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• Inhibidor selectivo de la recaptación de serotonina
• Antidepresivo
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• Psicofarmacología

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PSYCHIATRIC PHARMACOLOGY Receptor type Dopamine (D2) Serotonin 1A (5-HT1A) Serotonin 2A (5-HT2A) Serotonin 2C (5-HT2C) Class & MOA SSRIs: inhibit reuptake of serotonin as well as slight effects on histamineR, α1-R, and muscarinic-R

SNRIs: inhibits reuptake of both serotonin and norepinephrine

Atypical Antidepressants

Class & MOA

Effects of psychiatric drugs Antagonists  antipsychotic effect, relief of + symptoms of schizophrenia, ↑extrapyramidal symptoms, increased prolactin levels Agonists  antidepressant & anxiolytic effects Antagonists  improvement in neg symptoms of schizophrenia and improved cognition Antagonists  weight gain and associated risks Generic Agent Fluoxetine

Brand Prozac

Citalopram

Celexa

Escitalopram

Lexapro

Fluvoxamine

Luvox

Sertraline

Zoloft

Paroxetine

Paxil

Venlafaxine (ER avail)

Effexor

Duloxetine

Cymbalta

Desvenlafaxine Bupropion

Pristiq Wellbutrin

Mirtazapine

Remeron

Nefazodone Trazodone

Serzone Oleptro

Generic Agent

Brand

Receptor type Serotonin 3 (5-HT3) Alpha-1 adrenergic (α-1) Histamine (H1) Muscarinic (m1) Info

-Longest half-life = highest risk for serotonin syndrome -Many drug interactions -Most stimulating SSRI -Lowest weight gain = good for eating disorders -Low risk of sexual AEs

-Few drug interactions -Highest risk of GI problems -Shortest half-life = highest risk of d/c symptoms -Most sedating SSRI and greatest weight gain and greatest sexual AEs -Greatest anticholinergic activity -HTN -Sedating -Less AEs than venlafaxine -Works well for fibromyalgia -Good for sleep and pain

-AEs: GI, CNS, sexual, sedation, fatigue, dry mouth, hypotension, withdrawal if d/c abruptly, prolonged QT, rash, insomnia, asthenia, seizure, tremor, somnolence, mania, suicidal ideation, worsened depression -Risk of serotonin syndrome: shivering, hyperreflexia, myoclonus, ataxia, n/v/d

-Equally effective as SSRIs for treating major depression -May be more effective in the setting of diabetic neuropathy, fibromyalgia, msk pain, stress incontinence, sedation, fatigue, and patients with comorbid anxiety -AEs: GI, HTN, CNS, permanent sexual?, diaphoresis, dizziness, fatigue, insomnia, blurred vision, suicidal ideation, dysuria, worsened depression -Fewer drug interactions

-May increase sexual function -Has stimulant effects = good for comorbid ADHD or for helping quit smoking but don’t use if comorbid anxiety or eating disorder -AEs: lower seizure threshold, insomnia, nervousness, agitation, anxiety, tremor, arrhythmias, HTN, tachycardia, S-J, weight loss, GI, arthralgia or myalgia, confusion, dizziness, HA, psychosis, suicidal ideation -Less nausea and sexual AEs -Overdose is generally safe -AEs: the most sedating antidepressant (= good for insomnia!), weight gain, orthostatic hypotension, dizziness, dry mouth -AEs: arrhythmia, hyper or hypotension, diaphoresis, GI, hemolytic anemia, leukocytosis, dizziness, HA, insomnia, lethargy, memory impairment, seizure, somnolence, priapism, weight gain

Info

Class & MOA

Tricyclic Antidepressants: inhibits reuptake of both serotonin and norepinephrine

MAOIs: block destruction of monoamines centrally and peripherally

Mood Stabilizers

Class & MOA

Amitriptyline

Elavil

Clomipramine Desipramine Doxepin Imipramine Nortriptyline Phenelzine

Anafranil Norpramin Silenor Tofranil Pamelor Nardil

Tranylcypromine

Parnate

-Irreversible

Selegiline

Emsam (transdermal)

