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97 Cards in this Set
- Front
- Back
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***Depression*** |
SSRIs
Desipramine Nortriptyline Bupropion Venlafaxine MAOIs are reserved in patients do not respond, due to side effects and drug interactions |
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How long is an adequate therapy trial considered?
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6-8 weeks
***In 2005, the FDA required that all product labeling for antidepressants include a boxed warning for potential increased risk of clinical worsening and suicidality in children, adolescents, and young adults |
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Name the 6 SSRIs
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Citalopram (Celexa)
Escitalopram (Lexapro) Sertraline (Zoloft) Fluoxetine (Prozac) Paroxetine (Paxil) Fluvoxamine (Luvox) |
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Primary side effects of SSRIs
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Sexual dysfunction
Somnolence Fatigue Tremor Hallucinations Xerostomia |
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Pertinent drug interactions
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Other serotonergic medications:
- MAOIs - SSRIs - Triptans - Tramadol - St Johns wart - Linezolid (weak MAOI) |
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How long would you want to wait before d/c of and SSRI and induction of an MAOI?
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5 weeks for washout - long half-life
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Difference between citalopram and escitalopram
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Escitalopram (Lexapro) is only S isomer (citalopram is racemic mixture)
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Name the 9 tri-cyclic antidepressants
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Amitriptyline (Elavil)
Amoxipine Clomipramine Desipramine Doxepin Imipramie Nortriptyline (Pamelor) Protriptyline Trimipramine |
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Primary side effects of TCAs
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Anti-cholinergic effects
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TCAs
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Dangerous in overdose situations - avoid in patients with high suicidality
Also used in sleep disorders |
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Name 4 SNRIs
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Duloxetine (Cymbalta)
Venlafaxine (Effexor) Nefazadone (Serzone) Desvenlafaxine (Pristiq) |
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Name the MAOIs
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Isocarboxazid
Phenelzine Tranylcypromine Selegiline |
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MAOIs are used very infrequently due to side effect profile
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Selegiline is used primarily for parkinsons disease
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Common contraindications of MOAIs
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Cardiovascular disorder
HTN Cerebrovascular disorder General anesthesia History of HA Pheochromocytoma Severe renal impairment |
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While taking an MAOI, avoid caffeine, chocolate as well as these foods that contain tyramine
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Red wine
Aged cheeses Avocado Egg plant Figs Soy based foods |
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What is the MOA of bupropion (Wellbutrin, Zyban)
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Dopamine, Norepinephrine reuptake inhibitor
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What is an advantage of bupropion?
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No sexual side effects
Also used in smoking cessation |
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Bupropion is contraindicated in these situations
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MAOI
Bulimia or anorexia Seizure disorders |
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Major side effect of Bupropion
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Increased seizure activity
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Name the two tetracyclic anti-depressants
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Mirtazapine (Remeron)
Maprotiline |
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Name 4 SNRIs
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Duloxetine (Cymbalta)
Venlafaxine (Effexor) Nefazadone (Serzone) Desvenlafaxine (Pristiq) |
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Name the MAOIs
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Isocarboxazid
Phenelzine Tranylcypromine Selegiline |
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MAOIs are used very infrequently due to side effect profile
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Selegiline is used primarily for parkinsons disease
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Common contraindications of MOAIs
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Cardiovascular disorder
HTN Cerebrovascular disorder General anesthesia History of HA Pheochromocytoma Severe renal impairment |
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While taking an MAOI, avoid caffeine, chocolate as well as these foods that contain tyramine
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Red wine
Aged cheeses Avocado Egg plant Figs Soy based foods |
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What is the MOA of bupropion (Wellbutrin, Zyban)
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Dopamine, Norepinephrine reuptake inhibitor
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What is an advantage of bupropion?
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No sexual side effects
Also used in smoking cessation |
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Bupropion is contraindicated in these situations
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MAOI
Bulimia or anorexia Seizure disorders |
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Major side effect of Bupropion
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Increased seizure activity
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Name the two tetracyclic anti-depressants
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Mirtazapine (Remeron)
Maprotiline |
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Side effects of mirtazapine
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Increased appetite
Hyperlipidemia Weight gain Constipation Elevated LFTs |
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***Anxiety***
Name the benzodiazepines |
Alprazolam (Xanax)
Clonazepam (Klonopin) Clorazepate (Tranxene) Diazepam (Valium) Lorazepam (Ativan) Oxazepam |
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MOA of benzodiazepines
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Binds to GABA receptors
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Side effects of benzodiazepines
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Somnolence
Deceased libido Confusion Constipation Blurred vision |
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What pregnancy category are benzodiazepines?
