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QuickView for Paroxetine (compound)

Name: Paroxetine
PubChem Compound ID: 10066032
Description: A serotonin uptake inhibitor that is effective in the treatment of depression.
Molecular formula: C20H22FNO3
Molecular weight: 343.392 g/mol
Name: Paroxetine
Name (isomeric): DB00715
Drug Type: small molecule
Description: A serotonin uptake inhibitor that is effective in the treatment of depression.
Paroxetina [INN-Spanish]; Paroxetinum [INN-Latin]; Paroxetine Hcl
Brand: Pexeva, Paxil, Aropax, Seroxat, Seroxat CR, Paxil CR
Category: Antidepressants, Antidepressive Agents, Second-Generation, Selective Serotonin Reuptake Inhibitors (SSRIs), Serotonin Uptake Inhibitors
CAS number: 61869-08-7
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.
Paroxetine, an antidepressant drug of the selective serotonin reuptake inhibitor (SSRI) type, has no active metabolites and has the highest specificity for serotonin receptors of all the SSRIs. It is used to treat depression resistant to other antidepressants, depression complicated by anxiety, panic disorder, social and general anxiety disorder, o...
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Mechanism of Action:
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; paro...
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Absorption: Paroxetine hydrochloride is slowly, but completely absorbed following oral administration. The oral bioavailability appears to be low due to extensive first-pass metabolism. Paroxetine hydrochloride oral tablets and suspension are reportedly bioequivalent. Paroxetine mesylate is completely following oral administration. Absorption of either salt form is not substantially affected by food.
Protein binding: ~ 95% bound to plasma proteins.
Biotransformation: Paroxetine is extensively metabolized, likely in the liver. The main metabolites are polar and conjugated products of oxidation and methylation, which are readily eliminated by the body. The predominant metabolites are glucuronic acid and sulfate conjugates. Paroxetine metabolites do not possess significant pharmacologic activity (less than 2% that of parent compound). Paroxetine is metabolized by cytochrome P450 (CYP) 2D6. Enzyme saturation appears to account for the nonlinear pharmacokinetics observed with increasing dose and duration of therapy.
Route of elimination: Paroxetine is extensively metabolized and the metabolites are primarily excreted in the urine and to some extent in the feces.
Half Life: 21-24 hours
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.
Affected organisms: Humans and other mammals
Food interaction:
Take without regard to meals. Avoid alcohol.
Drug interaction:
PhenelzinePossible severe adverse reaction with this combination
AlmotriptanIncreased risk of CNS adverse effects
PropranololThe SSRI, paroxetine, may increase the bradycardic effect of the beta-blocker, propranolol.
DextromethorphanCombination associated with possible serotoninergic syndrome
TranylcypromineIncreased risk of serotonin syndrome. Concomitant therapy should be avoided. A significant washout period, dependent on the half-lives of the agents, should be employed between therapies.
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