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63 Cards in this Set
- Front
- Back
Which 2 of the following NT system is diffusely projecting systems?
- NE - DA - 5HT |
NE and 5HT
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What is the primary mode of NT release from central 5HT and NE systems?
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varicosities (bulgies in the axons), NT released from vesicles to extracellular space
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The following are characteristics of which 2 NT systems?
- project broadly throughout te cerebral cortex - autoregulate their own release |
NE and 5HT
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What is the rate limiting enzyme for the following NTs?
- NE - DA - 5HT |
NE: tyrosine hydroxylase
DA: tyrosine hydroxylase 5HT: tryptophan hydroxylase |
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What is the name of the NT transporter on synaptic vesicles?
What are some NT reuptake transporters? |
transporters on synaptic vesicles:
- VMAT: proton-monoamine antiporter transporters on cell membrane: - NET - 5HTT - DAT |
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Which subtype of 5HT receptor is G protein coupled?
Which subtype of 5HT receptor is most important for clinical depression? |
5HT3: G protein coupled
5HT1: most important in depression |
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Which of the following is expressed on serotonergic cell bodies in the raphe nuclei and in hippocampus?
- 5HT1A - 5HT1D - 5HT2A - 5HT2C |
5HT1A
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Which of the following mediates the autoinhibitory mechanism of NT?
- 5HT1A - 5HT1D - 5HT2A - 5HT2C |
5HT1D
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T/F: Depression is simply caused by deficiency of neurotransmitters.
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F.
It is the changes in the receptor sensitivity that mediates the clinical effects of antidepressant drugs. |
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What is the molecular mechanism of MAOI?
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block the deamination of monoamines by binding to and inhibiting the functional flavin moiety of MAO.
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The antidepressant effect of MAOI is primarily due to the inhibition of ____. (MAO-A or MAO-B)
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MAO-A
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Phenelzine is a type of ___.
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MAOI
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What are some side effects of phenelzine?
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MAOI
- hypertensive crisis if take tyramine containing food. - orthostatic hypotension (lightheadedness, sedation) - weight gain |
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What kind of food should be avoided in patients taking MAOI?
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Tyramine containing food:
- aged cheese - fermented soy/ soy sauce - pickled food - aged yeast extract - broad-pod beans - chianti/vermouth wine |
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What drugs should be avoided when taking MAOI?
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- stimulants
- sympathetomimetics - other antidepressants - L-DOPA - opioids |
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TCA with 2nd amines preferentially affect ___ system whereas TCA with tertiary amines preferentially affect ___ system.
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NE
5HT |
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TCA does not work on ___ system.
A. NE B. DA C. 5HT |
B.
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Which drug class do the following belong to?
- imipramine - desipramine - amitriptyline - nortriptyline |
TCA
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Which of 2 of the following have the fewest side-effects?
- imipramine - desipramine - amitriptyline - nortriptyline |
- desipramine
- nortriptyline |
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Which of the following has the most side-effects?
- imipramine - desipramine - amitriptyline - nortriptyline |
- amitriptyline
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What is the most dangerous side effects of TCA?
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Cardiovascular:
- conduction delays - bundle branch blocks - 1st degree atrioventricular blocks Effects are due to Na channels. |
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What types of receptors does TCA bind to and block? (5)
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- serotonin reuptake
- NE reuptake - alpha 1 adrenergic receptor - histamine receptor - M1 |
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High affinity to histamine receptor would cause what side effects?
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sedation
- weight gain - impaired coordination - orthostatic hypotention - cognitive impairment |
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High affinity to muscarinic receptor would cause what side effects of TCA?
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- dry mouth
- constipation - urinary hesitancy - - visual acuity - aggrevate glaucoma - tachycardia - cognitive impairment - sexual: impotence |
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High affinity to alpha adrenergic receptor would cause what side effects of TCA?
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- orthostatic hypotention
- reflex tachycardia - sex: ejaculation - tachycardia - cognitive impairment |
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What are some side effects of serotonin?
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- anxiety
- anorexia - nausea/vomit - insomnia - diarrhea - sedation - weight gain - sex: desire, arousal, orgasm HT2A: anxiety, akathisia, orgasm, ejaculation 2C:anxiety, panic attacks 3: nausea, vomit, diarrhea 4: cramps, diarrhea |
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What are some side effects of NE?
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- anxiety
- tremor - tachycardia |
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What symptoms can SSRI treat?
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- depression
- OCD - panic disorder - PTSD - social phobia |
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T/F: Low dose SSRI is nonselective, high dose is selective.
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F.
Low dose SSRI is selective, high dose is nonselective. |
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What drug class do the following belong to?
