06 Psychotherapeutic Agents Upd

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Pharmacology

Pharmacology

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  • 1. Antidepressants and Antipsychotics
  • 2.
    • The therapy of emotional and mental disorders
  • 3.
    • Anxiety
    • Grief
    • Depression
    • are normal human emotions
  • 4.
    • The ability to cope with these emotions can range from occasional depression or anxiety to constant emotional distress to the point ofinterfering with the ability to carry on normal daily living.
  • 5.
    • When these emotions significantly affect an individual’s ability to carry out normal daily functions, treatment with a psychotherapeutic drug is a possible option.
  • 6.
    • Three main emotional and mental disorders:
    • Psychoses
    • Affective disorders
    • Anxiety
  • 7.
    • Psychosis
    • A major emotional disorder that impairs the mental function of the affected individual to the point that the individual cannot participate in everyday life.
    • Hallmark: loss of contact with reality
  • 8.
    • Affective Disorders
    • Major emotional disorders that impair the mental function of the affected individual to the point that the individual cannot participate in everyday life.
  • 9.
    • Affective Disorders
    • Mania: abnormally pronounced emotions
    • Depression: abnormally reduced emotions
    • Bipolar affective disorder: exhibits both mania and depression
  • 10.
    • Pathophysiology
    • Biochemical Imbalance
    • Mental disorders are associated with abnormal levels of endogenous chemicals, such as neurotransmitters, in the brain.
  • 11.
    • Pathophysiology
    • Biochemical Imbalance
    • Brain levels of certain catecholamines play an important role in maintaining mental health.
      • Dopamine
      • Serotonin
      • Histamine
  • 12.
    • Pathophysiology
    • Biochemical Imbalance
    • Other biochemicals are necessary for normal mental function.
      • GABA
      • acetylcholine
      • lithium
  • 13.
    • Biogenic Amine Hypothesis
    • Depression and mania are due to an alteration in neuronal and synaptic catecholamine concentration at adrenergic receptor sites in the brain.
      • Depression: deficiency of catecholamine, especially norepinephrine
      • Mania: excess amines
  • 14.  
  • 15.
    • Drug Categories
    • Antidepressants
    • tricyclics, tetracyclics, SSRIs, MAOIs
    • Antimanic Agents
    • lithium
  • 16.
    • Cyclic antidepressants
      • tricyclics
      • tetracyclics
    • Monoamine oxidase inhibitors (MAOIs)
    • Second-generation antidepressants and SSRIs
  • 17.
    • Tricyclic antidepressants—primary: amitriptyline (Elavil), doxepin (Sinequan), imipramine (Tofranil)
    • Tricyclic antidepressants—secondary: desipramine (Norpramin), nortriptyline (Aventyl), protriptyline (Vivactil)
    • Tetracyclic antidepressants: amoxapine (Asendin), maprotiline (Ludiomil)
  • 18.
    • Block reuptake of neurotransmitters, causing accumulation at the nerve endings.
    • It is thought that increasing concentrations of neurotransmitters will correct the abnormally low levels that lead to depression.
  • 19.
    • Blockade of norepinephrine:
      • antidepressant, tremors, tachycardia, additive pressor effects with sympathomimetic drugs
    • Blockade of serotonin:
      • antidepressant, nausea, headache, anxiety, sexual dysfunction
  • 20.
    • Depression
    • Childhood enuresis (imipramine)
    • Obsessive-compulsive disorders (clomipramine)
    • Adjunctive analgesics
    • Trigeminal neuralgia
  • 21.
    • Sedation
    • Impotence
    • Orthostatic hypotension
    • Older patients:
      • dizziness, postural hypotension, constipation, delayed micturation, edema, muscle tremors
  • 22.
    • Lethal—70 to 80% die before reaching the hospital
    • CNS and cardiovascular systems are mainly affected
    • Death results from seizures or dysrhythmias
    • No specific antidote
      • Decrease drug absorption with activated charcoal
      • Speed elimination by alkalinizing urine
      • Manage seizures and dysrhythmias
      • Basic life support
  • 23.
    • Highly effective
    • Considered second-line treatment for depression not responsive to cyclics
    • Disadvantage: potential to cause hypertensive crisis when taken with tyramine
  • 24.
