チクロピジン
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2014/01/20 00:45:06」(JST)
[Wiki en表示]
|
This article does not cite any references or sources. Please help improve this article by adding citations to reliable sources. Unsourced material may be challenged and removed. (December 2009) |
Ticlopidine
|
|
Systematic (IUPAC) name |
5-(2-chlorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine |
Clinical data |
Trade names |
Ticlid |
AHFS/Drugs.com |
monograph |
MedlinePlus |
a695036 |
Pregnancy cat. |
B1 (AU) C (US) |
Legal status |
? |
Routes |
Oral |
Pharmacokinetic data |
Bioavailability |
>80% |
Protein binding |
98% |
Metabolism |
Hepatic |
Half-life |
*12 hours (single dose) |
Excretion |
Renal and fecal |
Identifiers |
CAS number |
55142-85-3 Y |
ATC code |
B01AC05 |
PubChem |
CID 5472 |
DrugBank |
DB00208 |
ChemSpider |
5273 Y |
UNII |
OM90ZUW7M1 Y |
KEGG |
D08594 Y |
ChEBI |
CHEBI:9588 Y |
ChEMBL |
CHEMBL833 Y |
Chemical data |
Formula |
C14H14ClNS |
Mol. mass |
263.786 g/mol |
SMILES
- Clc1ccccc1CN3Cc2c(scc2)CC3
|
InChI
-
InChI=1S/C14H14ClNS/c15-13-4-2-1-3-11(13)9-16-7-5-14-12(10-16)6-8-17-14/h1-4,6,8H,5,7,9-10H2 Y
Key:PHWBOXQYWZNQIN-UHFFFAOYSA-N Y
|
Y (what is this?) (verify) |
Ticlopidine (trade name Ticlid) is an antiplatelet drug in the thienopyridine family. Like clopidogrel, it is an adenosine diphosphate (ADP) receptor inhibitor. It is used in patients in whom aspirin is not tolerated, or in whom dual antiplatelet therapy is desirable. Because it has been reported to increase the risk of thrombotic thrombocytopenic purpura (TTP) and neutropenia, its use has largely been supplanted by the newer drug, clopidogrel, which is felt to have a much lower hematologic risk. Its niche role as an alternative in those patients who do not tolerate Clopidogrel has now been superdeded by Ticagrelor and Prasugrel. The usual dose is 250 mg twice daily by the oral route.
Action[edit]
- Inhibits platelet aggregation by altering the function of platelet membranes by blocking ADP receptors. This prevents the conformational change of glycoprotein IIb/IIIa which allows platelet binding to fibrinogen.
- Prolongs bleeding time.
- Decreased incidence of stroke in high-risk patients.
Contraindications[edit]
- Hypersensitivity
- Bleeding disorders
- Active bleeding
- Severe liver disease
Precautions[edit]
- Risk of bleeding (trauma, surgery, history of peptic ulcer disease)
- Renal or hepatic impairment
- Geriatric patients (increased sensitivity)
- Pregnancy, lactation, or children under 18
- Neutropenia
- Thrombotic thrombocytopenic purpura
Antithrombotics (thrombolytics, anticoagulants and antiplatelet drugs) (B01)
|
|
Antiplatelet drugs |
Glycoprotein IIb/IIIa inhibitors
|
- Abciximab
- Eptifibatide
- Tirofiban
|
|
ADP receptor/P2Y12 inhibitors
|
- thienopyridines
- Clopidogrel
- Prasugrel
- Ticlopidine
- nucleotide/nucleoside analogs
- Cangrelor
- Elinogrel
- Ticagrelor
|
|
Prostaglandin analogue (PGI2)
|
- Beraprost
- Iloprost
- Prostacyclin
- Treprostinil
|
|
COX inhibitors
|
- Acetylsalicylic acid/Aspirin#
- Aloxiprin
- Carbasalate calcium
- Indobufen
- Triflusal
|
|
Thromboxane inhibitors
|
- thromboxane synthase inhibitors
- Dipyridamole (+Aspirin)
- Picotamide
- receptor antagonist
|
|
Phosphodiesterase inhibitors
|
- Cilostazol
- Dipyridamole
- Triflusal
|
|
Other
|
|
|
|
Anticoagulants |
Vitamin K antagonists
(inhibit II, VII, IX, X)
|
- coumarins: Acenocoumarol
- Coumatetralyl
- Dicoumarol
- Ethyl biscoumacetate
- Phenprocoumon
- Warfarin#
- 1,3-Indandiones: Clorindione
- Diphenadione
- Phenindione
- other: Tioclomarol
|
|
Factor Xa inhibitors
(with some II inhibition)
