Tìm theo
Pipotiazine
Các tên gọi khác (4 ) :
  • Piportil
  • Pipothiazine
  • Pipotiazina
  • Pipotiazinum
phenothiazines
Thuốc Gốc
Small Molecule
CAS: 39860-99-6
ATC: N05AC04
CTHH: C24H33N3O3S2
PTK: 475.667
Pipotiazine has actions similar to those of other phenothiazines. Among the different phenothiazine derivatives, it appears to be less sedating and to have a weak propensity for causing hypotension or potentiating the effects of CNS depressants and anesthetics. However, it produces a high incidence of extra pyramidal reactions. It is used for the maintenance treatment of chronic non-agitated schizophrenic patients. Symptoms of overdose include severe extrapyramidal manifestations, hypotension, lethargy and sedation.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C24H33N3O3S2
Phân tử khối
475.667
Monoisotopic mass
475.196333317
InChI
InChI=1S/C24H33N3O3S2/c1-25(2)32(29,30)20-8-9-24-22(18-20)27(21-6-3-4-7-23(21)31-24)14-5-13-26-15-10-19(11-16-26)12-17-28/h3-4,6-9,18-19,28H,5,10-17H2,1-2H3
InChI Key
InChIKey=JOMHSQGEWSNUKU-UHFFFAOYSA-N
IUPAC Name
10-{3-[4-(2-hydroxyethyl)piperidin-1-yl]propyl}-N,N-dimethyl-10H-phenothiazine-2-sulfonamide
Traditional IUPAC Name
pipotiazine
SMILES
CN(C)S(=O)(=O)C1=CC2=C(SC3=CC=CC=C3N2CCCN2CCC(CCO)CC2)C=C1
Độ hòa tan
1.27e-02 g/l
logP
3.13
logS
-4.6
pKa (strongest acidic)
17.09
pKa (Strongest Basic)
8.86
PSA
64.09 Å2
Refractivity
134.12 m3·mol-1
Polarizability
53.17 Å3
Rotatable Bond Count
7
H Bond Acceptor Count
5
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
4
Bioavailability
1
Rule of Five
true
MDDR-Like Rule
true
Dược Lực Học : Pipotiazine has actions similar to those of other phenothiazines. Among the different phenothiazine derivatives, it appears to be less sedating and to have a weak propensity for causing hypotension or potentiating the effects of CNS depressants and anesthetics. However, it produces a high incidence of extra pyramidal reactions. It reduces activity of dopamine receptors in the limbic system. Its 5-HT antagonism helps normalize dopamine activity in the cortical regions.
Cơ Chế Tác Dụng : Pipotiazine has actions similar to those of other phenothiazines. Among the different phenothiazine derivatives, it appears to be less sedating and to have a weak propensity for causing hypotension or potentiating the effects of CNS depressants and anesthetics. However, it produces a high incidence of extra pyramidal reactions. It is used for the maintenance treatment of chronic non-agitated schizophrenic patients. Symptoms of overdose include severe extrapyramidal manifestations, hypotension, lethargy and sedation. Pipotiazine acts as an antagonist (blocking agent) on different postsysnaptic receptors -on dopaminergic-receptors (subtypes D1, D2, D3 and D4 - different antipsychotic properties on productive and unproductive symptoms), on serotonergic-receptors (5-HT1 and 5-HT2, with anxiolytic, antidepressive and antiaggressive properties as well as an attenuation of extrapypramidal side-effects, but also leading to weight gain, fall in blood pressure, sedation and ejaculation difficulties), on histaminergic-receptors (H1-receptors, sedation, antiemesis, vertigo, fall in blood pressure and weight gain), alpha1/alpha2-receptors (antisympathomimetic properties, lowering of blood pressure, reflex tachycardia, vertigo, sedation, hypersalivation and incontinence as well as sexual dysfunction, but may also attenuate pseudoparkinsonism - controversial) and finally on muscarinic (cholinergic) M1/M2-receptors (causing anticholinergic symptoms like dry mouth, blurred vision, obstipation, difficulty/inability to urinate, sinus tachycardia, ECG-changes and loss of memory, but the anticholinergic action may attenuate extrapyramidal side-effects).
Độc Tính : Symptoms of overdose include severe extrapyramidal manifestations, hypotension, lethargy and sedation.
Chỉ Định : For the maintenance treatment of chronic non-agitated schizophrenic patients.
Tương Tác Thuốc :
  • Donepezil Possible antagonism of action
  • Galantamine Possible antagonism of action
  • Telithromycin Telithromycin may reduce clearance of Pipotiazine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Pipotiazine if Telithromycin is initiated, discontinued or dose changed.
  • Terbinafine Terbinafine may reduce the metabolism and clearance of Pipotiazine. Consider alternate therapy or monitor for therapeutic/adverse effects of Pipotiazine if Terbinafine is initiated, discontinued or dose changed.
  • Triprolidine The antihistamine, Triprolidine, may increase the arrhythmogenic effect of the phenothiazine, Pipotiazine. Monitor for symptoms of ventricular arrhythmias.
  • Voriconazole Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of pipotiazine by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of pipotiazine if voriconazole is initiated, discontinued or dose changed.
Liều Lượng & Cách Dùng : Solution - Intramuscular
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Piportil L4 25 mg/ml
    Giá bán buôn : USD >17.45
    Đơn vị tính : ml
  • Biệt dược thương mại : Piportil L4 50 mg/ml
    Giá bán buôn : USD >56.19
    Đơn vị tính : ml
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Piportil L4
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01621
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=62867
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508263
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D08385
ChemSpider
http://www.chemspider.com/Chemical-Structure.56598.html
PharmGKB
http://www.pharmgkb.org/drug/PA10158
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