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Buspirone (Buspar) - Uses, Dose, MOA, Brands, Side effects

Buspirone (Buspar) is a drug used for the short-term treatment of anxiety. It is chemically unrelated to benzodiazepines and barbiturates.

It is used in the treatment of the following disorders:

For the management of GAD (generalized anxiety disorder) or for the short-term relief of the symptoms of anxiety.
For the treatment of Unipolar depression as Off Label Use.

Buspirone Dose in Adults

Buspirone in the treatment of Generalized anxiety disorder:

10 - 15 mg/day orally in 2 - 3 divided doses
The dose may be increased every 2 - 3 days in increments of 5 mg/day to a maximum of 60 mg/day in 2 divided doses.
The usual daily dose is 20 - 30 mg/day in 2 - 3 divided doses.

Off-label use of Buspirone in the treatment of Unipolar depression:

15 - 20 mg/day orally in two divided doses
The dose may be increased every 3 - 7 days in increments of 10 - 15 mg/day to a maximum of 60 mg/day in 2 divided doses.

Buspirone Dose in Children

Buspirone dose in children with anxiety disorders:

Children and Adolescents:
- Limited data is available.
- Most experts recommend initiating the drug at a low dose i.e. 5 mg once a day that may be increased to a maximum of 20 mg per day in two divided doses.
- In studies up to 60 mg daily buspirone has been used

Pregnancy Risk Factor B

There have been no adverse fetal events.

Use during Breastfeeding:

It is unknown if buspirone is excreted into breastmilk.
The manufacturer recommends that you stop breastfeeding while using it.

Buspirone Dose in Kidney disease:

Moderate to mild renal impairment
- Take care when using the drug in the kidney impairment.
- The manufacturer has not recommended dose adjustment.
Severe renal impairment
- It is best to avoid its use.

Buspirone Dose in Liver Disease:

Hepatic impairments mild to moderate:
- Take care when using the drug in liver disease.
- The manufacturer has not recommended dose adjustment.
Severe hepatic impairment
- It is best to avoid its use.

Common Side Effects Of Buspirone (Buspar):

Central nervous system:
- Dizziness

Less Common Side Effects Buspar:

Cardiovascular:
- Chest pain
Central nervous system:
- Drowsiness
- Headache
- Nervousness
- Confusion
- Excitement
- Numbness
- Outbursts of anger
- Abnormal dreams
- Ataxia
- Paresthesia
Dermatologic:
- Diaphoresis
- Skin rash
Gastrointestinal:
- Nausea
- Diarrhea
- Sore throat
Neuromuscular & skeletal:
- Weakness
- Musculoskeletal pain
- Tremor
Ophthalmic:
- Blurred vision
Otic:
- Tinnitus
Respiratory:
- Nasal congestion

Contraindications to Buspirone (Buspar):

The following patients are not recommended to take Buspirone:

It is an allergen that can cause allergic reactions in patients.
Monoamine oxidase inhibitors are used by patients.
Patients who receive linezolid or methyleneblue or Pimozide

Warnings and Precautions

Akathisia

Dopamine-related movement disorders such as dystonia, akathisia, and pseudoparkinsonism should be closely monitored.

CNS Depression:

CNS depression can result, which may lead to impairment of physical and higher-level mental functions.
The drug should not be used for patients who are unable to perform tasks such as driving or operating heavy machinery.

Serotonin syndrome

Serotonin syndrome, a potentially fatal condition, is mostly associated with the use of SSRIs.
Patients who have the following symptoms should be suspect:
- Mental status changes (hallucinations and agitations, delirium, and coma).
- autonomic instability: sweating, resting bradycardia/ tachycardia, and changes in blood pressure
- Neurological features (rigidity and tremor, seizures, and myoclonus).
- Gastrointestinal symptoms such as nausea, diarrhea, and vomiting.
Hepatic impairment
- It is best to avoid severe hepatic impairment and mild to moderate liver disease.
Renal impairment
- It is best to avoid severe renal impairment and mild to moderate renal disease.

