Neuro

Anxiolytic and Hypnotic Agents

1. Introduction

  • Anxiety: A feeling of tension, nervousness, apprehension, or fear involving unpleasant reactions to a stimulus.

2. Psychological States Affecting Anxiolytic and Hypnotic Drugs

  • Sedation: Loss of awareness and reaction to environmental stimuli.

  • Hypnosis: Extreme sedation leading to further CNS depression and sleep.

3. Benzodiazepines Overview

  • Definition:

    • Benzodiazepines are a class of central nervous system (CNS) depressants.

    • Used to manage anxiety, insomnia, muscle spasms, seizure disorders, and alcohol withdrawal.

  • Prescriptive Popularity & Advantages:

    • Among the most commonly prescribed sedative-hypnotic agents.

    • Noted for effectiveness, rapid onset, and relatively high safety margin compared with older barbiturates.

4. Benzodiazepines: Mechanism of Action

  • Working Process:

    • Benzodiazepines enhance the effects of gamma-aminobutyric acid (GABA), the main inhibitory neurotransmitter in the CNS.

    • Binding occurs on specific benzodiazepine receptors on the GABA-A receptor complex, increasing the frequency of chloride channel opening.

    • Chloride ion influx hyperpolarizes the neuron (less excitable), leading to CNS depression—producing sedation, anxiolysis, and muscle relaxation.

  • Key Concept:

    • Benzodiazepines do not directly activate GABA receptors; they potentiate GABA's natural inhibitory effect.

5. Pharmacologic Uses of Benzodiazepines

  • Categories:

    • Anxiolytic: Reduces anxiety and agitation.

    • Sedative-hypnotic: Promotes relaxation and sleep.

    • Anticonvulsant: Controls seizure activity.

    • Muscle relaxant: Decreases skeletal muscle tension.

    • Amnesic: Causes short-term memory loss (useful for medical procedures).

6. Actions & Indications of Benzodiazepines

  • Actions:

    • Lower doses assist with anxiety; higher doses induce sedation and hypnosis.

  • Indications:

    • Anxiety disorders, alcohol withdrawal, hyperexcitability, agitation, and preoperative relief of anxiety and tension for balanced anesthesia.

7. Common Benzodiazepines and Uses

  • Drug Name (Generic) | Common Brand | Primary Clinical Uses

    • Diazepam | Valium | Anxiety, muscle spasms, seizure disorders, alcohol withdrawal.

    • Lorazepam | Ativan | Anxiety, sedation before surgery, status epilepticus.

    • Alprazolam | Xanax | Generalized anxiety and panic disorders.

    • Clonazepam | Klonopin | Panic disorders, seizure disorders.

    • Temazepam | Restoril | Short-term treatment of insomnia.

    • Midazolam | Versed | Sedation and amnesia before procedures or surgery.

8. Pharmacokinetics of Benzodiazepines

  • Absorption:

    • Well absorbed from the GI tract.

  • Peak Levels:

    • Achieved in 30 minutes to 2 hours.

  • Distribution:

    • Lipid soluble, distributes well throughout the body, crosses the placenta, enters breast milk.

  • Metabolism:

    • Primarily metabolized in the liver; excretion is mainly in the urine.

9. Adverse Effects of Benzodiazepines

  • Common Adverse Effects:

    • Sedation, drowsiness, lethargy.

    • Depression.

    • Blurred vision.

    • Confusion.

    • Dry mouth.

    • Constipation.

    • Nausea/vomiting.

    • Hypotension.

    • Urinary retention.

10. Nursing Considerations for Benzodiazepines

10.1 Assessment
  • Obtain medication history regarding other CNS depressants (e.g., opioids, alcohol).

  • Assess level of anxiety, sleep patterns, or seizure activity prior to therapy.

  • Monitor vital signs, specifically respiratory rate and level of consciousness.

10.2 Implementation
  • Administer at bedtime for sleep aid.

  • Avoid abrupt discontinuation (can cause withdrawal symptoms such as tremors, seizures, anxiety).

  • Use the lowest effective dose for the shortest duration.

  • For IV preparations (e.g., lorazepam, diazepam), monitor for respiratory depression.

10.3 Patient Teaching
  • Avoid alcohol, opioids, and other sedatives while on benzodiazepines.

  • Caution against driving or operating machinery until effects are known.

  • Rise slowly to prevent orthostatic hypotension.

  • Do not stop suddenly; taper under provider supervision.

  • Secure medications due to the risk of misuse and dependence.

10.4 Evaluation
  • Observational outcomes: reduction in anxiety, improved sleep without excessive sedation, no signs of dependence or withdrawal.

11. Contraindications of Benzodiazepines

11.1 Absolute Contraindications
  • Conditions:

    • Known hypersensitivity/allergy (risk of severe allergic reaction).

    • Severe respiratory insufficiency or sleep apnea (further CNS depression may cause respiratory arrest).

    • Severe hepatic impairment (toxic accumulation for long-acting agents like diazepam).

    • Acute narrow-angle glaucoma (increases intraocular pressure).

    • Shock, coma, or acute intoxication (risk of respiratory and cardiovascular depression).

11.2 Relative Contraindications
  • Conditions:

    • Chronic obstructive pulmonary disease (COPD): may worsen hypoventilation; caution advised.

    • Elderly or debilitated patients: higher CNS sensitivity and fall risk.

    • Pregnancy and lactation: risks to the fetus or infant.

    • Substance use disorder (alcohol or drug dependence): high risk of tolerance and dependence.

    • Renal impairment: may prolong effects.

    • Depression/suicidal ideation: increased risk of mood worsening; appropriate mental health support required.

12. Drug Interactions for Benzodiazepines

  • Interacting Substances:

    • Alcohol: profound CNS and respiratory depression; contraindicated.

    • Opioids: increased risk of fatal respiratory depression.

    • Antihistamines, barbiturates, antipsychotics, antidepressants: additive sedation risk.

  • Drugs affecting metabolism:

    • Valproate, cimetidine, oral contraceptives can lead to increased drug levels.

    • Smoking can induce metabolism, potentially reducing effectiveness.

