Clomethiazole

CLINICAL USE

Alcohol withdrawal Insomnia Restlessness and agitation

DOSE IN NORMAL RENAL FUNCTION

Alcohol withdrawal: 2–4 capsules stat, then:Day 1: 3 capsules 3 or 4 times daily —Day 2: 2 capsules 3 or 4 times daily —Day 3: 1 capsule 4 times daily —Reduce over a further 4–6 days; give a —total treatment of not more than 9 daysInsomnia: 1–2 capsules at night Restlessness and agitation: 1 capsule 3 times daily

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :161.7

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :65

%Excreted unchanged in urine &nbsp &nbsp : 0.1–5

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :4–16

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :4/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

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : Dose as in normal renal function

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Unknown dialysability. Dose as in normal renal function

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Dialysed. Dose as in normal renal function

HDF/high flux &nbsp :Dialysed. Dose as in normal renal function

CAV/VVHD &nbsp &nbsp &nbsp:Dialysed. Dose as in normal renal function

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugsAntipsychotics: enhanced sedative effects Antivirals: concentration possibly increased by ritonavirCimetidine: inhibits metabolism of clomethiazole

ADMINISTRATION

Reconstition

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Route

Oral

Rate of Administration

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Comments

Syrup should be stored in a fridge

OTHER INFORMATION

Clomethiazole has a high hepatic extraction ratioIncreased cerebral sensitivity in renal impairmentManufacturers recommend caution should be observed in patients with chronic renal disease

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