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药品详细

Anisindione(茴茚二酮)

化学结构式图
中文名
茴茚二酮
英文名
Anisindione
分子式
C16H12O3
化学名
2-(4-methoxyphenyl)-2,3-dihydro-1H-indene-1,3-dione
分子量
Average: 252.2647
Monoisotopic: 252.07864425
CAS号
117-37-3
ATC分类
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Anisindione is a synthetic anticoagulant and an indanedione derivative. It prevents the formation of active procoagulation factors II, VII, IX, and X, as well as the anticoagulant proteins C and S, in the liver by inhibiting the vitamin K-mediated gamma-carboxylation of precursor proteins.

生产厂家
  • Schering corp sub schering plough corp
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. CONNELL WF, MAYER GA: Evaluation of anticoagulant therapy with anisindione (miradon). Can Med Assoc J. 1959 May 15;80(10):785-90. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Indanes
Substructures
  • Indanes
  • Phenols and Derivatives
  • Ethers
  • Benzene and Derivatives
  • Aromatic compounds
  • Anisoles
  • Benzoyl Derivatives
  • Phenyl Esters
  • Ketones
适应症
药理
Indication For the prophylaxis and treatment of venous thrombosis and its extension, the treatment of atrial fibrillation with embolization, the prophylaxis and treatment of pulmonary embolism, and as an adjunct in the treatment of coronary occlusion.
Pharmacodynamics Anisindione is a synthetic anticoagulant and an indanedione derivative. It is prescribed only if you cannot take coumarin-type anticoagulants such as coumadin as anisindione is a powerful drug with serious potential side effects. Anticoagulants decrease the clotting ability of the blood and therefore help to prevent harmful clots from forming in the blood vessels. These medicines are sometimes called blood thinners, although they do not actually thin the blood. They also will not dissolve clots that already have formed, but they may prevent the clots from becoming larger and causing more serious problems.
Mechanism of action Like phenindione, to which it is related chemically, anisindione exercises its therapeutic action by reducing the prothrombin activity of the blood. Anisindione prevents the formation of active procoagulation factors II, VII, IX, and X, as well as the anticoagulant proteins C and S, in the liver by inhibiting the vitamin K–mediated gamma-carboxylation of precursor proteins. Anisindione has no direct thrombolytic effect and does not reverse ischemic tissue damage, although it may limit extension of existing thrombi and prevent secondary thromboembolic complications.
Absorption Accumulation does not occur with repeated dosing.
Volume of distribution Not Available
Protein binding Not Known
Metabolism
Not Available
Route of elimination Not Available
Half life Not Known
Clearance Not Available
Toxicity An overdose is likely to cause abnormal bleeding, for which the symptoms include: bleeding from gums or nose, blood in urine or stools, excessive bleeding from minor cuts, patches of discoloration or bruises on the skin.
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 156.5 °C PhysProp
water solubility 79.8 mg/L Not Available
logP 2.88 SANGSTER (1993)
Predicted Properties
Property Value Source
water solubility 1.28e-02 g/l ALOGPS
logP 2.99 ALOGPS
logP 2.72 ChemAxon
logS -4.3 ALOGPS
pKa (strongest acidic) 4.5 ChemAxon
pKa (strongest basic) -4.8 ChemAxon
physiological charge -1 ChemAxon
hydrogen acceptor count 3 ChemAxon
hydrogen donor count 0 ChemAxon
polar surface area 43.37 ChemAxon
rotatable bond count 2 ChemAxon
refractivity 71.7 ChemAxon
polarizability 26.3 ChemAxon
药物相互作用
Drug Interaction
Acetaminophen Acetaminophen increases the anticoagulant effect of anisindione. Monitor for changes in the therapeutic and adverse effects of anisindione if acetaminophen is initiated, discontinued or dose changed.
Acetylsalicylic acid Acetylsalicylic acid increases effect of the anticoagulant, anisindione.
Allopurinol Allopurinol may increase the anticoagulant effect of anisindione.
Aminoglutethimide Aminoglutethimide may decrease the anticoagulant effect of anisindione.
Amiodarone Amiodarone may increase the anticoagulant effect of anisindione.
Amprenavir Amprenavir may increase the anticoagulant effect of anisindione by increasing its serum concentration.
Aprepitant Aprepitant may decrease the anticoagulant effect of anisindione by decreasing its serum concentration.
Atazanavir The protease inhibitor, atazanavir, may increase the anticoagulant effect of anisindione.
Azathioprine Azathioprine may decrease the anticoagulant effect of anisindione.
Azithromycin Azithromycin may increase the anticoagulant effect of anisindione by increasing its serum concentration.
Betamethasone The corticosteroid, betamethasone, alters the anticoagulant effect of anisindione.
Bosentan Bosentan may decrease the anticoagulant effect of anisindione by increasing its metabolism.
Capecitabine Capecitabine may increase the anticoagulant effect of anisindione by increasing its serum concentration.
