PSYCHOPHARM/PHARMACOKINETICS Flashcards
Name the drug to treat mania with the following AE: cutaneous side effects (especially psoriasis and alopecia), LMNOP-tremors, nephrogenic diabetes insipidus –no response to ADH– increased urination, hypothyroidism, Ebstein’s anomaly, GI complaints, weight gain
LITHIUM
Medication for mood stabilization with following AE: SJS, anemia, low platelets, liver failure and pancreatitis
Lamictal
Medication used for mood stabilization and schizophrenia with following AE: EPS, NMS, akathisia
Cariprazine (Vraylar)
When switching a patient from an SSRI to a MAOI, how long does your washout period need to be to prevent serotonin syndrome? And what SSRI requires an extended washout period?
14 days; Fluoxetine requires 28 days
What drugs are CYP450 inhibitors?
SICKFACES.COM
Sodium valproate
Isoniazid
Cimetidine
Ketoconazole
Fluconazole
Alcohol, Amiodarone&
Grapefruit Juice
Chloramphenicol
Erythromycin
Sulfonamides
Ciprofloxacin
Omeprazole
Metronidazole
What drugs are cyp450 inducers?
SCRAP GP
Sulfonylureas, Smoking, St. Johns worts
Carbamazepine, Corticosteroids
Rifamycins (Rifampicin, Rifabutin)
Alcohol (Chronic)
Phenytoin
Griseofulvin
Phenobarbital
Explain the effects on urine concentration and serum sodium concentration in the following scenarios?
1) SIADH
2) psychogenic polydipsia
3) diabetes insipidus
1) SIADH: up, down
2) psychogenic polydipsia: down, down
3) diabetes insipidus: down, up
Which Alzheimer’s drug MOA is blocking NMDA receptors reducing calcium influx into cells?
Memantine
T/F: HTN is a contraindication in prescribing Buproprion?
False
CYP2D6 Inhibitors
FCMQP
Fluoxetine
Cimetidine
Methadone
Quinidine
Paroxetine
CYP1A2 Inhibitors
Cirpofloxacin
Fluvoxamine
CYP2E1 inhibitors
Disulfiram
CYP1A2 inducers
insulin
omeprazole
Which MAO-I only acts on MAO-B at lower doses?
Selegiline
What is Buspirone’s relevant MOA?
serotonin 1A partial agonist
What is most common neuropsychiatric effect of steroids?
hypomania/mania
Desipramine and protriptyline are the most or least sedating TCA?
Least sedating
Amitryptyline and doxepin are 2 of the most sedating or least sedating TCAs?
Most sedating
Which of the TCAs is most likely to cause Parkinsonian symptoms?
amoxapine
Which 3 hydroxy-benzos have the shortest half-life because they are directly metabolized by glucoronidation (go straight to phase 2 metabolism)?
LOT
1. Lorazepam
2. Oxazepam
3. Temazepam
What medication is used to treat aggression in patients with SZ, conduct disorder or ID?
Lithium
If PPI, H2-histamines or antacids are mentioned in a question what is the red flag to watch out for?
Affecting absorption of drugs
Which phase of metabolism changes a metabolites biological properties (ie bio activation or inactivation of molecule) likely through CYP450 enzyme system?
Phase I
What does this pro-drug (metabolites of them are biologically active) become after being metabolized and by what enzyme?
1. Lisdexamfetamine
2. Codeine
- Becomes active metabolite D-amphetamine (by peptidase)
- Becomes active metabolite Morphine (by CYP2D6)
Why do we have to half the dose of lamictal when someone is also prescribed depakote?
Because Depakote inhibits UGT1A4 which is responsible for breaking down lamictal so since it’s inhibited need smaller dosing since it will be broken down at lower rate
What are 4 important drugs that go directly to Phase II metabolism?
Lorazepam, Oxazepam, Temazepam (all go out the liver)
Lamictal
Which anti-depressants are more affected by metabolic drug-drug interactions?
TCAs
Fluoxetine (Prozac)
Paroxetine (Paxil)
Fluvoxamine
Which drug used to treat psychosis as part of Parkison’s disease acts as an inverse agonist (bringing receptor activity below basal or constitutive level)?