    • phenelzine (Nardil)
    • tranylcypromine (Parnate)
    • isocarboxazid (Marplan)
  • 25.
    • Inhibit the MAO enzyme system in the CNS
    • Amines (dopamine, serotonin, norepinephrine) are not broken down, resulting in higher levels in the brain
    • Result: alleviation of symptoms of depression
  • 26.
    • Depression, especially types characterized by reverse vegetative symptoms such as increased sleep and appetite
    • Depression that does not respond to other agents such as tricyclics
  • 27.
    • Few side effects—orthostatic hypotension most common
    • Tachycardia Palpitations
    • Dizziness Drowsiness
    • Insomnia Headache
    • Anorexia Nausea
    • Blurred vision Impotence
  • 28.
    • Symptoms appear 12 hours after ingestion
    • Tachycardia, circulatory collapse, seizures, coma
    • Treatment: protect brain and heart, eliminate toxin
      • Gastric lavage
      • Urine acidification
      • Hemodialysis
  • 29.
    • Ingestion of foods and/or drinks with the amino acid TYRAMINE leads to hypertensive crisis, which may lead to cerebral hemorrhage, stroke, coma, or death
  • 30.
    • Avoid foods that contain tyramine!
    • Aged, mature cheeses (cheddar, blue, Swiss)
    • Smoked/pickled or aged meats, fish, poultry (herring, sausage, corned beef, salami, pepperoni, paté)
    • Yeast extracts
    • Red wines (Chianti, burgundy, sherry, vermouth)
    • Italian broad beans (fava beans)
  • 31.
    • Newer
    • Fewer side effects than tricyclics, but not superior in overall efficacy or onset of action
      • trazodone (Desyrel)
      • bupropion (Wellbutrin, Zyban)
      • selective serotonin reuptake inhibitors (SSRIs)
  • 32.
    • Selectively inhibit serotonin reuptake
    • Little or no effect on norepinephrine or dopamine reuptake
    • Results in increased serotonin concentrations at nerve endings
    • Advantage over tricyclics and MAOIs: Little or no effect on cardiovascular system
  • 33.
    • Used for depression—very few serious side effects
    • Bipolar affective disorder
    • Obesity
    • Eating disorders
    • Obsessive-compulsive disorder
    • Panic attacks
    • Myoclonus
    • Treatment of various substance abuse problems (bupropion [Zyban] is used for smoking cessation treatment)
  • 34.
    • Body System Effects
    • CNS Headache, dizziness, tremor, nervousness, insomnia, fatigue
    • GI Nausea, diarrhea, constipation, dry mouth
    • Other Sweating, sexual dysfunction
  • 35.
    • Highly bound to plasma proteins
    • Compete with other protein-binding drugs, resulting in more free, unbound drug to cause a more pronounced drug effect
  • 36.
    • Drugs used to treat serious mental illness
    • Behavioral problems or psychotic disorders
  • 37.
    • Thioxanthenes: chlorprothixene, thiothixene (Navane)
    • Butyrophenones: haloperidol (Haldol)
    • Dihydroindolones: molindone (Moban)
    • Dibenzoxazepine: loxapine (Loxitane)
    • Phenothiazines: three structural groups
  • 38.
    • Aliphatic: chlorpromazine (Thorazine), triflupromazine (Vesprin)
    • Piperidine: mesoridazine (Serentil), thioridazine (Mellaril)
    • Piperazine: fluphenazine (Prolixin), perphenazine (Trilafon), prochlorperazine (Compazine), trifluoperazine (Stelazine)
    • Largest group of psychotropic agents
  • 39.
    • clozapine (Clozaril)
    • risperidone (Risperdal)
    • olanzapine (Zyprexa)
    • quetiapine (Seroquel)
  • 40.
    • Block dopamine receptors in the brain (limbic system, basal ganglia)—areas associated with emotion, cognitive function, motor function
    • Dopamine levels in the CNS are decreased
    • Result: tranquilizing effect in psychotic patients
  • 41.
    • The newer, atypical antipsychotics also block specific serotonin receptors (serotonin-2 [5HT2] receptors).
    • This is responsible for their improved efficacy and safety profiles.
  • 42.
    • Block dopamine receptors in CNS
    • Block alpha receptors (causing hypertension, other cardiovascular effects)
    • Block histamine receptors (causing anticholinergic effects)
    • Block serotonin
    • Also function as antiemetics
    • Antianxiety effects
  • 43.
