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Buspirone HCl
Overview
What is Buspirone HCl?
Buspirone hydrochloride is an antianxiety agent that is not chemically or pharmacologically related to the benzodiazepines, barbiturates, or other sedative/anxiolytic drugs.
Buspirone hydrochloride is a white, crystalline, water soluble compound with a molecular weight of 422.0. Chemically buspirone hydrochloride is 8-[4-[4-(2-pyrimidinyl)-1-piperazinyl]-butyl]-8-azaspiro[4,5]decane-7,9- dione monohydrochloride. The molecular formula CHNO • HCl is represented by the following structural formula:
Each tablet for oral administration contains 5 mg, 10 mg, or 15 mg of buspirone hydrochloride USP (equivalent to 4.6 mg, 9.1 mg, and 13.7 mg of buspirone free base respectively). The 5 mg and 10 mg tablets are scored so they can be bisected. Thus, the 5 mg tablet can also provide a 2.5 mg dose, and the 10 mg tablet can provide a 5 mg dose. The 15 mg tablet is provided in a special tablet design. This tablet is scored so it can be either bisected or trisected. Thus, a single 15 mg tablet can provide the following doses: 15 mg (entire tablet), 10 mg (two-thirds of a tablet), 7.5 mg (one-half of a tablet), or 5 mg (one-third of a tablet). In addition, each tablet contains the following inactive ingredients: colloidal silicon dioxide, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and sodium starch glycolate.
What does Buspirone HCl look like?
What are the available doses of Buspirone HCl?
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What should I talk to my health care provider before I take Buspirone HCl?
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How should I use Buspirone HCl?
Buspirone hydrochloride tablets are indicated for the management of anxiety disorders or the short-term relief of the symptoms of anxiety. Anxiety or tension associated with the stress of everyday life usually does not require treatment with an anxiolytic.
The efficacy of buspirone has been demonstrated in controlled clinical trials of outpatients whose diagnosis roughly corresponds to Generalized Anxiety Disorder (GAD). Many of the patients enrolled in these studies also had coexisting depressive symptoms and buspirone relieved anxiety in the presence of these coexisting depressive symptoms. The patients evaluated in these studies had experienced symptoms for periods of 1 month to over 1 year prior to the study, with an average symptom duration of 6 months. Generalized Anxiety Disorder (300.02) is described in the American Psychiatric Association’s Diagnostic and Statistical Manual, lll1 as follows:
Generalized, persistent anxiety (of at least 1 month continual duration), manifested by symptoms from three of the four following categories:
The above symptoms would not be due to another mental disorder, such as a depressive disorder or schizophrenia. However, mild depressive symptoms are common in GAD.
The effectiveness of buspirone in long-term use, that is, for more than 3 to 4 weeks, has not been demonstrated in controlled trials. There is no body of evidence available that systematically addresses the appropriate duration of treatment for GAD. However, in a study of long-term use, 264 patients were treated with buspirone for 1 year without ill effect. Therefore, the physician who elects to use buspirone for extended periods should periodically reassess the usefulness of the drug for the individual patient.
The recommended initial dose is 15 mg daily (7.5 mg b.i.d.). To achieve an optimal therapeutic response, at intervals of 2 to 3 days the dosage may be increased 5 mg per day, as needed. The maximum daily dosage should not exceed 60 mg per day. In clinical trials allowing dose titration, divided doses of 20 to 30 mg per day were commonly employed.
The bioavailability of buspirone is increased when given with food as compared to the fasted state (see section). Consequently, patients should take buspirone in a consistent manner with regard to the timing of dosing; either always with or always without food.
When buspirone is to be given with a potent inhibitor of CYP3A4 the dosage recommendations described in the section should be followed.
What interacts with Buspirone HCl?
Buspirone tablets are contraindicated in patients hypersensitive to buspirone hydrochloride.
What are the warnings of Buspirone HCl?
Array
What are the precautions of Buspirone HCl?
General
While formal studies of the interaction of buspirone with alcohol indicate that buspirone does not increase alcohol-induced impairment in motor and mental performance, it is prudent to avoid concomitant use of alcohol and buspirone.
The syndrome of withdrawal from sedative/hypnotic/anxiolytic drugs can appear as any combination of irritability, anxiety, agitation, insomnia, tremor, abdominal cramps, muscle cramps, vomiting, sweating, flu-like symptoms without fever, and occasionally even as seizures.
