Psychiatric Pharmacology Flashcards
Cyclic Antidepressants drugs
- Amitriptyline
- Nortriptyline
- Imipramine
- Desipramine
- Clomipramine
- Doxepin
- Amoxapine
Haloperidol vs Chlorpromazine
Potency, EP symptoms, Anticholinergic effects
- Haloperidol: high potency, high EPS, and low anticholinergic
- Chlorpromazine: low potency, low EPS, and high anticholinergic
Carbamazepine and Valproic acid
Uses
- Epilepsy
- Acute mania
- Rapid cycling bipolar disorder
- Impulse control
Atomoxetine common uses
ADHD
Anti-psychotics mechanism of action
- Dopamine blockage at post-synaptic receptors
- Alpha-adrenergic blockade
- Anticholinergic action by blocking muscarinic receptors
- Blocks both NE and serotonin re-uptake
- Blocks histamine receptors
Note: All typicals block dopamine D2 receptors. Most Atypicals are D2 antagonists (except aripiprazole is D2 partial agonist) with varied effects on 5-HT2, dopamine, alpha and H1-receptors
Bupropion mechanism of action
Increases NE and dopamine via unknown mechanism
CNS stimulants common uses
- ADHD
- Narcolepsy
- Appetite control
Selective Serotonin Re-uptake Inhibitors (SSRIs) mechanism of action
Specific re-uptake inhibition of serotonin (5-HT), normally take 4-8 weeks to have an effect
Lithium Adverse effects
- Tremor, thirst, anorexia and GI distress commonly occur at therapeutic levels
- Life threatening seizures and coma
- Polyuria and polydipsia
- Edema
- Acne
- Benign leukocytosis
- Hypothyroidism with goiter (decreased TSH effect and inhibition of 5’-deiodinase)
- Nephrotoxicity (Thiazide increases toxicity)
- Nephrogenic Diabetes Insipidus (DI) (decreased ADH effect)
- Teratogenic (Ebstein anomaly of tricuspid valve)
Benzodiazepines
Uses
- Anxiety
- Acute and chronic alcohol withdrawal
- Convulsions
- Insomnia
- Restless leg
- Akathisia
- Panic disorder
Selective Serotonin Re-uptake Inhibitors (SSRIs) dugs
- Fluoxetine
- Paroxetine
- Sertraline
- Citalopram
- Fluvoxamine (approved for OCD)
- Escitalopram
Onset of EPS
- Hours to days: Acute dystonia (muscle spasm, stiffness, oculogyric crisis)
- Days to months: Akathisia (restlessness) and Parkinsonism (bradykinesia)
- Months to years: TD
Serotonin-Norepinephrine Re-uptake Inhibitors (SNRIs) Adverse effects
- Increased blood pressure (most common)
- Stimulant effects
- Sedation
- Nausea
Tardive Dyskinesia (TD) (Causes, Predisposing factors, Treatment)
- Supersensitivity of post-synaptic dopamine receptors
- Older patients, long-term Rx, smoking and DM
- No Rx, focus on prevention: pimozide or loxapine has less chance of inducing TD, clozapine not associated with it at all
Clozapine
Specific Adverse effects
- Agranulocytosis (weekly WBC count should be done)
- Increased salivation (“wet pillow” syndrome)
- Seizures
Mirtazapine mechanism of action
- Alpha-2 adrenergic antagonist (Stimulates NE and 5-HT release
- Blocks 5-HT2, 5-HT3 and H1 receptors
Trazodone mechanism of action
- 5-HT receptor antagonist (5-HT2)
- Alpha-1 adrenergic and H1 receptors blocker
- Weakly inhibits 5-HT re-uptake
CNS stimulants mechanism of action
Increase catecholamines in the synaptic cleft, especially NE and dopamine
Monoamine oxidase inhibitors (MAOIs) drugs
- Tranylcypromine
- Phenelzine
- Isocarboxazid
- Selegiline (selective MAOb inhibitor)
Typical vs Atypical anti-psychotics
- Typical blocks dopamine, while atypical blocks both dopamine and serotonin
- Typical treats mostly positive symptoms, while atypical treats positive and negative symptoms
- Typical has more side effects, while atypical has fewer side effects
Chlorpromazine
Specific Adverse effects
Corneal deposits
Risperidone
Specific Adverse effects
- Highest in raising prolactin levels
- Highest risk of movement disorders
Serotonin-Norepinephrine Re-uptake Inhibitors (SNRIs) Common uses
- Depression
- Generalized anxiety disorder
- Diabetic neuropathy
- Venlafaxine for social anxiety disorder, panic disorder, PTSD and OCD
Quetiapine
Specific Adverse effects
Lowest risk of movement side effects
Atomoxetine adverse effects
- Nausea
- Xerostomia (dry mouth)
- Decreased appetite
- Insomnia
- Fatigue
- Headache
- Cough
