P H R M A C O L O G Y - NOTE 11 - Anti-Depressants Drugs

                                                                                                                             ANTI-DEPRESSANT
                                                                                                                                  DRUGS

                                                                                                               ARI                                                MAOI

                                                                                                                                           Selective
                                   Tricyclic                               Heterocyclic                        SNARI         SSRI                                   Tranylcypromine
                                                                                                                                             NERI


                          Amitriptyline                            Amoxapine                         Venlafaxine              Fluoxetine      Imipramine               Selegiline



                          Nortriptyline                           Maprotiline                                                Fluvoxamine     Atomoxetine             Moclobemide



                           Imipramine                                Trazodone                                               Citalopram
                                                                                                                                                                               •  action of Tyramine
                                                                                                                                                             MAOI cause         (sympathomimetics)
                                                                                                                                                                               • Serotonin syndrom with SSRI

                          Clomipramine                               Bupropion                                                Sertraline                                              • does not cause
                                                                                                                                                           selective MAO-B I           tyramine related
                                                                                                                                                                                       reactions
                                                                                                                                                                                      • hyperthermia.
                                                                                                                                                               Serotonin              • muscle rigidity.
                                                                                                                                                             syndrom has              • myoclonus.
                                               Endogenous (melanocholic)




                       • griefe                                            •biochemical                        • bipolar                                                              • CVS & Resp. failure.
                                                                            disorder
Reactive (secondary)




                       • illness                                                                                 affective
                                                                                            Manic-depression




                                                                            (genatically)                        disorder                                                             •due to depletion
                                                                           •inability to                                                                     depression                of amine stores in
                                                                                                                                                                                       CNS
                                               depression
depression




                                                                            cope with
                                                                            minor life                                                                                                                         33
                                                                            events



                          ‫| نسألكم الدعاء‬
P H R M A C O L O G Y - NOTE 11 - Anti-Depressants Drugs



                                                    Amine Re-uptake Inhibitors (ARI)
                              DRUG                  PHARMACOKINETIC                MECHANISM OF ACTION                                              USES                                             SIDE EFFECT
                            Amitriptyline     Caution in glaucoma & BPH                     re-uptake of NE & 5-HT.                  Depression.                                      Anti-muscarinic
                                                    due to anti-muscarinic side effect.    also  concentration in synapse.           Anxiety disorders.                                      blurred vision, dry mouth.
anti-depreesant



                            Nortriptyline     Caution in driving & skill full word                                                     Chronic pain.                                           HR, confusion.
                                                   due to sedation                                                                                                                             constipation, urine retention .
    Tricyclic




                                                                                                                                         Enuresis.
                             Imipramine                                                                                                                                                   α – blocking
                                                                                                                                                                                                 ejaculation & orthostatic BP
                                                                                                                                                                                          sedation.
                            Clomipramine
                                                                                                                                                                                          Seizure.
                                                                                                                                                                                          Weight gain.
                                                                                                                                                                                          Sex disturbances.
                             Amoxapine                                                       re-uptake of NE & 5-HT.                Depression.                                       Parkinsonism.              moderate
anti-depreesant




                                                                                             D2 receptors.                          Anxiety disorders                                 Akathesia.                  sedation
  Heterocyclic




                                                                                                    So, it acts as anti-psychotic                                                       prolactin.                    &
                             Maprotiline                                                     re-uptake of NE & 5-HT                                                                    Seizures.                     anti-
                                                                                                                                                                                         Arrhythmias                muscarinic
                             Trazodone                                                                                                                                                   Induce sleep.
                             Bupropion                                                       re-uptake of NE, 5-HT & DA.                                                               Seizures.
                                                                                                                                                                                        Aggravate psychosis.
                             Venlafaxine      Low dose  acts as SSRI.                      re-uptake of 5-HT (& NE but less).     Depression.                                       Low dose
5-HT & N-ad RI




                                              High dose  acts as TSAs                                                               Anxiety disorders.                                      o Sedative & anti-muscarinic.
                 (SNARI)




                                                                                                                                      Chronic pain                                      High dose
                                                                                                                                                                                               o Sedative & anti-muscarinic.
                                                                                                                                                                                               o Nausea.
                                                                                                                                                                                               o  BP
                                                                                                                                                                                               o Sex distrabunces.
                             Fluoxetine                                                      re-uptake of 5-HT (more selective).   obsessive & compulsive D                            Transient nausea.




