Buspirone hydrochloride

CLINICAL USE

Anxiolytic

DOSE IN NORMAL RENAL FUNCTION

  • Initially 5 mg 2–3 times daily.
  • Usual range 15–30 mg daily in divided doses (maximum 45 mg daily)

    PHARMACOKINETICS

  • Molecular weight                           :422
  • %Protein binding                           :95
  • %Excreted unchanged in urine     : 0
  • Volume of distribution (L/kg)       :2.69–7.91
  • half-life – normal/ESRD (hrs)      :2–11/Increased by 2 hours1

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50     : Dose as in normal renal function
  • 10 to 20     : Dose as in normal renal function
  • <10           : Reduce by 25–50% if patient is anuric2

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD                :Not dialysed. Dose as in GFR <10 mL/min
  • HD                     :Not dialysed. Dose as in GFR <10 mL/min
  • HDF/high flux   :Unknown dialysability. Dose as in GFR <10 mL/min
  • CAV/VVHD      :Not dialysed. Dose as in normal renal function

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs

  • Antibacterials: concentration increased by erythromycin – reduce dose; concentration reduced by rifampicin
  • Antidepressants: risk of severe hypertension with MAOIs – avoid concomitant use
  • Antifungals: concentration increased by itraconazole – reduce dose
  • Antipsychotics: enhanced sedative effects; haloperidol concentration increased
  • Antivirals: concentration increased by ritonavir, increased risk of toxicity
  • Calcium-channel blockers: concentration increased by diltiazem and verapamil – reduce dose
  • Grapefruit juice: concentration increased by grapefruit juice – reduce dose

    ADMINISTRATION

    Reconstition

    Route

    Oral

    Rate of Administration

    Comments

    OTHER INFORMATION

  • Peak plasma levels occur 60–90 minutes after dosing
  • Steady state plasma concentrations achieved within 2 days, although response to treatment may take 2 weeks
  • Non-sedative Do not use in patients with severe hepatic disease
  • Use in severe renal impairment not recommended; risk of accumulation of active metabolites
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