N215 Unit 5 Chapter 16 Drugs for emotional disorders Flashcards
imipramine (Tofranil)
Therapeutic Class: Antidepressant; treatment of nocturnal enuresis in children
Pharmacologic Class: Tricyclic antidepressant
ACTIONS AND USES
Imipramine blocks the reuptake of serotonin and norepinephrine into nerve terminals. It is used mainly for major depression, although it is occasionally used for the treatment of nocturnal enuresis (bed wetting) in children. The nurse may find imipramine prescribed for a number of unlabeled uses, including intractable pain, anxiety disorders, and withdrawal syndromes from alcohol and cocaine. Therapeutic effectiveness may not occur for 2 or more weeks.
ADMINISTRATION ALERTS
- Paradoxical diaphoresis can be a side effect of TCAs; therefore, diaphoresis may not be a reliable indicator of other disease states such as hypoglycemia.
- Imipramine causes anticholinergic effects and may potentiate effects of anticholinergic drugs administered during surgery.
- Do not discontinue abruptly because rebound dysphoria, irritability, or sleeplessness may occur.
- Pregnancy category C.
PHARMACOKINETICS
Onset
Peak
Duration
Less than 1 h
1-2 h PO; 30 min IM
Variable
ADVERSE EFFECTS
Side effects include sedation, drowsiness, blurred vision, dry mouth, and cardiovascular symptoms such as dysrhythmias, heart block, and extreme hypertension. Agents that mimic the action of norepinephrine or serotonin should be avoided because imipramine inhibits their metabolism and may produce toxicity. Some patients may experience photosensitivity and hypersensitivity to tricyclic drugs.
Black Box Warning: Antidepressants increase the risk of suicidal thinking and behavior, especially in children, adolescents, and young adults with major depressive disorder and other psychiatric disorders. This drug is not approved for use in pediatric patients.
Contraindications: This drug should not be used in cases of acute recovery after MI, defects in bundle-branch conduction, narrow-angle glaucoma, and severe renal or hepatic impairment. Patients should not use this drug within 14 days of discontinuing MAOIs.
INTERACTIONS
Drug-Drug: Concurrent use of other CNS depressants, including alcohol, may cause sedation. Cimetidine (Tagamet) may inhibit the metabolism of imipramine, leading to increased serum levels and possible toxicity. Imipramine may reverse the antihypertensive effects of clonidine and potentiate CNS depression. Use of oral contraceptives may increase or decrease imipramine levels. Disulfiram may lead to delirium and tachycardia. Antithyroid agents may produce agranulocytosis. Phenothiazines cause increased anticholinergic and sedative effects. Sympathomimetics may result in cardiac toxicity. Methylphenidate or cimetidine may increase the effects of imipramine and cause toxicity. Phenytoin is less effective when taken with imipramine. MAOIs may result in neuroleptic malignant syndrome.
Lab Tests: Imipramine produces altered blood glucose tests. Elevation of serum bilirubin and alkaline phosphatase is likely.
Herbal/Food: Herbal supplements such as evening primrose oil or ginkgo may lower the seizure threshold. St. John’s wort used concurrently may cause serotonin syndrome.
Treatment of Overdose: There is no specific treatment for overdose. General supportive measures are recommended. Ensure an adequate airway, oxygenation, and ventilation. Monitor cardiac rhythm and vital signs. Gastric lavage may be indicated. Activated charcoal should be administered.
What drugs are used to treat emotional disorders?
ANTIDEPRESSANTS page 190
Tricyclic Antidepressants (TCAs) page 191 imipramine (Tofranil) page 194
Selective Serotonin Reuptake Inhibitors (SSRIs) page 191 sertraline (Zoloft) page 195
Atypical Antidepressants page 195
Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs) page 195
MAO Inhibitors (MAOIs) page 196 phenelzine (Nardil) page 196
DRUGS FOR BIPOLAR DISORDER page 200 lithium (Eskalith) page 202
Antiseizure Drugs page 201
Atypical Antipsychotic Drugs page 201
DRUGS FOR ATTENTION DEFICIT/HYPERACTIVITY DISORDER (ADHD) page 202
CNS Stimulants page 204 methylphenidate (Ritalin) page 205
Nonstimulant Drugs for ADHD
sertraline (Zoloft)
Therapeutic Class: Antidepressant
Pharmacologic Class: Selective serotonin reuptake inhibitor (SSRI)
ACTIONS AND USES
Sertraline is used for the treatment of depression, anxiety, obsessive-compulsive disorder, and panic. The antidepressant and anxiolytic properties of this drug can be attributed to its ability to inhibit the reuptake of serotonin in the brain. Other uses include premenstrual dysphoric disorder, post-traumatic stress disorder, and social anxiety disorder. Therapeutic actions include enhancement of mood and improvement of affect with maximum effects observed after several weeks.
