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Drug overview for BUCAPSOL (buspirone hcl):
Generic name: BUSPIRONE HCL (bue-SPYE-rone)
Drug class: Antianxiety Agents
Therapeutic class: Central Nervous System Agents
Buspirone hydrochloride is an anxiolytic agent.
No enhanced Uses information available for this drug.
Generic name: BUSPIRONE HCL (bue-SPYE-rone)
Drug class: Antianxiety Agents
Therapeutic class: Central Nervous System Agents
Buspirone hydrochloride is an anxiolytic agent.
No enhanced Uses information available for this drug.
DRUG IMAGES
No Image Available
The following indications for BUCAPSOL (buspirone hcl) have been approved by the FDA:
Indications:
Generalized anxiety disorder
Professional Synonyms:
None.
Indications:
Generalized anxiety disorder
Professional Synonyms:
None.
The following dosing information is available for BUCAPSOL (buspirone hcl):
For the management of anxiety disorders, the usual initial adult dosage of buspirone hydrochloride is 10-15 mg daily, usually in 2 or 3 divided doses. Dosage is increased as necessary in increments of 5 mg daily every 2-4 days, according to the patient's response and tolerance. In clinical studies, most patients responded to maintenance dosages of 15-30 mg daily in 2 or 3 divided doses.
Modification of the usual adult dosage does not appear necessary for geriatric patients. The manufacturer recommends that adult dosage not exceed 60 mg daily.
The manufacturer states that when buspirone is administered concomitantly with a potent CYP3A4 inhibitor, it should be administered at a low dosage (i.e., 2.5 mg once or twice daily) and that subsequent dosage adjustment of either drug should be based on clinical assessment. (See Drug Interactions: Drugs Affecting Microsomal Enzymes and see Dosage and Administration: Administration.)
Buspirone may have a slower onset of action than some anxiolytics (e.g., diazepam), and some patients may require motivation and education about the drug's effects during initial therapy to assure compliance. Symptomatic relief may occur during the first 2 weeks of buspirone therapy in some patients, but optimum anxiolytic effect usually requires at least 3-4 weeks of therapy; occasionally, 4-6 weeks may be required for optimum effect.
The efficacy of continued buspirone therapy for longer than 3-4 weeks has not been established by controlled studies. However, the drug has been used for longer periods (e.g., several months to a year) without unusual adverse effect or decreased efficacy in some patients. If buspirone is administered for longer than 3-4 weeks, the need for continued therapy should be reassessed periodically.
Dosage during prolonged maintenance therapy should be kept at the lowest effective level; once an adequate response has been achieved, dosage should be reduced gradually and subsequently adjusted according to the patient's response and tolerance.
Discontinuance of benzodiazepines and some other anxiolytic agents has been associated with symptoms of withdrawal, and buspirone will not prevent the development of these symptoms. Therefore, it is important that therapy with such agents be withdrawn gradually in patients being switched to buspirone, particularly when therapy with one of these agents has been prolonged and/or when relatively high dosages were used.
The need for modification of buspirone hydrochloride dosage in patients with renal impairment has not been fully elucidated, and the drug should be used with caution in such patients. There is some evidence that the pharmacokinetics of buspirone and its active metabolite, 1-pyrimidinylpiperazine (1-PP), are not affected substantially in patients with mild to moderate renal impairment. (See Pharmacokinetics: Elimination) In anuric patients, however, accumulation of 1-PP may occur, and adjustment in buspirone hydrochloride dosage may be necessary.
Some clinicians suggest that dosage of the drug be reduced by 25-50% in anuric patients. However, other clinicians state that because of the high interindividual and intraindividual variability in plasma concentrations of buspirone and 1-PP, it is difficult to make dosage adjustment recommendations for patients with renal impairment. Based on results from other studies, several clinicians state that because of the high interindividual and intraindividual variability in plasma buspirone concentrations, dosing recommendations for patients with renal impairment receiving buspirone cannot be made at this time.
In addition, the manufacturer states that the drug is not recommended for use in patients with severe renal impairment. The need for supplemental doses during hemodialysis has not been determined, but such doses do not appear necessary since the drug does not appear to be removed substantially by hemodialysis.
Buspirone hydrochloride should be used with caution in patients with impaired hepatic function, and the need for reduced dosage should be considered. (See Pharmacokinetics: Elimination.) The manufacturer states that the drug is not recommended for use in patients with severe hepatic impairment.
Modification of the usual adult dosage does not appear necessary for geriatric patients. The manufacturer recommends that adult dosage not exceed 60 mg daily.
The manufacturer states that when buspirone is administered concomitantly with a potent CYP3A4 inhibitor, it should be administered at a low dosage (i.e., 2.5 mg once or twice daily) and that subsequent dosage adjustment of either drug should be based on clinical assessment. (See Drug Interactions: Drugs Affecting Microsomal Enzymes and see Dosage and Administration: Administration.)
