Anti-Anxiety Drugs – Flashcards

benzodiazepine to relieve anxiety. Buspirone (BuSpar) is another anxiolytic medication (non-benzo). It is significantly different from benzodiazepines in that it is not a central nervous system (CNS) depressant. Mechanism of Action: Depresses all levels of the CNS; depresses nerve impulse transmission in the motor cortex Suppresses abnormal discharge in petit mal seizures Onset of benefits is immediate, and the margin of safety is high Therapeutic Effects: Produces anxiolytic, anticonvulsant effects

well absorbed from the GI tract, metabolized in the liver, and excreted in the urine. It is not removed by hemodialysis.

Route Onset Peak Half-Life Duration PO 20-60 minutes Unknown 18-50 hrs 12 hours or less

Buspirone is a drug in a class of its own that is used for the short-term treatment of anxiety. If a patient is switching from a benzodiazepine to buspirone, then buspirone should be initiated 2-4 weeks before the patient weans from the benzodiazepine.

Buspirone's mechanism of action as an anxiolytic is not well understood. It binds with high affinity to serotonin receptors and, to a lesser degree, dopamine receptors. It does not depress the CNS.

Buspirone is as effective as benzodiazepines are in the treatment of anxiety. However, buspirone has both advantages and disadvantages. Advantages: No abuse potential (may be especially appropriate for patients who abuse drugs or alcohol) Does not intensify the effects of CNS depressants (benzodiazepines, alcohol, barbituates) Disadvantages: Anxiolytic effects develop slowly (over 2-3 weeks) Not suitable for PRN use or when immediate relief is needed Although buspirone is labeled only for short-term treatment of anxiety, it can be taken for as long as a year with no reduction in benefit. Buspirone does not display cross-dependence with benzodiazepines.

Buspirone is well absorbed in the GI tract but undergoes extensive metabolism on its first pass through the liver. While administration with food delays absorption, it enhances the bioavailability by reducing first-pass metabolism. It is excreted in part by the kidneys, primarily as metabolites.

Route Onset Peak Elimination Half-Life Duration PO 2-3 week 40-60 minutes 2-3 hours Unknown

Buspirone is used for the short-term treatment of anxiety.

Benzodiazepines The major anxiolytic group is benzodiazepines. Benzodiazepines are the first-choice drugs for management of anxiety. Benzodiazepines are considered more effective than barbiturates.

Limbic Benzodiazepines work by depressing activity in the area of the brain known as the limbic system and in the brainstem.

2-3 weeks The initial response to buspirone takes 2-3 weeks to appear, and several more weeks must pass before the response peaks.

It is not a CNS depressant. Buspirone is not a central nervous system (CNS) depressant like other anxiolytics.

Because clonazepam is also used to treat seizure disorders, the nurse should assess the patient for a history of seizures prior to administration. The nurse should assess motor responses (e.g., agitation, trembling, tension) and autonomic responses (e.g., cold/clammy hands, diaphoresis) when clonazepam is given for a panic disorder.

Contraindications: Narrow-angle glaucoma, severe hepatic disease, pregnancy Cautions: Renal/hepatic impairment, impaired gag reflex, chronic respiratory disease, older adult patients, debilitated patients, depression, patients at risk for suicide or drug dependence ------------- Drug: Alcohol and other CNS depressants may increase CNS depressant effect CYP3A4 inhibitors (e.g., azole antifungals) may increase concentration, toxicity Herbal: Gotu kola, kava kava, SAMe, St. John's wort, and valerian may increase CNS depression St. John's wort may decrease concentration/effects Food: Grapefruit and grapefruit juice alter drug metabolism via inhibition of the cytochrome P450 system, which can result in prolonged effect, increased effect, and toxicity

PO May be taken without regard to food Should be swallowed whole with water Orally Disintegrating Tablet Open pouch, peel back foil; do not push tablet through foil Remove tablet with dry hands, place in mouth Swallow with or without water Use immediately after removing from package Panic Disorder PO: Adults, older adults Initially, 0.25 mg twice a day. Increase by increments of 0.125-0.25 mg every 3 days. Target dose: 1 mg/day. Maximum dose: 4 mg/day

Clonazepam should not be abruptly stopped. Adverse effects are primarily related to clonazepam's effects on the CNS. Abrupt withdrawal can result in pronounced restlessness, irritability, insomnia, hand tremors, abdominal/muscle cramps, diaphoresis, vomiting, and/or status epilepticus. Overdose can result in drowsiness, confusion, diminished reflexes, and/or coma. The antidote for clonazepam is flumazenil by intravenous injection.

