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, 1-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 (-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 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
-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 (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
-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
