principles of psychopharmacology

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principles of psychopharmacology
2013-03-17 01:00:18

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  1. Signal Transduction Cascades include?
    G-protein linked, ion-channel linked, hormone receptors and tyrosine kinases
  2. A neurotransmitter receptor type that is long acting, most common in the CNS, voltage channels are modulated either via G-Protein activation directly or through second messenger systems (cAMP), and 60% of psychotropic drugs target these receptors
    Metabotropic (G-protein)
  3. A neurotransmitter receptor type that is fast acting opening, fast synaptic transmission, will see results quickly at the cellular level is?
    Ionotropic (Ligand gated channel)
  4. May modulate voltage channels directly or indirectly.
    Metabotropic (G-proteins)
  5. Most common in the CNS
    Metabotropic (G-protein)
  6. fast acting
    Ionotropic (Ligand gated channels)
  7. Longer acting, slow
    Metabotropic (G-protein)
  8. Two receptor targets for G-proteins?
    • 12-Transmembrane region transporter (30%)
    • 7-Transmembrane region transporter (30%)
  9. The three ligand gated and voltage sensitive receptor targets?
    • 4-Transmembrane region transporter (20%)
    • 6-Transmembrane region transporter (10%)
    • Enzyme (10%)
  10. What Enyzmes (10%) are targets for psychotropic drugs?
    Monoamine oxidase and Acetylcholinesterase.
  11. Which two receptor targets are important when looking at Benzodiazepines?
    7-transmembrane region transporter and 4-transmembrane region transporter.
  12. Which receptor type either increases permeability or decreases permeability?
    Ligand Gated and Voltage Sensitive (40%)
  13. Sites of action of NT?
    Pre-synaptic: synthesis, release, storage, metabolism and re-uptake or Post-synaptic.
  14. Which receptor can regulate, open voltage gated channels or binds and uses second messengers which influences permeability?
  15. Pre-synaptic actions
    Synthesis, release, storage, metabolism and re-uptake.
  16. Amino acid neurotransmitters in the brain?
    Glutamate and GABA
  17. Monoamine neurotransmitters in the brain?
    Dopamine, Norepinephrine, Serotonin and Histamine.
  18. A neurotransmitter in the brain that is not an amino acid or monoamine?
  19. Primary excitatory NT in the brain
  20. NT that uses NMDA, AMPA & Kainate ionotropic receptor subtypes?
  21. NT that has an upstream effects on other NT pathways in brain?
  22. Implicated in Schizophrenia and delusional disorder?
  23. Implicated in seizure disorder?
    Glutamate & GABA
  24. Primary inhibitory NT in the brain?
  25. Two main receptor types of GABA?
    GABA A:ionotropic and fast & GABA B: metabotropic and long.
  26. Implicated in Schizophrenia, Bipolar Disorder and Anxiety Disorder?
  27. Implicated in pain management because innervation of opioid receptors?
  28. Implicated in mood and anxiety disorders such as depression, bipolar disorder and anxiety disorder?
  29. This NT has a neuronal pathway that originates in the Raphe Nucleus (in the midbrain pons area)?
    Serotonin (5HT)
  30. The NT implicated in mood, appetite and sleep?
    Serotonin (5HT)
  31. The number of receptor subtypes for Serotonin?
    13 receptor subtypes (12 are metabotropic)
  32. Presynaptic serotonin receptor subtype?
    5HT1a (autoreceptor) feedback loop, helps regulate, can shut off, so essentially are antagonist.
  33. Post synaptic Serotonin receptor subtypes?
    5HT2a, 5HT2c, 5HT3 AND 5HT4.
  34. Serotonin receptor subtypes that also works centrally in the spine and gut and can see sexual side effects and GI side effects?
    5HT2a, 5HT2c, 5HT3 & 5HT4.
  35. NT whose neuronal pathway is mostly in the Locus Coeruleus (innervates the prefrontal cortex)?
  36. NT implicated in arousal, attention and pain?
  37. NT whose receptors are metabotropic and include: Alpha 1 & 2 and Beta 1 & 2.
  38. NT whose neuronal pathway mostly begins in the Substatia Nigra?
  39. NT implicated in mood disorders, anxiety, ADHD, Dependence and addiction, Schizophrenia & Movement disorders?
  40. NT whose receptors are metabotropic and include:  D1-D5
  41. Alcohol, opioids, benzos and other addictive substances stimulate what NT to cause addiction (brain learns this feels good)?
  42. Dopamine receptor subtype that has to do with schizophrenia, movement disorders, attention span and reward centers?
    D2, 3 & 4
  43. Monoamine that has metabotropic receptors and Four subtypes H1-4? (also located in the stomach and released by mast cells)
  44. Monoamine implicated in sleep-wake cycle and antagonizes monoamine release in the CNS(can lead to mood problems)?
  45. Indications of Antidepressants?
    Depression, Anxiety, OCD, PTSD and eating disorders.
  46. Which individuals will you see more risk than benefit in Antidepressant therapy?
    Children, Adolescents & elderly.
  47. Fluoxetine (Prozac), Paroxetine (Paxil), Sertraline (Zoloft), Citalopram (Celexa), Escitalopram (Lexapro) are classified as what class and what is their primary use?
    SSRIs-Antidepressants that help with negative symptoms of depression.
  48. Metabolized by CYP450 (1A2, 2D6 and 3A4).