                                                                                                                                                                 depression
                                                                                                                                     Bulimia                                             Libido. (initial)




                                                                                                                                                                              anxiety
SSRI




                            Fluvoxamine                                                                                              obsessive & compulsive D                            Sex dysfunction. (maintenance
                              Citalopram                                                                                                                                                  therapy)
                              Sertraline
S NERI                       Imipramine                                                       re-uptake of NE (more selective).     Attention deficit hyperkinetic
                            Atomoxetine                                                                                                disorder.
                                                    Mono-Amine Oxide Inhibitors (MAOI)
                              DRUG                  PHARMACODYNAMIC                MECHNISM OF ACTION                                               USES                                             SIDE EFFECT
                           Tranylcypromine    Inhibits MAO-A & MAO- B.                     They  metabolism of amines by MAO.                                                          Headache.
                                                                                                     duration of action of                                                               Drowsiness.
                              Selegiline      Inhibit MAO- B.                                            NE, 5-HT & DA.                                                                   Weight gain.                            34
                                                                                                    also  concentration.                                                                 Postural PB.
                                               o MAO-A metabolizes NE , 5-HT & Tyramine.                                                                                                   Sex disturbances.
                                               o MAO-B metabolizes DA more than others.



‫| نسألكم الدعاء‬

Pharmacology .. Anti-Depressants Drugs

  • 1.
    P H RM A C O L O G Y - NOTE 11 - Anti-Depressants Drugs ANTI-DEPRESSANT DRUGS ARI MAOI Selective Tricyclic Heterocyclic SNARI SSRI Tranylcypromine NERI Amitriptyline Amoxapine Venlafaxine Fluoxetine Imipramine Selegiline Nortriptyline Maprotiline Fluvoxamine Atomoxetine Moclobemide Imipramine Trazodone Citalopram •  action of Tyramine MAOI cause (sympathomimetics) • Serotonin syndrom with SSRI Clomipramine Bupropion Sertraline • does not cause selective MAO-B I tyramine related reactions • hyperthermia. Serotonin • muscle rigidity. syndrom has • myoclonus. Endogenous (melanocholic) • griefe •biochemical • bipolar • CVS & Resp. failure. disorder Reactive (secondary) • illness affective Manic-depression (genatically) disorder •due to depletion •inability to depression of amine stores in CNS depression depression cope with minor life 33 events ‫| نسألكم الدعاء‬
  • 2.
    P H RM A C O L O G Y - NOTE 11 - Anti-Depressants Drugs  Amine Re-uptake Inhibitors (ARI) DRUG PHARMACOKINETIC MECHANISM OF ACTION USES SIDE EFFECT Amitriptyline  Caution in glaucoma & BPH   re-uptake of NE & 5-HT.  Depression.  Anti-muscarinic  due to anti-muscarinic side effect.  also  concentration in synapse.  Anxiety disorders.  blurred vision, dry mouth. anti-depreesant Nortriptyline  Caution in driving & skill full word  Chronic pain.  HR, confusion.  due to sedation   constipation, urine retention . Tricyclic Enuresis. Imipramine  α – blocking  ejaculation & orthostatic BP  sedation. Clomipramine  Seizure.  Weight gain.  Sex disturbances. Amoxapine   re-uptake of NE & 5-HT.  Depression.  Parkinsonism. moderate anti-depreesant   D2 receptors.  Anxiety disorders  Akathesia. sedation Heterocyclic  So, it acts as anti-psychotic  prolactin. & Maprotiline   re-uptake of NE & 5-HT  Seizures. anti-  Arrhythmias muscarinic Trazodone  Induce sleep. Bupropion   re-uptake of NE, 5-HT & DA.  Seizures.   Aggravate psychosis. Venlafaxine  Low dose  acts as SSRI.   re-uptake of 5-HT (& NE but less).  Depression.  Low dose 5-HT & N-ad RI  High dose  acts as TSAs  Anxiety disorders. o Sedative & anti-muscarinic. (SNARI)  Chronic pain  High dose o Sedative & anti-muscarinic. o Nausea. o  BP o Sex distrabunces. Fluoxetine   re-uptake of 5-HT (more selective). obsessive & compulsive D  Transient nausea. depression Bulimia  Libido. (initial) anxiety SSRI Fluvoxamine obsessive & compulsive D  Sex dysfunction. (maintenance Citalopram therapy) Sertraline S NERI Imipramine   re-uptake of NE (more selective).  Attention deficit hyperkinetic Atomoxetine disorder.  Mono-Amine Oxide Inhibitors (MAOI) DRUG PHARMACODYNAMIC MECHNISM OF ACTION USES SIDE EFFECT Tranylcypromine  Inhibits MAO-A & MAO- B.  They  metabolism of amines by MAO.   Headache.   duration of action of  Drowsiness. Selegiline  Inhibit MAO- B. NE, 5-HT & DA.  Weight gain. 34  also  concentration.  Postural PB. o MAO-A metabolizes NE , 5-HT & Tyramine.  Sex disturbances. o MAO-B metabolizes DA more than others. ‫| نسألكم الدعاء‬