Antidepressants Medical Presentation

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Published on : May 11, 2019 | Views : 3020 | Downloads : 2

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Slide 1-

Antidepressants
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The term depression refers to a depression of mood as is a chronic condition. Depression mood is accompanied by: low energy or fatigue sleep disturbances. Physical, social, and personal functioning are impaired. The risk of suicide is greatly increased.
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Types of depression
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Our target : When depression occurs, there may be a decreased amount of these two chemicals released from nerve cells in the brain So we have to inhibit the neurotransmitter break down
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Monoamine Oxidase Inhibitors plays the physiological role of oxidatively deaminating primary and secondary amines to aldehydes, ammonia neurotransmitter amines are deaminated primarily by type A, benzylamine by type B and tyramine by both type A and B MAO.
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Mechanism of Action: Inhibit MAO which catabolizes biogenic amines Side Effects: food containing tyramine (Cheese) leads to hypertensive crisis (Cheese effect) dryness of mouth, excessive perspiration, dizziness, blurred vision, nausea, constipation,hepatitis
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•A consequence of irreversible inactivation is that the action of the agents may continue for up to 2 weeks after administration is discontinued. Uses: atypical depressive illness they are drugs of second choice
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MAO inhibitors are divided into three groups: a)First generation MAO inhibitors: Irreversible Non-Selective MAOIs (e.g. iproniazide). b)Second generation MAO inhibitors: Irreversible Selective MAOIs c)Third generation: reversible Selective MAOIs
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a)First generation MAO inhibitors a)Iproniazid: Synthesis :
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Mechanism of action
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b) Phenelzine Sulphate Mechanism of action
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Tranylcypromine Mechanism of action
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L Deprenyl (Selegiline) Selegiline inhibits MAOB Irreversible Selective USES In its pill form, selegiline is used to treat symptoms of Parkinson's disease Selegiline is also delivered via a transdermal patch in this form it is used as a treatment for major depressive disorder
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Synthesis:
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Third generation MAO inhibitors: Reversible Selective MAOIs Moclobemide It is safer than irreversible MAOIs (less hypertensive crisis Synthesis:
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Tricyclic Antidepressants Mechanism of Action Tricyclic antidepressants potentiate the action of biogenic amines (mainly NA and 5-HT) by inhibiting their presynaptic uptake after release which leads to increased concentrations of these neurotramsmitters at the synapse.
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Side Effects: They block Cholinergic and histamine receptors, it has marked anticholinergic & sedative effects. Advantage: They are safer than MAOI , used with no diet control and used for children (bed wetting).
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1) Imipramine used in the treatment of major depression and enuresis (Nocturnal Enuresis) bed wetting. it has marked anticholinergic & sedative effects It is an Azepine Derivative
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Imipramine Synthesis
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SAR
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2) Desipramine It is a demethylated metabolite of imipramine with less anticholinergic, less sedative , more stimulatory
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Metabolism
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Clomipramine It is up to 50 Times as potent as imipramine
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4) Amitriptyline Double bond is responsible for rigidification. No geometric isomers. More potent than imipramine
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5) Nortriptyline less anticholinergic, less sedative & more stimulant action than amitriptyline. Nortriptyline is a SNERI
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Amitryptiline, Dothepine & Doxepine are bio- isosters
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Tetracyclic Antidepressants Morprotilin less cardiac side effects It can be viewed as a TCA with an ethylene-bridged central ring
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Selective Serotonin reuptake inhibitor Fluoxetine Synthesis :
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Metabolism
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Selective Norepinephrine Reuptake Inhibitors
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Lab 2.1