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Sertraline

CHEMBL809 Phase 4 承認済み Small molecule
Half-Life
26 hours
Bioavailability
—
Protein Binding
—
Molecular Weight
306.2 g/mol
LogP
4.8
Phase
4

Sertraline is one of the most widely prescribed selective serotonin reuptake inhibitors, a class that raises serotonin availability by blocking its reuptake into presynaptic neurons. The added serotonergic tone gradually lifts mood, eases anxiety, and improves sleep, with full benefit typically emerging only after several weeks of steady use. Its indications span major depression, post-traumatic stress disorder, obsessive-compulsive disorder, and panic disorder. A chlorinated small molecule (C17H17Cl2N) with a half-life of roughly 26 hours, it suits once-daily dosing and reaches steady state within about a week. The delayed onset reflects downstream neural adaptations rather than the immediate receptor effect, a pattern shared across antidepressants of this type. Sertraline is an approved first-line option for several mood and anxiety disorders.

One of the most widely prescribed antidepressants, this SSRI increases serotonin availability in the brain to lift mood, reduce anxiety, and improve sleep. It is used for depression, PTSD, OCD, panic disorder, and bipolar depression, typically taking several weeks to reach its full effect.

分子量

306.2290 g/mol

LogP

4.80

TPSA

12.00 Ų

リピンスキーの五則

適合

治療領域

Ovarian Cancer Pancreatic Cancer Bladder Cancer Thyroid Cancer Cardiovascular Disease Respiratory Disease Pain Management Non-Small Cell Lung Cancer Asthma Chronic Obstructive Pulmonary Disease Alzheimer's Disease Parkinson's Disease Epilepsy Migraine Schizophrenia Bipolar Disorder Generalized Anxiety Disorder Insomnia Infectious Disease Gastroesophageal Reflux Disease Inflammatory Bowel Disease Chronic Kidney Disease Non-Alcoholic Fatty Liver Disease Stroke Obesity Type 2 Diabetes Hypertension Major Depressive Disorder Breast Cancer Chronic Pain Hepatitis C Heart Failure Prostate Cancer Colorectal Cancer Leukemia

薬物分類

N — N - Nervous System

作用機序

Selective serotonin reuptake inhibitor (SSRI).

Pharmacokinetics (PK)

Half-Life 26 hours

Pharmacodynamics (PD)

機序

Selective serotonin reuptake inhibitor (SSRI).

2D構造

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SMILES

                    
CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21

                

                

                
                

                    
InChI

                    
InChI=1S/C17H17Cl2N/c1-20-17-9-7-12(13-4-2-3-5-14(13)17)11-6-8-15(18)16(19)10-11/h2-6,8,10,12,17,20H,7,9H2,1H3/t12-,17-/m0/s1

                

                

                

                    
                    

                        
Molecular Formula

                        
C17H17Cl2N

                    

                    
                    

                        
HBD / HBA

                        
1 / 1

                    

                    
                    

                        
回転可能結合数

                        
2

                    

                    
                    
                    

                        
重原子数

                        
20

                    

                    
                

            


            
            

                
                

                    
                    

                        

                            SLC6A4 (Serotonin Transporter)
                            Inhibitor
                        

                        
                        Primary Target
                        
                    

                    
                    

                        

                            CYP2D6 (Cytochrome P450 2D6)
                            Inhibitor
                        

                        
                    

                    
                

                
            


            
            

                
                

                    
                    
                        

                            

  
  Major


                            
                                Sertraline + Tramadol
                            
                        

                        
                        
Sertraline and tramadol together significantly increase serotonergic tone, posing a clinically meaningful risk of serotonin syndrome.

                        
                    
                    
                    
                        

                            

  
  Moderate


                            
                                Sertraline + Warfarin
                            
                        

                        
                        
Sertraline can modestly increase warfarin anticoagulation through weak CYP2C9 inhibition combined with SSRI-mediated platelet serotonin depletion.

                        
                    
                    
                    
                        

                            

  
  Moderate


                            
                                Sertraline + Sumatriptan
                            
                        

                        
                        
Sertraline and sumatriptan may interact to increase serotonergic tone, raising the theoretical risk of serotonin syndrome.

                        
                    
                    
                    
                        

                            

  
  Moderate


                            
                                Sertraline + Trazodone
                            
                        

                        
                        
Sertraline combined with trazodone may increase the risk of serotonin syndrome due to additive serotonergic effects.

                        
                    
                    
                    
                        

                            

  
  Major


                            
                                Sertraline + Duloxetine
                            
                        

                        
                        
Combining duloxetine and sertraline, two serotonergic antidepressants, markedly increases the risk of serotonin syndrome without added efficacy.

