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ATC Code A04
A04A Antiemetics and antinauseants A04AA Serotonin (5-HT3) antagonists :A04AA01 Ondansetron :A04AA02 Granisetron :A04AA03 Tropisetron :A04AA04 Dolasetron :A04AA05 Palonosetron :A04AA55 Palonosetron, combinations A04AD Other antiemetics :A04AD01 Scopolamine :A04AD02 Cerium oxalate :A04AD04 Chlorobutanol :A04AD05 Metopimazine :A04AD10 Dronabinol :A04AD11 Nabilone :A04AD12 Aprepitant :A04AD13 Casopitant :A04AD14 Rolapitant :A04AD51 Scopolamine, combinations :A04AD54 Chlorobutanol, combinations :QA04AD90 Maropitant Maropitant (INN; trade name: Cerenia ), used as maropitant citrate (USAN), is a neurokinin-1 (NK1) receptor antagonist developed by Zoetis specifically for the treatment of motion sickness and vomiting in dogs. It was approved by the FDA in 200 ... References {{Antiemetics and antinauseants A04 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antiemetic
An antiemetic is a drug that is effective against vomiting and nausea. Antiemetics are typically used to treat motion sickness and the side effects of opioid analgesics, general anaesthetics, and chemotherapy directed against cancer. They may be used for severe cases of gastroenteritis, especially if the patient is dehydrated. Some antiemetics previously thought to cause birth defects appear safe for use by pregnant women in the treatment of morning sickness and the more serious hyperemesis gravidarum. __TOC__ Types * 5-HT3 receptor antagonists block serotonin receptors in the central nervous system and gastrointestinal tract. As such, they can be used to treat post-operative and cytotoxic drug nausea & vomiting. However, they can also cause constipation or diarrhea, dry mouth, and fatigue. ** Dolasetron (Anzemet) can be administered in tablet form or in an injection. ** Granisetron (Kytril, Sancuso) can be administered in tablet (Kytril), oral solution (Kytril), inj ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chlorobutanol
Chlorobutanol (trichloro-2-methyl-2-propanol) is a preservative, sedative, hypnotic and weak local anesthetic similar in nature to chloral hydrate. It has antibacterial and antifungal properties. Chlorobutanol is typically used at a concentration of 0.5% where it lends long term stability to multi-ingredient formulations. However, it retains antimicrobial activity at 0.05% in water. Chlorobutanol has been used in anesthesia and euthanasia of invertebrates and fishes. It is a white, volatile solid with a camphor-like odor. Synthesis Chlorobutanol was first synthesized in 1881 by the German chemist Conrad Willgerodt (1841–1930). Chlorobutanol is formed by the reaction of chloroform and acetone in the presence of potassium or sodium hydroxide. It may be purified by sublimation or recrystallisation. Toxicity Chlorobutanol is highly toxic to the liver, is a skin irritant and a severe eye irritant. Parthenogenesis Chlorobutanol has proven effective at stimulating parthenoge ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Rolapitant
Rolapitant (INN, trade name Varubi in the US and Varuby in the European Union) is a drug originally developed by Schering-Plough and licensed for clinical development by Tesaro, which acts as a selective NK1 receptor antagonist (antagonist for the NK1 receptor). It has been approved as a medication for the treatment of chemotherapy-induced nausea and vomiting (CINV) after clinical trials showed it to have similar or improved efficacy and some improvement in safety over existing drugs for this application. Medical uses Rolapitant is used in combination with other antiemetic (anti-vomiting) agents in adults for the prevention of delayed nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy, including, but not limited to, highly emetogenic chemotherapy. The approved antiemetic combination consists of rolapitant plus dexamethasone and a 5-HT3 antagonist. Contraindications Under the US approval, rolapitant is contraindicated in combina ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Casopitant
Casopitant (), former tentative trade names Rezonic (U.S.) and Zunrisa (Europe), is an NK1 receptor antagonist which was undergoing research for the treatment of chemotherapy-induced nausea and vomiting. It was under development by GlaxoSmithKline. In July 2008, the company filed a marketing authorisation application with the European Medicines Agency. The application was withdrawn and development was discontinued in September 2009 because GlaxoSmithKline decided that further safety assessment was necessary. However, a 2022 review listed casopitant as under development as a potential novel antidepressant for the treatment of major depressive disorder, with a phase 2 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, dietar ... having been completed. References Abandoned ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Aprepitant
Aprepitant, sold under the brand name Emend among others, is a medication used to prevent chemotherapy-induced nausea and vomiting (CINV) and to prevent postoperative nausea and vomiting (PONV). It may be used together with ondansetron and dexamethasone. It is taken by mouth or administered by intravenous injection. Common side effects include tiredness, loss of appetite, diarrhea, abdominal pain, hiccups, itchiness, pneumonia, and blood pressure changes. Other severe side effects may include anaphylaxis. While use in pregnancy does not appear to be harmful, such use has not been well studied. Aprepitant belongs to the class of neurokinin-1 receptor antagonists medications. It works by blocking substance P from attaching to the NK1 receptors. Aprepitant was approved for medical use in the European Union and the United States in 2003. It is made by Merck & Co. It is on the World Health Organization's List of Essential Medicines. Medical uses Aprepitant is used to prevent ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nabilone
Nabilone, sold under the brand name Cesamet among others, is a synthetic cannabinoid with therapeutic use as an antiemetic and as an adjunct analgesic for neuropathic pain. It mimics tetrahydrocannabinol (THC), the primary psychoactive compound found naturally occurring in ''Cannabis''. The Food and Drug Administration in the United States has indicated nabilone for chemotherapy-induced nausea/vomiting. In other countries, such as Canada, it is widely used as an adjunct therapy for chronic pain management. Numerous trials and case studies have demonstrated modest effectiveness for relieving fibromyalgia and multiple sclerosis. Medical uses Nabilone is used to treat nausea and vomiting in people under chemotherapy. Nabilone has shown modest effectiveness in relieving fibromyalgia. A 2011 systematic review of cannabinoids for chronic pain determined there was evidence of safety and modest efficacy for some conditions. The main settings that have seen published clinical trials o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dronabinol
