hypnotics & anxiolytics 2

List of barbiturates

Phenobarbital

Thiopental

Methohexital

Secobarbital

Amobarbital

MOA of Barbiturates

Binds to GABA-A receptors → prolong open Cl- channels

Blocks excitatory glutamate receptors

T/F: Benzos have greater GABA enhancement than Barbiturates

False

T/F: Barbiturates have largely replaced by benzos in most clinical applications

True

Barbiturates indications

General anesthesia

Antiepileptic

Neuroprotection

Barbiturates combined with ___ results in more severe CNS depressions vs monotherapy

Ethanol

Barbiturates induces CYP450 enzymes in the ____ → chronic use diminishes effect of other drugs metabolized by the same enzyme

Liver

T/F: Antidepressants (first line for GAD) have higher physical dependance than benzos

False

T/F: SSRIs & SNRIs can be used in combo with low dose of benzos

True

List of course relevant Non-benzo Hypnotics

Zolpidem

Zaleplon

Eszopiclone

Ramelteon

Which non-benzo hypnotic acts as a subset of the benzo receptor family (GABA)

Zolpidem

Non-benzo hypnotic with a 30 min onset and 5hr duration

Zolpidem

Zolpidem adverse effects

Nightmares

Agitation

HA

GI upset

Non-benzo hypnotic with fewer residual effect on psychomotor and cognitive functions compared to Zolpidem or benzos

Zaleplon

Non-benzo hypnotic with 30 min onset and 3 hr duration

Zaleplon

Non-benzo hypnotic with 20min onset and 7hr duration

Eszopiclone

Non-benzo hypnotic with 30min onset and 7hr duration

Ramelton

Non-benzo hypnotic no recommended for pregnancy and breast feeding

Zaleplon

Non-benzo hypnotic that binds to GABA and indicated for Insomnia

Eszopiclone

Eszopiclone ADEs

CNS depression (high dose)

Dose adjustment with concomitant CNS depressants

Non-benzo hypnotic not recommended for long-term use in pregnancy

Eszopiclone

Buspirone indication

Chronic GAD

Buspirone is a full and partial agonist of which presynaptic and postsynaptic receptors, respectively

5HT1A

5HT1A agonist, Buspirone, increases what receptor action

Serotonin

Buspirone blocks what receptors in the presynapse to enhance its neurotransmission

Dopamine D2

Buspirone ADEs

HA, dizzy, lightheaded

Nervousness

Restless

Disadvantage of Buspirone

Slow onset of days to weeks

Selective MT1 and MT2 melatonin receptors

Ramelteon

Ramelteon indications

Insomnia

Ramelteon ADEs

Dizzy

Fatigue

Somnolence

Neuropeptide that regulates arousal, wakefulness, and appetite

List of Orexin receptor antagonists

Suvorexant (Belsomra)

Lemborexant (Dayvigo)

Daridorexant (Quiviviq)

Where do orexin producing neurons project from

Lateral hypothalamus

Orexin 1 and 2 receptors (OX1R, OX2R) are are also known as what type of receptors to mediate orexins

G-protein couples receptors (GPCRs)

Activation of OX2Rs depolarizes orexin neurons and result in what

Increase presynaptic glutamate release

Orexin receptor antagonists indication

Induce sleep via inhibition of excitatory neurotransmission

Orexin-RAs advantage

Target more localized area of brain

Orexin-RAs ADEs

Next day drowsiness

Deoendence

What atypical antidepressant is very effective in treating sleep disturbances in Alzheimer’s

Trazadone (Desyrel)

Which Atypical antidepressant helps insomnia symptoms in those with clinical depression

Mirtazapine (Remeron)

What drug class can treat mild insomnia as OTC hypnotics

Antihistamines

List on hypnotic antihistamines

Diphenhydramines (Benadryl)

Hydroxyzine (Vistaril, Atarax)

Doxylamine (Disclegis)

Ethanol MOA

Increase GABA mediated synaptic inhibition

Inhibits NMDA glutamate receptors

Ethanol indications

CNS depressant

Anxiolytic

Sedative

Ethanol ADEs

Liver disease

Gastritis

Nutritional deficiency

Cardiomyopathy

Ethanol combo w what drugs can cause synergistic CNS depression

Benzos

Antihistamines

Barbiturates