Random Flashcards
What is monoamine?
Molecule with a single amine group.
What are the 3 monoamine groups?
- catecholamines: NE, epinephrine, and DA
- tryptans: 5-HT and melatonin
- histamines
Antidepressants with anticholinergic effects
TCAs, paroxetine, and duloxetine
Antipsychotic with most antichol effect
- clozapine, olanzapine, most FGA
Which antidep we should avoid in moderate hepatic dx?
Duloxetine (also kidney dx)
Which antidepressants should have dose reduction with hep disease?
Citalopram
Escitalopram
Fluoxetine
Paroxetine
Which mood stabilizers require dose reduction in hep disease?
Carbamazepine
Valproate
Lamotrigine
Which SGA we should avoid in severe hep disease?
Iloperidone
Asenapine
Which SGA we should reduce dose in hep disease?
Lurasidone
Risperidone
Quetiapine
Brexpiprazole
Which FGA we should avoid in severe hep disease?
Phenotiazines (fluohenazine, perphenazine, trifluoperazine)
Which hypnotics should be avoided in severe hep disease?
Zaleplon
Zolpidem
Which hypnotics should have decrease in dose in hep disease?
Eszopione
Which antidepressant should be avoided in severe kidney disease?
Duloxetine
Which antidepressants should have dose reduction in kidney disease?
Mirtazapine
Paroxetine
Venlafazine
Which mood stabilizers should have dose reduction in kidney disease?
Gabapentin
Lamotrigine
Topiramate
Which mood stabilizer should be avoided in severe kidney disease?
Lithium
Which BZD should have dose reduction in kidney disease?
Chlordiazepoxide
Midazolam
Which hypnotics should have dose reduction in kidney disease?
Zaleplon
Zolpidem
Midazolam
Chlordiazepoxide
Which antidepressant should be avoided in pregnancy?
Paroxetine- concern for cardiac malformation.
Unsafe medications in pregnancy (category X)
- isotretinoin
- thalidomide
- some BZD (triazolam, estazolam, flurazepam, quazepam)
- leflunomide
Lithium’s risk in pregnancy
- increases risk of Ebstein’s anomaly (malformation of tricuspid valve)
- increases the risk from 1/20,000 to 1/2000-1/1000 -> 5-fold increase
- floppy baby syndrome (cianosis, hypotonicity) from exposure during labor
Lithium use in pregnancy- what to do
- get a echocardiogram if exposure during 1st trimester
- monitor levels and adjust dose due to shifting fluid levels
- prior to delivery decrease dose to half or stop temporarily
Valproate risk in pregnancy
- organ dysgenesis (fetal valproate syndrome): neural tube defects (from 0.03% to 1-5% - 20-50-fold increase) + craniofacial defects + cardiac abnormalities
- neonatal toxicity: withdrawal sx, liver tox, hypoglycemia
- neurobehavioral teratogenicity: lower IQ, possible ID/autism
Avoid use in pregnancy! If needed, supplement folate.
Carbamazepine risk in pregnancy
- organ dysgenesis (fetal carbamazepine synd): craniofacial defects (11%), fingernail hypoplasia (26%), developmental delay (20%), neural tube defects (0.5 - 1%), doll-like faces, long philtrum, palpebral folds
- neonatal tox: transient hep tox
- Avoid if possible. If needed, supplement with vitamin K
BZD risk in pregnancy
increases risk of oral cleft by 0.01% (not so intense)
Safest medication during lactation
Acetaminophen
Contra-ind in lactation
doxepin
Meds that interact with Li
NSAIDs, ACEi, and angio II antag
Meds that interact with TCAs and cause tox
fluoxetine and paroxetine (via CYP 2D6)
Meds that interact with carbamazepine
erythromycin (via CYP 3A4)
Med that interact with cariprazine, lurasidone , and quetiapine and cause reduction
carbamazepine (via CYP 3A4)
Med that interact with lamotrigine and lumateperone and cause tox
valproate (via UGT 1A4)
Med that interact with valproate, OCP, PPIs and cause reduction
carbamazepine
FGA and SGA - mostly metabolized by which CYP 450 enzymes? What are the exception?
