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Flashcards about Antidepressants
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What is depression?
A serious mood disorder affecting approximately 5% of the population.
What are the symptoms of depression?
Intense sadness, hopelessness, inability to experience pleasure, fatigue, sleep and appetite disturbances, and suicidal thoughts.
What does the biogenic amine hypothesis state?
Mood disorders result from abnormalities in serotonin, norepinephrine, or dopamine neurotransmission.
Besides depression, what other disorders are antidepressants effective in treating?
Panic disorder, phobic disorders, and obsessive-compulsive disorder.
How long does it take for antidepressants to have a therapeutic benefit?
After 2 to 3 weeks of dosing.
What effect do antidepressants have on normal individuals?
They do not elevate mood in normal individuals.
Name four tricyclic antidepressants (TCAs).
Amitriptyline, Imipramine, Clomipramine, Doxepin.
What is the mechanism of action of TCAs?
They inhibit the neuronal reuptake of norepinephrine and serotonin into presynaptic nerve terminals.
Besides norepinephrine and serotonin receptors, what other receptors do TCAs block?
Blockade of muscarinic receptors, alpha-adrenergic receptors and histaminic receptors.
What are the anticholinergic adverse effects of TCAs?
Blurred vision, dry mouth, urinary retention, tachycardia, and constipation.
How does imipramine control bedwetting in children?
By contraction of the internal sphincter of the bladder.
For what condition can Amitriptyline be used?
Chronic neuropathic pain and migraine.
What are the anticholinergic adverse effects of TCAs?
Dry mouth, blurred vision, constipation, urinary retention.
What cardiovascular adverse effect is associated with TCAs?
Postural (orthostatic) hypotension and reflex tachycardia.
What are the sedative adverse effects of TCAs?
Sedation, drowsiness, difficulty in concentration.
Name five Selective Serotonin Reuptake Inhibitors (SSRIs).
Fluoxetine, Paroxetine, Sertraline, Citalopram, Escitalopram.
What is the mechanism of action of SSRIs?
They specifically inhibit neuronal reuptake of serotonin.
How much greater selectivity do SSRIs have for serotonin transporters compared to norepinephrine transporters?
300- to 3000-fold.
What receptors do SSRIs have little blocking activity at?
Muscarinic, α-adrenergic, and histaminic H1 receptors.
What are some other indications of SSRIs besides depression?
Obsessive-compulsive disorders, Panic disorders and Generalized anxiety.
Which SSRI is approved for bulimia nervosa?
Only fluoxetine.
What are the common adverse effects of SSRIs?
Headache, anxiety, GI effects (nausea, vomiting, diarrhea), Weakness, fatigue, and sleep disturbances.
What are the possible causes of Sexual dysfunction due to SSRIs?
SSRIs may reduce NO production, increased serotonin inhibits dopamine and some SSRIs can raise prolactin levels.
Name three Serotonin/Norepinephrine Reuptake Inhibitors (SNRIs).
Duloxetine, Venlafaxine, Desvenlafaxine.
What is the mechanism of action of SNRIs?
They inhibit the reuptake of both serotonin and norepinephrine.
When are SNRIs indicated for treating depression?
Patients in whom SSRIs are ineffective and depression accompanied by chronic painful symptoms.
What pain conditions can SNRIs relieve?
Diabetic peripheral neuropathy, post-herpetic neuralgia, fibromyalgia, and low back pain.
Name four atypical antidepressants.
Mirtazapine, Bupropion, Nefazodone, Trazodone.
How does Mirtazapine enhance serotonin and norepinephrine neurotransmission?
Blocking presynaptic Alpha 2-adrenoceptor and noradrenergic modulation of serotonin systems.
For what type of patients is Mirtazapine useful?
Depressed patients having difficulty sleeping.
What are the common side effects of Mirtazapine?
Weight gain and sedation.
What is the mechanism of action of Bupropion?
A weak dopamine and norepinephrine reuptake inhibitor.
For what type of patients is Bupropion effective?
Patients who cannot tolerate S/E of SSRIs or non-responders of SSRIs.
What are the adverse effects of Bupropion?
Dry mouth, sweating, nervousness, tremor, dose-dependent increased risk for seizures.
For what type of patients are MAOIs indicated?
Depressed patients who are unresponsive or allergic to TCAs and SSRIs.
What is the function of monoamine oxidase (MAO)?
Oxidative deamination of biogenic amines.
What are the two isoenzyme forms of MAO?
MAO-A and MAO-B.
What does MAO-A preferentially deaminate?
5-HT and NA.
What does MAO-B preferentially deaminate?
Dopamine and phenethylamine
What type of MAO inhibitor is Moclobemide?
Moclobemide is a reversible and selective MAO-A inhibitor.