Anxiety & Sleep Drugs

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Questions and Answers

A patient with hepatic impairment requires a medication for insomnia. Which of the following would be LEAST appropriate?

  • Zolpidem
  • Temazepam
  • Ramelteon (correct)
  • Trazodone

Which of the following medications for insomnia carries the highest risk of next-day somnolence?

  • Eszopiclone (correct)
  • Buspirone
  • Ramelteon
  • Trazodone

A patient is prescribed Tylenol #3 for mild pain relief. What critical information should the pharmacist provide regarding its mechanism?

  • It acts as a peripheral mu-opioid antagonist.
  • It directly targets pain receptors in the brain.
  • It requires conversion by CYP2D6 into its active form. (correct)
  • It blocks the production of prostaglandins to reduce pain.

Which opioid medication is associated with a higher risk of 'dose dumping' when taken with alcohol?

<p>Opana (A)</p> Signup and view all the answers

A patient taking methadone for chronic pain reports signs of QT prolongation. Which factor most likely contributes to this adverse effect?

<p>NMDA antagonism (D)</p> Signup and view all the answers

Which medication used in OUD treatment discourages intravenous abuse due to its formulation?

<p>Suboxone (C)</p> Signup and view all the answers

Which of the following is a peripherally acting mu-opioid receptor antagonist used to treat opioid-induced constipation (OIC) without affecting central analgesia?

<p>Methylnaltrexone (D)</p> Signup and view all the answers

A patient using Duragesic (fentanyl patch) for chronic pain should be counseled to avoid:

<p>Applying the patch after a hot shower. (A)</p> Signup and view all the answers

Which inhaled asthma medication is approved for SMART therapy (Single Maintenance and Reliever Therapy)?

<p>Symbicort (C)</p> Signup and view all the answers

What is the primary mechanism of action of magnesium sulfate when used to treat severe asthma exacerbations?

<p>Calcium antagonist (B)</p> Signup and view all the answers

Which of the following asthma medications requires monitoring of IgE levels and patient weight for proper dosing?

<p>Omalizumab (D)</p> Signup and view all the answers

A patient with severe asthma who is not responding to other therapies is prescribed Tezepelumab. What is the target of this medication?

<p>TSLP (A)</p> Signup and view all the answers

Which of the following is a triple therapy inhaler for asthma maintenance that includes an ICS, LABA, and LAMA?

<p>Trelegy Ellipta (D)</p> Signup and view all the answers

Why is Airsupra (budesonide + albuterol) unique compared to other inhalers like Advair or Symbicort?

<p>It is a rescue combination inhaler. (B)</p> Signup and view all the answers

Which of the following medications used for anxiety has a delayed onset of action, typically requiring 2–4 weeks to achieve its full effect?

<p>Buspirone (C)</p> Signup and view all the answers

What is the primary mechanism of action of hydroxyzine in treating anxiety?

<p>H1 receptor antagonism (A)</p> Signup and view all the answers

Which medication used for insomnia requires a risk evaluation and mitigation strategy (REMS) program due to its potential for abuse and misuse?

<p>Suvorexant (C)</p> Signup and view all the answers

A patient with a history of alcohol abuse is prescribed a medication for insomnia. Which of the following medications should be used with caution due to the risk of additive CNS depression?

<p>Temazepam (D)</p> Signup and view all the answers

A patient taking mirtazapine for insomnia reports significant weight gain. What is the most likely mechanism contributing to this side effect?

<p>H1 blockade (D)</p> Signup and view all the answers

Which of the following asthma medications has a black box warning for neuropsychiatric events?

<p>Montelukast (D)</p> Signup and view all the answers

Flashcards

Zolpidem (Ambien)

Non-benzodiazepine GABAA agonist used to treat insomnia.

Eszopiclone (Lunesta)

Non-benzodiazepine GABAA agonist for insomnia.

Temazepam (Restoril)

Benzodiazepine that enhances GABAA receptor activity, used for insomnia

Ramelteon (Rozerem)

Melatonin receptor agonist used for insomnia.

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Suvorexant (Belsomra)

Orexin receptor antagonist used for insomnia.

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Doxepin

Sedating antihistamine (H1 antagonist) used off-label for insomnia.

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Trazodone

5-HT2 antagonist/reuptake inhibitor used off-label for insomnia.