The International Nonproprietary Name Dronabinol, also known as delta-9-tetrahydrocannabinol, or under the trade names Marinol, Syndros, Reduvo and Adversa, is a generic name for the molecule of delta-9-tetrahydrocannabinol in the pharmaceutical context. It has indications as an appetite stimulant, antiemetic, and sleep apnea reliever and is approved by the FDA as safe and effective for HIV/AIDS-induced anorexia and chemotherapy-induced nausea and vomiting only. Dronabinol is the principal psychoactive constituent enantiomer form, (−)-''trans''-Δ9-tetrahydrocannabinol, found in cannabis. Dronabinol does not include any other tetrahydrocannabinol (THC) isomers or any cannabidiol. Medical uses Appetite stimulant and anti-emetic Dronabinol is used to stimulate appetite and therefore weight gain in patients with HIV/AIDS and cancer. It is also used to treat chemotherapy-induced nausea and vomiting. Analgesic Dronabinol demonstrated analgesic efficacy in a majority of studies ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Metopimazine
Metopimazine (, , ), sold under the brand names Nortrip, Vogalen, and Vogalene, is an antiemetic of the phenothiazine group which is used to treat nausea and vomiting. It is marketed in Europe, Canada, and South America. As of August 2020, metopimazine has been repurposed and is additionally under development for use in the United States for the treatment of gastroparesis. Metopimazine has antidopaminergic, antihistamine, and anticholinergic activity. However, it has also been described as a highly potent and selective dopamine D2 and D3 receptor antagonist. The D2 receptor antagonism of metopimazine is thought to underlie its antiemetic and gastroprokinetic effects. It is said to not readily cross the blood–brain barrier and hence to have peripheral selectivity, in contrast to metoclopramide but similarly to domperidone. Unlike domperidone however, metopimazine shows no hERG inhibition and hence is expected to have a more favorable cardiovascular profile. In contrast to m ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cerium Oxalate
Cerium(III) oxalate (cerous oxalate) is the inorganic cerium salt of oxalic acid. It is a white crystalline solid with the chemical formula of Ce2(C2O4)3. It could be obtained by the reaction of oxalic acid with cerium(III) chloride. Uses Cerium(III) oxalate is used as an antiemetic. It has been identified as part of the invisible ink that was used by Stasi operatives during the Cold War. Toxicity Cerium(III) oxalate irritates skin and mucous membranes, and is a strong irritant to eyes. If it gets into the eyes, there is a danger of severe eye injury. Cerium salts increase the blood coagulation rate, and exposure to cerium salts can cause sensitivity to heat. Oxalates are corrosive to tissue and are powerful irritants. They have a caustic effect on the linings of the digestive tracts and can cause kidney The kidneys are two reddish-brown bean-shaped organs found in vertebrates. They are located on the left and right in the retroperitoneal space, and in adult ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Serotonin
Serotonin () or 5-hydroxytryptamine (5-HT) is a monoamine neurotransmitter. Its biological function is complex and multifaceted, modulating mood, cognition, reward, learning, memory, and numerous physiological processes such as vomiting and vasoconstriction. Approximately 90% of the serotonin that the body produces is in the intestinal tract. Biochemically, the indoleamine molecule derives from the amino acid tryptophan, via the (rate-limiting) hydroxylation of the 5 position on the ring (forming the intermediate 5-hydroxytryptophan), and then decarboxylation to produce serotonin. Serotonin is primarily found in the enteric nervous system located in the gastrointestinal tract (GI tract). However, it is also produced in the central nervous system (CNS), specifically in the raphe nuclei located in the brainstem, Merkel cells located in the skin, pulmonary neuroendocrine cells and taste receptor cells in the tongue. Additionally, serotonin is stored in blood platelets and is ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hyoscine Hydrobromide
Scopolamine, also known as hyoscine, or Devil's Breath, is a natural or synthetically produced tropane alkaloid and anticholinergic drug that is formally used as a medication for treating motion sickness and postoperative nausea and vomiting. It is also sometimes used before surgery to decrease saliva. When used by injection, effects begin after about 20 minutes and last for up to 8 hours. It may also be used orally and as a transdermal patch since it has been long known to have transdermal bioavailability Scopolamine is in the antimuscarinic family of drugs and works by blocking some of the effects of acetylcholine within the nervous system. Scopolamine was first written about in 1881 and started to be used for anesthesia around 1900. Scopolamine is also the main active component produced by certain plants of the nightshade family, which historically have been used as psychoactive drugs (known as ''deliriants'') due to their antimuscarinic-induced hallucinogenic ef ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Palonosetron
Palonosetron, sold under the brand name Aloxi, is used for the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV). It is a 5-HT3 antagonist. Palonosetron is administered intravenously, or as a single oral capsule. Freely available with registration. It has a longer duration of action than other 5-HT3 antagonists. The oral formulation was approved on August 22, 2008, for prevention of acute CINV alone, as a large clinical trial did not show oral administration to be as effective as intravenous use against delayed CINV. It is on the World Health Organization's List of Essential Medicines. The oral combination netupitant/palonosetron is approved for both acute and delayed CINV. Adverse effects The most common adverse effects are headache, which occurs in 4–11% of patients, and constipation in up to 6% of patients. In less than 1% of patients, other gastrointestinal disorders occur, as well as sleeplessness, first- and second-degree atrioventricular bl ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
