Cinacalcet

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Toxicological Effects
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Mimpara; Belgium: Mimpara; Bulgaria: Mimpara; Cyprus: Mimpara; Czech Republic: Mimpara; Denmark: Mimpara; Estonia: Mimpara; Finland: Mimpara; France: Mimpara; Germany: Mimpara; Greece: Mimpara; Hungary: Mimpara; Ireland: Mimpara; Italy: Mimpara; Latvia: Mimpara; Lithuania: Mimpara; Malta: Mimpara; Netherlands: Mimpara; Poland: Mimpara; Portugal: Mimpara; Romania: Mimpara; Slovakia: Mimpara; Slovenia: Mimpara; Spain: Mimpara; Sweden: Mimpara; UK: Mimpara.

North America

Canada: Sensipar; USA: Sensipar.

Asia

Japan: Regpara.

Drug combinations

Chemistry

Cinacalcet Hydrochloride: C~22~H~22~F~3~N.HCl. Mw: 393.87. (1) 1-Naphthalenemethanamine, α-methyl-N-[3-[3-(trifluoromethyl)phenyl]propyl]-, (αR)-, hydrochloride; (2) N-[(1R)-1-(Naphthalen-1-yl)ethyl]-3-[3-(trifluoromethyl)phenyl]propan-1-amine hydrochloride. CAS-364782-34-3; CAS-226256-56-0 (cinacalcet)(2002).

Pharmacologic Category

Other Miscellaneous Therapeutic Agents. Calcimimetic. (ATC-Code: H05BX01).

Mechanism of action

Increases the sensitivity of calcium-sensing receptors (principal regulators of PTH secretion) on the parathyroid glands to activation by extracellular calcium, thereby inhibiting PTH secretion. In dialysis, patients with secondary hyperparathyroidism, serum calcium and phosphorus concentrations usually decline as PTH concentrations decrease.

Therapeutic use

Secondary hyperparathyroidism in patients with chronic kidney disease on dialysis. Hypercalcemia in parathyroid carcinoma.

Pregnancy and lactiation implications

In animal studies, no teratogenic effects seen. There are no adequate studies in pregnant women. Not recommended during lactation.

Unlabeled use

Primary hyperparathyroidism.

Contraindications

Hypersensitivity to cinacalcet or any component of the formulation.

Warnings and precautions

Adynamic bone disease may develop if iPTH levels are suppressed. Hypocalcemia or symptoms of hypocalcemia (e.g. cramps, myalgia, paresthesia, seizure, tetany) might develop during treatment. Cinacalcet may cause a decrease in testosterone levels (free and total). Use with caution in cardiovascular disease (idiosyncratic hypotension and/or worsening of heart failure reported in impaired cardiovascular function). Use with caution in moderate-to-severe hepatic impairment (increased cinacalcet exposure and half-life). Not indicated for chronic kidney disease patients not receiving dialysis (increased incidence of hypocalcemia (<8.4 mg/dL) in patients not requiring dialysis). Use with caution in history of seizure disorder.

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