N215 Unit 5 Chapter 14 Drugs for Anxiety and Insomnia Flashcards
escitalopram oxalate (Lexapro)
Therapeutic Class: Antidepressant; anxiolytic
Pharmacologic Class: Selective serotonin reuptake inhibitor (SSRI)
ACTIONS AND USES
Escitalopram is a selective serotonin reuptake inhibitor (SSRI) that increases the availability of serotonin at specific postsynaptic receptor sites located within the CNS. Selective inhibition of serotonin reuptake results in antidepressant activity without production of symptoms of sympathomimetic or anticholinergic activity. This medication is indicated for conditions of generalized anxiety and depression. Off-label uses include the treatment of panic disorders.
ADMINISTRATION ALERTS
- This medication should not be started until 14 days have elapsed after discontinuing any MAOI drugs.
- In cases of renal or hepatic impairment or in older adults, reduced doses are advised.
- Dose increments should be separated by at least 1 week.
- Pregnancy category C.
PHARMACOKINETICS
Onset
Peak
Duration
With once-daily dosing, steady-state plasma concentrations can be reached within 1 wk
5 h
Variable
ADVERSE EFFECTS
Serious reactions include dizziness, nausea, insomnia, somnolence, confusion, and seizures if taken in overdose.
Black Box Warning: Antidepressants increase the risk of suicidal thinking and behavior in children, adolescents, and young adults with major depressive disorder and other psychiatric disorders.
Contraindications: This drug should not be used in patients who are breast-feeding or within 14 days of MAOI therapy.
INTERACTIONS
Drug-Drug: MAOIs should be avoided due to serotonin syndrome, marked by autonomic hyperactivity, hyperthermia, rigidity, diaphoresis, and neuroleptic malignant syndrome. Combination with MAOIs could result in hypertensive crisis, hyperthermia, and autonomic instability.
Escitalopram will increase plasma levels of metoprolol and cimetidine. Concurrent use of alcohol and other CNS depressants may enhance CNS depressant effects; patients should avoid alcohol when taking this drug.
Lab Tests: Unknown.
Herbal/Food: Use caution with herbal supplements such as St. John’s wort, which may cause serotonin syndrome and increase the effects of escitalopram.
Treatment of Overdose: There is no specific treatment for overdose. Treat symptoms, as indicated, including dizziness, confusion, nausea, vomiting, tremor, sweating, tachycardia, and seizures.
What drugs are used to treatment anxiety or insomnia?
ANTIDEPRESSANTS page 160 escitalopram oxalate (Lexapro) page 162
BENZODIAZEPINES page 163 lorazepam (Ativan) page 164
BARBITURATES page 164 phenobarbital (Luminal) page 179
NONBENZODIAZEPINE, NONBARBITURATE CNS DEPRESSANTS page 165 zolpidem (Ambien) page 166
Antiseizure Drugs page 166 valproic acid (Depakene, Depakote)
Beta Blockers page 166
atenolol (Tenormin)
propranolol (Inderal)
lorazepam (Ativan)
Therapeutic Class: Sedative-hypnotic; anxiolytic; anesthetic adjunct
Pharmacologic Class: Benzodiazepine; GABAA-receptor agonist
ACTIONS AND USES
Lorazepam is a benzodiazepine that acts by potentiating the effects of GABA, an inhibitory neurotransmitter, in the thalamic, hypothalamic, and limbic levels of the CNS. It is one of the most potent benzodiazepines. It has an extended half-life of 10 to 20 hours, which allows for once- or twice-a-day oral dosing. In addition to being used as an anxiolytic, lorazepam is used as a preanesthetic medication to provide sedation and for the management of status epilepticus. Unlabeled uses include the treatment of chemotherapy-induced nausea and vomiting.
ADMINISTRATION ALERTS
- When administering IV, monitor respirations every 5 to 15 minutes. Have airway and resuscitative equipment accessible.
- Pregnancy category D.
