CNS Flashcards
Excitatory NTs
Acetylcholine
Glutamate
Substance P
Enkephalins
Inhibitory NTs
Norepinephrine
Dopamine
Serotonin
GABA
Sedative Hypnotics
two categories, Benzodiazepines, Nonbenzodiazepines. main uses are for sleep, anxiety, seizures. highly lipid soluble, metabolized via liver (adipose sequestering, active metabolites)
GABA Receptor
Ion channel receptor, GABA binds and allows more chloride ions to enter the cell. This causes the cell to be hyperpolarized, Sedative hypnotics either mimic GABA or enhance the binding of GABA
Benzodiazepines MOA
Bind to the benzodiazepine receptor and facilitate opening of the GABA receptor
Benzodiazepines side effects
sedation, Anterograde amnesia (memory loss), Tolerance and dependence, Residual effects ( drowsiness, confusion, psychomotor slowing)
Alprazolam (Xanax)
benzodiazepine, short duration, used for anxiety
Lorazepam (Ativan)
benzodiazepine, Short duration, used for sleep, anxiety, seizures, alcohol withdrawal
Temazepam (Restoril)
benzodiazepine, Short duration, used for sleep
Clonazepam (Klonopin)
benzodiazepine, intermediate duration, used for Anxiety, sleep, seizure (ODT)
Chlordiazepoxide (Librium)
benzodiazepine, long duration, used for alcohol withdrawal
Diazepam (Valium)
benzodiazepine, Long duration, used for Muscle relaxant, anxiety, sleep, seizure (rectal)
Benzodiazepines and Older Adults
Decreased metabolism, Increased susceptibility to side effects, Increased body fat leading to more adipose sequestering
Barbiturates MOA
Binding site on the GABA receptor and increase the duration the GABA receptor is open
Antagonize glutamate
Barbiturates side effects
sedation, Narrow therapeutic index,
High abuse potential, Ataxia
Phenobarbital (Luminal)
barbiturate, Used for seizures, alcohol withdrawal, half life = days
Butalbital (Fioricet or Esgic)
barbiturate, used for Headaches
In combination with acetaminophen and caffeine
Primidone (Mysoline)
barbiturate, used for Essential tremors, seizures
Metabolized to phenobarbital, avoid in elderly
Zolpidem (Ambien)
Z drug, used for sleep
IR and CR formulations; Females receive higher blood levels than males
Zaleplon (Sonata)
z drug, used for sleep
high fat meal delay absorption
Eszopiclone (Lunesta)
Z drug, common use: sleep
Longer acting
Z drugs MOA
Selective agonist of GABAA receptor
Z drugs side effects
sedation,
Complex sleep behavior (black box)
Psychomotor slowing (increased in elderly)
Psychiatric and behavioral effects
Buspirone MOA
serotonin agonist
Buspirone indications
general anxiety disorder
Buspirone limitations
Moderate efficacy
Slow onset (2-4 weeks)
Frequent dosing
Buspirone advantages
Well tolerated
Low risk of tolerance / dependence
Pharmacokinetics of Antidepressants
Onset of action: 2-4 weeks
Full Effect:
~3 months
Initial increase in suicidal thoughts and behaviors
Selective Serotonin Receptor Inhibitor (SSRI) MOA
Inhibit the reuptake of serotonin into the presynaptic nerve (to leave more in synaptic cleft)
Selective for serotonin synapses
Selective Serotonin Receptor Inhibitor (SSRI) side effects
Nausea and diarrhea
Jitteriness, anxiety, headache
Sexual dysfunction
Withdrawal effects if abruptly stopped
Increase suicidal thoughts
Citalopram (Celexa)
SSRI, Depression, anxiety, cardiac toxicity