Tìm theo
Paliperidone
Các tên gọi khác (5 ) :
  • 9-Hydroxyrisperidone
  • Invega
  • Paliperidone
  • Ro-76477
  • SID90341688
Thuốc chống rối loạn tâm thần
Thuốc Gốc
Small Molecule
CAS: 144598-75-4
ATC: N05AX13
ĐG : Alza Corp.
CTHH: C23H27FN4O3
PTK: 426.4839
Paliperidone is the primary active metabolite of the older antipsychotic risperidone. While its specific mechanism of action is unknown, it is believed that paliperidone and risperidone act via similar if not the same pathways. It has been proposed that the drug's therapeutic activity in schizophrenia is mediated through a combination of central dopamine Type 2 (D2) and serotonin Type 2 (5HT2A) receptor antagonism. Paliperidone is also active as an antagonist at alpha 1 and alpha 2 adrenergic receptors and H1 histaminergic receptors, which may explain some of the other effects of the drug. Paliperidone was approved by the FDA for treatment of schizophrenia on December 20, 2006.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C23H27FN4O3
Phân tử khối
426.4839
Monoisotopic mass
426.206718955
InChI
InChI=1S/C23H27FN4O3/c1-14-17(23(30)28-9-2-3-19(29)22(28)25-14)8-12-27-10-6-15(7-11-27)21-18-5-4-16(24)13-20(18)31-26-21/h4-5,13,15,19,29H,2-3,6-12H2,1H3
InChI Key
InChIKey=PMXMIIMHBWHSKN-UHFFFAOYSA-N
IUPAC Name
3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-9-hydroxy-2-methyl-4H,6H,7H,8H,9H-pyrido[1,2-a]pyrimidin-4-one
Traditional IUPAC Name
3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-9-hydroxy-2-methyl-6H,7H,8H,9H-pyrido[1,2-a]pyrimidin-4-one
SMILES
CC1=C(CCN2CCC(CC2)C2=NOC3=C2C=CC(F)=C3)C(=O)N2CCCC(O)C2=N1
Độ hòa tan
Practically insoluble in water
logP
1.8
logS
-3.2
pKa (strongest acidic)
13.74
pKa (Strongest Basic)
8.76
PSA
82.17 Å2
Refractivity
116.04 m3·mol-1
Polarizability
45.95 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
5
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
5
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Paliperidone is an atypical antipsychotic developed by Janssen Pharmaceutica. Chemically, paliperidone is primary active metabolite of the older antipsychotic risperidone (paliperidone is 9-hydroxyrisperidone). While its specific mechanism of action is unknown, it is believed paliperidone and risperidone act via similar, if not the same, pathways.
Cơ Chế Tác Dụng : Paliperidone is the primary active metabolite of the older antipsychotic risperidone. While its specific mechanism of action is unknown, it is believed that paliperidone and risperidone act via similar if not the same pathways. It has been proposed that the drug's therapeutic activity in schizophrenia is mediated through a combination of central dopamine Type 2 (D2) and serotonin Type 2 (5HT2A) receptor antagonism. Paliperidone is also active as an antagonist at alpha 1 and alpha 2 adrenergic receptors and H1 histaminergic receptors, which may explain some of the other effects of the drug. Paliperidone was approved by the FDA for treatment of schizophrenia on December 20, 2006. Paliperidone is the major active metabolite of risperidone. The mechanism of action of paliperidone, as with other drugs having efficacy in schizophrenia, is unknown, but it has been proposed that the drug's therapeutic activity in schizophrenia is mediated through a combination of central dopamine Type 2 (D2) and serotonin Type 2 (5HT2A) receptor antagonism.
Dược Động Học :
▧ Absorption :
The absolute oral bioavailability of paliperidone following paliperidone administration is 28%.
▧ Volume of Distribution :
* 487 L
▧ Protein binding :
The plasma protein binding of racemic paliperidone is 74%.
▧ Metabolism :
Although in vitro studies suggested a role for CYP2D6 and CYP3A4 in the metabolism of paliperidone, in vivo results indicate that these isozymes play a limited role in the overall elimination of paliperidone. Four primary metabolic pathways have been identified in vivo, none of which could be shown to account for more than 10% of the dose: dealkylation, hydroxylation, dehydrogenation, and benzisoxazole scission. Paliperidone does not undergo extensive metabolism and a significant portion of its metabolism occurs in the kidneys.