Chlorpromazine and Thioridazine vs Haloperidol and Fluphenazine
(M block and Sedation)
- Chlorpromazine and Thioridazine high M block and sedation
- Haloperidol and Fluphenazine low in M block and sedation
Electroconvulsive Therapy (ECT) Important Notes
- Its not a first line treatment but should be considered for
- Highly suicidal patients
- Depressed pregnant patients
- Improvement associated with large increase in slow wave (delta) activity in the prefrontal area; greater increase = greater recovery
Extrapyramidal (EP) reactions Treatment
- Benztropine
- Trihexyphenidyl
- Diphenhydramine
- Benzodiazepines
Cyclic Antidepressants Adverse effects
- Anti-cholinergic effects: nortriptyline has less effects than amitriptyline
- CNS effects: drowsiness, insomnia and agitation, disorientation and confusion, headache and fine tremor
- Cardiovascular: most common in elderly and include tachycardia, orthostatic hypotension, and lethal arrhythmias in overdose
- Sexual:
- Men: impotence and testicular swelling
- Women: anorgasmia and breast enlargement (treat with cyproheptadine[5-HT2 receptor antagonist])
- Metabolic: changes in blood sugar levels
Mirtazapine adverse effects
- Somnolence
- Increased appetite
- Weight gain
- Dry mouth
Selective Serotonin Re-uptake Inhibitors (SSRIs) Common uses
- Depression
- Generalized anxiety disorder
- Panic disorder
- OCD
- Bulimia
- Social anxiety disorder
- PTSD
- Premature ejaculation
- Premenstrual dysphoric disorder
Anti-psychotics neurologic adverse effects
- Anticholinergic effects (especially in elderly): dry mouth, blurry vision, constipation, urinary retention and delirium. Also tachycardia and decreased seizure threshold
- CNS effects from H1 receptors blockage: weight gain, sedation, and impaired memory
- Extrapyramidal (EP) reactions due to decreasd dopamine
- Tardive dyskinesia (TD): tongue protrusion, tremors and spasms of the neck, body and limbs. rarely before 3 to 6 month (1 month if older than 60)
Extrapyramidal (EP) reactions names and timeline
- Dystonic reactions (jerky movements, trouble speaking): 1 week (younger at more risk)
- Akinesia: 2 weeks
- Rigidity: 3 weeks
- Tremors: 6 weeks
- Akathisia: 10 weeks
- Pisa and Rabbit syndromes: 18+ weeks
CNS stimulants drugs
- Methylphenidate
- Dextroamphetamine
- Methamphetamine
Selective Serotonin Re-uptake Inhibitors (SSRIs) Adverse effects
- Anorgasmia and delayed orgasm in 15-20% of patients
- Anxiety and agitation
- Bruxism
- Weight loss
- SIADH
Cyclic Antidepressants Common uses
- Major depression
- OCD (clomipramine)
- Phobic and panic anxiety states
- Peripheral neuropathy
- Chronic pain with or without depression
- Enuresis
- Migraine prophylaxis
Buspirone common uses
Generalized anxiety disorder
Lithium Mechanism of action
Prevents recycling of inositol (PIP2) by blocking inositol monophosphate (second messenger) which leads to decrease cAMP
Cyclic Antidepressants Toxicity
3 Cs
- Convulsions
- Coma
- Cardiotoxicity (arrhythmia due to Na+ channel inhibition) treat with NaHCO3 to prevent arrhythmia
Cyclic Antidepressants interactions and cautions
- Hypertensive crisis with MAO inhibitors
- Serotonin syndrome with SSRIs, MAO inhibitors, and meperidine (pethidine)
- Prevent antihypertensive action of alpha-2 agonists
- Potentiate effects of alcohol
- Manic episodes induced in 50% of bipolars
- Avoid during the first trimester of pregnancy
Cyclic Antidepressants mechanism of action
- Blocking re-uptake of serotonin and NE
- Blocking of alpha-1 adrenergic and muscarinic receptors
Monoamine oxidase inhibitors (MAOIs) Interactions
- Hypertensive crisis with SSRIs, TCAs, St. John’s wort, meperidine, dextromethorphan (used to prevent serotonin syndrome), alpha-1 agonists and levodopa. Also with tyramine containing foods: aged cheese, dried fish, sauerkraur, sausage, chocolate, avocado and red wine (the safe foods are cottage cheese and white wine). Rx: stop the medications and give phentolamine or chlorpromazine. Wait 2 weeks after stopping MAO inhibitors before starting serotonergic drugs or stopping dietary restrictions