13. Symptoms of Benzodiazepine Withdrawal

  • Aches/pains, abnormal body sensations, grand mal seizures, nausea, insomnia, delirium/detachment from reality, muscle spasms, anxiety/panic attacks, depression.

14. Other Anxiolytic and Hypnotic Drugs

14.1 Antihistamines
  • Examples:

    • Promethazine (Promethegan), diphenhydramine (generic).

  • Uses: Preoperative and postoperative medications; decrease narcotic need.

  • Note: Cause drowsiness but do not induce sleep.

14.2 Buspirone (Buspar) (Generic) 
  • Reduces anxiety signs/symptoms without severe CNS effects and adverse effect .

14.3 Dexmedetomidine (Precedex)
  • Used for sedation in intubated/mechanically ventilated patients.

14.4 Eszopiclone (Lunesta)
  • FDA approved for insomnia management.

15. Non-benzodiazepine Anxiolytics

15.1 Buspirone Overview
  • Definition: Prototype and most commonly used non-benzodiazepine anxiolytic.

  • Mechanism of Action:

    • Works on serotonin (5-HT1A) and dopamine (D2) receptors.

    • Does not affect GABA, causing minimal sedation and no dependence.

  • Onset: Takes 2–4 weeks for full effect (not for acute anxiety).

15.2 Common Side Effects
  • Dizziness, light-headedness, nausea, headache, nervousness/excitement at treatment start.

15.3 Contraindications / Cautions
  • Avoid use with MAO inhibitors (risk of hypertensive crisis).

  • Grapefruit juice can increase drug levels.

  • Use caution in liver/kidney impairment.

15.4 Nursing Considerations for Buspirone
  • Emphasize consistent use; not a PRN medication. must be taken consistenly 

  • Gradual relief expectations (2–4 weeks).

  • No alcohol/sedatives concurrently; monitor dizziness, especially in older adults.

  • Reinforce adherence, even if anxiety improves.

16. Other Anxiolytics

16.1 Sedating Antihistamines
  • Examples: Hydroxyzine (Vistaril, Atarax), Diphenhydramine (Benadryl).

  • Mechanism of Action: Block histamine (H1) receptors producing sedation/anxiolytic effects.

  • Uses: Short-term anxiety management or sleep promotion when benzodiazepines contraindicated.

16.2 Side Effects
  • Drowsiness, dry mouth, blurred vision, urinary retention (anticholinergic effects).

16.3 Nursing Considerations for Antihistamines
  • Avoid driving/operating machinery.

  • Encourage hydration/oral care for dry mouth.

  • Caution against concurrent alcohol/CNS depressants.

17. Hypnotics (Non-Benzodiazepines)

17.1 Overview of Hypnotics
  • Definition: Medications inducing and maintaining sleep, closely related to sedatives.

17.2 Sedatives vs. Hypnotics
  • Sedative: Reduces anxiety and promotes relaxation. Lower doses 

  • Hypnotic: Induces drowsiness and maintain sleep, usually at higher doses than sedatives.

  • Subclass of CNS depressants, often related to sedatives (clam with nessarily cauing sleep) 

17.3 Non-Benzodiazepine Hypnotics
  • Examples:

    • Zolpidem (Ambien), Zaleplon (Sonata), Eszopiclone (Lunesta).

  • Mechanism of Action: Act on GABA-A receptors but at different subunits than benzodiazepines.

    • Produce sedation with minimal anxiolytic/muscle-relaxant effects.

17.4 Therapeutic Uses of Non-Benzodiazepines
  • Short-term insomnia management, preoperative sedation, adjunct to anesthesia, control of anxiety, and treatment of nocturnal awakenings.

17.5 Advantages of Non-Benzodiazepine Hypnotics
  • Lower risk of dependence.

  • Minimal next-day sedation if used correctly.

  • Short half-life is beneficial for sleep onset.

17.6 Side Effects
  • Drowsiness, dizziness, headache, sleepwalking/sleep-driving (complex sleep behaviors), rare hallucinations/confusion (especially in older adults).

17.7 Nursing Considerations for Non-Benzodiazepine Hypnotics
  • Administer right before bedtime.

    • Patient must have at least 6–8 hours to sleep.

  • Avoid alcohol/CNS depressants.

  • Educate about potential sleep-related behaviors.

  • Caution in elderly to reduce the risk of confusion and falls.

18. Melatonin Receptor Agonists

18.1 Examples
  • Ramelteon (Rozerem), Tasimelteon (Hetlioz).

  • Mechanism of Action: Mimics the body’s natural melatonin by acting on melatonin receptors (MT1 and MT2) in the hypothalamus to regulate the sleep-wake cycle.

  • Uses: Sleep-onset insomnia and Tasimelteon for “non-24-hour sleep disorder” in blind individuals.

  • Advantages: No dependence or withdrawal, not a controlled substance.

18.2 Side Effects
  • Dizziness, fatigue, endocrine effects (elevated prolactin, decreased testosterone).

  • Nursing Considerations: Administer 30 minutes before bedtime.

  • Avoid high-fat meals (delays absorption).

  • Effects may take several days to become noticeable.

19. Barbiturates

19.1 Examples
  • Secobarbital, Pentobarbital.

  • Mechanism of Action: Depress CNS by enhancing GABA and directly opening chloride channels.

  • Uses: Occasionally used for anesthesia induction, seizure control (not typical for insomnia).

  • Risks: High potential for tolerance, dependence, and fatal overdose (respiratory depression).

20. Summary Table of Drugs

Drug/Class

Prototype

Key Use

Onset

Dependency Risk

Main Nursing Concern

Benzodiazepine

Temazepam

Sleep induction & maintenance

30–60 min

High

Respiratory depression, fall risk

Non-benzodiazepine

Zolpidem

Short-term insomnia

15–30 min

Moderate

Complex sleep behaviors

Melatonin agonist

Ramelteon

Difficulty falling asleep

30 min

None

Hormonal changes, dizziness

Antihistamine

Diphenhydramine

Mild insomnia

30–60 min

Low

Anticholinergic effects

Barbiturate

Secobarbital

Rare use

Rapid

Very high

Respiratory & CNS depression

Antidepressant Agents

21. Signs & Symptoms of Depression

  • Low energy levels.

