BusPIRone (Lexi-Drugs)

Drug Shortages

One or more forms of this drug may be in short supply or unavailable. Refer to the following for additional information:

ASHP: http://www.ashp.org/menu/DrugShortages

FDA: https://www.accessdata.fda.gov/scripts/drugshortages/dsp_ActiveIngredientDetails.cfm?AI=Buspirone+HCl+Tablets&st=c&tab=tabs-4&panels=0

Pronunciation

(byoo SPYE rone)

Brand Names: Canada

APO-BusPIRone; CO BusPIRone; DOM-BusPIRone; GMD-Buspirione; NU-BusPIRone [DSC]; PMS-BusPIRone; RIVA-BusPIRone; TEVA-BusPIRone

Pharmacologic Category

Antianxiety Agent, Miscellaneous

Dosing: Adult

Note: Periodically assess the usefulness of the drug for the individual patient.

Generalized anxiety disorder: Oral: Initial: 10 to 15 mg/day in 2 to 3 divided doses; may increase every 2 to 3 days in increments of 5 mg/day to a maximum of 60 mg/day; usual dose: 20 to 30 mg/day in 2 to 3 divided doses (Chessick 2006; Sramek 1999).

Unipolar depression, augmentation (alternative agent following antidepressant switch and other augmentation agents) (off-label use): Oral: Initial: 15 to 20 mg/day in 2 divided doses; may increase every 3 to 7 days in increments of 10 to 15 mg/day to a maximum of 60 mg/day in 2 divided doses (APA 2010; Appelberg 2001; Trivedi 2006).

Dosing: Geriatric

Refer to adult dosing.

Dosing: Renal Impairment: Adult

Mild to moderate impairment: There are no dosage adjustments provided in the manufacturer’s labeling; use with caution (these patients demonstrated increased plasma levels and a prolonged half-life of buspirone).

Severe impairment: Use not recommended.

Dosing: Hepatic Impairment: Adult

Mild to moderate impairment: There are no dosage adjustments provided in the manufacturer’s labeling; use with caution (these patients demonstrated increased plasma levels and a prolonged half-life of buspirone).

Severe impairment: Use not recommended.

Dosing: Pediatric

Anxiety disorders: Children and Adolescents: Oral: Limited information is available; dose is not well established. One pilot study of 15 children, 6-14 years of age (mean 10 years), with mixed anxiety disorders, used initial doses of 5 mg daily; doses were individualized with increases in increments of 5 mg/day every week as needed to a maximum dose of 20 mg/day divided into 2 doses; the mean dose required: 18.6 mg/day (Simeon, 1994). Some authors (Carrey, 1996 and Kutcher, 1992), based on their clinical experience, recommend higher doses (eg, 15-30 mg/day in 2 divided doses). An open-label study in 25 prepubertal inpatients (mean age: 8 ± 1.8 years; range: 5-11 years) with anxiety symptoms and moderately aggressive behavior used initial doses of 5 mg daily; doses were titrated upwards (over 3 weeks) by 5-10 mg every 3 days to a maximum dose of 50 mg/day; doses >5 mg/day were administered in 2 divided doses/day; buspirone was discontinued in 25% of the children due to increased aggression and agitation or euphoric mania; mean optimal dose (n=19): 28 mg/day; range: 10-50 mg/day; median: 30 mg/day (Pfeffer, 1997). Two placebo-controlled 6-week trials in children and adolescents (n=559; age: 6-17 years) with generalized anxiety disorder studied doses of 7.5-30 mg twice daily (15-60 mg/day); no significant differences between buspirone and placebo with respect to generalized anxiety disorder symptoms were observed (see package insert).

Dosing: Renal Impairment: Pediatric

Patients with impaired renal function demonstrated increased plasma levels and a prolonged half-life of buspirone. Use in patients with severe renal impairment not recommended.

Dosing: Hepatic Impairment: Pediatric

Patients with impaired hepatic function demonstrated increased plasma levels and a prolonged half-life of buspirone. Use in patients with severe hepatic impairment not recommended.

Use: Labeled Indications

Generalized anxiety disorder: Management of generalized anxiety disorder or the short-term relief of the symptoms of anxiety

Use: Off-Label: Adult

  Unipolar depression, augmentationLevel of Evidence [B, G]

Data from two randomized controlled trials in patients with nonpsychotic major depressive disorder without remission despite treatment with an SSRI (ie, citalopram and fluoxetine) support the use of buspirone as an augmentation strategy in the treatment of this condition. However, in comparison to bupropion, patients receiving buspirone had more adverse effects and less improvement in symptoms Ref. Additional trials may be necessary to further define the role of buspirone in this condition.

Based on the American Psychiatric Association (APA) practice guideline for the treatment of patients with major depressive disorder, buspirone (added to an SSRI) is an effective augmentation strategy for this condition.

