Psychopharmacology Khalid Bazaid MB BS FRCPC Assistant Professor

Psychopharmacology Khalid Bazaid, MB BS, FRCPC Assistant Professor Child & Adolescent Psychiatrist Department of Psychiatry College of Medicine King Saud University 9/18/2020 1

Outlines § The role of psychotropic medications 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 § Overview Psychotropic Medications Classifications 9/18/2020 2

Psychopharmacology The aim is learn how to choose a psychotropic drug that is more: • Less toxic • Effective • Better-tolerated • The most targeted therapeutic agents 9/18/2020 3

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 otherapies 9/18/2020 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 9/18/2020 5

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 9/18/2020 § 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 6

Reasons for Non- adherence: § Medications are expensive § Unpleasant side effects § Feel better and decide no longer need 9/18/2020 § Stigma associated with having a mental illness and taking medications § Paranoia or fears about medication usage particularly addition 7

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 9/18/2020 8

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 9/18/2020 9

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 9/18/2020 10

Psychotropic Medications Classifications § Antipsychotics (Neuroleptics) § Mood Stabilizers § Antidepressants § Anxiolytics (antianxiety) 9/18/2020 § Sedatives § Hypnotics § Psychostimulants § Antihistamines, antimuscarinics, dopamine agonists 11

Antipsychotics NEUROLEPTICS / MAJOR TRANQUILIZERS § Block D 2 receptors in the mesolimbic system § Not addictive § Treat all psychoses & psychotic symptoms Schizophrenia Disorders Tourette’s Syndrome Bipolar disorder Delirium, Dementia, and Delusions Major Depression with psychotic features Control of intractable hiccups Aggressive behavior 12

ANTIPSYCHOTIC DRUGS NEUROLEPTICS / MAJOR TRANQUILIZERS Mechanism of action § In typical antipsychotics – Blockage of D 2 – receptors in: § Nigro-strial (psychiatric tract) § Substantia Nigra (Neurological tract) § Tubero-infundibular tract (Endocrine tract) § In atypical antipsychotics: – Blockage of 5 HT 2 A/D 2 receptors 13

ANTIPSYCHOTIC DRUGS Side effects (hint) § High Potency typical antipsychotics: Neurological side effects e. g. Haloperidol § Low Potency typical antipsychotics: other side effects e. g. Chlorpromazine 14

ANTIPSYCHOTIC DRUGS Neurologic Side effects § Due to D 2 blockade Parkinsonian syndrome – – – Position & gait Apathy Drooling Fine tremor Staring eyes 15

ANTIPSYCHOTIC DRUGS Neurologic Side effects § Due to D 2 blockade – Parkinsonian syndrome – Akathesia (Motor restlessness) § § Subjective feelings of restlessness Objective signs of restlessness Feelings of anxiety, inability to relax, jitteriness, pacing, rocking motions while sitting, rapid alterations of position. More in middle aged women 16

ANTIPSYCHOTIC DRUGS Neurologic Side effects § Due to D 2 blockade Acute dystonia – Parkinsonian syndrome – Akathesia (Motor restlessness) § § Brief or prolonged muscle contraction leading to abnormal movements or postures e. g. Occulogyric crises, tongue protrusion, torticollis, laryngeal pharyngeal dystonias and dystonic Postures Early onset, more in young men and high doses of typical neurosleptics 17

ANTIPSYCHOTIC DRUGS Neurologic Side effects § Due to D 2 blockade – Parkinsonian syndrome – Akathesia (Motor restlessness) § Involuntary choreiform, athetoid or rhythmic movements of the tongue, jaw, trunk or extremities § More with long term typical neuroleptic treatment, old age, female sex, mood disorder, cognitive disorders. – Acute dystonia – Tardive Dykinesia 18

ANTIPSYCHOTIC DRUGS Neurologic Side effects § Due to D 2 blockade – Parkinsonian syndrome – Akathesia (Motor restlessness) § § § Muscular rigidity, , Hyper-thermia , Akinesia, mutism, obtundation & agitation, sweating, tachycardia, Hypertension. Increased WBC, increased CPK, liver enzymes, and plasma myoglobulin. Myoglobulinuria, may occur and may lead to renal failure. Symptoms evolve in 1 -3 days & may last 10 -14 days. May occur at any time More common in young men Mortality: 20% - 30%( higher with depot) – – – Acute dystonia Tardive Dyskinesia Neuroleptic malignant syndrome 19

ANTIPSYCHOTIC DRUGS Other Side effects § Muscarenic (anti-cholenergic): – – dry mouth Constipation Blurred vision, urinary retention Precipitation of narow angle glucoma § Alpha– 1–adrenergic blockade: – Orthostatic hypotension – Impotence – Impaired ejaculation 20

ANTIPSYCHOTIC DRUGS Other Side effects § CNS Side effects: – § Sedation Metabolic / Endocrine Side effects: – – § weight gain Increased BS & lipids Galactorrhea Amenorrhea Allergic Side effects – – Cholestatic jaundice Agranulostasis § Cardiac side effects: – EKG changes – Arrythmias § Occular Side effects: – Corneal Opacities – Retinitis pigmentoza § Dermatological Side effects: – Photosensitivities – Metallic discoloration – Contact dermatitis 21

Antipsychotics-Long acting preparation § Can 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 9/18/2020 22

Antidepressants § Treatment of depressive moods, including bipolar disease § 4 categories: – Tricyclics (TCA) – MAOI’s – SSRI’S – Atypical Antidepressants 9/18/2020 23

Major Indications for Antidepressants § Major Depressive disorder § Bipolar depression § Anxiety disorders: Ø Ø Ø Panic disorder Obsessive-Compulsive Phobic disorders § PTSD 9/18/2020 § § § § Substance Abuse Chronic Pain Tourette’s Disorder ADHD Eating disorders Sleep disorders Migraines Enuresis 24