Buspirone may have a slower onset of action than some anxiolytics (e.g., diazepam), and some patients may require motivation and education about the drug's effects during initial therapy to assure compliance. Symptomatic relief may occur during the first 2 weeks of buspirone therapy in some patients, but optimum anxiolytic effect usually requires at least 3-4 weeks of therapy; occasionally, 4-6 weeks may be required for optimum effect.
The efficacy of continued buspirone therapy for longer than 3-4 weeks has not been established by controlled studies. However, the drug has been used for longer periods (e.g., several months to a year) without unusual adverse effect or decreased efficacy in some patients. If buspirone is administered for longer than 3-4 weeks, the need for continued therapy should be reassessed periodically.
Dosage during prolonged maintenance therapy should be kept at the lowest effective level; once an adequate response has been achieved, dosage should be reduced gradually and subsequently adjusted according to the patient's response and tolerance.
Discontinuance of benzodiazepines and some other anxiolytic agents has been associated with symptoms of withdrawal, and buspirone will not prevent the development of these symptoms. Therefore, it is important that therapy with such agents be withdrawn gradually in patients being switched to buspirone, particularly when therapy with one of these agents has been prolonged and/or when relatively high dosages were used.
The need for modification of buspirone hydrochloride dosage in patients with renal impairment has not been fully elucidated, and the drug should be used with caution in such patients. There is some evidence that the pharmacokinetics of buspirone and its active metabolite, 1-pyrimidinylpiperazine (1-PP), are not affected substantially in patients with mild to moderate renal impairment. (See Pharmacokinetics: Elimination) In anuric patients, however, accumulation of 1-PP may occur, and adjustment in buspirone hydrochloride dosage may be necessary.
Some clinicians suggest that dosage of the drug be reduced by 25-50% in anuric patients. However, other clinicians state that because of the high interindividual and intraindividual variability in plasma concentrations of buspirone and 1-PP, it is difficult to make dosage adjustment recommendations for patients with renal impairment. Based on results from other studies, several clinicians state that because of the high interindividual and intraindividual variability in plasma buspirone concentrations, dosing recommendations for patients with renal impairment receiving buspirone cannot be made at this time.
In addition, the manufacturer states that the drug is not recommended for use in patients with severe renal impairment. The need for supplemental doses during hemodialysis has not been determined, but such doses do not appear necessary since the drug does not appear to be removed substantially by hemodialysis.
Buspirone hydrochloride should be used with caution in patients with impaired hepatic function, and the need for reduced dosage should be considered. (See Pharmacokinetics: Elimination.) The manufacturer states that the drug is not recommended for use in patients with severe hepatic impairment.
Buspirone hydrochloride is administered orally. Concomitant administration of the drug with food can increase oral bioavailability of buspirone. Therefore, the manufacturer states that the drug should be given in a consistent manner relative to food intake.
(See Drug Interactions: Food.) The 15- and 30- mg tablets are provided as Dividose(R) tablets and are scored to be broken in 2 halves (each providing a dose of 7.5 and 15 mg, respectively, or in 3 thirds) (each providing a dose of 5 and 10 mg, respectively).
(See Drug Interactions: Food.) The 15- and 30- mg tablets are provided as Dividose(R) tablets and are scored to be broken in 2 halves (each providing a dose of 7.5 and 15 mg, respectively, or in 3 thirds) (each providing a dose of 5 and 10 mg, respectively).
| DRUG LABEL | DOSING TYPE | DOSING INSTRUCTIONS |
|---|---|---|
| BUCAPSOL 7.5 MG CAPSULE | Maintenance | Adults take 1 capsule (7.5 mg) by oral route 2 times per day |
| BUCAPSOL 10 MG CAPSULE | Maintenance | Adults take 1 capsule (10 mg) by oral route 2 times per day |
| BUCAPSOL 15 MG CAPSULE | Maintenance | Adults take 1 capsule (15 mg) by oral route 2 times per day |
No generic dosing information available.
The following drug interaction information is available for BUCAPSOL (buspirone hcl):
There are 1 contraindications.
These drug combinations generally should not be dispensed or administered to the same patient. A manufacturer label warning that indicates the contraindication warrants inclusion of a drug combination in this category, regardless of clinical evidence or lack of clinical evidence to support the contraindication.
