haloperidol

CLINICAL USE

Sedative in severe anxiety Intractable hiccup Motor tics Nausea and vomiting Schizophrenia and other psychoses

DOSE IN NORMAL RENAL FUNCTION

Anxiety: 0.5 mg twice daily Hiccup: 1.5 mg 3 times daily Nausea and vomiting: maximum 10 mg/ day in divided doses; SC infusion: 2.5–10 mg dailySchizophrenia: Oral: 1.5–5 mg 2–3 times daily, up to 30 mg daily in resistant casesIM/IV: 2–10 mg initially then every 4–8 hours; maximum 18 mg dailyDeep IM: 50–300 mg every 4 weeks; higher doses may sometimes be requiredMotor tics: 0.5–1.5 mg 3 times daily, increased according to response

PHARMACOKINETICS

Molecular weight :375.9

%Protein binding :92

%Excreted unchanged in urine : 1

Volume of distribution (L/kg) :14–21

half-life – normal/ESRD (hrs) :12–38/–

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 : Start with lower doses. For single doses use 100% of normal dose. Accumulation with repeated dosage

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 :Not dialysed. 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

Anaesthetics: enhanced hypotensive effects

Analgesics: increased risk of convulsions with tramadol; enhanced hypotensive and sedative effects with opioids; possibly severe drowsiness with indometacin

Anti-arrhythmics: increased risk of ventricular arrhythmias with anti-arrhythmics that prolong the QT interval; increased risk of ventricular arrhythmias with amiodarone – avoid concomitant use

Antibacterials: increased risk of ventricular arrhythmias with moxifloxacin – avoid concomitant use; concentration reduced by rifampicin

Antidepressants: concentration increased by fluoxetine and venlafaxine; concentration of tricyclics increased

Anti-epileptics: metabolism increased by carbamazepine, primidone and phenobarbital; lowered seizure threshold

Antimalarials: avoid concomitant use with artemether/lumefantrine

Antipsychotics: avoid concomitant use of depot formulations with clozapine (cannot be withdrawn quickly if neutropenia occurs)

Antivirals: concentration possibly increased with ritonavirAnxiolytics and hypnotics: increased sedative effects; concentration increased by buspirone

Atomoxetine: increased risk of ventricular arrhythmias

Lithium: increased risk of extrapyramidal side effects and possibly neurotoxicity

Pentamidine: increased risk of ventricular arrhythmias

Sibutramine: increased risk of CNS toxicity – avoid concomitant use

ADMINISTRATION

Reconstition

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Route

Oral, IM or IV (slow bolus)

Rate of Administration

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Comments

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OTHER INFORMATION

May cause hypotension and excessive sedationIncreased CNS sensitivity in renally impaired patients – start with small doses; metabolites may accumulateEquivalent IV/IM dose = 40% of oral dose .

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