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Statements

Subject Item: n2:DB00715
rdf:type: n5:Drug
n5:description: Paroxetine hydrochloride and paroxetine mesylate belong to a class of antidepressant agents known as selective serotonin-reuptake inhibitors (SSRIs). Despite distinct structural differences between compounds in this class, SSRIs possess similar pharmacological activity. As with other antidepressant agents, several weeks of therapy may be required before a clinical effect is seen. SSRIs are potent inhibitors of neuronal serotonin reuptake. They have little to no effect on norepinephrine or dopamine reuptake and do not antagonize α- or β-adrenergic, dopamine D2 or histamine H1 receptors. During acute use, SSRIs block serotonin reuptake and increase serotonin stimulation of somatodendritic 5-HT1A and terminal autoreceptors. Chronic use leads to desensitization of somatodendritic 5-HT1A and terminal autoreceptors. The overall clinical effect of increased mood and decreased anxiety is thought to be due to adaptive changes in neuronal function that leads to enhanced serotonergic neurotransmission. Side effects include dry mouth, nausea, dizziness, drowsiness, sexual dysfunction and headache (see Toxicity section below for a complete listing of side effects). Side effects generally occur during the first two weeks of therapy and are usually less severe and frequent than those observed with tricyclic antidepressants. Paroxetine hydrochloride and mesylate are considered therapeutic alternatives rather than generic equivalents by the US Food and Drug Administration (FDA); both agents contain the same active moiety (i.e. paroxetine), but are formulated as different salt forms. Clinical studies establishing the efficacy of paroxetine in various conditions were performed using paroxetine hydrochloride. Since both agents contain the same active moiety, the clinical efficacy of both agents is thought to be similar. Paroxetine may be used to treat major depressive disorder (MDD), panic disorder with or without agoraphobia, obsessive-compulsive disorder (OCD), social anxiety disorder (social phobia), generalized anxiety disorder (GAD), post-traumatic stress disorder (PTSD) and premenstrual dysphoric disorder (PMDD). Paroxetine has the most evidence supporting its use for anxiety-related disorders of the SSRIs. It has the greatest anticholinergic activity of the agents in this class and compared to other SSRIs, paroxetine may cause greater weight gain, sexual dysfunction, sedation and constipation.
n5:dosage: n7:271B4C5A-363D-11E5-9242-09173F13E4C5 n7:271B4C5B-363D-11E5-9242-09173F13E4C5 n7:271B4C5C-363D-11E5-9242-09173F13E4C5 n7:271B4C5D-363D-11E5-9242-09173F13E4C5 n7:271B4C5E-363D-11E5-9242-09173F13E4C5 n7:271B4C5F-363D-11E5-9242-09173F13E4C5 n7:271B4C60-363D-11E5-9242-09173F13E4C5 n7:271B4C61-363D-11E5-9242-09173F13E4C5 n7:271B4C62-363D-11E5-9242-09173F13E4C5 n7:271B4C63-363D-11E5-9242-09173F13E4C5 n7:271B4C64-363D-11E5-9242-09173F13E4C5 n7:271B4C65-363D-11E5-9242-09173F13E4C5 n7:271B4C66-363D-11E5-9242-09173F13E4C5
n5:generalReferences: # Baldwin DS, Anderson IM, Nutt DJ, Bandelow B, Bond A, Davidson JR, den Boer JA, Fineberg NA, Knapp M, Scott J, Wittchen HU: Evidence-based guidelines for the pharmacological treatment of anxiety disorders: recommendations from the British Association for Psychopharmacology. J Psychopharmacol. 2005 Nov;19(6):567-96. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16272179 # Baldwin D, Bobes J, Stein DJ, Scharwachter I, Faure M: Paroxetine in social phobia/social anxiety disorder. Randomised, double-blind, placebo-controlled study. Paroxetine Study Group. Br J Psychiatry. 1999 Aug;175:120-6. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/10627793 # Yonkers KA, Gullion C, Williams A, Novak K, Rush AJ: Paroxetine as a treatment for premenstrual dysphoric disorder. J Clin Psychopharmacol. 1996 Feb;16(1):3-8. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/8834412 # Waldinger MD, Hengeveld MW, Zwinderman AH, Olivier B: Effect of SSRI antidepressants on ejaculation: a double-blind, randomized, placebo-controlled study with fluoxetine, fluvoxamine, paroxetine, and sertraline. J Clin Psychopharmacol. 1998 Aug;18(4):274-81. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/9690692 # Waldinger MD, Zwinderman AH, Olivier B: SSRIs and ejaculation: a double-blind, randomized, fixed-dose study with paroxetine and citalopram. J Clin Psychopharmacol. 2001 Dec;21(6):556-60. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/11763001
n5:group: investigational approved
n5:halfLife: 21-24 hours
n5:indication: Labeled indications include: major depressive disorder (MDD), panic disorder with or without agoraphobia, obsessive-compulsive disorder (OCD), social anxiety disorder (social phobia), generalized anxiety disorder (GAD), post-traumatic stress disorder (PTSD), and premenstrual dysphoric disorder (PMDD). Unlabeled indications include: eating disorders, impulse control disorders, vasomotor symptoms of menopause, obsessive-compulsive disorder (OCD) in children, and mild dementia-associated agitation in nonpsychotic individuals. Brisdelle, which consists of paroxetine mesylate is indicated for the treatment of moderate to severe vasomotor symptoms (like hot flashes) associated with menopause.