Successful treatment with clonazepam is evidenced by absence of seizures (if prescribed for seizure disorder) or calm demeanor and decreased restlessness (if prescribed for anxiety). When evaluating the patient, the nurse should do the following: Observe for excess sedation, respiratory depression, and/or suicidal ideation Assess children and older adults for paradoxical reactions, particularly during early therapy Initiate seizure precautions and observe frequently for recurrence of seizure activity Assist with ambulation if drowsiness or ataxia occurs For patients on long-term therapy, obtain liver and renal function tests, renal function tests; perform blood counts periodically

Prior to the administration of buspirone, the nurse should assess the degree and manifestations of anxiety. Offer emotional support by listening, making eye contact, conveying warmth and understanding in speech, and reflecting back to the patient what was said. Assess motor responses (e.g., agitation, trembling, tension). Assess autonomic responses (e.g., cold/clammy hands, diaphoresis).

The only reported contraindication is drug allergy. Cautions: Severe hepatic/renal impairment (not recommended), concurrent use of MAOIs (MAOIs should be discontinued at least 2 weeks prior to starting buspirone) Drug: CYP3A4 inhibitors (e.g., erythromycin, ketoconazole) may increase concentration/effect CYP3A4 inducers (e.g., rifampin) may decrease concentration/effect May increase effects of MAOIs Food: Grapefruit products may increase concentration, risk of toxicity Lab Values: May produce false positive urine metanephrine/catecholamine assay test

Buspirone tablets (BuSpar) are available in five strengths: 5-, 7.5-, 10-, 15-, and 30-mg. The initial dosage is 7.5 mg 2 times a day. Dosage may be increased to a maximum of 60 mg/day, titrated every 2 to 3 days by 5 mg over a 3-week period. PO Give without regard to food. Short-Term Management (Up to 4 weeks) of Anxiety Disorders PO: Adults: 7.5 mg twice a day. May increase by 5 mg/day every 2-4 days. Maintenance: 15-30 mg/day in 2-3 divided doses. Maximum: 60 mg/day.

Buspirone is usually well tolerated and has few adverse effects. The most common side effects include: Dizziness Nausea Headache Nervousness Sedation Lightheadedness Excitement There is little or no risk of suicide associated with buspirone. Large doses (up to 375 mg/day) have been given with only moderate adverse effects.

Buspirone therapy is determined to be effective when the patient experiences decreased anxiety as evidenced by a calm facial expression, decreased restlessness, lessened insomnia, and improved mental status. For patients on long-term therapy, complete blood counts and hepatic/renal function tests should be performed periodically. Assist with ambulation if drowsiness or dizziness occurs.

Children and older adults Paradoxical reactions (reactions opposite of those that would normally be expected) rarely occur with benzodiazepines, but are more likely to occur in children and older adults.

Alcohol Use of alcohol with benzodiazepines can result in additive CNS depression and even death.

Patients with a known drug allergy The only reported contraindication is a known drug allergy to Buspirone.

14 days A waiting period of at least 14 days must be allowed after discontinuation of MAOI therapy before buspirone is started due to risk of serotonin syndrome.

Patient teaching about benzodiazepines should focus on CNS effects, other adverse effects, and prevention of drug-drug interactions.

Advise the patient not to drive a motor vehicle or operate dangerous equipment when taking benzodiazepines, because sedation is a common side effect. Teach the patient ways to control excess stress and anxiety (e.g., relaxation techniques, long walks). Inform the patient that effective response may take 1 to 2 weeks. Encourage the patient to follow the drug regimen and not to abruptly stop taking the drug after prolonged use because withdrawal symptoms can occur. The drug dose is usually tapered when the drug is discontinued. Educate the patient about the development of tolerance to the sedating properties of benzodiazepines with chronic use. Instruct the patient to keep these and all psychotherapeutic drugs out of the reach of children. Advice the patient to carry a medical alert or other identification bracelet/necklace with his or her diagnoses and a list of drugs and allergies at all times. The drug list needs to be updated at least every 3 months. Instruct the patient to report depression, thoughts of suicide/self-harm, excessive drowsiness, GI symptoms, and worsening or loss of seizure control.

Warn the patient not to consume alcohol or other CNS depressants such as narcotics while taking an anxiolytic. Other CNS depressants can increase the effects of clonazepam. Teach the patient to avoid grapefruit juice, as it may affect the absorption of clonazepam. Instruct the patient not to take over-the-counter drugs or herbals without seeking advice from the prescriber. -------------- Encourage the patient to rise slowly from a sitting to a standing position to avoid dizziness from orthostatic hypotension. Educate the patient about types of effects that may occur: Frequent (37%-11%): Mild, transient drowsiness, ataxia, behavioral disturbances (aggression, irritability, agitation), esp. in children Occasional (10%-5%): Dizziness, ataxia, URI, fatigue Rare (4% or less): Impaired memory, dysarthria, nervousness, sinusitis, rhinitis, constipation, allergic reaction

Buspirone is generally well tolerated and has few side effects, but the nurse should provide the patient with the following information and instruction about the medication: Improvement may be noted in 7-10 days, but optimum therapeutic effect generally takes 3-4 weeks. Drowsiness usually disappears during continued therapy. Dizziness may occur, so transitioning slowly from lying to standing is recommended. Tasks that require alertness and the use of motor skills should be avoided until a response to the drug is established. Alcohol and grapefruit products should not be consumed when taking this medication. Severe renal and hepatic impairment can occur if Buspirone is taken with an MAOI.

