Fear God (UNDER CONSTRUCTION)

FEAR GOD

Revelation 14: 7 And I saw another angel fly in the midst of heaven, having the everlasting gospel to preach unto them that dwell on the earth, and to every nation, and kindred, and tongue, and people, 7Saying with a loud voice, Fear God, and give glory to him; for the hour of his judgment is come: and worship him that made heaven, and earth, and the sea, and the fountains of waters. 8And there followed another angel, saying, Babylon is fallen, is fallen, that great city, because she made all nations drink of the wine of the wrath of her fornication. 8And there followed another angel, saying, Babylon is fallen, is fallen, that great city, because she made all nations drink of the wine of the wrath of her fornication. 9And the third angel followed them, saying with a loud voice, If any man worship the beast and his image, and receive his mark in his forehead, or in his hand, 10The same shall drink of the wine of the wrath of God, which is poured out without mixture into the cup of his indignation; and he shall be tormented with fire and brimstone in the presence of the holy angels, and in the presence of the Lamb: 11And the smoke of their torment ascendeth up for ever and ever: and they have no rest day nor night, who worship the beast and his image, and whosoever receiveth the mark of his name. 12Here is the patience of the saints: here are they that keep the commandments of God, and the faith of Jesus.

Ecclesiastes 12:13 Let us hear the conclusion of the whole matter: Fear God, and keep his commandments: for this is the whole duty of man.14For God shall bring every work into judgment, with every secret thing, whether it be good, or whether it be evil.

Universality and Cosmology

ANALYZING UNDERLYING IMPETUSES AS REFLECTED IN HISTORY (1840's-present)
Religion Civil Rights Science and Technology Space Forms of government Wars and conflicts
Crimes against humanity Literature Entertainment

Universitarianism reflected in religions, military, and politics. (1800's) III

Showing posts with label disinformation. Show all posts
Showing posts with label disinformation. Show all posts

Sunday, October 17, 2010

Aleister Crowley

Aleister Crowley

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Aleister Crowley

Crowley in occult garb, 1911
Born Edward Alexander Crowley
12 October 1875
(1875-10-12) Royal Leamington Spa, Warwickshire, England
Died 1 December 1947 (aged 72)
Hastings
, East Sussex, England
Signature
Aleister Crowley (pronounced /ˈkroʊli/; 12 October 1875 – 1 December 1947), born Edward Alexander Crowley, and also known as both Frater Perdurabo and The Great Beast, was an influential English occultist, mystic and ceremonial magician, responsible for founding the religious philosophy of Thelema. Through this belief he came to see himself as the prophet who was entrusted with informing humanity that it was entering the new Aeon of Horus in 1904, a time when old ethical and religious systems would be replaced. Widely seen as one of the most influential occultists of all time, he was a member of the esoteric Hermetic Order of the Golden Dawn, as well as a co-founder of the A∴A∴ and eventually a leader of Ordo Templi Orientis (O.T.O.). He is known today for his magical writings, especially The Book of the Law, the central sacred text of Thelema, although he also wrote widely on other subjects, including a large amount of fiction and poetry.
Crowley was also a bisexual, recreational drug experimenter and social critic.[1] In many of these roles he "was in revolt against the moral and religious values of his time", espousing a form of libertinism based upon the rule of "Do What Thou Wilt".[2] Because of this, he gained widespread notoriety during his lifetime, and was denounced in the popular press of the day as "the wickedest man in the world."[3][4][5][6] Alongside his esoteric activities, he was an avid chess player, mountaineer, poet and playwright, and it has also been alleged that he was a spy for the British government.[7]
Crowley has remained an influential figure right up till this day, and in 2002, a BBC poll described him as being the seventy-third greatest Briton of all time. References to him can be found in the works of numerous writers, musicians and filmmakers,[8] and he has also been cited as a key influence on many later esoteric groups and individuals, including Kenneth Grant, Gerald Gardner and, to some degree, Austin Osman Spare.[9]