  • Disturbances in sleep patterns.

  • Lack of appetite.

  • Limited libido.

  • Inability to perform activities of daily living (ADLs).

  • Overwhelming feelings of sadness, despair, hopelessness, disorganization.

22. Biogenic Amine Theory of Depression

  • Theory posits that depression results from deficiency in norepinephrine (NE), dopamine, or serotonin (5-HT) due to:

    • Monoamine oxidase (MAO) may degrade these neurotransmitters affecting recycling/restoration.

    • Rapid neuronal firing may lead to depletion of neurotransmitters.

    • Increased number/sensitivity of postsynaptic receptors depletes neurotransmitter levels.

23. Actions of Antidepressant Therapy

  • Mechanisms:

    • Inhibit the effects of MAO, increasing NE or 5-HT in the synaptic cleft.

    • Block reuptake by the releasing nerve, increasing neurotransmitter levels in the synaptic cleft.

    • Regulate receptor sites and neurotransmitter breakdown leading to increased concentrations in the synaptic cleft.

24. Classifications of Antidepressants

  • Selective serotonin reuptake inhibitors (SSRIs).

  • Tricyclic antidepressants (TCAs).

  • MAO inhibitors (MAOIs).

  • Serotonin norepinephrine inhibitors (SNRIs).

25. Selective Serotonin Reuptake Inhibitors (SSRIs)

25.1 Overview
  • Definition: Major class of antidepressant and anxiolytic medications increasing serotonin levels in the brain.

  • Advantages:

    • Effective for depression and anxiety.

    • Safer than older antidepressants (TCAs, MAOIs).

    • Better tolerated with fewer cardiovascular/anticholinergic effects.

25.2 Mechanism of Action
  • Process: SSRIs block the reuptake of serotonin (5-HT) into the presynaptic neuron, increasing serotonin availability at the synaptic cleft, enhancing mood, energy, and emotional regulation.

  • Key Concept for Nursing: SSRIs selectively affect serotonin, not norepinephrine or dopamine minimizing side effects compared to older antidepressants.

25.3 SSRIs Action & Indications
  • Actions:

    • Specifically block the reuptake of 5-HT with minimal known effect on norepinephrine or other receptors. (USUALLY TIRED FIRST) 

  • Indications:

    • Depression, OCDs, panic attacks, bulimia, premenstrual dysphoric disorder, post-traumatic stress disorder, social phobias, social anxiety disorders.

26. Common SSRIs and Brand Names

Generic Name

Brand Name

Common Clinical Uses

Fluoxetine

Prozac

Depression, bulimia, OCD, panic disorder

Sertraline

Zoloft

Depression, PTSD, OCD, panic, anxiety

Paroxetine

Paxil

Anxiety, depression, panic, OCD

Citalopram

Celexa

Depression

Escitalopram

Lexapro

Depression, generalized anxiety disorder

Fluvoxamine

Luvox

OCD, social anxiety disorder

27. SSRI Pharmacologic Profile
  • Onset of Action: 2–4 weeks for mood improvement, up to 6–8 weeks for full therapeutic effect.

  • Metabolism: Primarily hepatic (CYP450).

  • Elimination: Renal.

  • Dosing: Generally once daily (morning preferred to avoid insomnia).

28. Common Adverse Effects of SSRIs

System

Effect

Nursing Consideration

CNS

Headache, insomnia, nervousness

May resolve after 1-2 weeks; take in AM.

GI

Nausea, diarrhea, loss of appetite

Take with food if needed.

Sexual

Decreased libido, delayed orgasm

Discuss openly; dose adjustment may help.

Weight

Gain (paroxetine) or loss (fluoxetine)

Monitor weight regularly.

Other

Dry mouth, sweating, tremor

Encourage fluids, oral care.

29. Life-Threatening Reactions with SSRIs
29.1 Serotonin Syndrome
  • Cause: Excessive serotonin, can occur from SSRI combinations with other serotonergic drugs (MAOIs, St. John's wort, triptans, tramadol).

  • Symptoms: Agitation, confusion, tremor, muscle rigidity, hyperreflexia, diaphoresis, fever, tachycardia; severe cases can lead to seizures, coma, or death.

  • Nursing Priority:

    • Stop SSRI immediately.

    • Notify provider.

    • Provide supportive care (IV fluids, cooling, benzodiazepines for agitation).

29.2 Suicidal Ideation
  • Monitor especially in children, adolescents, and young adults during early treatment for mood changes, agitation, or self-harm thoughts; report changes immediately.

30. Contraindications and Precautions for SSRIs
  • Conditions:

    • Concurrent use with MAOIs or within 14 days of stopping.

    • Liver disease (reduced metabolism; dose adjustment needed).

    • Pregnancy (especially paroxetine; possible teratogenic effects).

    • Bipolar disorder (may trigger mania; requires mood stabilizer co-therapy).

    • Seizure disorder; glaucoma (SSRIs lower seizure threshold slightly).

31. Nursing Considerations for SSRIs
  • Before Administration: Assess baseline mood, suicidal thoughts, anxiety levels.

  • Obtain medication history (especially MAOIs, herbal supplements).

  • Monitor liver/renal function as indicated.

32. During Therapy Considerations for SSRIs
  • Check clinical improvement after 2–4 weeks.

  • Watch for serotonin syndrome with new medications.

  • Reinforce adherence—missed doses reduce effectiveness.

  • Educate that energy may improve before mood, increasing suicide risk.

33. Patient Education for SSRIs
  • Take daily at the same time, preferably morning.

  • Do not stop abruptly without provider supervision.

  • Avoid alcohol and other CNS depressants.

  • Report increased anxiety, agitation, or suicidal thinking.

  • Avoid St. John’s wort (increases serotonin levels).

  • Continue even if better; full effect takes time.

34. Tricyclic Antidepressants (TCAs)

34.1 Overview
  • Definition: Older antidepressants introduced in the 1950s; largely replaced by SSRIs and SNRIs due to side effects but still used for specific conditions.

