04 - Psychiatric and CNS Drugs Flashcards by Helen Wang

SSRI work by increasing the amount of _____ in the synapse

Serotonin

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Most broadly prescribed class of antidepressants

SSRI

Also used for anxiety, OCD, social phobia, PTSD

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Examples of SSRIs

Fluoxetine
Sertraline
Paroxetine
Escitalopram

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Side effects of SSRIs

Insomnia
Agitation
Headache
Nausea
Diarrhea
Sexual dysfunction
Platelet dysfunction

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SSRI inhibit which hepatic cytochrome? This increase levels of

P450 (esp fluoxetine)

Increases levels of TCA, some neuroleptics, and antiarrhythmics (metoprolol)

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SSRIs can potentially cause ______ especially together with MAOIs, carbamazepine, or Linezolid (abx)

SEROTONIN SYNDROME

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Is overdose on SSRIs lethal?

Not typically

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Other commonly used antidepressants inhibit the reuptake of

Other neurotransmitters (dopamine, NE)

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Venlafaxine and bupropion side effects

Venlafaxine - minimal anticholinergic effect, hypotension

Bupropion - less sexual dysfunction, hypotension; also smoking cessation

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TCAs are highly effective but have poor

Side effect profiles

Anticholinergic (dry mouth, tachycardia, urinary retention, GI slowing)
Orthostatic hypotension, PR prolongation, cardiac depression
Sedation, lowered seizure threshold

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Is overdose on TCAs lethal?

Yes, it has a narrow therapeutic index

Myocardial depression, ventricular dysrhythmias

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Overdose on TCA can cause threat up to ____ days even after the comatose phase resolves

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At low doses, TCAs are commonly used for

Chronic pain syndromes

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TCAS work by blocking the reuptake of

NE (and sometimes serotonin)

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TCAs have ____ protein binding. What drugs can affect the protein binding of TCAs?

Strong

Phenytoin
Aspirin

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Examples of TCAs?

Amitriptyline
Nortriptyline
Imipramine
Clomiprimine

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Drug interactions with TCAs are related to their ____ effects and _____ uptake-blocking actions

Anticholinergic

Catecholamine

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With sympathomimetics, TCAs have exaggerated ____ response! especially with _____ agents. When is this not true?

Pressor
Indirect-acting agents

May have attenuated response with chronic TCA users

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Increases likelihood of postoperative delirium when used with TCAs

Atropine

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How do TCAs affect opioids and barbs?

Potentiates

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MAO is an enzyme that metabolizes

Catecholamines (monoamines)

Dopamine, serotonin, NE, Epi

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MAO subtype that metabolizes serotonin, NE, epi, and tryamine

MAO-A

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MAO-A and ____ leads to the formation of ____ which is seen in pheochromocytoma

COMT

Vanillylmandelic acid

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MAO subtype that metabolizes tyramine

MAO-B

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T or F? Most MAOIs are reversible and nonselective inhibitors

FALSE, irreversible and nonselective

Examples of MAOIs

Phenelzine Tranylcypromine Isocarboxazid Selegiline (Parkinson's)

Rarely used due to side effects and complex dosing

MAOIs

Some side effects of MAOIs?

``` Orthostatic hypotension Sexual dysfunction Weight gain Anticholinergic Sedation ```

Do MAOIs cause dysrhythmias?

If you take MAOIs, you should avoid ____ in your diet because it can lead to ______ response (like pheo!!!)

Tyramine Indirect sympathetic response Avocados, cheese, liver, fava beans, chianti

MAO-B inhibitors (selegiline) require no dietary restriction except at

Very high doses Because most tyramine is deaminated by MAO-A

Overdose of MAOIs is

Lethal Tachy, hyperthermia, hypermetabolism (rigidity), seizures, coma

A suggested treatment for MAOI overdose

Dantrolene

Should MAOIs be stopped 2-3 weeks before anesthesia?

No data to support

Sympathomimetics should be used ____ in conjunction with MAOIs. Consider using _____ > ______

With caution | Direct > indirect

Avoid using ____ with MAOIs during local/regional anesthetics

Epinephrine

Can cause excitatory OR depressive reactions with MAOIs

Opioids, mostly with meperidine

Lithium is the treatment of choice for ____ but requires measurement of

Bipolar disorder | Plasma concentrations

Lithium is filtered by the kidneys and reabsorbed in the

Proximal tubule (competes with Na)

Na depletion (dehydration, diuretics) can ____ lithium levels

INCREASE

Side effects of lithium

Polydipsia Polyurethane Hypothyroidism

Lithium causes a prolonged response to

Depolarizing and nondepolarizing NMB

Avoid using _____ with lithium

Diuretics (loop, thiazide) | NSAIDs

Lithium used with neuroleptic drugs increase risk of ____ side effects and

Extrapyramidal | NMS

Lithium toxicity is exacerbated by

Dehydration Na restriction Diuretics NSAIDs

Sever lithium toxicity may require

Osmotic diuresis or dialysis

Effects of lithium toxicity