EXCERPT

Theory of Crowley as a British spy

Richard B. Spence writes in his 2008 book Secret Agent 666: Aleister Crowley, British Intelligence and the OccultBritish Intelligence. While this may have already been the case during his many travels to Tsarist Russia, Switzerland, Asia, Mexico and North Africa that had started in his student days, he could have been involved with this line of work during his life in America during the First World War, under a cover of being a German propaganda agent and a supporter of Irish independence. Crowley's mission might have been to gather information about the German intelligence network, the Irish independent activists and produce aberrant propaganda, aiming at compromising the German and Irish ideals. As an agent provocateur he could have played some role in provoking the sinking of the RMS Lusitania, thereby bringing the United States closer to active involvement in the war alongside the Allies.[77] He also used German magazines The Fatherland and The International as outlets for his other writings. The question of whether Crowley was a spy has always been subject to debate, but Spence uncovered a document from the US Army's old Military Intelligence Division supporting Crowley's own claim to having been a spy: that Crowley could have been a lifelong agent for
Aleister Crowley was an employee of the British Government ... in this country on official business of which the British Consul, New York City has full cognizance.[78]


Friday, October 15, 2010

Pseudoephedrine

Pseudoephedrine

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Pseudoephedrine
Systematic (IUPAC) name
(R*,R*)-2-methylamino-1-phenylpropan-1-ol
Identifiers
CAS number 90-82-4
ATC code R01BA02
PubChem CID 7028
DrugBank DB00852
ChemSpider 6761
Chemical data
Formula C10H15NO 
Mol. mass 165.23
Pharmacokinetic data
Bioavailability ~100%[1]
Metabolism hepatic (10–30%)
Half-life 4.3-8 hours[1]
Excretion 43-96% renal[1]
Therapeutic considerations
Pregnancy cat. B2(AU) C(US)
Legal status Pharmacist Only (S3) (AU) P (UK)
Routes oral
 Yes(what is this?)  (verify)Y
Pseudoephedrine (PSE) [pronunciation: /ˌsuːdəʊɪˈfɛdɹɪn/ or /ˌsuːdoˈɛfədriːn/] is a sympathomimetic drug of the phenethylamine and amphetamine chemical classes. It is used as a nasal/sinus decongestant and stimulant, or as a wakefulness-promoting agent.
The salts pseudoephedrine hydrochloride and pseudoephedrine sulfate are found in many over-the-counter preparations either as a single ingredient or, more commonly, in combination with antihistamines, guaifenesin, dextromethorphan, paracetamol (acetaminophen), and/or NSAIDs (e.g., aspirin, ibuprofen, etc.).

Contents

[show]

[edit] Chemistry


Two pairs of enantiomers: Ephedrine (top) and Pseudoephedrine (bottom)
Pseudoephedrine is a diastereomer of ephedrine. Pseudoephedrine is a chiral molecule, meaning it occurs in both "left-handed" and "right-handed" configurations which are not superimposable.
Pseudoephedrine is a precursor of methamphetamine and methcathinone.

[edit] Nomenclature

The dextrorotary (+)- or d- enantiomer is (1S,2S)-Pseudoephedrine, whereas the levorotating (−)- or l- form is (1R,2R)-Pseudoephedrine.
In the outdated d/l system (+)-Pseudoephedrine is also referred to as l-Pseudoephedrine and (—)-Pseudoephedrine as d-Pseudoephedrine (in the Fisher projection then the phenylring is drawn at bottom). [2] [3]
Often the d/l system (with small caps) and the d/l system (with lower-case) are confused. The result is that the dextrorotary d-Pseudoephedrine is wrongly named d-Pseudoephedrine and the levorotary l-Ephedrine (the diastereomer) wrongly l-Ephedrine.
The IUPAC names of the two enantiomers are (1S,2S)- respectively (1R,2R)-2-methylamino-1-phenylpropan-1-ol. Synonyms for both are psi-Ephedrine and threo-Ephedrine.
Pseudoephedrine is the International Nonproprietary Name (INN) of the (+)-form, when used as pharmaceutical substance. [4]

