1. Psychopharmacology Khalid Bazaid, MB BS, FRCPC Assistant Professor
Child & Adolescent Psychiatrist
Department of Psychiatry
College of Medicine
King Saud University
4/22/2017
JES-2003 1

2. Outlines
The role of psychotropic in the mental health and its therapeutic indications
Identify specific cautions to be aware of the various psychotropic medications
Discuss the adherence to medication treatment
Psychotropic Medications Classifications
Discuss the functions of the brain and the way this can be altered by the use of psychotropic medications
Introduce you to the role of psychotropic in the mental health and its therapeutic indications
Discuss how the neurotransmitters are affected by various psychotropic medications
Identify specific cautions to be aware of the various psychotropic medications
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JES-2003 2

3. Psychopharmacology
The aim is learn how to choose a psychotropic drug that is more:
Effective
Less toxic
Better-tolerated
The most targeted therapeutic agents
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4. Psychotropic Drugs
Focus of all mental activity is the CNS (brain)
Origin of psychiatric illness caused by many factors:
Genetics
Neurodevelopment factors
Endocrinologic e.g. Hypothyroidism
Autoimmune system (infections)
Drugs
Psychosocial experiences, stressors … etc.
To date …Theories behind use of psychotropic drugs focuses on neurotransmitters and their receptors
Psychotropic drugs act by modulating neurotransmitters
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5. Use of psychotropic medications
Relieve or reduce symptoms/signs of dysfunctional thoughts, moods, or actions of mental illness
Improve client’s functioning
Increase compliance to other therapies
Relieve or reduce symptoms/signs of dysfunctional thoughts, moods, or actions of mental illness and/or caused its impact
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6. Therapeutic Effects of Psychotropic Medications
Do not “cure”
Relieve or decrease symptoms
Prevent or delay return of S/S
Cannot be used as the sole treatment for disorders
Need informed consent before starting
Are broad spectrum and have effects on a large number of S/S
Initial effects are sedative in nature
May take weeks for effects to be seen
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7. Reasons for Non- adherence:
Medications are expensive
Unpleasant side effects
Feel better and decide no longer need
Stigma associated with having a mental illness and taking medications
Paranoia or fears about medication usage particularly addition
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8. Encouraging Compliance to Medication Regimen
Follow-up appointments With client to verify that client understands:
the purpose, proper administration, intended effects, side and toxic effects of, and how to treat problems associated with medications
Appropriate lab tests must be conducted to prevent complications and assure correct levels of drugs
Encourage clients to participate in medication groups
Can use injections of antipsychotics which will last from 2-4 weeks if clients are non-compliant
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9. Efficacy of Psychotropics with Children & Elderly
Use with great caution
Start low and go slow for both elders and children
Children are faster metabolizer whereas elders have decrease liver & renal function
Risk of injuries and falls with elderly
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10. Client & Family Teaching
Purpose of the meds and benefits, side effects and how to treat SE
What S/S indicate a toxic effect, and how to treat, and whom to call.
Specific instructions about how to take the medications
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11. Psychotropic Medications Classifications
Antipsychotics (Neuroleptics)
Mood Stabilizers
Antidepressants
Anxiolytics (antianxiety)
Sedatives
Hypnotics
Psychostimulants
Antihistamines, antimuscarinics, dopamine agonists
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12. Psychotropic Medications Classifications … continued
In many instances, drugs have multiple indications:
SSRIs (selective serotonin reuptake inhibitors) are both antidepressants and anxiolytics.
SDAs (serotonin-dopamine antagonists) are both antipsychotics and mood stabilizers.
Psychotropic drugs have also been organized according to structure (e.g. Tricyclic).
mechanism (e.g. monoamine oxidase inhibitor [MAOI])

13. Antipsychotics Schizophrenia Disorders Bipolar disorder
Major Depression with psychotic features
Tourette’s Syndrome
Delirium, Dementia, and Delusions
Control of intractable hiccups
Aggressive behavior
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14. Antipsychotic - Neuroleptics
First generation
Post synaptic D2 receptor.
