Dopamine antagonist
Encyclopedia
Dopamine
Dopamine is a catecholamine neurotransmitter present in a wide variety of animals, including both vertebrates and invertebrates. In the brain, this substituted phenethylamine functions as a neurotransmitter, activating the five known types of dopamine receptors—D1, D2, D3, D4, and D5—and their...
receptors in the human body; they are found in the brain
Brain
The brain is the center of the nervous system in all vertebrate and most invertebrate animals—only a few primitive invertebrates such as sponges, jellyfish, sea squirts and starfishes do not have one. It is located in the head, usually close to primary sensory apparatus such as vision, hearing,...
, peripheral nervous system
Peripheral nervous system
The peripheral nervous system consists of the nerves and ganglia outside of the brain and spinal cord. The main function of the PNS is to connect the central nervous system to the limbs and organs. Unlike the CNS, the PNS is not protected by the bone of spine and skull, or by the blood–brain...
, blood vessels, gastrointestinal tract
Gastrointestinal tract
The human gastrointestinal tract refers to the stomach and intestine, and sometimes to all the structures from the mouth to the anus. ....
and the kidney
Kidney
The kidneys, organs with several functions, serve essential regulatory roles in most animals, including vertebrates and some invertebrates. They are essential in the urinary system and also serve homeostatic functions such as the regulation of electrolytes, maintenance of acid–base balance, and...
.
Uses and examples
- Used as atypical antipsychotics (coupled with serotonin antagonistSerotonin antagonistA serotonin antagonist is a drug used to inhibit the action at serotonin receptors.Many of the most important medications of this class selectively act at the 5-HT3 receptor, and thus are known as 5-HT3 antagonists...
effects): clozapineClozapineClozapine is an antipsychotic medication used in the treatment of schizophrenia, and is also used off-label in the treatment of bipolar disorder. Wyatt. R and Chew...
, risperidoneRisperidoneRisperidone is a second generation or atypical antipsychotic, sold under the trade name . It is used to treat schizophrenia , schizoaffective disorder, the mixed and manic states associated with bipolar disorder, and irritability in people with autism...
, olanzapineOlanzapineOlanzapine is an atypical antipsychotic, approved by the FDA for the treatment of schizophrenia and bipolar disorder...
, quetiapineQuetiapineQuetiapine , is an atypical antipsychotic approved for the treatment of schizophrenia, and bipolar disorder....
, and ziprasidoneZiprasidoneZiprasidone was the fifth atypical antipsychotic to gain FDA approval . In the United States, Ziprasidone is Food and Drug Administration approved for the treatment of schizophrenia, and the intramuscular injection form of ziprasidone is approved for acute agitation in schizophrenic patients...
- Used as antiemeticAntiemeticAn 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....
s: metoclopramideMetoclopramideMetoclopramide is an antiemetic and gastroprokinetic agent. It is commonly used to treat nausea and vomiting, to facilitate gastric emptying in people with gastroparesis, and as a treatment for the gastric stasis often associated with migraine headaches.-Medical uses:Metoclopramide is commonly...
, droperidolDroperidolDroperidol is an antidopaminergic drug used as an antiemetic and antipsychotic...
, domperidoneDomperidoneDomperidone is an antidopaminergic drug, developed by Janssen Pharmaceutica, and used orally, rectally or intravenously, generally to suppress nausea and vomiting, or as a prokinetic agent...
- Used as tricyclic antidepressantTricyclic antidepressantTricyclic antidepressants are heterocyclic chemical compounds used primarily as antidepressants. The TCAs were first discovered in the early 1950s and were subsequently introduced later in the decade; they are named after their chemical structure, which contains three rings of atoms...
s: amoxapineAmoxapineAmoxapine is a tetracyclic antidepressant of the dibenzoxazepine family, though it is often classified as a secondary amine tricyclic antidepressant.- Uses :...