  • Key Point: TCAs effective but have more side effects and higher toxicity risk in overdose.

34.2 Mechanism of Action of TCAs
  • Inhibit reuptake of norepinephrine and serotonin at synapses, thereby improving mood and emotional stability.

  • Also block acetylcholine (anticholinergic effects), histamine (sedation), and alpha-adrenergic receptors (hypotension)—explains their side effects.

  • Nursing Tip: Think of TCAs as “nonselective reuptake inhibitors.”

34.3 Common TCAs and Uses

Generic Name

Brand Name

Common Uses

Amitriptyline

Elavil

Depression, chronic pain, insomnia

Imipramine

Tofranil

Depression, childhood enuresis

Nortriptyline

Pamelor

Depression, neuropathic pain

Desipramine

Norpramin

Depression

Doxepin

Sinequan, Silenor

Anxiety, depression, insomnia

Clomipramine

Anafranil

Obsessive-compulsive disorder (OCD)

35. Therapeutic Uses of TCAs
  • Treat major depressive disorder (MDD) when SSRIs/SNRIs ineffective.

  • Used for anxiety disorders, obsessive-compulsive disorder (OCD), chronic neuropathic pain, fibromyalgia, insomnia, migraine prophylaxis, and nocturnal enuresis in children (imipramine) IN CHILDREN).

36. Pharmacokinetics of TCAs
  • Absorption: From the GI tract.

  • Peak: 2-4 hours.

  • Binding: To plasma proteins, lipid soluble.

  • Metabolism: In liver; excreted in urine.

  • Half-Life: 8-46 hours.

37. Contraindications of TCAs
  • Known allergy, recent MI, myelography, pregnancy, and lactation.

38. Adverse Effects of TCAs
  • 1. Anticholinergic Effects:

  • (Drying mouth” symptoms due to ACh blockade) 

    • Dry mouth, blurred vision, constipation, urinary retention, tachycardia, confusion (especially in elderly).

  • 2. Cardiovascular Effects:

    • Orthostatic hypotension, dysrhythmias, tachycardia (especially in overdose).

    • Nursing Tip: Monitor BP and heart rate, especially in older patients.

  • 3. CNS Effects:

    • Sedation, drowsiness, dizziness, confusion, tremors, seizures (in high doses).

    • Nursing Tip: Administer at bedtime to minimize daytime drowsiness and fall risk.

  • 4. Weight and Metabolic Effects: Weight gain (common) and increased appetite.

  • 5. Sexual Dysfunction: Decreased libido, erectile or orgasmic dysfunction.

(GIVE AT BEDTIME, TO REDUCE DAYTIME DROWSINESS & FALL RISK

39. Nursing Considerations for TCAs
  • Before Administration: Obtain mental health history, vital signs, cardiac history, baseline ECG (if older adult) (always monitor BP and HR). 

  • Assess for suicidal ideation—risk highest when energy improves but mood remains low.

  • Review medication list for interactions.

  • During Administration:

    • Administer at bedtime due to sedating effects.

  • Monitor orthostatic BP changes; teach the patient to rise slowly.

  • Evaluate for dry mouth, constipation, urinary retention; ensure adequate fluid/fiber intake.

  • For enuresis, administer 1 hour before bedtime (imipramine).

40. Patient Education for TCAs
  • Take exactly as prescribed; do not double doses if missed.

  • Therapeutic effects may take weeks.

  • Avoid alcohol/CNS depressants.

  • Report cardiac symptoms (palpitations/chest pain) or urinary retention immediately.

  • Do not stop abruptly: withdrawal symptoms possible.

  • Store medications securely due to overdose risk (especially important for suicidal patients).

41. SNRIs (Serotonin–Norepinephrine Reuptake Inhibitors)

41.1 Overview
  • Definition: Increase serotonin (5-HT) and norepinephrine (NE) levels in the brain; used for treating depression, anxiety disorders, and certain chronic pain conditions.

  • Mechanism of Action: Inhibit reuptake of serotonin and norepinephrine at the presynaptic neuron, improving mood and reducing anxiety/pain sensitivity.

  • Its similar to SSRIs but also boost norepinephrine, which improve energy, concentration and pain perception

41.2 Common Drugs in SNRI Class

Generic Name

Brand Name

Key Uses

Venlafaxine

Effexor XR

Depression, generalized anxiety disorder (GAD), panic disorder

Duloxetine

Cymbalta

Depression, GAD, fibromyalgia, neuropathic pain

Desvenlafaxine

Pristiq

Major depressive disorder

41.3 Common Side Effects of SNRIs
  • Nausea, dry mouth, dizziness, headache, insomnia or somnolence, sweating, increased blood pressure (from norepinephrine), sexual dysfunction.

41.4 Serious or Cautionary Effects
  • Hypertension: Regular BP monitoring is critical.

  • Serotonin Syndrome: Particularly with SSRIs or MAOIs; symptoms include agitation and increased autonomic instability.

  • Withdrawal symptoms can occur if discontinued abruptly; taper slowly.

  • Suicidal Ideation: Early treatment phase requires close mood monitoring.

41.5 Nursing Considerations for SNRIs
  • Monitor vital signs regularly—especially blood pressure.

  • Inform patients about therapeutic effects taking 2–4 weeks.

  • Avoid sudden cessation; gradual taper needed to prevent withdrawal.

  • Instruct against concurrent alcohol/CNS depressants.

  • Look for signs of serotonin syndrome.

41.6 Adverse Effects of SNRIs
  • Nausea, constipation, hyperhidrosis, erectile dysfunction, tachycardia, vomiting, palpitations, serotonin syndrome, hypertension, abnormal bleeding, angle closure glaucoma, urinary retention.

  • Drug Interactions: Be cautious with MAOIs, SSRIs, TCAs, serotonergic drugs, aspirin, and NSAIDs.

42. Monoamine Oxidase Inhibitors (MAOIs)

42.1 Overview
  • Definition: An older antidepressant class for major depressive disorder, particularly for unresponsive cases; requires strict dietary precautions due to hypertensive crisis risk.