Dopamine receptor antagonists (DRAs)
Low potency:
hypotension, sedation, weight gain
more anticholinergic
less antidopamenergic
less EPS.
e.g. Mellaril, chlorpromazine
High potency:
More antidopamenergic
more EPS
less anticholinergic
e.g. Haldol
Atypical Antipsychotics (2nd and 3rd generation)
D2, D4, 5HT2
Serotonin dopamine antagonists (SDAs)
Alpha adrenergic, muscarinic receptors
e.g.
Clozaril
Risperdal
Zyprexa
Seroquel
Abilify
Geodon
Invega
Zeldox

15. First Generation Antipsychotic
Block predominantly dopamine activity
High incidence of abnormal movements
little effect on serotonin
(Also blocks acetylcholine, norepinephrine to some degree)
Blocks the H receptor for histamine
results in sedation and weight gain
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16. Side Effects of 1st Gen Drugs-1
Dystonia (EPS)
spasms of the eye, neck-torticollis, back, tongue-happens within 72 hrs ( reversible)
Akathisia (EPS)
restlessness
Pseudoparkinson - S/S similar to Parkinson's-see in 1-2 weeks. May disappear. TX. With Cogentin
Tardive Dyskinesia-bizarre facial and tongue movements (irreversible)
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17. Side Effects of 1st Gen Drugs-2
Blurred vision, dry mouth, constipation and urinary retention, tachycardia-anticholinergic S/E
Sexual dysfunction
Severe dysrhythmias
Orthostatic hypotension
Agranulocytosis
In men can lead to gynecomastia
Amenorrhea
Galactorrhea
photosensitivity & skin rashes
Reduction is seizure threshold – Low potency
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18. Precautions and/or contraindicated When using 1st Gen Antipsychotics
Blood dyscrasias
Liver, renal, or cardiac insufficiency
CNS depressants, including ETOH
Tegretol in conjunction with antipsychotics causes up to 50% reduction in antipsychotic concentrations
SSRI’s in conjunction with antipsychotics may cause sudden onset of EPS
Don’t give if have: Parkinson's disease, prolactin dependent cancer of the breast
Cigarette smoking causes reduced plasma concentrations of antipsychotics
Antacids, activated charcoal can reduce the absorption of DRAs
Faverin in conjunction with antipsychotics causes increased concentrations of Haldol and Clozaril
Beta Blockers in conjunction with antipsychotics cause severe hypotension
Antidepressants in conjunction with antipsychotics may cause increased plasma level of both
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19. First Generation Antipsychotic Medications
Are useful in getting out of control behavior under control quickly.
These can be given with lithium to get treat acute mania.
Seroquel is effective in the maintenance treatment of Bipolar-Depressive phase
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20. Atypical Antipsychotics
Action: Blocks dopamine receptors and to a lesser degree serotonin receptors,
Also block receptors for norepinephrine , histamine, acetylcholine
Nicer drugs and are used more
Decrease positive and negative S/S of Schizophrenia
Lower Incidence of abnormal movements
Biggest S/E is weight gain e.g. Zyprexa
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21. Positive & Negative S/S of Schizophrenia
Hallucinations
Delusions
Abnormal thoughts
Bizarre behavior
Confused thoughts
Negative:
Blunted affect
Poverty of speech
Social withdrawal
Poor motivation
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22. Atypical Antipsychotics-2nd & 3rd generation: Clozaril (clozapine)
low incidence of abnormal movements
Most common S/E:
Nausea, constipation, sedation, drowsiness, weight gain
Other S/E are:
hypersalivation, tachycardia, dizziness, seizure risk
possible fatal side effect:
bone marrow suppression & Agranulocytosis (rare)
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23. Atypical Antipsychotics-2nd & 3rd generation - 2
Risperidone
Does not cause bone marrow suppression
Can cause at higher doses movement disorders
Available as a long acting injection
Can be used to treat mania
Seroquel (Quetiapine)
S/E sedation, weight gain and headache
Not associated with abnormal movements
May cause AV block
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24. Atypical Antipsychotics-2nd & 3rd generation - 3
Zyprexa (Olanzapine)
does not cause bone marrow suppression
Can cause weight gain & hyperglycemia
Drowsiness, dry mouth, constipation, and restlessness
Geodon (Ziprasidone)
Binds to multiple receptor sites
Drowsiness, headache, GI upset
Can prolong the QT interval-can be fatal if history of cardiac arrhythmias
Abilify (Aripiprazole)
Dopamine stabilizer
Partial agonist at the D2 receptor
In areas of the brain with excess dopamine, it lowers dopamine
In areas of low dopamine, it stimulates receptors to raise the dopamine level
Main S/E are headache, somnolence, agitation, anxiety, insomnia, and GI upset
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25. Antipsychotics-Long acting preparation
Can be given be given as an IM injection (depot preparations) if have difficulty taking oral meds.
