NationMaster - Encyclopedia: Aripiprazole

Aripiprazole (produced by Otsuka Pharmaceutical Co,. Ltd. and sold as Abilify®) is the sixth and most recent of the atypical antipsychotic medications to be approved by the Food and Drug Administration (FDA) for the treatment of schizophrenia. It has also recently received FDA approval for the treatment of acute manic and mixed episodes associated with bipolar disorder. In pharmacology and toxicology, a route of administration is the path by which a drug, fluid, poison or other substance is brought into contact with the body 1. ... The atypical antipsychotics (also known as second generation antipsychotics) are a class of prescription medications used to treat psychiatric conditions. ... The Food and Drug Administration (FDA) is an agency of the United States Department of Health and Human Services and is responsible for regulating food (humans and animal), dietary supplements, drugs (human and animal), cosmetics, medical devices (human and animal) and radiation emitting devices (including non-medical devices), biologics, and... For the classical mythological figures named Mania, see Mania (mythology). ... For other uses, see Bipolar. ...

Pharmacology

Aripiprazole possesses a novel mechanism of action when compared to the other FDA approved atypical antipsychotics (i.e. clozapine, olanzapine, quetiapine, ziprasidone, and risperidone). Aripiprazole appears to mediate its antipsychotic effects primarily by partial agonism at the D2 receptor. Partial agonism at D2 receptors has been shown to modulate dopaminergic activity in areas where dopamine activity may be high or low, such as the mesolimbic and mesocortical areas of the schizophrenic brain, respectively. In addition to partial agonist activity at the D2 receptor, aripiprazole is also a partial agonist at the 5-HT1A receptor, and like the other atypical antipsychotics, aripiprazole displays an antagonist profile at the 5-HT2A receptor. Aripiprazole has moderate affinity for histamine and alpha adrenergic receptors, and no appreciable affinity for cholinergic muscarinic receptors. The atypical antipsychotics (also known as second generation antipsychotics) are a class of prescription medications used to treat psychiatric conditions. ... Clozapine (sold as ClozarilÂ®, LeponexÂ®, FazacloÂ®) was the first of the atypical antipsychotics to be developed. ... Olanzapine (oh-LAN-za-peen, sold as ZyprexaÂ®, Zyprexa ZydisÂ®, or in combination with fluoxetine, as SymbyaxÂ®) was the third atypical antipsychotic to gain approval by the Food and Drug Administration (FDA) and has become one of the most commonly used atypical antipsychotics. ... Quetiapine (pronounced kwe-TYE-a-peen or ), marketed by AstraZeneca, with the brand name Seroquel, belongs to a series of neuroleptics known as atypical antipsychotics, which have, over the last two decades, become increasingly popular alternatives to typical antipsychotics, such as haloperidol (Haldol). ... Ziprasidone (marketed as GeodonÂ®, ZeldoxÂ®) was the fifth atypical antipsychotic to gain FDA approval. ... Risperdal tablets Risperidone (sold under the trade names Belivon, Rispen and Risperdal in the United States) is an atypical antipsychotic medication developed by Janssen Pharmaceutica. ... Agonists An agonist is a substance that binds to a receptor and triggers a response by the cell. ... Serotonin (5_hydroxytryptamine, or 5_HT) is a monoamine neurotransmitter synthesised in serotonergic neurons in the central nervous system and enterochromaffin cells in the gastrointestinal tract. ...

Pharmacokinetics

Aripiprazole displays linear kinetics with an elimination half-life of approximately 75 hours. Accordingly, steady state plasma concentrations are achieved in about 14 days. Cmax (maximum plasma concentration) is achieved in 3-5 hours after oral dosing. The bioavailabilty of the oral tablets is about 90%. The drug undergoes extensive hepatic metabolization (dehydrogenation, hydroxylation, and N-dealkylation). The active major metabolite is dehydro-aripiprazole with an elimination half-life of about 94 hours. The parent drug is excreted only in traces and the metabolites, whether active or not, are excreted via feces and urine.

