The evolution of antiplatelet therapy in the treatment of acute coronary syndromes: from aspirin to the present day.

Abstract:

:Our knowledge of the mechanisms of platelet-mediated thrombosis has increased dramatically over the last 40 years. This increased understanding has identified treatment strategies for acute coronary syndromes (ACS) by targeting key mediators of platelet activation and aggregation processes. Aspirin (acetylsalicylic acid) monotherapy improves patient outcomes by irreversibly inhibiting the cyclooxygenase (COX)-1 enzyme in the arachidonic acid pathway. The later-developed thienopyridines, prodrugs that irreversibly inhibit the P2Y(12) receptor, and therefore adenosine diphosphate (ADP) binding, further enhance platelet inhibition and patient outcomes. The thienopyridine clopidogrel has been the standard of care, but it is limited by variable response and treatment failure. A more potent thienopyridine, prasugrel, requires fewer hepatic metabolic steps for activation, and elicits significantly improved outcomes for patients with ACS. The increased potency of prasugrel is associated with an increase in Thrombolysis in Myocardial Infarction (TIMI)-defined major bleeding compared with clopidogrel. Ticagrelor represents a new chemical class of agents called the cyclopentyltriazolopyrimidines. It interacts reversibly with the platelet P2Y(12) receptor, and does not require metabolic bioactivation for activity. Data show a significant improvement in ischaemic outcomes, including mortality, for ticagrelor compared with clopidogrel, without an increase in overall major bleeding, although non-coronary artery bypass graft bleeding is increased. Glycoprotein IIb/IIIa targeted agents (abciximab, tirofiban and eptifibatide) are also used in ACS patients undergoing percutaneous coronary interventions. These inhibitors utilize a different mechanism of action by preventing fibrinogen-mediated platelet aggregation. Other therapeutic strategies for platelet inhibition are being evaluated, including the investigative protease-activated receptor (PAR)-1 and thromboxane A(2) antagonists. This review highlights the mechanisms of action of these agents, and the continuing evolution of ACS therapy.

journal_name

Drugs

journal_title

Drugs

authors

Angiolillo DJ

doi

10.2165/11640880-000000000-00000

subject

Has Abstract

pub_date

2012-11-12 00:00:00

pages

2087-116

issue

16

eissn

0012-6667

issn

1179-1950

pii

2

journal_volume

72

pub_type

杂志文章,评审

相关文献

DRUGS文献大全
  • Dulaglutide: A Review in Type 2 Diabetes.

    abstract::Subcutaneous dulaglutide (Trulicity®) is a once-weekly glucagon-like peptide-1 receptor agonist that is approved in numerous countries as an adjunct to diet and exercise for the treatment of adults with type 2 diabetes (T2D). In the clinical trial and real-world settings, once-weekly subcutaneous dulaglutide, as monot...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.1007/s40265-020-01260-9

    authors: Scott LJ

    更新日期:2020-02-01 00:00:00

  • Miconazole: a preliminary review of its therapeutic efficacy in systemic fungal infections.

    abstract::Miconazole is an imidazole antifungal drug which has recently become available for systemic use. Its antifungal activity has been well studied and it is active in vitro against a wide range of fungi. Published and unpublished reports of the use of miconazole in conditions such as systemic or mucocutaneous candidosis, ...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-198019010-00002

    authors: Heel RC,Brogden RN,Pakes GE,Speight TM,Avery GS

    更新日期:1980-01-01 00:00:00

  • Chemotherapeutic induction of labour. A rational approach.

    abstract::Induction of labour, defined as stimulation of uterine contractions before the spontaneous onset of labour, is indicated when the condition of the mother or fetus precludes awaiting the onset of spontaneous labour. In current medical practice, induction of labour comprises 2 phases: cervical priming and induction of c...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-199754010-00005

    authors: Xenakis EM,Piper JM

    更新日期:1997-07-01 00:00:00

  • Parenteral cephalosporin therapy in ambulatory care: advantages and disadvantages.

    abstract::Outpatient parenteral antibiotic therapy (OPAT) programmes are effective, well tolerated and economically advantageous in carefully selected patient populations. Inclusion criteria for patient selection for OPAT include good clinical appearance and uncomplicated infection. By virtue of their favourable microbiological...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-200059003-00003

    authors: Esposito S

    更新日期:2000-01-01 00:00:00

  • Sotagliflozin: A Review in Type 1 Diabetes.