    1A2 is induced by nicotine so smoking causes pt.s to metabolize drug faster.
  49. How do you prescribe SSRI's?
    Start low, go slow, usually increasing dose in 2-4 weeks depending on sx's (because you want to monitor for side effects).
  50. A generally safe medication and often non-lethal in overdose, however can interfere with clotting cascades?
    SSRI's (more serotonin can lead to bleeding)
  51. Chronic NSAID use or GERD can increased likelihood of GI bleed from ulcers using what class of antidepressants?
  52. SSRI common side effects?
    GI upset, akithesia (restlessness), sexual side effects, headache and dry mouth.
  53. SSRI serious side effects?
    Serotonin syndrome, increased suicidal thoughts in patients under 25 years old (black box warning).
  54. Can get QT prolongation in prolonged doses with which SSRI?
    Citalopram (Celexa)
  55. Are SSRI's fast acting on mood?
    No, will take awhile to act on mood b/c needs to change genetic expression.
  56. What is the MOA of SSRI's?
    Binds to serotinergic receptor site and blocks serotonin from getting on re-uptake pump(atpase pump). The pump is regulated by Na/Cl/K. This will increase the level of Serotonin in the synaptic cleft available to bind to the postsynaptic receptor.
  57. Dose range in 20-60mg at night and is FDA-approved for PTSD?
  58. Side effects of Paxil?
    Nausea, Headache, Lightheaded, anxiety, and sexual dysfunction.

    will also see some anticholinergic type reactions, dry mouth etc.
  59. If you miss a dose of paxil you get incredibly uncomfortable?
    Yes, so not good for young population, causes a discontinuation syndrome.
  60. Paroxetine (Paxil) affects which receptors and is metabolized by which pathway?
    M-ACH(muscarinic), NRI(Norepinephrine reuptake inhibitor), SRI(serotonergic reuptake inhibitor), NOS(nitric oxide) and is metabolized by cyp 2D6.
  61. Paroxetine (Paxil) is what pregnancy category?
    Category D because causes heart defects in the fetus.
  62. SSRI's given in combination with TCA's or MOAI's can cause what side effect?
    Serotonin syndrome

    Also can be caused by saint johns wart.
  63. Tramadol used in combination with SSRI's causes what side effect?
    Lowers seizure threshold.
  64. An SSRI that actively metabolizes into itself, half-life is long up to 30 days, and a good choice for a patient with compliance issues.
    Fluoxetine (Prozac)
  65. Venlafaxine (Effexor, Desvenlafaxine (Pristiq) and Duloxetine (Cymbalta) are which class of Antidepressant?
    SNRI (Serotonin–norepinephrine reuptake inhibitor)
  66. SNRI's are metabolized by which pathway?
    1A2 & 2D6