Metabolism

Aripiprazole is metabolized by the Cytochrome P450 isoenzymes 3A4 and 2D6. Accordingly, coadministration of aripiprazole with medications that may inhibit (e.g. paroxetine, fluoxetine) or induce (e.g. carbamazepine) these metabolic enzymes may increase or decrease, respectively, plasma concentrations of aripiprazole. Cytochrome P450 Oxidase (CYP2E1) Cytochrome P450 oxidase (commonly abbreviated CYP) is a generic term for a large number of related, but distinct, oxidative enzymes (EC 1. ... Paroxetine or paroxetine hydrochloride is a selective serotonin reuptake inhibitor (SSRI) antidepressant. ... Fluoxetine hydrochloride is an antidepressant drug used medically in the treatment of depression, body dysmorphic disorder, obsessive-compulsive disorder, bulimia nervosa, anorexia nervosa, premenstrual dysphoric disorder, hypochondriasis and panic disorder. ... Carbamazepine (sold under the brand-names Biston, Calepsin, Carbatrol, Epitol, Equetro, Finlepsin, Sirtal, Stazepine, Tegretol, Telesmin, Timonil) is an anticonvulsant and mood stabilizing drug, used primarily in the treatment of epilepsy and bipolar disorder. ...

Adverse events

Adverse events reported in the package insert for aripiprazole include headache, nausea, vomiting, somnolence, insomnia, and akathisia. While Otsuka Pharmaceuticals has reported that the overall risk of EPS (Extrapyramidal Symptoms) is low with aripiprazole, they have separated akathisia from their analysis. With this adverse event included - the risk for EPS become substantial, similar to that of Zyprexa or Risperdal.The risk of tardive dyskinesia with prolonged aripiprazole use is unclear. A headache is a condition of pain in the head; sometimes neck or upper back pain may also be interpreted as a headache. ... For the Beck song, see Nausea (song). ... Vomiting (also throwing up or emesis) is the forceful expulsion of the contents of ones stomach through the mouth and sometimes the nose. ... Somnolence (or drowsiness) is a state of near-sleep, a strong desire for sleep, or sleeping for unusually long periods. ... This article is about the sleeping disorder. ... Akathisia (or acathisia) is an often extremely unpleasant subjective sensation of inner restlessness that manifests itself with an inability to sit still or remain motionless, hence the origin of its name: Greek a (without) + kathesis (sitting). ... Olanzapine (Zyprexa® or in a combination with fluoxetine as Symbyax®) was the second atypical antipsychotic to gain FDA approval and has become one of the most commonly used atypical antipsychotics. ... Risperidone (Belivon®, Rispen®, Risperdal®) is an atypical antipsychotic medication. ... Tardive dyskinesia is a serious neurological disorder caused by the long-term and/or high-dose use of dopamine antagonists, usually antipsychotics and among them especially the typical antipsychotics. ...

Dosage forms

Warnings about medications with similar names

A warning has gone out recently because of this drug's name. The '-prazole' ending of this drug name makes this drug sound like it is one of the proton pump inhibitors (such as omeprazole, pantoprazole, lansoprazole) which are used in treating peptic ulcer disease. However, aripiprazole and these drugs are in an entirely different class of drugs altogether and confusing the two can lead to some unnecessary side effects. Proton pump inhibitors (or PPIs) are a group of drugs whose main action is pronounced and long-lasting reduction of gastric acid production. ... Omeprazole (INN) (IPA: ) is a proton pump inhibitor (brand names AntraÂ® in Italy) used in the treatment of dyspepsia, peptic ulcer disease (PUD), gastroesophageal reflux disease (GORD/GERD) and Zollinger-Ellison syndrome. ... Pantoprazole is a proton pump inhibitor drug used for short-term treatment of erosion and ulceration of the esophagus caused by gastroesophageal reflux disease. ... Lansoprazole, marketed as Takepron (in Japan), Prevacid and Zoton, is a proton pump inhibitor which prevents the stomach from producing acid. ... A benign gastric ulcer (from the antrum) of a gastrectomy specimen. ...

Aripiprazole was developed by Otsuka Pharmaceutical Co., Ltd and is manufactured by the Bristol Myers Squibb pharmaceutical company (NYSE: BMY). Bristol-Myers Squibb (NYSE: BMY), colloquially referred to as BMS, is a pharmaceutical corporation, formed by a 1989 merger between pharmaceutical companies Bristol-Myers Company, founded in 1887 by William McLaren Bristol and John Ripley Myers in Clinton, NY (both were graduates of Hamilton College), and Squibb Corporation. ... A pharmaceutical company, or drug company, is a commercial business licensed to research, develop, market and/or distribute drugs, most commonly in the context of healthcare. ... New York Stock Exchange (June 2003) The New York Stock Exchange (NYSE) is one of the largest stock exchanges in the world. ...

