Mod 5: CNS 2&3 - Anxiolytics, Antipsychotics, and Antidepressants

Vocabulary flashcards covering Central Nervous System pharmacology, including anxiolytics, hypnotics, antipsychotics, lithium, and antidepressants.

Benzodiazepines

Drug class that acts on GABA-A receptors in the thalamus, limbic structure, and cerebral cortex to inhibit the action of GABA, commonly used for short-term anxiolytic or sedative effects.

Benzodiazepine Black Box Warning

Warning regarding concomitant use with opioids, as well as the potential for addiction, abuse, misuse, and physical withdrawal.

Triazolam (Halcion)

A benzodiazepine indicated for sleep disorders requiring renal/hepatic dosing adjustment, used off-label for pre-procedure mild sedation.

Barbiturates

Drug class that depresses neuronal activity in the midbrain reticular formation, prolonging GABA-mediated chloride ion channel opening, blocking glutamic acid, and causing respiratory depression.

Phenobarbital

A long-acting (days) barbiturate indicated for status epilepticus, seizure disorder, sedation, and off-label for alcohol withdrawal.

Buspirone

A selective, nonsedating anxiolytic that acts as a full 5-HT agonist with some dopamine receptor activity, requiring weeks to achieve therapeutic effect and lacking anticonvulsant or muscle relaxant properties.

Melatonin Receptor Agonists

Drug class including Ramelteon and Tasimelteon that decreases latency of sleep onset with minimal rebound insomnia or withdrawal symptoms.

Orexin Receptor Antagonists

Drug class including Suvorexant (Belsomra), Lemborexant (Dayvigo), and Daridorexant (Quviviq) that induces sleep by blocking orexin receptors.

Nonbenzodiazepine Benzodiazepine Receptor Agonists (Z-drugs)

Agonists at the benzodiazepine receptor (e.g., Zaleplon, Zolpidem, Eszopiclone) indicated for short-term insomnia that carry a Black Box warning for complex sleep behaviors.

First-Generation Antipsychotics

Antipsychotic agents that reduce hallucinations and delusions primarily by blocking dopamine D2 receptors in the brain.

Low Potency First-Generation Antipsychotics

Agents such as Chlorpromazine and Thioridazine characterized by anticholinergic effects and fewer extrapyramidal side effects (EPSE).

High Potency First-Generation Antipsychotics

Agents such as Fluphenazine, Thiothixene, and Haloperidol that frequently cause extrapyramidal side effects (EPSE).

Clozapine (Clozaril)

Second-generation antipsychotic associated with agranulocytosis requiring weekly WBC monitoring for $6\,\text{months}$ then biweekly if stable, along with risk of weight gain, seizures, drooling, and hyperthermia.

Risperidone (Risperdal)

Second-generation antipsychotic requiring slow titration due to orthostasis, which carries an increased risk of EPSE at doses greater than $6\,\text{mg}$ daily.

Ziprasidone (Geodon)

Second-generation antipsychotic associated with orthostatic hypotension, minimal weight gain, and QT prolongation.

Cariprazine (Vraylar)

Second-generation antipsychotic with preferential D3 receptor affinity and higher $5\text{-HT}_A$ than D2 receptor affinity.

Lithium

Bipolar disorder agent with a $20\text{-hour}$ half-life whose serum levels increase with dehydration, NSAIDs, ACE inhibitors, and loop diuretics, and decrease with caffeine and theophylline.

Monoamine Oxidase Inhibitors (MAOIs)

Third-line antidepressants that inhibit MAO-A and MAO-B, requiring strict avoidance of tyramine-rich foods and specific sympathomimetics to prevent hypertensive crisis.

Tranylcypromine (Parnate)

An MAOI that carries Black Box warnings for both suicidality and hypertensive crisis.

Tricyclic Antidepressants (TCAs)

Antidepressant class structurally similar to phenothiazines that inhibits serotonin and norepinephrine reuptake, lowers seizure threshold, and causes anticholinergic, sedative, and cardiac side effects.

Clomipramine (Anafranil)

Tricyclic drug indicated specifically for OCD rather than depression.

Selective Serotonin Reuptake Inhibitors (SSRIs)

Antidepressants that decrease presynaptic serotonin reuptake, take $4\text{ to }8\,\text{weeks}$ for peak effect, and are contraindicated with MAOIs.

Citalopram (Celexa)

SSRI associated with QT prolongation that should be avoided in patients with bradycardia, hypokalemia, hypomagnesemia, recent MI, or uncompensated HF.

Paroxetine (Paxil)

Potent CYP2D6-inhibiting SSRI associated with an increased risk of fetal heart defects when taken in the first trimester.

Duloxetine (Cymbalta)

SNRI and moderate CYP2D6 inhibitor that has less effect on blood pressure but should be avoided in renal/hepatic impairment, alcohol abuse, and angle closure glaucoma.

Bupropion

Atypical antidepressant chemically similar to amphetamines that inhibits dopamine and norepinephrine reuptake, lowers seizure threshold, and is contraindicated in eating disorders and seizure disorders.

Dextromethorphan-Bupropion

Atypical antidepressant combination where bupropion inhibits CYP2D6 metabolism to extend the half-life and duration of action of dextromethorphan.

Mirtazapine

Tetracyclic atypical antidepressant that increases release of norepinephrine and serotonin, causing increased appetite and sedation.

MAOIs

Isocarboxazid, Phenelzine, Tranylcypromine, Selegiline

Tricyclics and Tetracyclics

Nortriptyline, Imipramine, Desipramine, Amitriptyline, Clomipramine, Doxepin, Trimipramine, Amoxapine, Protriptyline

SSRIs

Citalopram, Escitalopram, Fluoxetine, Fluvoxamine, Paroxetine, Sertraline

SNRIs

Duloxetine, Desvenlafaxine, Venlafaxine, Levomilnacipran, Milnacipran