The patient's culture, values, and beliefs should be taken into consideration when teaching about anxiolytics. In many cultures, mental health disorders are not discussed openly. Use simple and clear instructions, and modify methods and materials to meet patient and family needs. Ask family members to assist with translation only if an interpreter is not available, and do not ask private questions in public.

Ms. Gamez is a 35-year-old female who presents to the clinic with complaints of increasing anxiety and panic attacks. She states that they come on suddenly and without warning. Ms. Gamez has no medical history and is recently divorced. She states that her job is causing her a lot of stress in addition to the stress from dealing with the divorce. The health care provider refers Ms. Gamez for psychotherapy and prescribes buspirone 7.5 mg po BID.

Take long walks Teach the patient ways to control excess stress and anxiety by using relaxation techniques, such as taking long walks.

Suicidal thoughts Suicidal thoughts need to be reported immediately to a health care professional to avoid patient self harm. Suicidal thoughts can be an indication that therapy is not effective and the patient is unable to cope with the stressors of life.

"It will take 3-4 weeks for you to feel the full effect of this medication." It usually takes 3-4 weeks for the optimum therapeutic effect of buspirone.

Anxiety is a common mental health disorder in the United States. Treatments for anxiety include psychotherapy and drug therapy, with most people responding best to a combination of both. Drug therapy for anxiety disorders includes benzodiazepines, buspirone, and some antidepressants. Benzodiazepines are the first-choice drugs for anxiety, but they can cause excessive CNS depression. Buspirone is in a class of its own and has few adverse effects; however, it is for short-term use only. Patients taking anxiolytics should be warned about the possibility of increased CNS depression that can occur when the medications are combined with alcohol and narcotics.

Hold the medication and verify the order with the health care provider Because its therapeutic effects are delayed, buspirone is not suitable for PRN use or for patients who need immediate relief.

Blood pressure When taken orally, benzodiazepines have almost no effect on the heart and blood vessels. In contrast, when administered intravenously—even in therapeutic doses—benzodiazepines can produce profound hypotension and cardiac arrest.

Avoid abrupt cessation of treatment. Patients should be warned against abrupt cessation of treatment so that the intensity of withdrawal symptoms can be minimized by discontinuing treatment gradually. Doses should be slowly tapered over several weeks or months.

Buspirone Since buspirone has no abuse potential, it may be especially appropriate for patients known to abuse alcohol and/or other drugs.

Grapefruit juice Buspirone should not be taken with grapefruit juice because toxicity can occur.

"I need to start taking the buspirone 2-4 weeks before I start slowly decreasing my clonazepam." Buspirone does not display cross-dependence with benzodiazepines. Since the effects of buspirone are delayed, buspirone should be initiated 2-4 weeks before benzodiazepine withdrawal begins. When patients are switched from a benzodiazepine to buspirone, the benzodiazepine must be tapered slowly.

Flumazenil An overdose of benzodiazepines may result in any of the following symptoms: somnolence, confusion, and respiratory depression. Flumazenil is a benzodiazepine receptor blocker (antagonist) that is used to reverse the effects of benzodiazepines.

Benzodiazepine withdrawal When benzodiazepines are discontinued abruptly, withdrawal syndrome can follow. Symptoms include anxiety, insomnia, sweating, tremors, and dizziness. Withdrawal from long-term use can cause more serious reactions, such as panic, paranoia, delirium, hypertension, muscle twitches, and convulsions.

Respiratory depression Although benzodiazepines generally have minimal effects on respiration, in patients with COPD they may worsen hypoventilation and hypoxemia.

Call the health care provider to verify the route. Buspirone is only available as an oral medication. The medication should not be given intramuscularly.

Hold the erythromycin and notify the health care provider. Levels of buspirone can be greatly increased (5- to 13-fold) by erythromycin.

"This medication may make me dizzy; I will call for assistance when walking to the bathroom." Common side effects of buspirone include drowsiness, dizziness, headache, and nausea.

"Since I received this medication, I need to call my son to pick me up." Advise the patient refrain from driving a motor vehicle or operating dangerous equipment when taking anxiolytics, because sedation is a common side effect.

"Consult your health care provider before taking any herbal medications." Patients should consult with a health care provider prior to initiating herbal remedies while on anxiolytics due to the possibility of interactions.

"Did you have grapefruit juice with your breakfast?" Buspirone has an interaction with grapefruit juice that can lead to toxicity. Elevated levels of buspirone may cause drowsiness and subjective effects (dysphoria, feeling "spacey").