Lormetazepam

CLINICAL USE

Benzodiazepine:Insomnia (short-term use)

DOSE IN NORMAL RENAL FUNCTION

0.5–1.5 mg at night

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :335.2

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :85

%Excreted unchanged in urine &nbsp &nbsp : <6 (86 as metabolites)

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :4.6

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :11–16/Unchanged

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. Start with small doses

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : Dose as in normal renal function. Start with small doses

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:Unknown dialysability. Dose as in GFR 10 to 20 mL/min

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs

Antibacterials: metabolism possibly increased by rifampicin

Antipsychotics: increased sedative effects

Antivirals: concentration possibly increased by ritonavirDisulfiram: metabolism inhibited, increased sedative effectsSodium oxybate: enhanced effect – avoid concomitant use

ADMINISTRATION

Reconstition

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Route

Oral

Rate of Administration

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Comments

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OTHER INFORMATION

Increased CNS sensitivity in renal impairmentLong-term use may lead to dependence and withdrawal symptoms in certain patientsThe half-life of the glucuronide metabolite is increased in renal impairment

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