Pharm 2 Objective 2.1 Part 2 Central Nervous System Depressants and Stimulants Overview

Sedatives

Drugs that inhibit CNS, reducing nervousness and excitability.

Hypnotics

Drugs that induce sleep, more potent than sedatives.

Sedative-Hypnotics

Dose-dependent drugs calming CNS; induce sleep at high doses.

Barbiturates

First standard drugs for insomnia; habit-forming.

Benzodiazepines

Commonly prescribed sedative-hypnotics with favorable safety profiles.

Nonbenzodiazepines

Currently more frequently prescribed than benzodiazepines.

Anxiolytic

Medication specifically relieving anxiety.

Long Acting Benzodiazepines

Examples include clonazepam and diazepam.

Intermediate Acting Benzodiazepines

Examples include alprazolam and lorazepam.

Short Acting Benzodiazepines

Examples include midazolam and zolpidem.

Benzodiazepine Mechanism

Depress CNS activity via GABA receptors.

CNS Calming Effects

Benzodiazepines reduce agitation and sensory stimulation.

Indications for Benzodiazepines

Used for sedation, anxiety relief, and muscle relaxation.

Adverse Effects of Benzodiazepines

Include drowsiness, dizziness, and cognitive impairment.

Benzodiazepine Toxicity

Symptoms include somnolence, confusion, and coma.

Flumazenil

Antidote for benzodiazepine overdose.

Drug Interactions

Includes azole antifungals and grapefruit juice.

Barbiturate Safety

Low therapeutic index; less commonly used today.

Phenobarbital

Common example of a barbiturate.

Hangover Effect

Daytime sleepiness after benzodiazepine use.

Fall Hazard

Increased risk for older adults using benzodiazepines.

REM Sleep Suppression

Benzodiazepines suppress REM less than barbiturates.

Barbiturates

CNS depressants that enhance GABA effects.

Mechanism of Action

Inhibits nerve impulses in the cerebral cortex.

Indications for Barbiturates

Used as sedatives, anticonvulsants, and anesthesia.

Adverse Effects of Barbiturates

Includes cardiovascular, CNS, respiratory, gastrointestinal issues.

Vasodilation

Widening of blood vessels, causing hypotension.

CNS Depression

Range from drowsiness to coma and death.

Respiratory Depression

Decreased breathing rate, can lead to arrest.

Drug Interactions

Additive effects with alcohol and other depressants.

MAOIs

Prolong barbiturate effects by inhibiting metabolism.

Overdose Symptoms

Respiratory arrest and CNS depression.

Over-the-Counter Hypnotics

Nonprescription aids containing CNS-depressants like antihistamines.

Common OTC Hypnotics

Doxylamine, diphenhydramine, acetaminophen/diphenhydramine.

Muscle Relaxants

Relieve pain from skeletal muscle spasms.

Centrally Acting Muscle Relaxants

Act on CNS to relieve muscle spasms.

Direct Acting Muscle Relaxants

Act directly on skeletal muscle fibers.

Indications for Muscle Relaxants

Used for musculoskeletal pain and spasticity management.

Adverse Effects of Muscle Relaxants

Includes euphoria, dizziness, drowsiness, confusion.

Nursing Implications

Assess history and vital signs before therapy.

Hypnotic Administration Timing

Administer 30-60 minutes before bedtime.

REM Rebound

Increased REM sleep after stopping certain medications.

Caution in Older Adults

Increased sensitivity to CNS depressants.

Rebound insomnia

Sleep difficulties after stopping medication for 3-4 weeks.

Safety precautions

Use side rails, bed alarms, and assist ambulation.

Therapeutic effects monitoring

Assess sleep quality and reduction in awakenings.

Adverse effects monitoring

Watch for hangover effects and other side effects.

Central Nervous System Stimulants

Drugs that stimulate brain or spinal cord activity.

Excitatory neurotransmitters

Dopamine, norepinephrine, and serotonin in CNS.

