Pharm Mod 3 CNS

Amino acid building block of Serotonin.

Amino acid building block of NE.

With depression, there is decreased ______ and/or _______ neurotransmission

Purpose of serotonin or NE binding to autoreceptor.

SSRIs inhibit __________ back into the cell

When serotonin or NE is reuptaken into cell, what two things could happen?

After some time of treatment with antidepressants, _______ are downregulated.

Type of serotonin receptor responsible for improved mood.

Agonism of 5HT2 receptor (a SE of Serotoin) results in?

Agonism of 5HT3 receptor (a SE of Serotoin) results in?

SE of NE.

Off-target receptor effects of 5HT.

How do MAOIs work?

TCAs inhibit what?

SSRIs inhibit what?

Nonselective, irreversible MAOIs.

Nonselective, reversible MAOI.

Selective, reversible MAO-A inhibitors (RIMA).

_______ and _______ are irreversible against MAO-B, antagonizes both (transdermal patch)

Inhibition of MAO inhibits degradation of monoamines which increases available _______________

AE of MAOIs

PK of MAOI

MAOI DI

MAOIs are Hepatically metabolized to _______ metabolites which are subsequently hepatically _______ and _______ excreted

MAO-A inhibits degradation of __________.

MAO-B inhibits degradation of _________; at higher doses they can __________.

Foods high in tyramine (avoid with MAOIs)

How is tyramine toxicity avoided with MAOIs?

It could be dangerous to give MAOIs to what type of pt?

Doxepin (Sinequan)and Clomipramine (Anafranil) are what class of drugs?

Imipramine (Tofranil) is a ______ and is metabolized to ________.

What is the effect when Imipramine and Amitriptyline are metabolized (TCAs)?

Which TCAs have less AE and why?

______ amines have more effect on NE than 5HTP.

_________ amines (TCAs) have more effect on 5HTP than NE.

Amitriptyline (Elavil) is a _________ and is  metabolized to _________.

Doxepin (Sinequan)and Clomipramine (Anafranil) have more effect on ________ than _________.

Nortriptyline (Pamelor) and Desipramine (Norpramine) have more effect on ____ than on _______.

TCAs are very specific for ______ and ______ and do not have an effect on ________.

TCA's are used to treat _______ in low doses.

AE of TCAs (normally at higher doses).

TCAs antagonize ________ receptors which causes n/v, anorexia, dry mouth, blurred vision, confusion, constipation, tachycardia, urinary retention.

TCAs antagonize ________ receptors which causes sedation, wt gain, confusion.

TCAs antagonize __________ which causes orthostatic hypotension, reflex tachy, drowsiness, dizziness.

TCAs are substrates of CYP450, especially _______.

AEs of SSRIs.

Fluoxetine and paroxetine (SSRIs) are substrates and inhibitors of _______.

Sertraline (Zoloft) is metab by?

Two SSRIs with least DI potential.

What are the two SNRI's?

Venlafaxine (Effexor) is metabolized to active metabolite __________ by ________.

AE of Effexor (SNRI).

AE of Cymbalta (SNRI).

SNRI effective for depression and neuropathic pain.

Cymbalta is Metabolized by _________m

Bupropion (Wellbutrin) inhibits ______ and _____ reuptake.

CI to Bupropion.

Bupropion (Atypical Antidepressant) is hepatically metabolized by _______.

Why does Bupropion have the least sexual SE?

SE of Bupropion.

Mirtazapine (Remeron) antagonizes ______ and  _______ receptors more at higher doses and ________ receptors more at lower doses.

AE of Mirtazapine (Remeron) due to agonism of histamine.

How can you decrease the SE of the atypical antidepressant,  Mirtazapine (Remeron)?

Mirtazapine (Remeron) is a substrate of _______.

Nefazodone (Serzone) inhibits ______ transporter and antagonizes ______, causing less sexual dysfunction and has antianxiety properties.

Nefazodone (Serzone) antagonizes ________ and ________ receptors, causing sedation, & orthostasis.

AE of Nefazodone (Serzone).

Nefazodone (Serzone) is a substrate and inhibitor of ________.

Trazadone is used as an antidepressant only at _________ doses and as a sleep agent at _______ doses.

Which atypical antidepressant has the AE of priapism? What kind of dose causes this?

Trazadone is metabolized by ________.

Atypical antidepressant used for anxiety only.

Buspirone (Buspar) agonizes _______ receptor.

Two drugs used to tx narcolepsy.

TI of LIthium.

What can increase lithium levels? Why?

What is LIthium used to control?

Two drugs other than Lithium used to tx Bipolar.

AE of Lithium (generally w/ higher doses).

Half-life of Lithium.

Diuretics can confuse Lithium for _____ and result in ________.

How will Probenecid effect Lithium?

Triptans act as _______ agonists in vasculature, causing __________ of intracranial blood vessels.

What class of drugs is specific for migraine therapy?

Which triptan has the fastest onset of action? The longest?

__________ can significantly inhibit metabolism of rizatriptan (Maxalt).

Two triptans that can be administered as a nasal spray (important when pt has n/v).

CI of Triptans.

Most triptans are metabolized by _____, except for which ones? Why is this important?

Eletriptan is metabolized by ______ – do not administer within 72 hours of potent _______ inhibitors.

There is a risk of ____________ when triptans are used in combination with SSRIs and SNRIs.

_________ are 5HT1B/1D agonists.

Avoid Ergotamines in patients with _____________.

Ergotamine may be useful in patients with _________.

CI of DHE 45.

Benzamides butyrophenones, & phenothiazines are anti-emetics that antagonize __________.

Class of antiemetic drugs with least SE. Why?

5HT3 antagonists used as antiemetics.