-Reversible

Carbamazepine

Tegretol

Valproate

Depakene Depakote

Lamotrigine

Lamictal

Lithium

Eskalith Lithobid

Gabapentin

Neurontin

-MOA: antiepileptic; inhibits voltage-gated Na channels -AEs: diplopia, dizziness, drowsiness, nausea, Stevens-Johnson (don’t use in Asians), hypoCa, hypoNa, SIADH, hematologic, hepatitis  monitor CBC, LFTs, mental status, bone density, levels -Contraindicated with bone marrow depression -Decreases effectiveness of OCPs and warfarin -Pregnancy D -MOA: antiepileptic; increases GABA -AEs: GI upset, sedation, unsteadiness, tremor, thrombocytopenia, palpitations, immune hypersensitivity, ototoxicity  monitor CBC and LFTs and levels -Contraindicated with liver disease -Many drug interactions -Pregnancy D -MOA: blocks voltage-gated Na channels and inhibits glutamate release -AEs: nausea, diplopia, dizziness, unsteadiness, HA, rash, Stevens-Johnson, hematologic, liver failure -Overdose can be fatal -Interaction with valproate -Pregnancy C -Inhibits adenylate cyclase -AEs: diabetes insipidus, cognitive complaints, tremor, weight gain, sedation, diarrhea, nausea, hypothyroidism -Many drug interactions -Requires baseline BMP, TSH, EKG, Ca as well as monitoring of BMP and TSH q 6-12 mo -Monitoring for signs of toxicity: nausea, tremor, polyuria, thirst, weight gain, diarrhea, cognitive impairment -Need to monitor levels -Pregnancy D for neural tube defects -AEs: somnolence, dizziness, ataxia, fatigue, leukopenia, weight gain, Stevens-Johnson

Generic Agent

Brand

-Good for sleep, pain, and depression

-Least sedating

-Irreversible

-AEs: anticholinergic, CV, CNS, weight gain, sexual dysfunction, decreased seizure threshold -CV effects: orthostatic hypotension, conduction disturbance, cardiotoxicity  consider EKG prior to initiation -Overdose can be lethal -MAO-A acts on norepinephrine and serotonin -MAO-B acts on phenylethylamine and DA -AEs: anticholinergic, lower seizure threshold, weight gain, rash, orthostasis, sexual dysfunction, insomnia or somnolence, HA, HTN crisis in presence of monoamines -Must be on tyramine-free diet = no wine, beer, cheese, aged food, or smoked meats -Overdose is lethal -2 week washout period of other antidepressants needed before starting in order to prevent serotonin syndrome

Info

Benzodiazepines: GABA-R agonists  CNS inhibition

Other Anxiolytics

Typical Antipsychotics: nonselective DA-R antagonists

Atypical Antipsychotics: block postsynaptic DA-R, block serotonin-R, variable effect on histaminic and cholinergic-R

Chlordiazepoxide

Librium

Clorazepate Diazepam Flurazepam Alprazolam

Tranxene Valium Dalmane Xanax

Clonazepam

Klonopin

Lorazepam Temazepam Oxazepam Triazolam Buspirone

Ativan Restoril Serax Halcion BuSpar

Haloperidol (inj avail) Fluphenazine Perphenazine Thioridazine

Haldol

Chlorpromazine Aripiprazole Asenapine (SL tablet avail) Olanzapine (inj avail)

Thorazine Abilify Saphris

Prolixin Trilafon Mellaril

Ziprasidone

Zyprexa Zyprexa Relprevv (inj) Seroquel Risperdal Consta (inj) Geodon

Clozapine

Clozaril

Iloperidone

Fanapt

Lurasidone Paliperidone (inj avail)

Latuda Invega Invega Sustenna (inj)

Quetiapine Risperidone

-Long-acting -Used often during EtOH withdrawal -Long-acting -Long-acting -Long-acting -Intermediate acting -Approved for panic disorder -Intermediate acting -Approved for panic disorder -Intermediate acting -Intermediate acting -Short acting -Short acting -5-HT partial agonist -Gradual onset in 2 weeks -Does not potentiate effects of alcohol = useful in alcohols -Low addiction potential = good for pts who were addicted to benzos or other drugs -AEs: sexual, dizziness, nausea, HA -Drug interactions -Good for acute agitation as onset is 30 min

-AE: retinitis pigmentosa -Less risk of EPSEs -Less risk of EPSEs -Costs $$$ -High risk of weight gain and metabolic syndrome -Injectable can cause post-injection delirium  must give at healthcare facility and monitor for 3 hours -Need q 6 month eye exams due to risk of cataracts -Least amount of AEs -Highest risk of hyperprolactinemia -AE: dose-related QT prolongation -Less wt gain -The only atypical antipsychotic proven effective in treatment of schizophrenia -Use limited by AEs: high risk of weight gain and metabolic syndrome, seizures, agranulocytosis, myocarditis, lens opacities  need to monitor WBC and ANC frequently -Costs $$$ -Not proven better than other atypical antipsychotics -Best choice for reversing metabolic effects

Management of Psychiatric Drug Adverse Effects

Dystonias -Benztropine -Biperiden -Diphenhydramine -Trihexyphenidyl Akathisias = restlessness -Propranolol -Benzos

Parkinsonianism -Amantadine -Levodopa Extrapyramidal Symptoms -Parkinsonian syndrome, acute dystonias, akathisia -Benztropine -Benadryl