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Depressants Sedative Hypnotics Psyc 470 – Introduction to Chemical Addictions Alcohol • Oldest Sedative Hypnotic Depressants • Used thousands of years Sedative Hypnotics • Used mostly for self medication Psychology 470 Introduction to Chemical Additions Steven E. Meier, Ph.D. Listen to the audio lecture while viewing these slides 1 2 Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions Used for Many Things General Names • To relieve stress •Downers • Induce sleep • Sedatives • Reduce anxiety •Hypnotics • Minor Tranquilizers • Anxiolytics • Anti Anxiety Medications 3 4 Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions Classes of Compounds Based Historically Non-Barbiturates • Non-Barbiturates • Use began before 1900 • Barbiturates • Many compounds • Antianxiety Medications/Minor •Bromides * Tranquilizers • Chloral Hydrate * • Paraldehyde* •Urethane • Sulfonal • Most are not used today 5 6 1 Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions Bromides Problems • Sodium Bromide • 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 action potential •Can be toxic • Is eliminated slowly • Can still be used for epileptic seizures • Need to gradually increase the dosage and sedation but other drug groups are over days (titrate the patient) until the better desired effect occurs • Not used much today 7 8 Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions Chloral Hydrate (Noctec) Paraldehyde • Oldest sleep inducing (hypnotic) depressant • 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 respiration or BP • Drug is metabolized to acetaldehyde by •Toxic Doses the liver 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 9 10 Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions Barbital Barbiturates • Is a derivative of Barbituric acid • Barbituric Acid is the parent compound • Was introduced in 1903 of all barbiturates • Became extremely popular • Basic structure lacks CNS depressant • 1912 Phenobarbital 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 11 12 2 Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions Classified Ultra short • Usually used in IV anesthesia • Based on onset and duration of action • Onset of action - seconds to about •Ultra short one minute •Short •Some Drugs •Intermediate • Methohexital (Brevital) •Long • Thiamylal (Surital) • Thiopental (Pentothal) • Propofol (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 barbiturate • Is a potent sedative/depressant • Called “Natures Quaalude” • Produces • Is primarily used as a general • Disinhibition anesthetic • Excitement • Used also for • Drunken-like behavior (but without • Sleep disorders alcohol) •Alcohol and Opiate Abuse •Amnesia • Classic Date Rape Drug • Increases dopamine levels in the brain Results in euphoria 15 16 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 17 18 3 Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions Variety of Drugs Intermediate • Pentobarbital (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 • Secobarbital (Seconal) Reds • Used primarily for sleep or sedation • Used primarily as a sleep medication 19 20 Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions Types of Drugs Long • Amobarbital (Amytal) Blues • Used for continuous sedation • Aprobarbital (Alurate) • Used in epilepsy • Butabarbital (Butisol) • Used for mild anxiety • Onset of Action 1-2 hours • Duration of Action 6-12 hours 21 22 Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions Types of Drugs Mechanism of Action • Phenobarbital (Luminal) • Binds on the Picrotoxin binding site of • Mephobarbital (Mebaral) the GABAa receptor •Result • Decrease excitability of all tissue • CNS is more sensitive to Barbiturates • RIA system is most sensitive 23 24 4 Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions 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 suicides (mostly among women) • Weak, rapid pulse • Induces other enzymes and thus • Dilated Pupils breaks down other drugs faster. 25 26 Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions High Tolerance Non Barbiturates • Rapid down regulation • Chloral Hydrate is technically here too • During withdrawal •Many types • Increased stimulation • Glutethimide (Doriden) •Seizures • Methaqualone (Quaalude, Sopor) • Delirium • Methyprylon (Noludar) •Anxiety • Ethchlorvynol (Pladidyl) •Valmid 27 28 Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions Effects Behavioral Effects • Actions and addiction 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 29 30 5 Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions Antianxiety Medications / Minor Tranquilizers Carbanates • Two Different Groups •Meprobamate •Carbanates •Miltown • Benzodiazepines •Equanil 31 32 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 33 34 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 6 Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions Classification Short Acting • Two groups • Rapid onset, short duration •Short-acting • Used to treat insomnia • Intermediate-acting • Long term duration • Differ based on • How fast they take effect • Duration of action 37 38 Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions Types Intermediate • Midazolam (Versed) •Lroazepam (Ativan) • Oxazepam (Serax) • Clonazepam (Klonopin) • Temazepam (Restoril) • Quazepam (Dormalin) • Triazolam (Halcion) • Alprazolam (Xanax) • Estazolam (ProSom) •Quazepam (Doral) 39 40 Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions Long Term Types • Are primarily used to treat general • Alprazolam (Xanax) anxiety. • Chlordiazepoxide (Librium) • Can also be used for: • Diazepam (Valium) •Muscle relaxation • Clorazepate (Tranzene) • Adjunct to Anesthesia • Halazepam (Paxipam) •Oxazepam (Serax) •Prazepam (Centrax) • Flurazepam (Dalmane) 41 42 7 Psyc 470 – Introduction to Chemical Addictions Psyc 470 – Introduction to Chemical Addictions 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 seizure • Most completely block disorders • Intermediate-Acting 43 44 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
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