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Receptor Binding Profiles of Antidepressants

Receptor Binding Profiles of Antidepressants.png


Legend:
  • pKi ~X.X: Affinity with a pKi value of approximately X.X.
  • SERT: Serotonin transporter.
  • NET: Norepinephrine transporter.
  • DAT: Dopamine transporter.
  • 5-HTx: Various subtypes of serotonin receptors.
  • α1, α2: Adrenergic receptors.
  • H1: Histamine H₁ receptor.
  • M1: Muscarinic acetylcholine receptor.
  • Notes: Important information about the medication's mechanism of action or special properties.

Explanations of the Medications:

1. Selective Serotonin Reuptake Inhibitors (SSRIs)

  • Medications: Fluoxetine, Sertraline, Paroxetine, Citalopram, Escitalopram
  • Mechanism of Action: Selectively inhibit SERT, increasing serotonin levels in the synaptic cleft.
  • Indications: Treatment of depression, anxiety disorders, obsessive-compulsive disorder (OCD).
  • Side Effects: Nausea, sleep disturbances, sexual dysfunction.

2. Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs)

  • Medications: Venlafaxine, Duloxetine
  • Mechanism of Action: Inhibit SERT and NET, increasing serotonin and norepinephrine levels.
  • Indications: Depression, generalized anxiety disorder, neuropathic pain.
  • Side Effects: Nausea, sweating, increased blood pressure.

3. Tricyclic Antidepressants (TCAs)

  • Medications: Amitriptyline, Nortriptyline, Imipramine, Desipramine, Clomipramine
  • Mechanism of Action: Inhibit SERT and/or NET and act on various receptors (H1, M1, α1).
  • Indications: Severe depression, chronic pain, migraine prophylaxis.
  • Side Effects: Sedation, anticholinergic effects, orthostatic hypotension.

4. Norepinephrine-Dopamine Reuptake Inhibitor (NDRI)

  • Medication: Bupropion
  • Mechanism of Action: Inhibits NET and DAT, increasing norepinephrine and dopamine levels.
  • Indications: Depression, smoking cessation.
  • Side Effects: Insomnia, dry mouth, increased seizure risk.

5. Noradrenergic and Specific Serotonergic Antidepressant (NaSSA)

  • Medication: Mirtazapine
  • Mechanism of Action: Antagonist at presynaptic α2-adrenergic receptors and 5-HT₂/5-HT₃ receptors; increases the release of norepinephrine and serotonin.
  • Indications: Depression with sleep disturbances and loss of appetite.
  • Side Effects: Strong sedation, weight gain.

6. Selective Norepinephrine Reuptake Inhibitor (NRI)

  • Medication: Reboxetine
  • Mechanism of Action: Selectively inhibits NET, increasing norepinephrine levels.
  • Indications: Depression; off-label use for ADHD.
  • Side Effects: Sleep disturbances, dry mouth, increased blood pressure.

7. Agomelatine

  • Mechanism of Action: Agonist at melatonin receptors (MT1, MT2); antagonist at 5-HT₂C receptors.
  • Indications: Depression with sleep disturbances, circadian rhythm disorders.
  • Side Effects: Elevated transaminases (liver enzymes), headaches, dizziness.

Important Notes:

  • Data Variability: Exact pKi values can vary depending on the study.
  • Clinical Relevance: The effectiveness of an antidepressant depends not only on affinity to transporters and receptors but also on individual factors.
  • Side Effects: Antidepressants can have different side effects depending on their receptor profile.

Disclaimer: This table is for informational purposes only and does not replace professional advice from a healthcare provider. For questions about therapy or medications, please consult your doctor or pharmacist.


Sources:

  • PDSP Ki Database (University of North Carolina)
  • Stahl's Essential Psychopharmacology
  • Current scientific literature and pharmacological databases

PDF print version see attachment:
 

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