- fluoxetine - paroxetine - sertraline - citalopram |
SSRI
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Where is SSRI metabolized?
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Liver: it inhibits cytochrome P450 isoenzymes.
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What receptors do SSRIs have affinity for?
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Lots!
- SRI, NRI, DRI, 5HT2C - mACh - sigma actions - inhibit NOS - CYP450 - 2D6 - 3A4 - 1A2 |
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What are these symptoms called?
- mental disturbance: agitation, confusion, insomnia - autonomic disturbance: diaphoresis, hyperpyrexia, tachycardia, hypertension - motor hyperactivity: rigidity, tremor |
serotonin syndrome
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What drug withdrawal is this?
- flu-like symptoms - restless - confusion - irritability - sleep/wake cycle disturbance |
abrupt withdraw of SSRI
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Which class of drug is venlafaxine and duloxetine?
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mixed 5HT and NE: 5HT > NE
can elevate blood pressure, so need to monitor BP while taking them. |
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Mechanism and side effects.
mirtazapine |
mechanism:
- alpha2 antagonist, enhances NE - increase serotonine transmission - 5HT2A 5HT3 blocker side effects: - sedation - weight gain - low sexual dysfunction |
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Mechanism and side effects.
Bupropion |
mechanism:
- augment NE release - block DA reuptake side effects: - seizures |
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Mechanism and side effects.
trazadone |
mechanism:
- 5HT2A antagonist - weak serotonin reuptake block side effects: - extreme sedation - priapism |
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Trazadone is primarily prescribed for ____ at low doses.
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insomnia
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What is bupropion good for?
Who is it contraindicated for? |
good for:
- depression - smoking cessation contraindicated for: people at risk for seizures or bulemia nervosa |
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Mechanism of lithium.
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- enter via Na channel
- block PIP2 regeneration, thus inhibit central adrenergic, muscarinic, and serotoninergic NT. enhances 5HT decreases DA, NE transmission |
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Which is the only drug that decrease the risk of suicide in people with bipolar disorder?
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lithium
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What is the first line treatment in bipolar disorder?
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lithium
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How would a decrease in salt(sodium) intake alter lithium's effect?
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- sodium is preferentially absorbed in renal proximal tubule.
- decrease in Na intake would increase lithium absorption and potential drug toxicity. |
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What are some side effects of lithium?
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- weight gain
- polyuria/polydipsia - hypothyroidism - sedation - fine tremor |
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What is the therapeutic index of lithium?
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Very narrow: 0.6-1.2 mEq/l
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What happens when serum lithium level is greater than 1.5 mEq/l?
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- tremor
- blurred vision - vertigo - confusion, delirium - GI |
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What happens when serum lithium level is greater than 2.5 mEq/l?
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- seizures
- obtundation, coma - arrhythmia - permanent neurotoxicity - cardiopulmonary arrest, death |
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What drugs increase lithium levels?
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- ACE inhibitor
- NSAIDS - some antibiotics - diuretics |
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What drugs decrease lithium levels?
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- caffeine
- carbonic anhydrase inhibitor diuretics - laxatives - osmotic diuretics - theophylline |
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What drugs will cause additive side effects of lithium?
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- antipsychotics: increase EPS, seizure
- antidepressant: seizure |
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What happens if a pregnant woman take lithium?
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may cause cardiac anomalies in the newborn: eg. Ebsteins anomaly.
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A newborn baby has Ebsteins anomaly. What did the mother take when she was pregnant?
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lithium
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Valproate is approved for uses in ____.
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bipolar disorder, manic phase.
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Side effects of valproate.
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- neural tube defect in pregnancy
- dyspepsia/weight gain - dysphoria, fatigue, dizziness, drowziness - sedation - tremors - bipolar disorder |
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Carbamazepine can be used in ___.
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bipolar disorder, manic phase.
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Side effects of carbamazepine.
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- neural tube defect in pregnancy
- agranulocytosis, aplastic anemia - drowsiness - slurred speech, ataxia, impaired coordination |
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Mechanism of valproate.
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increases GABA in CNS
- inhibit enzymes that catabolize GABA - block reuptake of GABA |
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Mechanism of lamotrigine.
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- block voltage sensitive Na channels
- decrease presynaptic release of glutamate and aspartate. |
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Side effects of lamotrigine.
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- headache, dizziness, insomnia
- stevens-johnson syndrome |
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Hypericum(St. John's wart) may be used to treat ___.
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depression: MAOI and inhibition of MAO uptake
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What should you do if your patient with depression is also anemic (low RBC)?
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Add folate to the treatment.
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How does TMS work?
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Utilizes Eddy currents.
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