| Drug Interaction | Drug Names |
|---|---|
| Buspirone/MAOIs SEVERITY LEVEL: 1-Contraindicated Drug Combination: This drug combination is contraindicated and generally should not be dispensed or administered to the same patient. MECHANISM OF ACTION: Combination of MAOIs, which decrease the breakdown of serotonin, and buspirone, a 5-HT1A and moderate D2 agonist, may cause an increase in endogenous serotonin and dopamine, which in addition to buspirone's agonist effect, could lead to hypertensive crisis.(1-3) CLINICAL EFFECTS: Concurrent use of buspirone and a MAOI may result in hypertensive crisis.(2,3) PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: The US manufacturer of buspirone recommends that these drugs not be administered concomitantly. Use of MAOIs to treat depression with buspirone or within 14 days of stopping buspirone is contraindicated. Use of buspirone within 14 days of stopping an MAOI to treat depression is also contraindicated.(2) The US manufacturer of phenelzine states that concurrent use of buspirone is contraindicated. At least 14 days should elapse between the discontinuation of phenelzine and the initiation of buspirone.(3) In emergency situations in patients maintained on buspirone, weigh the availability and safety of alternatives to methylene blue against the risk of hypertensive crisis. If methylene blue therapy is required, the patient's buspirone should be immediately discontinued. Patients should be monitored for hypertensive crisis for 2 weeks or until 24 hours after the last dose of methylene blue, whichever comes first.(4) In non-emergency situations in patients maintained on buspirone when methylene blue therapy is planned, discontinue the patient's buspirone at least 2 weeks in advance of methylene blue therapy. The patient's buspirone therapy may be resumed 24 hours after the last dose of methylene blue.(4) Do not initiate buspirone therapy in patients receiving methylene blue until 24 hours after the last dose of these agents.(4) DISCUSSION: Several cases of elevated blood pressure have been reported in patients receiving MAOIs who were given buspirone.(2) No adverse sequelae have been reported in these patients. Furazolidone is known to inhibit monoamine oxidase. Methylene blue, when administered intravenously, has been shown to reach sufficient concentrations to be a potent inhibitor of MAO-A.(5,6) Metaxalone is a weak inhibitor of MAO.(7,8) |
AZILECT, EMSAM, FURAZOLIDONE, MARPLAN, MATULANE, METAXALONE, METHYLENE BLUE, NARDIL, PARNATE, PHENELZINE SULFATE, PROCARBAZINE HCL, PROVAYBLUE, RASAGILINE MESYLATE, SELEGILINE HCL, TRANYLCYPROMINE SULFATE, XADAGO, ZELAPAR |
There are 3 severe interactions.
These drug interactions can produce serious consequences in most patients. Actions required for severe interactions include, but are not limited to, discontinuing one or both agents, adjusting dosage, altering administration scheduling, and providing additional patient monitoring. Review the full interaction monograph for more information.
| Drug Interaction | Drug Names |
|---|---|
| Ioflupane I 123/Dopamine Transporter Binders SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction. MECHANISM OF ACTION: Ioflupane binds to the dopamine transporter. Agents that also bind to this transporter may affect the results of single photon emission computed tomography (SPECT) brain imaging using ioflupane.(1) CLINICAL EFFECTS: SPECT imaging using ioflupane may not be accurate in patients taking other drugs that bind to the dopamine transporter binders.(1) PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: It is unknown if discontinuing other agents that bind to the dopamine transporter prior to a scan with ioflupane will decrease interference with the scan.(1) Make sure the radiologist interpreting the scan knows the patient is taking another agent that binds to the dopamine transporter. Alternative diagnostic tools may need to be considered. DISCUSSION: Ioflupane binds to the dopamine transporter. Agents that also bind to this transporter may affect the results of the scan. These agents include amoxapine, amphetamine, armodafinil, benztropine, bupropion, buspirone, citalopram, cocaine, dexmethylphenidate, escitalopram, fluoxetine, fluvoxamine, mazindol, methamphetamine, methylphenidate, modafinil, norephedrine, paroxetine, phentermine, phenylpropanolamine, selegiline, and sertraline.(1) |
DATSCAN, IOFLUPANE I-123 |
