Flupentixol

CLINICAL USE

Antipsychotic:Schizophrenia and other psychoses Depression

DOSE IN NORMAL RENAL FUNCTION

Psychosis: Oral: 3–9 mg twice daily —Deep IM: 50 mg 4 weekly – 300 mg 2 —weekly; maximum dose 400 mg weekly; 20–40 mg every 2–4 weeks may be adequate in some patientsDepression: 0.5–3 mg daily (doses above 2 mg should be in 2 divided doses, and 2nd dose should not be after 4 pm)

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :434.5 (588.8 as decanoate)

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :>95

%Excreted unchanged in urine &nbsp &nbsp : Negligible

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :12–14

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :22–36 (IM: 3–8 days)/Increased

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 &nbsp &nbsp : Dose as in normal renal function

10 to 20 &nbsp &nbsp : Dose as in normal renal function

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : Start with quarter to half of the dose and titrate slowly

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Not dialysed. Dose as in GFR <10 mL/min

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Not dialysed. Dose as in GFR <10 mL/min

HDF/high flux &nbsp :Unknown dialysability. Dose as in GFR <10 mL/min

CAV/VVHD &nbsp &nbsp &nbsp:Not dialysed. Dose as in normal renal function

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs

Alcohol: enhanced effects

Anaesthetics: enhanced hypotensive effects

Analgesics: increased risk of convulsions with tramadol; enhanced hypotensive and sedative effects with opioids

Antidepressants: increased plasma level of tricyclics

Anti-epileptics: anticonvulsant effect antagonised

Antimalarials: avoid concomitant use with artemether/lumefantrine

Antipsychotics: avoid concomitant use of clozapine with depot preparations in case of neutropenia

Antivirals: concentration possibly increased with ritonavirAnxiolytics and hypnotics: increased sedative effects

Sibutramine: increased risk of CNS toxicity – avoid concomitant useAvoid concomitant use with drugs that prolong the QT interval

ADMINISTRATION

Reconstition

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Route

Oral, IM

Rate of Administration

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Comments

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OTHER INFORMATION

May cause hypotension and sedation in renal impairmentIncreased CNS sensitivity in renally impaired patients – start with small doses as can accumulateFor IM injection a 20 mg test dose should first be givenOral bioavailability is 40–55% Peak levels occur 7 days after IM injection and 4 hours after oral administration.

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