    abstract::Sotagliflozin (Zynquista™) is the first dual inhibitor of sodium-glucose co-transporter-1 and -2 (SGLT1 and 2). In the phase 3, inTANDEM 1-3 trials, adjunctive use of oral sotagliflozin (200 mg or 400 mg once daily) improved glycaemic control and reduced bodyweight and insulin requirements relative to placebo over 24 ...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.1007/s40265-019-01230-w

    authors: Deeks ED

    更新日期:2019-12-01 00:00:00

  • Cannabinoids: Current and Future Options to Treat Chronic and Chemotherapy-Induced Neuropathic Pain.

    abstract::Increases in cancer diagnosis have tremendous negative impacts on patients and their families, and major societal and economic costs. The beneficial effect of chemotherapeutic agents on tumor suppression comes with major unwanted side effects such as weight and hair loss, nausea and vomiting, and neuropathic pain. Che...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.1007/s40265-019-01132-x

    authors: Blanton HL,Brelsfoard J,DeTurk N,Pruitt K,Narasimhan M,Morgan DJ,Guindon J

    更新日期:2019-06-01 00:00:00

  • Antiviral therapy in human immunodeficiency virus infections. Current status (Part I).

    abstract::Antiviral therapy has in the past met with limited success and only a few antiviral drugs have been available. The human immunodeficiency virus (HIV) epidemic has created an urgent need for the development of antiviral therapy against this infection. HIV replication offers several targets for inhibitory compounds, the...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-199345040-00002

    authors: Sandström E,Oberg B

    更新日期:1993-04-01 00:00:00

  • Selection of vasodilator drugs for patients with severe chronic heart failure: an approach based on a new classification.

    abstract::Although vasodilator drugs are of proven worth in the management of patients with severe heart failure, a useful system of classification of vasodilator drugs has not yet been devised. The traditional system of classification based on the dominant arterial and/or venous sites of action as determined by limb plethysmog...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-198224010-00003

    authors: Packer M

    更新日期:1982-07-01 00:00:00

  • Oxaliplatin. A review of its pharmacological properties and clinical efficacy in metastatic colorectal cancer and its potential in other malignancies.

    abstract:UNLABELLED:Oxaliplatin is a platinum compound that inhibits DNA synthesis, primarily by causing intrastrand cross-links in DNA. Oxaliplatin has a broad spectrum of antineoplastic activity and has demonstrated a lack of cross-resistance with other platinum compounds. In patients with metastatic colorectal cancer, intrav...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-200060040-00005

    authors: Culy CR,Clemett D,Wiseman LR

    更新日期:2000-10-01 00:00:00

  • Effect of a single dose of cefotaxime or ceftriaxone on human faecal flora. A double-blind study.

    abstract::The effect of cefotaxime and ceftriaxone on faecal flora was investigated in women undergoing routine vaginal or abdominal hysterectomy. Three groups of 9 patients received, in a double-blind fashion and just before surgery, cefotaxime 2g intravenously, ceftriaxone 2g intravenously or no antibiotic (controls). Stools ...

    journal_title:Drugs

    pub_type: 临床试验,杂志文章

    doi:10.2165/00003495-198800352-00004

    authors: Michéa-Hamzehpour M,Auckenthaler R,Kunz J,Pechère JC

    更新日期:1988-01-01 00:00:00

  • Inhibiting costimulatory activation of T cells : a viable treatment option for rheumatoid arthritis?

    abstract::There is now good evidence that T cells play a central role in the inflammatory pathway that leads to the persistent synovitis that causes joint damage in rheumatoid arthritis (RA). T cells require two signals to become activated. The second step in the activation of T cells involves costimulatory pathways, the best d...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-200767010-00001

    authors: Pollard LC

    更新日期:2007-01-01 00:00:00

  • Effect of felodipine and metoprolol on muscle and skin arteries in hypertensive patients.

    abstract::The antihypertensive and vasodilator effects of felodipine, a new calcium antagonist of the dihydropyridine group, were examined in 15 patients with moderate to severe hypertension. Flow was measured simultaneously at the calf and finger using a venous occlusion ECG-triggered plethysmograph. Measurements were made at ...

    journal_title:Drugs

    pub_type: 杂志文章

    doi:10.2165/00003495-198500292-00024

    authors: Clement DL,De Pue NY

    更新日期:1985-01-01 00:00:00

  • Losartan/Hydrochlorothiazide: a review of its use in the treatment of hypertension and for stroke risk reduction in patients with hypertension and left ventricular hypertrophy.