▧ Route of Elimination :
One week following administration of a single oral dose of 1 mg immediate-release 14C-paliperidone to 5 healthy volunteers, 59% (range 51% – 67%) of the dose was excreted unchanged into urine, 32% (26% – 41%) of the dose was recovered as metabolites, and 6% – 12% of the dose was not recovered.
▧ Half Life :
The terminal elimination half-life of paliperidone is approximately 23 hours.
Độc Tính : The possibility of obtundation, seizures, or dystonic reaction of the head and neck following overdose may create a risk of aspiration with induced emesis.
Chỉ Định : For the treatment of schizophrenia.
Tương Tác Thuốc :
  • Amantadine The atypical antipsychotic agent, paliperidone, may decrease the therapeutic effect of the anti-Parkinson's agent, amantadine. This interaction may be due to the dopamine antagonist properties of paliperidone. Consider an alternate antipsychotic in those with Parkinson's disease or consider using clozapine or quetiapine if an atypical antipsychotic is necessary.
  • Apomorphine The atypical antipsychotic agent, paliperidone, may decrease the therapeutic effect of the anti-Parkinson's agent, apomorphine. This interaction may be due to the dopamine antagonist properties of paliperidone. Consider an alternate antipsychotic in those with Parkinson's disease or consider using clozapine or quetiapine if an atypical antipsychotic is necessary.
  • Bromocriptine The atypical antipsychotic agent, paliperidone, may decrease the therapeutic effect of the anti-Parkinson's agent, bromocriptine. This interaction may be due to the dopamine antagonist properties of paliperidone. Consider an alternate antipsychotic in those with Parkinson's disease or consider using clozapine or quetiapine if an atypical antipsychotic is necessary.
  • L-DOPA The atypical antipsychotic agent, paliperidone, may decrease the therapeutic effect of the anti-Parkinson's agent, levodopa. This interaction may be due to the dopamine antagonist properties of paliperidone. Consider an alternate antipsychotic in those with Parkinson's disease or consider using clozapine or quetiapine if an atypical antipsychotic is necessary.
  • Methotrimeprazine The CNS depressant agents, paliperidone and methotrimeprazine, may cause additive CNS depressant effects. Monitor for increased CNS depressant effects during concomitant therapy.
  • Metoclopramide Metoclopramide may increase the risk of extrapyramidal side effects of paliperidone. Concomitant therapy should be avoided.
  • Pramipexole The atypical antipsychotic agent, paliperidone, may decrease the therapeutic effect of the anti-Parkinson's agent, pramipexole. This interaction may be due to the dopamine antagonist properties of paliperidone. Consider an alternate antipsychotic in those with Parkinson's disease or consider using clozapine or quetiapine if an atypical antipsychotic is necessary.
  • Risperidone Paliperidone is the active metabolite of risperidone, 9-OH-risperidone. Concomitant therapy may increase the adverse effects of paliperidone due to additive paliperidone exposure. Consider alternate therapy.
  • Ropinirole The atypical antipsychotic agent, paliperidone, may decrease the therapeutic effect of the anti-Parkinson's agent, ropinirole. This interaction may be due to the dopamine antagonist properties of paliperidone. Consider an alternate antipsychotic in those with Parkinson's disease or consider using clozapine or quetiapine if an atypical antipsychotic is necessary.
  • Tacrine Tacrine, a central acetylcholinesterase inhibitor, may augment the central neurotoxic effect of antipsychotics such as Paliperidone. Monitor for extrapyramidal symptoms.
  • Tetrabenazine May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects. Similar pharmacologic properties thus combination therapy will worsen the severity of sedative, parkinsonian, and extrapyramidal adverse effects.
  • Triprolidine The CNS depressants, Triprolidine and Paliperidone, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Liều Lượng & Cách Dùng : Tablet, extended release - Oral - 3 mg
Tablet, extended release - Oral - 6 mg
Tablet, extended release - Oral - 9 mg
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Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01267
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=115237
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506296
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D05339
ChemSpider
http://www.chemspider.com/Chemical-Structure.103109.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/50458-554-01
PharmGKB
http://www.pharmgkb.org/drug/PA163518919
Wikipedia
http://en.wikipedia.org/wiki/Paliperidone
RxList
http://www.rxlist.com/cgi/generic/invega.htm
PDRhealth
http://www.pdrhealth.com/drugs/rx/rx-mono.aspx?contentFileName=inv1883.html&contentName=Invega&contentId=405
Drugs.com
http://www.drugs.com/cdi/paliperidone.html
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