ADMINISTRATION ALERTS
- It is recommended that sertraline be given in the morning or evening.
- When administering sertraline as an oral liquid, mix with water, ginger ale, lemon/lime soda, lemonade, or orange juice. Follow manufacturer’s instructions.
- Do not give concurrently with an MAOI or within 14 days of discontinuing MAOI medication.
- Pregnancy category C.
PHARMACOKINETICS
Onset
Peak
Duration
2-4 wk
Unknown
Variable (due to extensive binding with serum proteins)
ADVERSE EFFECTS
Adverse effects include agitation, insomnia, headache, dizziness, somnolence, and fatigue. Take extreme precautions in patients with cardiac disease, hepatic impairment, seizure disorders, suicidal ideation, mania, or hypomania.
Black Box Warning: Antidepressants increase the risk of suicidal thinking and behavior, especially in children, adolescents, and young adults with major depressive disorder and other psychiatric disorders.
Contraindications: Concomitant use of sertraline and MAOIs or primozide is not advised. Antabuse should be avoided because of the alcohol content of the drug concentrate.
INTERACTIONS
Drug-Drug: Highly protein bound medications such as digoxin and warfarin should be avoided owing to risk of toxicity and increased blood concentrations leading to increased bleeding. MAOIs may cause neuroleptic malignant syndrome, extreme hypertension, and serotonin syndrome, characterized by headache, agitation, dizziness, fever, diarrhea, sweating, and shivering. Use cautiously with other centrally acting drugs to avoid adverse CNS effects.
Lab Tests: Sertraline results in asymptomatic elevated liver function tests and a slight decrease in uric acid levels.
Herbal/Food: Patients should use caution if taking St. John’s wort or L-tryptophan to avoid serotonin syndrome.
Treatment of Overdose: There is no specific treatment for overdose. Emergency medical attention and general supportive measures may be necessary. Symptoms of overdose include nausea, vomiting, tremor, seizures, agitation, dizziness, hyperactivity, mydriasis, tachycardia, and coma.
phenelzine (Nardil) page 196
Therapeutic Class: Antidepressant
Pharmacologic Class: Monoamine oxidase inhibitor (MAOI)
ACTIONS AND USES
Phenelzine produces its effects by irreversible inhibition of monoamine oxidase; therefore, it intensifies the effects of norepinephrine in adrenergic synapses. It is used to manage symptoms of depression that are not responsive to other types of pharmacotherapy and is occasionally used for panic disorder. Drug effects may persist for 2 to 3 weeks after therapy is discontinued.
ADMINISTRATION ALERTS
- Washout periods of 2 to 3 weeks are required before introducing other drugs.
- Abrupt discontinuation of this drug may cause rebound hypertension.
- Pregnancy category C.
PHARMACOKINETICS
Onset
Peak
Duration
2 weeks
Variable
48-96 h
ADVERSE EFFECTS
Common side effects are constipation, dry mouth, orthostatic hypotension, insomnia, nausea, and loss of appetite. It may increase heart rate and neural activity, leading to delirium, mania, anxiety, and convulsions. Severe hypertension may occur when ingesting foods containing tyramine. Seizures, respiratory depression, circulatory collapse, and coma may occur in cases of severe overdose.
Black Box Warning: Antidepressants increase the risk of suicidal thinking and behavior, especially in children, adolescents, and young adults with major depressive disorder and other psychiatric disorders.
Contraindications: Patients with cardiovascular or cerebrovascular disease, hepatic or renal impairment, and pheochromocytoma should not use this drug.