[edit] Synthesis

Although pseudoephedrine occurs naturally as an alkaloid in certain plant species (for example, as a constituent of extracts from the ephedra species, also known as Ma Huang, in which it occurs together with other isomers of ephedrine), the majority of pseudoephedrine produced for commercial use is derived from yeast fermentation of dextrose in the presence of benzaldehyde. In this process, specialized strains of yeast (typically a variety of Candida utilis or Saccharomyces cerevisiae) are added to large vats containing water, dextrose and the enzyme pyruvate decarboxylase (such as found in beets and other plants). After the yeast has begun fermenting the dextrose, the benzaldehyde is added to the vats, and in this environment the yeast convert the ingredients to the precursor l-phenylacetylcarbinol (L-PAC). L-PAC is then chemically converted to pseudoephedrine via reductive amination.[5]
The bulk of pseudoephedrine is produced by commercial pharmaceutical manufacturers in India and China, where economic and industrial conditions favor the mass production of pseudoephedrine for export.[6]

[edit] Mechanism of action

Pseudoephedrine is a sympathomimetic amine. Its principal mechanism of action relies on its indirect action on the adrenergic receptor system. The vasoconstriction that pseudoephedrine produces is believed to be principally an α-adrenergic receptor response. [7]
While it may have weak or no direct agonist activity at α- and β-adrenergic receptors, the principal mechanism is to cause the release of endogenous norepinephrine (noradrenaline) from storage vesicles in presynaptic neurons. The displaced noradrenaline is released into the neuronal synapse where it is free to activate the postsynaptic adrenergic receptors. These adrenergic receptors are located on the muscles lining the walls of blood vessels. When activated by pseudoephedrine, the muscles contract, causing the blood vessels to constrict (vasoconstriction). The constricted blood vessels now allow less fluid to leave the blood vessels and enter the nose, throat and sinus linings, which results in decreased inflammation of nasal membranes as well as decreased mucus production. Thus, by constriction of blood vessels, mainly those located in the nasal passages, pseudoephedrine causes a decrease in the symptoms of nasal congestion.

Risperdal (psedoscience and the psychiatric equivalent to AIDS/HIV/H4)

Risperidone

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  (Redirected from Risperdal)
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Risperidone
Systematic (IUPAC) name
4-[2-[4-(6-fluorobenzo[d]isoxazol-3-yl)-
1-piperidyl]ethyl]-3-methyl-
2,6-diazabicyclo[4.4.0]deca-1,3-dien-5-one
Identifiers
CAS number 106266-06-2
ATC code N05AX08
PubChem CID 5073
IUPHAR ligand ID 96
DrugBank DB00734
ChemSpider 4895
Chemical data
Formula C23H27FN4O2 
Mol. mass 410.485 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability 70% (oral)
Metabolism Hepatic (CYP2D6-mediated)
Half-life 3–20 hours
Excretion Urinary
Therapeutic considerations
Pregnancy cat. C
Legal status Prescription only
Routes Oral and extended-release intramuscular injection
 Yes(what is this?)  (verify)Y
Risperidone (pronounced Ris-PEAR-rǐ-dōne) is an atypical antipsychotic used to treat schizophreniaschizoaffective disorder, the mixed and manic states associated with bipolar disorder, and irritability in children with autism. The drug was developed by Janssen-Cilag and first released in 1994[1]. It is sold under the trade name Risperdal in the Netherlands, United States, Canada, Australia, United Kingdom, Portugal, Spain, Turkey, New Zealand and several other countries, Risperdal or Ridal in New Zealand, Sizodon or Riscalin in India, Rispolept in Eastern Europe, and Russia, and Belivon, or Rispen elsewhere. (including adolescent schizophrenia),

Contents

[show]

