Monograph
L01BC07 - Azacitidine |
Propably not porphyrinogenic |
PNP |
Rationale
Azacitidine is not an inhibitor, an inducer or a substrate of CYP-enzymes and it is therefore probably not porphyrinogenic. Side effects such as nausea, vomiting, stress, anxiety and insomnia may be potentially porphyrinogenic.
Chemical description
Amino ribofuranosyl triazine. One terminal and three cyclic tertiary amine functions. One furane heterocyclic component.
Therapeutic characteristics
Antineoplastic agent effective via multiple mechanisms.
Common side effects that can be confused with an acute porphyria attack are vomiting, nausea, abdominal pain, diarrhoea, obstipation and musculoskeletal pain. Other common side effects are neutropenic infections (upper respirtory tract infection, urinary infection, sinuitis, pharyngitis, rhinitis, and herpes simplex), stress, anxiety and insomnia.
Hepatic exposure
Significant
Metabolism and pharmacokinetics
In vitro studies have shown that azactidine is not an inhibitor of CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6 and CYP3A4, or an inducer of CYP1A2, CYP2C19 and CYP3A4/5 via activation of CAR or PXR nuclear receptors (Chen 2010, Keating 2012). In vitro studies have also shown that azacitidine is not metabolized by CYP450-enzymes, UDP-glucuronosyltransferases (UGTs), sulfotransferases (SULTs) and glutathione transferases (GSTs) (SPC).
Azacitidine is metabolized by cytidine deaminase (Chabner 1973) and spontaneous hydrolysis (Beisler 1978). 50-85% is excreted in urine, while less than 1% is excreted in faeces. Elimination half-life is 41 ± 8 minutes.
Similar drugs
References
| # | Citation details | PMID |
|---|---|---|
| * | Scientific articles | |
| 1. | Isolation, characterization, and properties of a labile hydrolysis product of the antitumor nucleoside, 5-azacytidine.
Beisler JA. J Med Chem. 1978 Feb;21(2):204-8. |
74412 |
| 2. | Deamination of 5-azacytidine by a human leukemia cell cytidine deaminase.
Chabner BA, Drake JC, Johns DG. Biochem Pharmacol. 1973 Nov 1;22(21):2763-5. |
|
| 3. | In vitro assessment of cytochrome P450 inhibition and induction potential of azacitidine.
Chen Y, Liu L, et al. Cancer Chemother Pharmacol. 2010 Apr;65(5):995-1000. |
20119716 |
| 4. | Azacitidine: a review of its use in the management of myelodysplastic syndromes/acute myeloid leukaemia.
Keating GM. Drugs. 2012 May 28;72(8):1111-36. |
|
| * | Summary of Product Characteristics | |
| 5. | Norwegian medicines agency. Summary of Product Characteristics (SPC). (azacitidine).
|
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Tradenames
This list comprises raw data collected from different countries.
In some cases, a more comprehensive list of available drug packages is included.
Consequently, very similar terms may therefore appear multiple times.
Bold names are the searchable terms, while the gray names that follow are all mapped to the bolded term.
Note: The cleaning is done automatically by a proprietary algorithm, and it may produce errors.
We strive to improve it continuously.
Azacitidine Accord 25 mg/ml poeder voor suspensie voor injectie · Azacitidine betapharm 25 mg/ml, poeder voor suspensie voor injectie · Azacitidine CF 25 mg/ml, poeder voor suspensie voor injectie · Azacitidine Eugia 25 mg/ml, poeder voor suspensie voor injectie · Azacitidine Eureco-Pharma 25 mg/ml, poeder voor suspensie voor injectie · Azacitidine EVER Pharma 25 mg/ml poeder voor suspensie voor injectie · Azacitidine Hikma 25 mg/ml poeder voor suspensie voor injectie · Azacitidine Kabi 25 mg/ml poeder voor suspensie voor injectie · Azacitidine Mylan 25 mg/ml, poeder voor suspensie voor injectie · Azacitidine Sandoz 25 mg/ml, poeder voor suspensie voor injectie · Azacitidine STADA 25 mg/ml, poeder voor suspensie voor injectie · Azacitidine STADA Arzneimittel 25 mg/ml, poeder voor suspensie voor injectie · Azacitidine Tillomed 25 mg/ml poeder voor suspensie voor injectie · Azacitidine Vivanta 25 mg/ml, poeder voor suspensie voor injectie · Azacitidine Zentiva 25 mg/ml, poeder voor suspensie voor injectie · Laziros 25 mg/ml, poeder voor suspensie voor injectie · Onureg 200 mg filmomhulde tabletten · Onureg 300 mg filmomhulde tabletten · Vidaza 100 mg, poeder voor suspensie voor injectie 
Azacitidin Sandoz 25 mg/ml susp. inj. (pdr.) s.c. flac. · Azacitidine Accord 25 mg/ml susp. inj. (pdr.) s.c. flac. · Azacitidine Betapharm 25 mg/ml susp. inj. (pdr.) s.c. flac. · Azacitidine EG 25 mg/ml susp. inj. (pdr.) s.c. flac. · Azacitidine Eugia 25 mg/ml susp. inj. (pdr.) s.c. flac. · Azacitidine Eurogenerics 25 mg/ml susp. inj. (pdr.) s.c. flac. · Azacitidine Hikma 25 mg/ml susp. inj. (pdr.) s.c. flac. · Azacitidine Kabi 25 mg/ml susp. inj. (pdr.) s.c. flac. · Azacitidine Mylan 25 mg/ml susp. inj. (pdr.) s.c. flac. · Onureg 200 mg compr. pellic. · Onureg 300 mg compr. pellic. · Vidaza 25 mg/ml susp. inj. (pdr.) s.c. flac. 