  • Mechanism of Action: Block monoamine oxidase, increasing norepinephrine, serotonin, and dopamine in the brain for improved mood stabilization.

42.2 Common MAOIs

Generic Name

Brand Name

Phenelzine

Nardil

Tranylcypromine

Parnate

Isocarboxazid

Marplan

Selegiline (transdermal patch)

Emsam

42.3 Contraindications for MAOIs
  • Known allergy, pheochromocytoma, cardiovascular (CV) diseases, headaches, renal or hepatic impairment.

42.4 Major Adverse Effects of MAOIs
  • Hypertensive crisis (tyramine-rich food interactions).

  • Orthostatic hypotension, headache, dizziness, insomnia, weight gain, sexual dysfunction.

42.5 Drug-Drug Interactions of MAOIs
  • Concurrent antidepressants lead to hypertensive crisis or coma.

  • Increased sympathomimetic effects with Methyldopa (sympathomimetic effects increase).

  • Risk of hypoglycemia with insulin/oral antidiabetic agents (additive hypoglycemia).

42.6 Food Interactions with MAOIs
  • Tyramine-rich foods: Can cause severe hypertension due to norepinephrine release.

    • Foods to Avoid: Aged cheeses, cured meats, smoked/pickled foods, red wine, beer, soy products, avocados, overripe fruits, yeast extracts.

    • Hypertensive Crisis Signs: severe headache, neck stiffness, palpitations, nausea/vomiting, chest pain → medical emergency 

42.7 Nursing Interactions for MAOIs
  • Educate on strict tyramine-free diet.

  • Avoid concurrent SSRIs, SNRIs, TCAs, or St. John's wort due to serotonin syndrome risk.

  • Ensure 14 days gap between MAOI and other antidepressants.

  • Regularly monitor blood pressure.

  • Teach to rise slowly to prevent orthostatic hypotension.

  • Do not stop suddenly; taper under supervision.

43. Other Antidepressants

  • Used when first-line treatments (SSRIs, SNRIs, TCAs, MAOIs) are ineffective, poorly tolerated, or to meet special clinical needs (e.g., smoking cessation, insomnia).

  • Examples:

    • Bupropion (Wellbutrin, Zyban)

    • Milnacipran (Savella)

    • Mirtazapine (Remeron)

    • Nefazodone (generic)

    • Selegiline (Emsam)

    • Trazodone (Desyrel).

43.1 Bupropion (Wellbutrin, Zyban)
  • Mechanism: Inhibits norepinephrine and dopamine reuptake; does not affect serotonin.

  • Uses: Depression, seasonal affective disorder, smoking cessation (Zyban), off-label ADHD treatment.

  • Nursing Considerations: Contraindicated in seizure disorders/eating disorders (anorexia/bulimia); side effects include dry mouth, insomnia, tremor, weight loss; minimal sexual side effects compared to SSRIs. Take in the morning to avoid insomnia 

43.2 Milnacipran (Savella)
  • Mechanism: SNRI used primarily for fibromyalgia (not in the U.S. for major depression).

  • Nursing Considerations: Monitor for suicidal thoughts, potential serotonin syndrome, and avoid abrupt discontinuation to prevent withdrawal symptoms; possible side effects include nausea/constipation/increased heart rate.

43.3 Mirtazapine (Remeron)
  • Mechanism: Enhances norepinephrine and serotonin release by blocking presynaptic α-₂ adrenergic receptors; also blocks histamine receptors.

  • Key Features: Causes sedation and weight gain; beneficial in depressed patients needing improved appetite.

  • Side Effects: Increased appetite, drowsiness, dry mouth, elevated cholesterol.

  • Teaching: Take at bedtime to aid sleep  

43.4 Trazodone
  • Mechanism: Serotonin antagonist and reuptake inhibitor (SARI) with sedative effects from histamine blockade.

  • Clinical Use: Low doses for sleep for sleep aid ; higher doses for antidepressant effects.

  • Key Adverse Effects: Sedation, dizziness, orthostatic hypotension, priapism (requires emergency care).

44. Psychothera peutic Agents

  • Functions: Used to treat psychoses such as schizophrenia, bipolar disorder, narcolepsy, and attention deficit disorder (ADD). * Drug do not cure the disorder 

  • Effectiveness: Help patients manage symptoms, enabling more acceptable functioning and improved ADLs; utilized in both children and adults.

45. Schizophrenia Characteristics

  • Signs: Hallucinations, paranoia, delusions, speech abnormalities, affective problems.

  • Causes: Strong genetic association; may indicate a fundamental biochemical abnormality.

46. Bipolar Disorder Characteristics

  • Signs: Extremes of depression followed by hyperactivity and excitement.

  • Causes: Reflects a biochemical imbalance leading to neuronal instability.

47. Narcolepsy Characteristics

  • Symptoms: Daytime sleepiness, sudden loss of wakefulness.

  • Causes: Relate to stimulation problems by the reticular activating system (RAS).

48. Attention Deficit Disorders

  • Signs: Inability to focus on one activity for long; characterized by hyperkinesis (excessive involuntary, and often uncontrollably muscular activity or movement); usually diagnosed in school-aged children but can persist into adulthood.

49. Select Antipsychotic Agents

49.1 Traditional (First Generation) Antipsychotics
  • Examples:

    • Chlorpromazine (Thorazine), Fluphenazine (Prolixin, Permitil), Haloperidol (Haldol), Loxapine (Loxitane), Mesoridazine besylate (Serentil), Molindone (Moban).

49.2 Atypical (Second Generation) Antipsychotics
  • Examples:

    • Aripiprazole (Abilify), Clozapine (Clozaril), Iloperidone (Fanapt), Olanzapine (Zyprexa), Paliperidone (Invega), Quetiapine (Seroquel), Risperidone (Risperdal), Ziprasidone (Geodon).

49.3 Antipsychotic Drugs
  • Definition: Utilized primarily to treat schizophrenia; effective for more than just psychosis, assisting in manic episodes characterized by grandiosity, paranoia, and delusions.

  • Efficacy: These agents decrease hallucinations and delusions, aiding functional levels.