Level of Evidence Definitions
  Level of Evidence Scale
Clinical Practice Guidelines

Depression:

American Psychiatric Association, Practice Guideline for the Treatment of Patients with Major Depressive Disorder, Third Edition, May 2010

Administration: Oral

Administered with or without food, but must be consistent.

Administration: Pediatric

Oral: Administer in a consistent manner in relation to food (ie, either always with food or always without food); may administer with food to decrease GI upset

Dietary Considerations

Avoid large quantities of grapefruit juice.

Storage/Stability

Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C to 30°C (59°F to 86°F). Protect from light.

Medication Patient Education with HCAHPS Considerations

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience fatigue, dizziness, anxiety, headache, or nausea. Have patient report immediately to prescriber signs of serotonin syndrome (dizziness, severe headache, agitation, hallucinations, tachycardia, abnormal heartbeat, flushing, tremors, sweating a lot, change in balance, severe nausea, or severe diarrhea), agitation, abnormal movements, twitching, change in balance, difficulty speaking, or difficulty swallowing (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

Medication Safety Issues
  Sound-alike/look-alike issues:
Contraindications

Hypersensitivity to buspirone or any component of the formulation; concomitant use of MAOIs intended to treat depression or within 14 days of discontinuing MAOIs intended to treat depression; concomitant use of MAOIs within 14 days of discontinuing buspirone; initiation of buspirone in patients receiving reversible MAOIs (eg, linezolid, IV methylene blue).

Warnings/Precautions

Concerns related to adverse effects:

• Akathisia: Akathisia, or restlessness, has been reported in small number of patients; may be a result of central dopamine receptor antagonism. Monitor for signs of any dopamine-related movement disorders (eg, dystonia, akathisia, pseudo-parkinsonism, tardive dyskinesia).

• CNS depression: May rarely cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks that require mental alertness (eg, operating machinery or driving).

• Serotonin syndrome: Potentially life-threatening serotonin syndrome has occurred with serotonergic agents, including buspirone, particularly when used in combination with other serotonergic agents (eg, triptans, TCAs, fentanyl, lithium, tramadol, buspirone, St John’s wort, tryptophan) or agents that impair metabolism of serotonin (eg, MAOIs intended to treat psychiatric disorders, other MAOIs [ie, linezolid and IV methylene blue]). Monitor patients closely for signs of serotonin syndrome, such as mental status changes (eg, agitation, hallucinations, delirium, coma); autonomic instability (eg, tachycardia, labile blood pressure, diaphoresis, flushing, hyperthermia); neuromuscular changes (eg, tremor, rigidity, myoclonus); GI symptoms (eg, nausea, vomiting, diarrhea); and/or seizures. Discontinue treatment (and any concomitant serotonergic agent) immediately if signs/symptoms arise.

Disease-related concerns:

• Hepatic impairment: Use caution in patients with hepatic impairment; use in severe hepatic impairment is not recommended.

• Renal impairment: Use caution in patients with renal impairment; use in severe renal impairment is not recommended.

Concurrent drug therapy issues:

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Other warnings/precautions:

• Sedative/hypnotic withdrawal: Buspirone does not exhibit cross-tolerance with benzodiazepines or other sedative/hypnotic agents. If substituting buspirone for any of these agents, gradually withdraw the drug(s) prior to initiating buspirone.

Geriatric Considerations

Because buspirone is less sedating than other anxiolytics, it may be a useful agent in geriatric patients when an anxiolytic is indicated.

Warnings: Additional Pediatric Considerations

Buspirone does not possess antipsychotic activity and should not be used in place of appropriate antipsychotic treatment; two pediatric cases of possible psychotic deterioration have been reported (Soni, 1992).

Pregnancy Risk Factor

B

Pregnancy Considerations

Adverse events have not been observed in animal reproduction studies.

Breast-Feeding Considerations

It is not known if buspirone is present in breast milk.

In one case report, buspirone was not detected in the breast milk of a mother taking 15 mg three times daily during pregnancy and postpartum (samples obtained 13 days after delivery; limit of detection not noted) (Brent 1998).

Breastfeeding is not recommended by the manufacturer.

Briggs’ Drugs in Pregnancy & Lactation
Adverse Reactions

>10%: Central nervous system: Dizziness (3% to 12%)

1% to 10%:

Cardiovascular: Chest pain (≥1%)

Central nervous system: Drowsiness (10%), headache (6%), nervousness (5%), confusion (2%), excitement (2%), numbness (2%), outbursts of anger (2%), abnormal dreams (≥1%), ataxia (1%) paresthesia (1%)

Dermatologic: Diaphoresis (1%), skin rash (1%)

Gastrointestinal: Nausea (8%), diarrhea (2%), sore throat (≥1%)

Neuromuscular & skeletal: Weakness (2%), musculoskeletal pain (1%), tremor (1%)

Ophthalmic: Blurred vision (2%)

