Thiotepa.txt

CLINICAL USE

Alkylating antineoplastic agent

DOSE IN NORMAL RENAL FUNCTION

IM, bladder and intracavitary instillations: 60 mg in single or divided doses Intrathecal: maximum 10 mg Other doses depend on indication or local protocol

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp : 189.2

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp : 10–40

%Excreted unchanged in urine &nbsp &nbsp : <2

Volume of distribution (L/kg) &nbsp &nbsp &nbsp : 0.3–1.6

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp : 2.4

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 &nbsp &nbsp : IM: Use a reduced dose with caution

10 to 20 &nbsp &nbsp : IM: Use a reduced dose with caution

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : IM: Use a reduced dose with caution

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp: Unknown dialysability. Dose as in GFR <10 mL/min

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp : Dialysed. Dose as in GFR

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : mL/ min

HDF/high flux &nbsp : Dialysed. Dose as in GFR

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : mL/ min

CAV/VVHD &nbsp &nbsp &nbsp: Dialysed. Dose as in GFR=10– 20 mL/min

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs

Antipsychotics: avoid concomitant use with clozapine Avoid concomitant use with other myelosuppressive agents

ADMINISTRATION

Reconstition

1.5 mL water for injection

Route

IV, IM, intrathecal (can be administered directly into pleural, pericardial or peritoneal cavities and as a bladder instillation)

Rate of Administration

–

Comments

–

OTHER INFORMATION

Haemorrhagic cystitis has occurred Metabolised in liver to triethylene phosphoramide (TEPA). Only traces of unchanged thiotepa and (TEPA) are excreted in the urine, together with a large proportion of metabolites (60% within 72 hours) .

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