Pimavanserin (nuplazid): 5-HT 2A inverse agonist
What is the difference in monoamine/NT release between an agonist vs. antagonist ligand/drug acting on a pre-synaptic receptor?
agonists: increased negative feedback –> DECREASED release of monoamine
ie Clonidine, Guanfacine (alpha-2 agonist)
antagonist: receptor blocked from exerting its negative feedback effects —> continued release of monoamine
ie Mirtazapine (alpha 2-antagonist)
What is MOA of Buproprion?
Dopamine and NE reuptake inhibitors
What is MOA of Mirtazapine?
Blocks 5HT 2&3
histamine blocker —> drowsiness
alpha 1 antagonist –> orthostatic hypotension
What are the 4 anti-depressant drugs in the MAO-I class?
TIPS
Tranylcypromine
Isocarboxazid
Phenelzine
Selegeline
SSRIS increase risk of upper GI bleeding and bruising? T or F
TRUE
How many factors is your risk increased of torsades de pointes increased by if you have a QTC > 500ms?
2x-3x increased risk
An elderly person is visiting her opthamologist who gives her eyedrops to dilate her eyes. Several hours later she has lasting waxing and waning confusion what could be happening?
She could be delirious as the eye drops were anticholinergic and probably had some systemic effects as she likely was more vulnerable to delirium
Out of the following classes what meds should you AVOID giving to a patient with severe liver disease?
Antidepressants
SGA
FGA
Hypnotics
Antidepressants: Duloxetine
SGA:
Iloperidone, Asenapine
FGA:
Fluphenazine, perphenazine, trifluoperazine
Hypnotics:
Zaleplon, Zolpidem
Out of the following classes what meds should you AVOID giving to a patient with severe renal disease?
Antidepressants
Mood stabilizers
Antidepressants:
Duloxetine
Mood stabilizers:
Lithium
True OR False:
Intrauterine exposure to Valproic acid is a identifiable RF for Autism SD.
TRUE
True OR False:
Exposure to benzos in pregnancy increase risk of oral cleft by 0.01%.
TRUE
What is difference between pharmacodynamic DDI and pharmacokinetic DDI?
pharmacodynamic DDI : two drugs have additive activity when given together, more like how there individual results affect one another
pharmacokinetic DDI: talking about ADME effects (absorption, distribution, metabolism, excretion), affects concentration (up or down) of victim drug at its site of action
A man w/depression stopped his medications recently and developed a few days later electric-shock sensations in the head, flu-like symptoms, dizziness, excessive, vivid dreaming, and frequent crying spells. What class of medications did he likely stop?
SSRI or SNRI discontinuation reaction
- more common with shorter half-lives (fluvoxamine, venlafaxine, desvenlafaxine, paroxetine)
What is the MOA of Abilify?
partial dopamine agonist
What are the 3 FDA approved meds for treatment of Tourette syndrome?
1) pimozide
2) haldol
3) abilify
What is the MOA of disulfiram?
inhibits dopamine beta-hydroxylase which converts DA –> NE
A patient presents to clinic with GAD and vasomotor symptoms (ie menopausal symptoms), what is the best anti-depressant to start?
Venlafaxine (SNRI)
What are go to meds for tx of Bipolar disorder with mixed features?
Valproic Acid
Carbamezapine
SGA
What mood stabilizer has AE of hyperammonemia via inhibition of urea cycle (not 2/2 hepatotoxicity)?
Valproic acid
What should you treat hepatotoxicity (malaise, weakness, lethargy, facial edema, anorexia, vo miting) 2/2 valproic acid with?
IV L-carnitine
What is the mainstay of treatment of Lithium-induced NDI?
Amiloride
What is the MOA of Valproic acid?
blocks GABA transaminase –> increased synaptic levels of GABA
blocks Na channels
What is MOA of Lithium?
Lithium inhibits inositol monophosphatase
Which 2 SGA have diminished serum concentrations due to pt being a smoker b/c cigarette smoke is associated with increased CYP1A2 activity?
1) Clozapine
2) Olanzapine
What drug used to treat PMDD (although not first line) has an AE of birth defects in male fetuses?
Dutasteride (5-alpha reductase inhibitor drug)
Which HART medication used to treat HIV can result is associated with depression?