See
Information for Patients
To assure safe and effective use of buspirone hydrochloride tablets, the following information and instructions should be given to patients:
Laboratory Tests
There are no specific laboratory tests recommended.
Drug Interactions
Array
Psychotropic Agents
MAO Inhibitors:
Amitriptyline:
Diazepam:
Haloperidol:
Nefazodone: [See
]
Trazodone:
Triazolam/Flurazepam:
Other Psychotropics:
Buspirone has been shown in vitro to be metabolized by CYP3A4. This finding is consistent with the in vivo interactions observed between buspirone and the following:
Diltiazem and Verapamil:
Erythromycin:
Grapefruit Juice:
Itraconazole:
Nefazodone:
Rifampin:
Other Inhibitors and Inducers of CYP3A4:
Other Drugs
Cimetidine: Coadministration of buspirone with cimetidine was found to increase C (40%) and T (2-fold), but had minimal effects on the AUC of buspirone.
Protein Binding
In vitro
In vitro
Therapeutic levels of aspirin, desipramine, diazepam, flurazepam, ibuprofen, propranolol, thioridazine, and tolbutamide had only a limited effect on the extent of binding of buspirone to plasma proteins (see section).
Drug/Laboratory Test Interactions
Buspirone is not known to interfere with commonly employed clinical laboratory tests.
Carcinogenesis, Mutagenesis, Impairment of Fertility
No evidence of carcinogenic potential was observed in rats during a 24-month study at approximately 133 times the maximum recommended human oral dose; or in mice, during an 18-month study at approximately 167 times the maximum recommended human oral dose.
With or without metabolic activation, buspirone did not induce point mutations in five strains of Salmonella typhimurium (Ames Test) or mouse lymphoma L5178YTK+ cell cultures, nor was DNA damage observed with buspirone in Wi-38 human cells. Chromosomal aberrations or abnormalities did not occur in bone marrow cells of mice given one or five daily doses of buspirone.
Pregnancy: Teratogenic Effects
Pregnancy Category B: No fertility impairment or fetal damage was observed in reproduction studies performed in rats and rabbits at buspirone doses of approximately 30 times the maximum recommended human dose. In humans, however, adequate and well-controlled studies during pregnancy have not been performed. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.
Labor and Delivery
The effect of buspirone on labor and delivery in women is unknown. No adverse effects were noted in reproduction studies in rats.
Nursing Mothers
The extent of the excretion in human milk of buspirone or its metabolites is not known. In rats, however, buspirone and its metabolites are excreted in milk. Buspirone administration to nursing women should be avoided if clinically possible.
Pediatric Use
The safety and effectiveness of buspirone were evaluated in two placebo-controlled 6-week trials involving a total of 559 pediatric patients (ranging from 6 to 17 years of age) with GAD. Doses studied were 7.5-30 mg b.i.d. (15-60 mg/day). There were no significant differences between buspirone and placebo with regard to the symptoms of GAD following doses recommended for the treatment of GAD in adults. Pharmacokinetic studies have shown that, for identical doses, plasma exposure to buspirone and its active metabolite, 1-PP, are equal to or higher in pediatric patients than adults. No unexpected safety findings were associated with buspirone in these trials. There are no long-term safety or efficacy data in this population.
Geriatric Use
In one study of 6632 patients who received buspirone for the treatment of anxiety, 605 patients were ≥ 65 years old and 41 were ≥ 75 years old; the safety and efficacy profiles for these 605 elderly patients (mean age =70.8 years) were similar to those in the younger population (mean age = 43.3 years). Review of spontaneously reported adverse clinical events has not identified differences between elderly and younger patients, but greater sensitivity of some older patients cannot be ruled out.
There were no effects of age on the pharmacokinetics of buspirone (see section).
Use in Patients With Impaired Hepatic or Renal Function
Buspirone is metabolized by the liver and excreted by the kidneys. A pharmacokinetic study in patients with impaired hepatic or renal function demonstrated increased plasma levels and a lengthened half-life of buspirone. Therefore, the administration of buspirone to patients with severe hepatic or renal impairment cannot be recommended (see section).
What are the side effects of Buspirone HCl?
(See also)
Commonly Observed
The more commonly observed untoward events associated with the use of buspirone not seen at an equivalent incidence among placebo-treated patients include dizziness, nausea, headache, nervousness, lightheadedness, and excitement.
