Buspirone

Registered South African indications:

• Anxiety disorders

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Severe renal impairment
• Severe hepatic impairment
• Epilepsy
• Acute intoxication with alcohol, hypnotics, analgesics, or antipsychotic agents

Cautions

• Pregnancy
• Breastfeeding
• Mild to moderate renal impairment
• Mild to moderate hepatic impairment
• Acute closed angle glaucoma
• Myasthenia gravis
• Drug dependence
• Monotherapy for depression
• Children
• Galactose intolerance
• Lapp lactase deficiency 
• Glucose–galactose malabsorption

Forms avail. in SA and covered in this monograph: tab

Anxiety disorders
- With or without accompanying depression 

• Oral (tab): Initial: 5mg, 8-12hrly; Titrate by 5mg at 2-3 day intervals; Maintenance: 20-30mg/day, in divided doses; Max: 60mg/24hrs

Indicated for short term use only

May take 2-3 weeks for effect to be evident

Not established for use in children below 18 years

Pregnancy

• Caution; no evidence of risk in studies
• There are no or limited amount of data from the use of buspirone in pregnant women. Adverse effects have been reported only after the administration of high doses of buspirone. Animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity. As a precautionary measure, it is preferable to avoid the use of buspirone during pregnancy. The effect of buspirone on labour and delivery is unknown

Breastfeeding

• Caution; not recommended
• It is unknown whether buspirone or its metabolite/metabolites are excreted in human milk. A decision must be made whether to discontinue breastfeeding or to discontinue/abstain from buspirone therapy taking into account the benefit of breastfeeding for the child and the benefit of therapy for the woman

Renal Impairment

• Mild to moderate: Caution; no dose adjustment recommended Recommendation: Administer low dose, twice daily
• Severe: Contraindicated

Hepatic Impairment

• Mild to moderate: Caution; no dose adjustment recommended  
  Individual dosages should be titrated with care to reduce the chance of central undesirable effects
• Severe: Contraindicated

Elderly

• No dose adjustment recommended

Porphyria Information

• Probably not porphyrinogenic (PNP)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Fatigue
• Dizziness
• Headache
• Somnolence
• Paraesthesia
• Abnormal coordination 
• Tremor
• Serotonin syndrome
• Seizures 
• Extrapyramidal disorder
• Cogwheel rigidity
• Dyskinesia
• Dystonia
• Syncope
• Amnesia
• Ataxias
• Parkinsonism
• Akathisia
• Restless leg syndrome
• Restlessness
• Nervousness
• Insomnia
• Disturbance in attention
• Depression
• Confusional state
• Sleep disorder
• Anger
• Psychotic disorder
• Hallucination
• Depersonalization
• Labile affect 

Cardiovascular Disorders

• Tachycardia
• Chest pain

Respiratory Disorders

• Nasal congestion
• Pharyngolaryngeal pain

Gastrointestinal Disorders

• Nausea and vomiting
• Abdominal pain
• Dry mouth
• Diarrhoea
• Constipation

Genitourinary Disorders

• Urinary retention

Endocrine and Metabolic Disorders

• Galactorrhoea

Musculoskeletal Disorders

• Musculoskeletal pain

Skin and Subcutaneous Tissue Disorders

• Cold sweats
• Rash
• Angioneurotic oedema
• Ecchymosis
• Urticaria

Sensory Disorders 

• Blurred vision 
• Tinnitus 
• Tunnel vision

• Monoamine oxidase inhibitors
• Alcohol
• Central nervous system - active agents
• Erythromycin
• Itraconazole
• Diltiazem
• Verapamil
• Rifampicin
• Antidepressants 
• Baclofen
• Lofexidine
• Nabilone
• Antihistamines
• Selective serotonin reuptake inhibitors
• Protein bound agents
• Nefazodone
• Grapefruit juice
• CYP3A4 inhibitors
• CYP3A4 inducers
• Fluvoxamine
• Trazodone
• Cimetidine
• Nordiazepam
• Haloperidol
• Digoxin
• Warfarin
  

None routine

Buspirone hydrochloride is an anxiolytic agent. The exact mechanism of buspirone's anxiolytic action in humans is not fully understood. Buspirone does not act through a benzodiazepine receptor mechanism. Buspirone has been shown to have a high affinity for serotonin 5HT1A receptors in the dorsal rophe neurons and a moderate affinity for brain D2 dopamine receptors.

Tablet 10mg

• Pasrin (Pharmacare)