PSYCHIATRIC PHARMACOLOGY
Receptor type Effects of psychiatric drugs Receptor type
Dopamine (D2) Antagonists antipsychotic effect, relief of + symptoms of schizophrenia, Serotonin 3 (5HT3)
↑extrapyramidal symptoms, increased prolactin levels
Serotonin 1A (5HT1A) Agonists antidepressant & anxiolytic effects Alpha1 adrenergic (α1)
Serotonin 2A (5HT2A) Antagonists improvement in neg symptoms of schizophrenia and Histamine (H1)
improved cognition
Serotonin 2C (5HT2C) Antagonists weight gain and associated risks Muscarinic (m1)
Class & MOA Generic Agent Brand Info
SSRIs: inhibit Fluoxetine Prozac Longest halflife = highest risk for serotonin
reuptake of serotonin syndrome
as well as slight Many drug interactions
effects on Most stimulating SSRI AEs: GI, CNS, sexual, sedation, fatigue, dry mouth, hypotension,
histamineR, α1R, Lowest weight gain = good for eating disorders withdrawal if d/c abruptly, prolonged QT, rash, insomnia,
and muscarinicR Citalopram Celexa asthenia, seizure, tremor, somnolence, mania, suicidal ideation,
Escitalopram Lexapro Low risk of sexual AEs worsened depression
Risk of serotonin syndrome:
Fluvoxamine Luvox 1. Shivering
Sertraline Zoloft Few drug interactions 2. Hyperreflexia
Highest risk of GI problems 3. Myoclonus
Paroxetine Paxil Shortest halflife = highest risk of d/c symptoms 4. Ataxia
Most sedating SSRI and greatest weight gain and 5. N/V/D
greatest sexual AEs
Greatest anticholinergic activity
SNRIs: inhibits Venlafaxine Effexor HTN Equally effective as SSRIs for treating major depression
reuptake of both (ER avail) Sedating May be more effective in the setting of diabetic neuropathy,
serotonin and fibromyalgia, msk pain, stress incontinence, sedation, fatigue, and
Duloxetine Cymbalta Less AEs than venlafaxine
norepinephrine patients with comorbid anxiety
Works well for fibromyalgia
AEs: GI, HTN, CNS, permanent sexual?, diaphoresis, dizziness,
Good for sleep and pain
fatigue, insomnia, blurred vision, suicidal ideation, dysuria,
Desvenlafaxine Pristiq
worsened depression
Fewer drug interactions
Atypical Bupropion Wellbutrin May increase sexual function
Antidepressants 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, SJ,
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 Amitriptyline Elavil Good for sleep, pain, and depression
Antidepressants: AEs: anticholinergic, CV, CNS, weight gain, sexual dysfunction,
inhibits reuptake of decreased seizure threshold
both serotonin and Clomipramine Anafranil CV effects: orthostatic hypotension, conduction disturbance,
norepinephrine Desipramine Norpramin Least sedating cardiotoxicity consider EKG prior to initiation
Doxepin Silenor Overdose can be lethal
Imipramine Tofranil
Nortriptyline Pamelor
MAOIs: block Phenelzine Nardil Irreversible MAOA acts on norepinephrine and serotonin
destruction of MAOB acts on phenylethylamine and DA
monoamines Tranylcypromin Parnate Irreversible AEs: anticholinergic, lower seizure threshold, weight gain, rash,
e
centrally and orthostasis, sexual dysfunction, insomnia or somnolence, HA,
peripherally
Selegiline Emsam Reversible
(transdermal) HTN crisis in presence of monoamines
Must be on tyraminefree 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
Mood Stabilizers Carbamazepine Tegretol MOA: antiepileptic; inhibits voltagegated Na channels
AEs: diplopia, dizziness, drowsiness, nausea, StevensJohnson (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
Valproate Depakene MOA: antiepileptic; increases GABA
Depakote 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 voltagegated Na channels and inhibits glutamate release
AEs: nausea, diplopia, dizziness, unsteadiness, HA, rash, StevensJohnson, hematologic, liver failure
Overdose can be fatal
Interaction with valproate
Pregnancy C
Lithium Eskalith Inhibits adenylate cyclase
Lithobid 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 612 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
Gabapentin Neurontin AEs: somnolence, dizziness, ataxia, fatigue, leukopenia, weight gain, StevensJohnson
Class & MOA Generic Brand Info
Agent
Benzodiazepines: Chlordiazepoxi Librium Longacting
GABA-R agonists de Used often during EtOH withdrawal
CNS inhibition Clorazepate Tranxene Longacting
Diazepam Valium Longacting
Flurazepam Dalmane Longacting
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 5HT 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 Haloperidol (inj Haldol Good for acute agitation as onset is 30 min
Antipsychotics: avail)
nonselective DAR Fluphenazine Prolixin
antagonists Perphenazine Trilafon
Thioridazine Mellaril AE: retinitis pigmentosa
Less risk of EPSEs
Chlorpromazine Thorazine Less risk of EPSEs
Atypical Aripiprazole Abilify
Antipsychotics: Asenapine (SL Saphris Costs $$$
Block postsynaptic tablet avail)
DAR Olanzapine (inj Zyprexa High risk of weight gain and metabolic syndrome
avail) Zyprexa Injectable can cause postinjection delirium must give at healthcare facility and monitor for 3 hours
Block serotoninR
Variable effect on Relprevv
histaminic and (inj)
cholinergicR Quetiapine Seroquel Need q 6 month eye exams due to risk of cataracts
Risperidone Risperdal Least amount of AEs
Consta (inj) Highest risk of hyperprolactinemia
Ziprasidone Geodon AE: doserelated QT prolongation
Less wt gain
Clozapine Clozaril The only atypical antipsychotic proven effective in treatment of schizophrenia
Use limited by AEs: high risk of weight gain and metabolic syndrome, seizures, agranulocytosis, myocarditis, lens
opacities need to monitor WBC and ANC frequently
Iloperidone Fanapt Costs $$$
Not proven better than other atypical antipsychotics
Lurasidone Latuda Best choice for reversing metabolic effects
Paliperidone Invega
(inj avail) Invega
Sustenna
(inj)
Management of Psychiatric Drug Adverse Effects
Dystonias Parkinsonianism
Benztropine Amantadine
Biperiden Levodopa
Diphenhydramine
Trihexyphenidyl Extrapyramidal Symptoms
Parkinsonian syndrome, acute dystonias, akathisia
Akathisias = restlessness Benztropine
Propranolol Benadryl
Benzos
