Sedative - Hypnotic Drugs

seeking effects that include calming, sleep and intoxication

Subclasses of the Sedative - Hypnotics

Barbiturates
Non-Barbiturate sedative hypnotics Minor tranquilizers Major tranqulizers Inhalants
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Why are these drugs used?

Sedation
Coping with stress and anxiety Smoothing effects of stimulants Potentiation of narcotics Treatment of serious mental disorders Pleasurable sensations, including intoxication
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General Characteristics
Widespread CNS depression Potentiation / synergism with other depressant drugs Tolerance Physiological and / or psychological dependence (sedativism) Cross-tolerance Cross-dependence
anxiety euphoria relief
calmness sleep general coma anesthesia death

Barbiturates
Uses
Ultrashort acting (e.g., thiopental): surgical anesthetics Short-intermediate acting (e.g., secobarbital): sedativehypnotics Long acting (e.g., phenobarbital): sedative hypnotics; anticonvulsants

Problems most commonly abused (specifically the shortintermediate group) rapid development of tolerance & dependence withdrawal creates a medical emergency

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Non-Barbiturate Sedative Hypnotics

Uses
Alternative to barbiturates Specific to treatment for sleeplessness Examples: chloral hydrate, ethchlorvynol, and some of the benzodiazepines (flurazepam, triazolam, temazepam)

Problems
adverse drug reactions (especially with triazolam)

abuse potential (especially with street versions of methaqualone) rapid tolerance & dependence
rebound effects

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Anatomy of Sleep
Non-Rapid-Eye-Movement (non-REM) sleep: deep level of
sleep characterized by drops in blood pressure, heart and breathing rates, and body temperature; slow, even brain wave activity (serotonin)

Rapid-Eye-Movement (REM) sleep: shallow level of sleep

characterized by increases and fluctuations in blood pressure,

heart and breathing rates; complete relaxation of muscles in arms

and legs resulting in temporary paralysis; high level of brain activity (norepinephrine)
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Anatomy of Sleep
Awake Light sleep Deep sleep 0 1 2 3 4 5 6 7 8 REM NREM

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Anatomy of Sleep
REM Sleep Latency: from onset of sleep to the first REM (70 - 100 minutes)
hypnogogy

Sleep Cycle: from one REM sleep period to the next (~ 90 minutes); 4 6 cycles per night
As the night progresses, REM stages lengthen in time and less time is spent in Stages 3 & 4.
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Anatomy of Sleep
70 60 50 40 30 20 10 0 Young Adult Children - 1 yr Elderly REM Stage 1 Stage 2 Stage 3 & 4

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Sleep Deprivation
Stage 4 Deprivation - hypoactive;
depressed response state
exercise increases length of Stage 4

REM Deprivation - hyperactive;

increased response state
Balance seems to exist between waking and sleeping activity levels.
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REM Rebound
Most sedative - hypnotic sleep medicines depress the amount of REM and increase the amount of NREM (especially Stages 3 & 4) Once body is medicine-free, REM increases substantially (latency decreases, frequency and length increases) Best Choices: flurazepam (Rx); diphenhydramine (OTC); l-tryptophan (amino acid)
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Anti - Anxiety Medicines

Treatment of anxiety and neurotic conditions (including physical manifestations), not psychoses Benzodiazepines: diazepam (Valium) and alprazolam (Xanax) Beta-blockers: oxprenolon and propranolol
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