Antidepressant Drugs § Tricyclics- Amitriptyline, Imipramine § SSRI’s- Fluoxetine, Sertraline § MAOI’s- Phenelzine , Tranycypramine 9/18/2020 25

Atypical Antidepressants § Inhibits reuptake of serotonin: desyrel (Trazodone) § Norepinephrine Dopamine Reuptake Inhibitor (NDRI): Wellbutrin (Bupropion) 9/18/2020 § Serotonin Norepinephrine Reuptake Inhibitor-(SNRI): Effexor (venlafaxine) Cymbalta (duloxetine) § Increases release of serotonin & norepinephrine: Remeron (Mirtazapine) 26

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 9/18/2020 27

Atypical Antidepressants: Serotonin Norepinephrine Reuptake Inhibitor (SNRI) § SNRI-blocks uptake of serotonin and norepinephrine § Skipping 1 dose can cause withdrawal S/S § Drugs include Effexor & Cymbalta § Very effective in treating severe depression § Good for clients with anxiety § S/E: GI, sexual dysfunction, insomnia, agitation 9/18/2020 § Cymbalta is effective in treating somatic symptoms e. g. pain 28

ANTIDEPRESSANT DRUGS Side effects § HETEROCYCLICS: – Muscarenic (anti-cholenergic): § § Dry mouth Constipation Blurred vision, urinary retention Precipitation of narow angle glucoma § Alpha– 1–adrenergic blockade: – – – Orthostatic hypotension Impotence Impaired ejaculation 29

ANTIDEPRESSANT DRUGS Side effects Central anti-cholenergic syndrome: § § § Delirium Coma seizures Agitation Hallucinations Severe hypotension Supra-ventricular tachycardia Flushing Mydriasis Dry skin Hyperthermia Decreased bowel sounds. Management n Stop HCA immediately n Physostigmine (anticholinesterase inhibitor) 12 mg IV or IM every 20 – 60 minutes, until improvement occurs n Cardiac monitoring and life support (physostigmine may lead to severe BP drop and bronchial constriction) n Benzodiazepines may be used. 30

ANTIDEPRESSANTS Side effects § HETEROCYCLICS: § SSRI: – have a much better side effect profile: § Agitation § Sexual problems § Stomach upset § Hypersomnia/insomnia 31

ANTIDEPRESSANTS Side effects § § § HETEROCYCLICS: SSRI: MAOI: – Cardiovascular (orthostatic hypotension, tyramine hypertensive crisis) – Sexual (Impotence & delayed ejaculation) – Neurologic (insomnia, seizure& euphoria) – Hepatic: (Cholestatic reaction). 32

ANTIDEPRESSANTS Side effects § § § HETEROCYCLICS: SSRI: MAOI: – Interaction: – Diet: Aged cheese Pickled herriag Raisin Alcohol Chicken liver Beans Figs Yeast products Chocolate Amphetamines Decongestants & nasal sprays (Ephedrine…. ) Epinephrine (local anesthesia) Aldomet 33

MOOD STABLIZERS § § § Lithium Carbonate Sodium Valproate Carbamazepine Lamotrigine Topiramate Clozapine 34

MOOD STABLIZERS § Used in the treatment of Manic (Bipolar) disorder, and in some forms of depression § Drugs used: Lithium and Antiepileptic Drugs 35

Lithium § Mechanism of action unknown § Alters electrical conductivity – potential threat to all body functions that are regulated by electrical currents 9/18/2020 § 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 36

LITHIUM CARBONATE Side effects § § § § Neurological: Tremor (50%), weakness, cog-wheeling Renal: Occur in 10 -50 % e. g. polyuria, polydipsia, nephrogenic D. I. , nephrotic syndrome, (tubular changes with chronic use and high levels) Cardiac: Similar to those of hypokalimia e. g. U-wave and T-wave depression Endocrine: Goiter, hypothyroidism, abnormal thyroid functions (30 -40%) Dermatological: Acne, exacerbation of psoriasis ), hair loss. Pregnancy and lactation: Teratogenicity (level in milk=30 -100% of maternal blood level) Toxicity: (seizures, delirium, cerebellar signs, coma) occurs in blood level= 1. 2 – 2 m. Eq/l. Lethal levels above that. 37

Signs & Symptoms of Lithium Toxicity § Fine hand tremors that progress into coarse tremors § Mild GI upset progressing to persistent upset § Slurred speech and muscle weakness progressing to mental confusion 9/18/2020 § Severe Toxicity: – decrease level of consciousness to stupor and finally coma – Seizures, severe hypotension, severe polyuria with dilute urine 38

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 9/18/2020 39

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 9/18/2020 40

Benzodiazepines § Valium, Xanax, Ativan , Librium, Lexotanil § Risk of dependency § Avoid ETOH § Dalmane, Halcion (used as sleep aides-short term) § Causes sedationdon’t drive!! § Used for anxiety disorders, ETOH withdrawal, muscle spasm, sedation, insomnia, and epileptics/seizures 9/18/2020 41

Benzodiazepines § Side Effects – 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 9/18/2020 42

Non-benzodiazepine Anxiolytic § § § Bu. Spar (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 160 -550 times the daily recommended dose § Contraindications – – Use with caution in PG women Nursing mothers Clients with renal or hepatic disease Anyone taking MAOs 9/18/2020 43

Questions after lecture? § Please e-mail (kbazaid@ksu. edu. sa) or call (01 467 1717) § Interested in learning more about child and adolescent psychiatry? – – Arrange to attend OPD Consider an elective rotation during internship or otherwise 9/18/2020 44 44