Antidepressants Flashcards
(26 cards)
SNRIs (Serotonin & Norepinephrine Reuptake Inhibitors)
Venlafaxine (active metabolite: Desvenlafaxine); Duloxetine
Heterocyclic antidepressants (mostly tricyclics)
Imipramine (active metabolite: Despiramine)
Amitriptyline (active metabolite: Nortriptyline)
MAOIs (Monoamine oxidase inhibitors)
Isocarboxazid
Phenelzine
Tranylcypromine
Selegiline
Atypical antidepressants
Bupropion
Mirtazapine
Nefazodone
Trazodone
Characteristics general to all antidepressants
Equally effective in depressed patients
Similar delayed onset of therapeutic effects
Mostly work via direct/indirect increases in norepinephrine and/or serotonin levels in synaptic cleft
SSRI drugs
Fluoxetine
Citalopram (Escitalopram)
Paroxetine
Sertraline
Mirtazapine MOA
Blocks alpha-2 but not alpha-1 adrenergic receptors increasing serotonin & norepinephrine release in synaptic cleft
Strong anti-histaminergic effect- promotes drowsiness & stimulates appetite- useful in the elderly presenting w/ insomnia and weight loss
Mirtazapine adverse effects
Anti-histaminergic- sedation & weight gain
Mild anti-alpha-1 adrenergic & anti- cholinergic effects
Imipramine MOA
Antidepressant
Norepinephrine & serotonin reuptake inhibitor
Citalopram MOA
Antidepressant
Serotonin reuptake inhibitor
Fluoxetine MOA
Antidepressant
Serotonin reuptake inhibitor
Some norepinephrine reuptake inhibition
Duloxetine MOA
Antidepressant
Serotonin reuptake inhibitor
Mild norepinephrine reuptake inhibition
Venlafaxine MOA
Antidepressant
Serotonin reuptake inhibitor
Some norepinephrine reuptake inhibition
Receptor stimulation resulting in decreased norepinephrine/serotonin release
Pre-synaptic alpha-2-/5-HT10 auto- receptors on noradrenergic or serotonergic terminals
Receptor stimulation resulting in decreased serotonin release
Alpha-2 heteroreceptors on 5-HT nerve terminals
Receptor stimulation resulting in increase 5-HT activity
Alpha-1 adrenergic receptors on 5-HT neuronal dendrites
Antidepressant drugs causing sexual dysfunction
Decreasing order of potency: Fluoxetine Citalopram Venlafaxine Duloxetine Bupropion
Phenelzine MOA
Irreversibly inhibits MAO
Monoamine oxidase (MOA)
Primary enzymatic mechanism for the degradation of monoamines (dopamine, epinephrine, norepinephrine & serotonin)
MAO isoforms + role
MAO-A: primarily metabolizes norepinephrine & serotonin in the CNS
MAO-B: dopamine selective isoform
MAOIs drug interactions
Interact with tyramine in food- potential for hypertensive crisis
Foods containing tyramine:
Fermented foods- cheese, yogurt, sour cream, etc.
Wine & beer, chocolate, coffee, preserved fish (sardines, herring), dried fruits
Drugs contraindicated:
Amphetamines including methylphenidate
Sympathomimetics
Many other drugs metabolized by MAO
Bupropion MOA
Effective antidepressant
Structurally unrelated to other antidepressants
MOA is unknown
Also used in cessation smoking programs in combination with behavioral modification
Bupropion adverse effects
Increased risk of seizures
St. John’s Wart
Herbal treatment for depression
From plant Hypercium perforatum
Equally as effective as TCAs in short term treatment of mild to moderate major depression (1-3 months)