PHARMACOKINETICS
Onset
Peak
Duration
1-5 min IV; 15-30 min IM
2 h PO; 90 min IM
Variable
ADVERSE EFFECTS
The most common adverse effects of lorazepam are drowsiness and sedation, which may decrease with time. When given in higher doses or by the IV route, more severe effects may be observed, such as amnesia, weakness, disorientation, ataxia, sleep disturbance, blood pressure changes, blurred vision, double vision, nausea, and vomiting.
Contraindications: This drug should not be used in patients with acute narrow-angle glaucoma, primary depressive disorders, or psychosis, and should be avoided for the management of severe uncontrolled pain.
INTERACTIONS
Drug-Drug: Lorazepam interacts with multiple drugs. For example, concurrent use of CNS depressants, including alcohol, potentiates sedative effects and increases the risk of respiratory depression and death. Lorazepam may contribute to digoxin toxicity by increasing the serum digoxin level. Symptoms include visual changes, nausea, vomiting, dizziness, and confusion.
Lorazepam may decrease the antiparkinsonism effects of levodopa and increase phenytoin levels.
Lab Tests: Unknown.
Herbal/Food: Use cautiously with herbal supplements. For example, sedation-producing herbs such as kava, valerian, chamomile, or hops may have an additive effect with medication. Stimulant herbs such as gotu kola and ma huang may reduce the drug’s effectiveness.
Treatment of Overdose: If overdose occurs, flumazenil (Romazicon), a specific benzodiazepine receptor antagonist, can be administered to reverse CNS depressant effects.
phenobarbital (Luminal)
Therapeutic Class: Antiseizure drug (primary class); sedative
Pharmacologic Class: Barbiturate; GABAA receptor agonist
ACTIONS AND USES
Phenobarbital is a long-acting barbiturate used for the management of a variety of seizures. It is also used to promote sleep. Phenobarbital should not be used for pain relief, because it may increase a patient’s sensitivity to pain.
Phenobarbital acts biochemically by enhancing the action of the GABA neurotransmitter, which is responsible for suppressing abnormal neuronal discharges that can cause epilepsy.
ADMINISTRATION ALERTS
- Parenteral phenobarbital is a soft-tissue irritant. IM injections may produce a local inflammatory reaction. IV administration is rarely used, because extravasation may produce tissue necrosis.
- Controlled substance: Schedule IV.
- Pregnancy category D.
PHARMACOKINETICS
Onset
Peak
Duration
30-60 min PO; 15-30 min IV
1-2 h PO; 15 min IM; 1-5 min IV
2-3 h PO; 15-60 min IV
ADVERSE EFFECTS
Phenobarbital is a Schedule IV drug that may cause dependence. Common side effects include drowsiness, vitamin deficiencies (vitamin D; folate, or B9; and B12), and laryngospasms. With overdose, phenobarbital may cause severe respiratory depression, CNS depression, coma, and death.
Contraindications: Administration of phenobarbital is inadvisable in cases of hypersensitivity to barbiturates, severe uncontrolled pain, pre-existing CNS depression, porphyrias, severe respiratory disease with dyspnea or obstruction, and glaucoma or prostatic hypertrophy.
INTERACTIONS
Drug-Drug: Phenobarbital interacts with many other drugs. For example, it should not be taken with alcohol or other CNS depressants. These substances potentiate barbiturate action, increasing the risk of life-threatening respiratory depression or cardiac arrest. Phenobarbital increases the metabolism of many other drugs, reducing their effectiveness.
Lab Tests: Barbiturates may affect bromsulphalein tests and increase serum phosphatase.
Herbal/Food: Kava and valerian may potentiate sedation.
