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Opioid antagonist

Index Opioid antagonist

An opioid antagonist, or opioid receptor antagonist, is a receptor antagonist that acts on one or more of the opioid receptors. [1]

81 relations: Addiction, Alcohol dependence, Alcoholic drink, Alvimopan, Analgesic, Anesthesia, Antidote, Anxiety, AT-076, Axelopran, Barbiturate, Bevenopran, Buprenorphine, Buprenorphine/naltrexone, Buprenorphine/samidorphan, Butorphanol, Cancer, CERC-501, Cocaine dependence, Cyprodime, Depersonalization disorder, Depression (mood), Dezocine, Diprenorphine, Dissociation (psychology), Drug overdose, Drug withdrawal, Dysphoria, Endorphins, Eptazocine, Euphoria, Hallucination, Hannibal (TV series), Heroin, Homeostasis, House (season 2), House (TV series), Hypoventilation, Inverse agonist, J-113,397, JDTic, Levallorphan, Levorphanol, Low-dose naltrexone, Medicine, Methadone, Methylnaltrexone, Morphine, Nalbuphine, Naldemedine, ..., Nalmefene, Nalodeine, Nalorphine, Nalorphine dinicotinate, Naloxegol, Naloxone, Naltrexone, Naltrindole, Nociceptin receptor, Norbinaltorphimine, Opioid, Opioid modulator, Opioid overdose, Opioid receptor, Opioid use disorder, Paraneoplastic syndrome, Partial agonist, Pentazocine, PF-4455242, Phenazocine, Post-acute-withdrawal syndrome, Receptor antagonist, Samidorphan, Scientific method, Sedative, Side effect, Substance abuse, Substance dependence, Toxicity, Veterinary medicine, 6β-Naltrexol. Expand index (31 more) »


Addiction is a brain disorder characterized by compulsive engagement in rewarding stimuli despite adverse consequences.

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Alcohol dependence

Alcohol dependence is a previous psychiatric diagnosis in which an individual is physically or psychologically dependent upon alcohol (also known formally as ethanol).

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Alcoholic drink

An alcoholic drink (or alcoholic beverage) is a drink that contains ethanol, a type of alcohol produced by fermentation of grains, fruits, or other sources of sugar.

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Alvimopan (trade name Entereg) is a drug which behaves as a peripherally acting μ-opioid antagonist.

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An analgesic or painkiller is any member of the group of drugs used to achieve analgesia, relief from pain.

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In the practice of medicine (especially surgery and dentistry), anesthesia or anaesthesia (from Greek "without sensation") is a state of temporary induced loss of sensation or awareness.

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An antidote is a substance which can counteract a form of poisoning.

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Anxiety is an emotion characterized by an unpleasant state of inner turmoil, often accompanied by nervous behaviour such as pacing back and forth, somatic complaints, and rumination.

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AT-076 is a so-called opioid "pan" antagonist and is the first reasonably balanced antagonist known of all four opioid receptor types.

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Axelopran (INN, USAN) (developmental code name TD-1211) is a drug which is under development by Theravance Biopharma for the treatment of opioid-induced constipation.

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A barbiturate is a drug that acts as a central nervous system depressant, and can therefore produce a wide spectrum of effects, from mild sedation to death.

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Bevenopran (INN, USAN) (former developmental code names CB-5945, ADL-5945, MK-2402, OpRA III) is a peripherally selective μ- and δ-opioid receptor antagonist that was under development by Cubist Pharmaceuticals for the treatment of chronic opioid-induced constipation.

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Buprenorphine, sold under the brand name Subutex, among others, is an opioid used to treat opioid addiction, acute pain, and chronic pain.

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Buprenorphine/naltrexone is an experimental combination drug formulation of buprenorphine, a μ-opioid receptor (MOR) weak partial agonist and κ-opioid receptor (KOR) antagonist, and naltrexone, a MOR and KOR silent antagonist, which is under investigation for the potential treatment of psychiatric disorders.

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Buprenorphine/samidorphan (developmental code name ALKS-5461) is a combination drug formulation of buprenorphine and samidorphan acting as a κ-opioid receptor (KOR) antagonist which is under development by Alkermes as an adjunct to antidepressant therapy in treatment-resistant depression (TRD).

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Butorphanol (BC 2627) is a morphinan-type synthetic agonist–antagonist opioid analgesic developed by Bristol-Myers.

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Cancer is a group of diseases involving abnormal cell growth with the potential to invade or spread to other parts of the body.

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CERC-501 (originally known as LY-2456302) is a selective antagonist of the κ-opioid receptor (KOR) which was originally developed by Eli Lilly and is now under development by Janssen Pharmaceuticals for the treatment of major depressive disorder and substance use disorders including alcoholism, nicotine addiction, and illicit drug dependence.

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Cocaine dependence

Cocaine dependence is a psychological desire to use cocaine regularly.

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Cyprodime is an opioid antagonist from the morphinan family of drugs.

