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99 Cards in this Set
- Front
- Back
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List the classes of antidepressants you should know:
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Monoamine Oxidase Inhibitors (MAOIs)
Tricyclic Antidepressants (TCAs) Selective Serotonin Reuptake Inhibitors (SSRIs) Serotonin & Norepinephrine Reuptake Inhibitors (SNRIs) |
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Which condition is treated with lithium?
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Bipolar disorder.
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These drugs are tricyclic antidepressants (TCAs):
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Imipramine
Amitriptyline Desipramine Nortriptyline Doxepin Clomiphene Amoxapine |
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What are 5-HT reuptake inhibitors?
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A fancy name for serotonin reuptake inhibitors.
If you must know, it's 5-hydroxytryptamine. |
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What is the theraputic usage for TCAs (tricyclic antidepressants)?
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-Major Depression
-Chronic pain -OCD |
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This tricyclic antidepressant treats bed-wetting:
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Imipramine
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This is the least anticholinergic of the tricyclic antidepressant drugs:
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Desipramine
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This tricyclic antidepressant is used to treat OCD:
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Clomipramine
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This tricyclic antidepressant is used to treat neuropathic pain and migraine:
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Amitryptyline
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This tricyclic antidepressant involves the blockade of some types of D2 receptors:
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Amoxapine
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Which 3 important mechanistic effects are associated with TCAs?
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Activity as a(n):
-Antimuscarinic -α1 blocker -Histamine1 blocker |
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What results from the antimuscarinic activity of TCAs?
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-Mydriasis
-Cycloplegia -Urinary retention -Sedation |
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What results from the α1 blocking activity of TCAs?
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Hypotension + Orthostasis
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What results from the H1 blocking activity of TCAs?
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Sedation + Weight gain
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What happens in the case of overdose of TCAs?
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Coma, convulsion, and cardiotoxicity.
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________ polymorphism is associated with the slow metabolism of TCAs in the case of serotonin syndrome.
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CYP2D6
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One major benefit of this antidepressant drug is that it does not produce impotence:
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Bupropion
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What is used to treat TCA overdose?
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Sodium bicarbonate (attaches to Na+ channel to decrease C/V effects)
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What is the mechanism of action for bupropion?
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-Inhibition of DA and NE reuptake
-Noncompetitive antagonism at nicotinic receptor |
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What are the main theraputic uses for bupropion?
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-Major Depression
-Cessation of smoking |
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This drug is a partial nicotinic receptor agonist that has side effects of erratic behavior and suicide:
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Varenicline
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In which type of patient is bupropion contraindicated?
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The bulimic patient.
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What mechanism does bupropion follow on the M and H1 receptors?
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Bupropion doesn't have too much muscarinic activity and doesn't really act on the histamine receptor. That's one of the benefits of the drug.
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What is the mechanism of action of mirtazapine?
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-Blockage of α2 receptors
-↑ NE and 5-HT release -Opposite mechanism to Clonidine |
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How is mirtazapine used theraputically?
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For:
-Major depression -Sedation |
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What side effects (toxicity) are associated with mirazapine?
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Sedation + Weight gain.
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This class of antidepressants treats fibromyalgia:
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Serotonin-norepinephrine reuptake inhibitors (SNRIs)
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Which drugs are classified as serotonin-norepinephrine reuptake inhibitors (SNRIs)?
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Duloxetine
Venlafaxine Desvenlafaxine Milnacipran |
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What is the theraputic usage for SNRIs?
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-Major depression
-Chronic pain -Fibromyalgia -Neuropathic pain |
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Do SNRIs act on the H1 or M receptors?
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No.
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Which class of drugs is mechanistically most similar to TCAs?
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SNRIs
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One thing about these antidepressants is that they take ~4 weeks of administration to elicit a full effect:
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Selective Serotonin Reuptake Inhibitors (SSRIs)
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Which special conditions do SSRIs treat?
