pharm ch 12, kilgore lvl1
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| sedatives | drugs that have an inhibitory effect on the CNS
-can act as a hypnotic if given in large enough doses
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| Symptoms that sedatives reduce | -nervousness
-excitability
-irritability w/o causing sleep
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| hypnotics | cause sleep
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| dose size | helps determine if drug is sedative or hypnotic, larger doses are typically hypnotic
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| low doses | calm the CNS w/o inducing sleep
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| High doses | calm the CNS to the point of causing sleep
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| Sleep-cycle balance | all sleep needs to be balanced thru all the stages, and sleep drugs will suppress at least one aspect of the cycle
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| Non-REM sleep stage 1 | 2-5% of sleep time
-dozing/drifting off to sleep, can be easily awakened
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| Non-REM sleep stage 2 | 50% of sleep time
Relaxation, but person can easily be awakened
person has occasional REMS and slight eye movements
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| Non-REM sleep state 3 | 5% of sleep time
Deep sleep, difficult to wake person
vital stats may decrease
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| Non-REM sleep state 4 | 10-15% of sleep time
-very difficult to wake person who may be quite groggy if awakened
-dreamin occurs, esp about daily events
-sleep walking and enuresis can occur
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| REM sleep | REMs occur
vivd dreams occur
breathing may be irregular
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| Barbiturates | a sedative-hypnotic drug
-only a handful commonly used presently b/c of the safety and efficacy of benzodiazepines
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| Categories of Barbiturates | Ultrashort-anesthesia & other uses
Short & intermediate-sedative/hypnotic and convulsive condition control
Long- sedative/hypnotic, epileptic seizure prophylaxis & other uses
Long- sedative/hypnotic,
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| secobarbital | Short acting Barbiturate
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| Barbiturate therapeutic index | is very narrow, effective dose is very close to toxic level
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| how barbiturates work | in brainstem (reticular formation) bariturates inhibit GABA, therefore nerve impulses traveling in the cerebral cortex are also inhibited
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| low doses of barbiturates | sedative effects
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| high doese of barbiturates | hypnotic effects
& lowers respiratory rate
-alcholo will double the effect of barbituates
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| Barbiturate affect on enzymes | notorious inducer
-stimulates liver enzymes that cause the metabolism of many drugs shortening their duration of action
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| severe AEs of Barbiturates | -respiratory depression
-reduced REM sleep resulting in agitation (Psychotic) and inability to deal w/ normal stress
-overdose produces CNS depression (sleep to coma to death)
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| other therapeutic uses of barbiturates | -anesthesia induction
-uncontrollable seizures "Phenobarbital coma"
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| Benzodiazepines | most frequently prescribed sedative-hypnotic for it's favorable drug effect profiles
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| types of benzodiazepines | -sedative-hypnotic
-anxiolytic (medication that relieves anxiety)
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| long acting benzodiazepines | estazolam (Prosom)
flurazepam (Dalmane)
others
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| short acting benzodiazepines | temazepam (Restoril)
triazolam (Halcion)
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| Nonbenzoidazepine hypnotics | CNS depressants
share many characteristics of benzodiazepines
used to treat insomnia
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| types of nonbenzodiazepines | -salepion (Sonata)
-zolpidem (Ambien)
-eszoplicone (Lunesta)
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| affects of benzodiazepines | depress CNS activity
less suppression of REM sleep than barbiturates
Do not increase metabolism of other drugs
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| Benzodiazepines uses | -sedation,sleep induction, balanced anesthesia, moderate/conscious sedation
-skeletal muscle relaxation (mus. spasm relief)
-anxiety, agitation, depression and epilepsy relief,
-treatment of alcohol withdrawal
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| AEs of benzodiazepines | mild and infrequent
-fall hazard for frail/elderly persons
-avoid alcohol and other CNS depressants while taking bezodiazepines
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| Muscle relaxants | -act to relieve pain associ. w/ skeletal muscle spasms
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| Action of muscle relaxants | -CNS site of action
-structure and action similar to other CNS depressants
-acts directly on skeletal muscle & resembles GABA
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| muscle relaxant uses | -relief of muscle spasms
-mgmt of spasticity or severe chronic disorders
-MS, Cerebral palsy
-work best with concurrent physical therapy
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| dantrolene (Dantrium) | muscle relaxant used in malignant hyperthermia crisis
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| AEs of muscle relaxants | CNS depression symptoms
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| cyclobenzaprine (Flexeril) | commonly used muscle relaxant
central acting & treats spasticity
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| baclofen (Lioresal) | -muscle relaxant
-oral or intrathecal(spinal) route
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| temazepam (Restoril) | -benzodiazapine used for short-term MGMT of insomnia
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| zaleplon (Sonata) | -nonbeenzodiazepine hypnotic drug
-short acting (4 hrs to sleep minumim)
-effective up to 5 wks
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| zolpidem (Ambien) | - Short-acting nonbenzodiazepine hypnotic
-limit treatment of insomnia to 7-10 days
-more grogginess than sonata
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