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  2. ¨The main indications for pharmacotherapy in sleep
    disorders are as follows:
    • 1. To modify circadian rhythms
    • 2. To promote alertness
    • 3. and wakefulness (e.g. CNS stimulants)
    • 4. Most frequently used for excessive daytime sleepiness
    • 5. To promote and improve the quality of sleep
    • 6. To treat the large group of sleep disorders which lead to abnormal experiences, autonomic, and immunological activity, and motor activity during sleep, usually by modifying the nature or duration of individual sleep stages.
  3. Two other groups of dugs also have important effects on
    sleep although these are usually not the primary indication for their

    • 1. Drugs used to treat psychiatric or neurological disorders
    • 2. Drugs used for non-psychiatric or non-neurological disorders (Most of these affect sleep and wakefulness by altering neurotransmitter function within the brain)
  4. Melatonin

    The range of drugs that modify circadian rhythm is very limited. Melatonin is the only one that has a significant effect that is sustained
    • 1. Produced in the pineal gland
    • 2. Rapidly absorbed from the GI tract
    • 3. Peak concentration around 60 minutes
  5. Melatonin Effects on Sleep:
    Two Effects
    1. Sleep-phase alteration - Melatonin is excreted during the absence of light exposure and influences the timing of the SCN. If taken late in the evening it advances the next phase of sleep. If it is taken in the morning is causes a delay in the next phase of sleep.

    2. Hypnotic Effect - Melatonin is a mild hypnotic when given in the day at the time when levels are low. Causes the body temperature to decrease. Usually associated with sleep onset.

    3. Other actions - Vasoconstrictor, has a slight hypotensive effect.
  6. Melatonin Effects on sleep
    • Can accelerate the adaptations of the circadian rhythms to time zone changes causing jet lag
    • Can promote a more regular sleep-wake cycles in those who are blind and experience insomnia or EDS due to failure to entrain their circadian rhythms to environmental light exposure
    • Use in treating early morning wakening pattern of insomnia when there is a deficient secretion of melatonin
  7. CNS Stimulants
    • Used to combat EDS
    • Limited use due to tolerance, dependency, withdrawal symptoms, side-effects, drug interactions and the dangers of overdose.
  8. CNS Stimulants
    • Caffeine
    • 1. Has a greater effect on the CNS and skeletal muscle
    • 2. Reduce total sleep time
    • 3. Increase sleep latency
    • 4. Reduce the duration of N3 and REM
    • 5. Prolong wakefulness
    • 6. Increase mental activity
    • 7. Improve attention and vigilance (Does not improve mental function requiring originality)
  9. Caffeine Side-effects
    • 1.Respiratory stimulant and bronchodilator
    • 2. Diuresis
    • 3. Tachycardia
    • 4. Nausea, vomiting, abdominal pain and gastroesphogeal reflux
    • 5. Temors and muscle twitching
  10. Caffeine - Indications in sleep disorders
    • 1.EDS
    • 2. Central Sleep Apnea and Chyne-Stokes breathing
    • 3. Nocturnal Asthma
  11. CNS Stimulants - Nicotine
    • 1. In low does it is excitatory and in high does an inhibitory.
    • 2. Increase the release of dopamine.
  12. Nicotine - Effects on sleep
    • 1. Reduces the total sleep time
    • 2. Increases sleep latency
    • 3. Reduces sleep efficiency
    • 4. Reduces the duration of REM
  13. Nicotine - Effects on wakefulness
    • Low doses
    • 1. lead to mental relaxation
    • 2. Mild sedative
    • 3. Promotes sleep
    • High doses
    • 1. Stimulant
    • 2. Increasing arousal
    • 3. May cause agitation
    • 4. Can improve motor performance
    • 5. Commonly causes muscle tremors
    • 6. Overdoses can lead to dizziness, fits and delirium
  14. Nicotine - Other Actions
    • 1. Loss of appetite
    • 2. Nausea
    • 3. tachycardia
  15. CNS Stimulant: Cocaine
    • Increase alertness
    • Relieves fatigue
    • Euphoric action
    • Increases motor activity
  16. Cocaine - Effects on sleep
    • Chronic use - sleep deprivation
    • Reduces total sleep time
    • Increases sleep latency
    • Reduces N3 and REM sleep
  17. CNS Stimulant - Ecstasy
    Effects on Sleep
    • Reduces total sleep time
    • Increases sleep latency
    • Reduces total REM time (10% of total sleep time is spent in REM)
  18. Ecstasy - effects on wakefulness
    • Prolongs wakefulness
    • increases level of alertness
    • reduces fatigue
    • increases confidence and concentration
    • can lead to agitation and aggression
    • paranoid psychosis with auditory hallucinations (indistinguishable from schizophrenia)
  19. Ecstasy - other actions and side effects
    • appetite suppression
    • respiratory stimulant
    • raises body temp
    • tachycardia
    • mild hypertension
    • dry mouth
    • headache
    • tremors
Card Set
Pharmacology and Sleep
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