                        
                    
                    
                    
                        

                            

  
  Major


                            
                                Sertraline + Escitalopram
                            
                        

                        
                        
Co-prescribing two SSRIs leads to additive serotonin excess with no therapeutic benefit and high risk of serotonin syndrome.

                        
                    
                    
                    
                        

                            

  
  Moderate


                            
                                Sertraline + Aspirin
                            
                        

                        
                        
The combination of aspirin and sertraline increases upper GI bleeding risk through synergistic antiplatelet and platelet serotonin depletion effects.

                        
                    
                    
                    
                        

                            

  
  Moderate


                            
                                Sertraline + Fluconazole
                            
                        

                        
                        
Fluconazole inhibits CYP2C19 and CYP3A4, increasing sertraline plasma concentrations, which may enhance both therapeutic and adverse effects including QT prolongation.

                        
                    
                    
                    
                        

                            

  
  Moderate


                            
                                Sertraline + Ibuprofen
                            
                        

                        
                        
Ibuprofen combined with SSRIs markedly increases the risk of GI bleeding through synergistic impairment of platelet function and gastric mucosal defense.

                        
                    
                    
                    
                        

                            

  
  Moderate


                            
                                Sertraline + Lamotrigine
                            
                        

                        
                        
Sertraline may increase lamotrigine plasma concentrations by inhibiting its glucuronidation, potentially causing lamotrigine toxicity.

                        
                    
                    
                    
                        

                            

  
  Moderate


                            
                                Sertraline + Levothyroxine
                            
                        

                        
                        
Sertraline can increase levothyroxine clearance, particularly in patients with pre-existing hypothyroidism, potentially necessitating levothyroxine dose increases.

                        
                    
                    
                    
                        

                            

  
  Moderate


                            
                                Sertraline + Phenytoin
                            
                        

                        
                        
Phenytoin significantly reduces sertraline plasma concentrations via CYP enzyme induction, potentially causing antidepressant treatment failure.

                        
                    
                    
                    
                        

                            

  
  Moderate


                            
                                Sertraline + Carbamazepine
                            
                        

                        
                        
Carbamazepine, a potent enzyme inducer, significantly reduces sertraline plasma concentrations, potentially impairing antidepressant efficacy.

                        
                    
                    
                    
                        

                            

  
  Moderate


                            
                                Sertraline + Naproxen
                            
                        

                        
                        
Naproxen combined with sertraline increases the risk of upper GI bleeding through complementary impairment of platelet function and gastric mucosal defense.

                        
                    
                    
                

                
            


            
            

                
                


    
    
        
    
    
    
No side effects recorded

    
    
Side effect data is not yet available for this drug.

    



                
            


            
            
            

                
よくある質問

                

                    
                    

                        
                        

                            
One of the most widely prescribed antidepressants, this SSRI increases serotonin availability in the brain to lift mood, reduce anxiety, and improve sleep. It is used for depression, PTSD, OCD, panic disorder, and bipolar depression, typically taking several weeks to reach its full effect.

                        

                    

                    

                    

                    
                    

                        
                        

                            
Selective serotonin reuptake inhibitor (SSRI).

                        

                    

                    

                    
                    

                        
                        

                            
Key pharmacokinetic parameters for Sertraline: Half-life: 26 hours.

                        

                    

                    

                    

                        
                        

                            
Yes, Sertraline is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.

                        

                    

                

            

            

            
            
            

                
                
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Related Drugs


                
                

                    
Same Drug Class

                    

                        
                        
                            Acetaminophen
                            Small molecule
                        
                        
                        
                            Aspirin
                            Small molecule
                        
                        
                        
                            Escitalopram
                            Small molecule
                        
                        
                        
                            Fluoxetine
                            Small molecule
                        
                        
                    

                

                

                
                
                
            

            

            
            
{# References & Data Sources section for drug detail pages.
   Renders standard pharmacological database links plus the drug's data_sources field. #}


    
References & Data Sources

    
    
        
        
  • 
            
            
                ChEMBL — European Bioinformatics Institute (EBI).
                CHEMBL809.
                Open-access bioactivity database.
            
        
    • 
        
        
        
  • 
            
            
                PubChem — National Center for Biotechnology Information (NCBI).
                CID 68617.
                Chemical information database.
            
        
    • 
        
        
        
        
    

    
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-28.




        


        
        
    


    



    
医学的免責事項

    

        This content is for educational and informational purposes only. It is not a substitute for professional medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before making medication decisions.
    

    

        Data sources:
        ChEMBL,
        PubChem,
        DailyMed.