Chapter 10: Antidepressants

Depression

The symptoms of ______ 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.

Mania

is characterized by the opposite behavior: enthusiasm, anger, rapid thought and speech patterns, extreme self-confidence, and impaired judgment.

Antidepressant drugs

potentiate, either directly or indirectly, the actions of norepinephrine and/or serotonin (5-HT) in the brain.

Biogenic amine theory

proposes that depression is due to a deficiency of monoamines, such as norepinephrine and serotonin, at certain key sites in the brain.

mania

the biogenic amine theory proposes that _____ is caused by an overproduction of these neurotransmitters.

selective serotonin reuptake inhibitors (SSRIs)

are a group of antidepressant drugs that specifically inhibit serotonin reuptake

SSRIs

Because they have different adverse effects and are relatively safe even in overdose, the _____ have largely replaced TCAs and monoamine oxidase inhibitors (MAOIs) as the drugs of choice in treating depression.

Escitalopram

is the pure S-enantiomer of citalopram.

SSRIs

block the reuptake of serotonin, leading to increased concentrations of the neurotransmitter in the synaptic cleft.

fluoxetine

only ______ is approved for bulimia

paroxetine and fluvoxamine

are generally

more sedating than activating, and they may be useful in patients who have difficulty sleeping.

fluoxetine or sertraline

patients who are fatigued or complaining of excessive somnolence may benefit from one of the more activating SSRIs, such as ______ or _____

bupropion or mirtazapine

One option for managing SSRI-induced sexual dysfunction is to change the antidepressant to one with fewer sexual side effects, such as ______ or _____

Fluoxetine, sertraline, and fluvoxamine

approved for use in children to treat obsessive–compulsive disorder

fluoxetine and escitalopram

approved to treat childhood depression.

Citalopram

Overdose with SSRIs does not usually cause cardiac arrhythmias, with the exception of ______, which may cause QT prolongation.

fluoxetine

the lowest risk of causing an SSRI discontinuation syndrome due to its longer half-life and active metabolite.

SNRIs

These agents, termed _____, may be effective in treating depression in patients in whom SSRIs are ineffective.

Venlafaxine, desvenlafaxine, levomilnacipran, and duloxetine

inhibit the reuptake of both serotonin and norepinephrine

Venlafaxine

is a potent inhibitor of serotonin reuptake and, at medium to higher doses, is an inhibitor of norepinephrine reuptake.

norepinephrine

Venlafaxine is a potent inhibitor of serotonin reuptake and, at medium to higher doses, is an inhibitor of ______ reuptake.

Desvenlafaxine

the active, demethylated metabolite of venlafaxine.

Duloxetine

inhibits serotonin and norepinephrine reuptake at all doses.

milnacipran

an older SNRI used for the treatment of depression in Europe and fibromyalgia in the United States

Levomilnacipran

an enantiomer of milnacipran

atypical antidepressants

mixed group of agents that have actions at several different sites.

Bupropion

weak dopamine and norepinephrine reuptake inhibitor that is used to alleviate the symptoms of depression.

Bupropion

useful for decreasing cravings and attenuating withdrawal symptoms of nicotine in patients trying to quit smoking.

Mirtazapine

enhances serotonin and norepinephrine neurotransmission by serving as an antagonist at presynaptic α2 receptors.

Mirtazapine

is markedly sedating, which may be an advantage in depressed patients having difficulty sleeping.

Nefazodone and trazodone

These drugs are weak inhibitors of serotonin reuptake. Their therapeutic benefit appears to be related to their ability to block postsynaptic 5-HT2a receptors. Both agents are sedating, probably because of their potent histamine H1-blocking activity.

Trazodone

is commonly used off-label for the management of insomnia. ______ has been associated with priapism

Nefazodone

has been associated with a risk for hepatotoxicity.

Vilazodone

a serotonin reuptake inhibitor and a 5-HT1a partial agonist.

Vortioxetine

utilizes a combination of serotonin reuptake inhibition, 5-HT1a agonism, and 5-HT3 and 5-HT7 antagonism

Tricyclic Antidepressant

block norepinephrine and serotonin reuptake

Maprotiline and amoxapine

are related “tetracyclic” antidepressant agents and are commonly included in the general class of TCAs.

TCAs and amoxapine

are potent inhibitors of the neuronal reuptake of norepinephrine and serotonin

Maprotiline and desipramine

relatively selective inhibitors of norepinephrine reuptake.

TCAs

block serotonergic, α-adrenergic, histaminic, and muscarinic receptors.

Amoxapine

blocks 5-HT2 and dopamine D2 receptors.

desmopressin

Imipramine has been used to control bed-wetting in children older than 6 years of age; however, it has largely been replaced by _____

Amitriptyline

have been used to help prevent migraine headache and treat chronic pain syndromes

Doxepin

Low doses of TCA, especially ____, can be used to treat insomnia

Imipramine

Nortriptyline

______ is the most likely, and ______ the least likely, to cause orthostatic hypotension.

Monoamine oxidase (MAO)

a “safety valve” to oxidatively deaminate and inactivate any excess neurotransmitters

Selegiline

also used for the treatment of Parkinson’s disease. It is the only antidepressant available in a transdermal delivery system.

phenelzine

Most MAOIs, such as _____, form stable complexes with the enzyme, causing irreversible inactivation.

Selegiline and tranylcypromine

have an amphetamine-like stimulant effect that may produce agitation or insomnia.

Phentolamine and prazosin

are helpful in the management of tyramine-induced hypertension.

2 weeks

Both SSRIs and MAOIs require a washout period of at least ______ before the other type is administered

6 weeks

Both SSRIs and MAOIs require a washout period of at least 2 weeks before the other type is administered, with the exception of fluoxetine, which should be discontinued at least ______ before a MAOI is initiated.

Lithium salts

used acutely and prophylactically for managing bipolar patients.

Lithium

is effective in treating 60% to 80% of patients exhibiting mania and hypomania.

carbamazepine, valproic acid, and lamotrigine

antiepileptic drugs

carbamazepine, valproic acid, and lamotrigine

have been approved as mood stabilizers for bipolar disorder.

risperidone, olanzapine, ziprasidone, aripiprazole, asenapine, and quetiapine

The atypical antipsychotics ____, ____, ____, ____, ____, ____ are also used for the management of mania.