Tìm theo
Carboplatin
Các tên gọi khác (6 ) :
  • Carboplatin
  • CBDCA
  • cis-(1,1-Cyclobutanedicarboxylato)diammineplatinum(ii)
  • cis-Diammine(1,1-cyclobutanedicarboxylato)platinum
  • cis-Diammine(1,1-cyclobutanedicarboxylato)platinum(II)
  • Paraplatin
Thuốc chống ung thư và tác động vào hệ thống miễn dịch
Thuốc Gốc
Small Molecule
CAS: 41575-94-4
ATC: L01XA02
ĐG : APP Pharmaceuticals , http://www.apppharma.com
CTHH: C6H12N2O4Pt
PTK: 371.254
An organoplatinum compound that possesses antineoplastic activity. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C6H12N2O4Pt
Phân tử khối
371.254
Monoisotopic mass
371.044481331
InChI
InChI=1S/C6H8O4.2H3N.Pt/c7-4(8)6(5(9)10)2-1-3-6;;;/h1-3H2,(H,7,8)(H,9,10);2*1H3;/q;;;+2/p-2
InChI Key
InChIKey=OLESAACUTLOWQZ-UHFFFAOYSA-L
IUPAC Name
6,8-dioxa-7-platinaspiro[3.5]nonane-5,9-dione diamine
Traditional IUPAC Name
6,8-dioxa-7-platinaspiro[3.5]nonane-5,9-dione diamine
SMILES
N.N.O=C1O[Pt]OC(=O)C11CCC1
logP
1.06
pKa (Strongest Basic)
-6.6
PSA
52.6 Å2
Refractivity
29.01 m3·mol-1
Polarizability
14.06 Å3
Rotatable Bond Count
0
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Dược Lực Học : Carboplatin is an antineoplastic in the class of alkylating agents and is used to treat various forms of cancer. Alkylating agents are so named because of their ability to add alkyl groups to many electronegative groups under conditions present in cells. They stop tumor growth by cross-linking guanine bases in DNA double-helix strands - directly attacking DNA. This makes the strands unable to uncoil and separate. As this is necessary in DNA replication, the cells can no longer divide. In addition, these drugs add methyl or other alkyl groups onto molecules where they do not belong which in turn inhibits their correct utilization by base pairing and causes a miscoding of DNA. Alkylating agents are cell cycle-nonspecific. Alkylating agents work by three different mechanisms all of which achieve the same end result - disruption of DNA function and cell death.
Cơ Chế Tác Dụng : An organoplatinum compound that possesses antineoplastic activity. [PubChem] Alkylating agents work by three different mechanisms: 1) attachment of alkyl groups to DNA bases, resulting in the DNA being fragmented by repair enzymes in their attempts to replace the alkylated bases, preventing DNA synthesis and RNA transcription from the affected DNA, 2) DNA damage via the formation of cross-links (bonds between atoms in the DNA) which prevents DNA from being separated for synthesis or transcription, and 3) the induction of mispairing of the nucleotides leading to mutations.
Dược Động Học :
▧ Absorption :
The Cmax values and areas under the plasma concentration versus time curves from 0 to infinity (AUC inf) increase linearly with dose, although the increase was slightly more than dose proportional. Carboplatin exhibits linear pharmacokinetics.
▧ Volume of Distribution :
* 16 L [apparent volume of distribution, 30 minute IV infusion of 300 mg/m^2 to 500 mg/m^2]
▧ Protein binding :
Carboplatin is not bound to plasma protein. However, the platinum itself from carboplatin irreversibly binds to plasma proteins and is slowly eliminated with a minimum half-life of 5 days.
▧ Route of Elimination :
The major route of elimination of carboplatin is renal excretion. After 24 hours, all of the platinum is recovered in the urine as carboplatin. Whether biliary excretion occurs is not known.
▧ Half Life :
Initial plasma half-life (alpha) = 1.1 to 2 hours; Post distribution plasma half-life (beta) = 2.6 - 5.9 hours.