INTERACTIONS
Drug-Drug: Many drugs affect the action of phenelzine. Concurrent use of TCAs and SSRIs should be avoided because the combinations can cause temperature elevation and seizures. Opiates, should be avoided due to increased risk of respiratory failure or hypertensive crisis. Sympathomimetics may precipitate a hypertensive crisis. Caffeine may result in cardiac dysrhythmias and hypertension.
Lab Tests: Phenelzine can produce a slightly false increase in serum bilirubin. Because platelet functioning can be affected, careful attention should be devoted to complete blood count (CBC) results.
Herbal/Food: Concurrent use of ginseng may cause headaches, tremors, mania, insomnia, irritability, and visual hallucinations. Concurrent use of ma huang, ephedra, or St. John’s wort may result in a hypertensive crisis.
Treatment of Overdose: Intensive symptomatic and supportive treatment may be required. Induction of emesis or gastric lavage with instillation of charcoal slurry may be helpful. Signs and symptoms of CNS stimulation, including seizures, should be treated with IV diazepam, given very slowly. Hypertension should be treated appropriately with calcium channel blockers. Hypotension and vascular collapse should be treated with IV fluids and, if necessary, blood pressure titration with an IV infusion of a dilute pressor agent. Body temperature should be monitored closely, and respiration should be supported with appropriate measures.
lithium (Eskalith) page 202
Therapeutic Class: Mood stabilizing drug; bipolar affective disorder drug
Pharmacologic Class: Glutamate inhibitor; serotonin receptor antagonist
ACTIONS AND USES
Although the exact mechanism of action is not clear, lithium has been thought to alter ionic activity and the activities of neurons containing dopamine, norepinephrine, and serotonin by influencing their release, synthesis, and reuptake. More recent studies suggest that lithium may inhibit the action of glutamate, an excitatory neurotransmitter in the synapse. Other promising information indicates that serotonin at the receptor may be blocked and that glycogen synthase kinase-3 beta may be inhibited within the neuron. These actions tend to stabilize a wider range of cellular transduction pathways. Therapeutic actions are stabilization of mood during periods of mania and antidepressant effects during periods of depression. Lithium has neither antimanic nor antidepressant properties in individuals who do not have bipolar disorder. After taking lithium for 2 to 3 weeks, patients should be able to better concentrate and function in self-care.
ADMINISTRATION ALERTS
- Lithium has a narrow therapeutic/toxic ratio; the risk of toxicity is high.
- Acute overdosage may be treated by hemodialysis.
- Pregnancy category D.
PHARMACOKINETICS
Onset
Peak
Duration
5-7 days
10-21 days
Variable
ADVERSE EFFECTS
Lithium may cause dizziness, fatigue, short-term memory loss, increased urination, nausea, vomiting, loss of appetite, abdominal pain, diarrhea, dry mouth, muscular weakness, and slight tremors. Patients should not have a salt-free diet when taking this drug, because it reduces lithium excretion.
Black Box Warning: Toxicity is closely related to therapeutic serum concentrations; therefore, caution is warranted in terms of identifying prompt and accurate lithium serum concentrations.
Contraindications: This drug is contraindicated in debilitated patients and patients with severe cardiovascular disease, dehydration, or renal disease, and in cases of severe sodium depletion.
INTERACTIONS
Drug-Drug: Some drugs increase the rate at which the kidneys remove lithium from the bloodstream, including diuretics, sodium bicarbonate, and potassium citrate. Other drugs, such as methyldopa and probenecid, inhibit the rate of lithium excretion. Diuretics enhance excretion of sodium and increase the risk of lithium toxicity. Concurrent administration of anticholinergic drugs can cause urinary retention that, coupled with the polyuria effect of lithium, may cause a medical emergency. Alcohol can potentiate drug action.
Lab Tests: Unknown.
Herbal/Food: Unknown.