Azacitidina · Azacitidina Accordpharma 25 mg/ml Polvo Para Suspension Inyectable efg · Azacitidina Glenmark 25 mg/ml Polvo Para Suspension Inyectable efg · Azacitidina Kabi 25 mg/ml Polvo Para Suspension Inyectable efg · Azacitidina Mylan 25 mg/ml Polvo Para Suspension Inyectable efg · Azacitidina Sandoz 25 mg/ml Polvo Para Solucion Inyectable efg · Azacitidina Seacross 25 mg/ml Polvo Para Suspension Inyectable efg · Azacitidina Stada 25 mg/ml Polvo Para Suspension Inyectable efg · Azacitidina Zentiva 25 mg/ml Polvo Para Suspension Inyectable efg · Azacitidina Zentiva ks 25 mg/ml Polvo Para Suspension Inyectable efg · Onureg · ONUREG 200 mg COMPRIMIDOS RECUBIERTOS CON PELICULA · Vidaza 25 mg/ml Polvo Para Suspension Inyectable 
AZACITIDINA ONKO 25 mg/ml · AZACITIDINA SANDOZ 25 mg/ml · AZACITIDINA STADA 25 mg/ml · AZACITIDINE ACCORD 25 mg/ml · AZACITIDINE BETAPHARM 25 mg/ml · AZACITIDINE ZENTIVA 25 mg/ml · ETRAGA 25 mg/ml · LAZIROS 25 mg/ml · ONUREG 200 mg · ONUREG 300 mg · VIDACULEM 25 mg/ml · ZASSIDA 25 mg/ml 
Azacitidine · Onureg · Vidaza 
Azacitidin SUN · Azacitidin Tillomed · Azacitidine Accord · Azacitidine betapharm · Azacitidine EVER Pharma · Azacitidine Glenmark · Azacitidine Hikma · Azacitidine Kabi · Azacitidine Mylan · Azacitidine Sandoz · Azacitidine Stada · Azacitidine Zentiva · Etraga · Onureg · Vidaza 
Azacitidine Accord · Azacitidine betapharm · Azacitidine Stada 
Azacitidine Accord · Azacitidine Betapharm · Azacitidine Eugia · Azacitidine EVER Pharma · Azacitidine Glenmark · Azacitidine Kabi · Azacitidine Mylan · Azacitidine Onko · Azacitidine Pharmascience · Azacitidine Sandoz · Azacitidine STADA · Azacitidine Zentiva · Azculem · Etraga · Gerodaza · Onureg · Vidaza · Zassida 
Azacitidine Accord · Azacitidine EG · Azacitidine Eurogenerics · Azacitidine Kabi · Onureg · Vidaza 
Azacitidine Accord · Azacitidine Betapharm · Azacitidine Glenmark · Azacitidine Kabi · Azacitidine Mylan · Azacitidine STADA · Azacitidine STADA Arzneimittel AG · Azacitidine Zentiva · Azida · Etraga · Onureg · Vidaza · Zassida 
Azacitidine Accord · Azacitidine Betapharm · Azacitidine Glenmark · Azacitidine Hikma · Azacitidine Kabi · Azacitidine Lorien · Azacitidine Mylan · Azacitidine Sandoz · Azacitidine Stada · Azacitidine SUN · Azacitidine Tillomed · Etraga · Onureg · Vidaza 
Azacitidine Accord · Azacitidine Auxilia · Azacitidine betapharm · Azacitidine Kabi · Azacitidine Mylan · Azacitidine Seacross · Onureg · Vidaza 
Azacitidin HF · Azacitidin STADA® · Azacitidin Zentiva® · Azacitidine Accord · Vidaza®
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