Aripiprazole was approved by the FDA on November 15, 2002. November 15 is the 319th day of the year (320th in leap years) in the Gregorian calendar, with 46 days remaining. ... For album titles with the same name, see 2002 (album). ...

Side effects

Common side effects: Headache, unusual tiredness or weakness, nausea, vomiting, an uncomfortable feeling in the stomach, constipation, light-headedness, trouble sleeping, restlessness, sleepiness, shaking, and blurred vision.

Uncommon side effects: Uncontrollable twitching or jerking movements, tremors and seizure. Some people may feel dizzy, especially when getting up from a lying or sitting position, or may experience a fast heart rate.

Rare side effects: Combination of fever, muscle stiffness, faster breathing, sweating, reduced consciousness, and sudden change in blood pressure and heart rate. An analogue medical thermometer showing the temperature of 38. ... In medicine, hyperventilation (or hyperpnea) is the state of breathing faster or deeper (hyper) than necessary, and thereby reducing the carbon dioxide concentration of the blood below normal. ... Sweat redirects here. ... A sphygmomanometer, a device used for measuring blood pressure. ... Heart rate is a term used to describe the frequency of the cardiac cycle. ...

Very rare side effects: Allergic reaction (such as swelling in the mouth or throat, itching, rash), increased production of saliva, speech disorder, nervousness, agitation, fainting, reports of abnormal liver test values, inflammation of the pancreas, muscle pain, weakness, stiffness, or cramps. This article deals specifically with IgE-mediated hypersensitivity. ... It has been suggested that this article or section be merged with mouth (human). ... Look up Throat in Wiktionary, the free dictionary. ... An itch (Latin: pruritus) is a sensation felt on an area of skin that causes a person or animal to desire to scratch that area. ... A typical rash A rash is a change in the skin which affects its appearance or texture. ... Saliva is the watery and usually somewhat frothy substance produced in the mouths of humans and some animals. ... Speech disorders or speech impediments, as they are also called, are a type of communication disorders where normal speech is disrupted. ... This article includes a list of works cited or a list of external links, but its sources remain unclear because it lacks in-text citations. ... Agitation may have the following special meanings Agitation, an emotional state Agitation, putting into motion (by shaking or stirring) Agitation, a term from the lexicon of Communists: political activities aimed at urging people to do something This is a disambiguation page — a navigational aid which lists other pages that... The term Faint redirects here. ... Liver function tests (LFTs or LFs), which include liver enzymes, are groups of clinical biochemistry laboratory blood assays designed to give information about the state of a patients liver. ... Pancreatitis is inflammation of the pancreas. ... Myalgia means muscle pain and is a symptom of many diseases and disorders. ...

While taking aripiprazole, some elderly patients with dementia have suffered from stroke or 'mini' stroke. Some patients may experience high blood sugar, or the onset or worsening of diabetes. For other uses, see Dementia (disambiguation). ... A stroke, also known as cerebrovascular accident (CVA),[1] is an acute neurological injury in which the blood supply to a part of the brain is interrupted. ... Transient ischemic attacks (TIA) are caused by temporary disturbance of blood supply to a restricted area of brain and cause recurrent and brief (less than 24 hours) neurologic dysfunctions. ... In medicine, blood sugar is a term used to refer to levels of glucose in the blood. ... This article is about the disease that features high blood sugar. ...

See also

The medical expression Tardive Dysphrenia, was proposed by the American neurologist Stanley Fahn, the head of the Division of Movements Disorders of the Neurological Institute of New York, in collaboration with the psychiatrist David V Forrest in the 1970s. ...