Treatment of Overdose: There is no specific treatment for overdose. Treatment is supportive, including gastric lavage, correction of fluid and electrolyte imbalance, and regulation of renal functioning. Hemodialysis is an effective and rapid means of removing the ion from the severely toxic patient; however, recovery time may be prolonged.
methylphenidate (Ritalin) page 205
Therapeutic Class: Attention deficit-hyperactivity disorder drug
Pharmacologic Class: CNS stimulant
ACTIONS AND USES
Methylphenidate activates the reticular activating system, causing heightened alertness in various regions of the brain, particularly those centers associated with focus and attention. Activation is partially achieved by the release of neurotransmitters such as norepinephrine and dopamine. Impulsiveness, hyperactivity, and disruptive behavior are usually reduced within a few weeks. These changes promote improved psychosocial interactions and academic performance. A transdermal, extended-release form of methyphenidate was approved in 2006 (Daytrana).
ADMINISTRATION ALERTS
- Sustained-release tablets must be swallowed whole. Breaking or crushing SR tablets causes immediate release of the entire dose.
- Controlled substance: Schedule II drug.
- Pregnancy category C.
PHARMACOKINETICS
Onset
Peak
Duration
Less than 60 min
2 h; 3-8 sustained release
3-6 h; 8 h sustained release; 8-12 h extended release
ADVERSE EFFECTS
In a non-ADHD patient, methylphenidate causes nervousness and insomnia. All patients are at risk for irregular heartbeat, high blood pressure, and liver toxicity. Because methylphenidate is a Schedule II drug, it has the potential for causing dependence when used for extended periods. Periodic drug-free “holidays” are recommended to reduce drug dependence and to assess the patient’s condition.
Black Box Warning: Methylphenidate is a Schedule II drug with high abuse potential. Administration for longer periods of time may lead to drug dependence. Misuse may cause sudden death or a serious cardiovascular adverse event.
Contraindications: Patients with a history of marked anxiety, agitation, psychosis, suicidal ideation, glaucoma, motor tics, or Tourette’s disease should not use this drug.
INTERACTIONS
Drug-Drug: Methylphenidate interacts with many drugs. For example, it may decrease the effectiveness of anticonvulsants, anticoagulants, and guanethidine. Concurrent therapy with clonidine may increase adverse effects. Antihypertensives or other CNS stimulants could potentiate the vasoconstrictive action of methylphenidate. MAOIs may produce hypertensive crisis.
Lab Tests: Unknown.
Herbal/Food: Administration times relative to meals and meal composition may need individual titration.
Treatment of Overdose: There is no specific treatment for overdose. Signs and symptoms of acute overdose result principally from overstimulation of the CNS and from excessive sympathomimetic effects. Emergency medical attention and general supportive measures may be necessary.
risperidone (Risperdal)
Therapeutic Class: Atypical antipsychotic; schizophrenia drug
Pharmacologic Class: D2 dopamine receptor antagonist (weaker affinity for D1 receptors); serotonin (5-HT) receptor antagonist
ACTIONS AND USES
Therapeutic effects of risperidone include treatment and prevention of schizophrenia relapse and expression of bipolar mania symptoms. Risperidone also treats symptoms of irritability in children with autism. Expected results are a reduction of excitement, paranoia, or negative behaviors associated with psychosis. Effects occur primarily from blockade of dopamine type 2, serotonin type 2, and alpha2-adrenergic receptors located within the CNS. For a full range of effectiveness, the drug is sometimes combined with lithium (Eskalith) or valproate (Depakene, Depacon). Risperidone is a long-acting preparation, which, following IM administration, releases only a small amount. After a 3-week lag, the rest of the drug releases and lasts for approximately 4-6 weeks. PO preparations release sooner and have a 1-2 week onset of action.
ADMINISTRATION ALERTS
- Several weeks are required for therapeutic effectiveness.
- When switching from other antipsychotics, discontinue medications to avoid overlap.
- Pregnancy category C.
PHARMACOKINETICS
Onset
Peak
Duration
1-2 wk PO; 3 wk IM
4-6 wk
6 wk
ADVERSE EFFECTS
Common adverse effects are extrapyramidal symptoms (involuntary shaking of the head, neck, and arms), hyperactivity, fatigue, nausea, dizziness, visual disturbances, fever, and orthostatic hypotension. Risperidone may cause weight gain and hyperglycemia, thus worsening glucose control in diabetic patients.
Black Box Warning: Elderly patients with dementia-related psychosis are at increased risk for death when taking atypical antipsychotics.