Treatment of Overdose: There is no specific treatment for overdose. Drug removal may be accomplished by gastric lavage or use of activated charcoal. Hemodialysis may be effective in facilitating removal of phenobarbital from the body. Treatment is supportive and consists mainly of endotracheal intubation and mechanical ventilation. Treatment of bradycardia and hypotension may be necessary.
zolpidem (Ambien)
Therapeutic Class: Sedative-hypnotic
Pharmacologic Class: Nonbenzodiazepine GABAA receptor agonist; nonbenzodiazepine, nonbarbiturate CNS depressant
ACTIONS AND USES
Although it is a nonbenzodiazepine, zolpidem acts in a similar fashion to facilitate GABA-mediated CNS depression in the limbic, thalamic, and hypothalamic regions. It preserves stages III and IV of sleep and has only minor effects on REM sleep. The only indication for zolpidem is for short-term insomnia management (7 to 10 days).
ADMINISTRATION ALERTS
- Because of rapid onset, 7-27 minutes, give immediately before bedtime.
- Pregnancy category B.
PHARMACOKINETICS
Onset
Peak
Duration
7-27 min
0.5-2.3 h
6-8 h
ADVERSE EFFECTS
Adverse effects include daytime sedation, confusion, amnesia, dizziness, depression, nausea, and vomiting.
Contraindications: Lactating women should not take this drug.
INTERACTIONS
Drug-Drug: Drug interactions with zolpidem include an increase in sedation when used concurrently with other CNS depressants, including alcohol. Phenothiazines augment CNS depression.
Lab Tests: Unknown.
Herbal/Food: When taken with food, absorption is slowed significantly, and the onset of action may be delayed.
Treatment of Overdose: Generalized symptomatic and supportive measures should be applied with immediate gastric lavage where appropriate. IV fluids should be administered as needed. Use of flumazenil (Romazicon) as a benzodiazepine receptor antagonist may be helpful.
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.
Copyright © 2014 by Pearson Education, Inc. All rights reserved.
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atenolol (Tenormin)
Therapeutic Class: Antianginal drug
Pharmacologic Class: Beta-adrenergic blocker
ACTIONS AND USES
Atenolol is one of the most frequently prescribed drugs in the United States due to its relative safety and effectiveness in treating a number of chronic disorders, including HF, hypertension, angina, and MI. The drug selectively blocks beta1-adrenergic receptors in the heart. Its effectiveness in treating angina is attributed to its ability to slow heart rate and reduce contractility, both of which lower myocardial oxygen demand. As with other beta blockers, therapy generally begins with low doses, which are gradually increased until the therapeutic effect is achieved. Because of its 7- to 9-hour half-life, it may be taken once daily.
ADMINISTRATION ALERTS
- During IV administration, monitor ECG continuously; BP and pulse should be assessed before, during, and after the dose is administered.
- Assess pulse and BP before oral administration. Hold if the pulse is below 60 beats per minute or if the patient is hypotensive.
- Atenolol may precipitate bronchospasm in susceptible patients with initial doses.
- Pregnancy category D.
PHARMACOKINETICS
Onset
Peak
Duration
1 h
2-4 h
24 h
ADVERSE EFFECTS
Being a cardioselective beta1-adrenergic blocker, atenolol has few adverse effects on the lung. The most frequently reported adverse effects of atenolol include fatigue, weakness, bradycardia, and hypotension.
Black Box Warning: Abrupt discontinuation should be avoided in patients with ischemic heart disease; doses should be gradually reduced over a 1- to 2-week period. If angina worsens during the withdrawal period, the drug should be reinstituted.
Contraindications: Because atenolol slows heart rate, it should not be used in patients with severe bradycardia, atrioventricular (AV) heart block, cardiogenic shock, or decompensated HF. Due to its vasodilation effects, it is contraindicated in patients with severe hypotension.
INTERACTIONS
Drug-Drug: Concurrent use with CCBs may result in excessive cardiac suppression. Use with digoxin may slow AV conduction, leading to heart block. Concurrent use of atenolol with other antihypertensives may result in additive hypotension. Anticholinergics may cause decreased absorption from the gastrointestinal (GI) tract.
Lab Tests: Atenolol may increase values of the following blood tests: uric acid, lipids, potassium, creatinine, and antinuclear antibody.
Herbal/Food: Unknown.