[edit] Indications and Uses

  • treatment of schizophrenia in adults
  • treatment of schizophrenia in adolescents aged 13-17 years
  • alone or in combination with lithium or valproate, for the short-term treatment of acute manic or mixed episodes associated with Bipolar I Disorder in adults
  • alone in the short-term treatment of acute manic or mixed episodes associated with Bipolar I Disorder in children and adolescents aged 10-17 years
  • treatment of irritability associated with autistic disorder in children and young adults
  • it has also been used as a control drug for people with tourette syndrome and other tic disorders.
  • treatment of major depression with psychotic features
  • cure persistent or intractable hiccups[2]
Risperidone was approved by the United States Food and Drug Administration (FDA) in 1993 for the treatment of schizophrenia.[3]
On August 22, 2007, risperidone was approved as the only drug agent available for treatment of schizophrenia in youth ages 13–17; it was also approved that same day for treatment of bipolar disorder in youth and children ages 10–17, joining lithium. Risperidone contains the functional groups of benzisoxazolepiperidine as part of its molecular structure. In 2003 the FDA approved risperidone for the short-term treatment of the mixed and manic states associated with bipolar disorder. In 2006 the FDA approved risperidone for the treatment of irritability in children and adolescents with autism.[4] The FDA's decision was based in part on a study of autistic children with severe and enduring problems of violent meltdowns, aggression, and self-injury; risperidone is not recommended for autistic children with mild aggression and explosive behavior without an enduring pattern.[5] Like other atypical antipsychotics, risperidone has also been used off-label for the treatment of anxiety disorders, such as obsessive-compulsive disorder; severe, treatment-resistant depression with or without psychotic features; tourette syndrome; disruptive behavior disorders in children; and eating disorders, among others. In two small studies risperidone was reported to successfully treat the symptoms of phencyclidine (PCP) psychosis due to acute intoxication[6] and chronic use.[7] and
A 2009 Cochrane Library review found no evidence from randomized controlled trials that risperidone is effective for the treatment of attention-deficit hyperactivity disorder (ADHD) in people with intellectual disabilities.[8] A multi-year UK study by the Alzheimer's Research Trust suggested that this and other neuroleptic anti-psychotic drugs commonly given to Alzheimer's patients with mild behavioural problems often made their condition worse. The study concluded that:
For most patients with AD, withdrawal of neuroleptics had no overall detrimental effect on functional and cognitive status and by some measures improved functional and cognitive status. Neuroleptics may have some value in the maintenance treatment of more severe neuropsychiatric symptoms, but this possibility must be weighed against the unwanted effects of therapy.[9]

[edit] Availability


Risperdal 4 mg tablets (UK)
Janssen's patent on Risperdal expired on December 29, 2003, opening the market for cheaper generic versions of the drug from other companies, and Janssen's exclusive marketing rights expired on June 29, 2004 (the result of a pediatric extension.)
Risperidone is available as a tablet in 0.25, 0.5, 1, 2, 3 and 4 mg sizes, as an oral solution (30ml, 1 mg/ml), and as a 12.5 mg, 25 mg, 37.5 mg and 50 mg ampoule Risperdal Consta, which is a depot injectionRisperdal M-Tabs and elsewhere as Risperdal Quicklets. administered once every two weeks. It is also available as a wafer known in the United States and Canada as
Risperidone became available as a generic drug in October 2008 from Teva Pharmaceuticals, Dr. Reddy's Laboratories, Inc. and Patriot Pharmaceutics. The Patriot generic is Janssen Pharmaceutical's "authorized generic pharmaceutical."

[edit] Side effects

Risperidone has been associated with weight gain.[10] Other common side effects include akathisia, sedation, dysphoria, insomnia, sexual dysfunction, low blood pressure, high blood pressure, muscle stiffness, muscletremors, increased salivation, constipation, and stuffy nose. pain,
Many antipsychotics are known to cause hyperprolactinemia which may lead to hypogonadism-induced osteoporosis, galactorrhoea, gynaecomastia, irregular menstruation and sexual dysfunction. However, risperidone is known to increase prolactin to a greater extent than other atypical antipsychotics. Although lactation is possible in both sexes using other antipsychotic drugs, risperidone is the biggest offender.[11][12][13] It is thought that once risperidone raises prolactin, it may cause prolactinoma, a benign tumor of the pituitary gland. Tumors, in general, are not considered reversible. Medical therapy may help reduce tumor size and restore normal reproduction and pituitary function, however, dopamine agonists[14] There is a higher association between pituitary neoplasms with use of risperidone and amisulpride than with other antipsychotic agents. are not likely to be prescribed to antipsychotic users, thus, surgery or radiation treatment may be required. This condition may recur if the patient is switched to a different antipsychotic. Risperidone has been known to cause increased thoughts of suicide.
Risperidone can potentially cause tardive dyskinesia (TD),[15] extrapyramidal symptoms (EPS),[15] and neuroleptic malignant syndrome (NMS).[15] Risperidone may also trigger diabetes and more serious conditions of glucose metabolism, including ketoacidosis and hyperosmolar coma, according to an FDA Warning Letter issued to Janssen Pharmaceutica, Inc. on 19-Apr-04.[16]