Contraindications: If older adults with dementia-related psychoses are given risperidone, they are at an increased risk for heart failure, pneumonia, or sudden death. Patients with underlying cardiovascular disease may be especially prone to dysrhythmias and hypotension. Risperidone should be avoided in patients with a history of seizures, suicidal ideations, or kidney/liver disease.
INTERACTIONS
Drug-Drug: Patients taking risperidone should avoid CNS depressants such as alcohol, antihistamines, sedative-hypnotics, or opioid analgesics. These can increase some of the adverse effects of risperidone. Due to inhibition of liver enzymes, other drugs that increase adverse effects of risperidone include selective serotonin reuptake inhibitors (SSRIs) such as paroxetine (Paxil), sertraline (Zoloft), and fluoxetine (Prozac) and antifungal drugs such as fluconazole (Diflucan), itraconazole (Sporanox), and ketoconazole (Nizoral). Risperidone may interfere with elimination by the kidneys of clozapine (Clozaril), which also increases the risk of adverse reactions.
Lab Tests: Risperidone may cause increased serum prolactin levels and increased ALT (alanine aminotransferase) and AST (aspartate aminotransferase) liver enzyme levels. Other potential lab changes are anemia, thrombocytopenia, leukocytosis, and leukopenia.
Herbal/Food: Use with caution with herbal supplements, such as kava, valerian, or chamomile, which may increase risperidone’s CNS depressive effects.
Treatment of Overdose: Activated charcoal, which may be used with sorbitol, may be as or more effective than emesis or gastric lavage, and should be considered in treating overdosage. Establish and maintain the airway; ensure adequate oxygenation and ventilation. Maintain cardiovascular function.
Valproic Acid (Depakene, Depakote)
Therapeutic Class: Antiseizure drug
Pharmacologic Class: Valproate
ACTIONS AND USES
The mechanism of action of valproic acid is widespread. It has the same action as that of phenytoin, although effects on GABA and calcium channels also make this drug similar to benzodiazepines and succinimides. It is useful for a wide range of seizure types, including absence seizures and mixed types of seizures. Other uses include prevention of migraine headaches and treatment of bipolar disorder.
ADMINISTRATION ALERTS
- Valproic acid is a gastrointestinal (GI) irritant. Advise patients not to chew extended-release tablets because mouth soreness will occur.
- Do not mix valproic acid syrup with carbonated beverages because they will trigger immediate release of the drug, which causes severe mouth and throat irritation.
- Open capsules and sprinkle on soft foods if the patient cannot swallow them.
- Pregnancy category D.
PHARMACOKINETICS
Onset
Peak
Duration
Readily absorbed from the GI tract
1-4 h
Variable
ADVERSE EFFECTS
Side effects include sedation, drowsiness, GI upset, and prolonged bleeding time. Other effects include visual disturbances, muscle weakness, tremor, psychomotor agitation, bone marrow suppression, weight gain, abdominal cramps, rash, alopecia, pruritus, photosensitivity, erythema multiforme, and fatal hepatotoxicity.
Black Box Warning: May result in fatal hepatic failure, especially in children under the age of 2 years. Nonspecific symptoms often precede hepatic toxicity: weakness, facial edema, anorexia, and vomiting. Liver function tests should be performed prior to treatment and at specific intervals during the first 6 months of treatment. Valproic acid can produce life-threatening pancreatitis and teratogenic effects including spina bifida.
Contraindications: Hypersensitivity may occur. This medication should not be administered to patients with liver disease, bleeding dysfunction, pancreatitis, and congenital metabolic disorders.
INTERACTIONS
Drug-Drug: Valproic acid interacts with many drugs. For example, aspirin, cimetidine, chlorpromazine, erythromycin, and felbamate may increase valproic acid toxicity. Concomitant warfarin, aspirin, or alcohol use can cause severe bleeding. Alcohol, benzodiazepines, and other CNS depressants potentiate CNS depressant action. Use of clonazepam concurrently with valproic acid may induce absence seizures. Valproic acid increases serum phenobarbital and phenytoin levels. Lamotrigine, phenytoin, and rifampin lower valproic acid levels.
Lab Tests: Unknown.
Herbal/Food: Unknown.
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