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Asimadoline
Asimadoline (EMD-61753) is an experimental drug which acts as a peripherally selective κ-opioid receptor (KOR) agonist. Because of its low penetration across the blood–brain barrier, asimadoline lacks the psychotomimetic effects of centrally acting KOR agonists, and consequently was thought to have potential for medical use. It has been studied as a possible treatment for irritable bowel syndrome, with reasonable efficacy seen in clinical trials, but it has never been approved or marketed. See also * Eluxadoline * Fedotozine * Nalfurafine Nalfurafine (International Nonproprietary Name, INN, United States Adopted Name, USAN) (brand name Remitch; former developmental code names TRK-820, AC-820, MT-9938) is an antipruritic (anti-itch drug) that is marketed in Japan for the treatment ... * Trimebutine References {{Opioidergics Synthetic opioids Kappa-opioid receptor agonists Pyrrolidines Acetamides Peripherally selective drugs Abandoned drugs ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Eluxadoline
Eluxadoline, sold under the brand names Viberzi and Truberzi, is a medication taken by mouth for the treatment of diarrhea and abdominal pain in individuals with diarrhea-predominant irritable bowel syndrome (IBS-D). It was approved for use in the United States in 2015. The drug originated from Janssen Pharmaceutica and was developed by Actavis. Contraindications This drug is contraindicated in case of having: * Blockage of the gallbladder or a sphincter of Oddi problem * Problems with excessive alcohol use * Pancreatitis * Liver problems * Chronic or severe constipation Adverse effects Common adverse effects are constipation and nausea, but rates of discontinuation due to constipation were low for both eluxadoline and placebo. Rare adverse effects: fatigue, bronchitis, viral gastroenteritis. Rare serious adverse effects include pancreatitis with a general incidence of 0.3% - higher incidence with 100 mg dose (0.3%) than with 75 mg dose (0.2%). The risk is even greater ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Fedotozine
Fedotozine (INN; JO 1196 for the (-) tartrate salt) is an opioid drug of the arylacetamide series which acts as a peripherally specific selective κ1-opioid receptor agonist with preference for the κ1A subtype. It was under investigation for the treatment of gastrointestinal conditions like irritable bowel syndrome and functional dyspepsia and made it to phase III clinical trial Clinical trials are prospective biomedical or behavioral research studies on human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, drugs, diet ...s, but ultimately development was discontinued and it was never marketed. See also * Asimadoline * Trimebutine References {{Opioidergics Acetamides Analgesics Kappa-opioid receptor agonists Opioids Peripherally selective drugs Abandoned drugs ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nalfurafine
Nalfurafine (INN, USAN) (brand name Remitch; former developmental code names TRK-820, AC-820, MT-9938) is an antipruritic (anti-itch drug) that is marketed in Japan for the treatment of uremic pruritus in individuals with chronic kidney disease undergoing hemodialysis. It acts as a potent, selective, centrally-penetrant κ-opioid receptor (KOR) agonist, and is the first and currently the only selective KOR agonist to have been approved for clinical use. It has also been dubiously referred to as the "first non-narcotic opioid drug" in history. History Nalfurafine was derived from structural modification of the opioid antagonist naltrexone. It was first synthesized and characterized in 1998, and was approved for clinical use in Japan as an intravenous drug under the brand name Remitch in 2009. The developer of nalfurafine also sought approval in Europe under the brand name Winfuran, but the Marketing Authorization Application was declined by the European Medicines Agency. The drug w ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Trimebutine
Trimebutine is a drug with antimuscarinic and weak mu opioid agonist effects. It is used for the treatment of irritable bowel syndrome and other gastrointestinal disorders. The major product from drug metabolism of trimebutine in human beings is nortrimebutine, which comes from removal of one of the methyl groups attached to the nitrogen atom. Trimebutine exerts its effects in part due to causing a premature activation of phase III of the migrating motor complex in the digestive tract. Both trimebutine and its metabolite are commercially available. Brand names The maleic acid salt of trimebutine is marketed under the trademark A trademark (also written trade mark or trade-mark) is a type of intellectual property consisting of a recognizable sign, design, or expression that identifies products or services from a particular source and distinguishes them from othe ...s of Antinime, Cineprac, Colospasmyl, Colypan, Crolipsa, Debricol, Debridat, Digedrat, Espabion, Gast ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Kappa Opioid Receptor
Kappa (uppercase Κ, lowercase κ or cursive ; el, κάππα, ''káppa'') is the 10th letter of the Greek alphabet, representing the voiceless velar plosive sound in Ancient and Modern Greek. In the system of Greek numerals, has a value of 20. It was derived from the Phoenician letter kaph . Letters that arose from kappa include the Roman K and Cyrillic К. The uppercase form is identical to the Latin K. Greek proper names and placenames containing kappa are often written in English with "c" due to the Romans' transliterations into the Latin alphabet: Constantinople, Corinth, Crete. All formal modern romanizations of Greek now use the letter "k", however. The cursive form is generally a simple font variant of lower-case kappa, but it is encoded separately in Unicode for occasions where it is used as a separate symbol in math and science. In mathematics, the kappa curve is named after this letter; the tangents of this curve were first calculated by Isaac Barrow in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Agonist