Associated With Discontinuation of Treatment
One guide to the relative clinical importance of adverse events associated with buspirone is provided by the frequency with which they caused drug discontinuation during clinical testing. Approximately 10% of the 2200 anxious patients who participated in the buspirone premarketing clinical efficacy trials in anxiety disorders lasting 3 to 4 weeks discontinued treatment due to an adverse event. The more common events causing discontinuation included: central nervous system disturbances (3.4%), primarily dizziness, insomnia, nervousness, drowsiness, and lightheaded feeling; gastrointestinal disturbances (1.2%), primarily nausea; and miscellaneous disturbances (1.1%), primarily headache and fatigue. In addition, 3.4% of patients had multiple complaints, none of which could be characterized as primary.
Incidence in Controlled Clinical Trials
The table that follows enumerates adverse events that occurred at a frequency of 1% or more among buspirone patients who participated in 4-week, controlled trials comparing buspirone with placebo. The frequencies were obtained from pooled data for 17 trials. The prescriber should be aware that these figures cannot be used to predict the incidence of side effects in the course of usual medical practice where patient characteristics and other factors differ from those which prevailed in the clinical trials. Similarly, the cited frequencies cannot be compared with figures obtained from other clinical investigations involving different treatments, uses, and investigators. Comparison of the cited figures, however, does provide the prescribing physician with some basis for estimating the relative contribution of drug and nondrug factors to the side-effect incidence rate in the population studied.
| * Events reported by at least 1% of buspirone patients are included. | ||||
| - Incidence less than 1%. | ||||
| Buspirone | Placebo | |||
| (n = 477) | (n = 464) | Adverse Experience | ||
| Tachycardia/Palpitations | 1 | 1 | ||
| Dizziness | 12 | 3 | ||
| Drowsiness | 10 | 9 | ||
| Nervousness | 5 | 1 | ||
| Insomnia | 3 | 3 | ||
| Lightheadedness | 3 | - | ||
| Decreased Concentration | 2 | 2 | ||
| Excitement | 2 | - | ||
| Anger/Hostility | 2 | - | ||
| Confusion | 2 | - | ||
| Depression | 2 | 2 | ||
| Blurred Vision | 2 | - | ||
| Nausea | 8 | 5 | ||
| Dry Mouth | 3 | 4 | ||
| Abdominal/Gastric Distress | 2 | 2 | ||
| Diarrhea | 2 | - | ||
| Constipation | 1 | 2 | ||
| Vomiting | 1 | 2 | ||
| Musculoskeletal Aches/Pains | 1 | - | ||
| Numbness | 2 | - | ||
| Paresthesia | 1 | - | ||
| Incoordination | 1 | - | ||
| Tremor | 1 | - | ||
| Skin Rash | 1 | - | ||
| Headache | 6 | 3 | ||
| Fatigue | 4 | 4 | ||
| Weakness | 2 | - | ||
| Sweating/Clamminess | 1 | - |
Other Events Observed During the Entire Premarketing Evaluation of Buspirone
During the premarketing assessment, buspirone was evaluated in over 3500 subjects. This section reports event frequencies for adverse events occurring in approximately 3000 subjects from this group who took multiple doses of buspirone in the dose range for which buspirone hydrochloride is being recommended (i.e., the modal daily dose of buspirone fell between 10 and 30 mg for 70% of the patients studied) and for whom safety data were systematically collected. The conditions and duration of exposure to buspirone varied greatly, involving well-controlled studies as well as experience in open and uncontrolled clinical settings. As part of the total experience gained in clinical studies, various adverse events were reported. In the absence of appropriate controls in some of the studies, a causal relationship to buspirone treatment cannot be determined. The list includes all undesirable events reasonably associated with the use of the drug.
The following enumeration by organ system describes events in terms of their relative frequency of reporting in this data base. Events of major clinical importance are also described in the section.
The following definitions of frequency are used: Frequent adverse events are defined as those occurring in at least 1/100 patients. Infrequent adverse events are those occurring in 1/100 to 1/1000 patients, while rare events are those occurring in less than 1/1000 patients.
