PSYCHIATRIC PHARMACOLOGY

Receptor type Effects of psychiatric drugs Receptor type

Dopamine (D
2)
Antagonists antipsychotic effect, relief of + symptoms of schizophrenia,
extrapyramidal symptoms, increased prolactin levels
Serotonin 3 (5-HT
3
)
Serotonin 1A (5-HT
1A
) Agonists antidepressant & anxiolytic effects Alpha-1 adrenergic (-1)
Serotonin 2A (5-HT
2A
) Antagonists improvement in neg symptoms of schizophrenia and
improved cognition
Histamine (H
1
)

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






-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
Citalopram Celexa
-Low risk of sexual AEs


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

Desvenlafaxine Pristiq
Atypical
Antidepressants
Bupropion Wellbutrin

-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




Gabapentin Neurontin -AEs: somnolence, dizziness, ataxia, fatigue, leukopenia, weight gain, Stevens-Johnson







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

Akathisias = restlessness
-Propranolol
-Benzos
Parkinsonianism
-Amantadine
-Levodopa

Extrapyramidal Symptoms
-Parkinsonian syndrome, acute dystonias, akathisia
-Benztropine
-Benadryl