Otic: Tinnitus (≥1%)

Respiratory: Nasal congestion (≥1%)

<1%, postmarketing, and/or case reports: Acne vulgaris, akathisia, alcohol abuse, alopecia, altered sense of smell, amenorrhea, angioedema, anorexia, apathy, arthralgia, bradycardia, bruise, cardiac failure, cardiomyopathy, cerebrovascular accident, change in libido, claustrophobia, cogwheel rigidity, cold intolerance, conjunctivitis, delayed ejaculation, depersonalization, dissociative reaction, dysgeusia, dyskinesia, dysphoria, dyspnea, dystonia, dysuria, edema, emotional lability, eosinophilia, epistaxis, euphoria, extrapyramidal reaction, eye pain, facial edema, fear, fever, flatulence, flushing, galactorrhea, glossopyrosis, hallucination, hemorrhagic diathesis, hiccups, hyperacusis, hypersensitivity reaction, hypertension, hyperventilation, hypotension, impotence, increased appetite, increased intraocular pressure, increased serum ALT, increased serum AST, increased serum transaminases, inner ear disturbance, involuntary muscle movements, irritable bowel syndrome, laryngitis, leukopenia, malaise, memory impairment, menstrual disease, muscle cramps, muscle spasm, myocardial infarction, nocturia, parkinsonian-like syndrome, pelvic inflammatory disease, personality disorder, photophobia, pruritus, psychosis, rectal hemorrhage, restless leg syndrome, restlessness, roaring sensation in head, salivation, seizure, serotonin syndrome, skin blister, slowed reaction time, slurred speech, stiffness, stupor, suicidal ideation, syncope, thinning of nails, thrombocytopenia, thyroid disease, urinary frequency, urinary hesitancy, urinary incontinence, urinary retention, urticaria, vertigo, visual disturbance (tunnel vision), weight gain, weight loss, xeroderma

Allergy and Idiosyncratic Reactions
Metabolism/Transport Effects

Substrate of CYP2D6 (minor), CYP3A4 (major); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential

Drug Interactions 

Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy

Alizapride: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Antiemetics (5HT3 Antagonists): May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Risk C: Monitor therapy

Antipsychotic Agents: Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Risk C: Monitor therapy

Aprepitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy

Azelastine (Nasal): CNS Depressants may enhance the CNS depressant effect of Azelastine (Nasal). Risk X: Avoid combination

Blonanserin: CNS Depressants may enhance the CNS depressant effect of Blonanserin. Risk D: Consider therapy modification

Bosentan: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Risk C: Monitor therapy

Brimonidine (Topical): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Bromopride: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Bromperidol: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Buprenorphine: CNS Depressants may enhance the CNS depressant effect of Buprenorphine. Management: Consider reduced doses of other CNS depressants, and avoiding such drugs in patients at high risk of buprenorphine overuse/self-injection. Initiate buprenorphine patches (Butrans brand) at 5 mcg/hr in adults when used with other CNS depressants.Risk D: Consider therapy modification

Calcium Channel Blockers (Nondihydropyridine): May increase the serum concentration of BusPIRone. Exceptions: Bepridil. Risk C: Monitor therapy

Cannabidiol: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Cannabis: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Chlormethiazole: May enhance the CNS depressant effect of CNS Depressants. Management: Monitor closely for evidence of excessive CNS depression. The chlormethiazole labeling states that an appropriately reduced dose should be used if such a combination must be used. Risk D: Consider therapy modification

Chlorphenesin Carbamate: May enhance the adverse/toxic effect of CNS Depressants. Risk C: Monitor therapy

Clofazimine: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy

CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Risk C: Monitor therapy

Conivaptan: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination

CYP3A4 Inducers (Moderate): May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Risk C: Monitor therapy

CYP3A4 Inducers (Strong): May decrease the serum concentration of BusPIRone. Management: Consider alternatives to this combination. If coadministration of these agents is deemed necessary, monitor patients for reduced buspirone effects and increase buspirone doses as needed. Risk D: Consider therapy modification

CYP3A4 Inhibitors (Moderate): May decrease the metabolism of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy

CYP3A4 Inhibitors (Strong): May increase the serum concentration of BusPIRone. Management: Limit the buspirone dose to 2.5 mg daily and monitor patients for increased buspirone effects/toxicities if combined with strong CYP3A4 inhibitors. Risk D: Consider therapy modification

Dabrafenib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Seek alternatives to the CYP3A4 substrate when possible. If concomitant therapy cannot be avoided, monitor clinical effects of the substrate closely (particularly therapeutic effects). Risk D: Consider therapy modification

Dapoxetine: May enhance the adverse/toxic effect of Serotonin Modulators. Risk X: Avoid combination

Deferasirox: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Risk C: Monitor therapy

