Names and pronunciation
(byoo-spye′rone)
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Drug reference
(byoo-spye′rone)
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Func. class.: Antianxiety, sedative
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Chem. class.: Azaspirodecanedione
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Do not confuse: busPIRone/buPROPion
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ACTION: Acts by inhibiting the action of serotonin (5-HT); has shown little potential for abuse; a good choice with substance abuse
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USES: Generalized anxiety disorders
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CONTRAINDICATIONS: Chil- dren <18 yr, hypersensitivity, MAOIs Precautions: Pregnancy, breastfeeding, geriatric patients, impaired hepatic/renal function
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SIDE EFFECTS CNS: Dizziness, headache, stimula- tion, insomnia, nervousness, numb- ness, paresthesia, incoordination CV: Tachycardia, palpitations, hypo/ hypertension, chest pain EENT: Sore throat, tinnitus, blurred vision, nasal congestion; change in taste, smell GI: Nausea, dry mouth, diarrhea, con- stipation, increased appetite GU: Frequency, hesitancy, change in libido INTEG: Rash, edema, pruritus, alopecia, dry skin MISC: Sweating, fatigue, fever MS: Pain, weakness, muscle cramps, myalgia RESP: Hyperventilation, chest conges- tion, shortness of breath
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INTERACTIONS Increase: busPIRone—CYP3A4 inhibitors (erythromycin, itraconazole, nefazodone, ketoconazole, ritonavir, verapamil, dilTIA- Zem, several other protease inhibitors), dosage decrease may be needed Increase: B/P—procarbazine, MAOIs; avoid using together Increase: CNS depression—psychotro- pic products, alcohol (avoid use), moni- tor closely if used together Increase: serotonin syndrome—SSRIs, SNRIs, serotonin receptor agonists Decrease: busPIRone effects—rifAMPin Decrease: busPIRone action—CYP3A4 inducers (rifAMPin, phenytoin, PHENo- barbital, carBAMazepine, dexametha- sone), dosage increase may be needed Drug/Herb Increase: CNS depression—chamomile, kava kava, valerian Drug/Food Increase: peak concentration of busPI- Rone—grapefruit juice
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DOSAGE AND ROUTES Anxiety disorders • Adult: PO 7.5 mg bid; may increase by 5 mg/day q2-3days, max 60 mg/day Hepatic/renal dose • Adult: PO Do not use in severe renal/ hepatic disease
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Available forms: Tablets 5, 7.5, 10, 15, 30 mg
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Administer: B • With food, milk for GI symptoms; avoid grapefruit juice; give drug at same time of day, with/without food consistently • Crushed if patient unable to swallow medication whole • Sugarless gum, hard candy, frequent sips of water for dry mouth
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Assess: • B/P lying, standing; pulse; if systolic B/P drops 20 mm Hg, hold product, no- tify prescriber • CNS reactions because some may be unpredictable • Mental status: mood, sensorium, af- fect, sleeping pattern, drowsiness, dizzi- ness; withdrawal symptoms when dose reduced, product discontinued • Safety measures if drowsiness, dizzi- ness occurs • Beers: avoid in older adults with de- lirium or at high risk for delirium
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Evaluate: • Therapeutic response: decreased anxi- ety, restlessness, sleeplessness
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • That product may be taken consis- tently with/without food • To avoid OTC products, alcohol inges- tion, other psychotropic medications un- less approved by prescriber; to avoid large amounts of grapefruit juice • To avoid activities that require alert- ness because drowsiness may occur • Not to discontinue medication abruptly after long-term use; if dose is missed, do not double • To rise slowly because fainting may occur, especially among geriatric patients • That drowsiness may worsen at begin- ning of treatment; that 2 wk of therapy may be required before therapeutic ef- fects occur, max effect 3-6 wk • Serotonin syndrome: to report imme- diately (fever, tremor, sweating, diarrhea, delirium) • Pregnancy/breastfeeding: report if pregnancy is planned or suspected or if breastfeeding, use in pregnancy and breastfeeding isn’t recommended HIGH ALERT
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PHARMACOKINETICS Onset, duration unknown; Peak 40-90 min, half-life 2-4 hr, rapidly absorbed, metabolized by liver (CYP3A4), excreted in feces, protein binding 86%
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• Adult: PO 7.5 mg bid; may increase by 5 mg/day q2-3days, max 60 mg/day Hepatic/renal dose
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• Adult: PO Do not use in severe renal/ hepatic disease
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