    abstract::Losartan/hydrochlorothiazide (HCTZ) [Hyzaar(R)] is a fixed-dose combination of the angiotensin II receptor antagonist (angiotensin receptor blocker [ARB]) losartan and the thiazide diuretic HCTZ. It is indicated for the treatment of hypertension (including as initial therapy in severe hypertension) and for stroke risk...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-200969090-00008

    authors: Keating GM

    更新日期:2009-06-18 00:00:00

  • Brodalumab: First Global Approval.

    abstract::Brodalumab (Lumicef(®)) is a human monoclonal immunoglobulin G antibody that is being developed by Kyowa Hakko Kirin in Japan, where it has been approved for the treatment of psoriasis vulgaris, psoriatic arthritis, pustular psoriasis and psoriatic erythroderma. Brodalumab binds with high affinity to interleukin (IL)-...

    journal_title:Drugs

    pub_type: 杂志文章

    doi:10.1007/s40265-016-0634-8

    authors: Greig SL

    更新日期:2016-09-01 00:00:00

  • The coming era of quadrivalent human influenza vaccines: who will benefit?

    abstract::Influenza vaccines form the mainstay of public health and personal protection against infection with seasonal influenza viruses. These vaccines are designed to protect people against infection with the currently circulating influenza viruses. Since the late 1970s, this has required the use of a trivalent vaccine consi...

    journal_title:Drugs

    pub_type: 杂志文章

    doi:10.2165/11641110-000000000-00000

    authors: Barr IG,Jelley LL

    更新日期:2012-12-03 00:00:00

  • Remission, a therapeutic goal in inflammatory arthropathies? Clinical data from adalimumab studies.

    abstract::In recent years, there have been major advances in the management of rheumatoid arthritis (RA), leading to the development of tumour necrosis factor (TNF) antagonists. With these agents, it is possible to arrest joint damage and, by treating early in the disease course, to prevent joint damage. It is also now thought ...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-200666140-00001

    authors: Montecucco C

    更新日期:2006-01-01 00:00:00

  • Platelet GP IIb-IIIa Receptor Antagonists in Primary Angioplasty: Back to the Future.

    abstract::Coronary artery disease and acute myocardial infarction still represent the leading cause of mortality in developed countries. Therefore, great efforts have been made in the last decades to improve reperfusion strategies and adjunctive antithrombotic therapies. In fact, despite optimal epicardial recanalisation, a lar...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.1007/s40265-015-0425-7

    authors: De Luca G,Savonitto S,van't Hof AW,Suryapranata H

    更新日期:2015-07-01 00:00:00

  • New and Emerging Therapies for Alopecia Areata.

    abstract::Alopecia areata (AA) is an autoimmune condition that affects up to 2% of the general population. Currently available treatment options for AA are of limited efficacy and can be associated with adverse effects. The advancement in understanding of the genetic and molecular mechanisms of AA has led to the development of ...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.1007/s40265-020-01293-0

    authors: Pourang A,Mesinkovska NA

    更新日期:2020-05-01 00:00:00

  • Teicoplanin. A reappraisal of its antimicrobial activity, pharmacokinetic properties and therapeutic efficacy.

    abstract::Since an earlier review in the Journal substantial additional data have accumulated, further clarifying the in vitro activity, pharmacokinetic profile, clinical efficacy and tolerability of teicoplanin. Recent therapeutic trials confirm the efficacy of teicoplanin in the treatment of microbiologically confirmed Gram-p...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-199447050-00008

    authors: Brogden RN,Peters DH

    更新日期:1994-05-01 00:00:00

  • Current Treatments and New Developments in the Management of Glucocorticoid-induced Osteoporosis.

    abstract::Glucocorticoids (GCs) are often used for improvement of quality of life, particularly in the elderly, but long-term GC use may cause harm; bone loss and fractures are among the most devastating side effects. Fracture risk is particularly high in patients with a severe underlying disease with an urgent need for treatme...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.1007/s40265-019-01145-6

    authors: Raterman HG,Bultink IEM,Lems WF

    更新日期:2019-07-01 00:00:00

  • Comparative efficacy, safety and pharmacokinetics of verapamil SR vs verapamil IR in hypertensive patients.

    abstract::The antihypertensive effects of the regular immediate release formulation of verapamil (verapamil IR) and the newer sustained release formulation of verapamil (verapamil SR) were compared in Hispanic patients with untreated essential hypertension. Verapamil IR was given in 3 divided doses (80 or 160mg 3 times daily) a...

    journal_title:Drugs

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.2165/00003495-199200441-00002

    authors: Fuenmayor NT,Faggin BM,Cubeddu LX

    更新日期:1992-01-01 00:00:00

  • Metoprolol. An updated review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy, in hypertension, ischaemic heart disease and related cardiovascular disorders.