[edit] Pharmacology

This drug belongs to a class of antipsychotic drugs known as atypical antipsychotics that have more pronounced serotonin antagonism than dopamine antagonism, but risperidone is unique in this class because it retains dopamine antagonism. It has high affinity for D2 dopaminergic receptors. It has actions at several 5-HT (serotonin) receptor subtypes. These are 5-HT2C, linked to weight gain, 5-HT2A,linked to its antipsychotic action and relief of some of the extrapyramidal side effects (EPS) experienced with the typical neuroleptics.
It reaches peak plasma levels quickly regardless of whether it is administered as a liquid or pill. Risperidone is metabolised fairly quickly, so the potential for nausea subsides usually in two to three hours. However, the active metabolite, 9-hydroxy-risperidone, which has similar pharmacodynamics to risperidone, remains in the body for much longer, and has been developed as an antipsychotic in its own right, called paliperidone.
An intramuscular preparation, marketed as Risperdal Consta, can be given once every two weeks. It is slowly released from the injection site. This method of administration may be used on sanctioned patients who are declining, or consenting patients who may have disorganized thinking and cannot remember to take their daily doses.[17] Doses range from 12.5 to 50 mg given as an intramuscular injection once every two weeks.

Misinformation / Disinformation

Misinformation

Misinformation is false or inaccurate information that is spread unintentionally. It is distinguished from disinformation by motive in that misinformation is simply erroneous, while disinformation, in contrast, is intended to mislead.[1]
Makkai proposes the distinction between misinformation and disinformation to be a defining characteristic of idioms in the English language.[2] An utterance is only idiomatic if it involves disinformation, where the listener can decode the utterance in a logical, and lexically correct, yet erroneous way. Where the listener simply decodes the lexemes incorrectly, the utterance is simply misinformation, and not idiomatic.
Damian Thompson defines counterknowledge as "misinformation packaged to look like fact".[3] Using the definition above, this may refer to disinformation, as the motive is deliberate and often pecuniary.

Contents

[show]

[edit] Examples

According to Thompson, all three of the following statements are misinformations, or counterknowledge, packaged to look like fact:

Abilify (Phi)(ability)

Double play on words (Phi, Ability), comp. lexapro

 Aripiprazole

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Aripiprazole
Systematic (IUPAC) name
7-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy}-3,4-dihydroquinolin-2(1H)-one
Identifiers
CAS number 129722-12-9
ATC code N05AX12
PubChem CID 60795
IUPHAR ligand ID 34
DrugBank APRD00638
ChemSpider 54790
UNII 82VFR53I78
Chemical data
Formula C23H27Cl2N3O2 
Mol. mass 448.385
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability 87%
Protein binding >99%
Metabolism liver
Half-life 75h (active metabolite : 94h)
Excretion feces and urine
Therapeutic considerations
Licence data EU EMA:LinkUS FDA:link
Pregnancy cat. C (USA)
Legal status Prescription only
Routes oral (via tablets, orodispersable tablets, and oral solution); intramuscular
 Yes(what is this?)  (verify)Y
Aripiprazole (pronounced /ˌɛərɨˈpɪprəzoʊl/ AIR-i-PIP-rə-zohl; brand names: Abilify, Abilify Discmelt, Aripiprex) is an atypical antipsychotic and antidepressant used in the treatment of schizophrenia, bipolar disorder, and clinical depression. It was approved by the US Food and Drug Administration (FDA) for schizophrenia on November 15, 2002, for acute manic and mixed episodes associated with bipolar disorder on October 1, 2004, as an adjunct for major depressive disorder on November 20, 2007 and to treat irritability in children with autistic disorder in children on 20 November 2009.[1][2] Aripiprazole was developed by Otsuka in Japan, and in the United States, Otsuka America markets it jointly with Bristol-Myers Squibb.

