Brand name: Busp
Active ingredient (generic name): Buspirone
Manufacturer: Hexal
Importer: Behestan Darou
Pharmacotherapeutic group: anti-anxiety
Pharmaceutical form: 5mg tablets
Pharmacodynamic:
From animal studies it is known to interact with serotonin, noradrenaline (norepinephrine), acetylcholine and dopamine systems of the brain. Buspirone enhances the activity of specific noradrenergic and dopaminergic pathways, whereas the activity of serotonin and acetylcholine are reduced.
Pharmacokinetic:
Absorption: Buspirone hydrochloride is rapidly absorbed from the gastrointestinal tract reaching peak plasma concentrations within 40 to 90 minutes after administration by mouth. Systemic bioavailability is low because of extensive first-pass metabolism.
Distribution: Buspirone is about 95% bound to plasma proteins.
Metabolism: Metabolism in the liver is extensive via the cytochrome P450 isoenzyme CYP3A4. The elimination half-life of buspirone is usually about 2 to 4 hours but half-lives of up to 11 hours have been reported.
Elimination: Buspirone is excreted mainly as metabolites in the urine, and also the faeces.
Therapeutic indication:
Buspirone is indicated for the treatment of short-term management of anxiety disorders and the relief of symptoms of anxiety with or without accompanying symptoms of depression.
Dosage and administration:
Adults (including the elderly): the usual starting dosage is 5mg given two to three times per day. The dosage may be increased every 2-3 days.
Adverse reaction:
Nervous system Disorders: dizziness, headache, nervousness, light-headedness, excitement, paraesthesiae, sleep disturbances are amongst the most frequent adverse effects reported others are drowsiness, confusion, seizure and dry mouth.
Contraindication:
Buspirone is contraindicated in the following groups of patients.
• Patients with known hypersensitivity to buspirone hydrochloride or any ingredient in the tablet.
• Patients with epilepsy.
• Patients with severe renal or hepatic impairment
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Interaction with other medicines: • Antidepressants - the occurrence of elevated blood pressure in patients receiving buspirone and monoamine oxidase inhibitors (phenelzine and tranylcypromine) has been reported. Buspirone should not be used concomitantly with a MAOI. In healthy volunteers no interaction with the tricyclic antidepressant amitriptyline was seen. • Cytochrome P450 3A4 (CYP3A4) inhibitors – • Rifampicin – coadministration of rifampicin, a potent inducer of CYP3A4, with buspirone has been shown to considerably decrease the plasma concentration and pharmacodynamic effects of buspirone. Buspirone should be used with caution in combination with serotonergic drugs (including MAOIs, L-tryptophan, triptans, tramadol, linezolid, SSRIs, lithium and St. John's Wort) as there are isolated reports of serotonin syndrome occurring in patients on concomitant SSRI therapy. If this condition is suspected, treatment with buspirone should be immediately discontinued and supportive symptomatic treatment should be initiated. |
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