Psychopharm: Sleep and Wakefulness

Comprehensive vocabulary flashcards covering sleep physiology, neurotransmitters, and the pharmacotherapy of insomnia, sleep apnea, RLS, narcolepsy, and circadian rhythm disorders.

Sleep Cycle

A biological unit of sleep lasting approximately $90$ minutes, through which humans cycle through various NREM and REM stages.

N3 Sleep

A stage of NREM sleep often referred to as deep or slow-wave sleep, essential for physical recovery and growth hormone secretion.

GABA (\gamma-Aminobutyric acid)

An inhibitory neurotransmitter crucial for initiating sleep by reducing neuronal excitability.

Orexin

Also called hypocretin; a neurotransmitter that promotes wakefulness, arousal, and motor activity.

Process S

The Homeostatic Sleep Drive, which reflects the accumulation of the need for sleep throughout prolonged wakefulness.

Process C

Circadian Rhythms governed by the suprachiasmatic nucleus (SCN), regulating the timing of sleepiness and wakefulness.

Benzodiazepine Mechanism of Action

Binds to $GABA_A$ receptors at allosteric sites, facilitating GABA action to increase the frequency of chloride ion ($Cl^-$) channel opening and lead to neuronal hyperpolarization.

Lorazepam (Ativan)

An intermediate-duration benzodiazepine with a half-life of $12$ hours that can be used in patients with hepatic impairment because it lacks CYP3A4 activity.

Triazolam (Halcion)

A short-acting benzodiazepine with a half-life of $1.5$ to $5.5$ hours, primarily used for sleep onset rather than maintenance.

Benzodiazepine Black Box Warning

Warns of the risk of respiratory depression, coma, and death when used concomitantly with opioid medications.

Non-Benzodiazepine Hypnotics (Z-drugs)

Medications like Zolpidem and Eszopiclone that enhance GABAergic neurotransmission by binding to specific subunits of the $GABA_A$ receptor complex, primarily used for sleep initiation.

Z-drug Black Box Warning

Rare but serious complex sleep-related behaviors, such as sleepwalking, which are contraindicated if they occur once within the class.

Ramelteon (Rozerem)

A highly selective melatonin receptor agonist that binds to $MT_1$ and $MT_2$ receptors in the suprachiasmatic nucleus to regulate circadian rhythms.

Tasimelteon (Hetlioz)

A melatonin receptor agonist specifically approved for Non-24-Hour Sleep-Wake Disorder, particularly in blind individuals.

Dual Orexin Receptor Antagonists (DORAs)

A class of medications, including Suvorexant and Lemborexant, that block $OX1R$ and $OX2R$ to diminish the wake drive.

Antihistamine Mechanism for Sleep

Blockade of $H_1$ histamine receptors in the brain, which leads to sedation because histamine is a wake-promoting neurotransmitter.

Modafinil (Provigil)

A medication providing wakefulness by targeting dopamine transporters; used as adjunctive therapy in sleep apnea and first-line for narcolepsy.

Dopamine Agonists in RLS

Commonly the first-line treatment for Restless Leg Syndrome; includes medications like Pramipexole, Ropinirole, and the transdermal patch Rotigotine.

Augmentation

The worsening of Restless Leg Syndrome (RLS) symptoms associated with long-term use of dopamine agonists.

Alpha-2-Delta Calcium Channel Ligands

A class including Gabapentin enacarbil and Pregabalin that inhibits calcium influx into neurons to stabilize membranes, used for RLS and neuropathic pain.

Sodium Oxybate (Xyrem)

A CNS depressant effective for both excessive daytime sleepiness (EDS) and cataplexy in patients with narcolepsy.

Pitolisant (Wakix)

A histamine $H_3$ receptor antagonist/inverse agonist that increases the release of histamine to treat narcolepsy.

Solriamfetol (Sunosi)

A dual dopamine and norepinephrine reuptake inhibitor (DNRI) approved for excessive daytime sleepiness in narcolepsy.

Chronotherapy

A non-pharmacological treatment for circadian rhythm disorders involving the gradual, systematic adjustment of sleep times.

Lorazepam (Pronunciation: loe-RAZ-e-pam)

What is the brand name for this medication?

Brand Name: Ativan

Triazolam (Pronunciation: try-AH-zoe-lam)

What is the brand name for this medication?

Brand Name: Halcion

Ramelteon (Pronunciation: ram-EL-te-on)

What is the brand name for this medication?

Brand Name: Rozerem

Tasimelteon (Pronunciation: tas-i-MEL-te-on)

What is the brand name for this medication?

Brand Name: Hetlioz

Suvorexant (Pronunciation: soo-vo-REX-ant)

What is the brand name for this medication?

Brand Name: Belsomra

Lemborexant (Pronunciation: lem-bo-REX-ant)

What is the brand name for this medication?

Brand Name: Dayvigo

Gabapentin enacarbil (Pronunciation: gab-a-PEN-tin en-ACK-er-bil)

What is the brand name for this medication?

Brand Name: Horizant

Pregabalin (Pronunciation: preg-AB-a-lin)

What is the brand name for this medication?

Brand Name: Lyrica

Sodium Oxybate (Pronunciation: so-dee-um OXY-bate)

What is the brand name for this medication?

Brand Name: Xyrem

Pitolisant (Pronunciation: pit-OH-li-sant)

What is the brand name for this medication?

Brand Name: Wakix

Modafinil (Pronunciation: mo-DAF-i-nil)

What is the brand name for this medication?

Brand Name: Provigil

Solriamfetol (Pronunciation: sol-ree-am-FET-ol)

What is the brand name for this medication?

Brand Name: Sunosi