Contents

[show]

[edit] Indications and usage

[edit] Schizophrenia

Aripiprazole has been approved by the FDA for the treatment of schizophrenia.[3]

[edit] Bipolar disorder

Aripiprazole has been approved by the FDA for the treatment of acute manic and mixed episodes, in both pediatric patients aged 10–17 and in adults.[4] Several double-blind, placebo-controlled trials support this use.[5][6][7][8] In addition, it is often used as maintenance therapy, either on its own or in conjunction with a mood stabilizer such as lithium or valproate. This use is also supported by a handful of studies.[9][10]haloperidol at reducing manic symptoms,[11][unreliable source?] and is much better tolerated by patients.[12] Aripiprazole is at least as effective as
Aripiprazole's use as a monotherapy in bipolar depression is more controversial. While a few pilot studies have found some effectiveness[13][14] (with one finding a reduction in anhedonia symptoms[15]), two large, double-blind, placebo-controlled studies found no difference between aripiprazole and placebo.[16] One study reported depression as a side effect of the drug.[17]

[edit] Major depression (Unipolar depression)

In 2007, aripiprazole was approved by the FDA for the treatment of unipolar depression when used adjunctively with an antidepressant medication.[18] It has not been FDA-approved for use as monotherapy in unipolar depression.

[edit] Autism

In 2009, the United States FDA approved Abilify to treat irritability in persons with autism.[19] It was approved on the basis of two studies that showed it reduced aggression towards others, self-injury, quickly changing moods, irritability, and temper tantrums in autistic males and females 6–17 years of age.

[edit] Cocaine dependency

Perhaps owing to its mechanism of action relating to dopamine receptors, there is some evidence to suggest that aripiprazole blocks cocaine-seeking behaviour in animal models without significantly affecting other rewarding behaviours (such as food self-administration). [20]

[edit] Pharmacology

  • D2 Partial Agonist (Ki = 0.34 nM)
  • D3 Antagonist (?)
  • 5-HT1A Partial Agonist (Ki = 0.34 nM)
  • 5-HT2A Antagonist (Ki = 0.8 nM)
  • 5-HT2C Partial Agonist (Ki = 15 nM)
  • 5-HT7 Antagonist (Ki = 39 nM)
  • SRI (?)
  • Antihistamine (Ki = 61 nM)
  • α-adrenergic antagonist (Ki = 57 nM)
  • mACh receptor antagonist (?)
Aripiprazole's mechanism of action is different from those of the other FDA-approved atypical antipsychoticsclozapine, olanzapine, quetiapine, ziprasidone, and risperidone). Rather than antagonizing the D2 receptor, aripiprazole acts as a D2 partial agonist (Ki = 0.34 nM).[21][22] Aripiprazole is also a partial agonist at the 5-HT1A receptor (Ki = 1.65 nM), and like the other atypical antipsychotics displays an antagonist profile at the 5-HT2A receptor (Ki = 0.8 nM).[23][24] It also antagonizes the 5-HT7 receptor (Ki = 39 nM) and acts as a partial agonist at the 5-HT2C receptor (Ki = 15 nM), both with high affinity. The latter action may underlie the minimal weight gain seen in the course of therapy.[25] Aripiprazole has moderate affinity for histamine (Ki = 61 nM) and α-adrenergic (Ki = 57 nM) receptors and for the serotonin transporter, and no appreciable affinity for cholinergic muscarinic receptors.[26] (e.g.,
D2 and D3 receptor occupancy levels are high, with average levels ranging between ~71% at 2 mg/day to ~96% at 40 mg/day.[27][28] Most atypical antipsychotics bind preferentially to extrastriatal receptors, but aripiprazole appears to be less preferential in this regard, as binding rates are high throughout the brain.[29]
Recently, it has been demonstrated that in 5-HT7 receptor knockout mice, aripiprazole does not reduce immobility time in the forced swim test (FST), and actually increases it.[30][31] This implicates 5-HT7amisulpride.[30][31][32] antagonism as playing a major role in aripiprazole's antidepressant effects, similarly to
Aripiprazole produces 2,3-dichlorophenylpiperazine (DCPP) as a metabolite similarly to how trazodone and nefazodone reduce to 3-chlorophenylpiperazine (mCPP) and niaprazine converts to 4-fluorophenylpiperazine[33] It is unknown whether DCPP contributes to aripiprazole's pharmacology in any way, but the possibility cannot be excluded. (pFPP).