1A2, 2D6, 3A4
- lumateperone (phase 2)
- olanzapine (phase 2)
- ziprasidone (aldehyde oxidase)
OCPs- mostly metabolized by which CYP 450 enzymes?
3A4
TCAs - inhibit which of the CYP 450 enzymes?
2C19
fluoxetine - inhibits which of the CYP 450 enzymes?
2C19, 2D6 , (some 2C9)
fluvoxamine - inhibits which of the CYP 450 enzymes?
1A2, 2C9, 2C19, (some 3A4)
paroxetine and other SSRIs/SNRIs- inhibits which of the CYP 450 enzymes?
2D6
Drugs that could interact and cause hypertensive crisis
- MAOI
- bupropion
- L-dopa
- methylphenidate
- pseudoephedrine
- tyramine-rich foods
Drugs that could interact and cause serotonin synd
- MAOI, TCA, SSRI, mirtazapine
- opiates: methadone, meperidine, fentanyl, tramadol
- linezolin (Zyvox) - ATB with MAOI activity
- methylene blue
Serotonin synd
Confusion, agitation, dilated pupils, headache, autonomic instab, N/V, diarrhea, tachycardia, tremor, sweating
Only conclusive rec re: genotyping (International society of psychiatric genotyping 2019)
- HLA-A and HLA-B prior to use of carbamazepine and oxcarbazepine
- genetic info for CYP 2C19 and CYP 2D6 would likely be most beneficial for pt with inadequate response or adverse reaction to a previous antidepressant or antipsychotic trial
Caffeine - metabolized by which CYP 450?
What increases caffeine’s level? What meds’s levels are increased by caffeine?
1A2 (and inhibits it) = same as fluvoxamine and opposite of smoking
- levels increased by: fluvox, fluoxetine, parox, cimetidine, omeprazole
- caffeine increases: asenapine, clozapine, pimozide, duloxetine, ropinirole
Grapefruit - metabolized by which CYP 450? What other meds are met by the same enzyme?
What meds’s levels are increased by grapefruit?
Grapefruit interferes with gut absorption of which meds?
3A4 (and inhibits it) = same as lumateperone, pimozide, erythromycin, ketoconazole, cannabidiol
- increases level of many BZD, amphetamine, sertraline, morphine, buprenorphine, buspirone, some antipsychotics
- decreases gut absorption of digoxin and statins
cannabidiol
- pharmacokinetic caution with which meds?
- metabolized by which CYP 450?
- inhibits which CYP 450 enzyme?
- other pharmacodynamic cautions
- valproate, clobazam, acetaminophem = all increase ALT/AST
- 3A4, 2C9, 2C19
- 3A4 -> can increase level of BZD, opioids
- CNS depressants (alcohol, opioids, BZD, etc)
Cigarette and cannabis smoking induces what CYP 450 enzyme?
Which substance is responsible for it?
It means decrease in which meds?
- 1A2
- polycyclic aromatic hydrocarbons
- some TCAs, dulo, fluvo, mirta, trazodone, FGA, clozapine, olanzapine, asenapine, alprazolam, diazepam, ropinirole, heparin, caffeine
Hospitalization / quitting may result in increase level of those meds!
St. John’s Wort
- met and inducer of what P 450?
- decreases level of what?
- another important pharmacodynamic concern
- 3A4
- OCP, sertraline, valproate, phenytoin, haloperidol, MDZ
- inhibits reuptake of 5-HT, NE, and DA - can contribute to serotonin synd
Omeprazol and other PPIs
- inhibits what enzyme?
- met by which enzyme?
- 2C19 - increases level of citalopram (max dose 20 mg daily), escitalopram, DZP
- 3A4
Cimetidine inhibits which enzyme?
Increases level of which meds?
- 3A4
- chlordiazepoxide, diazepam, some TCAs, citalopram
Elevated gastric pH increases absorption of which med?
amphetamines
Meds assoc with orthostatic hypotension
- phenelzine
- tranylcypromine
- clozapine
- quetiapine
Antidep more likely to cause manic-flip
TCAs