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Category D
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What pregnancy category are SSRIs?
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Category C
Except paroxetine is category D |
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Category C =
Category D = |
Have not been studied in humans, but appear to cause harm in animal studies
Have been shown to cause harm in humans |
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How long do SSRIs, SNRIs or MOAIs generally take to work?
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2-4 weeks
Avoid alcohol Do not abruptly discontinue |
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Which SSRIs are indicated for GAD?
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Escitalopram
Paroxetine Venlafaxine |
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Which SSRIs are indicated for OCD?
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Fluoxetine
Paroxetine Sertraline Fluvoxamine |
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Which SSRIs are indicated for panic disorder?
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Fluoxetine
Paroxetine Sertraline Venlafaxine |
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Which SSRIs are indicated for SAD?
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Paroxetine
Sertraline Venlafaxine |
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Which SSRI is indicated for PTSD?
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Sertraline
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Besides SSRIs, benzodiazepines, propranolol, what options do you have in treating anxiety?
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Buspirone (Buspar)
Venlafaxine (Effexor) Nefazodone (Serzone) Hydroxyzine (Vistaril) Meprobamate |
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Advantages/Disadvantages of Buspirone
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Advantage = Pregnancy category B
Disadvantage = Do not use in renal or hepatic impairment |
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Nefazodone has unlabeled use in GAD, Panic disorder, PTSD, SAD
However, it has a black box warning for this |
Suicidal ideation
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Mechanism of hydroxyzine
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Competes with histamine for H-1 receptor sites on effector cells in GI, blood vessels, and respiratory tract
It is an antihistamine (little affinity for cholinergic receptors - no cholinergic side effects) and an anxiolytic (stemming from its 5-HT2 antagonist properties) |
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Avoid hydroxyzine in
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elderly and renal impairment
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***Bipolar Disorder***
Differentiate type I vs type II |
Type I - Major depressive and manic episodes
Type II - Major depressive and hypomanic episodes (no history of full manic episode) |
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What are the first line options for acute manic episodes?
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Lithium
Valproate Aripiprazole Quetiapine Risperidone Ziprasadone Olanzapine Carbamezepine |
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What are the first line options for acute depressive episodes?
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Lamotrigine
OR Lamotrigine + antimania therapy |
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What is the maintenance therapy for bipolar disorder?
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Lithium + Valproate
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Lithium MOA
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Alters Na channels leading to a shift toward intraneuronal metabolism of catecholamines
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Serum drug monitoring concentration
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0.6-1.5
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Primary side effects of Lithium
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Diarrhea
Vomiting Drowsiness Muscle weakness Coordination Ataxia Blurred vision Tinnitus |
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Significant drug interactions exist with lithium and these two classes of drug
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ACEI's
Diuretics Decreased lithium clearance and increased toxicity |
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Brand names and MOAs for Valproic acid, Oxcarbazepine, Lamotrigine
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Depakote - Increased GABA
Trileptal - Blocks voltage-gated Na channels resulting in stabilization of hyperexitable neuronal membranes Lamotrigine - Effects Na channels stabilizing neuronal membranes |
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What serious side effects exist with Valproic acid?
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Hepatic impairment
Thrombocytopenia Pancreatitis |
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What serious side effects exist with Oxcarbazepine?
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Hyponatremia
Rash (possibly Stevens-Johnson syndrome) |
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What serious side effects exist with Lamotrigine?
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Diplopia
Stevens-Johnson syndrome |
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***Schizophrenia***
Tardive Dyskinesia is caused by long-term dopamine antagonism |
It can reversed at first, but after a long period of time is not reversible
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Options for treating tardive dyskinesia
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Prevention is best treatment
Use lowest effective dose Possibly irreversible - d/c if possible Switch to atypical or clozapine Use anti-cholinergics only when indicated and for the shortest possible time |
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Lithium MOA
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Alters Na channels leading to a shift toward intraneuronal metabolism of catecholamines
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Serum drug monitoring concentration
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0.6-1.5
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Primary side effects of Lithium
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Diarrhea
Vomiting Drowsiness Muscle weakness Coordination Ataxia Blurred vision Tinnitus |
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Significant drug interactions exist with lithium and these two classes of drug
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ACEI's
Diuretics Decreased lithium clearance and increased toxicity |
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Brand names and MOAs for Valproic acid, Oxcarbazepine, Lamotrigine
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Depakote - Increased GABA
Trileptal - Blocks voltage-gated Na channels resulting in stabilization of hyperexitable neuronal membranes Lamotrigine - Effects Na channels stabilizing neuronal membranes |
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What serious side effects exist with Valproic acid?