Dimethindene (Topical): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Doxylamine: May enhance the CNS depressant effect of CNS Depressants. Management: The manufacturer of Diclegis (doxylamine/pyridoxine), intended for use in pregnancy, specifically states that use with other CNS depressants is not recommended. Risk C: Monitor therapy

Dronabinol: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Droperidol: May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (eg, opioids, barbiturates) with concomitant use. Exceptions to this monograph are discussed in further detail in separate drug interaction monographs. Risk D: Consider therapy modification

Duvelisib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy

Enzalutamide: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Concurrent use of enzalutamide with CYP3A4 substrates that have a narrow therapeutic index should be avoided. Use of enzalutamide and any other CYP3A4 substrate should be performed with caution and close monitoring. Risk D: Consider therapy modification

Erythromycin (Systemic): May increase the serum concentration of BusPIRone. Management: Limit the buspirone dose to 2.5 mg twice daily and monitor for increased buspirone effects/toxicities if combined with erythromycin. Risk D: Consider therapy modification

Esketamine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Flunitrazepam: CNS Depressants may enhance the CNS depressant effect of Flunitrazepam. Risk D: Consider therapy modification

Fosaprepitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy

Fosnetupitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy

Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination

Grapefruit Juice: May increase the serum concentration of BusPIRone. Management: Monitor for increased effect of buspirone if combined with grapefruit juice. Patients should avoid consuming large quantities of grapefruit juice. Risk D: Consider therapy modification

HYDROcodone: CNS Depressants may enhance the CNS depressant effect of HYDROcodone. Management: Avoid concomitant use of hydrocodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug.Risk D: Consider therapy modification

HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Idelalisib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination

Ioflupane I 123: BusPIRone may diminish the diagnostic effect of Ioflupane I 123. Risk C: Monitor therapy

Ivosidenib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Risk C: Monitor therapy

Kava Kava: May enhance the adverse/toxic effect of CNS Depressants. Risk C: Monitor therapy

Larotrectinib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy

Lofexidine: May enhance the CNS depressant effect of CNS Depressants. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs. Risk C: Monitor therapy

Lorlatinib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Avoid concurrent use of lorlatinib with any CYP3A4 substrates for which a minimal decrease in serum concentrations of the CYP3A4 substrate could lead to therapeutic failure and serious clinical consequences. Risk D: Consider therapy modification

Magnesium Sulfate: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Metaxalone: May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Risk C: Monitor therapy

Methotrimeprazine: CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce adult dose of CNS depressant agents by 50% with initiation of concomitant methotrimeprazine therapy. Further CNS depressant dosage adjustments should be initiated only after clinically effective methotrimeprazine dose is established. Risk D: Consider therapy modification

Methylene Blue: BusPIRone may enhance the serotonergic effect of Methylene Blue. This could result in serotonin syndrome. Risk X: Avoid combination

Methylphenidate: May enhance the adverse/toxic effect of Serotonin Modulators. Specifically, the risk of serotonin syndrome or serotonin toxicity may be increased. Risk C: Monitor therapy

Metoclopramide: Serotonin Modulators may enhance the adverse/toxic effect of Metoclopramide. This may be manifest as symptoms consistent with serotonin syndrome or neuroleptic malignant syndrome. Risk C: Monitor therapy

MetyroSINE: CNS Depressants may enhance the sedative effect of MetyroSINE. Risk C: Monitor therapy

MiFEPRIStone: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Minimize doses of CYP3A4 substrates, and monitor for increased concentrations/toxicity, during and 2 weeks following treatment with mifepristone. Avoid cyclosporine, dihydroergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus, and tacrolimus. Risk D: Consider therapy modification

Minocycline: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Mirtazapine: CNS Depressants may enhance the CNS depressant effect of Mirtazapine. Risk C: Monitor therapy

Mitotane: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Doses of CYP3A4 substrates may need to be adjusted substantially when used in patients being treated with mitotane. Risk D: Consider therapy modification

Monoamine Oxidase Inhibitors: BusPIRone may enhance the adverse/toxic effect of Monoamine Oxidase Inhibitors. Specifically, blood pressure elevations been reported. Risk X: Avoid combination

Nabilone: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Nefazodone: BusPIRone may enhance the serotonergic effect of Nefazodone. This could result in serotonin syndrome. Nefazodone may increase the serum concentration of BusPIRone. Management: Limit the buspirone dose to 2.5 mg daily and monitor patients for increased buspirone effects/toxicities if combined with nefazodone. Additionally, monitor patient for signs of serotonin toxicity/serotonin syndrome if these agents are combined. Risk D: Consider therapy modification

Netupitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy

Opioid Agonists: CNS Depressants may enhance the CNS depressant effect of Opioid Agonists. Management: Avoid concomitant use of opioid agonists and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug.Risk D: Consider therapy modification

Orphenadrine: CNS Depressants may enhance the CNS depressant effect of Orphenadrine. Risk X: Avoid combination

