PSYCHIATRIC PHARMACOLOGY

Receptor type Effects of psychiatric drugs Receptor type

Dopamine (D2) Antagonists  antipsychotic effect, relief of + symptoms of schizophrenia, Serotonin 3 (5-HT3)
↑extrapyramidal symptoms, increased prolactin levels
Serotonin 1A (5-HT1A) Agonists  antidepressant & anxiolytic effects Alpha-1 adrenergic (α-1)
Serotonin 2A (5-HT2A) Antagonists  improvement in neg symptoms of schizophrenia and Histamine (H1)
improved cognition
Serotonin 2C (5-HT2C) Antagonists  weight gain and associated risks Muscarinic (m1)
Class & MOA Generic Agent Brand Info
SSRIs: inhibit Fluoxetine Prozac -Longest half-life = highest risk for serotonin syndrome
reuptake of serotonin -Many drug interactions
as well as slight -Most stimulating SSRI
effects on histamine- -Lowest weight gain = good for eating disorders
R, α1-R, and Citalopram Celexa
muscarinic-R -Low risk of sexual AEs
Escitalopram Lexapro -AEs: GI, CNS, sexual, sedation, fatigue, dry mouth, hypotension,
Fluvoxamine Luvox 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,
Sertraline Zoloft -Few drug interactions n/v/d
-Highest risk of GI problems
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
SNRIs: inhibits Venlafaxine (ER Effexor -HTN -Equally effective as SSRIs for treating major depression
reuptake of both avail) -Sedating -May be more effective in the setting of diabetic neuropathy, fibromyalgia,
serotonin and msk pain, stress incontinence, sedation, fatigue, and patients with comorbid
norepinephrine Duloxetine Cymbalta -Less AEs than venlafaxine anxiety
-Works well for fibromyalgia -AEs: GI, HTN, CNS, permanent sexual?, diaphoresis, dizziness, fatigue,
-Good for sleep and pain insomnia, blurred vision, suicidal ideation, dysuria, worsened depression
Desvenlafaxine Pristiq -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, 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 Amitriptyline Elavil -Good for sleep, pain, and depression
Antidepressants:
inhibits reuptake of -AEs: anticholinergic, CV, CNS, weight gain, sexual dysfunction, decreased
both serotonin and Clomipramine Anafranil seizure threshold
norepinephrine Desipramine Norpramin -Least sedating -CV effects: orthostatic hypotension, conduction disturbance, cardiotoxicity
Doxepin Silenor  consider EKG prior to initiation
Imipramine Tofranil -Overdose can be lethal
Nortriptyline Pamelor
MAOIs: block Phenelzine Nardil -Irreversible -MAO-A acts on norepinephrine and serotonin
destruction of -MAO-B acts on phenylethylamine and DA
monoamines Tranylcypromine Parnate -Irreversible -AEs: anticholinergic, lower seizure threshold, weight gain, rash, orthostasis,
centrally and sexual dysfunction, insomnia or somnolence, HA, HTN crisis in presence of
peripherally Selegiline Emsam -Reversible monoamines
(transdermal) -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
Mood Stabilizers Carbamazepine Tegretol -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
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 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 -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 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
Gabapentin Neurontin -AEs: somnolence, dizziness, ataxia, fatigue, leukopenia, weight gain, Stevens-Johnson
 Class & MOA Generic Agent Brand Info
Benzodiazepines: Chlordiazepoxide Librium -Long-acting
GABA-R agonists  -Used often during EtOH withdrawal
CNS inhibition 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 Haloperidol (inj Haldol -Good for acute agitation as onset is 30 min
Antipsychotics: avail)
nonselective DA-R 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 $$$
block postsynaptic tablet avail)
DA-R, block Olanzapine (inj Zyprexa -High risk of weight gain and metabolic syndrome
serotonin-R, variable avail) Zyprexa -Injectable can cause post-injection delirium  must give at healthcare facility and monitor for 3 hours
effect on histaminic Relprevv (inj)
and cholinergic-R Quetiapine Seroquel -Need q 6 month eye exams due to risk of cataracts
Risperidone Risperdal -Least amount of AEs
Consta (inj) -Highest risk of hyperprolactinemia
Ziprasidone Geodon -AE: dose-related QT prolongation
-Less wt gain
Clozapine Clozaril -The only atypical antipsychotic proven effective in treatment of schizophrenia
-Use limited by AEs: high risk of weight gain and metabolic syndrome, seizures, agranulocytosis, myocarditis, lens opacities  need
to monitor WBC and ANC frequently
Iloperidone Fanapt -Costs $$$
-Not proven better than other atypical antipsychotics
Lurasidone Latuda -Best choice for reversing metabolic effects
Paliperidone (inj Invega
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