| Selected Sensitive CYP3A4 Substrates/Oral Lefamulin SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction. MECHANISM OF ACTION: Lefamulin is considered a moderate inhibitor of CYP3A4. FDA defines a moderate inhibitor as a drug which increases the area-under-curve (AUC) of a sensitive substrate by 2- to 5-fold.(1,4) CLINICAL EFFECTS: Concurrent use of oral lefamulin may lead to increased serum levels and adverse effects of drugs sensitive to inhibition of the CYP3A4 pathway.(1) PREDISPOSING FACTORS: With darifenacin, the risk of anticholinergic toxicities including cognitive decline, delirium, falls and fractures is increased in geriatric patients using more than one medicine with anticholinergic properties.(5) PATIENT MANAGEMENT: If oral lefamulin must be coadministered with a sensitive CYP3A4 substrate, it is recommended to closely monitor for adverse effects of the CYP3A4 substrate.(1) Drug-specific recommendations: The manufacturer of abemaciclib recommends monitoring for adverse reactions and considering a dose reduction of abemaciclib in 50 mg decrements as detailed in prescribing information (based on starting dose, previous dose reductions, and combination or monotherapy use) with concurrent use of moderate CYP3A4 inhibitors.(2) The US manufacturer of sirolimus protein-bound injection (Fyarro) states a dose reduction to 56 mg/m2 is recommended when used concurrently with moderate or weak CYP3A4 inhibitors. Concurrent use with strong CYP3A4 inhibitors should be avoided.(3) DISCUSSION: In a study, oral lefamulin tablets administered concomitantly with and at 2 or 4 hours before oral midazolam (a CYP3A4 substrate) increased the area-under-curve (AUC) and maximum concentration (Cmax) of midazolam by 200% and 100%, respectively. No clinically significant effect on midazolam pharmacokinetics was observed when co-administered with lefamulin injection.(1) Sensitive CYP3A4 substrates linked to this monograph include: abemaciclib, acalabrutinib, alfentanil, alprazolam, atorvastatin, brotizolam, budesonide, buspirone, cobimetinib, darifenacin, ebastine, eletriptan, elvitegravir, everolimus, lovastatin, lurasidone, maraviroc, midazolam, nisoldipine, paritaprevir, sildenafil, simvastatin, sirolimus, ticagrelor, triazolam, and ulipristal.(1,4,6) |
XENLETA |
| Buspirone; Dexfenfluramine; Fenfluramine/Linezolid SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction. MECHANISM OF ACTION: Linezolid is a weak, reversible inhibitor of monoamine oxidase. Buspirone is a 5-HT1A and moderate D2 agonist, while fenfluramine is an agonist of 5HT-2. Combination of these agents may result an increase in endogenous serotonin and dopamine.(1-6) CLINICAL EFFECTS: Concurrent use of buspirone, dexfenfluramine or fenfluramine with linezolid may result in elevated blood pressure leading to hypertensive crisis.(1-3) PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: The US manufacturers of buspirone and fenfluramine state that concurrent use of linezolid is contraindicated.(1,2) The manufacturer of linezolid does not contraindicate the use of serotonergic agents but states that they should not be coadministered unless clinically appropriate and the patient is closely monitored.(3) This recommendation is consistent with the 2011 FDA Drug Safety Communication on linezolid and serotonergic psychiatric medications.(8,9) In non-emergency situations in patients maintained on buspirone, dexfenfluramine or fenfluramine, when linezolid therapy is planned, discontinue the patient's buspirone, dexfenfluramine or fenfluramine at least 2 weeks in advance of linezolid therapy.(6) In emergency situations in patients maintained on buspirone, dexfenfluramine or fenfluramine, weigh the availability and safety of alternatives to linezolid against the risk of hypertensive crisis. If linezolid therapy is required, the patient's buspirone, dexfenfluramine or fenfluramine should be immediately discontinued. Patients should be monitored for hypertensive crisis for 2 weeks or until 24 hours after the last dose of linezolid, whichever comes first.(6) The patient's buspirone, dexfenfluramine or fenfluramine therapy may be resumed 24 hours after the last dose of linezolid.(6) If concurrent therapy is warranted, patients should be monitored closely for hypertensive crisis. DISCUSSION: Several cases of elevated blood pressure have been reported in patients receiving MAOIs who were given buspirone.(1) No adverse sequelae have been reported in these patients. |
LINEZOLID, LINEZOLID-0.9% NACL, LINEZOLID-D5W, ZYVOX |
There are 7 moderate interactions.
The clinician should assess the patient’s characteristics and take action as needed. Actions required for moderate interactions include, but are not limited to, discontinuing one or both agents, adjusting dosage, altering administration.