[edit] Pharmacokinetics

Aripiprazole displays linear kinetics and has an elimination half-life of approximately 75 hours. Steady-state plasma concentrations are achieved in about 14 days. Cmax (maximum plasma concentration) is achieved 3–5 hours after oral dosing. Bioavailability of the oral tablets is about 90% and the drug undergoes extensive hepatic metabolization (dehydrogenation, hydroxylation, and N-dealkylation), principally by the enzymes CYP2D6 and CYP3A4. Its only known active metabolite is dehydro-aripiprazole, which typically accumulates to approximately 40% of the aripiprazole concentration. The parenteral drug is excreted only in traces, and its metabolites, active or not, are excreted via feces and urine.[26] When dosed daily, brain concentrations of aripiprazole will increase for a period of 10–14 days, before reaching stable constant levels. This phenomenon is due to the long half life of aripiprazole, and is responsible for many of the adverse side effects that appear after multiple days of dosing (whereas the first dose normally does not cause these side effects).

[edit] Patent status

Otsuka's US patent on aripiprazole expires on October 20, 2014;[34] however, due to a pediatric extension, a generic will not become available until at least April 20, 2015.[4] Barr Laboratories (now Teva Pharmaceuticals) initiated a patent challenge under the Hatch-Waxman Act in March 2007.[35] As of 14 August 2009, this challenge is still in court. (2009 -08-14)

[edit] Side effects

Akathisia[36], headache, unusual tiredness or weakness, nausea, vomiting, an uncomfortable feeling in the stomach, constipation, light-headedness, insomnia, sleepiness, shaking, and blurred vision.
Uncontrollable twitching or jerking movements, tremors, seizure, and weight gain. Some people may feel dizzy, especially when getting up from a lying or sitting position, or may experience a fast heart rate.
Neuroleptic malignant syndrome (Combination of fever, muscle stiffness, faster breathing, sweating, reduced consciousness, and sudden change in blood pressure and heart rate.)
Aripiprazole also causes sexual dysfunction.
Tardive dyskinesia (As with all antipsychotic medication, patients using aripiprazole may develop the permanent neurological disorder tardive dyskinesia.[37][38][39])
Stroke (While taking aripiprazole some elderly patients with dementia have suffered from stroke or 'mini' stroke.)
Other elderly patients may experience high blood sugar or the onset or worsening of diabetes.
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.

[edit] Overdosage

Children or adults who ingested acute overdoses have usually manifested central nervous system depression ranging from mild sedation to coma; serum concentrations of aripiprazole and dehydroaripiprazole in these patients were elevated by up to 3-4 fold over normal therapeutic levels, yet no deaths have yet been recorded.[40]

[edit] Drug interactions

Aripiprazole is a substrate of CYP2D6 and CYP3A4. Coadministration with medications that inhibit (e.g. paroxetine, fluoxetine) or induce (e.g. carbamazepine) these metabolic enzymes are known to increase and decrease, respectively, plasma levels of aripiprazole.[41] As such, anyone taking Abilify should be aware that their dosage of Abilify may need to be decreased.
Aripiprazole may change the subjective effects of alcohol. One study[42] found that aripiprazole increased the sedative effect and reduced the sense of euphoria normally associated with alcohol consumption. However, another alcohol study[43] found that there was no difference in subjective effect between a placebo group and a group taking aripiprazole.

[edit] Dosage forms

  • Intramuscular injection, solution: 7.5 mg/mL (1.3 mL)
  • Solution, oral: 1 mg/mL (150 mL) [contains propylene glycol, sucrose 400 mg/mL, and fructose 200 mg/mL; orange cream flavor]
  • Tablet: 2 mg, 5 mg, 10 mg, 15 mg, 20 mg, 30 mg
  • Tablet, orally disintegrating: 10 mg [contains phenylalanine 1.12 mg; creme de vanilla flavor]; 15 mg [contains phenylalanine 1.68 mg; creme de vanilla flavor]

[edit] Synthesis

Aripiprazole synth.png
U.S. Patent 5,006,528


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