Postmarketing Experience
Postmarketing experience has shown an adverse experience profile similar to that given above. Voluntary reports since introduction have included rare occurrences of allergic reactions (including urticaria), angioedema, cogwheel rigidity, dizziness (rarely reported as vertigo), dystonic reactions, ataxias, extrapyramidal symptoms, dyskinesias (acute and tardive), ecchymosis, emotional lability, serotonin syndrome, transient difficulty with recall, urinary retention, and visual changes (including tunnel vision), parkinsonism, akathisia, restless leg syndrome, and restlessness. Because of the uncontrolled nature of these spontaneous reports, a causal relationship to buspirone treatment has not been determined.
What should I look out for while using Buspirone HCl?
Buspirone tablets are contraindicated in patients hypersensitive to buspirone hydrochloride.
The administration of buspirone to a patient taking a monoamine oxidase inhibitor (MAOI) may pose a hazard.
What might happen if I take too much Buspirone HCl?
How should I store and handle Buspirone HCl?
Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F) [see USP Controlled Room Temperature].Keep out of reach of children.Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F) [see USP Controlled Room Temperature].Keep out of reach of children.Buspirone HCl Tablets USP are supplied as follows:5 mg tablets: White, oval, biconvex, scored tablets, debossed WATSON and 657, in bottles of 100, 500, and 1000.10 mg tablets: White, oval, biconvex, scored tablets, debossed WATSON and 658, in bottles of 100, 500, and 1000.15 mg tablets: White, oval shaped, scored tablets, debossed with the Watson logo and 718, and scoring on both sides so it can be either bisected or trisected, in bottles of 60, 180, 500, and 1000.Store at 20° - 25°C (68°- 77°F). [See USP controlled room temperature]. Protect from temperatures greater than 30°C (86°F).Dispense in a tight, light-resistant container as defined in USP/NF.Buspirone HCl Tablets USP are supplied as follows:5 mg tablets: White, oval, biconvex, scored tablets, debossed WATSON and 657, in bottles of 100, 500, and 1000.10 mg tablets: White, oval, biconvex, scored tablets, debossed WATSON and 658, in bottles of 100, 500, and 1000.15 mg tablets: White, oval shaped, scored tablets, debossed with the Watson logo and 718, and scoring on both sides so it can be either bisected or trisected, in bottles of 60, 180, 500, and 1000.Store at 20° - 25°C (68°- 77°F). [See USP controlled room temperature]. Protect from temperatures greater than 30°C (86°F).Dispense in a tight, light-resistant container as defined in USP/NF.Buspirone HCl Tablets USP are supplied as follows:5 mg tablets: White, oval, biconvex, scored tablets, debossed WATSON and 657, in bottles of 100, 500, and 1000.10 mg tablets: White, oval, biconvex, scored tablets, debossed WATSON and 658, in bottles of 100, 500, and 1000.15 mg tablets: White, oval shaped, scored tablets, debossed with the Watson logo and 718, and scoring on both sides so it can be either bisected or trisected, in bottles of 60, 180, 500, and 1000.Store at 20° - 25°C (68°- 77°F). [See USP controlled room temperature]. Protect from temperatures greater than 30°C (86°F).Dispense in a tight, light-resistant container as defined in USP/NF.Buspirone HCl Tablets USP are supplied as follows:5 mg tablets: White, oval, biconvex, scored tablets, debossed WATSON and 657, in bottles of 100, 500, and 1000.10 mg tablets: White, oval, biconvex, scored tablets, debossed WATSON and 658, in bottles of 100, 500, and 1000.15 mg tablets: White, oval shaped, scored tablets, debossed with the Watson logo and 718, and scoring on both sides so it can be either bisected or trisected, in bottles of 60, 180, 500, and 1000.Store at 20° - 25°C (68°- 77°F). [See USP controlled room temperature]. Protect from temperatures greater than 30°C (86°F).Dispense in a tight, light-resistant container as defined in USP/NF.Buspirone HCl Tablets USP are supplied as follows:5 mg tablets: White, oval, biconvex, scored tablets, debossed WATSON and 657, in bottles of 100, 500, and 1000.10 mg tablets: White, oval, biconvex, scored tablets, debossed WATSON and 658, in bottles of 100, 500, and 1000.15 mg tablets: White, oval shaped, scored tablets, debossed with the Watson logo and 718, and scoring on both sides so it can be either bisected or trisected, in bottles of 60, 180, 500, and 1000.Store at 20° - 25°C (68°- 77°F). [See USP controlled room temperature]. Protect from temperatures greater than 30°C (86°F).Dispense in a tight, light-resistant container as defined in USP/NF.