External links

Category: Atypical antipsychotics The term antipsychotic is applied to a group of drugs used to treat psychosis. ... A section of the Anatomical Therapeutic Chemical Classification System. ... Phenothiazines are the largest of the 5 main classes of antipsychotic drugs. ... Typical antipsychotics (sometimes referred to as conventional antipsychotics or conventional neuroleptics) are a class of antipsychotic drugs first developed in the 1950s and used to treat psychosis (in particular, schizophrenia), and are generally being replaced by atypical antipsychotic drugs. ... Chlorpromazine was the first antipsychotic drug, used during the 1950s and 1960s. ... Fluphenazineis a typical antipsychoticdrug. ... SerentilÂ® (mesoridazine besylate) is a neuroleptic drug that is used in the treatment of schizophrenia, organic brain disorders, psychoneuroses, and alcoholism. ... This article needs to be cleaned up to conform to a higher standard of quality. ... Prochlorperazine is a highly potent neuroleptic, which is 10 to 20-times more potent than chlorpromazine. ... Promazine is an antipsychotic medication. ... Thioridazine is a piperidine phenothiazine antipsychotic drugs and is used in the treatment of schizophrenia and psychosis. ... Trifluoperazine (EskazinylÂ®, EskazineÂ®, JatroneuralÂ®, ModalinaÂ®, StelazineÂ®, TerfluzineÂ®) is a typical antipsychotic drug of the phenothiazine group. ... Typical antipsychotics (sometimes referred to as conventional antipsychotics or conventional neuroleptics) are a class of antipsychotic drugs first developed in the 1950s and used to treat psychosis (in particular, schizophrenia), and are generally being replaced by atypical antipsychotic drugs. ... Chlorprothixene is a typical antipsychotic drug of the thioxanthine class. ... Droperidol (DropletanÂ®) is an antidopaminergic drug used as an antiemetic and antipsychotic. ... Flupentixol is a synthetic compound that acts on a subset of dopamine receptors. ... Benperidol is a drug which is a butyrophenone derivative. ... Haloperidol (sold as AloperidinÂ®, BioperidoloÂ®, BrotoponÂ®, DozicÂ®, Einalon SÂ®, EukystolÂ®, HaldolÂ®, HalostenÂ®, KeselanÂ®, LintonÂ®, PelucesÂ®, SerenaceÂ®, SerenaseÂ®, SigaperidolÂ®) is a conventional butyrophenone antipsychotic drug. ... Categories: Stub | Typical antipsychotics ... Molindone is a therapeutic antipsychotic, used in the treatment of Schizophrenia. ... Pimozide (sold as OrapÂ®) is an antipsychotic drug. ... Sulforidazine a typical antipsychotic and a metabolite of thioridazine; it is more potent than the parent compound. ... Thiothixene is an antipsychotic drug of the conventional or typical antipsychotics class. ... The atypical antipsychotics (also known as second generation antipsychotics) are a class of prescription medications used to treat psychiatric conditions. ... Amisulpride (brand name SolianÂ®) is an antipsychotic drug sold by Sanofi laboratories. ... Clozapine (sold as ClozarilÂ®, LeponexÂ®, FazacloÂ®) was the first of the atypical antipsychotics to be developed. ... Melperone is sold under the tradenames Buronil, Burnil, and Eunerpan and is a conventional butyrophenone antipsychotic drug. ... Olanzapine (oh-LAN-za-peen, sold as ZyprexaÂ®, Zyprexa ZydisÂ®, or in combination with fluoxetine, as SymbyaxÂ®) was the third atypical antipsychotic to gain approval by the Food and Drug Administration (FDA) and has become one of the most commonly used atypical antipsychotics. ... Quetiapine (pronounced kwe-TYE-a-peen or ), marketed by AstraZeneca, with the brand name Seroquel, belongs to a series of neuroleptics known as atypical antipsychotics, which have, over the last two decades, become increasingly popular alternatives to typical antipsychotics, such as haloperidol (Haldol). ... Risperdal tablets Risperidone (sold under the trade names Belivon, Rispen and Risperdal in the United States) is an atypical antipsychotic medication developed by Janssen Pharmaceutica. ... Paliperidone is an atypical antipsychotic being developed by Janssen. ... Sertindole (brand names: Serlect®, Serdolect®) is one of the newer antipsychotic medications to hit the market. ... Sulpiride (sold as MeresaÂ®, Sulpirid RatiopharmÂ®, Sulpirid NeuraxpharmÂ®,Bosnyl, DogmatilÂ®) is an anti-psychotic drug used mainly in the treatment of psychosis (e. ... Ziprasidone (marketed as GeodonÂ®, ZeldoxÂ®) was the fifth atypical antipsychotic to gain FDA approval. ... Zotepine (Nipolept) is an atypical antipsychotic indicated for acute and chronic schizophrenia. ...

Contents

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