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Encyclopedia > Atomoxetine
Atomoxetine
Systematic (IUPAC) name
(3R)-N-methyl-3-(2-methylphenoxy)-3-phenyl-propan-1-amine
Identifiers
CAS number 83015-26-3
ATC code N06BA09
PubChem 54841
DrugBank APRD00614
Chemical data
Formula C17H21NO 
Mol. mass 255.355 g/mol
291.820 g/mol (hydrochloride)
Pharmacokinetic data
Bioavailability 63 to 94%
Protein binding 40%
Metabolism Hepatic, via CYP2D6
Half life 5 hours
Excretion Renal (>80%) and fecal (<17%)
Therapeutic considerations
Pregnancy cat.

B3(AU) C(US) Image File history File links This is a lossless scalable vector image. ... Image File history File links No higher resolution available. ... IUPAC nomenclature is a system of naming chemical compounds and of describing the science of chemistry in general. ... CAS registry numbers are unique numerical identifiers for chemical compounds, polymers, biological sequences, mixtures and alloys. ... The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs. ... A section of the Anatomical Therapeutic Chemical Classification System containing Psychoanaleptics. ... PubChem is a database of chemical molecules. ... The DrugBank database available at the University of Alberta is a unique bioinformatics and cheminformatics resource that combines detailed drug (i. ... A chemical formula is a concise way of expressing information about the atoms that constitute a particular chemical compound. ... For other uses, see Carbon (disambiguation). ... This article is about the chemistry of hydrogen. ... General Name, symbol, number nitrogen, N, 7 Chemical series nonmetals Group, period, block 15, 2, p Appearance colorless gas Standard atomic weight 14. ... General Name, symbol, number oxygen, O, 8 Chemical series nonmetals, chalcogens Group, period, block 16, 2, p Appearance colorless (gas) pale blue (liquid) Standard atomic weight 15. ... The molecular mass (abbreviated Mr) of a substance, formerly also called molecular weight and abbreviated as MW, is the mass of one molecule of that substance, relative to the unified atomic mass unit u (equal to 1/12 the mass of one atom of carbon-12). ... In pharmacology, bioavailability is used to describe the fraction of an administered dose of unchanged drug that reaches the systemic circulation, one of the principal pharmacokinetic properties of drugs. ... A drugs efficacy may be affected by the degree to which it binds to the proteins within blood plasma. ... Drug metabolism is the metabolism of drugs, their biochemical modification or degradation, usually through specialized enzymatic systems. ... The liver is an organ in vertebrates including humans. ... Cytochrome P450 2D6 (CYP2D6), a member of the cytochrome P450 mixed-function oxidase system, is one of the most important enzymes involved in the metabolism of xenobiotics in the body. ... The biological half-life of a substance is the time required for half of that substance to be removed from an organism by either a physical or a chemical process. ... The kidneys are important excretory organs in vertebrates. ... The kidneys are the organs that filter wastes (such as urea) from the blood and excrete them, along with water, as urine. ... The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical, if it is used as directed by the mother during pregnancy. ... For other uses, see Australia (disambiguation). ... For other uses of terms redirecting here, see US (disambiguation), USA (disambiguation), and United States (disambiguation) Motto In God We Trust(since 1956) (From Many, One; Latin, traditional) Anthem The Star-Spangled Banner Capital Washington, D.C. Largest city New York City National language English (de facto)1 Demonym American...

Legal status

POM(UK) Unscheduled (U.S.) The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction. ... Zoloft, an antidepressant and antianxiety medication A prescription drug is a licensed medicine that is regulated by legislation to require a prescription before it can be obtained. ...

Routes Oral (Capsules: 10, 18, 25, 40, 60, 80 and 100 mg)

Atomoxetine is the first non-stimulant drug approved for the treatment of attention-deficit hyperactivity disorder (ADHD). It is sold in the form of the hydrochloride salt of atomoxetine. This chemical is manufactured and marketed under the brand name Strattera® by Eli Lilly and Company and as a generic Attentin by Torrent Pharmaceuticals. There is currently no generic available within the United States due to patent restrictions. 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. ... Stimulants are drugs that temporarily increase alertness and wakefulness. ... Attention-Deficit/Hyperactivity Disorder (ADHD) previously known as Attention Deficit Disorder (ADD), is generally considered to be a developmental disorder, largely neurological in nature, affecting about 5% of the worlds population. ... In chemistry, hydrochlorides are salts resulting, or regarded as resulting, from the reaction of hydrochloric acid with an organic base (mostly amines). ... Eli Lilly and Company (NYSE: LLY) is a global pharmaceutical company and one of the worlds largest corporations. ... A generic drug (pl. ... Torrent Pharmaceuticals Ltd. ... For other uses, see Patent (disambiguation). ...