Oxomemazine: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

OxyCODONE: CNS Depressants may enhance the CNS depressant effect of OxyCODONE. Management: Avoid concomitant use of oxycodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Risk D: Consider therapy modification

Palbociclib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy

Paraldehyde: CNS Depressants may enhance the CNS depressant effect of Paraldehyde. Risk X: Avoid combination

Perampanel: May enhance the CNS depressant effect of CNS Depressants. Management: Patients taking perampanel with any other drug that has CNS depressant activities should avoid complex and high-risk activities, particularly those such as driving that require alertness and coordination, until they have experience using the combination. Risk D: Consider therapy modification

Piribedil: CNS Depressants may enhance the CNS depressant effect of Piribedil. Risk C: Monitor therapy

Pitolisant: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Combined use of pitolisant with a CYP3A4 substrate that has a narrow therapeutic index should be avoided. Other CYP3A4 substrates should be monitored more closely when used with pitolisant. Risk D: Consider therapy modification

Pramipexole: CNS Depressants may enhance the sedative effect of Pramipexole. Risk C: Monitor therapy

Resveratrol: May increase the serum concentration of BusPIRone. Risk C: Monitor therapy

ROPINIRole: CNS Depressants may enhance the sedative effect of ROPINIRole. Risk C: Monitor therapy

Rotigotine: CNS Depressants may enhance the sedative effect of Rotigotine. Risk C: Monitor therapy

Rufinamide: May enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced. Risk C: Monitor therapy

Sarilumab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Risk C: Monitor therapy

Selective Serotonin Reuptake Inhibitors: BusPIRone may enhance the serotonergic effect of Selective Serotonin Reuptake Inhibitors. This may cause serotonin syndrome. Selective Serotonin Reuptake Inhibitors may decrease the metabolism of BusPIRone. Management: The combination of a selective serotonin reuptake inhibitor and buspirone should be undertaken with great caution. When combined treatment is clinically indicated, monitor closely for signs of serotonin toxicity/serotonin syndrome. Risk D: Consider therapy modification

Serotonin Modulators: May enhance the adverse/toxic effect of other Serotonin Modulators. The development of serotonin syndrome may occur. Exceptions: Nicergoline; Tedizolid.Risk C: Monitor therapy

Serotonin Reuptake Inhibitor/Antagonists: BusPIRone may enhance the serotonergic effect of Serotonin Reuptake Inhibitor/Antagonists. Management: The combination of a serotonin reuptake inhibitor,antagonist and buspirone should be undertaken with great caution. When combined treatment is clinically indicated, monitor closely for signs of serotonin toxicity/serotonin syndrome. Risk D: Consider therapy modification

Siltuximab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Risk C: Monitor therapy

Simeprevir: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy

Sodium Oxybate: May enhance the CNS depressant effect of CNS Depressants. Management: Consider alternatives to combined use. When combined use is needed, consider minimizing doses of one or more drugs. Use of sodium oxybate with alcohol or sedative hypnotics is contraindicated. Risk D: Consider therapy modification

St John’s Wort: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling. Risk D: Consider therapy modification

Stiripentol: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring. Risk D: Consider therapy modification

Suvorexant: CNS Depressants may enhance the CNS depressant effect of Suvorexant. Management: Dose reduction of suvorexant and/or any other CNS depressant may be necessary. Use of suvorexant with alcohol is not recommended, and the use of suvorexant with any other drug to treat insomnia is not recommended. Risk D: Consider therapy modification

Tapentadol: May enhance the CNS depressant effect of CNS Depressants. Management: Avoid concomitant use of tapentadol and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Risk D: Consider therapy modification

Tetrahydrocannabinol: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Tetrahydrocannabinol and Cannabidiol: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Thalidomide: CNS Depressants may enhance the CNS depressant effect of Thalidomide. Risk X: Avoid combination

Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Risk C: Monitor therapy

Trimeprazine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Yohimbine: May diminish the therapeutic effect of Antianxiety Agents. Risk C: Monitor therapy

Zolpidem: CNS Depressants may enhance the CNS depressant effect of Zolpidem. Management: Reduce the Intermezzo brand sublingual zolpidem adult dose to 1.75 mg for men who are also receiving other CNS depressants. No such dose change is recommended for women. Avoid use with other CNS depressants at bedtime; avoid use with alcohol. Risk D: Consider therapy modification

Food Interactions

Food may decrease the absorption of buspirone, but it may also decrease the first-pass metabolism, thereby increasing the bioavailability of buspirone. Grapefruit juice may cause increased buspirone concentrations. Management: Administer with or without food, but must be consistent. Avoid intake of large quantities of grapefruit juice.

Test Interactions

The presence of buspirone may result in a false positive on a urinary assay for metanephrine/catecholamine; discontinue buspirone ≥48 hours prior to collection of urine sample for catecholamines.