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owl:sameAs: n20:DB00715 n31:DB00715
dcterms:title: Paroxetine
adms:identifier: n12:22416 n13:7936 n14:PA450801 n15:43815 n16:D02362 n17:0029-3210-13 n18:C07415 n21:39888 n22:DB00715 n23:46504821 n25:Paroxetine
n5:mechanismOfAction: Paroxetine is a potent and highly selective inhibitor of neuronal serotonin reuptake. Paroxetine likely inhibits the reuptake of serotonin at the neuronal membrane, enhances serotonergic neurotransmission by reducing turnover of the neurotransmitter, therefore it prolongs its activity at synaptic receptor sites and potentiates 5-HT in the CNS; paroxetine is more potent than both sertraline and fluoxetine in its ability to inhibit 5-HT reuptake. Compared to the tricyclic antidepressants, SSRIs have dramatically decreased binding to histamine, acetylcholine, and norepinephrine receptors. The mechanism of action for the treatment of vasomotor symptoms is unknown.
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n5:patent: n6:6703408 n6:2445678 n6:2168829 n6:5789449
n5:routeOfElimination: Approximately 64% of a 30 mg oral solution of paroxetine was excreted in the urine with 2% as the parent compound and 62% as metabolites. Approximately 36% of the dose was excreted in the feces (via bile), mostly as metabolites and less than 1% as parent compound.
n5:synonym: Paroxetine Paroxetina (-)-(3S,4R)-4-(P-Fluorophenyl)-3-((3,4-(methylenedioxy)phenoxy)methyl)piperidine (3S-trans)-3-((1,3-Benzodioxol-5-yloxy)methyl)-4-(4-fluorophenyl)piperidine Paroxetinum
n5:toxicity: LD50=500mg/kg (orally in mice). Symptoms of overdose include: coma, dizziness, drowsiness, facial flushing, nausea, sweating, tremor, vomiting. Side effects include: nervous system effects such as asthenia, somnolence, dizziness, insomnia, tremor, and nervousness; GI effects such as nausea, decreased appetite, constipation, diarrhea, and dry mouth; impotence, ejaculatory dysfunction (principally ejaculatory delay), and other male genital disorders; female genital disorders (principally anorgasmia or difficulty reaching climax/orgasm); and sweating. Discontinuation syndrome may occur with abrupt withdrawal. Symptoms of discontinuation syndrome include flu-like symptoms, insomnia, nausea, imbalance, sensory changes, and hyperactivity.
n5:volumeOfDistribution: 3.1-28 L/kg observed in animal studies. Paroxetine distributes throughout the body, including the central nervous system, with only 1% remaining in the plasma.
n27:hasAHFSCode: n32:28-16-04-20
n5:foodInteraction: Take without regard to meals. Avoid alcohol.
n5:proteinBinding: ~ 95% bound to plasma proteins.
n5:salt
n5:synthesisReference: Charles M. Zepp, Yun Gao, Donald L. Heefner, "Method of preparing optically pure precursors of paroxetine." U.S. Patent US5258517, issued January, 1976.
n29:hasConcept: n30:M0026386
foaf:page: n4:paroxetine.html n26:parox.htm
n5:IUPAC-Name: n10:271B4C6B-363D-11E5-9242-09173F13E4C5
n5:InChI: n10:271B4C71-363D-11E5-9242-09173F13E4C5
n5:Molecular-Formula: n10:271B4C70-363D-11E5-9242-09173F13E4C5
n5:Molecular-Weight: n10:271B4C6D-363D-11E5-9242-09173F13E4C5
n5:Monoisotopic-Weight: n10:271B4C6E-363D-11E5-9242-09173F13E4C5
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n5:Water-Solubility: n10:271B4C69-363D-11E5-9242-09173F13E4C5 n10:271B4C80-363D-11E5-9242-09173F13E4C5
n5:logP: n10:271B4C6A-363D-11E5-9242-09173F13E4C5 n10:271B4C67-363D-11E5-9242-09173F13E4C5 n10:271B4C82-363D-11E5-9242-09173F13E4C5
n5:logS: n10:271B4C68-363D-11E5-9242-09173F13E4C5
n27:hasATCCode: n28:N06AB05
n5:H-Bond-Acceptor-Count: n10:271B4C77-363D-11E5-9242-09173F13E4C5
n5:H-Bond-Donor-Count: n10:271B4C78-363D-11E5-9242-09173F13E4C5
n5:InChIKey: n10:271B4C72-363D-11E5-9242-09173F13E4C5
n5:Polar-Surface-Area--PSA-: n10:271B4C73-363D-11E5-9242-09173F13E4C5
n5:Polarizability: n10:271B4C75-363D-11E5-9242-09173F13E4C5
n5:Refractivity: n10:271B4C74-363D-11E5-9242-09173F13E4C5
n5:Rotatable-Bond-Count: n10:271B4C76-363D-11E5-9242-09173F13E4C5
n5:absorption: Paroxetine hydrochloride is slowly, but completely absorbed following oral administration. Paroxetine mesylate salt is also completely absorbed after oral dosing. The oral bioavailability appears to be low due to extensive first-pass metabolism. Paroxetine hydrochloride oral tablets and suspension are reportedly bioequivalent. Absorption of either salt form is not substantially affected by food. Peak concentrations of Brisbelle (mesylate salt) were reached at 6 hours (3 to 8 hours range). Steady state Cmax was 13.10 ng/mL. The steady state AUC (0-last) was 237 hr*ng/mL. Paroxetine mesylate generally follows non-linear pharmacokinetics because CYP2D6, the enzyme that is part responisible for paroxetine metabolism, is readily saturable.
n5:affectedOrganism: Humans and other mammals
n5:casRegistryNumber: 61869-08-7
n5:category
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