Atomoxetine is classified as a norepinephrine reuptake inhibitor (Noradrenaline reuptake inhibitor), and is approved for use in children, adolescents, and adults. However, its efficacy has not been studied in children under six years old. Its advantage over stimulants for the treatment of ADHD is that it has less abuse potential than stimulants, is not scheduled as a controlled substance and has proven in clinical trials to offer 24 hour coverage of symptoms associated with ADHD in adults and children. Norepinephrine reuptake inhibitors (NRIs) are compounds that increase amounts of the neurotransmitter norepinephrine in the brain by inhibiting its reuptake at synapses. ... In health care, including medicine, a clinical trial (synonyms: clinical studies, research protocols, medical research) is a process in which a medicine or other medical treatment is tested for its safety and effectiveness, often in comparison to existing treatments. ...


Strattera was originally intended to be a new antidepressant drug; however, in clinical trials, no such benefits could be proven. Since norepinephrine is believed to play a role in ADHD, Strattera was tested and subsequently approved as an ADHD treatment. Prozac, a selective serotonin reuptake inhibitor (SSRI) Serotonin-norepinephrine reuptake inhibitor, Venlafaxine An antidepressant, is a psychiatric medication or other substance (nutrient or herb) used for alleviating depression or dysthymia (milder depression). ... Norepinephrine (INN)(abbr. ...

Contents

Nomenclature

Atomoxetine was originally known as "tomoxetine". However, the U.S. Food and Drug Administration (FDA) requested the name be changed because, in their opinion, the similarity of "tomoxetine" to "tamoxifen" (a breast cancer drug) could lead to dispensing errors at pharmacies. “FDA” redirects here. ... Tamoxifen is an orally active selective estrogen receptor modulator (SERM) which is used in the treatment of breast cancer and is currently the worlds largest selling drug for this indication. ...


Chemistry and composition

Atomoxetine is designated chemically as (-)-N-methyl-3-phenyl-3-(o-tolyloxy)-propylamine hydrochloride, and has a molecular mass of 291.82. It has a solubility of 27.8 mg/mL in water. Atomoxetine is a white solid that exists as a granular powder inside the capsule, along with pre-gelatinized starch and dimethicone. The capsule shells contain gelatin, sodium lauryl sulfate, FD&C Blue No. 2, synthetic yellow iron oxide, titanium dioxide, red iron oxide, edible black ink, and trace amounts of other inactive ingredients. The molecular mass (abbreviated Mr) of a substance, formerly also called molecular weight and abbreviated as MW, is the mass of one molecule of that substance, relative to the unified atomic mass unit u (equal to 1/12 the mass of one atom of carbon-12). ... Solubility is a chemical property referring to the ability for a given substance, the solute, to dissolve in a solvent. ... Modified starch is a food additive which is prepared by treating starch or starch granules, causing the starch to be partially degraded. ... Polydimethylsiloxane (PDMS) is the most widely used silicon-based organic polymer, and is particularly known for its unusual rheological (or flow) properties. ... For the art collective, see Gelitin. ... Sodium dodecyl sulfate (SDS or NaDS) (CH3(CH2)11OSO3Na) (FW 288. ... Indigo dye indigo molecule Indigo dye is an important dyestuff with a distinctive blue color (see indigo). ... Flash point non-flammable Related Compounds Other cations Titanium(II) oxide Titanium(III) oxide Titanium(III,IV) oxide Zirconium dioxide Hafnium dioxide Except where noted otherwise, data are given for materials in their standard state (at 25 Â°C, 100 kPa) Infobox disclaimer and references Titanium dioxide, also known as titanium... Iron(III) oxide — also known as ferric oxide, Hematite, red iron oxide, synthetic maghemite, colcothar, or simply rust — is one of several oxide compounds of iron, and has paramagnetic properties. ...


