Monograph
H05BX01 - Cinacalcet |
Propably not porphyrinogenic |
PNP |
Important Information
Risk for gastrointestinal adverse events in the form of nausea and vomiting motivates vigilance against insufficient intake of food, especially of carbohydrate.
Side effects
Common adverse reactions of cinacalcet that can be confused with an acute porphyric attack are nausea and vomiting. These side effects may potentially be porphyrinogenic if leading to a decrease in carbohydrate intake.
Rationale
Cinacalcet is a not an inducer or a mechanism-based inhibitor of CYP enzymes and is therefore probably not porphyrinogenic.
Chemical description
Cinacalcet is a trifluorometyl phenyl propyl naphthalene methanamine.
Therapeutic characteristics
Cinacalcet is a calcimimetic drug indicated for patients with secondary hyperparathyroidism (HPT) in advanced renal insufficiency under treatment in chronic dialysis, parathyroid carcinoma or primary HPT where operation is unsuitable or contraindicated.
It is administered orally and has a terminal elimination half-life of 30 to 40 hours.
Metabolism and pharmacokinetics
Cinacalet is metabolized by multiple CYP enzymes, primarily CYP3A4, CYP1A2 and CYP2D6.
The major routes of metabolism are N-dealkylation, leading to carboxylic acid derivatives, and oxidation of the naphthalene ring system to form dihydrodiols. The oxidative metabolites are conjugated before elimination (Pandhi 2009).
Strong, competitive inhibition of CYP 2D6 is shown in vitro and in vivo (Harris 2007, Nakashima 2007, SPC).
Based on in vitro data cinacalcet does not inhibit other CYP enzymes at concentrations achieved clinically, including CYP1A2, CYP2C8, CYP2C9, CYP2C19, and CYP3A4 and it does not induce CYP1A2, CYP2C19 and CYP3A4 (SPC). In vivo data indicates that cinacalcet does not affect the metabolism of substrates of CYP3A4, CYP1A2 or CYP2C9 (pandhi 2009, SPC).
References
# | Citation details | PMID |
---|---|---|
* | Scientific articles | |
1. | Pharmacokinetics of desipramine HCl when administered with cinacalcet HCl.
Harris RZ, Salfi M et al. Eur J Clin Pharmacol. 2007 Feb;63(2):159-63. |
16680561 |
2. | Effect of cinacalcet hydrochloride, a new calcimimetic agent, on the pharmacokinetics of dextromethorphan: in vitro and clinical studies.
Nakashima D, Takama H et al. J Clin Pharmacol. 2007 Oct;47(10):1311-9. |
17652181 |
3. | Clinical pharmacokinetic and pharmacodynamic profile of cinacalcet hydrochloride.
Padhi D, Harris R. Clin Pharmacokinet. 2009;48(5):303-11. Review. |
19566113 |
* | Summary of Product Characteristics | |
4. | The electronic Medicines Compendium (emc). Summary of Product Characteristics (SPC). Mimpara. (Last edition:
July.2014). |
Similar drugs
Tradenames and packages
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Netherlands
CALCEDEM · CALCEDEM 30 mg filmomhulde tabletten · CALCEDEM 60 mg filmomhulde tabletten · CALCEDEM 90 mg filmomhulde tabletten · Cinacalcet · Cinacalcet 30 mg Teva, filmomhulde tabletten · Cinacalcet 60 mg Teva, filmomhulde tabletten · Cinacalcet 90 mg Teva, filmomhulde tabletten · Cinacalcet Accord 30 mg filmomhulde tabletten · Cinacalcet Accord 60 mg filmomhulde tabletten · Cinacalcet Accord 90 mg filmomhulde tabletten · Cinacalcet Accordpharma 30 mg, filmomhulde tablet · Cinacalcet Accordpharma 60 mg, filmomhulde tablet · Cinacalcet Accordpharma 90 mg, filmomhulde tablet · Cinacalcet Amarox 30 mg filmomhulde tabletten · Cinacalcet Amarox 60 mg filmomhulde tabletten · Cinacalcet Amarox 90 mg filmomhulde tabletten · Cinacalcet Aristo 30 mg, filmomhulde tabletten · Cinacalcet Aristo 60 mg, filmomhulde tabletten · Cinacalcet Aristo 90 mg, filmomhulde tabletten · Cinacalcet Aurobindo 30 mg, filmomhulde tabletten · Cinacalcet Aurobindo 60 mg, filmomhulde tabletten · Cinacalcet Aurobindo 90 mg, filmomhulde tabletten · Cinacalcet CF 30 mg, filmomhulde tabletten · Cinacalcet CF 60 mg, filmomhulde tabletten · Cinacalcet CF 90 mg, filmomhulde tabletten · Cinacalcet Devatis 30 mg filmomhulde tabletten · Cinacalcet Devatis 60 mg filmomhulde tabletten · Cinacalcet Devatis 90 