Can use lower doses when given IM, so less risk of tardive dyskinesia
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26. Neuroleptic Malignant Syndrome
Rare, but fatal complication from all antipsychotic drugs
See more with 1st generation drugs
Severe muscle rigidity
High temperature
Associated S/S:
Tachycardia
Hypertension
Stupor
Coma
Abnormal labs including leukocytosis , Elevated Creatinine phosphokinase (CPK) & LFT
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27. Mood Stabilizers
Used in the treatment of Manic (Bipolar) disorder, and in some forms of depression
Drugs used: Lithium and Antiepileptic Drugs
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28. Lithium Mechanism of action unknown Alters electrical conductivity
potential threat to all body functions that are regulated by electrical currents
Can cause polyuria and polydipsa due to Na and K alterations
Has the lowest therapeutic index of all psych drugs
Have to monitor blood levels
Interacts with Sodium and Potassium
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29. Lithium
Maintenance blood levels of lithium are usually mEq (toxicity occurs with levels > 1.5 mEq/L)
Sign of toxicity is a fine intention tremor that becomes more pronounced and coarse
Risk of thyroid & kidney disease
If toxic S/S occur discontinue the drug and notify health care provider
Lithium should be taken with food
Client must eat a balanced diet with normal sodium intake and take in adequate fluid (about 2-3 liters/day).
Excretion is via renal system
Dehydration and salt restriction can increase lithium levels & cause toxicity.
Takes 2-3 weeks for lithium to become effective (may use antipsychotic until therapeutic levels are reached)
Therapeutic index
From Wikipedia, the free encyclopedia
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This article needs additional citations for verification. Please help improve this article by adding reliable references. Unsourced material may be challenged and removed. (May 2010) The therapeutic index (also known as therapeutic ratio), is a comparison of the amount of a therapeutic agent that causes the therapeutic effect to the amount that causes death. Quantitatively, it is the ratio given by the lethal dose divided by the therapeutic dose. A therapeutic index is the lethal dose of a drug for 50% of the population (LD50) divided by the minimum effective dose for 50% of the population (ED50). A higher therapeutic index is preferable to a lower one: a patient would have to take a much higher dose of such a drug to reach the lethal threshold than the dose taken to elicit the therapeutic effect.
Generally, a drug or other therapeutic agent with a narrow therapeutic range (i.e. having little difference between lethal and therapeutic doses) may have its dosage adjusted according to measurements of the actual blood levels achieved in the person taking it. This may be achieved through therapeutic drug monitoring (TDM) protocols. The therapeutic index for diazepam is somewhat forgiving at about 100. Other drugs, however, are much less so, such as Digoxin, with an index of 2 or 3. [1] Other examples of drugs with a narrow therapeutic range, which may require drug monitoring both to achieve therapeutic levels and to minimize toxicity, include: dimercaprol, theophylline, warfarin and lithium carbonate. Some antibiotics require monitoring to balance efficacy with minimizing adverse effects, including: gentamicin, vancomycin, amphotericin B, and polymyxin B.