, clomipramineClomipramineClomipramine is a tricyclic antidepressant . It was developed in the 1960s by the Swiss drug manufacturer Geigy and has been in clinical use worldwide ever since.- Indications :...
Side effects
- ParkinsonismParkinsonismParkinsonism is a neurological syndrome characterized by tremor, hypokinesia, rigidity, and postural instability. The underlying causes of parkinsonism are numerous, and diagnosis can be complex...
– due to effects on the nigrostriatal pathway - HyperprolactinaemiaHyperprolactinaemiaHyperprolactinaemia or hyperprolactinemia is the presence of abnormally-high levels of prolactin in the blood. Normal levels are less than 500 mIU/L for women, and less than 450 mIU/L for men....
– due to effects on the tuberoinfundibular pathway - Tardive dyskinesiaTardive dyskinesiaTardive dyskinesia is a difficult-to-treat form of dyskinesia that can be tardive...
(long term use) - galactorrheaGalactorrheaGalactorrhea or galactorrhoea is the spontaneous flow of milk from the breast, unassociated with childbirth or nursing.Contemporary Maternal-Newborn Nursing Care defines galactorrhea as "nipple discharge." -Causes:...
- due to removal of dopamine-mediated inhibition of prolactinProlactinProlactin also known as luteotropic hormone is a protein that in humans is encoded by the PRL gene.Prolactin is a peptide hormone discovered by Henry Friesen...
release from lactotroph cells in the anterior pituitary
Other side effects may include menstrual dysfunction, low libido, and impotence.
Examples
Examples of Dopamine antagonists include:- acepromazineAcepromazineAcepromazine or acetylpromazine is a phenothiazine derivative antipsychotic drug. It was first used in humans in the 1950s, but is now little used in humans...
- amisulprideAmisulprideAmisulpride , is an atypical antipsychotic used to treat psychosis in schizophrenia and episodes of mania in bipolar disorder. In small doses it is also used to treat depression. It was introduced by Sanofi-Aventis in the 1990s.-Pharmacology:Amisulpride functions primarily as a D2 and D3 receptor...
- amoxapineAmoxapineAmoxapine is a tetracyclic antidepressant of the dibenzoxazepine family, though it is often classified as a secondary amine tricyclic antidepressant.- Uses :...
- azaperoneAzaperoneAzaperone is a pyridinylpiperazine and butyrophenone neuroleptic drug with sedative and antiemetic effects, which is used mainly as a tranquilizer in veterinary medicine. It is used mainly in pigs and elephants. More rarely it may be used in humans as an antipsychotic drug, but this is uncommon...
- benperidolBenperidolBenperidol is a drug which is a highly potent butyrophenone derivative. It is in fact the most potent neuroleptic on the European market, with chlorpromazine equivalency as high as 75 to 100 ....
- bromoprideBromoprideBromopride is a dopamine antagonist with prokinetic properties widely used as an antiemetic, closely related to metoclopramide. It is not available in the United States.Bromopride appears to be safe and effective for use in pregnancy.-Indications:...
- butaclamolButaclamolButaclamol is an antipsychotic which was never marketed. Sold as the hydrochloride salt for use in research, the compound acts as a dopamine receptor antagonist....
- clomipramineClomipramineClomipramine is a tricyclic antidepressant . It was developed in the 1960s by the Swiss drug manufacturer Geigy and has been in clinical use worldwide ever since.- Indications :...
(mild) - chlorpromazineChlorpromazineChlorpromazine is a typical antipsychotic...
- chlorprothixeneChlorprothixeneChlorprothixene is a typical antipsychotic drug of the thioxanthene class and was the first of the series to be synthesized...
- clopenthixolClopenthixolClopenthixol , also known as clopentixol, is a typical antipsychotic drug of the thioxanthene class. It was introduced by Lundbeck in 1961....
- domperidoneDomperidoneDomperidone is an antidopaminergic drug, developed by Janssen Pharmaceutica, and used orally, rectally or intravenously, generally to suppress nausea and vomiting, or as a prokinetic agent...
