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Session 3 Pharm- 6
Pharm -6- Antidepressants
Question | Answer |
---|---|
What two areas of the brain are proposed to be the sites where depression reside because of the high levels of NE and 5-HT receptors in these locations | Raphe Nuclei and Locus Ceruleus |
Where do 90% of NE neurons in the brain originate from | locus ceruleus or the sky blue place involved in arousal, stress and panic |
What portion of the brain has extensive projection to the rest of the brain and is responsible for regulation of mood, appetite and sleep | raphe nuclei |
What is the main tx for depression | psych counseling is necessary drugs are only adjunct to treatment |
Why does it take up to several weeks for antidepressants to work | you have to get desensitization of the alpha 2 and 5ht receptors on the presynaptic terminal to prevent feedback inhibition of NE and serotonin release from the presynaptic auto receptors. This takes time |
TCAs have a different adaptive change than the other anti depressants to reach therapeutic levels what is the difference | TCAs alpha 1 receptors do not desensitize instead it is postsynaptic Beta receptors that are desensitized |
Why is depression treatment split into three phases, acute phase, continuation phase and maintenance phase | each phase has a different goal. Acute phase is first 6- 8 weeks needed to see reduction of symptoms, Continuation phase is 6 months of continued tx to avoid relapse, and maintenance phase is more therapy for recurring depression pt |
What phase of depression tx if aimed at preventing relapse and is set at about 6 months of continued depression therapy after tx of symptoms | continuation phase |
What is the 1st line tx for depression | SSRIs |
What type of drug is fluoxetine (Prozac) | SSRI |
What type of drug is Sertraline (Zoloft) | SSRI |
What type of drug is Citalopram (Celexa) | SSRI |
What type of drug is Escitalopram (Lexapro) | SSRI |
What type of drug is Fluvoxamine (Fluvox) | SSRI |
What type of drug is Paroxetine (Paxil) | SSRI |
Pt is taking TCAs and you want to switch them over to SSRI what two SSRI should you not prescribe this patient because you could induce a TCA toxicity | Paroxetine (Paxil) and Fluoxetine (Prozac) |
What are the possible S/E of SSRIs | SEXUAL DYSFUNCTION, GI problems such as abdominal cramp/pain, belching, bloating, constipation, diarrhea, dyspepsia, indigestion, flatulence. S/E reduce with continued treatment are not permanent |
Pt is experiencing S/E from the SSRI you just prescribed a couple of days ago what should you tell them | The S/E are likely to diminish if possible they should try and continue taking the drug and see if they decrease |
Pt is completely cured of depression what needs to be done with their SSRI tx | they need to be tapered of slowly to avoid withdrawal effects |
What are the signs of SSRI withdrawal | FLUSH- Flu like fatigue, diarrhea, nausea, diaphoresis, Lightheadedness, Uneasiness, Sleep/Sensory disturbances, Headache |
Your Pt figured if one anti depression med was good two would be even better and decided to combine their current SSRI with another one they had in the house what complication could this cause | Serotonin syndrome- a potentially fatal hyperserotonergic state marked by severe muscle rigidity and myoclonus, hyperthermia, cardiovascular instability, marked CNS stimulatory effects such as seizures |
A Pt just arrive in the ER suffering from Serotonin Syndrome what tx are you going to give | d/c serotonergic meds, give an antiseizure drug and 5-HT blockers |
What type of drug is Venlafaxine (Effexor) | SNRI |
What type of drug is Duloxetine (Cymbalta) | SNRI |
When would you likely use and SNRI over an SSRI | major depressive disorder or depression with neuropathic pain (SSRIs are not useful for neuropathic pain), can be used to treat GAD |
What are the S/E of SNRI | same as SSRI GI symptoms and SEXUAL dysfunction |
Sexual Dysfunction a S/E of SSRIs and SNRIs can lead a patient to be non compliant what can you prescribe them that has less side effects | atypical antidepressants such as mirtazapine, Trazodone, nefazodone, bupropion. You can also give sildenafil (Viagra) along with the antidepressants as an option |
What type of drug is imipramine (Tofranil) | Tertiary TCA |
What type of drug is clomipramine (Anafranil) | Tertiary TCA |
What type of drug is Trimipramine (Surmontil) | Tertiary TCA |
What type of drug is Amitriptyline (Elavil) | Tertiary TCA |
What type of drug is Doxepin (Adapin) | Tertiary TCA |
What is the MOA of the tertiary TCAs | non selective inhibition of NE and 5HT reuptake except Clomipramine (Anafranil) which selectively blocks 5-HT reuptake |
What is the MOA of secondary TCAs | inhibit NE reuptake except Amoxapine which inhibits NE and DA reuptake |
What type of drug is Desipramine (Norpramin) | Secondary TCA |
What type of drug is Amoxapine (Asendin) | Secondary TCA |
What type of drug is Maprotiline (Ludiomil) | Secondary TCA |
What type of drug is Nortriptyline (Pamelor) | Secondary TCA |
What type of drug is protriptyline (Vivactil) | Secondary TCA |
What class of anti depressant has the MOA of non selectively blocking reuptake of NE and 5-HT but has higher S/E profile because it also blocks H1-histamine receptors, muscarinic receptors and alpha 1 receptors | TCAs |