Efavirenz
—a nonnucleoside reverse transcriptase inhibitor (NNRTIs)
Benzos act on GABA-A receptors as agonists –> activation and increased chloride inflow. Benzos have high affinity for different subunits within the GABA receptor.
Benzos can act as hypnotics or anxioloytics, which subunits do each have affinity for?
hypnotic: α-1 subunit of GABA
anxiolytic: α2 and α3 subunit of GABA
What medication do you give to reverse the effects of intoxication of the following medications?
A) Benzos
B) anticholinergic poisoning
C) organophosphate poisoning
A) Flumazenil
B) If patient awake + gag reflex present –> Activated charcoal
if not –> Physostygmine
C) Pralidoxime
MOA of most effective anti-psychotics?
Post synaptic D2 receptor antagonists
OR
partial agonists
Which AP has a completely different MOA and does not act on D2 receptor?
Pimavanserin: 5-HT-2a inverse agonist/antagonist
Put these AP in order of least to most potent:
Fluphenazine (prolixin)
Haloperidol
Chlorpromazine (thorazine)
Thorazine –> Fluphenazine –> Haldol
Anti-psychotics have black box warning for elderly. Which is best choice given highest NNH and lower RR?
Quetiapine
What AP is associated with the dermatologic side effect of photosensitivity?
Chlorpromazine (Thorazine)
What medication do you use to manage following EPS from AP?
A) akathisia (3)
B) dystonia (2)
C) parkinsonism (2)
A) Beta-blockers, Benzos (increase mortality 2/2 SI and poisoning), Mirtazapine
B) benztropine, benadryl
C) benztropine, amantadine
What is the interaction between caffeine and Fluvoxamine?
Fluvoxamine inhibits CYP1A2 leading to increased levels of caffeine
What 2 drugs are seen as the 1st line agents for treating acute depression in bipolar patients?
Seroquel
Lurasidone
Lithium-induced nephrogenic diabetes insipidus is usually a self-limiting condition in which there is a down-regulation of channel aquaporin-2 in the luminal wall of the cell’s surface, leading to decreased urine osmolality and increased urine volume (polyuria). ADH levels are adequate or even high, but its action on the V2 receptor is defective.
What are the symptoms of NMS?
FEVER
fever, encephalopathy, vital sign instability, elevated enzymes (CPK), muscle rigidity
Interferon 1-beta is avoided in use with patients who suffer from what psychiatric disorder?
Depression and SI
What mood stabilizer is associated with causing PCOS in females?
Valproic acid
What 2 drugs/drug classes can induce symptoms of kleptomania?
- Abilify
- Dopamine agonists (ie bromocriptine for PD)
Combination of haloperidol and _______ (drug) can cause an encephalopathic syndrome resembling neuroleptic malignant syndrom (NMS) in some patients.
Lithium
What is one of the most common adverse effects of bupropion?
dizziness
Aspirin, can _______ (increase or reduce) the elimination of valproic acid and result in elevated blood concentrations of valproic acid.
reduce
What drug used to treat Crohn’s and MS has an increased risk of the development of progressive multifocal leukoencephalopathy (due to JC virus infection) with its use.
Natalizumab
Which TCA has possible side effect of TD?
Amoxapine
T/F: Topiramate is cleared by the kidney unchanged.
True
Correctly sequence opiates by onset of withdrawal symptoms starting with the shortest time and proceeding to the longest time.
Meperidine
Heroin
Methadone
Morphine
Heroin, meperidine, morphine, methadone
T/F: Galantamine, used to treat Alzheimers, is contraindicated in severe renal and hepatic impairment.
True
Which of the following TCAs can lead to TD due to its metabolite having dopamine receptor antagonist properties?
DAANDI-C
Doxepin, amytriptyline, amoxapine, nortryptyline, desiparamine, imipramine, clomipramine
Amoxapine
What is the treatment for acute dystonia, Parkinsonism, akinesia, akathisia from anti-psychotics?
Benztropine
Yohimbine can be used to induce panic attacks through what MOA that increases activity of noradrenergic activity in the locus ceruleus?
α2-adrenergic receptor antagonist
Which class of anti-hypertensives is not associated with depression?
ACE-I
(-pril)