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30. Signs & Symptoms of Lithium Toxicity
Severe Toxicity:
decrease level of consciousness to stupor and finally coma
Seizures, severe hypotension, severe polyuria with dilute urine
Fine hand tremors that progress into coarse tremors
Mild GI upset progressing to persistent upset
Slurred speech and muscle weakness progressing to mental confusion
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31. Lithium
Lithium serum concentrations are increased by Flouxetine (Prozac), ACE inhibitors, Thiazide diuretics, and NSAIDs
Lithium serum concentrations are decreased by theophylline, osmotic diuretics, and urine alkalinizers
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32. Contraindications for Lithium
Renal disease
Cardiac disease
Severe dehydration
Sodium depletion
Brain damage
Pregnancy or lactation
Use with caution in the elderly or clients with diabetics, thyroid disorders, urinary retention, and seizures
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33. Anticonvulsants/Antiepileptic Drugs
Causes an increase in GABA in the CNS-which causes a decrease in anxiety.
Reduce the mood swings with bipolar
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34. Anticonvulsants/Antiepileptic Drugs
Tegretol (carbamazepine)-also used to treat severe pain (i.e. trigeminal neuralgia), cause agranulocytosis and aplastic anemia
Depakote (Valproic acid)-can cause hepatic failure, pancreatitis, & thrombocytopenia. Watch for liver failure
Klonopin (Clonazepam)
Lamictal (Lamotrigine)-can have a rare but fatal dermatological condition
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35. Toxic Effects of Anticonvulsants
Tegretol can cause agranulocytosis and aplastic anemia
Depakote can cause liver dysfunction, hepatic failure, and blood dyscrasias including thrombocytopenia
Depakote interacts with drugs that are metabolized by the liver
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36. Contraindications for Anticonvulsants
Hepatic or renal disease
Pregnancy
Lactation
Presence of blood dyscrasias
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37. Psychoeducation when using anticonvulsants
Monitor blood levels of mood stabilizers to prevent toxicity
Monitor liver, renal function tests and CBCs
Depakote must be swallowed whole, not cut, chewed, or crushed to prevent irritation
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38. Evolution of Antidepressant Drugs
1950
1960
1970
1980
1990
2000
2009
Phenelzine
Phenelzine
Imipramine
Imipramine
Maprotiline
Maprotiline
Fluoxetine
Fluoxetine
Nefazodone
Escitalopram
Valdoxan
Isocarboxazide
Isocarboxazid
Clomipramine
Clomipramine
Amoxapine
Amoxapine
Sertraline
Sertraline
Mirtazapine
Duloxetine
Tranylcypromine
Tranylcypromine
Nortriptyline
Nortriptyline
Mianserine
Paroxetine
Reboxetine
Trazodone
Amitriptyline
Amitriptyline
Fluvoxamine
Venlafaxine
Citalopram
Tianeptine
Desipramine
Desipramine
Bupropion
Milnacipran
Moclobemide 38

39. Antidepressants
Treatment of depressive moods, including bipolar disease
4 categories:
Tricyclics (TCA)
MAOI’s
SSRI’S
Atypical Antidepressants
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40. Antidepressant Drugs Tricyclics- Elavil, Tofranil
SSRI’s- Lustral, Seroxat
MAOI’s- Nardil, Parnate
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41. Atypical Antidepressants
Inhibits reuptake of serotonin:
Trazodone (desyrel)
Norepinephrine Dopamine Reuptake Inhibitor (NDRI): Wellbutrin (Bupropion)
Sertonin Norepinephrine Reuptake Inhibitor-(SNRI): Effexor (venlafaxine)
Cymbalta (duloxetine)
Increases release of serotonin & norepinephrine: Remeron (mirtazapine)
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42. Atypical Antidepressants
Trazodone:
alternative to TCA’s, may cause orthostatic hypotension, sedation, and priapism in males
Remeron:
causes sedation, weight gain, dry mouth, constipation
Wellbutrin (zyban): rarely causes sedation, weight Gain, or sexual dysfunction
Used for smoking cessation. Most common S/E are headaches, insomnia & nausea