Monitoring Parameters

Mental status, symptoms of anxiety, signs/symptoms of serotonin syndrome.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral, as hydrochloride:

Generic: 5 mg, 7.5 mg, 10 mg, 15 mg, 30 mg

Dosage Forms: Canada

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral, as hydrochloride:

Generic: 5 mg, 10 mg

Anatomic Therapeutic Chemical (ATC) Classification
  • N05BE01
Generic Available (US)

Yes

Pricing: US

Tablets (busPIRone HCl Oral)

5 mg (per each): $0.06 – $0.77

7.5 mg (per each): $1.09 – $1.58

10 mg (per each): $0.09 – $1.35

15 mg (per each): $0.11 – $2.12

30 mg (per each): $1.26 – $3.64

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer’s AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Mechanism of Action

The mechanism of action of buspirone is unknown. Buspirone has a high affinity for serotonin 5-HT1A and 5-HT2 receptors, without affecting benzodiazepine-GABA receptors. Buspirone has moderate affinity for dopamine D2 receptors.

Pharmacodynamics/Kinetics

Absorption: Rapid and complete; bioavailability is limited by extensive first-pass effect; only ~1% of the oral dose reaches the systemic circulation unchanged

Distribution: Vd: 5.3 L/kg (Gammans 1986)

Protein binding: ~86%

Metabolism: Hepatic oxidation, primarily via CYP3A4 to several metabolites including an active metabolite, 1-pyrimidinylpiperazine (1-PP; exhibits about 25% of the activity of buspirone); extensive first-pass effect

Bioavailability: Increased with food

Half-life elimination: 2 to 3 hours; increased with renal or hepatic impairment

Time to peak, serum: 40 to 90 minutes

Excretion: Urine: 29% to 63% (primarily as metabolites); feces: 18% to 38%

Pharmacodynamics/Kinetics: Additional Considerations

Renal function impairment: AUC increased 4-fold.

Hepatic function impairment: AUC increased 13-fold.

Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions

Effects on Dental Treatment

Key adverse event(s) related to dental treatment: Xerostomia (normal salivary flow resumes upon discontinuation).

Effects on Bleeding

No information available to require special precautions

Index Terms

BuSpar; Buspirone Hydrochloride

FDA Approval Date
September 29, 1986
References

American Psychiatric Association (APA). Practice guideline for the treatment of patients with major depressive disorder. 3rd ed. http://psychiatryonline.org/pb/assets/raw/sitewide/practice_guidelines/guidelines/mdd.pdf. Published May 2010.

Appelberg BG, Syvälahti EK, Koskinen TE, Mehtonen OP, Muhonen TT, Naukkarinen HH. Patients with severe depression may benefit from buspirone augmentation of selective serotonin reuptake inhibitors: results from a placebo-controlled, randomized, double-blind, placebo wash-in study. J Clin Psychiatry. 2001;62(6):448-452.[PubMed 11465522]

Brent NB, Wisner KL. Fluoxetine and carbamazepine concentrations in a nursing mother/infant pair. Clin Pediatr (Phila). 1998;37(1):41-44.[PubMed 9475699]

Buspirone tablets [prescribing information]. East Brunswick, NJ: Strides Pharma Inc; February 2017.

Chessick CA, Allen MH, Thase M, et al. Azapirones for generalized anxiety disorder. Cochrane Database Syst Rev. 2006;(3):CD006115.[PubMed 16856115]

Gammans RE, Mayol RF, LaBudde JA. Metabolism and disposition of buspirone. Am J Med. 1986;80(3B):41-51.[PubMed 3515929]

Sramek JJ, Hong WW, Hamid S, Nape B, Cutler NR. Meta-analysis of the safety and tolerability of two dose regimens of buspirone in patients with persistent anxiety. Depress Anxiety. 1999;9(3):131-134.[PubMed 10356651]

Trivedi MH, Fava M, Wisniewski SR, et al. Medication augmentation after the failure of SSRIs for depression. N Engl J Med. 2006;354(12):1243-1252.[PubMed 16554526]

Brand Names: International

Actium (PY); Ansial (AR); Ansitec (BR); Anxiolan (TH); Anxiron (AE, CY, HN, HU, IQ, IR, JO, LB, LY, OM, SA, SY, YE); Anxut (DE); Bespar (DE, GR); Busiral (AE, CY, IQ, IR, JO, LB, LY, OM, SA, SY, YE); Busone (KR); Busp (TW); Buspalex (EG); Buspar (AT, CH, CZ, DK, EC, EE, EG, FI, FR, GB, HK, IE, IT, KR, LU, MT, MX, NL, NZ, PK, PT, RU, SA, SE, SK, TR, ZA); Busparium (UY); Busper (BD); Buspin (IN); Buspon (TR); Busron (KR, LK); Dalpas (VE); Dergelasen (CO); Duvaline (PY); Exupar (EG); Kallmiren (AE, CY, IQ, IR, JO, LB, LY, OM, SA, SY, YE); Loxapin (MT); Normaton (DO, GT, PA, SV); Pasrin (ZA); Paxon (CL); Relac (TW); Relax (EC); Sepirone (TW); Seropar (EG); Sorbon (IL); Spamilan (PL); Spitomin (BG, HU, LT, LV, RO, SK, UA); Suxin (CN); Travin (HR)