- Serotonin syndrome with SSRIs, TCAs and meperidine
Varenicline mechanism of action
Partial agonist of nicotinic receptors
Anti-psychotics common uses
- Psychotic symptoms: hallucinations, alteration of affect, ideas of reference, delusions, etc. (schizophrenia and bipolar disorder)
- Tourette’s syndrome
- Movement disorder: Huntington’s, hemiballism
- OCD
- Nausea and vomiting (drug and radiation induced)
- Intractable hiccups
- Pruritis
Trazodone adverse effects
- Priapism
- Cardiac arrythmias
- Sedation
- Postural hypotension
Selective Serotonin Re-uptake Inhibitors (SSRIs) Toxicity and interactions
- Serotonin syndrome
- With MAO inhibitors, meperidine and TCAs
- Most inhibit cytochrome P450 (especially fluvoxamine and fluoxetine)
- Increased levels of benzodiazepines in treatment of anxiety disorder
- Citalopram is safer for interaction
Thioridazine
Specific Adverse effects
- Cardiotoxicity (torsades “quinidine-like”)
- Retinitis pigmentosa (retinal deposits)
- Retrograde ejaculation
Varenicline adverse effects
Sleep disturbances
Anti-psychotics non-neurologic adverse effects
- Cardiovascular: orthostatic hypotension (do not use epinephrine; lowers blood pressure further)
- Particular taste (also dental cavities)
- Vomiting: common with long term use especially among smokers
- Sexual effects: due to elevated prolactin
- Men: decreased libido, inhibition of ejaculation, retrograde ejaculation and gynecomastia
- Women: breast enlargement and lactation, changes in libido, and dysmenorrhea
- Altered bodily response to temperature
Monoamine oxidase inhibitors (MAOIs) Common uses
- Atypical depression
- Anxiety
Monoamine oxidase inhibitors (MAOIs) mechanism of action
Inhibit MAOa and MAOb (enzymes that metabolizes serotonin, epinephrine and NE)
Typical or First generation anti-psychotics
- Chlorpromazine
- Thioridazine
- Fluphenazine
- Haloperidol
- Trifluoperazine (high potency)
Electroconvulsive Therapy (ECT) Mechanism of action and uses
- Electricity is passed from frontal cortex to the striatum, usually requires 5-10 treatments. and only relative C/I is increased intracranial pressure. 90% show immediate improvement
- Uses: depression, schizoaffective disorder, and bipolar disorder
Olanzapine
Specific Adverse effects
Highest incidence of diabetes, weight gain and increase cholesterol
Buspirone mechanism of action
Stimulates 5-HT1a receptors
Neuroleptic Malignant Syndrome (NMS)
Diagnosis and Treatment
- Fever, encephalopathy, vitals unstable, Increased enzymes and rigidity of muscles with myoglobinuria
- Dantrolene and bromocriptine (D2 agonist)
Atypical or Second generation anti-psychotics
- -pines: Clozapine, Olanzapine, Quetiapine, Asenapine
- -dones: Risperidone, Ziprasidone, Lurasidone, Iloperidone, Paliperidone
- Others: Aripiprazole
Trazodone common uses
- Depression
- Insomnia
- Erectile dysfunctio
Atomoxetine mechanism of action
Selective NE re-uptake inhibitor
Ziprasidone
Specific Adverse effects
Prolongs QT interval
Buspirone adverse effects
- Dizziness
- Headache
- Somnolence
- Premature ejaculation
Varenicline common uses
Smoking cessation
Bupropion adverse effects
- Increased risk of seizures (anorexic/bulimic patients)
- Appetite suppressant
- Agitation
- Insomnia
- Headache
Lithium Common uses
- Long-term control and prophylaxis of bipolar disorder, migraine cluster headache and chronic aggression
- Combined with TCAs for resistant depression
Atypical anti-psychotics which one is highest in alpha block and which one in sedation
- Alpha block is clozapine
- Sedation is risperidone
Haloperidol
Specific Adverse effects
Most likely cause of neuroleptic malignant syndrome (NMS) and TD
Cyclic Antidepressants Withdrawal
- Akathisia, dyskinesia, anxiety, sweating, dizziness, vomiting, cholinergic rebound, and depression rebound
- After prolonged use, withdraw gradually
Serotonin-Norepinephrine Re-uptake Inhibitors (SNRIs) drugs
- Venlafaxine
- Desvenlafaxine
- Duloxetine
- Levomilnacipran
- Milnacipran
Bupropion common uses
- Depression
- Smoking cessation
Serotonin-Norepinephrine Re-uptake Inhibitors (SNRIs) Mechanism of action
Inhibit 5-HT and NE re-uptake