Sympathomimetic drugs

Mimic effects of sympathetic nervous system stimulation.

Drug classification

Based on chemical structure and therapeutic action.

Attention-Deficit Hyperactivity Disorder

Common psychiatric disorder affecting 3-10% of children.

ADHD symptoms

Inattention, hyperactivity, and impulsivity in behavior.

Narcolepsy

Neurological disorder causing sudden sleep attacks.

Cataplexy

Sudden muscle weakness while awake, often knees.

Migraine characteristics

Recurring headache lasting 4-72 hours, often unilateral.

Migraine symptoms

Nausea, photophobia, phonophobia, and pulsatile pain.

Aura

Sensory disturbances preceding a migraine attack.

Amphetamines

Stimulants like methylphenidate used for ADHD.

Modafinil

Nonamphetamine stimulant for narcolepsy treatment.

Atomoxetine

Nonstimulant drug for ADHD management.

Lisdexamfetamine

Prodrug for dextroamphetamine, treats ADHD.

CNS effects of amphetamines

Elevated mood, increased alertness, decreased fatigue.

Respiratory effects of amphetamines

Bronchial relaxation and increased respiration.

Therapeutic uses of stimulants

ADHD, narcolepsy, anorexia, and migraine treatments.

Adverse Effects

Wide range of effects related to drug dosage.

Common Adverse Effects

Includes palpitations, tachycardia, and hypertension.

Amphetamine Derivatives

Stimulants used for ADHD and narcolepsy treatment.

Atomoxetine

Nonstimulant drug prescribed for ADHD.

Dextroamphetamine Sulphate

Brand name: Dexedrine®, used for ADHD.

Amphetamine Aspartate

Brand name: Adderall®, commonly prescribed for ADHD.

Methylphenidate Hydrochloride

First drug approved for ADHD treatment.

Extended-Release Methylphenidate

Includes Ritalin SR®, Concerta®, and Biphentin®.

Antimigraine Drugs

Serotonin agonists, also known as triptans.

Sumatriptan

Brand name: Imitrex®, used for migraine relief.

Ergot Alkaloids

Formerly mainstay treatment for migraines, now less common.

Mechanism of Action of Triptans

Stimulate 5-HT receptors, causing vasoconstriction.

Ergot Alkaloids Mechanism

Constrict blood vessels in the brain.

Adverse Effects of Triptans

Include vasoconstriction and injection site irritation.

Adverse Effects of Ergot Alkaloids

Nausea, vomiting, and muscle pain.

Nursing Implications for ADHD Drugs

Administer last dose 4-6 hours before bedtime.

Medication-Free Times

May be ordered for ADHD treatment monitoring.

Selective Serotonin Receptor Agonists

Available as dissolvable wafers and nasal sprays.

Immediate Medical Attention Signs

Chest pain, confusion, or vision changes.

Monitor for Therapeutic Responses

Essential for assessing drug efficacy.

Journal for Therapy Response

Instruct patients to track their treatment outcomes.

ADHD

Decreased hyperactivity, increased attention span.

Narcolepsy

Condition characterized by decreased sleepiness.

Serotonin agonist

Reduces migraine frequency, duration, severity.

Drug Diversion

Transfer of drugs to unlawful distribution channels.

Medication tampering

Altering medications for misuse or diversion.

Consequences of drug diversion

Harms clients, nurses, and healthcare settings.

Seizure

Abnormal electrical activity in brain nerve cells.

Convulsion

Involuntary muscle contractions throughout the body.

Epilepsy

Chronic condition with recurrent seizure patterns.

Primary epilepsy

No identifiable cause; about 50% of cases.

Secondary epilepsy

Identifiable cause such as trauma or infection.

Generalized onset seizures

Seizures affecting both hemispheres of the brain.

Tonic-clonic seizures

Characterized by convulsions and loss of consciousness.

Atonic seizures

Sudden loss of muscle tone.