Buspirone (Patient Education – Adult Medication)
You must carefully read the “Consumer Information Use and Disclaimer” below in order to understand and correctly use this information
Pronunciation

(byoo SPYE rone)

What is this drug used for?
  • It is used to treat anxiety.
  • It may be given to you for other reasons. Talk with the doctor.
What do I need to tell my doctor BEFORE I take this drug?
  • If you have an allergy to buspirone or any other part of this drug.
  • If you are allergic to any drugs like this one, any other drugs, foods, or other substances. Tell your doctor about the allergy and what signs you had, like rash; hives; itching; shortness of breath; wheezing; cough; swelling of face, lips, tongue, or throat; or any other signs.
  • If you have taken certain drugs used for low mood (depression) like isocarboxazid, phenelzine, or tranylcypromine or drugs used for Parkinson’s disease like selegiline or rasagiline in the last 14 days. Taking this drug within 14 days of those drugs can cause very bad high blood pressure.
  • If you are taking any of these drugs: Linezolid or methylene blue.
  • If you are taking tryptophan.
  • If you have any of these health problems: Kidney disease or liver disease.
  • This is not a list of all drugs or health problems that interact with this drug.
  • Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take this drug with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.
What are some things I need to know or do while I take this drug?
  • Tell all of your health care providers that you take this drug. This includes your doctors, nurses, pharmacists, and dentists.
  • Avoid driving and doing other tasks or actions that call for you to be alert until you see how this drug affects you.
  • Avoid drinking alcohol while taking this drug.
  • Talk with your doctor before you use other drugs and natural products that slow your actions.
  • If you drink grapefruit juice or eat grapefruit often, talk with your doctor.
  • This drug may affect certain lab tests. Tell all of your health care providers and lab workers that you take this drug.
  • Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using this drug while you are pregnant.
  • Tell your doctor if you are breast-feeding. You will need to talk about any risks to your baby.
What are some side effects that I need to call my doctor about right away?
  • WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:
  • Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
  • Restlessness.
  • Trouble controlling body movements, twitching, change in balance, trouble swallowing or speaking.
  • A very bad and sometimes deadly health problem called serotonin syndrome may happen. The risk may be greater if you take this drug with drugs for depression, migraines, or certain other drugs. Call your doctor right away if you have agitation; change in balance; confusion; hallucinations; fever; fast or abnormal heartbeat; flushing; muscle twitching or stiffness; seizures; shivering or shaking; sweating a lot; very bad diarrhea, upset stomach, or throwing up; or very bad headache.
What are some other side effects of this drug?
  • All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:
  • Dizziness.
  • Feeling sleepy.
  • Feeling nervous and excitable.
  • Headache.
  • Upset stomach.
  • These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.
  • You may report side effects to your national health agency.
How is this drug best taken?
  • Use this drug as ordered by your doctor. Read all information given to you. Follow all instructions closely.
  • Take with or without food but take the same way each time. Always take with food or always take on an empty stomach.
  • To gain the most benefit, do not miss doses.
  • Keep taking this drug as you have been told by your doctor or other health care provider, even if you feel well.
What do I do if I miss a dose?
  • Take a missed dose as soon as you think about it.
  • If it is close to the time for your next dose, skip the missed dose and go back to your normal time.
  • Do not take 2 doses at the same time or extra doses.
How do I store and/or throw out this drug?
  • Store at room temperature.
  • Protect from light.
  • Store in a dry place. Do not store in a bathroom.
  • Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets.
  • Throw away unused or expired drugs. Do not flush down a toilet or pour down a drain unless you are told to do so. Check with your pharmacist if you have questions about the best way to throw out drugs. There may be drug take-back programs in your area.
General drug facts
  • If your symptoms or health problems do not get better or if they become worse, call your doctor.
  • Do not share your drugs with others and do not take anyone else’s drugs.
  • Keep a list of all your drugs (prescription, natural products, vitamins, OTC) with you. Give this list to your doctor.
  • Talk with the doctor before starting any new drug, including prescription or OTC, natural products, or vitamins.
  • Some drugs may have another patient information leaflet. If you have any questions about this drug, please talk with your doctor, nurse, pharmacist, or other health care provider.
  • If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.
Buspirone (Patient Education – Pediatric Medication)
You must carefully read the “Consumer Information Use and Disclaimer” below in order to understand and correctly use this information
Pronunciation

(byoo SPYE rone)

