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Depressants Sedative Hypnotics

Depressants Sedative Hypnotics

Psyc 470 – Introduction to Chemical

Alcohol

• Oldest • Used thousands of years Sedative • Used mostly for self Psychology 470 Introduction to Chemical Additions Steven E. Meier, Ph.D.

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Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions

Used for Many Things General Names

• To relieve stress •Downers • Induce • • Reduce •Hypnotics • Minor Tranquilizers • • Anti Anxiety

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Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions

Classes of Compounds Based Historically Non-

• Non-Barbiturates • Use began before 1900 • Barbiturates • Many compounds • Antianxiety Medications/Minor • * Tranquilizers • * • * •Urethane • Sulfonal • Most are not used today

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1 Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions

Bromides Problems

• Sodium • Lots of side effects • One of the earliest Sedative Hypnotics • Takes a long time to administer and • Behaves like a chloride ion eliminate from the system • Shuts down the •Can be toxic • Is eliminated slowly • Can still be used for epileptic • Need to gradually increase the dosage and but other drug groups are over days (titrate the patient) until the better desired effect occurs • Not used much today

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Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions

Chloral Hydrate (Noctec) Paraldehyde

• Oldest sleep inducing (hypnotic) • Is a polymer of acetaldehyde • First synthesized in 1832 • Occasionally used to treat DT’s • Induces sleep in approximately ½ hour • Therapeutic Doses • Sleep occurs in about 15 minutes • Little effect on or BP • Drug is metabolized to acetaldehyde by •Toxic Doses the and eliminated through the • Severe respiration depression and low BP lungs – gives an odor. • Alco ho l + Chlo ral Hydrate = •Knockout Drops • Highly toxic to the liver, stomach and • Mickey Finn kidneys • Still used today but not as much

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Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions

Barbital Barbiturates

• Is a derivative of • Barbituric Acid is the parent compound • Was introduced in 1903 of all barbiturates • Became extremely popular • Basic structure lacks CNS depressant • 1912 was introduced activities • Need other alkyl or methyl groups to • Since then >2500 analogues have been get sedative activity synthesized • How you get all the different types • 50 commercially available • About 20 are still on the market

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2 Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions

Classified Ultra short • Usually used in IV • Based on onset and duration of action • - seconds to about •Ultra short one minute •Short •Some Drugs •Intermediate • (Brevital) •Long • (Surital) • Thiopental (Pentothal) • (Diprovan) • Gamma-Hydroxybutyric Acid (GHB)*** • Not preferred by drug abusers • Works to fast 13 14

Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions

Gamma-Hydroxybutyric Acid (GHB) Gamma-Hydroxybutyric Acid (GHB)

• Is a • Is a potent sedative/depressant • Called “Natures Quaalude” • Produces • Is primarily used as a general • Disinhibition • Excitement • Used also for • Drunken-like behavior (but without • Sleep disorders ) •Alcohol and Abuse • • Classic • Increases dopamine levels in the brain Results in

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Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions

Side Effects Short

• Commonly see • Preferred by users • Respiratory Depression • Onset of action - 20-30 minutes •Seizures • Lasts 3-6 hours (usually 4) • Vomiting • Primarily used for sleep or sedation

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Variety of Drugs Intermediate

• (Nembutal) Yellows • Also preferred by abusers Yellow Jackets • Onset of action - 40-60 minutes • Is often used in Veterinary anesthesia • Duration of action - 4-6 hours • (Seconal) Reds • Used primarily for sleep or sedation • Used primarily as a sleep medication

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Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions

Types of Drugs Long

• (Amytal) Blues • Used for continuous sedation • (Alurate) • Used in • (Butisol) • Used for mild anxiety • Onset of Action 1-2 hours • Duration of Action 6-12 hours

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Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions

Types of Drugs

• Phenobarbital (Luminal) • Binds on the binding site of • Mephobarbital (Mebaral) the GABAa •Result • Decrease excitability of all tissue • CNS is more sensitive to Barbiturates • RIA system is most sensitive

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Behavioral Effects Side Effects of Barbiturates

• Disinhibition • Decrease REM sleep • Slurred Speech • Result – Person is not as rested in the • Disorientation morning • Appears drunk but has no alcohol odor • High potential for abuse • Decreased respiration • 25% of all (mostly among women) • Weak, rapid pulse • Induces other enzymes and thus • Dilated Pupils breaks down other drugs faster.