Buspirone: Drug Interaction

Risk Factor C (Monitor therapy)
Alcohol (Ethyl)	CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl).
Alizapride	May enhance the CNS depressant effect of CNS Depressants.
Antiemetics (5HT3 Antagonists)	May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
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.
Aprepitant	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Bosentan	May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).
Brexanolone	CNS Depressants may enhance the CNS depressant effect of Brexanolone.
Brimonidine (Topical)	May enhance the CNS depressant effect of CNS Depressants.
Bromopride	May enhance the CNS depressant effect of CNS Depressants.
Calcium Channel Blockers (Nondihydropyridine)	May increase the serum concentration of BusPIRone. Exceptions: Bepridil.
Cannabidiol	May enhance the CNS depressant effect of CNS Depressants.
Cannabis	May enhance the CNS depressant effect of CNS Depressants.
Chlorphenesin Carbamate	May enhance the adverse/toxic effect of CNS Depressants.
Clofazimine	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
CNS Depressants	May enhance the adverse/toxic effect of other CNS Depressants.
CYP3A4 Inducers (Moderate)	May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).
CYP3A4 Inhibitors (Moderate)	May decrease the metabolism of CYP3A4 Substrates (High risk with Inhibitors).
Deferasirox	May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).
Dimethindene (Topical)	May enhance the CNS depressant effect of CNS Depressants.
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.
Dronabinol	May enhance the CNS depressant effect of CNS Depressants.
Duvelisib	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Esketamine	May enhance the CNS depressant effect of CNS Depressants.
Fosaprepitant	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Fosnetupitant	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
HydrOXYzine	May enhance the CNS depressant effect of CNS Depressants.
Ioﬂupane I 123	BusPIRone may diminish the diagnostic effect of Ioﬂupane I 123.
Ivosidenib	May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).
Kava Kava	May enhance the adverse/toxic effect of CNS Depressants.
Larotrectinib	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
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.
Magnesium Sulfate	May enhance the CNS depressant effect of CNS Depressants.
Metaxalone	May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
Methylphenidate	May enhance the adverse/toxic effect of Serotonin Modulators. Speciﬁcally, the risk of serotonin syndrome or serotonin toxicity may be increased.
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.
MetyroSINE	CNS Depressants may enhance the sedative effect of MetyroSINE.
Minocycline	May enhance the CNS depressant effect of CNS Depressants.
Mirtazapine	CNS Depressants may enhance the CNS depressant effect of Mirtazapine.
Nabilone	May enhance the CNS depressant effect of CNS Depressants.
Netupitant	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Palbociclib	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Piribedil	CNS Depressants may enhance the CNS depressant effect of Piribedil.
Pramipexole	CNS Depressants may enhance the sedative effect of Pramipexole.
Resveratrol	May increase the serum concentration of BusPIRone.
ROPINIRole	CNS Depressants may enhance the sedative effect of ROPINIRole.
Rotigotine	CNS Depressants may enhance the sedative effect of Rotigotine.
Ruﬁnamide	May enhance the adverse/toxic effect of CNS Depressants. Speciﬁcally, sleepiness and dizziness may be enhanced.
Sarilumab	May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).
Serotonin Modulators	May enhance the adverse/toxic effect of other Serotonin Modulators. The development of serotonin syndrome may occur. Exceptions: Nicergoline; Tedizolid.
Siltuximab	May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).
Simeprevir	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Tetrahydrocannabinol	May enhance the CNS depressant effect of CNS Depressants.
Tetrahydrocannabinol and Cannabidiol	May enhance the CNS depressant effect of CNS Depressants.
Tocilizumab	May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).
Trimeprazine	May enhance the CNS depressant effect of CNS Depressants.
Yohimbine	May diminish the therapeutic effect of Antianxiety Agents.
Risk Factor D (Consider therapy modification)
Blonanserin	CNS Depressants may enhance the CNS depressant effect of Blonanserin.
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.
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.
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.
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.
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).
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.
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.
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.
Flunitrazepam	CNS Depressants may enhance the CNS depressant effect of Flunitrazepam.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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 Factor X (Avoid combination)
Azelastine (Nasal)	CNS Depressants may enhance the CNS depressant effect of Azelastine (Nasal).
Bromperidol	May enhance the CNS depressant effect of CNS Depressants.
Conivaptan	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Dapoxetine	May enhance the adverse/toxic effect of Serotonin Modulators.
Fusidic Acid (Systemic)	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Idelalisib	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Methylene Blue	BusPIRone may enhance the serotonergic effect of Methylene Blue. This could result in serotonin syndrome.
Monoamine Oxidase Inhibitors	BusPIRone may enhance the adverse/toxic effect of Monoamine Oxidase Inhibitors. Speciﬁcally, blood pressure elevations been reported.
Orphenadrine	CNS Depressants may enhance the CNS depressant effect of Orphenadrine.
Oxomemazine	May enhance the CNS depressant effect of CNS Depressants.
Paraldehyde	CNS Depressants may enhance the CNS depressant effect of Paraldehyde.
Thalidomide	CNS Depressants may enhance the CNS depressant effect of Thalidomide.

Monitor:

Mental status
Symptoms of anxiety
Clinical features of serotonin syndrome.

How to take Buspirone (Buspar)?

It may be taken with or without meals regularly.

Mechanism of action of Buspirone (Buspar):

Buspirone's mechanism of action is unknown.
It is highly receptive to serotonin 5-HT-1A, 5-HT-2 receptors and has little effect on benzodiazepine GABA receptors.

Absorption: Absorption is fast and complete.

Metabolism. It goes through extensive first-pass metabolism. Only 1% of the drug makes it into the systemic circulation. It is metabolized via CYP3A4 enzymes in the liver. Buspirone is 25% active in the metabolites.

Protein Binding: 86% of the drug's total is protein-bound.

Bioavailability is increased with food intake.

Half-life elimination: It takes between 2 and 3 hours, while peak serum concentration can take approximately 40 to 90 minutes. It is excreted in the urine as metablites

International Brand Names of Buspirone:

APO-BusPIRone
CO BusPIRone
DOM-BusPIRone
GMD-Buspirione
NU-BusPIRone
PMS-BusPIRone
RIVA-BusPIRone
TEVA-BusPIRone
Actium
Ansial
Ansitec
Anxiolan
Anxiron
Anxut
Bespar
Busiral
Busone
Busp
Buspalex
Buspar
Busparium
Busper
Buspin
Buspon
Dalpas
Dergelasen
Duvaline
Exupar
Kallmiren
Loxapin
Normaton
Pasrin
Paxon
Relac
Relax
Sepirone
Seropar
Sorbon
Spamilan
Spitomin
Suxin
Travin

Buspirone brand Names in Pakistan:

Buspirone 5 mg Tablets in Pakistan
Anziron	Star Laboratories (Pvt) Ltd.
Benzodep	The Schazoo Laboratories Ltd.
Biropar	Lowitt Pharmaceuticals (Pvt) Ltd
Buspar	GlaxoSmithKline
Busron	S.J. & G. Fazul Ellahie (Pvt) Ltd.
Nanzo	Wilshire Laboratories (Pvt) Ltd.
Novatil	Xenon Pharmaceuticals (Pvt) Ltd.
Nupir	Neutro Pharma (Pvt) Ltd.
Vurinil	Century Pharmaceuticals (Pvt) Ltd.