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Mirtazapine

Alpha-2 antagonist and H1 blocker used off-label for insomnia.

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Buspirone (Buspar)

5-HT1A partial agonist used to treat anxiety.

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Hydroxyzine (Vistaril)

Antihistamine (H1 antagonist) used for anxiety on an as-needed basis (PRN).

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Pregabalin (Lyrica)

Inhibits voltage-gated Ca2+ channels; used off-label for anxiety.

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Codeine + APAP (Tylenol #3)

Mu-opioid agonist, C-III, requires CYP2D6 activation, ceiling effect.

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Hydrocodone + APAP (Vicodin)

Mu-opioid agonist, risk of liver toxicity due to APAP.

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Hydrocodone ER (Zohydro ER, Hysingla ER)

Mu-opioid agonist, abuse-deterrent formulation.

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Tramadol (Ultram)

Mu-opioid agonist + SNRI, BBW: seizures, serotonin syndrome, CYP2D6.

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Albuterol (ProAir HFA, Ventolin HFA)

Beta-2 agonist; overuse indicates poor asthma control.

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Budesonide/Formoterol (Symbicort)

ICS + LABA for both rescue and maintenance.

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Dupilumab (Dupixent)

IL-4/IL-13 antagonist used for eosinophilic or steroid-dependent asthma.

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Omalizumab (Xolair)

Anti-IgE mAb, dosed by IgE and weight, q2-4w

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Ipratropium (Atrovent HFA)

SAMA – muscarinic antagonist; Add to SABA for moderate-severe exacerbation.

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Study Notes

Anxiety & Sleep Drugs

  • Ambien (Zolpidem):
    • Indicated for insomnia.
    • A non-benzodiazepine GABAA agonist.
    • Classified as C-IV.
    • Potential for complex sleep behaviors, such as sleep driving.
    • Should be avoided in elderly patients.
  • Lunesta (Eszopiclone):
    • Used for insomnia.
    • A non-benzodiazepine GABAA agonist.
    • Classified as C-IV.
    • May cause a bitter taste.
    • Has a long half-life.
  • Restoril (Temazepam):
    • Indicated for insomnia.
    • A benzodiazepine that works on GABAA receptors.
    • Classified as C-IV.
    • Listed in the Beers Criteria.
    • Carries a risk of tolerance.
  • Rozerem (Ramelteon):
    • Used for insomnia.
    • A melatonin receptor agonist.
    • Not a scheduled drug.
    • Should be avoided in patients with hepatic impairment.
  • Belsomra (Suvorexant):
    • Indicated for insomnia.
    • An orexin receptor antagonist.
    • Classified as C-IV.
    • May cause next-day somnolence.
  • Doxepin (Doxepin):
    • Used for insomnia.
    • An H1 antagonist and TCA at low doses.
    • Should be taken without food.
    • Listed in the Beers Criteria.
  • Trazodone (Trazodone):
    • Used off-label for insomnia.
    • A 5-HT2 antagonist/reuptake inhibitor.
    • Sedating.
    • Potential risk of orthostasis.
    • Carries a warning for priapism.
  • Mirtazapine (Mirtazapine):
    • Used off-label for insomnia.
    • An alpha-2 antagonist and H1 blocker.
    • Sedating at low doses.
    • Can cause weight gain.
  • Buspar (Buspirone):
    • Indicated for anxiety.
    • A 5-HT1A partial agonist.
    • Has a delayed onset of 2–4 weeks.
    • No abuse potential.
  • Vistaril (Hydroxyzine):
    • Used as needed (PRN) for anxiety.
    • An H1 antagonist.
    • Sedating.
    • Has anticholinergic side effects.
  • Lyrica (Pregabalin):
    • Used off-label for anxiety.
    • Inhibits voltage-gated Ca2+ channels.
    • Classified as C-V.
    • Can cause sedation, dizziness, and weight gain.

