Cinacalcet

CLINICAL USE

Calcimimetic agent:Treatment of secondary hyperparathyroidism in patients with CKD 5 on dialysisTreatment of hypercalcaemia in patients with parathyroid carcinoma

DOSE IN NORMAL RENAL FUNCTION

Secondary hyperparathyroidism: 30–180 mg once daily Parathyroid carcinoma: 30 mg twice daily increasing to a maximum of 90 mg 4 times a day

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :393.9 as hydrochloride

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :93–97

%Excreted unchanged in urine &nbsp &nbsp : 80

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :1000 litres

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :30–40/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:Not dialysed. Dose as in normal renal function

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Not dialysed. Dose as in normal renal function

HDF/high flux &nbsp :Unlikely to be dialysed. Dose as normal renal function

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

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugsAntifungals: metabolism inhibited by ketoconazoleTobacco: metabolism increased by tobacco

ADMINISTRATION

Reconstition

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Route

Oral

Rate of Administration

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Comments

Take with food or shortly after a meal

OTHER INFORMATION

Adjust dose according to response Monitor calcium levels to prevent hypocalcaemiaCan be used in combination with vitamin D analogues and phosphate bindersSteady state is achieved after 7 days Metabolised by cytochrome P450 2 D6, CYP3 A4 and CYP1 A2.

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