| Drug Interaction | Drug Names |
|---|---|
| Buspirone/Nefazodone SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed. MECHANISM OF ACTION: Nefazodone inhibits the metabolism of buspirone by CYP3A4.(1,2) Buspirone may interfere with the metabolism of nefazodone. CLINICAL EFFECTS: Concurrent use of nefazodone and buspirone may result in elevated levels of and increased effects from buspirone, including lightheadedness, asthenia, dizziness, and somnolence.(1,2) Concurrent use of higher doses of buspirone with nefazodone may result in increased levels and effects of nefazodone.(1) PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: The manufacturer of nefazodone and buspirone recommends a low dose of buspirone (2.5 mg daily) in patients receiving concurrent therapy with these agents.(1,2) Patients receiving concurrent therapy should be monitored for increased effects of both agents. The dosage of buspirone may need to be adjusted if nefazodone is withdrawn from therapy. DISCUSSION: In a study in healthy subjects, concurrent use of buspirone (2.5 mg or 5 mg twice daily) with nefazodone (250 mg twice daily) resulted in increases in the maximum concentration (Cmax) and area-under-curve (AUC) of buspirone, up to 20-fold and up to 50-fold, respectively. The concentration of 1-pyrimidinylpiperazine (a buspirone metabolite) decreased 50%. In subjects taking 2.5 mg of buspirone with nefazodone, the side effect profile was similar to those of subjects taking either drug alone. In subjects taking 5 mg of buspirone, the AUC of nefazodone, of the hydroxynefazodone metabolite of nefazodone, and of the meta-chlorophenylpiperazine metabolite of nefazodone increased by 23%, 17%, and 9%, respectively.(1,2) The Cmax of nefazodone and hydroxynefazodone increased by 8% and 11%, respectively.(2) Subjects also reported side effects of lightheadedness, asthenia, dizziness, and somnolence.(1,2) |
NEFAZODONE HCL |
| Select Sedative Hypnotics; Buspirone/Strong CYP3A4 Inducers SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed. MECHANISM OF ACTION: Strong inducers of CYP3A4 may induce the metabolism of buspirone,(1-3) eszopiclone,(4) zopiclone,(5) and zolpidem.(6) CLINICAL EFFECTS: Concurrent use of strong CYP3A4 inducers may result in decreased levels and clinical effectiveness of buspirone,(1-3) eszopiclone,(4) zopiclone,(5) and zolpidem.(6) PREDISPOSING FACTORS: Induction effects may be more likely with regular use of the inducer for longer than 1-2 weeks. PATIENT MANAGEMENT: The dose of buspirone may need adjusting to maintain anxiolytic effect.(1) Concurrent use of strong CYP3A4 inducers with zolpidem is not recommended.(6) If concomitant therapy is warranted, patients should be counseled about possible decreased buspirone or hypnotic effectiveness. DISCUSSION: In a randomized, placebo-controlled, cross-over study in 10 subjects, rifampin (600 mg daily) decreased buspirone (30 mg single dose) maximum concentration (Cmax), area-under-curve (AUC), and half-life by 89.6%, 83.7%, and 54%, respectively. During the placebo phase, all subjects had measurable plasma buspirone concentrations at 10 hours after administration; however, no subject had measurable plasma buspirone concentrations at 6 hours after administration during the rifampin phase.(2) The Cmax of the buspirone piperazine metabolite increased by 35%.(3) There were significant decreases in the effects of buspirone in the postural sway test with eyes closed, the visual analogue scale (VAS) test for subjective drowsiness, and the VAS test for overall drug effect during concurrent rifampin. Buspirone side effects were reported more often during the placebo phase.(2) In a study in 8 subjects, rifampin (600 mg daily for 6 days) decreased the area-under-curve (AUC) of a single dose of zopiclone (10 mg) by 82%. The maximum concentration (Cmax) and half-life of zopiclone were decreased by 71% and 15%, respectively. A significant reduction in zopiclone effects were seen in 3 of 5 psychomotor tests.(5) In a randomized cross-over study in 8 subjects, rifampin (600 mg daily for 6 days) decreased the AUC, Cmax, and half-life of a single dose of zolpidem (20 mg) by 73%, 58%, and 36%, respectively. A significant reduction in zolpidem effects were seen in all 6 psychomotor tests.(6,7) Similar effects are expected with eszopiclone.(4) |
ASA-BUTALB-CAFFEINE-CODEINE, ASCOMP WITH CODEINE, BRAFTOVI, BUTALB-ACETAMINOPH-CAFF-CODEIN, BUTALBITAL, BUTALBITAL-ACETAMINOPHEN, BUTALBITAL-ACETAMINOPHEN-CAFFE, BUTALBITAL-ASPIRIN-CAFFEINE, CARBAMAZEPINE, CARBAMAZEPINE ER, CARBATROL, CEREBYX, DILANTIN, DILANTIN-125, DONNATAL, EPITOL, EQUETRO, ERLEADA, FIORICET, FIORICET WITH CODEINE, FOSPHENYTOIN SODIUM, LYSODREN, MITOTANE, MYSOLINE, ORKAMBI, PENTOBARBITAL SODIUM, PHENOBARBITAL, PHENOBARBITAL SODIUM, PHENOBARBITAL-BELLADONNA, PHENOBARBITAL-HYOSC-ATROP-SCOP, PHENOHYTRO, PHENYTEK, PHENYTOIN, PHENYTOIN SODIUM, PHENYTOIN SODIUM EXTENDED, PRIFTIN, PRIMIDONE, RIFADIN, RIFAMPIN, SEZABY, TEGRETOL, TEGRETOL XR, TENCON, TIBSOVO, XTANDI |
