Cinacalcet

From Anvita Health Wiki

Contents 1 Introduction 2 Indications 3 Dosage 4 Pharmacokinetics 5 Monitor 6 Adverse-effects 7 Drug-interactions 8 Mechanism-of-action 9 Notes 10 More General Terms 11 Internet Database 12 References

Introduction

• Tradename: Sensipar (new 2004)

Indications

• secondary hyperparathyroidism in dialysis patients
• primary hyperparathyroidism (unlabeld use)
• parathyroid carcinoma

Dosage

• start 30 mg PO QD, administer with food
• increase every 2-4 weeks (30 mg)
• maximum dose 180 mg, 360 mg ( parathyroid carcinoma)
• no dosage adjustment in the elderly
• may be taken with vitamin D &/or phosphate binders

• Tabs: 30, 20, 90 mg

Pharmacokinetics

• metabolized by cyt P450 3A4, cyt P450 1A2 & cyt P450 2D6
• inhibits cyt P450 2D6
• volume of distribution 1000 L
• terminal 1/2life of 30-40 hours
• nadir in serum PTH (intact) level 2-6 hours after dose
• 80% excreted in the urine as inactive metabolites 15% excreted in the feces
  

• elimination by hemodialysis = -

Monitor

• serum Ca+2 prior to intiation & within 1 week of intiation or dosage adjustment
• maintanence serum Ca+2 every 2 months

Adverse-effects

• common > 10%

• hypocalcemia ( myalgia, muscle cramps)
• nausea/vomiting, diarrhea

• less common 1-10%

• hypertension (7%), dizziness (10%), seizure (1%) anorexia (6%), weakness (7%), chest pain (6%)

Drug-interactions

• cinacalcet is increased by cyt P450 3A4 inhibitors

• erythromycin, ketoconazole, grapefruit etc

• cinacalcet can inrease levels of drugs metabolized by cyt P450 2D6

• amitriptyline, fluoxetine, paroxetine, codeine

Mechanism-of-action

• calcimimetic
• increases sensitivity of parathyroid Ca+2-sensing receptors [2]
• generally normalizes parathyroid hormone, serum Ca+2 & serum phosphate

Notes

• Manufacturer: Amgen

More General Terms

• metabolic agent (metabolic modifier)

Internet Database

PubChem: 156419
PubChem: 156418

References

1. New Drug: Cinacalcet (Sensipar) Prescriber's Letter 11(4):23-24 2004 Detail-Document#: [1] (subscription needed) [2]
2. Journal Watch 24(11):90, 2004 Block GA, Martin KJ, de Francisco AL, Turner SA, Avram MM, Suranyi MG, Hercz G, Cunningham J, Abu-Alfa AK, Messa P, Coyne DW, Locatelli F, Cohen RM, Evenepoel P, Moe SM, Fournier A, Braun J, McCary LC, Zani VJ, Olson KA, Drueke TB, Goodman WG. Cinacalcet for secondary hyperparathyroidism in patients receiving hemodialysis. N Engl J Med. 2004 Apr 8;350(15):1516-25. PMID: [3]
   - Curhan G. Fooling the parathyroid gland--will there be health benefits? N Engl J Med. 2004 Apr 8;350(15):1565-7. No abstract available. PMID: [4]
3. Lexi-Comp

cinacalcet (Sensipar, Mimpara)