Pain Management & Opioid Use Disorder (OUD) Drugs

Opioids & Combo Products

  • Tylenol #3 (Codeine + APAP):
    • Indicated for mild to moderate pain.
    • A mu-opioid agonist.
    • Classified as C-III.
    • Requires CYP2D6 activation.
    • Has a ceiling effect.
  • Vicodin (Hydrocodone + APAP):
    • Used for moderate pain.
    • A mu-opioid agonist.
    • Classified as C-II.
    • Risk of liver toxicity.
  • Zohydro ER (Hydrocodone ER):
    • Indicated for severe pain.
    • A mu-opioid agonist.
    • Classified as C-II.
    • Features abuse-deterrent properties.
    • Does not contain APAP.
  • Hysingla ER (Hydrocodone ER):
    • Used for severe pain.
    • A mu-opioid agonist.
    • Classified as C-II.
    • Provides 24-hour duration.
    • Features abuse-deterrent properties.
  • Ultram (Tramadol):
    • Indicated for moderate pain.
    • A mu-opioid agonist and SNRI.
    • Classified as C-IV.
    • Black Box Warning for seizures and serotonin syndrome.
    • Metabolized by CYP2D6.
  • Nucynta (Tapentadol):
    • Used for moderate to severe pain.
    • A mu-opioid and NRI.
    • Classified as C-II.
    • Causes less nausea.
    • Should be avoided with MAOIs.
  • MS Contin (Morphine ER):
    • Indicated for severe pain.
    • A mu-opioid agonist.
    • Classified as C-II.
    • Requires renal dosing.
    • M6G is an active metabolite.
  • Kadian (Morphine ER):
    • Used for severe pain.
    • A mu-opioid agonist.
    • Classified as C-II.
    • Capsules can be opened and sprinkled on applesauce.
    • Do not crush.
  • OxyContin (Oxycodone ER):
    • Indicated for severe pain.
    • A mu-opioid agonist.
    • Classified as C-II.
    • A CYP3A4 substrate.
    • High abuse risk.
  • Opana (Oxymorphone):
    • Used for severe pain.
    • A mu-opioid agonist.
    • Classified as C-II.
    • Black Box Warning: Alcohol increases absorption, leading to dose dumping.

Fentanyl Products

  • Duragesic (Fentanyl patch):
    • Indicated for severe chronic pain.
    • A mu-opioid agonist.
    • Classified as C-II.
    • Not for opioid-naive patients.
    • Patch is applied every 72 hours.
    • Avoid heat exposure.
  • Actiq (Fentanyl lozenge):
    • Used for breakthrough cancer pain.
    • A mu-opioid agonist.
    • Classified as C-II.
    • Subject to REMS.
    • Rapid onset.
    • Only for opioid-tolerant patients.

Methadone & Buprenorphine

  • Dolophine (Methadone):
    • Indicated for severe pain and OUD.
    • A mu-opioid agonist and NMDA antagonist.
    • Classified as C-II.
    • Can cause QT prolongation.
    • Variable half-life.
    • Metabolized by CYP3A4.
  • Subutex (Buprenorphine):
    • Used for OUD and pain.
    • A partial mu-agonist and kappa antagonist.
    • Classified as C-III.
    • Has a ceiling effect on respiratory depression.
  • Suboxone (Buprenorphine/Naloxone):
    • Indicated for OUD.
    • A partial mu-agonist and antagonist.
    • Classified as C-III.
    • Naloxone discourages IV abuse.
  • Sublocade (Buprenorphine ER injection):
    • Used for OUD.
    • A partial mu-agonist.
    • Classified as C-III.
    • Administered as a subcutaneous monthly injection for maintenance.
  • Belbuca (Buprenorphine buccal):
    • Indicated for chronic pain.
    • A partial mu-agonist.
    • Classified as C-III.
    • Lower abuse potential.

OIC & Reversal

  • Narcan (Naloxone):
    • Indicated for opioid overdose.
    • A mu-opioid antagonist.
    • Not scheduled.
    • Short half-life.
    • Repeat dosing may be needed.
  • Relistor (Methylnaltrexone):
    • Used for OIC.
    • A peripheral mu-antagonist.
    • Administered subcutaneously or orally.
    • Does not reverse central analgesia.
  • Movantik (Naloxegol):
    • Indicated for OIC.
    • A peripheral mu-antagonist.
    • A CYP3A4 substrate.
    • Avoid strong inhibitors.