What is this drug used for?
  • It is used to treat anxiety.
  • It may be given to your child for other reasons. Talk with the doctor.
What do I need to tell the doctor BEFORE my child takes this drug?
  • If your child has an allergy to this drug or any part of this drug.
  • If your child is allergic to any drugs like this one or any other drugs, foods, or other substances. Tell the doctor about the allergy and what signs your child had, like rash; hives; itching; shortness of breath; wheezing; cough; swelling of face, lips, tongue, or throat; or any other signs.
  • If your child has taken certain drugs used for low mood (depression) like isocarboxazid, phenelzine, or tranylcypromine or drugs used for certain other health problems in the last 14 days. Taking this drug within 14 days of those drugs can cause very bad high blood pressure.
  • If your child is taking any of these drugs: Linezolid or methylene blue.
  • If your child is taking tryptophan.
  • If your child has any of these health problems: Kidney disease or liver disease.
  • This is not a list of all drugs or health problems that interact with this drug.
  • Tell the doctor and pharmacist about all of your child’s drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for your child to take this drug with all of his/her drugs and health problems. Do not start, stop, or change the dose of any drug your child takes without checking with the doctor.
What are some things I need to know or do while my child takes this drug?
  • Tell all of your child’s health care providers that your child is taking this drug. This includes your child’s doctors, nurses, pharmacists, and dentists.
  • Alcohol may interact with this drug. Be sure your child does not drink alcohol.
  • Talk with the doctor before giving your child other drugs and natural products that may slow your child’s actions.
  • If your child drinks grapefruit juice or eats grapefruit often, talk with your child’s doctor.
  • Have your child avoid tasks or actions that call for alertness until you see how this drug affects your child. These are things like riding a bike, playing sports, or using items such as scissors, lawnmowers, electric scooters, toy cars, or motorized vehicles.
  • This drug may affect certain lab tests. Tell all of your child’s health care providers and lab workers that your child takes this drug.
  • If your child is pregnant or breast-feeding a baby:
  • Talk with the doctor if your child is pregnant, becomes pregnant, or is breast-feeding a baby. You will need to talk about the benefits and risks to your child and the baby.
What are some side effects that I need to call my child’s doctor about right away?
  • WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your child’s doctor or get medical help right away if your child has any of the following signs or symptoms that may be related to a very bad side effect:
  • Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
  • Restlessness.
  • Trouble controlling body movements, twitching, change in balance, trouble swallowing or speaking.
  • A very bad and sometimes deadly health problem called serotonin syndrome may happen. The risk may be greater if your child takes this drug with drugs for depression, migraines, or certain other drugs. Call your child’s doctor right away if your child has agitation; change in balance; confusion; hallucinations; fever; a fast or abnormal heartbeat; flushing; muscle twitching or stiffness; seizures; shivering or shaking; sweating a lot; very bad diarrhea, upset stomach, or throwing up; or very bad headache.
What are some other side effects of this drug?
  • All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your child’s doctor or get medical help if any of these side effects or any other side effects bother your child or do not go away:
  • Dizziness.
  • Feeling sleepy.
  • Feeling nervous and excitable.
  • Headache.
  • Upset stomach.
  • These are not all of the side effects that may occur. If you have questions about side effects, call your child’s doctor. Call your child’s doctor for medical advice about side effects.
  • You may report side effects to your national health agency.
How is this drug best given?
  • Give this drug as ordered by your child’s doctor. Read all information given to you. Follow all instructions closely.
  • Give this drug with or without food but give it the same way each time. Always give with food or always give on an empty stomach.
  • To gain the most benefit, do not miss giving your child doses.
  • Keep giving this drug to your child as you have been told by your child’s doctor or other health care provider, even if your child feels well.
What do I do if my child misses a dose?
  • Give a missed dose as soon as you think about it.
  • If it is close to the time for your child’s next dose, skip the missed dose and go back to your child’s normal time.
  • Do not give 2 doses at the same time or extra doses.
How do I store and/or throw out this drug?
  • Store at room temperature.
  • Protect from light.
  • Store in a dry place. Do not store in a bathroom.
  • Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets.
  • Throw away unused or expired drugs. Do not flush down a toilet or pour down a drain unless you are told to do so. Check with your pharmacist if you have questions about the best way to throw out drugs. There may be drug take-back programs in your area.
General drug facts
  • If your child’s symptoms or health problems do not get better or if they become worse, call your child’s doctor.
  • Do not share your child’s drug with others and do not give anyone else’s drug to your child.
  • Keep a list of all your child’s drugs (prescription, natural products, vitamins, OTC) with you. Give this list to your child’s doctor.
  • Talk with your child’s doctor before giving your child any new drug, including prescription or OTC, natural products, or vitamins.
  • Some drugs may have another patient information leaflet. If you have any questions about this drug, please talk with your child’s doctor, nurse, pharmacist, or other health care provider.
  • If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.