Tìm theo
Risperidone
Các tên gọi khác (8 ) :
  • Risperdal
  • risperdone
  • Risperidona
  • Risperidonum
  • Risperin
  • Rispolept
  • Rispolin
  • Sequinan
Thuốc điều trị về tâm thần
Thuốc Gốc
Small Molecule
CAS: 106266-06-2
ATC: N05AX08
ĐG : Advanced Pharmaceutical Services Inc.
CTHH: C23H27FN4O2
PTK: 410.4845
Risperidone, a benzisoxazole derivative, is an atypical antipsychotic drug with high affinity for 5-hydrotryptamine (5-HT) and dopamine D2 receptors. It is used primarily in the management of schizophrenia, inappropriate behavior in severe dementia and manic episodes associated with bipolar I disorder. Risperidone is effective for treating the positive and negative symptoms of schizophrenia owing to its affinity for its “loose” binding affinity for dopamine D2 receptors and additional 5-HT antagonism compared to first generation antipsychotics, which are strong, non-specific dopamine D2 receptor antagonists.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C23H27FN4O2
Phân tử khối
410.4845
Monoisotopic mass
410.211804333
InChI
InChI=1S/C23H27FN4O2/c1-15-18(23(29)28-10-3-2-4-21(28)25-15)9-13-27-11-7-16(8-12-27)22-19-6-5-17(24)14-20(19)30-26-22/h5-6,14,16H,2-4,7-13H2,1H3
InChI Key
InChIKey=RAPZEAPATHNIPO-UHFFFAOYSA-N
IUPAC Name
3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-2-methyl-4H,6H,7H,8H,9H-pyrido[1,2-a]pyrimidin-4-one
Traditional IUPAC Name
risperidone
SMILES
CC1=C(CCN2CCC(CC2)C2=NOC3=C2C=CC(F)=C3)C(=O)N2CCCCC2=N1
Độ tan chảy
170 °C
Độ hòa tan
2.8mg/L
logP
2.5
logS
-3.4
pKa (Strongest Basic)
8.76
PSA
61.94 Å2
Refractivity
114.55 m3·mol-1
Polarizability
45.27 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
4
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
5
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Risperidone is an atypical antipsychotic medication. It is most often used to treat delusional psychosis (including schizophrenia), but risperidone is also used to treat some forms of bipolar disorder and psychotic depression. It also has shown some success in treating symptoms of Asperger's Syndrome and autism. Risperidone is now the most commonly prescribed antipsychotic medication in the United States.
Cơ Chế Tác Dụng : Risperidone, a benzisoxazole derivative, is an atypical antipsychotic drug with high affinity for 5-hydrotryptamine (5-HT) and dopamine D2 receptors. It is used primarily in the management of schizophrenia, inappropriate behavior in severe dementia and manic episodes associated with bipolar I disorder. Risperidone is effective for treating the positive and negative symptoms of schizophrenia owing to its affinity for its “loose” binding affinity for dopamine D2 receptors and additional 5-HT antagonism compared to first generation antipsychotics, which are strong, non-specific dopamine D2 receptor antagonists. Blockade of dopaminergic D2 receptors in the limbic system alleviates positive symptoms of schizophrenia such as hallucinations, delusions, and erratic behavior and speech. Blockade of serotonergic 5-HT2 receptors in the mesocortical tract, causes an excess of dopamine and an increase in dopamine transmission, resulting in an increase in dopamine transmission and an elimination of core negative symptoms. Dopamine receptors in the nigrostriatal pathway are not affected by risperidone and extrapyramidal effects are avoided. Like other 5-HT2 antagonists, risperidone also binds at alpha(1)-adrenergic receptors and, to a lesser extent, at histamine H1 and alpha(2)-adrenergic receptors.
Dược Động Học :
▧ Absorption :
Well absorbed. The absolute oral bioavailability of risperidone is 70% (CV=25%). The relative oral bioavailability of risperidone from a tablet is 94% (CV=10%) when compared to a solution.
▧ Volume of Distribution :
* 1 to 2 L/kg
▧ Protein binding :
Risperidone, ~88% bound; 9-hydroxyrisperidone, ~77% bound.
▧ Metabolism :
Extensively metabolized by hepatic cytochrome P450 2D6 isozyme to 9-hydroxyrisperidone, which has approximately the same receptor binding affinity as risperidone. Hydroxylation is dependent on debrisoquine 4-hydroxylase and metabolism is sensitive to genetic polymorphisms in debrisoquine 4-hydroxylase. Risperidone also undergoes N-dealkylation to a lesser extent.
