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					CNS Depressant Drugs


  Sedatives, Hypnotics, Inhalants
          . . . and Alcohol . . .
[Alcohol treated in a Separate Chapter]
CNS Depressants
a.k.a. “Sedative-Hypnotics”

   Also called “downers”, anxiolytics, sleeping
    pills, relaxants.
   Includes several chemical classes
   Common, widespread, effect on CNS
    can be summed up as decreased neural
    activity.
Dose-related Variability in Effects
        “Sedative” vs. “Hypnotic”


   LOW Doses = Sedatives --Prescribed in
    daytime for anxiety (a.k.a. “anxiolytics”)

   HIGH Doses = Hypnotics --Prescribed at
    night for insomnia (a.k.a. “sleeping pills”)
    Clinical Uses & Limitations
Rapid tolerance develops, therefore . . . CNS depressants
should be used only for short periods of time!


   Tx for occasional
    [not chronic] insomnia


   Tx for acute
     [not chronic] anxiety

   One exception . . . .
. . . Seizure Disorder is an Exception
    Tx for chronic seizure disorder (epilepsy).
    Needs to be treated long term, 24-7-365
     with an effective anticonvulsant
     But rapid tolerance develops to depressant meds,
     therefore . . .
    Recalibration is needed as tolerance develops.
     May even need to change meds occasionally.
       drowsiness when dose is too high
       seizure may occur when dose is too low,
        or upon withdrawal
Classification by Duration of Effects
        “Short-acting” vs. “Long-acting”

   Ultra short-acting -- 15 min. to 3 hours
    Med Tx = anesthetic induction
   Short-acting -- 3 to 6 hours
    Med Tx = sleep aid (hypnotic), pre-surgical
    sedative, emergency seizure control
   Intermediate-acting -- 6 to 12 hours
    Med Tx = all-day sedative for anxiety!
   Long-acting -- 12 to 24 hours
    Med Tx = anticonvulsant, or all-day sedative
Clinical Uses of Sedatives

   Short-Acting Sedatives       Long-Acting Sedatives
      Insomnia                     Epilepsy / Seizure
      Acute alcohol                Anxiety disorders
       withdrawal                    (phobia, panic
       (prescribed or self-          attack, obsessive
       medication)                   compulsive disorder,
      Pre-anesthetic drug           etc.)
       (anesthetic                  Muscle Relaxants to
       induction).                   reduce painful
                                     muscle spasms.
    CNS Effects
 Depression of the CNS, ranging from
  mild sedation to coma, or even death.
 Degree of CNS depression related to:

       type of drug
       dose
       route of administration
       expectations
       condition of patient/user
    Depressants: Patterns of Abuse
   Intoxication is qualitatively similar to being
    drunk on alcohol. Especially true with
    *short-acting sedatives in larger doses.
   4 basic patterns of abuse:
       Elderly – accidental related to sleeping pills.
       Middle-Age - accidental – anti-anxiety
       Young users --intentional combined w/
        alcohol for quicker intoxication
       Deviant sexual predation --planned
        criminal sexual assault upon another
        human being.
Types of Sedatives

   2 main classes used clinically
      Benzodiazepines--safer clinically
      Barbiturates--more bang; more abused

   Of the 2 types, barbiturates* are more
    potent and have “greater potential for
    abuse” and related problems.


                                      Bang !
Benzodiazepine Sedatives
                Well-known Benzo’s:

                   Valium = diazepam


                   Xanax = alprazolam


                   Librium = chlordiazepoxide
        Anxiety, Sedation, Sleep
 Ativan              Serax
 Rohypnol            Dalmane
 Klonopin            Restoril
 Tranxene            Halcion
 Sonata              Ambien
 Mylostan            Lunesta




    Muscle Relaxant, Anticonvulsant
 Benzodiazepine Action
 Most prescribed class of drugs
 Safer than barbiturates
 Slightly different NT action
  than barbiturates
 Enhance the action of GABA
       Bind near GABA sites
       GABA is an inhibitory NT;
        therefore calms CNS
       Benzo’s cause more GABA activity
        than normal, resulting in sedation.
Physical Side Effects
Parasympathetic Branch of Autonomic NS
    Reduced breathing rate

    Hypotension ( BP)

    Bradycardia (slow   )

    Depressed gag reflex
Other Serious Side Effects

  CNS: drowsiness, ataxia, depression,
   slurred speech, dizziness, impaired
   vision, confusion, amnesia, sleep
   disturbances, coma, or death

  CV: cardiovascular emergency,
   dysrythmia

  GI: nausea
Behavioral Toxicity


   Behavioral toxicity from sedatives:

    VERY similar to alcohol intoxication!!
    Impaired judgment, poor coordination,
    loss of inhibition, tendency toward
    violence, euphoria, sexual arousal etc.
Dependence Potential

  Potential for both physical & psychological
   dependence with powerful depressants.
  Major considerations (1) type of drug,
   (2) dose, and (3) duration of effect/ time
   course.
                              The Bigger, Quicker Bang . . .
                                 the more potential for
                                      dependence!

Short-acting Types cause a quicker, more intense effect
Dependence & Duration of Effects

   SHORT-ACTING depressants (quick, but short
    duration) result in a “bigger bang” and
    therefore are much worse than longer-
    acting (slower) depressants .
    Increased potential for dependence!
    More severe withdrawal.

                           Bigger Bang . . .
                         but doesn’t last long!
Withdrawal Danger from Sedatives

    Withdrawal symptoms:
      Increased anxiety, insomnia, tremors,
       confusion, hallucinations
      Seizures 2-3 days following
      5% die from abrupt withdrawal
    Physiological Toxicity !
 Sedative   abuse can be deadly
 Decrease in respiratory rate
 May stop breathing entirely!
 Especially dangerous combined w/ alcohol

      ALCOHOL + Sedatives = possible death

   Sudden withdrawal from sedatives may
    result in seizure/convulsions.
    This can also be deadly.
   Gradual, clinical “detox” is advised.
Intentional or Accidental Danger

				
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posted:7/3/2011
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