5th Antidepressant Drug

Introduction
● Depression is due to a deficiency of mono- amines, such as norepinephrine

and serotonin, at certain key sites in the brain. Conversely, the theory Depression
proposes that mania is caused by an overproduction of these

neurotransmitters.
● The symptoms of depression are feelings of sadness and hopelessness, as

well as the inability to experience pleasure in usual activities, changes in
sleep patterns and appetite, loss of energy, and suicidal thoughts.
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Classification of antidepressant drugs
● Most antidepressant drugs potentiate, either directly or indirectly, the actions of
norepinephrine and/or serotonin (5-HT) in the brain.
Antidepressant classes:
1. Selective serotonin reuptake inhibitors
2. Serotonin-norepinephrine reuptake inhibitors
3. Atypical antidepressants
4. Tricyclic antidepressants
5. Monoamine oxidase inhibitors
5
Actions: The SSRIs block the reuptake of serotonin, leading to increased concentrations of
the neurotransmitter in the synaptic cleft.
Therapeutic uses: The primary indication for SSRIs is depression. other psychiatric
disorders also respond favorably to SSRIs, including obsessive-compulsive disorder, panic
disorder, generalized anxiety disorder, posttraumatic stress disorder, social anxiety
disorder, pre-menstrual dysphoric disorder, and bulimia nervosa (only fluoxetine is
approved for bulimia).
SSRIs Drugs: Fluoxetine, Citalopram, Escitalopram, Fluvoxamine, Paroxetine, and
Sertraline
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Note Antidepressants, including SSRIs, typically take at least 2 weeks to produce significant
improvement in mood, and maximum benefit may require up to 12 weeks or more
● Common adverse effects include GIT effects (nausea, vomiting, diarrhea), sexual
dysfunction, sleep disturbances (insomnia & somnolence), and agitation.
● Discontinuation syndrome occurs after abrupt withdrawal of SSRIs particularly agents
with shorter half lives and inactive metabolites.
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2. Serotonin-Norepinephrine Reuptake Inhibitors
Actions: SNRis inhibit the reuptake of both serotonin & norepinephrine,
increasing the levels of these neurotransmitters in the brain.
Indications: SNRIs are used for depression, generalized anxiety disorder,
and chronic pain conditions like fibromyalgia (Depression is often
accompanied by chronic pain, such as backache and muscle aches, for
which SNRIs are effective). Also, it is useful in the treatment of Diabetic
neuropathic pain.
SNRIs Drugs: Duloxetine, Venlafaxine, desvenlafaxine, levomilnacipran.
● The SNRis, have little activity at a-adrenergic, muscarinic, or
histamine receptors thus, have fewer receptor-mediated adverse
effects than the TCAs. 8
3. Atypical antidepressants
A typical antidepressant is a mixed group of agents that have actions at several different
sites.
This group includes:
Brexanolone is used for postpartum depression.
Bupropion is a weak dopamine and norepinephrine reuptake inhibitor. Used for
depression and smoking cessation withdrawal symptoms
Mirtazapine enhances serotonin and norepinephrine neurotransmission by serving as an
antagonist at central presynaptic a2 receptors. It causes sedation because of its potent
antihistaminic activity.
Other drugs: nefazodone, trazodone, vilazodone, and vortioxetine.
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4. Tricyclic Antidepressants
Mechanism of action
1. The TCAs inhibit norepinephrine and serotonin reuptake into the pre-
synaptic neuron.
2. TCAs also block serotonergic, a-adrenergic, histaminic, and muscarinic
receptors.
TCAs Drugs:
● Amitriptyline, Amoxapine, Clomipramine, Desipramine, Doxepin,
Imipramine, Maprotiline, Nortriptyline, Protriptyline, Trimipramine
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4. Tricyclic Antidepressants
The TCAs are effective in treating moderate to severe depression. Some patients
with panic disorder also respond to TCAs.
● Imipramine is used as an alternative to desmopressin or nonpharmacologic

therapies (enuresis alarms) in the treatment of bed-wetting in children.
● The TCAs, particularly amitriptyline, have been used to help prevent migraine
headaches and treat chronic pain syndromes (for example, neuropathic pain).
● Low doses of TCAs, especially doxepin, can be used to treat insomnia.
● Adverse effect: TCAs has anticholinergic, antihistaminic, antiadrenergic side

effects. 11
5. Monoamine Oxidase Inhibitors
Location: Monoamine oxidase (MAO) is a mitochondrial

enzyme found in nerves and other tissues, such as the
gut and liver. In the neuron, MAO functions to
oxidatively deaminate and inactivate any excess
neurotransmitters (for example, norepinephrine,
dopamine, and serotonin) that may leak out of synaptic
vesicles when the neuron is at rest.
Therapeutic uses: These are used for depressed

patients who are unresponsive or intolerant to other
antidepressants.
● considered last-line agents in many treatment
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settings.
5. Monoamine Oxidase Inhibitors
mechanism of action: MAOIs may irreversibly or reversibly inactivate the
enzyme, resulting in increased stores of norepinephrine, serotonin, and dopamine
within the neuron and subsequent diffusion of excess neurotransmitters into the
synaptic space.
● These drugs inhibit not only MAO in the brain but also MAO in the liver and gut
which catalyzes oxidative deamination of drugs and potentially toxic
substances, such as tyramine, which is found in certain foods. The MAOIs,
therefore, show a high incidence of drug-drug and drug-food interactions.
MAOIs Drugs: Phenelzine, Tranylcypromine, Isocarboxazid, and Selegiline.
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6.Serotonin-Dopamine Antagonists
● The serotonin-dopamine antagonists (SDAs), or atypical antipsychotics,

are occasionally used as adjunctive treatments to antidepressants if the
patient does not respond to monotherapy.
● Aripiprazole, brexpiprazole, quetiapine, and the combination of fluoxetine
and olanzapine are approved for use as adjuncts in major depressive
disorder (MOD).
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Experiment
Aim of Actophotometer test?
To assess the effects of the drug on the locomotor activity of the

rats. understanding how these medications impact the spontaneous
activity levels or behavioral patterns of the rats.
If the drug reduces the locomotor activity, indicate its potential

effectiveness in treating symptoms associated with psychosis or
related disorders.
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Introduction

● Depression is due to a deficiency of mono- amines, such as norepinephrine

proposes that mania is caused by an overproduction of these

● The symptoms of depression are feelings of sadness and hopelessness, as

● Imipramine is used as an alternative to desmopressin or nonpharmacologic

● Low doses of TCAs, especially doxepin, can be used to treat insomnia.

● Adverse effect: TCAs has anticholinergic, antihistaminic, antiadrenergic side

Location: Monoamine oxidase (MAO) is a mitochondrial

Therapeutic uses: These are used for depressed

MAOIs Drugs: Phenelzine, Tranylcypromine, Isocarboxazid, and Selegiline.

● The serotonin-dopamine antagonists (SDAs), or atypical antipsychotics,

Aim of Actophotometer test?

To assess the effects of the drug on the locomotor activity of the

If the drug reduces the locomotor activity, indicate its potential

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