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Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions

High Tolerance Non Barbiturates

• Rapid down regulation • is technically here too • During withdrawal •Many types • Increased stimulation • (Doriden) •Seizures • (Quaalude, Sopor) • • (Noludar) •Anxiety • (Pladidyl) •Valmid

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Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions

Effects Behavioral Effects

• Actions and properties are • Slurred speech similar to classic barbiturates • Disorientation • Act as sedatives or hypnotics • Drunken behavior without the odor of • Side effects are the same as alcohol barbiturates • Overdoses are harder to treat • Have same behavioral effects • Luding out (Quaaludes with wine) • Very dangerous with alcohol

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5 Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions Antianxiety Medications / Minor Tranquilizers Carbanates

• Two Different Groups • •Carbanates •Miltown • •Equanil

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Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions

Action Behavior

• Works similar to intermediate-acting • Same as traditional barbiturates barbiturates but is less toxic •Sedation • Produces less sedation but can be long •Muscle relaxation lasting • Reduces anxiety • Doesn’t give as great of respiratory • Can help prevent seizures suppression as barbiturates • Mild euphoria

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Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions

Interesting Points Benzodiazepines • Newest class of sedative-hypnotics • Primarily used up until the 1950’s but still occasionally used today. • Are one of the most widely prescribed medications • Can overdose on 20-30 pills • Are frequently abused • When overdosing, causes a ball of pills in the stomach. Requires the stomach • Like carbonates are used to: to be pumped to ensure all of the drug • Produce sedation is out of the stomach. • Induce sleep • Benzodiazepines do a better job and are • Relieve anxiety safer •Muscle relaxation • Prevent seizures 35 36

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Classification Short Acting

• Two groups • Rapid onset, short duration •Short-acting • Used to treat • Intermediate-acting • Long term duration • Differ based on • How fast they take effect • Duration of action

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Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions

Types Intermediate

• (Versed) •Lroazepam (Ativan) • (Serax) • (Klonopin) • (Restoril) • (Dormalin) • (Halcion) • (Xanax) • (ProSom) •Quazepam (Doral)

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Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions

Long Term Types

• Are primarily used to treat general • Alprazolam (Xanax) anxiety. • (Librium) • Can also be used for: • (Valium) •Muscle relaxation • (Tranzene) • Adjunct to Anesthesia • (Paxipam) •Oxazepam (Serax) • (Centrax) • (Dalmane)

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Other Uses Site of Action for Benzodiazepines

• Midazolam (Versed) • GABAa Receptor • Injectable Anesthetic •Can • Short acting • Completely block • Clonazepam (Klonopin) • Partially Block • Used for the treatment of • Most completely block disorders • Intermediate-Acting

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Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions

For Anxiety For Muscle Relaxation

• Shut down structures associated with • Shut down structures in fearful responses •Spinal Cord • • Cerebellum • Orbitofrontal Cortex •Brain Stem •Insula • Other structures

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Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions

Antiepileptic Pleasure

• Shut down structures in the • Shut down structures in the • Cerebellum • Nucleus Acumbens • • Ventral Tegmentum

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Partial Agonists (Rohypnol)

• Block only particular types of receptors • Is technically a • Reduces anxiety • Commercially marketed outside the US • Doesn’t give you the high • Is similar to Halcion) • Where new research is going • Reduces anxiety • Causes sedation • Causes amnesia

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Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions

Combined with Alcohol Side Effects

• Acts like Chloral Hydrate • Similar to Barbiturates • Acts like GHB •Sedation • Also called a date-rape drug • Motor impairments •Drowsiness • Mental • Amnesia (especially when taken with alcohol •Others • Generally is dose related

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Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions

Other Issues Differences from Barbiturates • Not as dangerous • Can significantly impair cognitive performance (especially memory) • Can increase the effects of barbiturates •Synergistic effects • Decreases academic performance • Do not usually give as great of • Reduces psychomotor functioning sedation • Effects can occur for long periods after • Better for daytime use the drugs are discontinued • Work on different binding sites • Impairments decrease over time • Can be used with alcohol withdrawal (usually) • Don’t see as great of tolerance effects and takes longer too 53 54

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In General

• Both Barbiturates and Benzodiazepines tend to slow the system down • Work on the GABAa receptor (and others as well) • When used correctly are very effective for what they do. • Both develop tolerance • Both have opposite withdrawal effects

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