    1A2 is induced by nicotine so smoking causes pt.s to metabolize drug faster.
  67. Common side effects of SNRI's include?
    Headache, anxiety, GI disturbance, sexual side effects(b/c serotonergic innervation), potential impact on BP(b/c alpha and beta innervation)
  68. Serious side effects of SNRI's?
    Serotonin syndrome(autonomic instability, high fever, supportive measures), suicidal ideation in patients under 25 years old.
  69. Dose range: 75-300mg and is used as a dual agent, often poor tolerance at higher doses and minimal drug interactions.
    Venlafaxine XR (Effexor XR)
  70. Common side effects of Venlafaxine xr (effexor xr) are?
    nausea, headache, lightheaded, anxiety, sexual dysfunction, sweats, elevated blood pressure (higher doses).
  71. What SNRI do you want to continually monitor bp which pt. is taking?
    Venlafaxine xr(effexor xr), increased DBP 10-20mmhg so be careful with HTN.
  72. With Effexor over what dose to you see it target NE?
    Over 150mg so monitor bp.
  73. Which SNRI is FDA approved for diabetic neuropathy, pain and depression?
    Duloxetine (Cymbalta)
  74. Buproprion (Wellbutrin) is classified as?
    NDRI (Norepinephrine-dopamine reuptake inhibitor)

    Comes in two formulations SR (most common) and Extended-Release (XR)
  75. Wellbutrin is metabolized by what pathway?
  76. Side effects of Welbutrin SR?
    • Headache, sweats, anxiety & insomnia.
    • Also, lowers seizure threshold and can cause irritability/anxiety.
  77. Do you give wellbutrin to an individual with an eating disorder?
    No, because lowers the seizure threshold.

    Also do not use with Alcohol.
  78. True or False, Can use wellbutrin for negative symptoms of depression while waiting for SSRI's?
    Yes, also helps with sexual dysfunction of SSRI's.
  79. How does wellbutrin target sxs of ADHD?
    b/c targets dopamine and works on frontal cortex for executive functioning.
  80. True of False, Does SR formulation have lower incidence of seizures?
  81. Wellbutrin is useful for?
    anergic or "low energy" depression, smoking cessation, mitigating SSRI induced sexual dysfunction and may be combined with Celexa to augment treatment of depression or chronic pain complaints.
  82. What receptors do wellbutrin SR target?
    DRI(Dopamine reuptake inhibitor)and NRI (Norephinephrine re-uptake inhibitor).
  83. True or False, wellbutrin is pregnancy cat C?
  84. Atomomextine (Straterra) and Mirtazepine (Remeron) are classified as what?
    NRI (Norephinephrine re-uptake inhibitor) and NaSSA (Noradrenergic and specific serotonergic antidepressant).
  85. NRI and NaSSA's are metabolized by what pathway?
    1A2, 2D6 and 3A4

    1A2 is induced by nicotine so smoking causes pt.s to metabolize drug faster.
  86. Common side effects for Mirtazapine (Remeron) include?
    Sedation and Weight gain.

    People can wake up next morning and feel hung over need to teach to sleep 8 hours.
  87. Remeron causes less what than SSRI's?
    Less sexual and anxiety side effects than SSRI's.
  88. True or False, is Remeron useful as a dual mechanism in partial responders with chronic pain?
  89. True or False the higher the dose the more weight gain and sedation?
    False, the lower the dose the more weight gain and sedation.
  90. What receptors are targeted by Remeron?
    Alpha 2 is main receptor, also Serotonin and histamine receptors.
  91. Is Remeron addictive?
  92. What does of Remeron is useful to promote sleep?
  93. Nortriptyline (Pamerlor), Amitriptyline (Elavil), Imipramine (Tofranil), Desimipramine, Doxepine, Clomipramine (Anafranil) are classified as what type of antidepressant?
    TCA's (Trycyclic Antidepressants)
  94. TCA's are metabolized by which pathway?
    1A2, 2C19, 2D6, 3A4

    1A2 is induced by nicotine so smoking causes pt.s to metabolize drug faster.

