Unit 5: Sedatives, Hypnotics, and Anti-anxiety Drug Therapy Study Notes

Sedatives: Agents designed to reduce the desire for physical activity and produce mental relaxation in the patient.
Hypnotics: Agents designed specifically to induce and maintain sleep.

Mechanism of Action (MOA):
- Barbiturates depress the Central Nervous System (CNS).
- They mimic the neurotransmitter Gamma-Aminobutyric Acid (GABA) by increasing chloride ( $Cl^-$ ) influx.
- This influx causes hyperpolarization of nerve membranes, making them less likely to fire.
- They specifically decrease the activity of the reticular formation.
Patient Teaching and Side Effects:
- Sleep Cycle Disruption: Barbiturates disrupt the natural sleep cycle, leading to a loss of REM (Rapid Eye Movement) sleep, which is essential for mental restoration.
- Drug Discontinuation (d/c): After stopping the drug, patients may experience increased dreaming and possible nightmares as the brain attempts to "make up" for the lost REM sleep.
- Physical Side Effects: Dry mouth, lethargy, and drowsiness.
- Cognitive and Reflexive Impairment: Patients exhibit depressed reflexes and impaired judgment.
- Safety Cautions: Warning against driving or operating heavy machinery.
- Monitoring: Healthcare providers must monitor for the development of tolerance and addiction.
- Drug Interactions: Alcohol consumption significantly increases the CNS-depressing effects of barbiturates.

Mechanism of Action (MOA): These drugs increase the inhibitory effects of GABA.
Therapeutic Uses: Uses vary depending on the specific drug, but generally include:
- Decreasing awakenings throughout the night.
- Increasing total sleep time.
- Inducing and maintaining sleep.
- Assistance for patients having difficulty falling asleep.
Patient Teaching and Side Effects:
- General Effects: Headhouses, dizziness, gastrointestinal (GI) upset, memory disturbances, and confusion.
- Ambien® (Zolpidem): Specifically noted for causing nightmares, night terrors, and sleepwalking.
- Safety and Monitoring: Monitor for dependence and tolerance; alcohol increases the effects of these drugs.

Mechanism of Action (MOA): Increases the inhibitory activity of GABA; also functions as an antianxiety (anxiolytic) medication.
Impact on Sleep: Unlike barbiturates, benzodiazepines do not significantly interfere with REM sleep, allowing for better mental restoration.
Patient Teaching and Side Effects:
- Hangover Effect: Possible residual grogginess the next day.
- General Side Effects: Drowsiness, headache.
- Safety: Alcohol increases effects; monitor for tolerance and dependence.
General Guidelines for Sedative-Hypnotics:
- Alcohol Contraindication: No alcohol should be consumed while taking benzodiazepines or barbiturates due to the risk of further depressing CNS activity.
- Administration: Should be taken on an as-needed (PRN) basis rather than daily to prevent dependency, tolerance, and withdrawal symptoms associated with abrupt discontinuation.

Definition: An unpleasant feeling, uneasiness, fear, or worry occurring more days than not for at least a $6$ -month period.
Physiological Response: Characterized by an increase in activities within the sympathetic system, limbic system, and reticular formation.
Neurotransmitter Imbalance: Thought to involve an imbalance in GABA, Serotonin ( $5HT$ ), Dopamine ( $DA$ ), and Norepinephrine ( $NE$ ).
Diagnostic Requirements: For adults, $3$ out of the following $6$ symptoms are required (children only require $1$ for diagnosis):
- Restlessness, feeling "keyed up," or "on edge."
- Being easily fatigued.
- Difficulty concentrating or the mind going blank.
- Irritability.
- Muscle tension.
- Sleep disturbance (including difficulty falling/staying asleep, or restless/unsatisfying sleep).
Functional Impact: The condition must cause significant distress or impairment in social, occupational, or other important areas of functioning.
Classification: Subcategories are determined by the DSM-5 (Diagnostic and Statistical Manual of Mental Disorders, 5th Edition).

Antidepressants: SSRIs (Selective Serotonin Reuptake Inhibitors), SNRIs (Serotonin-Norepinephrine Reuptake Inhibitors), and miscellaneous agents.
Azapirones (Nonbenzodiazepines).
Benzodiazepines: Should be used on a PRN (as-needed) basis, not for long-term maintenance therapy.

Mechanism of Action by Area:
- GABA Action: Increases inhibitory action of GABA to decrease CNS activity ( $\text{Anti-anxiety}$ ).
- Limbic System: Decreases activity to reduce emotional and behavioral responses ( $\text{Anti-anxiety}$ ).
- Reticular Formation: Decreases activity to reduce alertness and wakefulness ( $\text{Sedative/Hypnotic}$ ).
- Cerebral Cortex and Medulla: Decreases activity, leading to a decrease in higher learning and motor function ( $\text{Anticonvulsant}$ ).
- Spinal Cord: Decreases activity to reduce muscle tone ( $\text{Skeletal muscle relaxant}$ ).
Drug Examples: Often identified by the suffixes "-pam" or "-lam" (e.g., Temazepam).
Benzodiazepine Side Effects:
- Drowsiness and dizziness.
- Confusion and mild GI upset.
- Long-term Effects: Potential for memory loss.
- Safety: Monitor for dependence/addiction; ability to operate vehicles may be impaired.

Mechanism of Action (MOA): Binds to Serotonin ( $5HT$ ) receptors, reducing levels of $5HT$ and the overall level of anxiety.
Patient Teaching and Side Effects:
- Side Effects: Dizziness, lightheadedness, feeling tired.
- Therapeutic Lag: The full therapeutic effect is reached in $3$ to $4$ weeks.
- Prescription Protocol: Must be prescribed as a regular regimen; it is not for "as needed" use.
- Safety Profile: Low abuse potential; notably, there is no interaction with alcohol.

Scenario: A patient visits a physician with significant worry persisting for $3$ months regarding job performance, bonuses, retirement savings, marriage, finances, parenting, and education costs.
Condition Discussion: Based on the symptoms (worry about many aspects of life), a diagnosis would be evaluated against the $6$ -month criteria mentioned in DSM-5. Currently, at $3$ months, it may not yet meet the full duration requirement for generalized anxiety disorder but shows significant distress.
Potential Classification: Possible drug classifications include anxiolytics (benzodiazepines for short-term/PRN or Azapirones for a regimen).
Holistic Interventions: The patient could benefit from non-pharmacological interventions such as exercise, meditation, counseling, or environmental changes to manage the job-related stress.