Carbamazepine Carbamazepine may decrease the anticoagulant effect of anisindione by decreasing its serum concentration.
Cefotetan The cephalosporin, cefotetan, may increase the anticoagulant effect of anisindione.
Cefoxitin The cephalosporin, cefoxitin, may increase the anticoagulant effect of anisindione.
Ceftriaxone The cephalosporin, ceftriaxone, may increase the anticoagulant effect of anisindione.
Celecoxib Celecoxib may increase the anticoagulant effect of anisindione.
Cholestyramine The bile acid sequestrant, cholestyramine, may decrease the anticoagulant effect of anisindione by decreasing its absorption.
Cimetidine Cimetidine may increase the anticoagulant effect of anisindione.
Ciprofloxacin The quinolone antibiotic, ciprofloxacin, may increase the anticoagulant effect of anisindione.
Cisapride Cisapride may increase the anticoagulant effect of anisindione.
Citalopram The SSRI, citalopram, increases the effect of anticoagulant, anisindione.
Clarithromycin The macrolide, clarithromycin, may increase the anticoagulant effect of anisindione.
Clofibrate The fibrate increases the anticoagulant effect
Colestipol The bile acid sequestrant, colestipol, may decrease the anticoagulant effect of anisindione by decreasing its absorption.
Cyclophosphamide The antineoplastic agent, cyclophosphamide may alter the anticoagulant effect of anisindione.
Danazol The androgen, danazol, may increase the anticoagulant effect of anisindione.
Demeclocycline The tetracycline, demeclocycline, may increase the anticoagulant effect of anisindione.
Dexamethasone The corticosteroid, dexamethasone, alters the anticoagulant effect of anisindione.
Dextrothyroxine The thyroid hormone, dextrothyroxine, increase the anticoagulant effect of anisindione.
Diclofenac The NSAID, diclofenac, may increase the anticoagulant effect of anisindione.
Dicloxacillin Dicloxacillin may decrease the anticoagulant effect of anisindione.
Diflunisal The NSAID, diflunisal, may increase the anticoagulant effect of anisindione.
Disulfiram Disulfiram may increase the anticoagulant effect of anisindione.
Doxycycline The tetracycline, doxycycline, may increase the anticoagulant effect of anisindione.
Erythromycin The macrolide, erythromycin, may increase the anticoagulant effect of anisindione.
Ethchlorvynol Ethchlorvynol may decrease the anticoagulant effect of anisindione.
Ethinyl Estradiol Increased thrombotic risk due to estrogen
Etodolac The NSAID, etodolac, may increase the anticoagulant effect of anisindione.
Etoricoxib Etoricoxib may increase the anticoagulant effect of anisindione.
Fenofibrate Fenofibrate may increase the anticoagulant effect of anisindione.
Fenoprofen The NSAID, fenoprofen, may increase the anticoagulant effect of anisindione.
Fluconazole Fluconazole may increase the serum concentration of anisindione by decreasing its metabolism.
Fludrocortisone The corticosteroid, fludrocortisone, alters the anticoagulant effect of anisindione.
Fluorouracil The antineoplasic agent, fluorouracil, may increase the anticoagulant effect of anisindione.
Fluoxetine The SSRI, fluoxetine, increases the effect of anticoagulant, anisindione.
Fluoxymesterone The androgen, fluoxymesterone, may increase the anticoagulant effect of anisindione.
Flurbiprofen The NSAID, flurbiprofen, may increase the anticoagulant effect anisindione.
Fluvastatin Fluvastatin may increase the anticoagulant effect of anisindione. Monitor for changes in the therapeutic and adverse effects of anisindione if fluvastatin if initiated, discontinued or dose changed.
Fluvoxamine Fluvoxamine may increase the anticoagulant effect of anisindione by increasing its serum concentration.
Fosamprenavir The protease inhibitor, fosamprenavir, may increase the anticoagulant effect of anisindione.
Fosphenytoin Increased hydantoin levels and risk of bleeding
Gefitinib Gefitinib may increase the anticoagulant effect of anisindione.
Gemcitabine Gemcitabine may increase the anticoagulant effect of anisindione.
Gemfibrozil Gemfibrozil may increase the anticoagulant effect of anisindione.
Glutethimide Glutethimide may decrease the anticoagulant effect of anisindione.
Griseofulvin Griseofulvin may decrease the anticoagulant effect of anisindione.
Hydrocortisone The corticosteroid, hydrocortisone, alters the anticoagulant effect of anisindione.
Ibuprofen The NSAID, ibuprofen, may increase the anticoagulant effect of anisindione.
Imatinib Imatinib may increase the anticoagulant effect of anisindione.
Indinavir The protease inhibitor, indinavir, may increase the anticoagulant effect of anisindione.
Indomethacin The NSAID, indomethacin, may increase the anticoagulant effect of anisindione.
Isoniazid Isoniazid may increase the anticoagulant effect of anisindione.
Itraconazole Itraconazole may increase the anticoagulant effect of anisindione.
