Diazepam

CLINICAL USE

Benzodiazepine:Perioperative sedation (IV) Anxiolytic Muscle relaxant Status epilepticus

DOSE IN NORMAL RENAL FUNCTION

Pre-med: Oral: 5 mg, IV:

10 to 20 : mg or 100–200 mcg/kg; PR: 500 mcg/kg repeated after 12 hours as rectal solution Anxiety: Oral: 2 mg 3 times a day, increasing if necessary to 15–30 mg daily in divided doses; PR: 10–30 mg daily in divided dosesIM/IV: 5–10 mg repeated after not less than 4 hoursInsomnia: 5–15 mg at night Status epilepticus: IV: 10 mg, repeated after 10 minutes if required; PR: 500 mcg/kg

PHARMACOKINETICS

Molecular weight :284.7

%Protein binding :95–99

%Excreted unchanged in urine : <1

Volume of distribution (L/kg) :0.95–2

half-life – normal/ESRD (hrs) :24–48/Increased

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 : Dose as in normal renal function

10 to 20 : Use small doses and titrate to response

<10 : Use small doses and titrate to response

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 GFR=10–20 mL/min

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugsAntibacterials: metabolism enhanced by rifampicin; metabolism inhibited by isoniazidAntipsychotics: increased sedative effects; increased risk of hypotension, bradycardia and respiratory depression with parenteral diazepam and IM olanzapine; concentration of zotepine increasedAntivirals: increased risk of prolonged sedation with amprenavir; concentration possibly increased by ritonavirSodium oxybate: enhanced effects of sodium oxybate – avoid

ADMINISTRATION

Reconstition

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Route

IV injection, infusion, oral, PR

Rate of Administration

5 mg (1 mL)/minute

Comments

Injection can be mixed with sodium chloride 0.9% or glucose 5% to 40 mg in 500 mL

OTHER INFORMATION

Active metabolites renally excreted; therefore accumulate in renal impairmentIncreased cerebral sensitivity in renal impairment which may result in excessive sedation and encephalopathyAlways have flumazenil available to reverse effectProtein binding decreased in ERF Volume of distribution increased in ERF IV emulsion formulation (Diazemuls) less likely to cause thrombophlebitis

See how to identify renal failure stages according to GFR calculation

See how to diagnose irreversible renal disease

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