Chapter 14: Serotonergics Flashcards by Sonya Narla

Name the inhibitors of serotonin storage (displace 5-HT, DA, and NE from storage vesicles)

Modafinil
Dextroamphetamine 
Lisdexamfetamine
Amphetamine
Methylphenidate

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Name the drugs that inhibit MAO, increase 5-HT and NE availability in the presynaptic

Iproniazid
Phenelzine
Isocarboxazid
Selegiline

Moclobemide
Befloxatone
Brofaromine

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Name the tricyclic antidepressants (TCAs)

AmiTRIPtyline (and other -triptylines)
Clomipramine
Imipramine
Doxepin

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What is the MOA of TCAs?

Inhibit re-uptake of 5-HT and NE from the synaptic cleft….by blocking 5-HT and NE re-uptake transporters

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Name the SSRIs

Citalopram
Fluoxetine
Fluvoxamine
Praxoetine
Sertraline

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What is the MOA of SSRIs?

selectively block 5-HT transporters (similar to TCAs, but way more selective so have less side effects)

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MOA of SNRIs - compare to SSRIs

Block 5-HT re-uptake transporters and NE re-uptake transporter….SSRIs = just serotonin

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Name the SNRIs

Venlafaxine
Duloxetine
Desvenlafaxine
Milnacipram

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Name the NRIs

Atomoxetine

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Bupropion MOA?

weakly inhibits neuronal uptake of 5-HT, dopamine, and NE

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Mirtazapine MOA?

blocks 5-HT 2 receptors and alpha-2 autoreceptor

–> decrease 5-HT2 synapse neurotransmission while increasing NE neurotransmission

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MOA of nefazodone and trazodone

block postsynaptic 5-HT2 receptors

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Name the serotonin receptor AGONISTS

Buspirone
SumaTRIPTAN
RizaTRIPTAN
and other TRIPTANs

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Name the serotonin receptor ANTAGONISTS

Ketanserin
OndanSETRON
Tegaserod
Prucalopride
AloSETRON

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MOA of Lithium

Blocks regeneration of PIP2 –> inhibits adrenergic, muscarinic, and serotonergic neurotransmission

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What is the major route of excretion of lithium?

Kidneys

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Patients being treated with lithium, who are dehydrated, or taking diuretics concurrently, could develop

Lithium toxicity, lithium-induced nephrogenic diabetes insipidus

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Drug increases the renal clearance hence decreases levels of lithium

theophylline

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Lithium is associated with this congenital defect

Cardiac anomalies and is contraindicated in pregnancy or lactation

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Lithium side effects?

Tremor, sedation, ataxia, aphasia = acute lithium intoxication

Hypothyroid and Goiter

Reversible diabetes insipidus

EEG and ECG abnormalities

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Acute lithium toxicity is a medical emergency and may require _____ for treatment

dialysis

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_____ or _____ can lead to increased Lithium reabsorption in the _____ ______ = increased plasma lithium

NSAIDs or hyponatremia

Proximal tubule

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Lithium clinical application?

Bipolar - drug of choice

Has been shown to reduce suicide risk!

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Inhibitor of MAO type B which metabolizes dopamine, used adjunct to levodopa or as sole agent in newly diagnosed pt’s

Selegiline

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Example of three antidepressants that are indicated for obsessive compulsive disorder

Clomipramine, fluoxetine and fluvoxamine

TCA used in obsessive compulsive disorder (OCD), most significant of TCA's for ________

Clomipramine | Risk of seizure, weight gain, and neuropsychiatric signs and symptoms

Sedation is a common side effect of these drugs, they lower seizure threshold, uses include BAD, acute panic attacks, phobias, enuresis, and chronic pain and their overdose can be deadly

TCAs

Three Cs of TCA toxicity

Coma, Convulsions, Cardiac problems (arrhythmias and wide QRS)

What should you do before starting TCAs??

ECG - rule out conduction system disease first

TCA used in chronic pain, a hypnotic, and has marked antimuscarinic effects

Amitryptyline

TCA used in chronic pain, enuresis, and OCD

Imipramine

TCA with greatest sedation of this group, and marked antimuscarinic effects, used for sleep

Doxepin

Significant adverse effects of TCAs in elderly patients?

Orthostatic hypotension

SSRIs have a ____ therapeutic index than TCAs, making them ____ toxic.

higher therapeutic index = less toxic

What is serotonin syndrome?

Caused by SSRI + MAOI = | hyperthermia, mm rigidity, myoclonus, rapid fluctuations in mental status and vital signs

Major adverse effects of SSRIs

Serotonin syndrome May precipitate mania in a bipolar patient Sexual dysfunction Vasospasm

SSRI discontinuation syndrome = ?

anxiety, GI flu symptoms, insomnia, depersonalization, and frank suicidality

Except for these agents all SSRI have significant inhibition of CytP450 enzymes

Citalopram and its metabolite escitalopram

SSRI's less likely to cause a withdrawal syndrome

Fluoxetine

SSRI with long T1/2 and can be administered once weekly for maintenance, not acute tx

Fluoxetine

SSRI indicated for premenstrual dysphoric disorder

Fleuxetine

Well-tolerated and are first-line antidepressants

SSRIs, buproprion, and venlafaxine

Usual time needed for full effect of antidepressant therapy

2-3 weeks

What are the first line agents for tx of depression, anxiety, and OCD?

SSRIs

Using MAOs with foods high in tyramine can cause what...?

Hypertensive crisis

Drugs used to treat ADHD?

Amphetimine Methyphenidate Dextroamphetamine Lisdexamfetamine

Unicyclic antidepressant least likely to affect sexual performance, used for management of nicotine withdrawal, SE's include dizziness, dry mouth, aggravation of psychosis, and seizures

buproprion

How does venlafaxine act differently at low and high concentrations?

Low - SSRI | High - increase NE levels

What class of drugs should be used to medically complicated or fragile patients? (Example: depression with comorbidity or psych disorder)

SNRIs!!!!!!

SNRI used to treat fibromyalgia?

Milnacipran

Why would you potentially use Atomoxetine over amphetamines for ADHD?

Lower abuse potential and a longer half life (once daily dosing)

Side effects of atomoxetine?

Heart stuff - MI, prolonged QT, sudden cardiac death

Drug used to help with smoking cessation. What is the MOA?

Buproprion inhibits uptake of 5HT, DA, NE

DO NOT USE buproprion in patients with ____

seizure electrolyte abnormalities bulimia/anorexia MAOI

Drugs used to treat migraine headaches?

TRIPTANS

Non sedating, non addictive drug used to treat anxiety =

buspirone

Serotonin receptor antagonist used to treat nausea

ondansetron - 5HT -3 antagonist

Serotonin receptor antagonists used to treat irritable bowel syndrome with constipation predominance?

tegaserod | prucalopride

Serotonin receptor antagonists used to treat irritable bowel syndrome with diarrhea predominance?

alosetron

5HT -1 signaling mechanism

decrease cAMP; increase K channel opening

5HT -2 signaling mechanism

increase IP3 and DAG

5HT -3 signaling mechanism

ligand gated ion channel - THE ONLY ONE!

5HT-4,6,7 signaling mechanism

increase cAMP

Chapter 14: Serotonergics Flashcards

(63 cards)