    A lot of drug interactions
  95. Common uses for TCA's?
    Sleep, migraine prophylaxis, chronic pain
  96. Serious side effects of TCA's?
    Lethal in overdose, if arrhythmia doesn't kill, acute renal failure will...Nephrologist's worst ngihtmare.

    Get an EKG before using as an anti-depressant.
  97. Isocarboxazid (Marplan), Phenelzine (Nardil), Selegiline, Tranylcypromine (Parnate) are classified as?
    MAOI's (Monoamine Oxidase Inhibitors)
  98. Interactions of MAOI's include?
    Tyramine, sympathomimetic agents, serotonergic agents, OTC cold medicines.
  99. Serious side effects of MAOI's include?
    Hypertensive crisis, serotonin syndrome.
  100. Is MAOI an target an enzyme?
    • yes
    • Monoamine oxidase
  101. What three NT do MAOI's help build up?
    DA, 5HT, NE
  102. 3 antidepressant worst for weight gain include?
    Remeron, Paxil and Elavil
  103. Weight neutral antidepressants include?
    prozac (early effect of anorexia) and wellbutrin.
  104. Indications for Antipsychotics?
    Thought disorders: schizophrenia and delusional disorders, Bipolar disroder (manic episodes), mood lability (inconsistent mood), impulse control (kids with ADHD and adults) and sleep.
  105. Haldol, Phenothiazines are classified as?
    Typical (First Generation) Antipsychotics
  106. Olanzapine (Zyprexa), Risperidone (Risperdal), Quetiapine (Seroquel), Ziprasidone (Geodon), Aripiprazole (Abilify), Paliperidone, Clozapine (Clozaril) are classified as?
    Atypical (Second Generation) Antipsychotics.
  107. Does typical or atypical antipsychotics have a higher incidence or Tardive Dyskinesia (TD) and other forms of EPS (Extrapyramidal symptoms)?
    Typical is more prevalent for TD and EPS, although still present with atypicals.
  108. What is a serious side effect of atypical antipsychotics?
    Neuroleptic Malignant Syndrome (NMS) also will see tardive dyskinesia (irreversible) and EPS (reversible).
  109. What receptor does typical antipsychotics work on?
  110. Atypical (second generation) antipsycotics are metabolized by what pathway?

    1A2 is induced by nicotine so smoking causes pt.s to metabolize drug faster.
  111. What do you need to monitor when a pt. is on atypical antipsychotics?
    must monitor BMI, metabolic panal, CBC periodically. Also monitor pt. for abnormal movements.
  112. What test can you do to monitor for EPS and TD sxs?
    Aims test (Abnormal involuntary movement scale)
  113. What is a severe side effect for atypical antipsychotics?
    Neuroleptic Malignant Syndrome (NMS)
  114. Can you gain weight while taking a atypical antipsycotic?
    yes, can gain a lot of weight quickly.
  115. Common side effects of Quetiapine (Seroquel) are?
    difficulty arising(can feel hungover), weight gain, increased risk for hyperlipidemia and/or impaired glucose tolerance.
  116. Seroquel's non-FDA uses include?
    irritability, impulsivity, atypical anxiety, ruminative worry and insomnia.
  117. Does seroquel interact with alcohol?
    Alternative to benzos has limited interaction with alcohol.
  118. What receptors does Seroquel target?
    D2, serotinergic, histamine and alpha 1 &2.
  119. What do you want to monitor when a patient is on Seroquel?
    CBC, Serum glucose, BMI & BP.
  120. Indications for Mood-Stabilizers/Anti-seizure medications?
    • Bipolar Disorder (Mania and depression)
    • Seizure Control
    • Chronic pain (Neuropathic pain and Migraine prophylaxis).
    • Impulse Control
  121. What NT do anti-seizure meds target?
    GABA (inhibitory NT)
  122. Carbamazepine (Tegretol), Oxcarbazepine (Trileptal), Lamotrogine (Lamictal), Topiramate (Topamax), Valproate (Depakote), Gabapentin (Neurontin), Phenytoin (Dilantin), Pregabalin (Lyrica) and Lithium are classified as?
    Mood-Stabilizers/Anti-Seizure medications.
  123. Side effects of Depakote (Valproic acid) are?
    • Sedation, profound weight gain
    • less commonly: hirsutism(excessive hairiness in women), polycystic ovaries, alopoecia and thrombocytopenia (20%).
  124. Depakote is non-FDA approved for?
    irritability, impulsivity adn hyperarousal.
  125. MOA of Depakote is?
    Block voltage-gated sodium channels, facilitate the inhibitory actions of GABA, inhibit calcium currents and block glutamate receptors.
  126. Therapeutic Drug monitoring for Depakote includes?
    BMI/WT, Drug levels ongoing(trough levels), CBC: initial and ongoing, q 3 months, LFT: initial and ongoing q 3-6 months.
  127. Therapeutic Drug monitoring for Carbamazapine (tegratol)/Oxacarbazepine includes?
    Drug levels ongoing, CBC:initial and ongoing, need to monitor q 2 weeks during first 2-3 months of treatment, LFT's: initial and ongoing, Thyroid: initial and ongoing and Kidney.