    abstract::During the intervening years since metoprolol was first reviewed in the Journal (1977), it has become widely used in the treatment of mild to moderate hypertension and angina pectoris. Although much data have accumulated, its precise mechanisms of action in these diseases remain largely uncertain. Optimum treatment of...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-198631050-00002

    authors: Benfield P,Clissold SP,Brogden RN

    更新日期:1986-05-01 00:00:00

  • Ambulatory blood pressure monitoring.

    abstract::This paper reviews the evidence that, in patients with hypertension, end-organ damage correlates more closely with blood pressure values obtained by ambulatory blood pressure monitoring than with those obtained by conventional sphygmomanometry. However, ambulatory blood pressure monitoring is not suitable for routine ...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-199200441-00004

    authors: Mancia G,Omboni S,Ravogli A,Frattola A,Villani A

    更新日期:1992-01-01 00:00:00

  • Benzbromarone: a review of its pharmacological properties and therapeutic use in gout and hyperuricaemia.

    abstract::Benzbromarone1 is a benzofuran derivative which lowers serum urate and increases urinary urate excretion in normal, hyperuricaemic and gouty subjects. In open short- and long-term studies benzbromarone reduced serum uric acid levels by one-third to one-half and maintained its effectiveness for periods of up to 8 years...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-197714050-00002

    authors: Heel RC,Brogden RN,Speight TM,Avery GS

    更新日期:1977-11-01 00:00:00

  • The Role of Anti-PD-1/PD-L1 Agents in Melanoma: Progress to Date.

    abstract::The discovery of immune inhibitory checkpoints has revolutionized the approach to the systemic treatment of cancer. The programmed death 1 (PD-1) inhibitory checkpoint, in particular, has played a key role in understanding how certain cancers can evade immune surveillance. Blocking the interaction between the PD-1 rec...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.1007/s40265-015-0376-z

    authors: Tsai KK,Daud AI

    更新日期:2015-04-01 00:00:00

  • NSAIDs and gastrointestinal cancer prevention.

    abstract::Numerous studies report the relationship between aspirin and other nonsteroidal anti-inflammatories (NSAIDs) and cancer incidence, in particular for colorectal cancer. This paper systematically reviews the evidence of the effect of aspirin and other NSAIDs on the primary prevention of colorectal and other gastrointest...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-200262060-00006

    authors: Jolly K,Cheng KK,Langman MJ

    更新日期:2002-01-01 00:00:00

  • Depression, circadian rhythms and trimipramine.

    abstract::During depression, chronobiological disorders occur, such as disturbances in body temperature and early urinary excretion of a noradrenaline metabolite. Sleep patterns are disturbed in 90% of depressed patients; early REM sleep and shortened slow-wave sleep (stages 3 and 4), resulting in an increase in REM sleep, have...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-198900381-00003

    authors: Rüther E

    更新日期:1989-01-01 00:00:00

  • Meningococcal groups C and Y and haemophilus B tetanus toxoid conjugate vaccine (HibMenCY-TT; MenHibrix(®)): a review.

    abstract::The meningococcal groups C and Y and Haemophilus b (Hib) tetanus toxoid conjugate vaccine (HibMenCY-TT) contains Neisseria meningitidis serogroup C and Y capsular polysaccharide antigens, and Hib capsular polysaccharide [polyribosyl-ribitol-phosphate (PRP)]. The HibMenCY-TT vaccine is available in the USA for use as a...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.1007/s40265-013-0048-9

    authors: Perry CM

    更新日期:2013-05-01 00:00:00

  • 5-HT3 receptor antagonists for the prevention of chemotherapy-induced nausea and vomiting. A comparison of their pharmacology and clinical efficacy.

    abstract::In the mid-1980s it was discovered that serotonin (5-hydroxytryptamine; 5-HT) was at least partially responsible for producing chemotherapy-induced nausea and vomiting. It was therefore realised that serotonin receptor blockade with serotonin 5-HT3 receptor antagonists could inhibit chemotherapy-induced nausea and vom...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-199855020-00002

    authors: Gregory RE,Ettinger DS

    更新日期:1998-02-01 00:00:00

  • Epidemiology of high blood pressure and obesity.

    abstract::The relationship between bodyweight and arterial pressure was first discovered early this century. More recently, epidemiological studies have confirmed the correlation between bodyweight and blood pressure in both adults and children. Serum cholesterol levels, blood glucose levels, uric acid levels and blood pressure...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-199300462-00025

    authors: Martínez FJ,Sancho-Rof JM

    更新日期:1993-01-01 00:00:00