Cinacalcet
Cinacalcet.JPG

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                           :393.9 as hydrochloride
  • %Protein binding                           :93–97
  • %Excreted unchanged in urine     : 80
  • Volume of distribution (L/kg)       :1000 litres
  • half-life – normal/ESRD (hrs)      :30–40/Unchanged

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50     : Dose as in normal renal function
  • 10 to 20     : Dose as in normal renal function
  • <10           : Dose as in normal renal function

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD                :Not dialysed. Dose as in normal renal function
  • HD                     :Not dialysed. Dose as in normal renal function
  • HDF/high flux   :Unlikely to be dialysed. Dose as normal renal function
  • CAV/VVHD      :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

    Route

    Oral

    Rate of Administration

    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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