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
Side Effects of Hydroxyzine
Sedation, dry mouth, tremor
Convulsions in high doses
Bronchodilation, respiratory depression
Use of hydroxyzine
Anxiety and tension
Treatment of Choice for Depression
CBT + Anti-depressants (SSRIs)
MOA of SSRI
Selective inhibition of 5-HT reubtake by Serotonin reuptake transporter (SERT)
SERT 300x»_space;> NERT
Do SSRIs have action at A, H1 or M receptors?
Little to NO ACTION!
5-HT1 receptor activity
Anti-depresssant
Anxiety
5-HT2 receptor activity
Insomnia
Anxiety
Agitation
Sexual Dysfunction
5-HT3 receptor activity
Nausea, GI effects
Common side effects
Nausea, GI distress, diarrhea
Sexual side effects (decreased libido, delayed orgasm)
Anxiety, panic attacks, insomnia, agitation
Others SEs:
Cardiac: QT prolongation, bleeding risks (impaired PLT aggregation)
Bone Fractures
Nocturnal bruxism
Most significant side effect due to combining SSRIs or with MAOIs due to elevated 5-HT
Serotonin Syndrome
Serotonin Syndrome symptoms
Myclonus, agitation, GI cramping, HTN
Extrapyramidal symptoms
Akathesia, Dystonia
Discontinuation Syndrome
Dysphoria, agitation, seizures, paranoia
Why should you not combine SSRIs with Tramadol?
Increased risk of seizures
Fluoxetine (What is Trade name?)
Prozac (what is generic?)
Fluoxetine (Prozac) Use
Major Depression Disorder (drug of choice)
OCD, atypical depression, anxiety, panic disorder, bulimia nervosa, binge eating
Which anti-depressant has less anorgasmia effects?
Fluoxetine (Prozac)
Escitalopram (what is the trade name?)
Lexapro (what is generic?)
Escitalopram (Lexapro) Use
MDD, GAD
*Preferred in patients with anxiety and depression
Difference between Escitalopram (Lexapro) and Citalopram (Celexa)
Escitalopram (Lexapro) is more activating and 2x more potent than celexa
Sertraline (what is trade name?)
Zoloft (what is generic name?)
Sertraline (Zoloft) Use
MDD, OCD, Panic, Anxiety, PTSD, ETOH dependence, premenstrual dsyphoric disorder
Why is Zoloft often used frequently?
4-5x more potent and selective than Prozac, often works better, well tolerated with less side effects (more selective)
Paroxetine (what is trade name?)
Paxil (what is generic name?)
Paroxetine (Paxil) Use
MDD, OCD, Panic, Social and GAD, PTSD, vasomotor symptoms
Which is the most potent SSRI?
Paxil
Which SSRI is more sedating but it is usually transient?
Paxil
Which SSRI is used first line for OCD?
Fluvoxamine (Luvox)
MOA of SNRI
Inhibition of SERT and NERT (Norepinephrine reuptake transporter)
SERT 5x > NERT
No action at alpha, H1 or muscarininc
Side Effects of SNRI
N/V/D, decreased appetite, dry mouth, constipation
Insomnia, sedation, dizziness
Sexual dysfunction
increased BP
Which Side Effect of SNRIs is not seen in SSRIs?
Elevated BP, urinary retention
Venlafazine (what is the trade name?)
Effexor (what is generic name?)
Venlafazine use
MDD, GAD, Social anxiety, panic
What is a consideration with using Venlafazine (Effexor)?
Overdose can be lethal
Side effect of Venlafazine (Effexor)?
Diastolic HTN
Duloxetine
Cymbalta
Which SNRI can be used for Diabetic Peripheral Neuropathy, Fibromyalgia, Chronic Pain?
Duloxetine (Cymbalta)