|
Heparin group/
glycosaminoglycans/
(bind antithrombin)
|
- low molecular weight heparin
- Bemiparin
- Certoparin
- Dalteparin
- Enoxaparin
- Nadroparin
- Parnaparin
- Reviparin
- Tinzaparin
- oligosaccharides
- heparinoid
- Danaparoid
- Dermatan sulfate
- Sulodexide
|
|
Direct Xa inhibitors
|
- xabans
- Apixaban
- Betrixaban
- Darexaban
- Edoxaban
- Otamixaban
- Rivaroxaban
|
|
|
Direct thrombin (II) inhibitors
|
- bivalent: Hirudin
- Bivalirudin
- Desirudin
- Lepirudin
- univalent: Argatroban
- Dabigatran
- Melagatran‡
- Ximelagatran‡
|
|
Other
|
- Antithrombin III
- Defibrotide
- Protein C
- Ramatroban
- REG1
|
|
|
Thrombolytic drugs/
fibrinolytics |
- plasminogen activators: r-tPA
- Alteplase
- Reteplase
- Tenecteplase
- UPA
- Anistreplase
- Monteplase
- Streptokinase#
- other serine endopeptidases: Ancrod
- Brinase
- Fibrinolysin
|
|
Non-medicinal |
|
|
- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
|
cell/phys (coag, heme, immu, gran), csfs
|
rbmg/mogr/tumr/hist, sysi/epon, btst
|
drug (B1/2/3+5+6), btst, trns
|
|
|
|
UpToDate Contents
全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.
English Journal
- Effects of various factors of ultrasonic treatment on the extraction recovery of drugs from fish tissues.
- Magiera S1, Pardylla A2, Baranowska I2.
- Ultrasonics sonochemistry.Ultrason Sonochem.2015 Sep;26:388-98. doi: 10.1016/j.ultsonch.2015.03.005. Epub 2015 Mar 12.
- In the present research, a combined extraction method of ultrasound-assisted extraction (UAE) in conjunction with solid phase extraction (SPE) was applied to isolation and enrichment of selected drugs (metoprolol, ticlopidine, propranolol, carbamazepine, naproxen, acenocumarol, diclofenac, ibuprofen
- PMID 25794999
- P2Y12 receptor inhibitors for secondary prevention of ischemic stroke.
- Liu F1, Tantry US, Gurbel PA.
- Expert opinion on pharmacotherapy.Expert Opin Pharmacother.2015 Jun;16(8):1149-65. doi: 10.1517/14656566.2015.1035256. Epub 2015 Apr 14.
- INTRODUCTION: Ischemic stroke (IS) is a major cause of death and disability worldwide. The P2Y12 receptor plays a critical role in the formation of a stable thrombus leading to ischemic complications. Therefore, P2Y12 receptor inhibitors constitute a major antiplatelet strategy in the secondary prev
- PMID 25873127
- Balancing the risks and benefits of dual platelet inhibition.
- Keaney JF Jr1.
- The New England journal of medicine.N Engl J Med.2015 May 7;372(19):1854-6. doi: 10.1056/NEJMe1502137. Epub 2015 Mar 14.
- PMID 25773507
Japanese Journal
- 周術期の抗血栓療法をヘパリンに置換した手術症例の検討
- 松岡 崇志,井上 幸治,水野 桂 [他]
- 泌尿器科紀要 58(5), 223-226, 2012-05
- … In transurethral surgery, patients taking warfarin and antiplatelet drugs (aspirin or ticlopidine) had a statistically significant increase in bleeding complications compared to patients taking warfarin alone. …
- NAID 40019283461
- 症例報告 硬膜外ブロック後に生じた腰椎硬膜外血腫の1例
Related Links
- * Estimated from figure. Comment Ticlopidine has been linked to more than 50 cases of clinically apparent, acute liver injury in the published literature. Most cases were reported from Europe, probably because it was ...
- Ticlopidine also is used before open heart surgery and in the treatment of sickle cell disease, certain types of kidney disease (primary glomerulonephritis), and blocked arteries in the legs. Talk to your doctor about the ...
Related Pictures
★リンクテーブル★
[★]
- 英
- ticlopidine
- 化
- 塩酸チクロピジン ticlopidine hydrochloride
- 商
- ジルペンダー、ソーパー、ソロゾリン、チクピロン、ニチステート、パチュナ、パナピジン、パナルジン、パラクロジン、ビーチロン、ピエテネール、ヒシミドン、ファルロジン、マイトジン
- 関
- その他の血液・体液用薬
作用機序
- 血小板膜にあるACを持続的に活性化→細胞内cAMP↑→細胞内Ca増加抑制→血小板活性化抑制 (SPC.293)
[★]
- 関
- ticlopidine