Unit 3 Sedative Flashcards
Cerebrum
frontal, temporal, parietal, occipital lobes
Cerebral cortex - sensory & motor function, cognition, short-term memory, speech
Diencephalon
Area of brain that encloses 3rd ventricle
Thalamus (sensory relays) & hypothalamus (temperature, appetite, emotional & hormonal regulation)
Mesencephalon (midbrain)
Bridge between cerebrum/diencephalon & brainstem
Brainstem
Pons & medulla oblongata - involved in control of respiration & cardiovascular function
Reticular formation - control of consciousness, arousal & alertness
Cerebellum
planning & coordination of motor movements & motor patterns
Maintenance of balance & posture
Basal Ganglia
Deep within cerebral hemispheres
Striatum (cuadate nucleus & putamen), globus pallidus, lentiform nucleus, & substantia nigra
Control of motor activities
Limbic System
Amygdala, hippocampus, cingulate gyrus, prefrontal cortex, Hypothalamus, thalamic nuclei, mamillary bodies
Control of emotional & behavioral activity
Sedative Anxiolytics
Agents exert a calming effect or sedation with concomitant relief of anxiety at relatively low doses
Hypnotics
Agents that produce drowsiness & encourage onset & maintenance of a state of sleep
Anxiety
complex subjective feelings & behavior characterized by overwhelming & continuous worrying about life events
Benzodiazepine Sedative-Hypnotic
Flurazepam, Temazepam, Triazolam, Midazolam
Benzodiazepine Anxiolytic
Alprazolam, Clorazepate, Diazepam, Lorazepam, Oxazepam
Benzodiazepine like (Z-drugs)
Zolpidem, Zaleplon, Eszopiclone
Anziolytic Serotonin agonists
Buspirone
Anxiolytic Beta-blockers
Propranolol (symptom relief)
Barbiturates
Pentobarbital, Phenobarbital, Thiopental
Antihistamines
Hydroxyzine, Diphenhydramine
Melatonin agonist
Ramelteon
Alcohols
Ethanol
Which dose-dependent depression of CNS drug is safest to use? (linear or non-linear)
Non-linear (plateau before reaching coma & death)
Provide better therapeutic window than linear sloped drugs
Sedative-Hypnotics therapeutic uses
Relief of anxiety, relief of insomnia, sedation & amnesia, epilepsy/seizure states, control of withdrawal states, muscle relaxation
Electronegative substituent in 7th position on benzodiazepines is required for
sedative-hypnotic activity
Benzodiazepine pharmacokinetics
Good oral absorption
Metabolized by liver (CYP3A4 + glucuronidation)
Benzodiazepines with inactive water-soluble glucuronides
Lorazepam, oxazepam
Rapid metabolism, short duration
Benzodiazepines with weakly active, short-lived active metabolites
Alprazolam, trazolam
Short duration, little clinical significance (not often used)
Midazolam 1/2 life & indication
Short acting, preanesthetic
Triazolam 1/2 life & indication
Short acting, insomnia & preanesthetic
Alprazolam 1/2 life & indication
Intermediate acting, anxiety & antidepressant
Clonazepam 1/2 life & indication
Intermediate acting, seizures
Estazolam 1/2 life & indication
Intermediate acting, insomnia
Lorazepam 1/2 life & indication
Intermediate acting, anxiety, insomnia, seizures, preanesthetic
Oxazepam 1/2 life & indication
Intermediate acting, anxiety
Temazepam 1/2 life & indication
Intermediate acting, insomnia
Chlordiazepoxide 1/2 life & indication
Long lasting; anxiety, preanesthetic, withdrawal
Clorazepate 1/2 life & indication
Long lasting; anxiety & seizures
Diazepam 1/2 life & indication
Long lasting; anxiety, preanesthetic, seizures, withdrawal
Flurazepam 1/2 life & indication
Long lasting, insomnia
Prazepam 1/2 life & indication
Long lasting, anxiety
Quazepam 1/2 life & indication
Long lasting, insomnia
Age on benzodiazepines
Elderly hepatic processing slows, increased Vd, decreased rate of elimination
Benzodiazepines MOA
Potentiate effects of GABA at A receptor (chloride ion channels)
Increase frequency of opening & conductance of Cl channels = influx chloride ion = increased membrane hyperpolarization/neuronal inhibition
GABA A receptor alpha 1 subunit induces
Sedation, anticonvulsant action, anterograde amnesia