Side effects

The most common side effect in adults is drowsiness. This can be counteracted in some patients by measures as simple as a cup of coffee, or breathing exercises, while others become exhausted a short while after taking the pills, and can sleep for up to 10+ hours. Some patients tend to feel lightheaded, dizzy, or "buzzed" as a minor side effect along with the drowsiness. To diminish these side effects, which can interfere with daytime work, study, etc., dosing time is sometimes changed to just before bed; as Strattera is long-acting, it does not "wear off" overnight. Mild hallucinations can be experienced under high doses (300mg).


Also very common is digestive discomfort, such as heartburn. The most common side effects in children and adolescents (and, after drowsiness, in adults) are upset stomach, sporadic nausea, and sudden vomiting. The medication's tendency to decrease appetite may contribute to this problem, as taking Strattera on an empty stomach is usually discouraged; it can also be a problem in itself, in the form of hunger pangs. Consumption of dairy products can cause further upset.


A significant minority of adult male patients taking Strattera suffer minor to severe sexual side effects, including erectile dysfunction, retrograde ejaculation, painful orgasm, and the decoupling of orgasm from ejaculation, wherein ejaculation takes place up to ten seconds before or after orgasm. Erectile dysfunction (ED) or impotence is a sexual dysfunction characterized by the inability to develop or maintain an erection of the penis. ... In males, retrograde ejaculation occurs when the fluid to be ejaculated, which would normally exit via the urethra, is redirected towards the urinary bladder. ... // An orgasm (sexual climax) is the conclusion of the plateau phase of the sexual response cycle, and is experienced by both males and females. ... Ejaculation is the ejecting of semen from the penis, and is usually accompanied by orgasm. ...


Occasionally after prolonged use some teenagers have experienced slow onset mild depression while using Strattera [citation needed]


Two confirmed cases of liver injury have been reported by Eli Lilly and Company out of approximately two million prescriptions written. In both cases upon discontinuation of atomoxetine, patients' liver functions returned to normal. Eli Lilly and Company (NYSE: LLY) is a global pharmaceutical company and one of the worlds largest corporations. ...


Discontinuation adverse effects

Further information: Chemical synapse

The central nervous system (CNS) adapts to the presence of psychoactive drugs. Such adaptation commonly involves the readjustment of neuroreceptors to compensate for the acute pharmacological action of the medication. This adaptation theory also explains why withdrawal symptoms and signs can occur on the discontinuation of such medications as clearance of drug can occur at a rate faster than the brain can readjust to the absence of medication. Hence, pharmacodynamic and pharmacokinetic factors contribute to the risk of a withdrawal syndrome. Illustration of the major elements in a prototypical synapse. ... Pharmacodynamics is the study of the biochemical and physiological effects of drugs and the mechanisms of drug action and the relationship between drug concentration and effect. ... Pharmacokinetics is a branch of pharmacology dedicated to the study of the time course of substances and their relationship with an organism or system. ...


Psychiatric reactions

In September 2005, Strattera was determined to increase risk of suicidal thoughts among children and adolescents; one attempted suicide and five cases of suicidal thoughts were reported out of 1,357 young patients taking Strattera, while none was reported out of a control group of 851 taking placebos. [1], [2]. The FDA has required that black box warnings be placed on all antidepressant medications warning they may result in increased risk of suicidal tendencies in children and adolescents; therefore, Strattera bears such a warning. It has been suggested that this article or section be merged with Black_Box_Warning. ...


In less than three years on the market 10,988 adverse "psychiatric reactions" have been reported to Eli Lilly for the ADHD drug Strattera, according to the British Medicines and Healthcare products Regulatory Agency (MHRA), January 2006.


Potential for abuse

To date, the potential for abuse of Strattera has not been exhaustively researched. The two studies that have been performed suggest that atomoxetine has a low to moderate risk for abuse, since it has a long titration time (meaning that it may have no effect on the user unless they've been taking it regularly for days) and does not produce strong stimulating effects like most other ADHD medications (which are usually dopamine reuptake inhibitors). Monkeys will not self-administer atomoxetine at the doses tested (Gasior et al, Neuropharm 30:758, 2005; Wee & Woolverton, Drug Alcohol Depend 75:271, 2004). However, rats, pigeons and monkeys trained to distinguish cocaine or methamphetamine from saline indicate that atomoxetine produces effects indistinguishable from low doses of cocaine or methamphetamine, but not at all like high doses of cocaine (Spealman, JPET 271:53, 1995; Sasaki et al., Psychopharm 120:303, 1995). No place preference studies have been conducted with atomoxetine. It may be abused if taken in larger amounts than the daily dosage, the effects may be compared to those experienced on amphedemines that are also used for ADHD medication. This does not cite any references or sources. ... Cocaine is a crystalline tropane alkaloid that is obtained from the leaves of the coca plant. ... This article is about the psychostimulant, d-methamphetamine. ...