Clinical Information
Chemical Structure
No Image foundClinical Pharmacology
The mechanism of action of buspirone is unknown. Buspirone differs from typical benzodiazepine anxiolytics in that it does not exert anticonvulsant or muscle relaxant effects. It also lacks the prominent sedative effect that is associated with more typical anxiolytics. In vitro preclinical studies have shown that buspirone has a high affinity for serotonin (5-HT) receptors. Buspirone has no significant affinity for benzodiazepine receptors and does not affect GABA binding or when tested in preclinical models.
Buspirone has moderate affinity for brain D2-dopamine receptors. Some studies do suggest that buspirone may have indirect effects on other neurotransmitter systems.
Buspirone is rapidly absorbed in man and undergoes extensive first-pass metabolism. In a radiolabeled study, unchanged buspirone in the plasma accounted for only about 1% of the radioactivity in the plasma. Following oral administration, plasma concentrations of unchanged buspirone are very low and variable between subjects. Peak plasma levels of 1 to 6 ng/mL have been observed 40 to 90 minutes after single oral doses of 20 mg. The single-dose bioavailability of unchanged buspirone when taken as a tablet is on the average about 90% of an equivalent dose of solution, but there is large variability.
The effects of food upon the bioavailability of buspirone have been studied in eight subjects. They were given a 20 mg dose with and without food; the area under the plasma concentration-time curve (AUC) and peak plasma concentration (C) of unchanged buspirone increased by 84% and 116% respectively, but the total amount of buspirone immunoreactive material did not change. This suggests that food may decrease the extent of presystemic clearance of buspirone. (See section.)
A multiple-dose study conducted in 15 subjects suggests that buspirone has nonlinear pharmacokinetics. Thus, dose increases and repeated dosing may lead to somewhat higher blood levels of unchanged buspirone than would be predicted from results of single-dose studies.
An protein binding study indicated that approximately 86% of buspirone is bound to plasma proteins. It was also observed that aspirin increased the plasma levels of free buspirone by 23%, while flurazepam decreased the plasma levels of free buspirone by 20%. However, it is not known whether these drugs cause similar effects on plasma levels of free buspirone in vivo, or whether such changes, if they do occur, cause clinically significant differences in treatment outcome. An in vitro study indicated that buspirone did not displace highly protein-bound drugs such as phenytoin, warfarin, and propranolol from plasma protein, and that buspirone may displace digoxin.
Buspirone is metabolized primarily by oxidation, which has been shown to be mediated by cytochrome P450 3A4 (CYP3A4). (See section.) Several hydroxylated derivatives and a pharmacologically active metabolite, 1-pyrimidinylpiperazine (1-PP), are produced. In animal models predictive of anxiolytic potential, 1-PP has about one quarter of the activity of buspirone, but is present in up to 20-fold greater amounts. However, this is probably not important in humans: blood samples from humans chronically exposed to buspirone do not exhibit high levels of 1-PP; mean values are approximately 3 ng/mL and the highest human blood level recorded among 108 chronically dosed patients was 17 ng/mL, less than 1/200th of 1-PP levels found in animals given large doses of buspirone without signs of toxicity.
In a single-dose study using C-labeled buspirone, 29% to 63% of the dose was excreted in the urine within 24 hours, primarily as metabolites; fecal excretion accounted for 18% to 38% of the dose. The average elimination half-life of unchanged buspirone after single doses of 10 to 40 mg is about 2 to 3 hours.
Non-Clinical Toxicology
Buspirone tablets are contraindicated in patients hypersensitive to buspirone hydrochloride.The administration of buspirone to a patient taking a monoamine oxidase inhibitor (MAOI) may pose a hazard.
Amitriptyline:
Diazepam:
Haloperidol:
Trazodone:
Triazolam/Flurazepam:
Other Psychotropics:
While formal studies of the interaction of buspirone with alcohol indicate that buspirone does not increase alcohol-induced impairment in motor and mental performance, it is prudent to avoid concomitant use of alcohol and buspirone.
The syndrome of withdrawal from sedative/hypnotic/anxiolytic drugs can appear as any combination of irritability, anxiety, agitation, insomnia, tremor, abdominal cramps, muscle cramps, vomiting, sweating, flu-like symptoms without fever, and occasionally even as seizures.
See
(See also)
Reference
This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"
While we update our database periodically, we cannot guarantee it is always updated to the latest version.
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