| Buspirone/Strong CYP3A4 Inhibitors SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed. MECHANISM OF ACTION: Strong inhibitors of CYP3A4 may inhibit the metabolism of buspirone.(1-4) CLINICAL EFFECTS: Concurrent use of a strong CYP3A4 inhibitor may result in elevated levels of and increased effects from buspirone, including lightheadedness, asthenia, dizziness, and somnolence.(1-4) PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: The Australian,(2) UK,(3) and US(4) manufacturers of buspirone recommend a lower dose of 2.5 mg twice daily of buspirone in patients receiving strong CYP3A4 inhibitors. DISCUSSION: In a study in 8 healthy subjects, pretreatment with 4 days of erythromycin (1.5 g/day) increased the area-under curve (AUC) and maximum concentration (Cmax) of a single dose of buspirone (10 mg) by 6-fold and 5-fold, respectively. The relative increase in buspirone AUC varied by 15-fold. There was a significant difference in scores on the Digit Symbol Substitution test when buspirone was administered with erythromycin.(1) In a study in 8 healthy subjects, pretreatment with itraconazole (200 mg daily for 4 days) increased the Cmax and AUC of buspirone by 13-fold and 19-fold, respectively.(1,2) However, only the Critical Flicker Fusion test showed statistically significant differences when compared to the administration of buspirone alone.(1) In a study in 6 subjects, pretreatment with itraconazole (200 mg daily for 4 days) increased the Cmax and AUC of buspirone by 10.5-fold and 14.5-fold, respectively. The Cmax and AUC of the piperazine metabolite of buspirone increased by 57% and 50%, respectively.(3) In a study in healthy subjects, concurrent use of buspirone (2.5 mg or 5 mg twice daily) with nefazodone (250 mg twice daily) resulted in increases in the Cmax and AUC of buspirone, up to 20-fold and up to 50-fold, respectively. The concentration of 1-pyrimidinylpiperazine (a buspirone metabolite) decreased 50%.(4) |
CLARITHROMYCIN, CLARITHROMYCIN ER, E.E.S. 200, E.E.S. 400, ERY-TAB, ERYPED 200, ERYPED 400, ERYTHROCIN LACTOBIONATE, ERYTHROCIN STEARATE, ERYTHROMYCIN, ERYTHROMYCIN ESTOLATE, ERYTHROMYCIN ETHYLSUCCINATE, ERYTHROMYCIN LACTOBIONATE, EVOTAZ, GENVOYA, KALETRA, KORLYM, KRAZATI, LANSOPRAZOL-AMOXICIL-CLARITHRO, LOPINAVIR-RITONAVIR, MIFEPREX, MIFEPRISTONE, NORVIR, NOXAFIL, OMECLAMOX-PAK, PAXLOVID, POSACONAZOLE, PREZCOBIX, RITONAVIR, STRIBILD, SYMTUZA, TUKYSA, TYBOST, VFEND, VFEND IV, VIRACEPT, VOQUEZNA TRIPLE PAK, VORICONAZOLE, ZOKINVY, ZYDELIG, ZYKADIA |
| Buspirone/Diltiazem; Verapamil SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed. MECHANISM OF ACTION: Diltiazem and verapamil may inhibit the metabolism of buspirone by CYP3A4.(1) CLINICAL EFFECTS: Concurrent use of diltiazem(1,2) or verapamil(1) may result in increased levels of and effects from buspirone, including lightheadedness, asthenia, dizziness, and somnolence.(3) PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: Patients receiving concurrent therapy with buspirone and either diltiazem or verapamil should be monitored for adverse effects. The dosage of buspirone may need to be adjusted.(1,2) DISCUSSION: In a randomized, 3-way cross-over study in 9 healthy subjects, concurrent diltiazem (60 mg 3 times daily) and verapamil (80 mg 3 times daily) increased the area-under-curve (AUC) of a single dose of buspirone (10 mg) by 5.5-fold and 3.4-fold, respectively. Buspirone maximum concentration (Cmax) increased by 4.1-fold and 3.4-fold, respectively. Overall drug effects were increased with concurrent diltiazem and verapamil. (1) |
CARDIZEM, CARDIZEM CD, CARDIZEM LA, CARTIA XT, DILT-XR, DILTIAZEM 12HR ER, DILTIAZEM 24HR ER, DILTIAZEM 24HR ER (CD), DILTIAZEM 24HR ER (LA), DILTIAZEM 24HR ER (XR), DILTIAZEM HCL, DILTIAZEM HCL-0.7% NACL, DILTIAZEM HCL-0.9% NACL, DILTIAZEM HCL-NACL, DILTIAZEM-D5W, MATZIM LA, TIADYLT ER, TIAZAC, TRANDOLAPRIL-VERAPAMIL ER, VERAPAMIL ER, VERAPAMIL ER PM, VERAPAMIL HCL, VERAPAMIL SR |
| Select Benzodiazepines; Buspirone/Itraconazole;Ketoconazole SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed. MECHANISM OF ACTION: Itraconazole and ketoconazole may inhibit the metabolism of brotizolam, buspirone, diazepam, etizolam, flunitrazepam, and midazolam injection by CYP3A4.(1-23) CLINICAL EFFECTS: Inhibition of benzodiazepine or buspirone metabolism may produce increased levels of these agents, as well as increased clinical effects. Toxic effects of increased benzodiazepine levels include profound sedation, respiratory depression, coma, and/or death. Increased effects from buspirone may include lightheadedness, asthenia, dizziness, and somnolence. PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: The US manufacturer of buspirone recommends a low dose of buspirone (2.5 mg daily) be used in patients receiving potent inhibitors of CYP3A4.