50. Overview of Antipsychotic Drugs

  • Functionality: Treating psychotic disorders (schizophrenia, bipolar disorder, severe depression).

  • Classification:

    • Typical (First-Generation): e.g., Haloperidol (Haldol), Chlorpromazine (Thorazine).

    • Atypical (Second-Generation): e.g., Clozapine (Clozaril), Risperidone (Risperdal).

    • Goals: controls symptoms such as hallucinations, delusions, agitation, and disorganized thought  

50.1 Mechanism of Action
  • Typical Antipsychotics: Blocks D2 dopamine receptors—reduces positive symptoms of psychosis.

  • Mechanism: block dopamine D2 receptors in the brain→ reduced postive symptoms of psychosis 

  • Atypical Antipsychotics: Block D2 and 5-HT2 serotonin receptors—addresses both positive and negative symptoms.

50.2 Risks of Antipsychotic Medications
  • Adverse Effects: Extrapyramidal symptoms (EPS): dystonia, akathisia, parkinsonism, tardive dyskinesia; neuroleptic malignant syndrome (NMS): fever, rigidity, altered mental status; sedation, hypotension, anticholinergic effects.

  • Nursing Care: Monitor adverse reactions like EPS and NMS; intervene immediately if NMS occurs.

Atypical (Second-Generation)
Antipsychotics
❖ Examples: Clozapine (Clozaril), Risperidone (Risperdal),
Olanzapine (Zyprexa), Quetiapine (Seroquel),
Aripiprazole (Abilify).

Mechanism: Block dopamine (D2) and serotonin (5-
HT2) receptors → treat both positive and negative
symptoms.

Advantages: Fewer EPS, improved mood and cognition.

Major Risks: Weight gain, metabolic syndrome,
diabetes, hyperlipidemia.

Teaching: Encourage healthy diet, monitor glucose and
lipids.

Contraindications
o Underlying diseases that could be exacerbated by
dopamine-blocking effects of these drugs
o CNS depression
o Circulatory collapse
o Parkinson’s disease
o Coronary disease
o Severe hypotension
o Prolonged QT interval


Clozapine (Clozaril)
❖ Special Considerations:
o Reserved for treatment-resistant schizophrenia.
❖ Risk of agranulocytosis (decreased WBCs).
❖ Monitor: CBC weekly for first 6 months, then biweekly.
o Report signs of infection (fever, sore throat)
immediately.

Other effects: Weight gain, sedation, hypotension.


Haloperidol (Haldol)
❖ Use: Acute psychosis, agitation, Tourette’s syndrome.

Adverse Effects:
❖ High risk for EPS and NMS.

Nursing Interventions:
❖ Assess for muscle stiffness, rigidity, fever, and confusion.
❖ If NMS suspected → stop drug, maintain airway, apply
cooling measures, administer dantrolene or
bromocriptine per protocol.



Adverse Effects

o Sedation
o Weakness
o Tremors
o Constipation
❖ Drug-Drug Interactions
o Beta blockers, alcohol, anticholinergics, ziprasidone,
thioridazine
o Drowsiness
o Extrapyramidal
effects
o Dry mouth
o Nasal congestion


51. Common Adverse Effects of Antipsychotics

  • Sedation, weakness, tremors, constipation; specific drug-drug interactions (e.g., beta blockers, alcohol may enhance sedative effects).

52. Extrapyramidal Symptoms (EPS)
  • Types:

    • Dystonia: Involuntary muscle spasms (face, neck).

    • Akathisia: Restlessness, inability to remain still.

    • Pseudoparkinsonism: Tremors, rigidity, bradykinesia.

    • Tardive Dyskinesia: Involuntary movements (e.g., lip smacking).

  • Treatment: Introduce anticholinergic drugs (benztropine, diphenhydramine) for management; education on early recognition is critical for prevention.

53. Neuroleptic Malignant Syndrome (NMS)
  • Definition: A life-threatening emergency characterized by symptoms such as high fever, muscle rigidity, altered mental state, and autonomic instability.

  • Management: Immediate medication immediately , supportive therapies (fluids, cooling). Administer dantrolene or bromocriptine as necessary. Monitor: vitals signs, Ck levels, renal functions 

54. Nursing Responsibilities for Antipsychotic Therapies

  • Baseline Assessment: Include mental status, vital signs, weight, lab values (glucose, lipids, CBC).

  • Monitoring: Observe for EPS, orthostatic hypotension, sedation, and metabolic changes.

  • Educations: adherence is critical, sudden withdrawal may worsen symptoms 

  • Promote Safety: slow position changes, fall precautions 

55. Overview of Bipolar Disorder

  • Definition: A chronic mood disorder with alternating episodes of mania and depression.

  • Goals of Treatment: Mood stabilization, relapse prevention, functional improvement.

  • Medication Classes: Include mood stabilizers, anticonvulsants acting as mood stabilizers, atypical antipsychotics, cautiously administered antidepressants.

56. Drugs for Bipolar Disorders

Medication

Uses

Lithium (Lithobid)

Main mood stabilizer

Aripiprazole (Abilify)

Atypical antipsychotic

Lamotrigine (Lamictal)

Anticonvulsant/mood stabilizer

Olanzapine (Zyprexa)

Atypical antipsychotic

Quetiapine (Seroquel)

Atypical antipsychotic

Ziprasidone (Geodon)

Atypical antipsychotic

57. Mood Stabilizer: Lithium Carbonate
  • Mechanism: Alters sodium transport in neurons, stabilizing neurotransmission.

  • Therapeutic Range: 0.6–1.2 mEq/L; toxicity signs begin above >1.5 mEq/L.

  • Nursing Interventions: Regularly monitor lithium serum levels, renal, and thyroid function; maintain consistent sodium and fluid intake; educate on hydration to avoid dehydration.