    Will be more concerned with agranulocytosis.
  128. Therapeutic drug monitoring for Lithium includes?
    • BMI/WT:b/c weight gain
    • Drug levels ongoing, CBC: initial and ongoing, need to monitor q 3-6 months LFT's: initial and ongoing. Kidney function test, Urine Specific Gravity & Chem-7.
  129. Is Lithium lethal in overdose?
  130. Special considerations for Lithium include?
    Hydration (can become toxic if dehydrated), Salt intake(need to decrease) and environmental.
  131. Common side effect for Lamotrogine?
    Rash most common side effect, benign rash common up to 10% of patients (rash on extremities).
  132. Serious side effect of Lamotrogine?
    Steven-Johnson's syndrome, severe rash is usually centrally located, lips, mouth, mucosa, blistering rash and painful to touch.
  133. What do you do if you see a rash on a pt. that is taking Lamotrogine?
    Stop med immediately, if suspect serious rash, order CBC, LFT's, Chem-7 and send to ED for further eval and management.
  134. Stimulants used in ADHD/ADD are?
    Methylphenidate (Ritalin) and Amphetamine Salts (Adderall).
  135. non-stimulants used in ADHD/ADD include?
    Atomextine (Straterra) & Buproprion SR or XL (Welbutrin).
  136. Are stimulants short or long acting?
  137. What is the neurocircuitry of stimulants?
    Dysregulation of DA and NE in the prefrontal cortex.
  138. What is the MOA of stimulants?
    Inhibition of DA transporter primarily, some action on NE transporter.
  139. Common side effects of stimulants include?
    Headaches, irritability, decreased appetite.

    May need big meal at bedtime.
  140. What do you want to monitor if a pt. is on a stimulant?
    Baseline EKG, BP, HT/WT.
  141. True or False, stimulants are helpful for post stroke patients with cognitive deficits?
  142. Trazodone, Zolpidem (Ambien), Eszopiclone (Lunesta), Zalpelon (Sonata), melatonin agonists and benzodiazepines are classified as what?
  143. Non-controlled drugs MOA that are sedatives/hypnotics are?
    involves histamine

    Can also involve melatonin.
  144. Controlled drugs MOA that are sedative/hypnotics are?
    Targets GABA sub-receptors.
  145. Controlled sedative drugs that have a low degree of tolerance, dependence or withdrawal include?
    the "z" drugs (Zolpidem, Zalpelon, Zopiclone, Ezopiclone).
  146. Potential serious side effects for controlled sedative drugs include:
    Amnesia and sleep walking.

    Teach them to take right before they go to bed, not before they do anything else.
  147. Common side effects of Trazodone (Deseryl) include?
    • dry mouth, difficulty arising, can increase vivid dreaming.
    • uncommon: priapism.