(23) Monitor patients receiving concurrent therapy with itraconazole or ketoconazole and hepatically metabolized benzodiazepines carefully for increased effects including unusual dizziness or lightheadedness, extreme sleepiness, slowed or difficult breathing, or unresponsiveness. DISCUSSION: In a randomized, double-blind, cross-over study in 10 healthy males, itraconazole (200 mg daily for 4 days) increased the area-under-cure (AUC) and half-life of a single dose of brotizolam (0.5 mg) by 142% and 410%, respectively. Brotizolam clearance decreased by 76%. Brotizolam effects were increased.(6) Ketoconazole has been shown to inhibit brotizolam metabolism in vitro.(7) In a randomized, double-blind, cross-over study in 10 healthy males, itraconazole (200 mg daily for 4 days) increased the AUC and half-life of a single dose of diazepam (5 mg); however, there were no significant effects on diazepam pharmacodynamics.(8) In a randomized, double-blind, cross-over study in 12 healthy males, itraconazole (200 mg daily for 7 days) increased the AUC and half-life of a single dose of etizolam (1 mg) by 53% and 44%, respectively. There were no significant effects on etizolam pharmacodynamics.(9) Ketoconazole has been shown to inhibit flunitrazepam metabolism in vitro.(10) In a study in 9 healthy subjects, itraconazole increased the AUC of oral midazolam by 8-fold. Increased effects were also noted.(11) In a double-blind cross-over study in 12 subjects, itraconazole increased the AUC, maximum concentration (Cmax), and half-life of oral midazolam by 6-fold, 2.5-fold, and 2-fold, respectively. Increased effects were also noted.(12) In a cross-over study in 12 subjects, one dose of itraconazole increased the AUC and Cmax of oral midazolam by 3.5-fold and by 2-fold, respectively. Six doses of itraconazole increased the AUC of oral midazolam by almost 7-fold. Increased midazolam effects were seen.(13) In a double-blind, cross-over study, itraconazole increased midazolam AUC by 10-fold. Subjects also experienced significantly increased sedation and amnesiac effects.(14) Itraconazole has also been shown to inhibit midazolam metabolism in vitro.(15,16) In a study in healthy subjects, ketoconazole increased the AUC of oral midazolam by 771.9%.(17) In a double-blind, cross-over study, ketoconazole increased midazolam AUC by 15-fold. Subjects also experienced significantly increased sedation and amnesiac effects.(14) In a study in 11 healthy subjects, administration of ketoconazole (400 mg daily) for 1 day, 2 days, and 5 days increased the AUC of a single dose of oral midazolam (2 mg) by 10.28-fold, 13.14-fold, and 13.96-fold, respectively, and the Cmax by 5.01-fold, 5.29-fold, and 5.42-fold, respectively.(18) In a study in healthy subjects, ketoconazole (200 mg twice daily) reduced the clearance of midazolam 6-fold.(19) Ketoconazole has also been shown to inhibit the metabolism of midazolam in vitro.(15,16,20-22) In a study in 8 healthy subjects, pretreatment with itraconazole (200 mg daily for 4 days) increased the maximum concentration (Cmax) and area-under-curve (AUC) of buspirone by 13-fold and 19-fold, respectively.(1,2) However, only the Critical Flicker Fusion test showed statistically significant differences when compared to the administration of buspirone alone.(2) In a study in 6 subjects, pretreatment with itraconazole (200 mg daily for 4 days) increased the Cmax and AUC of buspirone by 10.5-fold and 14.5-fold, respectively. The Cmax and AUC of the piperazine metabolite of buspirone increased by 57% and 50%, respectively.(3) Ketoconazole has been shown to inhibit the metabolism of buspirone in vitro.(4) |
ITRACONAZOLE, ITRACONAZOLE MICRONIZED, KETOCONAZOLE, SPORANOX, TOLSURA |
| Buspirone; Diazepam/Ribociclib SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed. MECHANISM OF ACTION: Ribociclib may inhibit the metabolism of buspirone or diazepam by CYP3A4.(1) CLINICAL EFFECTS: Concurrent use of ribociclib may result in increased levels of and effects from buspirone or diazepam. Increased effects from diazepam may include profound sedation, respiratory depression, coma, and/or death. Increased effects from buspirone may include lightheadedness, asthenia, dizziness, and somnolence. PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: Patients receiving concurrent therapy with buspirone or diazepam and ribociclib should be monitored for adverse effects. The dosage of buspirone or diazepam may need to be adjusted.(1,2) The manufacturer of buspirone states that when administered with a potent inhibitor of CYP3A4, a low dose of buspirone used cautiously is recommended. DISCUSSION: In a study in healthy subjects, concomitant administration of ribociclib (400 mg once daily for 8 days) with midazolam increased the midazolam maximum concentration (Cmax) and area-under-curve (AUC) by 2.1-fold and 3.8-fold, respectively. Administration of ribociclib 600 mg once daily is predicted to increase the midazolam Cmax and AUC by 2.4-fold and 5.2-fold, respectively. |