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Hepatic impairment
Thrombocytopenia Pancreatitis |
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What serious side effects exist with Oxcarbazepine?
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Hyponatremia
Rash (possibly Stevens-Johnson syndrome) |
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What serious side effects exist with Lamotrigine?
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Diplopia
Stevens-Johnson syndrome |
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***Schizophrenia***
Tardive Dyskinesia is caused by long-term dopamine antagonism |
It can reversed at first, but after a long period of time is not reversible
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Options for treating tardive dyskinesia
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Prevention is best treatment
Use lowest effective dose Possibly irreversible - d/c if possible Switch to atypical or clozapine Use anti-cholinergics only when indicated and for the shortest possible time |
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PORT Guidelines
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"Second Generation medications, including clozapine and several adjunctive agents have been evaluated for the treatment of TD. However, there is insufficient evidence to support a recommendation for the use of any specific agent to treat TD"
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Name the typical anti-psychotics
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Chlorpromazine (Thorazine)
Fluphenazine (Prolixin) Perphenazine (Trilafon) Trifluoperazine ***All block dopamine in brain Prochlorperazine (Compazine) Thioridazine (Mellaril) |
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Continued
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Haloperidol (Haldol)
Pimozide Loxapine (Loxitane) Molindone (Moban) Thiothixene (Navane) |
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Name the atypical anti-psychotics
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Aripiprazole (Abilify)
Olanzapine (Zyprexa) Quetiapine (Seroquel) Risperidone (Risperdal) Ziprasidone (Geodon) Clozapine (Clozaril) ***Mixed dopamine/serotonin antagonist activity |
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Name the primary side effects of typical anti-psychotics
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Orthostatic hypotension
Sedation Xerostomia Constipation Urinary retention Blurred vision Photosensitivity EPS |
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Name the primary side effects of atypical anti-psychotics
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Weight gain
Hyperglycemia Hyperlipidemia Sedation Prolonged QT-interval Rare = Hyperprolactinemia, EPS, Tardive dyskinesia |
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Which agent has the lowest risk of metabolic syndrome?
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Aripiprazole
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What dangerous side effect is associated with clozapine?
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Agranulocytosis
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Hyperprolactinemia caused by dopamine antagonism can cause
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galactorrhea
amenorrhea loss of libido (men and women) decreased bone mineral density (men and women) gynecomastia hypospermatogenesis |
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Which anti-psychotic is most likely to cause hyperprolactinemia
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Risperidone
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PORT Guidelines
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Clozapine should be offered to people with SZ who continue to experience persistent and clinically significant positive symptoms after 2 adequate trials of other anti-psychotic agents
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Which anti-psychotic is associated with the greatest degree seizure threshold lowering?
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Clozapine
Don't give with Bupropion! |
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What is the interaction between clozapine and cigarette smoking?
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Clozapine = CYP 1A2 substrate
Cigarette smoking is a CYP 1A2 inducer The levels of clozapine would be lower than if you didn't smoke. If you stopped smoking while on clozapine, the levels would increase. |
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Which agent has the most anticholinergic effects?
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Clozapine
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Clozapine can also cause hypotension. What situation is most relevant to this?
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If you stop taking clozapine for more than 48 hours, you must start at a lower dose to avoid marked hypotension
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PORT Guidelines for first episode of positive symptoms
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Anti-psychotic medications, other than clozapine and olanzapine
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Why is Olanzapine not considered first line agent?
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Lacks extremely sedating properties of clozapine, but has significant weight gain
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Clozapine
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Most efficacious, but most dangerous - therefore not a first line option
Most likely to cause anti-cholinergic effects, lower seizure thresshold, orthostatic hypotension, sedation, weight gain, diabetes, obesity, and dyslipidemia Also agranulocytosis and multiple drug interactions |
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Anticholinergic effects
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Clozapine > Olanzapine > Quetiapine > Risperidone = Ziprasidone = Aripiprazole
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Weight gain
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Clozapine = Olanzapine > Quetiapine = Risperidone > Ziprasidone > Aripiprazole
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Orthostatic hypotension
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Clozapine > Risperidone = Quetiapine > Olanzapine = Ziprasidone = Aripiprazole
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Prolactin
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Risperidone > Olanzapine = Ziprasidone = Quetiapine = Clozapine > Arirpiprazole
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One advantage of using conventional anti-psychotics over atypical anti-psychotics?
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Cost
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Atypicals and Typicals are equally effective for positive symptoms
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Typicals can actually worsen negative symptoms
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What makes an atypical anti-psychotic atypical?
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Little to no EPS
Minimal increase in prolactin Decrease in both positive and negative symptoms 5HT2 antagonism Fast receptor dissociation from D2 receptors |