May lower seizure threshold
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43. Atypical Antidepressants: serotonin norepinephrine reuptake inhibitor (SNRI)
Skipping 1 dose can cause withdrawal S/S
Very effective in treating severe depression
Cymbalta is effective in treating somatic symptoms e.g. pain
SNRI-blocks uptake of serotonin and norepinephrine
Drugs include Effexor
& Cymbalta
Good for clients with anxiety
S/E:GI, sexual dysfunction, insomnia, agitation
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44. Major Indications for Antidepressants
Major Depressive disorder
Bipolar depression
Anxiety disorders:
Panic disorder
Obsessive-Compulsive
Phobic disorders
PTSD
Substance Abuse
Chronic Pain
Tourette’s Disorder
ADHD
Eating disorders
Sleep disorders
Migraines
Enuresis
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45. TriCyclicAntidepressant (TCA): Tryptizol, Pamelor, Tofranil, Anafranil, Aventyl, Asendin, Sinequan
Other side effects:
Orthostatic hypotension
Sedation
Weight gain
Confusion-esp. elderly
Arrhythmias
Blocks the reuptake of norepinephrine and serotonin
Tricyclic drugs block the muscarine receptors causing anticholinergic side effects
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46. TCA’s Contraindications
Do not mix with ETOH (none of the psych drugs should be mixed with ETOH)
Dementia
Suicidal clients
Cardiac disease
Pregnancy
Seizure disorders
Urinary retention
Dose for elderly should be ½ of adult dose
TCA’s and MAOIs are effective in treatment of depression
are not as safe nor well tolerated as the newer antidepressants
Toxic Effects:
possibility of cardiac toxicity in overdose
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47. SSRI’s Prozac, Lustral, Seroxat, Faverin, Cipralex, Serzone
Blocks the reuptake of serotonin into the neuron
Are very safe and are not lethal in overdose
Good choice with the elderly-very few side effects
If used with MAOI’s may cause Serotonin Syndrome: seizure, death
If used with TCA’s may cause TCA toxicity
Takes 2 weeks to feel effects
Side-effect: GI, CNS however the biggest is sexual dysfunction & weight gain
Contraindication: Cardiac dysrhythmias
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48. MAOI’s
Nardil, Parnate
Inhibits MAO, thus interfering with breakdown of norepinephrine, dopamine, and serotonin
Avoid foods with tyramine (aged cheese, red wine, beer, chocolate, etc.)
MAOI’s don’t play well with other drugs!!
Toxic effects: hypertensive crises
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49. Adverse effets linked with neurotransmitter
activity and receptor binding
Activating side effects
5-HT2 agonism
Weight gain
Ach
antagonism
Blurred vision
Nausea
5-HT3 agonism
Activating effects
NE reuptake
inhibition
Postural hypotension
Dizziness
Reflex tachycardia
α2 antagonism
Priapism
DA reuptake
Psychomotor activation
Traditional
Antidepressants
5-HT reuptake
H1 antagonism
α1 antagonism
Dry mouth
Urinary retention
Tremor-CV troubles
Sexual dysfunction
GI disturbances
Sedation/ drowsiness
Constipation
Sinus tachyardia
Memory dysfunction
Psychosis - Abuse
The “cleaner” the drug, the better the side effect profile. Agents that have greater affinities for multiple receptors will, by definition, run a greater risk of creating unwanted side effects. This slide shows the relationship between neurotransmitter affinity, receptor activity, and clinical side effects.
Adapted from Richelson 1993

50. Antianxiety/Anxiolytic Drugs
GABA exerts an inhibitory effect on neurons
These drugs enhance its effect and produce a sedative effect
Therefore reduce anxiety
The most common used drugs here are the Benzodiazepines
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51. Benzodiazepines Valium, Xanax, Ativan , Librium, Lexotanil
Dalmane, Halcion (used as sleep aides-short term)
Used for anxiety disorders, ETOH withdrawal, muscle spasm, sedation, insomnia, and epileptics/seizures
Risk of dependency
Avoid ETOH
Causes sedation-don’t drive!!