58. Lithium: Key Nursing Considerations

Levels

Symptoms

Nursing Actions

Less than 1.5

Lethargy, muscle weakness

Assess for toxicity

1.5-2

ECG changes, nausea

Monitor regularly

2-2.5

Ataxia, seizures

Review patient status immediately

>2.5

Multiorgan toxicity

Push for immediate medical approval

Lithium
❖Pharmacokinetics
o Absorbed from GI tract
o Peak in 30 minutes
o Distribution pattern in the body as water
o Slowly crosses the blood-brain barrier.
o Excreted from the kidney, 80% is
reabsorbed
o Crosses the placenta – associated with
congenital abnormalities
o Enters the breast milk
❖Contraindications
o Allergy, renal, cardiac disease, leukemia,
metabolic disorders, pregnancy, lactation

Assessment                         Action

Dehydration           →           Encourage fluids 

Diuretics/NSAIDs   →           Avoid- raises lithium levels 

Tremor, confusion   →          Assess for toxicity 

Renal/thyroid          →           Monitor every 6 months 

Nursing Considerations for
Antimanic Drugs
❖Assess:
o History and Physical Exam, known allergies
to lithium; renal or CV disease; dehydration;
sodium depletion, use of diuretics
o Protracted sweating, or diarrhea; suicidal
or impulsive patients with severe
depression; pregnancy or lactation; and
infection with fever CNS orientation, affect
o Urinary output, liver and renal function tests
o Serum Lithium levels


59. Nursing Responsibilities for Antimanic Drugs
  • Assess: mental and physical health history, allergies, kidney disease, CV disease, dehydration status; monitor urine output and lab levels carefully.

60. Anticonvulsants as Mood Stabilizers
  • Examples: Valproic acid (Depakote), Carbamazepine (Tegretol), Lamotrigine (Lamictal).

  • Mechanism: Modulate GABA and glutamate levels to stabilize mood.

61. Valproic Acid (Depakote)
  • Mechanism: Increases GABA levels for stabilize mood

  • Adverse Effects: Monitor renal function due to hepatotoxicity and pancreatitis; report weight gain and GI upset in patients.

62. Carbamazepine (Tegretol)
  • Mechanism: Reduces neuronal excitability via sodium channel inhibition.

  • Adverse Effects: Monitor CBC for possible bone marrow suppression; report signs of rash or fever.

63. Lamotrigine (Lamictal)
  • Mechanism: Modulates glutamate release in the brain.

  • Adverse Effects: Beware of rashes; Stevens-Johnson syndrome risk requires immediate action if detected.

  • Teaching: titrate slowly, stop immediately if rasg develops 

64. Atypical Antipsychotics Overview
  • Examples: Olanzapine, Risperidone, Quetiapine, Aripiprazole.

  • Mechanism: Block both dopamine and serotonin receptors for effective amenity.

  • Uses: Treat acute mania, bipolar depression, and maintenance therapy.

  • Adverse Effects: Pay attention to weight loss/gain, monitoring glucose for hyperglycemia /lipid changes in high-risk patients.

65. Antidepressants in Bipolar Disorder
  • Use only short-term for depressive episodes and always in combination with mood stabilizers to prevent mania.

  • Examples: Fluoxetine (Prozac), Sertraline (Zoloft).

66. Key Takeaways

  • Be alert for lithium toxicity; withhold dose upon suspicion.

  • Regularly monitor liver functions for those prescribed valproic acid.

  • Report fever/sore throat in patients administered carbamazepine → possible agranulocytosis.

  • Titrate lamotrigine slowly, with immediate discontinue if upon rash appearance.

Central Nervous System Stimulants

67. Actions of CNS Stimulants

  • Mechanism of Action:

    • Act on cortical and the reticular activating system (RAS), potentially through releasing catecholamines from presynaptic neurons, leading to increased stimulation of postsynaptic neurons.

  • Indications:

    • Treatment of attention-deficit syndromes; narcolepsy management.

68. Overview of CNS Stimulants
  • Mechanism: Increase the levels of dopamine, norepinephrine, and serotonin in the CNS.

  • Therapeutic Uses:

    • ADHD, narcolepsy, and short-term obesity treatments (appetite suppression).

  • Note: These are controlled substances with a potential for high abuse.

69. Amphetamine and Dextroamphetamine (Adderall)
  • Mechanism: Promotes norepinephrine and dopamine release, increasing alertness and focus.

  • Uses: Effective for ADHD and narcolepsy.

  • Side Effects: Insomnia, weight loss, tachycardia, hypertension, irritability.

  • Teaching Points: [Take in the morning, monitor appetite/weight, avoid caffeine/stimulants, do not discontinue abruptly].

70. Methylphenidate (Ritalin, Concerta)
  • Mechanism: Blocks reuptake of dopamine/norepinephrine.

  • Uses: Indicates ADHD and narcolepsy; assess growth in children.

  • Adverse Effects: Decreased appetite, insomnia, tachycardia, nervousness; follow signs of abuse.

71. Modafinil (Provigil)
  • Mechanism: Enhances wakefulness by altering dopamine pathways.

  • Uses: Effective for narcolepsy, shift-work sleep disorder.

  • Side Effects: Headache, insomnia, nausea, anxiety.

  • Teaching: Administer in the morning; caution for driving until side effects are clear.

72. Phentermine (Adipex-P, Suprenza)
  • Mechanism: Enhances norepinephrine/dopamine release and suppresses appetite.

  • Use: Short-term obesity management alongside dietary changes and exercise.

  • Adverse Effects: Increased heart rate, elevated BP, insomnia, nervousness, dry mouth; contraindications include cardiovascular conditions and diabetes.

73. Phentermine Teaching Points
  • Administration must be in the morning to preempt insomnia.

  • Avoiding caffeine/stimulants; short use duration only (few weeks) with dietary/exercise integration needed.

74. Non-Stimulant ADHD Medications
  • Example: Atomoxetine (Strattera).

  • Mechanism: Functions as a selective norepinephrine reuptake inhibitor (SNRI).

  • Advantages: Lower abuse potential; less controlled substance nature.

  • Adverse Effects: Fatigue, GI upset, and potential suicidal ideation risks in children.

  • Nursing Care: Monitor mood changes and liver toxicity.

75. Stimulants Nursing Implications
  • Monitor: HR, BP, weight, overall growth.

  • Assessment: Quality of sleep, appetite, psychiatric changes.