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-PTSD
-Premenstrual dysphoric disorder -Bulimia |
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Which drugs are classified as selective serotonin reuptake inhibitors (SSRIs)?
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-Fluoxetine
-Fluvoxamine -Citalopram -Paroxetine -Sertraline -Escitalopram |
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Which classes of drugs are associated with serotonin syndrome?
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TCAs, SSRIs, and MAOIs
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Which drug of the SSRIs is most interactive with CYP450-2D6?
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Fluoxetine
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Which drugs of the SSRIs are the least interactive with CYP450-2D6?
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Sertraline, Citalopram, and Escitalopram
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What side effects are associated with SSRIs?
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Insomnia
Headache Nausea Vomiting Platelet abnormalities Impotence |
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Which drug classes have the side effect of impotence and priapism, respectively?
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SSRIs = impotence
SARIs = priapism |
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Which antidepressant drugs are classified as serotonin reuptake inhibitors and blockers (SARIs)?
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Trazodone + Nefazodone
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What are the mechanisms of action of trazodone and nefazodone?
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-Serotonin reuptake inhibition / block (SARI)
-α1 block -H1 block |
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How are SARIs used theraputically?
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-Major depression
-Sedation -Sleep aid |
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What mechanisms involved with SARIs permit priapism and sedation?
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Priapism = block of α1 receptors (vasodilation)
Sedation = block of H1 |
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This antidepressant drug is hepatotoxic:
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Nefazodone
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What should you be wary of when prescribing trazodone as an antidepressant?
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That trazodone levels will be increased if the patient is also taking drugs that inhibit CYP3A4 metabolism.
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When prescribing this type of antidepressant, you should tell your patients to avoid tyramine-containing foods such as aged cheese and meats, red wine, avocado, and chocolate.
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Monoamine Oxidase Inhibitors (MAOIs)
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What is the theraputic usage for MAOIs?
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Refractory depression.
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Which antidepressant drugs block MAOA receptors (MAOIA)?
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Phenelzine
Tranylcypromine Isocarboxazid |
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Which antidepressant drugs block MAOB receptors (MAOIB)?
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Selegiline
*only dopamine |
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How is selegiline used theraputically?
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-Parkinson's disease
-Major depression |
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What happens if a patient taking MAOIs decides to eat a lot of cheese and meat?
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Hypertension
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Which drugs would elicit Serotonin syndrome when interacting with MAOIs?
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-SSRIs
-TCAs -Meperidine -Dextromethorphan -Triptans -Linezolid -St. John's Wort |
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What would happen if a patient takes St. John's Wort with MAOIs?
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Serotonin Syndrome
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What is the mechanism of action of lithium?
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Blocking the anenylyl cyclase signaling for NE.
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What side effects are associated with lithium?
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-Tremors
-Leukocytosis -Polyuria / Polydipsia -Hypothyroidism -Ebstein anomaly |
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How can the side effect of tremors be avoided when administering lithium?
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Using beta-blockers.
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Which mechanism is responsible for causing polyuria and polydipsia when administering lithium?
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When using lithium, ADH response is lost.
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What is ADH?
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Anti-diuretic hormone.
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What is the benefit of administering amiloride with lithium?
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Amiloride prevents the diabetes insipitus symptoms induced by lithium.
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What is the mechanism by which amiloride attenuates polyuria and polydipsia caused by lithium?
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Blocking lithium entry through the sodium channel.
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What is Ebstein's anomaly?
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When the tricuspid valve leaflets extend into the apex of the right ventricle, causing murmur, regurgitation, and hypertrophy.
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What is an alternative to lithium treatment during pregnancy?
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lamotrigine
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What can happen if a patient takes lithium while pregnant?
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The child has an increased risk of developing Ebstein's anomaly.
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What are 4 important drugs used to treat bipolar mania / bipolar syndrome?