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52. Benzodiazepines Side Effects Toxic Effects Contraindications Teaching
Drowsiness, confusion, sedation, and lethargy
Toxic Effects
Respiratory depression esp. with ETOH use!
Contraindications
Combination with other CNS depressants
Renal or hepatic dysfunction (may use Ativan)
History of drug abuse or addiction
Depression and suicidal tendencies
Teaching
Use short term due to risk of drug dependency
Avoid ETOH and other CNS depressants
Can impair ability to drive
Sudden D/C of benzodiazepines might cause withdrawal s/s
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53. Non-benzodiazepine Anxiolytic
BuSpar (Buspirone)
Reduces anxiety without strong sedative-hypnotic properties
Not a CNS depressant
Takes 2 weeks to feel effects
No potential for addiction
Side Effects
Dizziness, dry mouth, nervousness, diarrhea, headache, excitement
Toxic Effects
Lethal dose is times the daily recommended dose
Contraindications
Use with caution in PG women
Nursing mothers
Clients with renal or hepatic disease
Anyone taking MAOs
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54. Sedative/Hypnotic Drugs
Anxiolytic and hypnotic
Can lead to tolerance and dependency
Use for short term
Drugs used
benzodiazepines: Dalmane, Restoril, Halcion
Non-benzodiazepines: Ambien, Sonata, Lunestra
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55. Psychoeducation when using Benzodiazepine Teaching
Use short term(1-2 weeks)
Carefully need to taper these off-never stop cold turkey
Do not take with other meds without talking to provider first
Do not drive if sedated on these!!
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56. Client Teaching for Non-benzodiazepines
Long term use not recommended
Do not drive when taking
Can repeat Sonata up to 4 hours before arising
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57. ADD/ADHD-Psychostimulants
S/E: wt. loss, anorexia, insomnia, headache, long-term growth suppression
Potential for abuse
Also used to treat narcolepsy
Ritalin, Adderall, Dexedrine, Concerta,
Daytrana
Action=
increasing the release and blocking the reuptake of monoamines (dopamine, norepinephrine)
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58. ADD/ADHD-Psychostimulants
Intended effects:
Increased attention span & concentration
Decreased distractibility, hyperactivity, and impulsivity
Treatment of ADHD, ADD, & narcolepsy
S/E:
Anorexia
Wt. loss
Growth retardation in children
Insomnia
Headache
Cardiovascular effects-high blood pressure, dysrhythmias
Contraindications:
Hx of drug abuse & dependency, severe anxiety, anorexia, MAIOIs
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59. ADD/ADHD- Non-Stimulants
Strattera (atomoxetine)
Controls symptoms thru selective inhibition of norepinephrine
Takes 1-3 weeks to feel effects
No abuse potential and is not considered a controlled substance
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60. Meds used to Treat Extrapyramidal SE
Cogentin
Benadryl
Artane
Symmetrel
Requip
Akineton
Kemadrin
These meds should be taken simultaneously with antipsychotic meds to prevent EPS
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61. Herbal Medicines Ginkgo biloba-helps with memory Kava-Kava
St. John’s Wart
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62. Questions after lecture?
Please or call ( )
Interested in learning more about child and adolescent psychiatry?
Arrange to attend OPD
Consider an elective rotation during internship or otherwise
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63. Meds for Alzheimer’s
Drugs here are used to slow the progression of the disease
Memantine (Namenda, Ebixa)
Cognex (tacrine)
Aricept (donepezil)
Exelon (Rivastigmine)
Razadyne (galantamine)
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64. PET Scan=positron-emission tomography (PET) scans
Useful in identifying physiological and biochemical changes as they occur in living tissue
i.e. clients with schizophrenia PET scans show a decrease of glucose in the frontal lobes of unmedicated clients, also can indicate mood disorders, ADHD
Radioactive substance is injected, travels to the brain, and illuminates the brain. Have 3D visualizations of the CNS
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