busPIRone (Rx)
Generic: BusPIRone
Brand: BuSpar, BuSpar Dividose, PMS- Buspirone
(bvo- spye'rone)
Pharmacological Action
Acts by inhibiting the action of serotonin (5- HT) by binding to serotonin and dopamine receptors; also increases norepinephrine metabolism; has shown little potential for abuse, a good choice in substance abuse
Therapeutic outcome: Decreased anxiety
Uses
Management and short- term relief of generalized anxiety disorders
Contraindications
Hypersensitivity, child < 18 yr
Precautions: Pregnancy B, breastfeeding, geriatric, impaired renal/hepatic function
Dosage & Routes
Adult: PO 7.5 mg tid; may increase by 5 mg/day q2- 3 days; max 60 mg/day Renal/hepatic dose:
Adult: PO reduce by 25% - 50% in mild to moderate hepatic disease, do not use in severe hepatic disease, Ccr 11- 70 ml/min reduce dose by 25% - 50%, Ccr < 10 ml/min do not use
Available forms: Tabs 5, 7.5, 10, 15, 30 mg
Implementation Give with food or milk for GI symptoms (avoid grapefruit juice); sugarless gum, hard candy, frequent sips of water for dry mouth May be crushed
Adverse Effects
CNS: Dizziness, headache, depression, stimulation, insomnia, nervousness, light- headedness, numbness, paresthesia, incoordination, tremors, excitement, involuntary movements, confusion, akathisia, nightmares, hostility
CV: Tachycardia, palpitations, hypo/hypertension, CVA, CHF, MI
EENT: Sore throat, tinnitus, blurred vision, nasal congestion, red, itching eyes, change in taste, smell
GI: Nausea, dry mouth, diarrhea, constipation, flatulence, increased appetite, rectal bleeding
GU: Frequency, hesitancy, menstrual irregularity, change in libido
INTEG: Rash, edema, pruritus, alopecia, dry skin
MISC: Sweating, fatigue, weight gain, fever, serotonin syndrome
MS: Pain, weakness, muscle cramps, spasms
RESP: Hyperventilation, chest congestion, shortness of breath
Pharmacokinetics
Absorption: Rapid
Distribution: Protein binding 86%
Metabolism: Liver, extensively
Excretion: Feces
Half-life: 2-3 hr
Pharmacodynamics
Onset: Unknown
Peak: 40-90 min
Duration: Unknown
Interactions
Individual drugs
Alcohol: increased CNS depression; avoid use
Drug classifications Products metabolized by CYP3 A4 (erythromycin, itraconazole, nefazodone, ketoconazole, ritonavir, several other protease inhibitors): increased busPIRone levels MAOIs, procarbazine: increased B/P, do not use together Products induced by CYP3 A4 (rifampin, phenytoin, PHENobarbital, carbAMazepine, dexamethasone): decreased busPIRone action
Psychotropics: increased CNS depression, avoid use Selective serotonin reuptake inhibitors (SNRIs, serotonin receptor agonists): increase serotonin syndrome
Drug/food Grapefruit juice: increased peak concentration of busPIRone
Nursing Considerations
Assessment - Assess anxiety reaction: inability to sleep, apprehension, dread, foreboding, or uneasiness related to unidentified source of danger - Assess for previous product dependence or tolerance; if patient is product dependent or tolerant, amount of medication should be restricted - Monitor B/P (lying, standing), pulse; if systolic B/P drops 20 mm Hg, hold product, notify prescriber; check I&O; may indicate renal dysfunction - Monitor mental status: mood, sensorium, affect, sleeping patterns, drowsiness, dizziness, suicidal tendencies; withdrawal symptoms when dose is reduced or product discontinued - Assess for CNS reaction, some reactions may be unpredictable
Patient/family education - Teach patient that product may be taken consistently with or without food; if dose is missed take as soon as remembered; do not double doses - Caution patient to avoid OTC preparations unless approved by the prescriber; to avoid alcohol ingestion and other psychotropic medications unless prescribed; that 1- 2 wk of therapy may be required before therapeutic effects occur; to avoid large amounts of grapefruit juice - Caution patient to avoid driving and activities requiring alertness since drowsiness may occur; until medication response is known, tell patient that drowsiness may worsen at beginning of treatment - Instruct patient not to discontinue medication abruptly after long- term use; if dose is missed, do not double - Advise patient to rise slowly or fainting may occur, especially in geriatric Serotonin syndrome: Teach patient to report immediately (fever, tremor, sweating, diarrhea, delirium)
Evaluation
Positive therapeutic outcome: Increased well- being, Decreased anxiety, restlessness, sleeplessness, dread
Reference
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