An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the agonist, while an inverse agonist causes an action opposite to that of the agonist. Etymology From the Greek αγωνιστής (agōnistēs), contestant; champion; rival < αγων (agōn), contest, combat; exertion, struggle < αγω (agō), I lead, lead towards, conduct; drive Types of agonists can be activated by either endogenous agonists (such as |
Blood–brain Barrier
The blood–brain barrier (BBB) is a highly selective semipermeable membrane, semipermeable border of endothelium, endothelial cells that prevents solutes in the circulating blood from ''non-selectively'' crossing into the extracellular fluid of the central nervous system where neurons reside. The blood–brain barrier is formed by endothelial cells of the Capillary, capillary wall, astrocyte end-feet ensheathing the capillary, and pericytes embedded in the capillary basement membrane. This system allows the passage of some small molecules by passive transport, passive diffusion, as well as the selective and active transport of various nutrients, ions, organic anions, and macromolecules such as glucose and amino acids that are crucial to neural function. The blood–brain barrier restricts the passage of pathogens, the diffusion of solutes in the blood, and Molecular mass, large or Hydrophile, hydrophilic molecules into the cerebrospinal fluid, while allowing the diffusion of Hydr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Psychotomimetic
A drug with psychotomimetic (also known as psychotogenic) actions mimics the symptoms of psychosis, including delusions and/or delirium, as opposed to only hallucinations. Psychotomimesis is the onset of psychotic symptoms following the administration of such a drug. Some rarely used drugs of the opioid class have psychotomimetic effects. Particularly, mixed kappa receptor agonist mu receptor antagonist opioid analgesics can cause dose-related psychotomimesis. This adverse effect, incidence 1–2%, limits their use. Pentazocine and butorphanol fall under this opioid class. There is evidence that cannabinoids are psychotomimetic, especially delta-9-tetrahydrocannabinol (Δ9-THC). D'Souza et al. (2004) found that intravenous THC produced effects that resemble schizophrenia in both the positive symptoms (hallucinations, delusions, paranoia, and disorganized thinking) and negative symptoms (avolition, asociality, apathy, alogia, and anhedonia). Certain strains of cannabis may be mor ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Irritable Bowel Syndrome
Irritable bowel syndrome (IBS) is a "disorder of gut-brain interaction" characterized by a group of symptoms that commonly include abdominal pain and or abdominal bloating and changes in the consistency of bowel movements. These symptoms may occur over a long time, sometimes for years. IBS can negatively affect quality of life and may result in missed school or work (absenteeism) or reduced productivity at work (presenteeism). Disorders such as anxiety, major depression, and chronic fatigue syndrome are common among people with IBS.The cited review is based on sources ranging from 1988 to 2001 and is probably biased relative to a more recent research. The causes of IBS may well be multi-factorial. Theories include combinations of "gut–brain axis" problems, alterations in gut motility, visceral hypersensitivity, infections including small intestinal bacterial overgrowth, neurotransmitters, genetic factors, and food sensitivity. Onset may be triggered by an intestinal infec ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Clinical Trial
Clinical trials are prospective biomedical or behavioral research studies on human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, drugs, dietary choices, dietary supplements, and medical devices) and known interventions that warrant further study and comparison. Clinical trials generate data on dosage, safety and efficacy. They are conducted only after they have received health authority/ethics committee approval in the country where approval of the therapy is sought. These authorities are responsible for vetting the risk/benefit ratio of the trial—their approval does not mean the therapy is 'safe' or effective, only that the trial may be conducted. Depending on product type and development stage, investigators initially enroll volunteers or patients into small pilot studies, and subsequently conduct progressively larger scale comparative studies. Clinical trials can vary i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Synthetic Opioids
Opioids are substances that act on opioid receptors to produce morphine-like effects. Medically they are primarily used for pain relief, including anesthesia. Other medical uses include suppression of diarrhea, replacement therapy for opioid use disorder, reversing opioid overdose, and suppressing cough. Extremely potent opioids such as carfentanil are approved only for veterinary use. Opioids are also frequently used non-medically for their euphoric effects or to prevent withdrawal. Opioids can cause death and have been used for executions in the United States. Side effects of opioids may include itchiness, sedation, nausea, respiratory depression, constipation, and euphoria. Long-term use can cause tolerance, meaning that increased doses are required to achieve the same effect, and physical dependence, meaning that abruptly discontinuing the drug leads to unpleasant withdrawal symptoms. The euphoria attracts recreational use, and frequent, escalating recreational use of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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