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Depersonalization disorder

Depersonalization disorder (DPD), also known as depersonalization/derealization disorder, is a mental disorder in which the person has persistent or recurrent feelings of depersonalization or derealization.

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Depression (mood)

Depression is a state of low mood and aversion to activity that can affect a person's thoughts, behavior, tendencies, feelings, and sense of well-being.

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Dezocine (INN, USAN) (brand name Dalgan) is a marketed opioid analgesic of the benzomorphan group.

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Diprenorphine (brand name Revivon; former developmental code name M5050), also known as diprenorfin, is a non-selective, high-affinity, weak partial agonist of the μ- (MOR), κ- (KOR), and δ-opioid receptor (DOR) (with equal affinity) that is employed in veterinary medicine as an opioid antagonist.

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Dissociation (psychology)

In psychology, dissociation is any of a wide array of experiences from mild detachment from immediate surroundings to more severe detachment from physical and emotional experiences.

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Drug overdose

The term drug overdose (or simply overdose or OD) describes the ingestion or application of a drug or other substance in quantities greater than are recommended or generally practiced.

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Drug withdrawal

Drug withdrawal is the group of symptoms that occur upon the abrupt discontinuation or decrease in intake of medications or recreational drugs.

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Dysphoria (from δύσφορος (dysphoros), δυσ-, difficult, and φέρειν, to bear) is a profound state of unease or dissatisfaction.

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Endorphins (contracted from "endogenous morphine") are endogenous opioid neuropeptides and peptide hormones in humans and other animals.

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Eptazocine (Sedapain) is an opioid analgesic which was introduced in Japan by Morishita in 1987.

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Euphoria is an affective state in which a person experiences pleasure or excitement and intense feelings of well-being and happiness.

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A hallucination is a perception in the absence of external stimulus that has qualities of real perception.

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Hannibal (TV series)

Hannibal is an American psychological horror–thriller television series developed by Bryan Fuller for NBC.

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Heroin, also known as diamorphine among other names, is an opioid most commonly used as a recreational drug for its euphoric effects.

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Homeostasis is the tendency of organisms to auto-regulate and maintain their internal environment in a stable state.

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House (season 2)

The second season of House premiered on September 13, 2005 and ended on May 23, 2006.

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House (TV series)

House (also called House, M.D.) is an American television medical drama that originally ran on the Fox network for eight seasons, from November 16, 2004 to May 21, 2012.

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Hypoventilation (also known as respiratory depression) occurs when ventilation is inadequate (hypo meaning "below") to perform needed gas exchange.

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Inverse agonist

In the field of pharmacology, an inverse agonist is an agent that binds to the same receptor as an agonist but induces a pharmacological response opposite to that agonist.

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J-113,397 is an opioid drug which was the first compound found to be a highly selective antagonist for the nociceptin receptor, also known as the ORL-1 receptor.

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JDTic is a selective, long-acting ("inactivating") antagonist of the κ-opioid receptor (KOR).

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Levallorphan (INN, BAN) (brand names Lorfan, Naloxifan, Naloxiphan), also known as levallorphan tartrate (USAN), is an opioid modulator of the morphinan family used as an opioid analgesic and opioid antagonist/antidote.

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Levorphanol (INN; brand name Levo-Dromoran) is an opioid medication used to treat moderate to severe pain.

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Low-dose naltrexone

Low-dose naltrexone (LDN) describes the off-label use of the medication naltrexone at low doses for diseases such as Crohn's disease and multiple sclerosis.

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Medicine is the science and practice of the diagnosis, treatment, and prevention of disease.

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Methadone, sold under the brand name Dolophine among others, is an opioid used to treat pain and as maintenance therapy or to help with tapering in people with opioid dependence.

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Methylnaltrexone (MNTX, brand name Relistor), used in form of methylnaltrexone bromide (INN, USAN, BAN), is one of the newer agents of peripherally acting μ-opioid antagonists that act to reverse some of the side effects of opioid drugs such as constipation without affecting analgesia or precipitating withdrawals.

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Morphine is a pain medication of the opiate variety which is found naturally in a number of plants and animals.

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Nalbuphine, sold under the brand names Nubain and Nalpain among others, is a opioid analgesic which is used in the treatment of pain.

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Naldemedine (INN, USAN; S-297,995, Symproic) is a peripherally-selective μ-opioid receptor antagonist developed by Shionogi which is approved for the treatment of opioid-induced constipation in adult patients with chronic non-cancer pain.

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Nalmefene (trade name Selincro), originally known as nalmetrene, is an opioid antagonist used primarily in the management of alcohol dependence.

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Nalodeine, also known more commonly as N-allylnorcodeine, is an opioid antagonist (specifically, an antagonist of the μ-opioid receptor) that was never marketed but is of notability in having been the first opioid antagonist to have been discovered.

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Nalorphine (brand names Lethidrone, Nalline), also known as N-allylnormorphine, is a mixed opioid agonist–antagonist with opioid antagonist and analgesic properties.