``` Lethargy Weakness QRS widening Heart block Hypotension Confusion Seizures ```

Used for treatment of schizophrenia or bipolar disorder

Antipsychotic drugs (neuroleptics)

Examples of antipsychotic drugs

``` Chloropromazine (thorazine) Clozapine (clozaril) Haloperidol (haldol) Risperidone (risperdal) Droperidol ```

Antipsychotic drugs work by blocking ____ receptors

Dopamine

One side effect of all neuroleptics except _____ is _____, which are movement disorders

Clozapine | Extrapyramindal effects

Tardive dyskinesia is the abnormal, _____ movement of

Involuntary Face, neck, tongue Caused by neuroleptics

Acute dystonic reaction is acute muscle _____ in the face, neck, tongue and

Rigidity/clamping Larynx Caused by neuroleptics

What is the treatment for acute dystonic reaction?

Diphenhydramine Benztropine These are anticholinergics

Other extrapyramidal effects caused by neuroleptics?

Parkinsonism - rigidity, tremor, bradykinesia/akinesia | Akathesia - restlessness

Neuroleptic malignant syndrome causes rigidity that may lead to _____ and renal failure (myonecrosis)

Ventilators requirement

Symptoms of NMS?

Hyperthermia Muscular hypertonicity Autonomic instability Mental status changes

What is the incidence and mortality of NMS?

Incidence: 0.5-1% Mortality: 20-30%

Treatment for NMS?

Dantrolene (relax muscles) | Amantadine/bromocriptine (dopamine agonists)

Nondepolarizing NMBs will cause _____ in NMS but not in MH

Flaccid paralysis

Neuroleptics cause alpha blockade, which leads to these side effects?

``` Orthostatic hypotension Prolonged QTc (->VTach) ```

Neuroleptics block the inhibition of prolactin, causing

Galactorrhea | Gynecomastia

Neuroleptics decrease corticotropin release, leading to

Decreased corticosteroids

Weight gain and hyperglycemia are side effects of

Neuroleptics

CNS effects of neuroleptics

Sedation, antiemetic, dysphoric response (droperidol)

Which neuroleptic causes agranulocytosis?

Clozapine

How do neuroleptics affect opioids?

Potentiate on

Best drugs to stop a seizure QUICKLY

Barbs Benzos Propofol

Which channel does phenytoin block?

Na Also Ca and NMDA

What percent of phenytoin is protein bound? Caution with

90% | Hypoalbuminemia

Therapeutic serum level of phenytoin?

10-20 mcg/mL

Phenytoin levels can be increased by

Amiodarone Fluconazole Isoniazid Coumadin

Phenytoin levels can be decreased by

``` Chronic alcohol Antineoplastics Phenobarbital Diazepam Calcium ```

Phenytoin is metabolized by hepatic enzymes with ____ kinetics at high plasma levels

Zero order

Side effects of phenytoin?

CNS - nystagmus, ataxia, NV Gingival hyperplasia Teratogen

How can you avoid hypotension with phenytoin?

Slow infusion <50 mg/min Can precipitate

What can you infuse more quickly without hypotension than phenytoin?

Fosphentoin - prodrug

Levetiracetam (keppra)

Unknown mechanism No significant side effects, no hepatic metabolism, min protein binding Decreased dosing in renal

Gabapentin is most commonly used for

Chronic neuropathic pain, diabetic neuropathy Requires multiple daily doses No protein binding, no hepatic metabolism

Medication used for Parkinson's?

Levodopa

Levodopa is a dopamine precursor that unlike dopamine can cross

Blood brain barrier

What converts levodopa to dopamine?

Dopa carboxylase

Levodopa is up usually given with ____ to prevent decarboxylation before crossing the BBB

Carbidopa

Levodopa does not cause orthostatic hypotension

False

Abrupt cessation of levodopa causes

Parkinsonian symptoms, NMS Dr. Altose asks, "when was your last dose and what happens if you miss a dose?"

You may need to give levodopa _____ via NG

Intraoperatively

Can cause skeletal rigidity when used with levodopa

Haloperidol, droperidol Due to dopamine antagonism Usually avoid metoclopramide and promethazine

How does levodopa act with anticholinergic drugs?

Synergistically

Dopamine agonists at such ad bromocriptine and pergolide are used for

Parkinson's disease

Anticholinergic drugs (benzotropine) restore ______ balance with Parkinson's. They help with _____ and salivation but very little with

Ach/dopamine Tremor and salivation Rigidity

Amantadine may facilitate _____ release and delay ____? What is it used for?

Dopamine Reuptake Parkinson's

MAO-B inhibitor that can be used for Parkinson's treatment?

Selegiline - not involved and NE metabolism