Antidepressants & Antipsychotics Flashcards by K W

What are the 3 mechanisms of termination of NT synaptic activity?

Reuptake
Enzyme degradation
Diffusion

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What are the two types of biogenic amines?

ACh and Monoamines

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What are the two types of monoamines?

Serotonin and Catecholamines

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What are the 3 types of catecholamines?

NE, epi, DA

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What adverse effects are caused by blocking the DA2 receptor? (2)

EPS AE

Prolactin release

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What are the AEs caused by blocking the H1 receptor?

Sedation, impaired cognition

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What AEs are caused by blocking the M1 receptor?

Opposite of DUMBBELSS (Constipation, urinary retention, blurred vision, closed-angle glaucoma, tachycardia, hypomania, dry mouth/eyes, hypohidrosis) and altered cognition

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What AEs are caused when blocking the alpha 1 adrenergic receptor?

Orthostatic hypotension, reflex bradycardia

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Name 2 tricyclic antidepressants (TCAs).

Amitriptyline, nortriptyline

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What is the MOA of TCAs?

Blocks NE and 5-HT uptake into presynaptic nerve terminal

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Common indications for TCAs?

Depression unresponsive to SSRIs and SNRIs, insomnia, various pain syndromes

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Name all receptors blocked by TCAs (besides blocking NET and SERT).

M1, H1, alpha 1 adrenergic

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Name common TCA AEs (3)

Lower seizure threshold
Serotonin syndrome
Cardiac toxicity (Prolonged QT, cardiac depression, life-threatening arrhythmias with OD)

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Describe TCA OD.

LD 8x average dose.
Symptoms - cardiotoxicity, seizures, respiratory depression, hypotension.
Arrhythmias can persist 10 days b/c t1/2 ~81 hours.

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Name 4 drug classes with which TCAs can interact.

CNS depressants (ex., opioids)
Other serotonergic drugs
Sympathomimetics (hypertension with ex., epi)
Antimuscarinics (delirium, confusion, hypotension)

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MOA of SSRIs?

Inhibit 5-HT reuptake transporter (SERT).

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Why do SSRIs have a lower risk of AEs than TCAs?

No/minor blockade of H1, ACh, and NE receptors; also less risk of cardiac toxicity/death

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Name 7 common SSRIs.

Fluoxetine, fluvoxamine, citalopram, escitalopram, sertraline, paroxetine

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State 2 points regarding SSRI pharmacokinetics.

Metabolized in liver

Variable 1/2 lives (around 20-24 hours). EXCEPTION: fluoxetine 4-9 days.

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Name 8 SSRI AEs

Serotonin syndrome
Hyponatremia
Withdrawal syndrome
Bleeding
Sweating
Nausea/diarrhea
Sexual dysfunction

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Describe the s/s, time frame, and management of serotonin syndrome.

Agitation, confusion, hyperreflexia, clonus, diaphoresis, autonomic instability, fever, death
2-72 hours after treatment initiation
Discontinue drug and provide supportive care

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Name 3 MOAs that can cause serotonin syndrome through DDIs

Drugs that decrease 5-HT reuptake (antidepressants, opioids, ondansetron, meth/coke)
Direct 5-HT receptor stimulators (triptans)
DDIs involving CYP enzymes

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Which SSRIs affect CYP enzymes and in what way?

Fluoxetine and fluvoxamine INHIBIT CYP enzymes

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Which SSRI is least likely to cause withdrawal syndrome?

Fluoxetine due to long t1/2

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MOA of SNRIs?

Blocks SERT and NET activity

What aspect of SNRI MOA makes this class effective for treating pain syndromes?

NET blockade (on label for duloxetine)

Patients are at risk for what AE after taking SNRIs in addition to those imposed by SSRIs?

Hypertension (lower risk with duloxetine than venlafaxine)

Name 2 SNRIs.

Venlafaxine, duloxetine

Which atypical antidepressant does NOT cause sexual dysfunction?

Bupropion (Wellbutrin)

Major mechanism of bupropion?

Increase synaptic NE and DA activity (block NET and DAT and increase their release); noncompetitive antagonist of nicotinic receptors

Indications for bupropion?

