pain arises in the absence of any detectable stimulus, damage or disease. Pain is the most common reason for physician consultation in most developed countries. It is a major symptom in many medical conditions, and can interfere with a person's quality of life and general fun ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Analgesics
An analgesic drug, also called simply an analgesic, antalgic, pain reliever, or painkiller, is any member of the group of drugs used for pain management. Analgesics are conceptually distinct from anesthetics, which temporarily reduce, and in some instances eliminate, sensation, although analgesia and anesthesia are neurophysiologically overlapping and thus various drugs have both analgesic and anesthetic effects. Analgesic choice is also determined by the type of pain: For neuropathic pain, recent research has suggested that classes of drugs that are not normally considered analgesics, such as tricyclic antidepressants and anticonvulsants may be considered as an alternative. Various analgesics, such as many NSAIDs, are available over the counter in most countries, whereas various others are prescription drugs owing to the substantial risks and high chances of overdose, misuse, and addiction in the absence of medical supervision. Etymology The word ''analgesic'' derives ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