Expanded Asthma Drug Chart

Rescue & Maintenance Inhalers

  • ProAir HFA (Albuterol):
    • Rescue inhaler (SABA).
    • A beta-2 agonist.
    • Use more than twice a week indicates poor asthma control.
    • May cause tremor and tachycardia.
  • Ventolin HFA (Albuterol):
    • Rescue inhaler (SABA).
    • A beta-2 agonist.
    • Interchangeable with ProAir.
  • Xopenex (Levalbuterol):
    • Rescue inhaler (SABA).
    • R-isomer of albuterol.
    • Fewer side effects but more costly.
  • AirSupra (Budesonide + Albuterol):
    • Rescue combination inhaler.
    • Contains an ICS and SABA.
    • For adults only.
    • Maximum of 12 puffs per day.
  • Symbicort (Budesonide/Formoterol):
    • Used for SMART therapy.
    • Contains an ICS and LABA.
    • Used for both rescue and maintenance.
  • Dulera (Mometasone/Formoterol):
    • Maintenance inhaler.
    • Contains an ICS and LABA.
    • Not FDA-approved for SMART; maintenance only.
  • Advair (Fluticasone/Salmeterol):
    • Maintenance inhaler.
    • Contains an ICS and LABA.
    • Not for SMART, as salmeterol is too slow for rescue.
  • Breo Ellipta (Fluticasone/Vilanterol):
    • Maintenance inhaler.
    • Contains an ICS and LABA.
    • Dosed once daily.
  • Trelegy Ellipta (Fluticasone/Umeclidinium/Vilanterol):
    • Maintenance inhaler (Triple therapy).
    • Contains an ICS, LAMA, and LABA.
    • Dosed once daily.
    • Not for children.

Biologics for Severe Asthma

  • Dupixent (Dupilumab):
    • Indicated for eosinophilic or steroid-dependent asthma.
    • An IL-4/IL-13 antagonist.
    • Also used for eczema and nasal polyps.
  • Nucala (Mepolizumab):
    • Indicated for eosinophilic asthma.
    • An IL-5 antagonist.
    • Administered subcutaneously every 4 weeks.
  • Fasenra (Benralizumab):
    • Indicated for eosinophilic asthma.
    • An IL-5Rα cytolytic mAb.
    • Administered subcutaneously every 4 weeks for 3 doses, then every 8 weeks.
  • Cinqair (Reslizumab):
    • Indicated for eosinophilic asthma.
    • An IL-5 antagonist.
    • Administered via IV infusion only; for adults ≥18.
  • Xolair (Omalizumab):
    • Indicated for allergic asthma (IgE-based).
    • An anti-IgE mAb.
    • Dosed based on IgE levels and weight, every 2–4 weeks.
  • Tezspire (Tezepelumab):
    • Indicated for severe asthma (including non-eosinophilic).
    • A TSLP blocker.
    • Works across phenotypes.
    • Administered subcutaneously every 4 weeks.

Additional Asthma Therapies

  • QVAR RediHaler (Beclomethasone):
    • Maintenance inhaler (ICS).
    • A corticosteroid.
    • Rinse mouth after use.
  • Pulmicort Flexhaler (Budesonide):
    • Maintenance inhaler (ICS).
    • A corticosteroid.
    • Also available as nebules for children.
  • Alvesco HFA (Ciclesonide):
    • Maintenance inhaler (ICS).
    • A corticosteroid.
    • A prodrug; less thrush.
  • Arnuity Ellipta (Fluticasone):
    • Maintenance inhaler (ICS).
    • A corticosteroid.
    • Dosed once daily.
  • Spiriva Respimat (Tiotropium):
    • Add-on LAMA.
    • A muscarinic antagonist.
    • Used if ICS + LABA is not sufficient.
  • Singulair (Montelukast):
    • Indicated for allergic asthma and rhinitis.
    • A leukotriene receptor antagonist.
    • Black Box Warning: neuropsychiatric events.
  • Prednisone (Prednisone):
    • Used for exacerbations.
    • An oral corticosteroid.
    • Administered in burst doses.
    • Taper if used for more than 14 days.
  • Methylprednisolone (Medrol):
    • Used for exacerbations.
    • A corticosteroid.
    • Used in hospital settings or as a burst dose.
  • Magnesium sulfate (IV MgSOâ‚„):
    • Used for severe exacerbations.
    • A Ca2+ antagonist (bronchodilation).
    • Used in ER/hospital settings for status asthmaticus.
  • Ipratropium (Atrovent HFA):
    • Add-on rescue medication (nebulizer).
    • A SAMA – muscarinic antagonist.
    • Added to SABA for moderate-severe exacerbations.

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