▧ Route of Elimination :
Risperidone is extensively metabolized in the liver.In healthy elderly subjects, renal clearance of both risperidone and 9-hydroxyrisperidone was decreased, and elimination half-lives were prolonged compared to young healthy subjects.
▧ Half Life :
20-24 hours
Độc Tính : Symptoms of overdose include drowsiness, sedation, tachycardia, hypotension, and extrapyramidal symptoms. LD50=82.1mg/kg (orally in mice).
Chỉ Định : For the treatment of schizophrenia in adults and in adolescents, ages 13 to 17, and for the short-term treatment of manic or mixed episodes of bipolar I disorder in children and adolescents ages 10 to 17. May also be used to manage symptoms of inappropriate behavior due to aggression and/or psychosis in patients with severe dementia.
Tương Tác Thuốc :
  • Artemether Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Carbamazepine Decreases the effect of risperidone
  • Donepezil Possible antagonism of action
  • Fluoxetine The SSRI, fluoxetine, increases the effect and toxicity of risperidone.
  • Galantamine Possible antagonism of action
  • Indinavir Increased risk of extrapyramidal symptoms
  • Itraconazole Increases the level of risperidone
  • Lumefantrine Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Paliperidone 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.
  • Paroxetine The SSRI, paroxetine, increases the effect and toxicity of risperidone.
  • Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor (AChEI), Tacrine, and/or the anticholinergic/antipsychotic, Risperidone, may be reduced due to antagonism. This interaction may be beneficial when the anticholinergic action is a side effect. AChEIs may also augment the central neurotoxic effect of antipsychotics. Monitor for extrapyramidal symptoms and decreased efficacy of both agents.
  • Tacrolimus Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
  • Terbinafine Terbinafine may reduce the metabolism and clearance of Risperidone. Consider alternate therapy or monitor for therapeutic/adverse effects of Risperidone if Terbinafine is initiated, discontinued or dose changed.
  • Tetrabenazine May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
  • Thiothixene May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration.
  • Toremifene Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration.
  • Trimethobenzamide Trimethobenzamide and Risperidone, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Trimipramine Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
  • Triprolidine Triprolidine and Risperidone, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Additive CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects.
  • Trospium Trospium and Risperidone, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Voriconazole Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
  • Vorinostat Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
  • Ziprasidone Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Zuclopenthixol Additive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Liều Lượng & Cách Dùng : Injection, powder, for suspension - Intramuscular - 12.5 mg
Injection, powder, for suspension - Intramuscular - 25 mg
Injection, powder, for suspension - Intramuscular - 37.5 mg
Injection, powder, for suspension - Intramuscular - 50 mg
Solution - Oral - 1 mg/ml
Tablet, film coated - Oral - 0.25 mg
Tablet, film coated - Oral - 0.5 mg
Tablet, film coated - Oral - 1 mg
Tablet, film coated - Oral - 2 mg
Tablet, film coated - Oral - 3 mg
Tablet, film coated - Oral - 4 mg
Tablet, orally disintegrating - Oral - 0.5 mg
Tablet, orally disintegrating - Oral - 1 mg
Tablet, orally disintegrating - Oral - 2 mg
Tablet, orally disintegrating - Oral - 3 mg
Tablet, orally disintegrating - Oral - 4 mg
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Janssen
    Sản phẩm biệt dược : Risperdal
  • Công ty : Janssen
    Sản phẩm biệt dược : Risperdal Consta
  • Công ty : Janssen
    Sản phẩm biệt dược : Risperdal M-Tab
  • Công ty : Janssen
    Sản phẩm biệt dược : Risperidal M-Tab
  • Công ty :
    Sản phẩm biệt dược : Risperin
  • Công ty :
    Sản phẩm biệt dược : Rispolept
  • Công ty :
    Sản phẩm biệt dược : Rispolin
  • Công ty :
    Sản phẩm biệt dược : Sequinan
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00734
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5073
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505850
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00426
ChemSpider
http://www.chemspider.com/Chemical-Structure.4895.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0904-5973-61
PharmGKB
http://www.pharmgkb.org/drug/PA451257
Wikipedia
http://en.wikipedia.org/wiki/Risperidone
RxList
http://www.rxlist.com/cgi/generic/risperid.htm
PDRhealth
http://www.pdrhealth.com/drugs/rx/rx-mono.aspx?contentFileName=ris1382.html&contentName=Risperdal&contentId=667
Drugs.com
http://www.drugs.com/risperidone.html
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