▧ Clearance :
* 4.4 L/hour [total body clearance, 30 minute IV infusion of 300 mg/m^2 to 500 mg/m^2]
Độc Tính : Toxic by ingestion. May be create toxic effect through inhalation or skin contact. May cause reproductive defects. May act as a sensitizer. ORL-RAT LD50 343 mg kg-1; SCN-RAT LD50 72 mg kg-1; IPN-MUS LD50 118 mg kg-1
Chỉ Định : For the initial treatment of advanced ovarian carcinoma in established combination with other approved chemotherapeutic agents. One established combination regimen consists of PARAPLATIN and cyclophosphamide. It is also indicated for the palliative treatment of patients with ovarian carcinoma recurrent after prior chemotherapy, including patients who have been previously treated with cisplatin.
Tương Tác Thuốc :
  • Bendamustine Increases toxicity through pharmacodynamic synergism. Additive myelosuppression.
  • Docetaxel Platinum derivatives such as carboplatin may enhance the myelosuppressive effect of taxane derivatives such as docetaxel. Administer taxane derivative before platinum derivative when given as sequential infusions to limit toxicity. Administering the taxane derivative before the platinum derivative seems prudent.
  • Fosphenytoin The antineoplasic agent decreases the effect of hydantoin
  • Leflunomide Immunosuppressants such as carboplatin may enhance the adverse/toxic effect of leflunomide. Specifically, the risk for hematologic toxicity such as pancytopenia, agranulocytosis, and/or thrombocytopenia may be increased. Consider eliminating the use of a leflunomide loading dose in patients who are receiving other immunosuppressants in order to reduce the risk for serious adverse events such as hematologic toxicity. Also, patients receiving both leflunomide and another immunosuppressive medication should be monitored for bone marrow suppression at least monthly throughout the duration of concurrent therapy.
  • Natalizumab Immunosuppressants such as natalizumab may enhance the adverse/toxic effect of natalizumab. Specifically, the risk of concurrent infection may be increased. Patients receiving natalizumab should not use concurrent immunosuppressants.
  • Paclitaxel Platinum derivatives such as carboplatin may enhance the myelosuppressive effect of taxane derivatives such as paclitaxel. Administer taxane derivative before platinum derivative when given as sequential infusions to limit toxicity. Administering the taxane derivative before the platinum derivative seems prudent.
  • Phenytoin The antineoplasic agent decreases the effect of hydantoin
  • Pimecrolimus Pimecrolimus may enhance the adverse/toxic effect of immunosuppressants such as carboplatin. Avoid use of pimecrolimus cream in patients receiving immunosuppressants.
  • Roflumilast Roflumilast may enhance the immunosuppressive effect of immunosuppressants such as carboplatin. he Canadian roflumilast product monograph recommends avoiding concurrent use of roflumilast with any immunosuppressant medications due to the antiinflammatory/immune altering effects of roflumilast and the lack of relevant clinical experience with such use. Of note, this recommendation to avoid concurrent use does not apply to either inhaled corticosteroids (which have much more limited systemic immune-suppressing actions) or short-term systemic corticosteroid use. U.S. prescribing information does not contain this warning; but it appears prudent to avoid this combination when possible.
  • Sorafenib Sorafenib may enhance the adverse/toxic effect of carboplatin. Concurrent use of sorafenib with carboplatin and placlitaxel in patients with squamous cell lung cancer is contraindicated. The use of this combination in other settings is not specifically contraindicated, but any such use should be approached with added caution.
  • Tacrolimus Tacrolimus (Topical) may enhance the adverse/toxic effect of immunosuppressants such as carboplatin. Avoid use of tacrolimus ointment in patients receiving immunosuppressants.
  • Topotecan Administration of Topotecan after Carboplatin therapy may increase the risk of hematologic toxicity, such as neutropenia and/or thrombocytopenia. A dose adjustment may be required or the sequence of administration reversed.
  • Trastuzumab Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
Liều Lượng & Cách Dùng : Injection, powder, lyophilized, for solution - Intravenous - 150 mg
Injection, solution - Intravenous - 50 mg/5 mL; 150 mg/15 mL; 450 mg/45 mL; 600 mg/60 mL
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Paraplatin
  • Công ty :
    Sản phẩm biệt dược : Paraplatin-AQ
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00958
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=38904
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507170
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01363
ChemSpider
http://www.chemspider.com/Chemical-Structure.436073.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0703-3249-11
PharmGKB
http://www.pharmgkb.org/drug/PA448803
Wikipedia
http://en.wikipedia.org/wiki/Carboplatin
RxList
http://www.rxlist.com/cgi/generic3/carboplat.htm
Drugs.com
http://www.drugs.com/cdi/carboplatin.html
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