KISQALI |
| Ziprasidone/Serotonergic Agents SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed. MECHANISM OF ACTION: Ziprasidone is a 5-HT1A agonist and serotonin and norepinephrine reuptake inhibitor. Concurrent administration with one or more serotonergic agents may increase serotonin effects, resulting in serotonin toxicity.(1,2) CLINICAL EFFECTS: Concurrent use of ziprasidone and other serotonergic agents may result in serotonin syndrome, a potentially life-threatening condition with symptoms including altered mental status, hypertension, restlessness, myoclonus, hyperthermia, hyperreflexia, diaphoresis, shivering, and tremor.(1) PREDISPOSING FACTORS: Serotonin syndrome risk is dose-related. Higher systemic concentrations of either drug would be predicted to increase risk for serotonin toxicity.(2) Concomitant therapy with multiple agents which increase brain serotonin concentrations may also increase risk for serotonin syndrome.(2) PATIENT MANAGEMENT: Caution patients about the risk of serotonin syndrome with the concomitant use of ziprasidone with other serotonergic drugs. Instruct patients to contact their healthcare provider, or report to the emergency room, should they experience signs or symptoms of serotonin syndrome.(1) DISCUSSION: Several cases of serotonin syndrome have been reported in patients receiving ziprasidone.(4-6) |
GEODON, ZIPRASIDONE HCL, ZIPRASIDONE MESYLATE |
The following contraindication information is available for BUCAPSOL (buspirone hcl):
Drug contraindication overview.
No enhanced Contraindications information available for this drug.
No enhanced Contraindications information available for this drug.
There are 0 contraindications.
There are 0 severe contraindications.
There are 4 moderate contraindications.
Clinically significant contraindication, where the condition can be managed or treated before the drug may be given safely.
| Moderate List |
|---|
| Chronic kidney disease stage 4 (severe) GFR 15-29 ml/min |
| Chronic kidney disease stage 5 (failure) GFr<15 ml/min |
| Disease of liver |
| Parkinsonism |
The following adverse reaction information is available for BUCAPSOL (buspirone hcl):
Adverse reaction overview.
No enhanced Common Adverse Effects information available for this drug.
No enhanced Common Adverse Effects information available for this drug.
There are 10 severe adverse reactions.
| More Frequent | Less Frequent |
|---|---|
| None. |
Hostility |
| Rare/Very Rare |
|---|
|
Akathisia Angioedema Chest pain Dyskinesia Extrapyramidal disease Parkinsonism Tachycardia Urinary retention Urticaria |
There are 34 less severe adverse reactions.
| More Frequent | Less Frequent |
|---|---|
|
Dizziness Headache disorder Nausea Nervousness |
Acute cognitive impairment Ataxia Depression Diarrhea Excitement General weakness Hyperhidrosis Hypoesthesia Myalgia Paresthesia Skin rash Tremor |
| Rare/Very Rare |
|---|
|
Accidental fall Arthralgia Blurred vision Concentration difficulty Cramps Drowsy Fatigue Fever Insomnia Muscle rigidity Muscle spasm Muscle weakness Nasal congestion Nightmares Palpitations Sore throat Tinnitus Xerostomia |
The following precautions are available for BUCAPSOL (buspirone hcl):
No enhanced Pediatric Use information available for this drug.
Contraindicated
Severe Precaution
Management or Monitoring Precaution
Contraindicated
| None |
Severe Precaution
| None |
Management or Monitoring Precaution
| None |
Reproduction studies in rats and rabbits using oral buspirone hydrochloride dosages up to 30 times the maximum recommended human dosage have not revealed evidence of fetal abnormality or impaired fertility. There are no adequate and controlled studies to date using buspirone in pregnant women, and the drug should be used during pregnancy only when clearly needed. The effect of buspirone on labor and delivery in women is not known, but no adverse effects were observed during reproduction studies in animals.
Although the extent of distribution of buspirone and its metabolites into human milk is not known, the drug and its metabolites are distributed into milk in rats. Therefore, the manufacturer recommends that the use of buspirone in nursing women be avoided whenever clinically possible.
No enhanced Geriatric Use information available for this drug.
The following prioritized warning is available for BUCAPSOL (buspirone hcl):
No warning message for this drug.
No warning message for this drug.
The following icd codes are available for BUCAPSOL (buspirone hcl)'s list of indications:
| Generalized anxiety disorder | |
| F41.1 | Generalized anxiety disorder |
| F41.9 | Anxiety disorder, unspecified |
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