Ketoconazole Ketoconazole may increase the anticoagulant effect of anisindione.
Ketoprofen The NSAID, ketoprofen, may increase the anticoagulant effect of anisindione.
Ketorolac The NSAID, ketorolac, may increase the anticoagulant effect of anisindione.
Leflunomide Leflunomide may increase the anticoagulant effect of anisindione.
Levamisole Levamisole may increase the anticoagulant effect of anisindione.
Levofloxacin The quinolone antibiotic, levofloxacin, may increase the anticoagulant effect of anisindione.
Levothyroxine The thyroid hormone, levothyroxine, increase the anticoagulant effect of anisindione.
Lovastatin Lovastatin may increase the anticoagulant effect of anisindione. Monitor for changes in the therapeutic and adverse effects of anisindione if lovastatin if initiated, discontinued or dose changed.
Lumiracoxib Lumiracoxib may increase the anticoagulant effect of anisindione.
Medroxyprogesterone Medroxyprogesterone may increase the anticoagulant effect of anisindione.
Mefenamic acid The NSAID, mefanamic acid, may increase the anticoagulant effect of anisindione.
Mefloquine Mefloquine may increase the anticoagulant effect of anisindione.
Meloxicam Meloxicam may increase the anticoagulant effect of anisindione.
Mercaptopurine Mercaptopurine may decrease the anticoagulant effect of anisindione.
Methimazole The antithyroid agent, methimazole, may decrease the anticoagulant effect of anisindione.
Metronidazole Metronidazole may increase the anticoagulant effect of anisindione.
Miconazole Miconazole may increase the serum concentration of anisindione by decreasing its metabolism.
Minocycline The tetracycline, minocycline, may increase the anticoagulant effect of anisindione.
Mitotane Mitotane may decrease the anticoagulant effect of anisindione.
Moxifloxacin The quinolone antibiotic, moxifloxacin, may increase the anticoagulant effect of anisindione.
Nabumetone The NSAID, nabumetone, may increase the anticoagulant effect anisindione.
Nalidixic Acid The quinolone antibiotic, nalidixic acid, may increase the anticoagulant effect of anisindione.
Naproxen The NSAID, naproxen, may increase the anticoagulant effect of anisindione.
Nelfinavir The protease inhibitor, nelfinavir, may increase the anticoagulant effect of anisindione.
Nevirapine Nevirapine may decrease the anticoagulant effect of anisindione.
Norfloxacin The quinolone antibiotic, norfloxacin, may increase the anticoagulant effect of anisindione.
Ofloxacin The quinolone antibiotic, ofloxacin, may increase the anticoagulant effect of anisindione.
Orlistat Orlistat may increase the anticoagulant effect of anisindione.
Oxaprozin The NSAID, oxaprozin, may increase the anticoagulant effect of anisinodione.
Oxyphenbutazone The NSAID, oxyphenbutazone, may increase the anticoagulant effect of anisindione.
Paroxetine The SSRI, paroxetine, increases the effect of the anticoagulant, anisindione.
Pentoxifylline Pentoxifylline may increase the anticoagulant effect of anisindione.
Phenobarbital The barbiturate, phenobarbital, decreases the anticoagulant effect of anisindione.
Phenylbutazone The NSAID, phenylbutazone, may increase the anticoagulant effect of anisindione.
Phenytoin Increased hydantoin levels and risk of bleeding
Piroxicam The NSAID, piroxicam, may increase the anticoagulant effect of anisindione.
Prednisolone The corticosteroid, prednisolone, alters the anticoagulant effect of anisindione.
Prednisone The corticosteroid, prednisone, alters the anticoagulant effect of anisindione.
Primidone The barbiturate, primidone, decreases the anticoagulant effect of anisindione.
Propafenone Propafenone may increase the anticoagulant effect of anisindione.
Propoxyphene Propoxyphene may increase the anticoagulant effect of anisindione.
Propylthiouracil The anti-thyroid agent, propylthiouracil, may decrease the anticoagulant effect of anisindione.
Quinidine Quinidine may increase the anticoagulant effect of anisindione.
Quinine Quinine may increase the anticoagulant effect of anisindione.
Ranitidine Ranitidine may increase the anticoagulant effect of anisindione. (Conflicting evidence)
Rifabutin Rifabutin, may decrease the anticoagulant effect of anisindione.
Rifampin Rifampin may decrease the anticoagulant effect of anisindione.
Telithromycin Telithromycin may increase the anticoagulant effect of anisindione.
Tenoxicam The NSAID, tenoxicam, may increase the anticoagulant effect of anisindione.
Testosterone The androgen may increase the anticoagulant effect of anisindione.
Tetracycline Tetracycline may increase the anticoagulant effect of anisindione.
Tigecycline Tigecycline may increase the anticoagulant effect of anisindione.
Triamcinolone The corticosteroid, triamcinolone, alters the anticoagulant effect of anisindione.
食物相互作用
Not Available

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