Depression, smoking cessation

Bupropion AEs?

``` CNS stimulation (agitation, insomnia, tremor) DECREASED seizure threshold NO sexual dysfunction! ```

What serotonin modulator is mainly used as a hypnotic?

Trazodone

MOA of trazodone?

Blocks 5-HT2 receptors, H1, and alpha 1 adrenergic receptors; inhibits SERT at high doses

AEs of trazodone? (2)

Priapism | Postural hypotension

A 29-year-old male veteran with a 2-month history of progressively worsening lower back pain was admitted for revision of a discectomy. His routine medications included fluoxetine (Prozac) and tramadol (Ultram). His perioperative medications included several opioids. One hour after return to his room he was found to be agitated , hypertensive, diaphoretic and with spontaneous clonus. He was subsequently diagnosed with the serotonin syndrome. ``` Which opioid is most likely to have triggered this response? A. Morphine B. Hydromorphone (Dilaudid) C. Oxycodone (Oxycontin) D. Fentanyl (Duragesic) ```

SSRI/SNRI will generally be (continued/discontinued) perioperatively unless ...? In which case...?

continued; the patient is a high risk for bleeding; SSRI will be held

TCAs may be DC's perioperatively depending on __ risk

Drugs with what centrally-acting receptor can increase post-op confusion and delirium?

Muscarinic

Drugs blocking what receptor may decrease GI motility and cause urinary retention postoperatively?

Muscarinic

Where in the body are MAO enzymes active?

Gut, liver, and CNS

Monoamine oxidase inactivates what NTs?

5-HT, NE, DA

What does MAO-A inactivate?

NE, 5-HT, and dietary tyramine

What does tyramine cause? In the presence of MAOIs?

Release of NE from nerve terminals; dangerous hypertension

What does MAO-B do? What condition are MAO-B inhibitors used to treat?

Inactivates DA; Parkinson's

Name some nonselective MAO irreversible inhibitors. (3)

Phenylzine, tranylcypromine, selegiline

What is unique about selegiline?

Available as a patch for depression | Also, lower concentrations mainly inhibit MAO-B for Parkinson's

Why are MAOIs reserved for refractory or atypical depression?

The potential for life-threatening interactions with tyramine-containing foods (but less likely with selegeline patch)

Discuss MAOI impact on blood pressure (2)

Orthostatic hypotension at normal doses Hypertensive crisis with tyramine-containing foods (aged meats/cheese, wine/beer, yeast extracts, cured fish, fermented soybeans)

Name 3 DDIs for MAOIs and their effects.

Sympathomimetics - increased hypertension Other serotonergic drugs - serotonin syndrome Meperidine - hyperpyrexia

What factors can increase risk of lithium toxicity?

Low sodium leading to the retention of chemically-similar lithium Renal impairment Pregnancy/lactation - teratogenic

DDIs with lithium?

``` NSAIDs ACEIs ARBs Thiazide diuretics (All of the above will decrease lithium excretion) ```

What are common AEs with normal levels of lithium?

GI efx, thirst, cardiac efx, tremor, polyuria

What are uncommon AEs with normal levels of lithium?

Hypo/hyperthyroidism, renal damage, leukocytosis, dermatologic reactions

What are AEs with toxic levels of lithium?

Tremor, ataxia, convulsions, hypotension, arrhythmias, coma, death

What commonly used anesthetic drug may be prolonged by lithium?

NM blockers

What labs should be checked perioperatively if the patient is on lithium?

Lithium levels, electrolyte levels, and thyroid hormone | Also maintain adequate hydration

A 57-year-old woman complains of persistent pain associated with fibromyalgia. She has lost interest in most her hobbies and often feels despondent. Which of the following medications is most likely to address her pain and depression? ``` A. Citalopram (Celexa) B. Bupropion (Wellbutrin) C. Duloxetine (Cymbalta) D. Selegiline (Emsam) E. Phenelzine (Nardil) ```

What is a non-psychiatric indication for antipsychotics?

Antiemetic

What kind of antipsychotics most effectively treat positive schizophrenia symptoms?

Conventional OR atypical

What class of antipsychotics most effectively treats negative symptoms of schizophrenia?

Atypical antipsychotics

Cognitive symptoms of schizophrenia are NOT worsened by what kind of antipsychotics?

