- 関
- antiplatelet agent、antiplatelet drug、platelet antagonist、platelet inhibitor
WordNet
- limit, block, or decrease the action or function of; "inhibit the action of the enzyme"; "inhibit the rate of a chemical reaction"
- control and refrain from showing; of emotions, desires, impulses, or behavior (同)bottle up, suppress
- limit the range or extent of; "Contact between the young was inhibited by strict social customs"
- a substance that retards or stops an activity
- tiny bits of protoplasm found in vertebrate blood; essential for blood clotting (同)blood_platelet, thrombocyte
PrepTutorEJDIC
- 〈感情・欲望・行動・作用など〉‘を'抑制する / (…しないように)〈人〉‘を'抑制する,妨げる《+『名』+『from』+『名』(do『ing』)》
- 抑制する人(物) / 化学反応抑制剤
- 〈U〉集合 / 〈C〉集合体,集団
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/07/01 05:44:27」(JST)
[Wiki en表示]
An antiplatelet drug (antiaggregant) is a member of a class of pharmaceuticals that decrease platelet aggregation [1] and inhibit thrombus formation. They are effective in the arterial circulation, where anticoagulants have little effect.[citation needed]
They are widely used in primary and secondary prevention of thrombotic cerebrovascular or cardiovascular disease.
|
Contents
- 1 Choice of antiplatelet drug
- 2 Antiplatelet drugs
- 3 Usage
- 3.1 In dental implants procedures
- 3.2 Prevention and treatment of arterial thrombosis
- 4 Drug toxicity
- 5 See also
- 6 References
|
Choice of antiplatelet drug[edit]
A 2006 review [2] states: "...low-dose aspirin increases the risk of major bleeding 2-fold compared with placebo. However, the annual incidence of major bleeding due to low-dose aspirin is modest—only 1.3 patients per thousand higher than what is observed with placebo treatment. Treatment of approximately 800 patients with low-dose aspirin annually for cardiovascular prophylaxis will result in only 1 additional major bleeding episode."
Antiplatelet drugs[edit]
The class of antiplatelet drugs include:
- Irreversible cyclooxygenase inhibitors
- Adenosine diphosphate (ADP) receptor inhibitors
- Clopidogrel (Plavix)
- Prasugrel (Effient)
- Ticagrelor (Brilinta)
- Ticlopidine (Ticlid)
- Phosphodiesterase inhibitors
- Glycoprotein IIB/IIIA inhibitors (intravenous use only)
- Abciximab (ReoPro)
- Eptifibatide (Integrilin)
- Tirofiban (Aggrastat)
- Adenosine reuptake inhibitors
- Dipyridamole (Persantine)
- Thromboxane inhibitors
- Thromboxane synthase inhibitors
- Thromboxane receptor antagonists
Usage[edit]
In dental implants procedures[edit]
Dental implant procedures can be safely performed in patients on long-term antiplatelet medication, with no interruption or alteration of their medication. Such patients do not have an increased risk of prolonged or excessive postoperative bleeding.[3]
Prevention and treatment of arterial thrombosis[edit]
Treatment of established arterial thrombosis includes the use of antiplatelet drugs and thrombolytic therapy. Antiplatelet drugs alter the platelet activation at the site of vascular damage crucial to the development of arterial thrombosis.
- Aspirin irreversibly inhibits the enzyme COX, resulting in reduced platelet production of TXA2 (thromboxane - powerful vasoconstrictor that lowers cyclic AMP and initiates the platelet release reaction).
- Dipyridamole inhibits platelet phosphodiesterase, causing an increase in cyclic AMP with potentiation of the action of PGI2 – opposes actions of TXA2
- Clopidogrel affects the ADP-dependent activation of IIb/IIIa complex
- Glycoprotein IIb/IIIa receptor antagonists block a receptor on the platelet for fibrinogen and von Willebrand factor. 3 classes:
- Murine-human chimeric antibodies (e.g., abciximab)
- Synthetic peptides (e.g., eptifibatide)
- Synthetic non-peptides (e.g., tirofiban)
- Epoprostenol is a prostacyclin that is used to inhibit platelet aggregation during renal dialysis (with or without heparin) and is also used in primary pulmonary hypertension.
Thrombolytic therapy is used in myocardial infarction, cerebral infarction, and, on occasion, in massive pulmonary embolism. The main risk is bleeding. Treatment should not be given to patients having had recent bleeding, uncontrolled hypertension or a hemorrhagic stroke, or surgery or other invasive procedures within the previous 10 days.
- Streptokinase forms a complex with plasminogen, resulting in a conformational change that activates other plasminogen molecules to form plasmin.
- Plasminogen activators (PA), tissue-type plasminogen activators (alteplase, tenecteplase) are produced by recombinant technology.
Drug toxicity[edit]
Drug toxicity may be increased when multiple antiplatelet drugs are used. Gastrointestinal bleeding is a common adverse events seen in many patients.[4]
See also[edit]
- Anticoagulant drug
- Thrombolytic drug
- Nitrophorin
References[edit]
- ^ "Antiplatelet agents" at Dorland's Medical Dictionary[dead link]
- ^ The American Journal of Medicine, Volume 119, Issue 8 , Pages 624-638, August 2006: Systematic Review and Meta-analysis of Adverse Events of Low-dose Aspirin and Clopidogrel in Randomized Controlled Trials Retrieved 2013-02-08
- ^ Mihai Bogdan Bucur (Nov 2011). "Antiplatelet treatment implications in oral implantology" (HTML). Rev. chir. oro-maxilo-fac. implantol. (in (Romanian)) 2 (3): 6–9. ISSN 2069-3850. 39. Retrieved 2012-04-15. (webpage has a translation button)
- ^ Shehab, Nadine; Laurence S. Sperling, Scott R. Kegler, Daniel S. Budnitz (2010-11-22). "National Estimates of Emergency Department Visits for Hemorrhage-Related Adverse Events From Clopidogrel Plus Aspirin and From Warfarin". Arch Intern Med 170 (21): 1926–1933. doi:10.1001/archinternmed.2010.407. PMID 21098354. Retrieved 2010-11-23.
|
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
- 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
- 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
- Synthesis and biological evaluation of N-arylpiperazine derivatives of 4,4-dimethylisoquinoline-1,3(2H,4H)-dione as potential antiplatelet agents.