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Lithium
Valproate Carbamazepine Lamotrigine |
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Valproic acid, carbamazepine, and lamotrigine are all used to treat...
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Partial and tonic-clonic seizures.
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These drugs are associated with Stevens-Johnson syndrome:
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Carbamazepine + Lamotrigine
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What is the mechanism of action of valproic acid?
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-Blocks Na+ & T-type Ca2+ channels
-↓ glutamate at NMDA receptors -↑ GABA receptor action -↑ GABA synthesis -Blocks GABA degradation |
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What is the mechanism of action of carbamazepine?
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-Blocks Na+ channels
-Blocks NE reuptake |
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What is the mechanism of action of lamotrigine?
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-Potentiation (↑) of GABA
-Blocks VG Na+ channels -Blocks glutamate |
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Which drug is used to treat Lennox-Gastaut syndrome?
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lamotrigine
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Which drug is used to treat trigeminal neuralgia?
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Carbamazepine
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Which drug is used to treat migrane prophylaxis (in addition to bipolar syndrome)?
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Valproic Acid
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Which drugs cause neural tube defects?
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Valproic Acid + Carbamazepine
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Which drug has a Black Box Warning?
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Lamotrigine (for SJS syndrome)
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What is a Black Box Warning?
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The strictest warning label that can be placed on prescription drugs (by the FDA).
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Which 2 drugs treat absence seizures (in addition to bipolar disorder)?
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Valproic Acid + Lamotrigine
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This drug has a side effect of hepatitis:
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Valproic Acid
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What is the action of valproic acid and carbamazepine on CYP2D6 and CYP3A4?
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Valproic acid = Inhibitor of CYP2D6 and CYP3A4
Carbamazepine = Inducer of CYP3A4 |
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What side effects are associated with carbamazepine?
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-Drowsiness
-Ataxia -Diplopia |
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What is SIADH?
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Syndrome of Inappropriate Antidiuretic Hormone Secretion (water intoxication)
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Which mood stabilizing drug is associated with aplastic anemia?
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Carbamazepine
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Which mood stabilizing drug is associated with SIADH?
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Carbamazepine
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What about lithium treatment can be especially dangerous?
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Its narrow theraputic index (toxicity ≥ 1.5 mEq).
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Which atypical antipsychotics should you know?
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Risperidone
Olanzapine Quetiapine Aripiprazole Ziprasidone |
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What is the general mechanistic goal for atypical antipsychotics?
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To increase DA.
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What is the mechanism of action of risperidone?
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Blockade of:
-5-HT2A >>> D2 -D3 -D4 |
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All atypical antipsychotics prolong the _______ interval.
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QT
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What is the QT interval?
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The interval of electrical impulses in the heart. (Q and T-waves)
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What is the mechanism of action of olanzapine?
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Blockade of:
5-HT2A > H1 > D4 > D2 > α1 > D1 |
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What is the mechanism of action of quetiapine?
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Blockade of:
H1 > α1 > M1,3 > D2 (short) > 5-HT2A |
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What is the mechanism of action of aripiprazole?
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-Partial D2 agonist
-5-HT2A antagonist |
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What is the mechanism of action of ziprasidone?
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-Blocks 5-HT reuptake
-Blocks NE reuptake |
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Which atypical antipsychotic drug has few ANS and extrapyramidal effects?
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Olanzapine.
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Which atypical antipsychotic drug has the side effect of hyperlipidemia and hyperglycemia due to increased prolactin?
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Risperidone.
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Which atypical antpsychotic drug has a side effect of hypotension (from blocking α1 receptor)?
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Risperidone.
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Which atypical antipsychotic drug has a side effect of akathisia?
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Aripiprazole.
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Which atypical antipsychotic drug has side effects including skin reactions and eosinophilia?
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Ziprasidone.
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What is akathisia?
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A state of agitation or distress (resulting from antipsychotics).
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What is eosinophilia?
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Increased eosinophils in the blood, often due to allergic reaction.
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