    Avoid in pt. s with ptsd that have nightmares or males with erectile dysfunction.
  148. Trazodone is useful for?
    Useful for sleep aide, although sometimes can exacerbate nightmares.
  149. When a male is using Trazodone, you need to advise him to?
    Go to ED if sustained, or painful, erection more than 1 hour.
  150. Side effects of Zolpidem (Ambien) include?
    Sedation, Memory problems and amnesia.

    May have dependency of abuse potential, do not use with alcohol.
  151. Is Ambien approved for long term use?
  152. True or False, Ambien helps with the maintenance of sleep?
    False, helps with the initiation of sleep not with the maintenance of sleep.
  153. What does of Remeron is used to promote sleep?
  154. What benefit does Remeron have over SSRI's?
    Less sexual and anxiety side effects than SSRI's.
  155. What is a common side effect of Remeron?
    Sedation, weight gain particularly in lower doses NOT higher doses.
  156. What receptors does Remeron target?
    Alpha 2, Serotonergic, and histamine.
  157. Can Remeron be useful in partial responders who are having chronic pain?
  158. Benzodiazepines, Antihistamines, antihypertensives and buspirone(buspar) are all classified as?
    Anxiolytics (decrease anxiety)
  159. Alprazolam (Xanax), Lorazepam (Ativan), Clonazepam (Klonopin), Diazepam (Valium), Chlordiazepoxide (Librium), Temazepam (Restoril), Midozalam (Versed) are all classified as?
  160. Hydroxyzine (Atarax or vistaril) and Cyproheptadine (Periactin) are classified as?
  161. Propranolol and Clonidide (Catapress) are used an anxiolytics and are classified as?
  162. Side effects of Clonazepam (Klonopin) include?
    Sedation, hypnotic
  163. Cautions you should take when using Klonopin include?
    Using weapons, driving vehicles, operating heavy machinery and no alcohol.
  164. Is Klonopin hepatically metabolized?
  165. Do you have a risk for tolerance, dependence and difficulty discontinuing with Klonopin?
  166. What receptors to Klonopin target?
    Binds to benzodiazapine site of GABA receptor and leads to enhanced GABAnergic inhibition.
  167. What is the difference between dependence versus addiction?
    Dependence is the physical dependence and addiction is the psychological dependence.

    Dopamine's role in award centers increases addiction.
  168. The constellation of sx's when a drug is no longer available is known as?
  169. Substances of withdrawal include?
    Opioids, Alcohol, Benzodiazepines, Cocaine, Caffeine and Nicotine

    Alcohol and benzos can have life-threatening withdrawal sx's.
  170. Medications for opioid dependence include?
    • Opioid Antagoinist: Naloxone and Naltrexone.
    • Opioid Agonist/Partial Agonists: Methadone, Buprenorphine.
    • Combo med :Buprenorphine and Naloxone (Suboxone).
    • Withdrawal syndrome: Clonidine and Proranolol (decreases discomfort and hyperarousal).
  171. Medications for ETOH dependence?
    Benzodiazepine use during acute phase: lorazepam (ativan), diazepam (valium) and chlordiazepoxide (librium).
  172. Medications for ETOH dependence?
    NMDA Anagonist (upstream effect): Acamprosate.
  173. Medications for ETOH dependence?
    Disulfarim (Antabuse)
  174. With Antabuse what do you need to frequently monitor?
  175. What is the MOA of Antabuse?
    Interferes with acetic acid metabolism and causes excessive build up of acetaldehyde (responsible for hangover symptoms).
  176. Side effect of Antabuse
  177. Medication for nightmares include?
    Prazosin (Minipress)
  178. MOA of Minipress?
    A lipid soluable, generic, alpha-1 adrenergic antagonist. Counteracts NE/sympathetic discharge associated with dreaming and modulates corresponding increase in CRF associated with sleep dysfunction.
  179. What is the use of Minipress?
    trauma nightmares in combat veterans
  180. What do you need to monitor if a pt. is on minipress (Prazosin)?
    initial orthostatics and ongoing BP monitoring.