Psychopharm Concepts Flashcards
Efficacy vs Effectiveness
Efficacy is controlled setting. Effectiveness is real world with missed doses.
When antacid pops up in the vignette?
They are trying to cue you in that something is impairing/changing the absorption.
Do children have more or less total body water than adults?
More total body water, less fat. They will have increased volume of distribution for water soluble drugs .
What is Phase I metabolism?
Adding a ‘handle’ on the drug mostly through CYP450. This means oxidation, reduction, or hydrolysis.
3A4 inhibitors?
Ketoconazole, grapefruit juice, erythyromycin , cimetidine, nifedipine, verapamil
What all drugs will carbamazepine induce?
depakote, haldol, OCP, protease inhibitors, midazolam, vincristine.
What enzyme does smoking induced
1A2 (the 1 looks like a cigarette). This will impact imipramine, clomipramine, luvox, trazdoone, thiothixine, haldol, fluphenazine, olanzapine, xanax, valium
Phase II Metabolism
Conjugation of drug with endogenous substrates (glucuronic acid, glutathione, sulfate, acettie.
- Glucuronides are excreted into bile while all others go into urine.
What does ‘Out the Liver Mean?’
Drugs that go directly to Phase II metabolism. (Oxazepam, temaepam, lorazepam, Lamictal).
How does remeron get its antidepressant effects?
Via alpha 2 antagonism which is a negative feedback loop. Ultimately increases level of monoamines.
What is an example of an inverse agonist?
Pimavanserin (nuplazid)
How are remeron and clonidine/guanfacine opposites?
Remeron is alpha 1 and alpha 2 antagonism
Clonidine is alpha 2 agonism.
How do the triptans work?
Constrict cranial arteries. Mechanism is that they are 5-HT1D agonists.
What makes aripiprazole unique?
It is an antipsychotic that is a partial agonist at 5HT2a and D2.
What are the 3 subgroups of monoamines?
1) Catecholamines (catechol group: NE, E, D)
2) Tryptamines (serotonin, melatonin)
3) Histamines
What cardiac problems can lithium cause?
Supraventricular arrythmias suh as sick sinus syndrome and tachy-brady syndrome. Can prolong PR interval.
Which med may SHORTEN QTc?
bupropion
Which 3 antipsychotics are the most likely to cause hypotension/falls?
Clozapine, seroquel, and chlorpromazine
Two main drugs to avoid in renal disease?
Lithium and duloxetine
In addition to the NTD, what other defects can depakote cause to baby?
Neurobehavioral teratogenicity: lower IQ, possible ID, and linked to autism. Can also have withdrawal sx, liver toicity, and hypoglycemia.
BZD and risk to baby
Cleft abnormalities can happen along with floppy baby syndrome if given right before birth.
Is doxepin safe for lactation?
No, it is the worst. L5 category.
What should you counsel anyone when giving luvox?
Caution on caffeine consumption. Luvox inhibits CYP1A2 metabolism of caffeine. Pt can develop caffeine intoxication including palpitations, anxiety, insomnia, dyspepsia, and loose stools.
Which carbamazepine interactions should one be aware of?
- erythrymocyin leads to carbamazepine toxicity
- Lowers valproate
- Lowers OCP, increased risk of pregnancy.
Common luvox interactions
- Warfarin toxicity
- Theophylline toxicity
- Clozapine toxicity
- Caffeine toxicity
Linezolid interactions
Antibiotic with MAOI activity, can lead to serotonin syndrome.
Methylene blue
Can lead to serotonin syndrome.
What is significant about ST. John’s Wort?
3A4 inducer which can decrease the plasma levels of OCP, increasing risk of pregnancy. Pharmacodynamically, it can combine with fluoxetine to cause serotonin syndrome.
What does grapefruit inhibit?
3A4 inhibitor. Separating ingestion of grapefruit from drug does not work bc cell neds 24 hours to replace 50% of inactivated 3A4 enzyme.
Buspar and grapefruit
Grapefruit can have 9x increase area under curve of buspar, vastly increased concentrations.
Cannabidiol and CYP
3A4 inhibitor which could increase bzd and opioid levels
PPI interactions
PPI’s cause 2C19 inhibition which increases levels of citalopram, escitalopram, and diazepam.