    • Treatment of serious mental illnesses:
      • Bipolar affective disorder
      • Depressive and drug-induced psychoses
      • Schizophrenia
      • Autism
    • Movement disorders (such as Tourette’s syndrome)
    • Some medical conditions
      • Nausea, intractable hiccups
  • 44.
    • Body System Effects
    • CNS Sedation, delirium
    • Cardiovascular Orthostatic hypotension, syncope, dizziness, ECG changes
    • Dermatologic Photosensitivity, skin rash, hyperpigmentation, pruritus
  • 45.
    • Body System Effects
    • GI Dry mouth, constipation
    • GU Urinary hesitancy or retention, impaired erection
    • Hematologic Leukopenia and agranulocytosis
    • Metabolic/endocrine Galactorrhea, irregular menses increased appetite, polydipsia
  • 46.
    • Before beginning therapy, assess both the physical and emotional status of patients
    • Obtain baseline VS, including postural BP readings
    • Obtain liver and renal function tests (and baseline platelet levels for MAOIs)
  • 47.
    • Assess for possible contraindications to therapy, cautious use, and potential drug interactions
    • Assess LOC, mental alertness, potential for injury to self and others
    • Check the patient’s mouth to make sure oral doses are swallowed
  • 48.
    • Provide simple explanations about the drug, its effects, and the length of time before therapeutic effects can be expected
    • Abrupt withdrawal should be avoided
    • Advise patients to change positions slowly to avoid postural hypotension and possible injury
  • 49.
    • The combination of drug therapy and psychotherapy is emphasized because patients need to learn and acquire more effective coping skills
    • Only small amounts of medications should be dispensed at a time to minimize the risk of suicide attempts
    • Simultaneous use of these agents with alcohol or other CNS depressants can be fatal
  • 50.
    • Antidepressants
    • Many cautions, contraindications, and interactions exist pertaining to the use of antidepressants.
    • Inform patients that it may take 1 to 3, even 4, weeks to see therapeutic effects.
    • Monitor patients closely during this time and provide support.
  • 51.
    • Antidepressants
    • Sedation often occurs with tricyclic therapy; notify physician if this lasts more than 2 weeks.
    • Assist elderly or weakened patients with ambulation and other activities as falls may occur due to drowsiness or postural hypotension.
  • 52.
    • Antidepressants
    • Tricyclics may need to be weaned and discontinued before undergoing surgery to avoid interactions with anesthetic agents.
    • Monitor for side effects and discuss with patients.
    • Encourage patients to wear medication ID badges naming the agent being taken.
  • 53.
    • Antidepressants
    • Caffeine and cigarette smoking may decrease effectiveness of medication therapy
    • Instruct patients and family regarding tyramine-containing foods and signs and symptoms of hypertensive crisis
  • 54.
    • Antipsychotics—Phenothiazines
    • Instruct patients to wear sunscreen due to photosensitivity
    • Avoid taking antacids or antidiarrheal preparations within 1 hour of a dose
    • Do not take alcohol or other CNS depressants with these medications
  • 55.
    • Antipsychotics—Phenothiazines
    • Long-term haloperidol therapy may result in tremors, nausea, vomiting, or uncontrollable shaking of small muscle groups; these symptoms should be reported to the physician
    • Oral forms may be taken with meals to decrease GI upset
    • These agents may cause drowsiness, dizziness, or fainting; instruct patients to change positions slowly
  • 56.
    • Monitor for therapeutic effects:
    • Monitor mental alertness, cognition, affect, mood,ability to carry out activities of daily living, appetite, and sleep patterns
    • Monitor the patient’s potential for self-injury during the delay between the start of therapy and symptomatic improvement
  • 57.
    • Monitor for therapeutic effects
    • For antidepressants:
      • Improved sleep patterns and nutrition, increased feelings of self-esteem, decreased feeling of hopelessness, increased interest in self and appearance, increased interest in daily activities, fewer depressive manifestations or suicidal thoughts or ideations
  • 58.
    • Monitor for therapeutic effects
    • For antipsychotics:
      • Improved mood and affect, alleviation of psychotic symptoms and episodes
      • Decrease in hallucinations, paranoia, delusions, garbled speech, inability to cope