- droperidolDroperidolDroperidol is an antidopaminergic drug used as an antiemetic and antipsychotic...
- eticloprideEticloprideEticlopride is a dopamine antagonist used in pharmacological research....
- flupenthixol
- fluphenazineFluphenazineFluphenazine is a typical antipsychotic drug used for the treatment of psychoses such as schizophrenia and acute manic phases of bipolar disorder. It belongs to the piperazine class of phenothiazines....
- fluspirileneFluspirileneFluspirilene is a diphenylbutylpiperidine antipsychotic drug, used for the treatment of schizophrenia. It is administered intramuscularly. It was discovered at Janssen Pharmaceutica in 1963.-Chemistry:...
- haloperidolHaloperidolHaloperidol is a typical antipsychotic. It is in the butyrophenone class of antipsychotic medications and has pharmacological effects similar to the phenothiazines....
- iodobenzamideIBZMIBZM is a chemical substance. Pharmaceutically it is a dopamine antagonist and it can be used by nuclear medicine physicians as a radioactive tracer for SPECT where the radioactive isotope is iodine-123 or iodine-125...
- loxapineLoxapineLoxapine is a typical antipsychotic medication, used primarily in the treatment of schizophrenia. It is a member of the dibenzoxazepine class and as a dibenzazepine derivative, it is structurally related to clozapine...
- mesoridazineMesoridazineMesoridazine is a piperidine neuroleptic drug belonging to the class of drugs called phenothiazines, used in the treatment of schizophrenia. It is a metabolite of thioridazine...
- levomepromazineLevomepromazineLevomepromazine in Germany and Methotrimeprazine in America is an aliphatic phenothiazine neuroleptic drug...
- metoclopramideMetoclopramideMetoclopramide is an antiemetic and gastroprokinetic agent. It is commonly used to treat nausea and vomiting, to facilitate gastric emptying in people with gastroparesis, and as a treatment for the gastric stasis often associated with migraine headaches.-Medical uses:Metoclopramide is commonly...
- nafadotrideNafadotrideNafadotride is a dopamine antagonist with reasonable selectivity for the D3 subtype ....
- nemonaprideNemonaprideNemonapride is a atypical antipsychotic approved in Japan for the treatment of schizophrenia. It was launched by Yamanouchi in 1991. Nemonapride acts as a D2 and D3 receptor antagonist, and is also a potent 5-HT1A receptor agonist. It has affinity for sigma receptors.- References :...
- penfluridolPenfluridolPenfluridol is a highly potent, first generation diphenylbutylpiperidine antipsychotic. It was discovered at Janssen Pharmaceutica in 1968. Related to other diphenylbutylpiperidine antipsychotics, pimozide and fluspirilene, penfluridol has an extremely long elimination half-life and its effects...
- perazinePerazinePerazine is a moderate-potency typical antipsychotic of the phenothiazine class. It is quite similar to chlorpromazine, and acts as a dopamine antagonist.- External links :...
- perphenazinePerphenazinePerphenazine is a typical antipsychotic drug. Chemically, it is classified as a piperazinyl phenothiazine. It has been in clinical use for decades....
- pimozidePimozidePimozide is an antipsychotic drug of the diphenylbutylpiperidine class. It was discovered at Janssen Pharmaceutica in 1963. It has a high potency compared to chlorpromazine . On a weight basis it is even more potent than haloperidol. It also has special neurologic indications for Tourette syndrome...
- prochlorperazineProchlorperazineProchlorperazine is a dopamine receptor antagonist that belongs to the phenothiazine class of antipsychotic agents that are used for the antiemetic treatment of nausea and vertigo. It is also a highly-potent typical antipsychotic, 10-20x more potent than chlorpromazine...
- promazinePromazinePromazine is a medication that belongs to the phenothiazine class of antipsychotics. An older medication used to treat schizophrenia, it is still prescribed, alongside newer agents such as olanzapine and quetiapine...