Treatment of Overdose: The most serious symptoms of atenolol overdose are hypotension and bradycardia. Atropine or isoproterenol may be used to reverse bradycardia. Atenolol can be removed from the systemic circulation by hemodialysis.
Copyright © 2014 by Pearson Education, Inc. All rights reserved.
propranolol (Inderal)
Therapeutic Class: Class II antidysrhythmic
Pharmacologic Class: Beta-adrenergic antagonist
ACTIONS AND USES
Propranolol is a nonselective beta-adrenergic blocker, affecting beta1 receptors in the heart and beta2 receptors in pulmonary and vascular smooth muscle. Propranolol reduces heart rate, slows myocardial conduction velocity, and lowers BP. Propranolol is most effective in treating tachycardia that is caused by excessive sympathetic stimulation. It is approved to treat a wide variety of diseases, including HTN, angina, and migraine headaches, and for prevention of MI.
Propranolol has several off-label indications, including reducing portal HTN and bleeding due to esophageal varices, reducing the tachycardia, tremor, and nervousness associated with thyroid crisis (storm), panic attacks, post-traumatic stress disorder (PTSD), chronic agitation, aggressive behavior, and involuntary movements of essential tremor. The drug is available in tablet, extended-release capsules, and IV formulations. InnoPran XL is a long-acting form of the drug that has a timed delivery system designed for bedtime dosing, with a peak effect in the morning.
ADMINISTRATION ALERTS
- Abrupt discontinuation may cause MI, severe HTN, and ventricular dysrhythmias.
- Swallow extended-release tablets whole: Do not crush or chew contents.
- If pulse is less than 60 beats per minute, notify the health care provider.
- Pregnancy category C.
PHARMACOKINETICS (PO)
Onset
Peak
Duration
30-60 min PO
1-2 h (6 h extended release)
6-12 h
ADVERSE EFFECTS
Common adverse effects of propranolol include fatigue, hypotension, and bradycardia. Because of the ability of propranolol to slow the heart rate, patients with serious cardiac disorders such as HF must be carefully monitored. Adverse effects such as diminished libido and impotence may result in nonadherence in male patients. Propranolol should be used cautiously in patients with diabetes due to its hypoglycemic effects and because it may mask the symptoms of hypoglycemia as the adrenergic “fight-or-flight” to hypoglycemia is blocked. This drug should be used with caution in patients with reduced renal output, because the drug may accumulate to toxic levels in the blood and cause dysrhythmias.
Black Box Warning: Abrupt withdrawal is not advised in patients with angina or heart disease. Dosage should gradually be reduced over 1 to 2 weeks and the drug should be reinstituted if angina symptoms develop during this period.
Contraindications: Because of its depressive effects on the heart, propranolol is contraindicated in patients with cardiogenic shock, sinus bradycardia, greater than first-degree heart block, and HF. Because it constricts smooth muscle in the airways, the drug is contraindicated in patients with COPD or asthma.
INTERACTIONS
Drug-Drug: Concurrent administration with other beta blockers may produce additive effects on the heart, and bradycardia or hypotension may result. Because both propranolol and calcium channel blockers suppress myocardial contractility, their concurrent use may lead to additive bradycardia. Phenothiazines can add to the hypotensive effects of propranolol. Propranolol should not be given within 2 weeks of a monoamine oxidase (MAO) inhibitor, because severe bradycardia and hypotension could result. Use of ethanol or antacids containing aluminum hydroxide gel will slow the absorption of propranolol and reduce its therapeutic effects. Administration of beta-adrenergic agonists such as albuterol will antagonize the actions of propranolol.
Lab Tests: Propranolol may give a false increase for urinary catecholamines.
Herbal/Food: Unknown.
Treatment of Overdose: Treatment is targeted to reversing hypotension with vasopressors, and bradycardia with atropine or isoproterenol. Intravenous glucagon reverses the cardiac depression caused by beta blocker overdose by enhancing myocardial contractility, increasing heart rate, and improving AV node conduction.
