Serotonin 2C (5-HT 2C ) Antagonists weight gain and associated risks Muscarinic (m 1 ) Class & MOA Generic Agent Brand FDA Info SSRIs: inhibit reuptake of serotonin as well as slight effects on histamine- R, 1-R, and muscarinic-R Fluoxetine Prozac
-Longest half-life = highest risk for serotonin syndrome -Many drug interactions -Most stimulating SSRI -Lowest weight gain = good for eating disorders
Escitalopram Lexapro Fluvoxamine Luvox OCD child/adles Sertraline Zoloft -Few drug interactions -Highest risk of GI problems MDD OCD Panic >6 y/o PTSD PMDD SAD Paroxetine Paxil -Shortest half-life = highest risk of d/c symptoms -Most sedating SSRI and greatest weight gain and greatest sexual AEs -Greatest anticholinergic activity Panic d/o SNRIs: inhibits reuptake of both serotonin and norepinephrine Venlafaxine (ER avail) Effexor -HTN -Sedating GAD -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 Duloxetine Cymbalta -Less AEs than venlafaxine -Works well for fibromyalgia -Good for sleep and pain
-May increase sexual function -Has stimulant effects = good for comorbid ADHD or for helping quit smoking but dont 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 Mirtazapine
Remeron -Less nausea and sexual AEs -Overdose is generally safe -AEs: the most sedating antidepressant (= good for insomnia!), weight gain, orthostatic hypotension, dizziness, dry mouth Nefazodone Serzone Trazodone
Oleptro -AEs: arrhythmia, hyper or hypotension, diaphoresis, GI, hemolytic anemia, leukocytosis, dizziness, HA, insomnia, lethargy, memory impairment, seizure, somnolence, priapism, weight gain
Class & MOA Generic Agent Brand Info Class & MOA Tricyclic Antidepressants: inhibits reuptake of both serotonin and norepinephrine Amitriptyline Elavil
-Good for sleep, pain, and depression
-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 Clomipramine Anafranil Desipramine Norpramin -Least sedating Doxepin Silenor Imipramine Tofranil Nortriptyline Pamelor MAOIs: block destruction of monoamines centrally and peripherally Phenelzine Nardil -Irreversible -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 Tranylcypromine Parnate -Irreversible Selegiline Emsam (transdermal) -Reversible Mood Stabilizers Carbamazepine Tegretol -MOA: antiepileptic; inhibits voltage-gated Na channels -AEs: diplopia, dizziness, drowsiness, nausea, Stevens-Johnson (dont 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 Valproate Depakene Depakote -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 Lamotrigine Lamictal -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 Lithium Eskalith Lithobid -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
Class & MOA Generic Agent Brand Info Benzodiazepines: GABA-R agonists CNS inhibition Chlordiazepoxide Librium -Long-acting -Used often during EtOH withdrawal Clorazepate Tranxene -Long-acting Diazepam Valium -Long-acting Flurazepam Dalmane -Long-acting Alprazolam Xanax -Intermediate acting -Approved for panic disorder Clonazepam Klonopin -Intermediate acting -Approved for panic disorder Lorazepam Ativan -Intermediate acting Temazepam Restoril -Intermediate acting Oxazepam Serax -Short acting Triazolam Halcion -Short acting Other Anxiolytics Buspirone BuSpar -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 Typical Antipsychotics: nonselective DA-R antagonists Haloperidol (inj avail) Haldol -Good for acute agitation as onset is 30 min Fluphenazine Prolixin Perphenazine Trilafon Thioridazine Mellaril -AE: retinitis pigmentosa -Less risk of EPSEs Chlorpromazine Thorazine -Less risk of EPSEs Atypical Antipsychotics: block postsynaptic DA-R, block serotonin-R, variable effect on histaminic and cholinergic-R
Aripiprazole Abilify Asenapine (SL tablet avail) Saphris -Costs $$$ Olanzapine (inj avail) Zyprexa Zyprexa Relprevv (inj) -High risk of weight gain and metabolic syndrome -Injectable can cause post-injection delirium must give at healthcare facility and monitor for 3 hours Quetiapine Seroquel -Need q 6 month eye exams due to risk of cataracts Risperidone Risperdal Consta (inj) -Least amount of AEs -Highest risk of hyperprolactinemia Ziprasidone Geodon -AE: dose-related QT prolongation -Less wt gain Clozapine
Clozaril -The only atypical antipsychotic proven effective in treatment of schizophrenia -Use limited by AEs: high risk of weight gain and metabolic syndrome, seizures, agranulocytosis, myocarditis, lens opacities need to monitor WBC and ANC frequently Iloperidone Fanapt -Costs $$$ -Not proven better than other atypical antipsychotics Lurasidone Latuda -Best choice for reversing metabolic effects Paliperidone (inj avail) Invega Invega
Sustenna (inj)
Management of Psychiatric Drug Adverse Effects Dystonias -Benztropine -Biperiden -Diphenhydramine -Trihexyphenidyl