- racloprideRacloprideRaclopride is a synthetic compound that acts as an antagonist on D2 dopamine receptors.It can be radiolabelled with the carbon-11 radioisotope and used in positron emission tomography scanning to assess the degree of dopamine binding to the D2 Dopamine receptor.For example, one study found...
- remoxiprideRemoxiprideRemoxipride is an atypical antipsychotic which was previously used in Europe for the treatment of schizophrenia but was withdrawn due to toxicity concerns . It was initially launched by AstraZeneca in 1990 and suspension of its use began in 1993...
- risperidoneRisperidoneRisperidone is a second generation or atypical antipsychotic, sold under the trade name . It is used to treat schizophrenia , schizoaffective disorder, the mixed and manic states associated with bipolar disorder, and irritability in people with autism...
- spiperoneSpiperoneSpiperone is a psychoactive drug and research chemical belonging to the butyrophenone chemical class. It functions as a 5-HT1A, 5-HT2A, 5-HT7, and D2 receptor antagonist, and has been used to identify these receptors when labeled with tritium. It has negligible affinity for the 5-HT2C receptor...
- spiroxatrineSpiroxatrineSpiroxatrine is drug which acts as a selective antagonist at both the 5-HT1A receptor and the α2C adrenergic receptor. It is an analogue of spiperone, and also has some dopamine antagonist effects....
- stepholidineStepholidine-Stepholidine is a naturally occurring chemical compound found in the herb Stephania intermedia. Stepholidine is a dual D2 receptor antagonist and D1 receptor agonist, and has shown antipsychotic activity in animal studies.-See also:*Apomorphine...
- sulpirideSulpirideSulpiride is an...
- sultoprideSultoprideSultopride is an atypical antipsychotic of the benzamide chemical class used in Europe, Japan, and Hong Kong for the treatment of schizophrenia. It was launched by Sanofi-Aventis in 1976. Sultopride acts as a selective D2 and D3 receptor antagonist...
- tetrahydropalmatineTetrahydropalmatineTetrahydropalmatine is an alkaloid found in several different plant species, mainly in the Corydalis family, but also in other plants such as Stephania rotunda. These plants have traditional uses in Chinese herbal medicine...
- thiethylperazineThiethylperazineThiethylperazine is an antiemetic of the phenothiazine class. Though it was never licensed or used as an antipsychotic, it may have such effects....
- thioridazineThioridazineThioridazine is a piperidine typical antipsychotic drug belonging to the phenothiazine drug group and was previously widely used in the treatment of schizophrenia and psychosis...
- thiothixeneThiothixeneThiothixene is a typical antipsychotic drug of the thioxanthene class used in the treatment of psychoses like schizophrenia. It was introduced on July 24, 1967 by Pfizer.-Chemistry:*Bloom, B. M.; Muren, J. F.; 1967, See also:...
- tiaprideTiaprideTiapride is a benzamide derivative with dopamine antagonist actions similar to sulpiride. It has been used as an antipsychotic and in the treatment of various movement disorders and alcoholism....
- trifluoperazineTrifluoperazineTrifluoperazine is a typical antipsychotic of the phenothiazine chemical class.- Uses :...
- trifluperidolTrifluperidolTrifluperidol is a typical antipsychotic of the butyrophenone chemical class. It has general properties similar to those of haloperidol, but is considerably more potent by weight, and causes relatively more severe side effects, especially tardive dyskinesia and other extrapyramidal effects. It is...
- triflupromazineTriflupromazineTriflupromazine is an antipsychotic medication of the phenothiazine class. Among different effects of triflupromazine indication for use of this drug is severe emesis...
- ziprasidoneZiprasidoneZiprasidone was the fifth atypical antipsychotic to gain FDA approval . In the United States, Ziprasidone is Food and Drug Administration approved for the treatment of schizophrenia, and the intramuscular injection form of ziprasidone is approved for acute agitation in schizophrenic patients...