| Drug ID: | D208 |
| Drug Name: | Paroxetine |
| Synonyms: |
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| Type: | small molecule |
| DrugBank ID: |
DB00715
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| DrugBank Description: |
Paroxetine is a selective serotonin reuptake inhibitor (SSRI) drug commonly known as Paxil. It has a variety of uses, including the treatment of anxiety disorders, major depression, posttraumatic stress disorder, and symptoms of menopause, among others.[T653] It was approved by the FDA in the early 1990s and marketed by SmithKline Beecham.[L7712,L7715] A unique feature of this drug is that it is highly potent and selective in its inhibition of serotonin reuptake and has little effect on other neurotransmitters.[A31914] Because of its potent inhibition of serotonin reuptake, paroxetine is more likely to cause withdrawal effects upon cessation. Paroxetine is well tolerated in most patients with a similar adverse effect profile to other members of its drug class.[A31914] The controlled release formulation was designed to decrease the likelihood of nausea that is sometimes associated with paroxetine.[L7700,L7742]
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| PubChem ID: |
43815
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| CasNo: |
61869-08-7
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| Repositioning for NAFLD: |
Yes
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| SMILES: |
FC1=CC=C(C=C1)[C@@H]1CCNC[C@H]1COC1=CC2=C(OCO2)C=C1
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| Structure: |
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| InChiKey: |
AHOUBRCZNHFOSL-YOEHRIQHSA-N
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| Molecular Weight: |
329.3654
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| DrugBank Targets: |
Sodium-dependent serotonin transporter; Sodium-dependent noradrenaline transporter; 5-hydroxytryptamine receptor 2A; Alpha-1 adrenergic receptors; Alpha-2 adrenergic receptors; Beta adrenergic receptor; Dopamine D2 receptor; Histamine H1 receptor; Serotonin Receptors; Muscarinic acetylcholine receptor; 5-hydroxytryptamine receptor 2B; D(1) dopamine receptor
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| DrugBank MoA: |
Paroxetine enhances serotonergic activity via the inhibition presynaptic reuptake of serotonin by the serotonin (SERT) receptor.[A5492,A181772] This inhibition raises the level of serotonin in the synaptic cleft, relieving various symptoms. This drug has been demonstrated to be a stronger inhibitor of serotonin reuptake than other members of the same drug class, including [Citalopram], [Fluoxetine], and [Fluvoxamine].[A31914] The mechanism of action of paroxetine in relieving the vasomotor symptoms of menopause is unknown, according to the Brisdelle prescribing information[L7703], but may occur due to its effects on thermoregulation.[A181973]
Paroxetine shows a clinically insignificant affinity for adrenergic alpha-1 and alpha-2 receptors and β-adrenergic receptors, dopamine D1 and D2 receptors, histamine H1 receptors and serotonin 5-HT1A, 5-HT2A and 5-HT2C receptors.[A31914] This drug shows some affinity for muscarinic cholinergic receptors and 5-H2B receptors.[A181829,A181847] The delayed onset of paroxetine therapeutic effects may be explained by the initial paroxetine actions on the 5-HT neurons. In rats, paroxetine activates 5-HT1A receptors when it is first administered, inhibiting the stimulation of the 5-HT neurons and subsequent release of serotonin at the synaptic cleft.[A31914]
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| DrugBank Pharmacology: |
Paroxetine treats the symptoms of depression, various anxiety disorders, posttraumatic stress disorder, obsessive-compulsive disorder, and the vasomotor symptoms of menopause via the inhibition of serotonin reuptake.[T653,L3358,L7703] The onset of action of paroxetine is reported to be approximately 6 weeks.[A181874]
Due its serotonergic activity, paroxetine, like other SSRI drugs, may potentiate serotonin syndrome. This risk is especially high when monoamine oxidase (MAO) inhibitors are given within 2 weeks of paroxetine administration. Upon cessation of MAO inhibitors, a 2-week interval before paroxetine administration is recommended. Do not coadminister these agents.[T656]
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| DrugBank Indication: |
Paroxetine is indicated for the management of depression, obsessive-compulsive disorder, panic disorder, social anxiety disorder, generalized anxiety disorder, posttraumatic stress disorder.[L3358] One form of paroxetine, commercially known as Brisdelle, is used to manage mild to moderate vasomotor symptoms of menopause.[L7703] Off-label, paroxetine may be used for the treatment of premature ejaculation or irritable bowel syndrome (IBS).[A1093,A181754,A181904]
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