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Samidorphan
Samidorphan (, ) (developmental code names ALKS-33, RDC-0313), is an opioid antagonist which in the form of olanzapine/samidorphan (brand name Lybalvi) is used in the treatment of schizophrenia and bipolar disorder. Samidorphan reduces the weight gain associated with olanzapine. Samidorphan is taken by mouth. Samidorphan was under development as a standalone medication for various indications but has been discontinued. Buprenorphine/samidorphan for the treatment of major depressive disorder was rejected by the Food and Drug Administration due to insufficient evidence of effectiveness but remains in preregistration as of September 2021. Development of baclofen/samidorphan has also been discontinued. Development Samidorphan has been investigated for the treatment of alcoholism and cocaine addiction by its developer, Alkermes, showing similar efficacy to naltrexone but possibly with reduced side effects. However, it has attracted much more attention as part of the combination p ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Buprenorphine/samidorphan
Buprenorphine/samidorphan (developmental code name ALKS-5461) is a combination formulation of buprenorphine and samidorphan which is under development as an add on to antidepressants in treatment-resistant depression (TRD). ALKS-5461 failed to meet its primary efficacy endpoints in two trials from 2016. On the basis of a third study that did meet its primary endpoints, Alkermes initiated a rolling New Drug Application with the FDA. In November 2018, an FDA panel voted against recommending approval, finding that evidence was insufficient. As such, approval of the medication was rejected in 2019. It is a κ-opioid receptor (KOR) antagonist and is being developed by Alkermes. Pharmacology Pharmacodynamics ALKS-5461 is a (1:1 ratio) combination of: (1) buprenorphine, a weak partial agonist of the μ-opioid receptor (MOR), antagonist/very weak partial agonist of the κ-opioid receptor (KOR), and, to a lesser extent, antagonist of the δ-opioid receptor (DOR) and weak partial ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Olanzapine/samidorphan
Olanzapine/samidorphan (OLZ/SAM), sold under the brand name Lybalvi, is a fixed-dose combination medication for the treatment of schizophrenia and bipolar I disorder. It contains olanzapine, an atypical antipsychotic, and samidorphan, an opioid antagonist. Samidorphan reduces the weight gain associated with olanzapine Olanzapine (sold under the trade name Zyprexa among others) is an atypical antipsychotic primarily used to treat schizophrenia and bipolar disorder. For schizophrenia, it can be used for both new-onset disease and long-term maintenance. It is ta ... while still allowing olanzapine to exert its therapeutic effect. The formulation was approved for medical use in the United States in May 2021. References External links * * Alpha-1 blockers Antihistamines Atypical antipsychotics Combination drugs Dopamine antagonists Experimental drugs Mu-opioid receptor antagonists Muscarinic antagonists Serotonin receptor antagonists {{Nervous-system-d ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Buprenorphine
Buprenorphine is an opioid used to treat opioid use disorder, acute pain, and chronic pain. It can be used under the tongue (sublingual), in the cheek (buccal), by injection (intravenous and subcutaneous), as a skin patch (transdermal), or as an implant. For opioid use disorder, it is typically started when withdrawal symptoms have begun and for the first two days of treatment under direct observation of a health-care provider. In the United States, the combination formulation of buprenorphine/naloxone (Suboxone) is usually prescribed to discourage misuse by injection. Maximum pain relief is generally within an hour with effects up to 24 hours. Buprenorphine affects different types of opioid receptors in different ways. Depending on the type of receptor, it may be an agonist, partial agonist, or antagonist. In the treatment of opioid use disorder buprenorphine is an agonist/antagonist, meaning that it relieves withdrawal symptoms from other opioids and induces some eu ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alkermes (company)
Alkermes plc is a pharmaceutical company that focuses on central nervous system (CNS) diseases like schizophrenia, bipolar disorder, depression, addiction and multiple sclerosis. The company was founded in 1987 by Michael Wall. In September 2011 Alkermes, Inc. merged with Elan Drug Technologies (EDT), the former drug formulation and manufacturing division of Élan Corporation, plc. The company is headquartered in Dublin, and has an R&D center in Waltham, Massachusetts, and manufacturing facilities in Athlone, Ireland, and Wilmington, Ohio. Products Alkermes has more than 20 commercial drug products and candidates that address serious and chronic illnesses, including schizophrenia, depression, addiction, and diabetes mellitus. Among these products, five are primary to the company: risperidone (microspheres) long-acting injectable (''Risperdal Consta'') for schizophrenia and bipolar 1 disorder, paliperidone palmitate (''Invega Sustenna'' in the U.S., ''Xeplion'' in Europe) for ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Opioid Antagonist
An opioid antagonist, or opioid receptor antagonist, is a receptor antagonist that acts on one or more of the opioid receptors. Naloxone and naltrexone are commonly used opioid antagonist drugs which are competitive antagonists that bind to the opioid receptors with higher affinity than agonists but do not activate the receptors. This effectively blocks the receptor, preventing the body from responding to opioids and endorphins. Some opioid antagonists are not pure antagonists but do produce some weak opioid partial agonist effects, and can produce analgesic effects when administered in high doses to opioid-naive individuals. Examples of such compounds include nalorphine and levallorphan. However, the analgesic effects from these specific drugs are limited and tend to be accompanied by dysphoria, most likely due to additional agonist action at the κ-opioid receptor. As they induce opioid withdrawal effects in people who are taking, or have recently used, opioid full agonist ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Naltrexone
