Pharmacology of antidepressants Flashcards
What are the two types of mood disorders
Unipolar (depression) and Bipolar (manic-depressive)
T/F: Mood disorders are episodic
True
What are the tertiary TCAs, what type of inhibiton does it favor
Imipramine, Amitriptyline, Doxepin, Trimipamine, Clomipramine/ greater Serotonin reuptake inhibition
What are the secondary TCAs, what type of inhibiton does it favor
Despiramine, Nortriptyline, Protriptyline/ greater norepinephrine reuptake inhibition
What is the chronic effects of TCAs, what is the theory behind it
Desensitization, decrease in beta-adnergic receptors and serotonin receptors/ Desensitization leads to delayed therapeutic antidepressant response
What are the TCA therapeutic effects
Antidepressant activity (specific mood-elevating effect), antipanic activity, antiobsessional activity (5-HT inhibition), sedation in non-depressed individuals
What receptors are antagonized by TCAs
muscarinic receptors, alpha-1 norepinephrine receptors, histamine-1 and histamine-2 receptors
What side effects of TCAs are due to antagonizing histamine receptors
weight gain and drowsiness
What side effects of TCAs are due to muscarinic receptors
Constipation, blurred vision, dry mouth, urinary retention, memory impairment
What side effects of TCAs are due to antagonizing alpha-1 receptors
Dizziness, orthostatic hypotension
What are other side effects of TCAs
Tremor (beta-adnergic stimulation), cardiac arrhythmias with seizures and coma (Sodium channel blockade)
T/F: TCAs are associated with high suicide potential
True
What are the selective serotonin reuptake inhibitors
Fluoxetine, Sertraline, Paroxetine, Citalopram, Escitalopram
What is the MOAs of nefazadone and trazodone
Inhibition of serotonin uptake carrier, antagonism of serotonin receptors, antagonism of alpha-1 adnergic receptors, chronically down-regulates receptors
What are the side effects of nefazadone and trazodone
Sedation (most prominent), dry mouth (alpha adnergic antagonism), hyptotension, hepatoxicity (nefazodone BBW), trazodone (painful priapism)
T/F: Nefazadone and Trazadone have antimuscarinic activity
False: Nefazodone and Trazodone has NO ANTIMUSCARINIC activity
What atypical antidepressent is similar to nefazodone and trazodone, whats the difference
Vilazodone, partial serotonin 1A agonist activity
What NDRI not only takes up norepiphrine but at high enough concentrations dopamine as well, what happens when chronically used, side effects
Bupropion/ down-regulates beta-adnergic receptors/ mild psychomotor agitation, insomnia, seizures
What are the dose-dependent MOAs of venlafaxine
Inhibition of serotonin uptake carrier (low doses), inhibiton of norepinephrine carrier ( medium doses), inhibition of dopamine carrier (high doses), down regulates those receptors
What are the side effects of venlafaxine
Increased diastolic blood pressure (NE stimulation), Nausea (serotonin 3 mediated)
T/F: Venlafaxine has no antagonism of muscarinic, alpha-adnergic, or histamine 1 receptors
True
What is the active metabolite of venlafaxine, what makes it different
Desevenlafaxine, NOT a substrate for CYP 2D6
What receptors does Mirtazapine antagonize, therapeutic effects
alpha2-adnergic, serotonin-2, serotonin-3, histamine-1, antianxiolytic and antidepressant
What are the side effects of mirtazapine
weight gain and drowsiness
What is the MOA of maprotiline, side effects
Selective NE uptake inhibition, chronically: down regulates receptors/ sedation (histamine-1 antagonism), orthostatic hypotension (alpha-1 antagonism), seizures
What the MAO inhibitors
Phenelzine (hydrazine), Isocarboxizid (hydrazide), tranylcypromine (amphetamine derivative), moclobemide (reversible MAO inhibitor)
T/F: MAO inhibitors only increase the amount of dopamine present
False: Due to MAO-inhibitors there is an accumulation of norepinephrine, dopamine, and serotonin in the synaptic cleft
What are the pharmacologic effects
Mood-elevating action in depressed patients, mild stimulant action in non-depressed individuals, antipanic action, antiarcoleptic action
What is the tyramine effect associated with MAO inhibitors
Tyramine that is usually metabolized by MAO is not leading to severe hypertension due to build-up
What are drug-drug interactions for MAO inhibitors
Pseudoephedrine, SSRIs (serotonin syndrome), Meperidine
T/F: At subanesthetic doses, ketamine can exert immediate antidepressant effect in patients with resistant bipolar or unipolar depression with IMMEDIATE reduction in suicidal thoughts
True
What does ketamine cause when subanesthetic doses are given
Release of glutamate
