Exam 3

Temazepam brand

Restoril

Temazepam class

Benzodiazepine

Temazepam use

Insomnia

Temazepam MOA

Binds to benzodiazepine receptors, enhances GABA effects

Temazepam dose

7.5-30 mg PO qHS PRN

Temazepam contraindications

Avoid abrupt withdrawal

Temazepam BBW

Use with opioids may result in profound sedation, respiratory depression, coma, or death

Clonazepam brand

Klonopin

Clonazepam class

Benzodiazepine

Clonazepam use

Seizure disorders, panic disorder

Clonazepam MOA

Binds to benzodiazepine receptors, enhances GABA effects

Clonazepam dose

0.5-5 mg PO TID

Clonazepam contraindications

Hepatic impairment, avoid abrupt withdrawal

Clonazepam BBW

Use with opioids may result in profound sedation, respiratory depression, coma, or death

Lorazepam brand

Ativan

Lorazepam class

Benzodiazepine

Lorazepam use

Anxiety, status epilepticus

Lorazepam MOA

Binds to benzodiazepine receptors, enhancing GABA effects

Lorazepam dose

2-6 mg PO/IM/IV divided BID or TID

Lorazepam contraindications

Sensitivity to polyethylene glycol, respiratory impairment, sleep apnea, avoid abrupt withdrawal

Lorazepam BBW

Use with opioids may result in profound sedation, respiratory depression, coma, or death

Diazepam brand

Valium, Diastat

Diazepam class

Benzodiazepine

Diazepam use

Seizure disorders, anxiety, sedation

Diazepam MOA

Binds to benzodiazepine receptors, enhances GABA effects

Diazepam dose

2-10 mg PO BID-QID or 5-10 mg IM/IV q3-4h

Diazepam contraindications

Avoid abrupt withdrawal

Diazepam BBW

Use with opioids may result in profound sedation, respiratory depression, coma, or death

Alprazolam brand

Xanax

Alprazolam class

Benzodiazepine

Alprazolam use

Anxiety, panic disorder

Alprazolam MOA

Binds to benzodiazepine receptors, enhances GABA effects

Alprazolam dose

IR: 0.5-3 mg PO TID, ER: 3-6 mg PO qD

Alprazolam contraindications

Avoid abrupt withdrawal

Alprazolam BBW

Use with opioids may result in profound sedation, respiratory depression, coma, or death

Trazodone brand

Trazodone

Trazodone class

Serotonin reuptake inhibitor antidepressant

Trazodone use

Major depressive disorder, insomnia

Trazodone MOA

Antagonizes serotonin 5-HT2A/C and alpha-1 adrenergic receptors, inhibits serotonin reuptake

Trazodone dose

50-100 mg PO BID or TID

Trazodone contraindications

Avoid abrupt withdrawal

Trazodone BBW

May cause suicidal thoughts in children and young adults

Hydroxyzine brand

Atarax, Vistaril

Hydroxyzine class

H1 antihistamine

Hydroxyzine use

Anxiety, pruritus, urticaria

Hydroxyzine MOA

Non selectively antagonizes central and peripheral histamine H1 receptors

Hydroxyzine dose

25-100 mg PO/IM q4-6h PRN

Hydroxyzine contraindications

QT prolongation, hypersensitivity to cetirizine or levocetirizine

Hydroxyzine BBW

None

Zolpidem brand

Ambien

Zolpidem class

Anxiolytic, hypnotic

Zolpidem use

Short term insomnia

Zolpidem MOA

Interacts with GABA-benzodiazepine receptor complexes

Zolpidem dose

IR: 5-10 mg PO qHS, ER: 6.25-12.5 mg PO qHS

Zolpidem contraindications

Alcohol use, hepatic impairment, history of complex sleep behavior

Zolpidem BBW

Complex sleep behaviors may occur including sleep walking, sleep driving, and other activities

Ramelteon brand

Rozerem

Ramelteon class

Sedative/hypnotic, melatonin receptor agonist

Ramelteon use

Delirium

Ramelteon MOA

Potent selective agonist of melatonin receptors (MT1, MT2), little affinity for MT3, acts within the suprachiasmatic nucleus of the hypothalamus

Ramelteon dose

8 mg PO within 30 minutes of bedtime

Ramelteon contraindications

Avoid alcohol

Ramelteon BBW

None

Eszopiclone brand

Lunesta

Eszopiclone class

Non-benzodiazepine hypnotic

Eszopiclone use

Insomnia

Eszopiclone MOA

Interacts with GABA-receptor complexes coupled to binding domains close to benzodiazepine receptors

Eszopiclone dose

1-3 mg PO qHS

Eszopiclone contraindications

Use with caution in patients with a history of drug dependence

Ezoclipone BBW

None

In general what is the order of effect as the dose of CNS depressants increase?

Sedation → Hypnosis → Anesthesia

What effect does an anxiolytic have?

Mild calming effect

What effect does a sedative have?

Greater calming effect which typically includes drowsiness

What effect do hypnotics have?

Induce and sustain sleep from which the patient can be aroused

What effect do anesthetics have?

Intense, non-selective CNS depression which requires the removal of drug for patient arousal

What is the MOA of benzodiazepines?

Cause conformational change in receptor which leads to greater frequency of GABA binding

What drug class is this?

Benzodiazepine

What is this?

Diazepam

How is this structure transformed into nordiazepam?

N-demethylation by CYP2C19

What is this?

Alprazolam

What does the fixed triazole group do to this structure’s activity?

Increases potency

What is this?

Lorazepam

What is this?

Oxazepam

What is this?

Chlordiazepoxide

What is this?

Clorazepate dipotassium

What is this?

Temazepam

What is this?

Triazolam

What is this?

Flurazepam

What is this?

Midazolam

What is this?

Flumazenil

What does this do?

Reverse sedative effect of benzodiazepines

What is this?

Zolpidem

What is this and how is it metabolized?

Zaleplon, aldehyde oxidase

What is this?

Eszopiclone

How is this metabolized?

N-oxidation and N-demethylation via CYP3A4 and CYP2E1

In what situation do we need to reduce the dose of this drug?

Severe hepatic impairment

What is this drug class?

Barbiturate

If someone uses alcohol acutely, how does this affect CYP450 metabolism?

Inhibits CYP450

If someone uses alcohol chronically, how does this affect CYP450 metabolism?

Induces CYP450

What does the highlighted group do?

Antagonizes opioids (structure is naltrexone)