- Marcinkowska M1, Kotańska M2, Zagórska A1, Śniecikowska J1, Kubacka M2, Siwek A3, Bucki A1, Pawłowski M1, Bednarski M4, Sapa J4, Starek M5, Dąbrowska M5, Kołaczkowski M1.
- Journal of enzyme inhibition and medicinal chemistry.J Enzyme Inhib Med Chem.2018 Dec;33(1):536-545. doi: 10.1080/14756366.2018.1437155.
- PMID 29482394
- Molecular mechanisms of platelet activation and aggregation induced by breast cancer cells.
- Zarà M1, Canobbio I1, Visconte C1, Canino J1, Torti M2, Guidetti GF1.
- Cellular signalling.Cell Signal.2018 Aug;48:45-53. doi: 10.1016/j.cellsig.2018.04.008. Epub 2018 Apr 26.
- PMID 29705335
- Dabigatran affects thrombin-dependent platelet aggregation after a week-long therapy.
- Sokol J1, Nehaj F2, Ivankova J1, Mokan M2, Mokan M2, Stasko J1.
- Scandinavian cardiovascular journal : SCJ.Scand Cardiovasc J.2018 Aug;52(4):227-231. doi: 10.1080/14017431.2018.1480798. Epub 2018 May 29.
- PMID 29842807
Japanese Journal
- ネフローゼ症候群の合併が，閉塞血管再開通の阻害因子となった可能性が考えられた脳塞栓症の1例
- 中西 俊人,渡邉 聖樹,中島 誠,野尻 奈央,小田 晶,安東 由喜雄
- 臨床神経学 55(1), 18-22, 2015
- 症例は65歳男性である．突然発症の左片麻痺を主訴に搬送され，急性期脳梗塞の診断でrecombinant tissue plasminogen activator（rt-PA）静注療法が施行されたが，症状の改善がなく緊急脳血管内血行再建術をおこなった．血栓吸引をおこない部分再開通をえたが，その後再閉塞をきたした．入院後，蛋白尿や低アルブミン血症の存在から腎生検をおこない，ALアミロイドーシスによるネ …
- NAID 130004921295
- 1,4-Benzoxazine-3(4H)-ones as Potent Inhibitors of Platelet Aggregation : Design, Synthesis and Structure-Activity Relations
- Liu Chang,Tan Jia-Lian,Xiao Si-Yu [他]
- Chemical and pharmaceutical bulletin 62(9), 915-20, 2014-09
- NAID 40020173364
- 微小循環モデルにおけるシロスタゾールとGPIIb/IIIa阻害薬の血液レオロジーに及ぼす影響
- 木村 友美,内山 真一郎
- 東京女子医科大学雑誌 84(E1), E111-E117, 2014-01-31
- 虚血性脳血管障害の二次予防や急性期治療のための抗血小板薬としてphosphodiesterase type 3阻害薬と血小板膜糖蛋白(GP)IIb/IIIa阻害薬が注目されている.本研究では、微小循環モデル(Micro Channel Array Flow Analyzer;MC-FAN)を用いて、in vitro におけるシロスタゾール、GP IIb/IIIa阻害薬FK419およびtirofib …
- NAID 110009752563
Related Links
- Platelet activation and coagulation normally do not occur within an intact blood vessel. After vessel wall injury, platelet-plug formation is initiated by the adherence of platelets to subendothelial collagen. In high shear arterial blood ...
- Chemical Entities of Biological Interest (ChEBI) is a freely available dictionary of molecular entities focused on 'small' chemical compounds. ... ChEBI Name platelet aggregation inhibitor ChEBI ID CHEBI:50427 Definition A drug or ...
★リンクテーブル★
[★]
- 英
- antiplatelet agent、antiplatelet drug、platelet aggregation inhibitor
- 関
- 抗血小板薬、血小板凝集阻害剤、血小板凝集抑制薬、血小板抑制薬、血小板凝集抑制剤、抗血小板剤、トロンボキサン合成酵素阻害薬
[★]
- 英
- antiplatelet drug、platelet aggregation inhibitor
- 関
- 血小板凝集阻害薬、抗血小板薬、血小板凝集抑制薬、血小板凝集抑制剤、抗血小板剤
[★]
- 関
- antiplatelet agent、antiplatelet drug、platelet aggregation inhibitor、platelet antagonist
[★]
- 英
- platelet aggregation inhibitor
- 関
- 血小板凝集阻害薬、血小板凝集阻害剤、血小板凝集抑制薬
[★]
- 英
- platelet aggregation inhibitor
- 関
- 抗血小板薬
[★]
- 関
- abrogate、block、depress、depression、deter、inhibition、interdict、prevent、prevention、repress、repression、restrain、restraint、suppress、suppression
[★]
- 関
- agglutinate、agglutination、aggregate、assemblage、assemble、assembly、clump、come together、convergence、populate、population
[★]
- 関
- blocker、depressant、suppressant