Off-label uses

While depression is most commonly associated with the neurotransmitter serotonin, an imbalance of other neurotransmitters may also result in clinical depression. To that end, atomoxetine, which inhibits the reuptake of norepinephrine, was originally explored by Eli Lilly as a treatment for depression, but did not show a benefit to risk ratio in trials. Failed clinical trials are not submitted to drug regulatory agencies and are considered trade secrets. Subsequently, Lilly then chose to pursue an ADHD treatment route for atomoxetine. Many patients have seen a pronounced anti-depressive effect in conjunction with other antidepressants. More study is needed to understand the full pharmacodynamics.[1][2][3][4] Serotonin (pronounced ) (5-hydroxytryptamine, or 5-HT) is a monoamine neurotransmitter synthesized in serotonergic neurons in the central nervous system (CNS) and enterochromaffin cells in the gastrointestinal tract of animals including humans. ... Norepinephrine (INN)(abbr. ...


Experimental uses

A small (40 people), 10-week, double-blind clinical trial was reported in the Journal of Clinical Psychiatry on the effectiveness of atomoxetine for treating binge eating disorder. The results of the trial was that atomoxetine was "associated with a significantly greater rate of reduction in binge-eating episode frequency, weight, [and] body mass index." The average daily dose given was 106 mg/day. The authors concluded that atomoxetine is effective for short term treatment of binge eating disorder.[5] The references in this article would be clearer with a different and/or consistent style of citation, footnoting or external linking. ...


A preliminary 12-week, randomized, double-blind, placebo-controlled trial was conducted at Duke University Medical Center which studied the effectiveness of atomoxetine on adult obese women. The study included 30 obese women with an average body mass index of 36.1. Fifteen women were given atomoxetine therapy starting at 25 mg/day with a gradual increase to 100 mg/day over 1 week. Fifteen women were given a placebo with identical dosing. By the end of the trial, the atomoxetine group lost an average of 3.6 kg (3.7% of their body mass) vs a 0.1 kg gain in the placebo group (0.2% gain). Three participants in the atomoxetine group and none in the placebo group lost greater than 5% of their mass.[6] This page is a candidate for speedy deletion because: it contains no encyclopedic content If you disagree with its speedy deletion, please explain why on its talk page or at Wikipedia:Speedy deletions. ...


References

  1. ^ Biederman J, Spencer TJ (March, 2006). "Atomoxetine and adult attention-deficit/hyperactivity disorder: the effects of comorbidity.". 
  2. ^ Adli M, Pilhatsch MK (March, 2006). "Augmentation with atomoxetine in treatment-resistant depression with psychotic features. A case report.". 
  3. ^ Price LH, Carpenter LL (Oct, 2005). "Augmentation with open-label atomoxetine for partial or nonresponse to antidepressants.". 
  4. ^ Biederman, J, Kratochvil CJ (Sept, 2005). "Atomoxetine alone or combined with fluoxetine for treating ADHD with comorbid depressive or anxiety symptoms.". 
  5. ^ McElroy, Susan (2007), "Atomoxetine in the Treatment of Binge-Eating Disorder: A Randomized Placebo-Controlled Trial", Journal of Clinical Psychiatry 68 (3): 390–398, PMID 17388708, <http://www.psychiatrist.com.prxy3.ursus.maine.edu/privatepdf/2007/v68n03/v68n0306.pdf>
  6. ^ Gadde, K.M. (July 2006), "Atomoxetine for weight reduction in obese women: a preliminary randomised controlled trial", International Journal of Obesity 30 (7): 1138–1142, PMID 16418753

External links


  Results from FactBites:
 
atomoxetine: Information From Answers.com (1854 words)
Atomoxetine is a prescription drug that is used to treat symptoms of impulsivity, inattentiveness, and hyperactivity, which are hallmark features of attention deficit hyperactivity disorder (ADHD).
Atomoxetine should be initiated at a total daily dose of 1 mg/lb (0.5 mg/kg) in children that weigh less than 150 lb (70 kg).
Atomoxetine is classified as a norepinephrine reuptake inhibitor, and is approved for use in children, adolescents, and adults.
  More results at FactBites »

 
 

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