  • Teaching: Restrict evening dosing, limit caffeine intake, report chest pain or palpitations.

  • Promote adherence: Safety protocols around controlled dosing.

76. Stimulants Contraindications & Precautions
  • Contraindications: Severe anxiety, agitation, cardiac disease or arrhythmias, hyperthyroidism, history of substance abuse.

  • Caution: MAO inhibitors risk of hypertensive crisis; standard protocol should be maintained.

77. Commercially Available Stimulants

Drug (Brand name)

Indication

Risks

Dextroamphetamine (Dexedrine, others)

ADHD

Contraindicate in substance abuse, cardiac disease, hyperthyroidism

Amphetamine/dextroamphetamine combinations (Adderall, others)

ADHD

Methyphenidate (Ritalin, Concerta, others)

ADHD, narcolepsy

Phentermine (Adipex-P, others)

Obesity

Phendimetrazine (Bontril, others)

Obesity

Modafinil (Provigil, others)

Narcolepsy

78. Key Takeaways
  • CNS stimulants significantly boost CNS activity, improving suspension.

  • Major risks include adverse effects and the potential for abuse.

  • Nurses play pivotal roles in monitoring growth, vitals, and mental health side effects, ensuring safe compliance.

Pain 

  • Sensory and emotional
    experience associated
    with actual or potential
    tissue damage
    ❖ Acute or chronic
    ❖ Drugs Used to Relieve Pain
    o Narcotics: Opium
    derivatives used to treat
    many types of pain
    o Antimigraine Drugs:
    Reserved for the
    treatment of migraine
    headaches

Pain Receptors
❖ Opioid receptors
o CNS
o Nerves in the periphery
o Cells in the
gastrointestinal (GI) tract

Pain is a subjective experience mediated by nociceptors.
❖ Drug classes used for pain:
o Narcotic (opioid) agonists.
o Narcotic antagonists and mixed agents.
o Non-opioid analgesics (NSAIDs, acetaminophen).
o Anti-migraine agents (triptans, ergots).

Narcotic (Opioid) Agonists
❖ Examples: Morphine, Fentanyl, Hydromorphone,
Oxycodone, Codeine.

Mechanism: Bind to mu and kappa opioid receptors,
altering perception and response to pain.
❖ Therapeutic Uses: Moderate to severe pain, anesthesia
adjunct, acute MI, cancer pain.
❖ Adverse Effects: Respiratory depression, constipation,
sedation, hypotension, urinary retention.


Nursing Responsibilities for Narcotics
❖ Assess pain level, respiratory rate, and sedation level
before administration.
❖ Hold if RR < 12/min; notify provider.
❖ Administer slowly IV to prevent respiratory depression.
❖ Encourage fluids, fiber, and ambulation to prevent
constipation.
❖ Use stool softeners as needed.




Narcotic Antagonists
❖ Example: Naloxone (Narcan).

Mechanism: Competes with opioids at receptor sites,
reversing respiratory and CNS depression.
❖ Use: Opioid overdose, postoperative respiratory
depression, newborn resuscitation.
❖ Nursing Care:
o Administer IV, IM, or intranasal.
o Onset 1–2 min IV.
o Monitor for return of pain and withdrawal symptoms.

Mixed Agonist-Antagonist Opioids
❖ Examples: Butorphanol (Stadol), Pentazocine (Talwin).

Mechanism: Stimulate kappa receptors, block or weakly
stimulate mu receptors.
❖ Use: Moderate pain, labor pain, pain with lower risk of
respiratory depression.
❖ Nursing Note: Can precipitate withdrawal in opioid-
dependent patients.

Opioid overdose- Key actions
❖ Signs: Respiratory rate < 10, pinpoint pupils,
unresponsiveness.

Nursing Interventions:
Administer Naloxone immediately.
❖ Support airway, oxygenation, and monitor vital signs.
❖ Reassess frequently—Naloxone’s half-life is shorter than
many opioids.

Migraine Headaches
o Severe, throbbing
headaches on one
side of the head
o Common
o Classic
❖ Cluster Headaches
o Begin during sleep; involve sharp, steady
eye pain, sweating, flushing, tearing, and
nasal congestion
❖ Tension Headaches
o Usually occur at times of stress; dull band
of pain around the entire head


Anti-Migraine Medications: Overview
❖ Pathophysiology: Migraine pain caused by cranial
vessel dilation and inflammation.

Drug Classes:
o Triptans (Serotonin 5-HT1 agonists) – cause
vasoconstriction.
o Ergot derivatives – older drugs, constrict
intracranial vessels.
o Preventive agents – beta-blockers,
anticonvulsants, supplement “cocktails”


Triptans (Sumatriptan, Rizatriptan)
❖ Mechanism: Stimulate 5-HT1 receptors → cranial
vasoconstriction and decreased neuroinflammation.
❖ Use: Acute migraine attacks (not prevention).

Adverse Effects: Chest tightness, dizziness, tingling,
hypertension.
❖ Contraindications: Coronary artery disease,
uncontrolled hypertension.

Ergotamine (Ergomar) and
Dihydroergotamine (DHE)
❖ Mechanism: Vasoconstriction of dilated cranial blood
vessels.
❖ Adverse Effects: Nausea, vomiting, muscle pain,
tingling in extremities.
❖ Toxicity (Ergotism): Peripheral ischemia—cold, pale
extremities, numbness.
❖ Teaching: Avoid use with triptans within 24 hours
(severe vasospasm risk).


Nursing Responsibilities for Pain
Medications
❖ Assess pain and sedation before/after administration.
❖ Monitor vital signs and level of consciousness.
❖ Evaluate for side effects: respiratory depression,
constipation, orthostatic hypotension.
❖ Educate on safe storage, use, and risk of dependence.
❖ Teach early intervention for migraine and avoidance of
triggers.


Key Takeaways
❖ Opioid agonists: effective for severe pain; monitor for
respiratory depression.
❖ Naloxone: life-saving reversal agent.
❖ Anti-migraine meds: triptans for acute attacks, ergots as
older options.
❖ Nurses play a vital role in assessment, safety, and
education.