Psych Pharm Flashcards
What receptors do Benzodiazepines interact with?
GABA-A
Bind between alpha and gamma subunits
Effect of BZDs at the receptor
Binds when GABA is bound, resulting in increase in Cl- causing hyperpolarization and decreased action potentials = CNS Depression
Short acting BZDs
Alprazolam (Xanax)
Midazolam (Versed)
Triazolam (Halcion)
Oxazepamn (Serax)
Intermediate acting BZDs
Lorazepam (Ativan)
Temazepam (Restoril)
Long acting BZDs
Diazepam (Valium)
Flurazepam (Dalmane)
Clonazepam (Klonipin)
Chlordiazepoxide (Librium)
Side Effects of BZDs
Drowsiness Sedation Ataxia/Impaired motor function Confusion, anterograde amnesia (caution in elderly) Tolerance + Withdrawal
BZD effect on Pediatrics
Paradoxical Effects - hyperactivity and aggression
BZD Toxicity
Occurs when taken with more benzos, ETOH or CNS depressants
Results in severe drowsiness, ataxia
Which BZDs are not metabolized by the liver CYP enzymes?
Lorazepam (Ativan)
Temazepam (Restoril)
Which BZD is used also as a muscle relaxant and for Status Epilepticus?
Diazepam (Valium)
What med is used in BZD overdose?
Flumazenil
Flumazenil MOA
Competitive antagonist at BZD site at GABA-A
Blocks effects of BZDs and related drugs
Considerations with Flumazenil in treating BZD OD
Requires multiple doses to prevent recurrence/sedation due to short half life
Need to still establish an airway
Barbituates MOA
Non-selective GABA-A agonist and increases the duration of the Cl- channel opening
What is so dangerous about barbituates?
Non-selective GABA-A action results in all levels of CNS depression and central respiratory arrest
At toxic doses can also bind in absence of GABA and suppress activation of Glutamate NMDA
Side Effects of Barbituates
CNS and respiratory depression
Alkalinization of urine
Tolerance + Physical Dependence
Tolerance considerations w/ Barbituates
Increased metabolic clearance results in tolerance
BUT DOES NOT with respiratory depression - can be fatal!!!
DOES NOT occur with anti-seizure effects
Barbituates withdrawal s/s
8-12 hr: anxiety, tremors, restlessness, weakness, N/V, insomnia
2 days: increased SNS activity, delirium, seizures, death
Medication used to treat Epileptic Seizures
Phenobarbital
MOA of Buspirone (Buspar)
Partial 5-HT1A, 5-HT2 receptor
No interaction with GABAn
Use of Buspirone (Buspar)
Generalized Anxiety Disorder
Advantage of Buspar
Little abuse potential
Can be combined with CNS depressants, no sedative effects
No rebound anxiety or withdrawal
Side Effects of Buspar
Restlessness, dizziness, tachycardia, palpitations
Hydroxyzine MOA
Antagonist of H1 receptor (similar to benadryl)
Results in sedation/calmnness