mg filmomhulde tabletten · Cinacalcet DOC 30 mg, filmomhulde tabletten · Cinacalcet DOC 60 mg, filmomhulde tabletten · Cinacalcet DOC 90 mg, filmomhulde tabletten · Cinacalcet Genepharm 30 mg filmomhulde tabletten · Cinacalcet Genepharm 60 mg filmomhulde tabletten · Cinacalcet Genepharm 90 mg filmomhulde tabletten · Cinacalcet Genthon 30 mg, filmomhulde tabletten · Cinacalcet Genthon 60 mg, filmomhulde tabletten · Cinacalcet Genthon 90 mg, filmomhulde tabletten · Cinacalcet Glenmark 30 mg filmomhulde tabletten · Cinacalcet Glenmark 60 mg filmomhulde tabletten · Cinacalcet Glenmark 90 mg filmomhulde tabletten · Cinacalcet Heaton 30 mg, filmomhulde tabletten · Cinacalcet Heaton 60 mg, filmomhulde tabletten · Cinacalcet Hetero 30 mg filmomhulde tabletten · Cinacalcet Hetero 60 mg filmomhulde tabletten · Cinacalcet Hetero 90 mg filmomhulde tabletten · Cinacalcet Macleods 30 mg filmomhulde tabletten · Cinacalcet Macleods 60 mg filmomhulde tabletten · Cinacalcet Macleods 90 mg filmomhulde tabletten · Cinacalcet Mylan 30 mg, filmomhulde tabletten · Cinacalcet Mylan 60 mg, filmomhulde tabletten · Cinacalcet Mylan 90 mg, filmomhulde tabletten · Cinacalcet Pharmazac 30 mg, filmomhulde tabletten · Cinacalcet Pharmazac 60 mg, filmomhulde tabletten · Cinacalcet Pharmazac 90 mg, filmomhulde tabletten · Cinacalcet Rafarm 30 mg filmomhulde tabletten · Cinacalcet Rafarm 60 mg filmomhulde tabletten · Cinacalcet Rafarm 90 mg filmomhulde tabletten · Cinacalcet Reddy 30 mg filmomhulde tabletten · Cinacalcet Reddy 60 mg filmomhulde tabletten · Cinacalcet Reddy 90 mg filmomhulde tabletten · Cinacalcet Will Pharma 30 mg, filmomhulde tabletten · Cinacalcet Will Pharma 60 mg, filmomhulde tabletten · Cinacalcet Will Pharma 90 mg, filmomhulde tabletten · Cinglan · Cinglan 30 mg filmomhulde tabletten · Cinglan 60 mg filmomhulde tabletten · Cinglan 90 mg filmomhulde tabletten · Mimpara · Mimpara 1 mg granulaat in capsules om te openen · Mimpara 2,5 mg granulaat in capsules om te openen · Mimpara 30 mg, filmomhulde tabletten · Mimpara 5 mg granulaat in capsules om te openen · Mimpara 60 mg, filmomhulde tabletten · Mimpara 90 mg, filmomhulde tablettenBelgium
Cinacalcet · Cinacalcet AB 30 mg compr. pellic. · Cinacalcet AB 60 mg compr. pellic. · Cinacalcet AB 90 mg compr. pellic. · Cinacalcet Accordpharma 30 mg compr. pellic. · Cinacalcet Accordpharma 60 mg compr. pellic. · Cinacalcet Accordpharma 90 mg compr. pellic. · Cinacalcet Viatris 30 mg compr. pellic. · Cinacalcet Viatris 60 mg compr. pellic. · Cinacalcet Viatris 90 mg compr. pellic. · Mimpara · Mimpara 1 mg gran. · Mimpara 2.5 mg gran. · Mimpara 30 mg compr. pellic. · Mimpara 5 mg gran. · Mimpara 60 mg compr. pellic. · Mimpara 90 mg compr. pellic.United Kingdom
Cinacalcet · Cinacalcet 30mg tablets · Cinacalcet 60mg tablets · Cinacalcet 90mg tablets · Mimpara · Mimpara 1mg granules in capsules for opening · Mimpara 2.5mg granules in capsules for opening · Mimpara 30mg tablets · Mimpara 5mg granules in capsules for opening · Mimpara 60mg tablets · Mimpara 90mg tabletsDenmark
Cinacalcet · Cinacalcet "Accord" · Cinacalcet "Accordpharma" · Cinacalcet "Amarox" · Cinacalcet "Glenmark" · Cinacalcet "Mylan" · Cinacalcet "Nordic Prime" · Cinacalcet "Orion" · Cinacalcet "Sandoz" · Cinacalcet "Sigillata" · Cinacalcet "Stada" · Cinacalcet "Teva" · MimparaNorway
Cinacalcet Accordpharma · Cinacalcet Mylan · Cinacalcet STADAPoland
Cinacalcet Accord · Cinacalcet Accordpharma · Cinacalcet Aristo · Cinacalcet Aurovitas · Cinacalcet Mylan · Cinacalcet Reddy · Cinacalcet Sandoz · Micalcet · MimparaLuxembourg
MIMPARA · MIMPARA-30 · MIMPARA-60 · MIMPARA-90Iceland
Cinacalcet · Cinacalcet Accord · Cinacalcet Accordpharma · Cinacalcet Mylan · Cinacalcet STADA · Cinacalcet WH · MimparaFinland
Cinacalcet · Cinacalcet Mylan · Cinacalcet Accord · Cinacalcet Accordpharma · Cinacalcet Orion · Cinacalcet Stada · Cinacalcet Viatris · Mimpara · SinafexLatvia
Cinacalcet · Cinacalcet Accord · Cinacalcet Accordpharma · Cinacalcet Mylan · MimparaSerbia
Cineset · Cineset®
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