PAROXETINE- paroxetine hydrochloride hemihydrate tablet, film coated, extended release
Lupin Pharmaceuticals, Inc.
Suicidality and Antidepressant Drugs
Antidepressants increased the risk compared to placebo of suicidal thinking and behavior (suicidality) in children, adolescents, and young adults in short-term studies of major depressive disorder (MDD) and other psychiatric disorders. Anyone considering the use of paroxetine hydrochloride or any other antidepressant in a child, adolescent, or young adult must balance this risk with the clinical need. Short-term studies did not show an increase in the risk of suicidality with antidepressants compared to placebo in adults beyond age 24; there was a reduction in risk with antidepressants compared to placebo in adults aged 65 and older. Depression and certain other psychiatric disorders are themselves associated with increases in the risk of suicide. Patients of all ages who are started on antidepressant therapy should be monitored appropriately and observed closely for clinical worsening, suicidality, or unusual changes in behavior. Families and caregivers should be advised of the need for close observation and communication with the prescriber. Paroxetine hydrochloride is not approved for use in pediatric patients (see WARNINGS: Clinical Worsening and Suicide Risk, PRECAUTIONS: Information for Patients, and PRECAUTIONS: Pediatric Use).
DESCRIPTION
Paroxetine hydrochloride hemihydrate USP is an orally administered psychotropic drug with a chemical structure unrelated to other selective serotonin reuptake inhibitors or to tricyclic, tetracyclic, or other available antidepressant or antipanic agents. It is the hydrochloride salt of a phenylpiperidine compound identified chemically as (-)-(3S , 4R)-4-(p-Fluorophenyl)-3-([(3,4 methylenedioxy) phenoxy]methyl)piperidine hydrochloride hemihydrate and has the empirical formula of C19 H21 ClFNO3 �1/2H2 O. The molecular weight is 374.83.
CLINICAL PHARMACOLOGY
Pharmacodynamics: The efficacy of paroxetine in the treatment of major depressive disorder, panic disorder, social anxiety disorder, and premenstrual dysphoric disorder (PMDD) is presumed to be linked to potentiation of serotonergic activity in the central nervous system resulting from inhibition of neuronal reuptake of serotonin (5-hydroxy-tryptamine, 5-HT). Studies at clinically relevant doses in humans have demonstrated that paroxetine blocks the uptake of serotonin into human platelets. In vitro studies in animals also suggest that paroxetine is a potent and highly selective inhibitor of neuronal serotonin reuptake and has only very weak effects on norepinephrine and dopamine neuronal reuptake. In vitro radioligand binding studies indicate that paroxetine has little affinity for muscarinic, alpha1 -, alpha2 -, beta-adrenergic-, dopamine (D2 )-, 5-HT1 -, 5-HT2 -, and histamine (H1 )-receptors; antagonism of muscarinic, histaminergic, and alpha1 -adrenergic receptors has been associated with various anticholinergic, sedative, and cardiovascular effects for other psychotropic drugs.
INDICATIONS AND USAGE
Major Depressive Disorder: Paroxetine extended-release tablets are indicated for the treatment of major depressive disorder.
The efficacy of paroxetine extended-release tablets in the treatment of a major depressive episode was established in two 12-week controlled trials of outpatients whose diagnoses corresponded to the DSM-IV category of major depressive disorder.
Panic Disorder: Paroxetine extended-release tablets are indicated for the treatment of panic disorder, with or without agoraphobia, as defined in DSM-IV. Panic disorder is characterized by the occurrence of unexpected panic attacks and associated concern about having additional attacks, worry about the implications or consequences of the attacks, and/or a significant change in behavior related to the attacks.
Social Anxiety Disorder: Paroxetine extended-release tablets are indicated for the treatment of social anxiety disorder, also known as social phobia, as defined in DSM-IV (300.23). Social anxiety disorder is characterized by a marked and persistent fear of 1 or more social or performance situations in which the person is exposed to unfamiliar people or to possible scrutiny by others.
Premenstrual Dysphoric Disorder: Paroxetine extended-release tablets are indicated for the treatment of PMDD.
The efficacy of paroxetine extended-release tablets in the treatment of PMDD has been established in 3 placebo-controlled trial.