Because TCAs block Alpha 1 receptor what S/E do you see | orthostatic Hypotension |
Because TCAs block muscarinic receptors what S/E do you see | dry mouth (xerostomia), Blurred vision, Constipation |
What S/E do you see in TCAs due to their blockade of histamine receptors | sedation |
What are two concerning S/E for patients that they are most likely to notice with TCAs | Weight Gain, Sexual Dysfunction |
If a patient has a dysfunctional CYP2D6 gene what problem might they have | may have a hard time metabolizing certain TCAs so you may want to be selective in which drug you prescribe them |
Since TCAs have a higher S/E profile than SSRIs or SNRIs when would you want to use them | depression resistant to SSRIs and SNRIs, good for nocturnal enuresis in children over 12, approved for ADD/ADHD in children over 6 and Clomipramine is used for OCD |
When are TCAs contraindicated | Pt with glaucoma as it can aggravate it, epileptic patients, caution in elderly patients or patients with recent MI |
Why do you want to be careful in how big of a dose of TCA you prescribe a Pt | There is a high overdose potential that can be potentially fatal especially with imipramine. Signs are confusion, mania, cardiac dysrhythmias |
What do you have to caution patient against using while taking TCAs because they can potentiate the sedative effects of the TCAs | EtOH and Anesthetics |
What type of drug is Mirtazapine (Remeron) | Atypical Antidepressant |
What type of drug is Trazodone (Desyrel) | Atypical Antidepressant |
What type of drug is Nefazodone (Serzone) | Atypical Antidepressant |
What type of drug is Bupropion (Wellbutrin) | Atypical Antidepressant |
What type of drug is Atomoxetine (Strattera) | Atypical Antidepressant |
What class of antidepressant has no common MOA but generally are believed to non selectively antagonize presynaptic receptors enhancing release of NE and 5-HT | Atypical Antidepressant |
Which Atypical antidepressant blocks 5HT 2alpha receptor and inhibits reuptake of 5HT and NE used as an antidote to sexual dysfunction associated with SSRI and SNRIs but can cause hepatotoxicity | Nefazodone (Serzone) |
Which atypical antidepressant doesn’t actually treat depression very well and has been repackaged to treat nicotine addiction. It has a short half life can cause dry mouth, sweating, tremor, seizures at high doses | Bupropion (Wellbutrin) |
what tx might you consider for a pt with major depression that has resisted SSRIs, SNRIs and TCA treatment | MAOI |
What are the two isoenzymes of MAO | MAO-A and MAO-B MAO-A preferentially deaminates NE, EPI, Serotonin. MAO-B deaminates Dopamine and Tyramine |
What type of drug is Phenelzine (Nardil) | Non specific irreversible MAOI |
What type of drug is Isocarboxazid | Hydrazine class irreversible inhibitor of MAOIs |
What type of drug is Tranylcypromine (Parnate) | Non specific irreversible MAOI amphetamine derivative |
What type of drug is Moclobemide | MAOI specific for MAO-A isoenzyme (targets NE, EPI and Serotonin preferentially) |
What type of drug is Selegiline (EMSAM, Selegiline patch) | MAO-B specific MAOI (preferentially targets dopamine and tyramine) |
What are the S/E of MAOIs | sedation, orthostatic hypotension, CNS stimulation, Weight Gain, Decreased sexual function, GI s/e and N/V |
What dietary education do you have to give a pt when you prescribe them MAOIs | avoid cheese, wine and preserved foods as they contain tyramine and have an interaction with MAOIs |
Can you give MAOIs as a adjunct to SSRI therapy or TCA therapy | No, it can cause serotonin syndrome if you combine them |
What SSRI, SNRI or TCA would you most likely prescribe for ADD/ADHD | Imipramine (Tofranil) a tertiary amine or Atomoxetine (Strattera) an atypical antidepressant |
What SSRI, SNRI or TCA would you most likely prescribe for OCD | SSRIs; Fluvoxamine (Fluvox), Fluoxetine (Prozac): TCA- Clomipramine (Anafranil) |
What SSRI, SNRI or TCA would you most likely prescribe for nocturnal enuresis (bed wetting ) | Desipramine (Norpramin) secondary TCA (not first line though) |
Pt is suffering from neuropathic pain what antidepressants would you likely use for their depression | TCAs or SNRIs remember SSRIs aren't very effective for neuropathic pain |
what type of bipolar disorder is marked by manic episodes | bipolar I |
what type of bipolar disorder is marked by hypomanic states | bipolar II |
What is the tx for bipolar generally include | Lithium, Carbamazepine or Valproic acid, antipsychotics, antidepressants |
What is the main prophylactic tx for bipolar disorder | Lithium |
What is the MOA of lithium | interferes with resynthesis of PIP2 |
Pt is bipolar and taking a thiazides what interaction might occur if the pt is prescribe lithium for their bipolar disorder | lithium gets retained in situation that cause depletion of Na+. Thiazides cause diuresis and therefore lithium will get retained you have to monitor this as lithium has a low therapeutic index and can become toxic |
Why do you need to monitor patients lithium levels | lithium has a low therapeutic index and can be toxic causing vomiting, diarrhea, coarse tremor, ataxia, coma, convulsions chronic intoxication can cause neurologic damage |
Is there an antidote to lithium toxicity | No dialysis is the most effective tx |
What are some s/e of lithium at normal doses | Nausea, diarrhea, drowsiness, polyuria, polydipsia, weight gain, decreased thyroid function |