Naltrexone, sold under the brand name Revia among others, is a medication primarily used to manage alcohol or opioid use disorder by reducing cravings and feelings of euphoria associated with substance use disorder. It has also been found to be effective in the treatment of other addictions and may be used for them off-label. An opioid-dependent person should not receive naltrexone before detoxification. It is taken by mouth or by injection into a muscle. Effects begin within 30 minutes. A decreased desire for opioids may take a few weeks to occur. Side effects may include trouble sleeping, anxiety, nausea, and headaches. In those still on opioids, opioid withdrawal may occur. Use is not recommended in people with liver failure. It is unclear if use is safe during pregnancy. Naltrexone is an opioid antagonist and works by blocking the effects of opioids, including both opioid drugs as well as opioids naturally produced in the brain. Naltrexone was first made in 1965 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
κ-opioid Receptor
The κ-opioid receptor or kappa opioid receptor, abbreviated KOR or KOP, is a G protein-coupled receptor that in humans is encoded by the ''OPRK1'' gene. The KOR is coupled to the G protein Gi/G0 and is one of four related receptors that bind opioid-like compounds in the brain and are responsible for mediating the effects of these compounds. These effects include altering nociception, consciousness, motor control, and mood. Dysregulation of this receptor system has been implicated in alcohol and drug addiction. The KOR is a type of opioid receptor that binds the opioid peptide dynorphin as the primary endogenous ligand (substrate naturally occurring in the body). In addition to dynorphin, a variety of natural alkaloids, terpenes and synthetic ligands bind to the receptor. The KOR may provide a natural addiction control mechanism, and therefore, drugs that target this receptor may have therapeutic potential in the treatment of addiction. There is evidence that distribution ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Abuse Potential
Substance abuse, also known as drug abuse, is the use of a drug in amounts or by methods which are harmful to the individual or others. It is a form of substance-related disorder. Differing definitions of drug abuse are used in public health, medical and criminal justice contexts. In some cases, criminal or anti-social behaviour occurs when the person is under the influence of a drug, and long-term personality changes in individuals may also occur. In addition to possible physical, social, and psychological harm, the use of some drugs may also lead to criminal penalties, although these vary widely depending on the local jurisdiction.. Drugs most often associated with this term include: alcohol, amphetamines, barbiturates, benzodiazepines, cannabis, cocaine, hallucinogens (although there is no known ''psychedelic'', one of the three categories of hallucinogens, that has been found to have any addictive potential), methaqualone, and opioids. The exact cause of substance abuse i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antidepressant
Antidepressants are a class of medication used to treat major depressive disorder, anxiety disorders, chronic pain conditions, and to help manage addictions. Common side-effects of antidepressants include dry mouth, weight gain, dizziness, headaches, sexual dysfunction, and emotional blunting. There is a slight increased risk of suicidal thinking and behavior when taken by children, adolescents, and young adults. Discontinuation syndrome may occur after stopping any antidepressant which resembles recurrent depression. Some research regarding the effectiveness of antidepressants for depression in adults has found benefits, whilst other research has not. Evidence of benefit in children and adolescents is unclear. The twenty-one most commonly prescribed antidepressant medications are more effective than placebo for the short-term (acute) treatments of adults with major depressive disorder. There is debate in the medical community about how much of the observed effects of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Oral Administration
Oral administration is a route of administration where a substance is taken through the mouth. Per os abbreviated to P.O. is sometimes used as a direction for medication to be taken orally. Many medications are taken orally because they are intended to have a systemic effect, reaching different parts of the body via the bloodstream, for example. Oral administration can be easier and less painful than other routes, such as injection. However, the onset of action is relatively low, and the effectiveness is reduced if it is not absorbed properly in the digestive system, or if it is broken down by digestive enzymes before it can reach the bloodstream. Some medications may cause gastrointestinal side effects, such as nausea or vomiting, when taken orally. Oral administration can also only be applied to conscious patients, and patients willing and able to swallow. Terminology ''Per os'' (; ''P.O.'') is an adverbial phrase meaning literally from Latin "through the mouth" or "by mouth ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Euphoria
Euphoria ( ) is the experience (or affect) of pleasure or excitement and intense feelings of well-being and happiness. Certain natural rewards and social activities, such as aerobic exercise, laughter, listening to or making music and dancing, can induce a state of euphoria. Euphoria is also a symptom of certain neurological or neuropsychiatric disorders, such as mania. Romantic love and components of the human sexual response cycle are also associated with the induction of euphoria. Certain drugs, many of which are addictive, can cause euphoria, which at least partially motivates their recreational use. Hedonic hotspots – i.e., the pleasure centers of the brain – are functionally linked. Activation of one hotspot results in the recruitment of the others. Inhibition of one hotspot results in the blunting of the effects of activating another hotspot. Therefore, the simultaneous activation of every hedonic hotspot within the reward system is believed to ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