Atypicals

What about the MOA of 1st generation antipsychotics (FGAs/neuroleptics) make them more likely to cause movement disorders than 2nd generation (SGAs/atypicals)?

FGAs have a higher affinity for DA2 receptor; SGAs moderately block 5-HT2 receptors and rapidly dissociate from DA2.

What other receptors are blocked by FGA and SGAs?

Alpha 1 adrenergic, muscarinic, and histamine

What is the MOA of the 3rd generation antipsychotic Abilify?

Dopamine system stabilizer - DA partial agonist; also 5-HT2 receptor antagonist

What lower potency 1st generation antipsychotic places the patient at higher risk for sedation, hypotension, and antimuscarinic effects?

Chlorpromazine

What medium potency antipsychotic is used primarily as an antimetic?

Promethazine

What high potency SGAs place the patient at a lower risk of sedation but a higher risk of EPS symptoms?

Haloperidol | Droperidol

What is a severe AE of antipsychotics caused by insufficient dopamine?

Acute dystonia (severe muscle spasm including torticollis, oculogyric crisis, trismus)

How is acute dystonia treated?

Centrally acting antimuscarinic (benztropine) and diphenhydramine

What is late-occurring EPS termed?

Tardive dyskinesia (oral, facial dyskinesias, lip smacking, choreoathoid movements)

What are some adverse effects common to all classes of antipsychotics?

Reduced seizure threshold Prolonged QT/related arrhythmias Neuroleptic malignant syndrome

What are risk factors for prolonged QT interval? (5)

Bradycardia, HF, prior MI, hypokalemia, hypomagnesemia

What commonly-used perioperative drug is most likely to cause QT prolongation?

``` Amiodarone Others (inhaled anesthetics, antiemetics, methadone) ```

What antipsychotics are most associated with prolonged QT? (3)

``` Haloperidol (esp. IV) Droperidol Ziprasidone (Geodon) ```

What s/s characterize neuroleptic malignant syndrome?

Fever, "lead-pipe" rigidity, dysautonomia, altered mental status

What dopamine blockers are most implicated in NMS?

FGA, SGA, D2 antagonist emetics, and dopaminergic withdrawal

Compare and contrast onset of SS and NMS.

Within 24 hours and within days, respectively

Compare and contrast NM findings with SS and NMS.

Hyperreactivity (tremor, clonus, reflexes) and bradyreflexia/severe muscular rigidity, respectively

Compare and contrast causative agents of SS and NMS.

Serotonin agonist and dopamine antagonist

Compare and contrast resolution timeline of SS and NMS

Within 24 hours and days to weeks, respectively

Describe 5 antipsychotic DDIs.

Epinephrine - blunted pressor effect with drugs that cause alpha blockade (such as chlorpromazine) Antimuscarinics (additive) CNS depressants (additive) Levodopa (since it is metabolized to DA, antipsychotics will antagonize the effects - watch for psychosis) Dopamine (decreased DA effectiveness)

Name 4 second generation antipsychotics

Olanzapine Ziprasidone Risperidone Quetiapine

Why are SGAs preferred over FGAs?

They relive both positive and negative symptoms and generally have a lower SE profile

SGAs carry an increased risk of _________ AEs over FGAs.

metabolic - hyperglycemia, dyslipidemia

Which antipsychotic carries the highest risk of prolonged QT?

Ziprasidone

What is the 3rd generation antipsychotic/DA system stabilizer?

Aripiprazole (Abilify)

``` A patient that received promethazine (Phenergan) for post-operative nausea suddenly develops a sustained, involuntary muscle contraction involving the neck. Which of the following would most likely be used to treat this reaction? A. Diphenhydramine (Benadryl) B. Chlorpromazine (Thorazine) C. Dantrolene (Dantrium) D. Lorazepam (Ativan) ```

``` A 58-year-old man with a history of schizophrenia, generalized anxiety disorder and bradycardia is in the PACU following an appendectomy. He has received ondansetron and droperidol perioperatively. He took his home medications the day of surgery. Which of the following is most likely to increase his risk of arrhythmia? A. Aripiprazole (Abilify) B. Ziprasidone (Geodon) C. Sertraline (Zoloft) D. Duloxetine (Cymbalta) ```

Antidepressants & Antipsychotics Flashcards

(89 cards)