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Nalorphine dinicotinate

Nalorphine dinicotinate (trade name Nimelan), also known as N-allylnormorphine dinicotinate, dinicotinoylnalorphine, or niconalorphine, is a semisynthetic, mixed opioid agonist-antagonist which is described as an narcotic antagonist but may produce limited analgesia and sedation at higher doses in opioid naive patients (with limited euphoria and dependence liability).

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Naloxegol (INN; PEGylated naloxol; trade names Movantik and Moventig) is a peripherally selective opioid antagonist developed by AstraZeneca, licensed from Nektar Therapeutics, for the treatment of opioid-induced constipation.

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Naloxone, sold under the brandname Narcan among others, is a medication used to block the effects of opioids, especially in overdose.

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Naltrexone, sold under the brand names ReVia and Vivitrol among others, is a medication primarily used to manage alcohol or opioid dependence.

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Naltrindole is a highly potent, highly selective delta opioid receptor antagonist used in biomedical research.

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Nociceptin receptor

The nociceptin opioid peptide receptor (NOP), also known as the nociceptin/orphanin FQ (N/OFQ) receptor or kappa-type 3 opioid receptor, is a protein that in humans is encoded by the OPRL1 (opioid receptor-like 1) gene.

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Norbinaltorphimine (nor-BNI or nBNI) is an opioid antagonist used in scientific research.

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Opioids are substances that act on opioid receptors to produce morphine-like effects.

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Opioid modulator

An opioid modulator (or opioid receptor modulator) is a drug which has mixed agonist and antagonist actions at different opioid receptors and thus cannot clearly be described as either an opioid agonist or antagonist.

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Opioid overdose

An opioid overdose is toxicity due to excessive opioids.

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Opioid receptor

Opioid receptors are a group of inhibitory G protein-coupled receptors with opioids as ligands.

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Opioid use disorder

Opioid use disorder is a medical condition characterized by a problematic pattern of opioid use that causes clinically significant impairment or distress.

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Paraneoplastic syndrome

A paraneoplastic syndrome is a syndrome (a set of signs and symptoms) that is the consequence of cancer in the body, but unlike mass effect, is not due to the local presence of cancer cells.

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Partial agonist

In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist.

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Pentazocine, sold under the brand name Talwin among others, is a painkiller used to treat moderate to severe pain.

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PF-4455242 is a selective, short-acting (non-"inactivating") antagonist of the κ-opioid receptor.

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Phenazocine (brand names Prinadol, Narphen) is an opioid analgesic drug, which is related to pentazocine and has a similar profile of effects.

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Post-acute-withdrawal syndrome

Post-acute-withdrawal syndrome (PAWS) describe a set of persistent impairments that occur after withdrawal from alcohol, opiates, benzodiazepines, antidepressants and other substances.

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Receptor antagonist

A receptor antagonist is a type of receptor ligand or drug that blocks or dampens a biological response by binding to and blocking a receptor rather than activating it like an agonist.

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Samidorphan (INN, USAN) (developmental code names ALKS-33, RDC-0313), also known as 3-carboxamido-4-hydroxynaltrexone, is an opioid antagonist that preferentially acts as an antagonist of the μ-opioid receptor (MOR).

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Scientific method

Scientific method is an empirical method of knowledge acquisition, which has characterized the development of natural science since at least the 17th century, involving careful observation, which includes rigorous skepticism about what one observes, given that cognitive assumptions about how the world works influence how one interprets a percept; formulating hypotheses, via induction, based on such observations; experimental testing and measurement of deductions drawn from the hypotheses; and refinement (or elimination) of the hypotheses based on the experimental findings.

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A sedative or tranquilliser is a substance that induces sedation by reducing irritability or excitement.

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Side effect

In medicine, a side effect is an effect, whether therapeutic or adverse, that is secondary to the one intended; although the term is predominantly employed to describe adverse effects, it can also apply to beneficial, but unintended, consequences of the use of a drug.

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Substance abuse

Substance abuse, also known as drug abuse, is a patterned use of a drug in which the user consumes the substance in amounts or with methods which are harmful to themselves or others, and is a form of substance-related disorder.

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Substance dependence

Substance dependence also known as drug dependence is an adaptive state that develops from repeated drug administration, and which results in withdrawal upon cessation of drug use.

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Toxicity is the degree to which a chemical substance or a particular mixture of substances can damage an organism.

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Veterinary medicine

Veterinary medicine is the branch of medicine that deals with the prevention, diagnosis and treatment of disease, disorder and injury in non-human animals.

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6β-Naltrexol, or 6α-hydroxynaltrexone, is a major active metabolite of naltrexone formed by hepatic dihydrodiol dehydrogenase which acts as a potent, peripherally selective opioid neutral antagonist.

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Narcotic antagonist, Narcotic antagonists, Opiate antagonist, Opioid receptor antagonist.


[1] https://en.wikipedia.org/wiki/Opioid_antagonist

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