Abstract:
:Arachidonic acid is normally stored in membrane-bound phospholipids and released by the action of phospholipases. Enzymatic conversion of released arachidonic acid into biologically active derivatives proceeds through one of several routes. Cyclo-oxygenase converts arachidonic acid to unstable cyclic endoperoxides from which prostaglandins, prostacyclin and thromboxanes are derived. Formation of the leukotrienes from arachidonic acid is initiated by the action of 5-lipoxygenase producing leukotriene A4. Hydrolysis of leukotriene A4, or the incorporation of glutathione results in the formation of leukotriene B4 and C4, respectively. In addition, 12- and 15-lipoxygenase can catalyse arachidonic acid conversion and lipoxins A and B are amongst the possible products. Many of these metabolites of arachidonic acid feature prominently in the development of inflammation. Prostaglandin E2 and prostacyclin are potent vasodilators, while leukotriene D4 causes cellular adhesion, chemotaxis of neutrophils and degranulation. Leukotrienes C4, D4 and E4 contribute to inflammation by increasing vascular permeability. Leukotrienes are also believed to play an important pathophysiological role in allergic broncho-constriction of asthma. Through pharmacological intervention in the arachidonic acid cascade various anti-inflammatory agents have been developed. These include aspirin-like drugs, which inhibit cyclo-oxygenase. Corticosteroids appear to indirectly inhibit phospholipases thus preventing release of arachidonic acid. Future progress in this field is likely to produce drugs which antagonise arachidonic acid derivatives or inhibit the enzymes involved in their synthesis with greater specificity.
journal_name
Drugsjournal_title
Drugsauthors
Samuelsson Bdoi
10.2165/00003495-198700331-00003subject
Has Abstractpub_date
1987-01-01 00:00:00pages
2-9eissn
0012-6667issn
1179-1950journal_volume
33 Suppl 1pub_type
杂志文章相关文献
DRUGS文献大全abstract::Dementia is commonly diagnosed at a time of major domestic breakdown, when symptoms are severe and family and community patience has been eroded. In order to encourage early referral and identification of patients with treatable conditions, a Memory Clinic is held at the University Hospital in Cardiff. The clinic prov...
journal_title:Drugs
pub_type: 杂志文章
doi:10.2165/00003495-198700332-00016
更新日期:1987-01-01 00:00:00
abstract::Four medicinal cancer biological blockbusters will end their patent lifespan by 2020. It is estimated that the total market for cancer biologicals will reach approximately US$68 billion at that time. Approximately 20 biosimilars have entered the European market since the launch of the original approval guidelines in 2...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.1007/s40265-017-0743-z
更新日期:2017-06-01 00:00:00
abstract::The original article has been corrected. ...
journal_title:Drugs
pub_type: 杂志文章,已发布勘误
doi:10.1007/s40265-020-01280-5
更新日期:2020-03-01 00:00:00
abstract::The common clinical problem of recurrent symptomatic urinary tract infections (UTI) in young women may be inconvenient and distressing to both the patient and her family, particularly if the infections are not managed in a rational manner. A suggested approach is included in table 1. ...
journal_title:Drugs
pub_type: 杂志文章
doi:10.2165/00003495-197713020-00003
更新日期:1977-02-01 00:00:00
abstract::67 samples of 15 different tissues were obtained from 26 patients who were given an intravenous bolus dose of temocillin approximately 3 to 4 hours prior to surgery. 50 tissue samples were obtained from 19 patients who received 1g temocillin and 17 tissue samples were obtained from 7 patients who received 2g temocilli...
journal_title:Drugs
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.2165/00003495-198500295-00034
更新日期:1985-01-01 00:00:00
abstract::Osteoarthritis, the most common rheumatic disease, presents the clinician with a major therapeutic and management task. The chronic and progressive course of the disease is punctuated by pain, declining function and escalating disability. This article attempts to deal with the pharmacological therapeutic options avail...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-199141020-00005
更新日期:1991-02-01 00:00:00
abstract::Canagliflozin (Invokana™), an oral selective sodium-glucose co-transporter 2 (SGLT2) inhibitor, is under global development with Mitsubishi Tanabe Pharma and Janssen Pharmaceuticals, a subsidiary of Johnson and Johnson, for the treatment of type 2 diabetes mellitus. SGLT2 are mainly located in the proximal tubule of t...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.1007/s40265-013-0064-9
更新日期:2013-06-01 00:00:00
abstract::Acamprosate (calcium acetylhomotaurinate), a synthetic compound with a similar chemical structure to that of gamma-aminobutyric acid, is thought to act via several mechanisms affecting multiple neurotransmitter systems; inhibition of neuronal hyperexcitability by antagonism of excitatory amino acid activity and reduct...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-199753060-00008
更新日期:1997-06-01 00:00:00
abstract::The size of the antibiotic market in developing countries is double that seen in developed countries. There are some valid reasons for this difference, one of which is the higher frequency of diverse infections in the developing world. However, other factors are involved: for example, antibiotics are available without...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-199300453-00009
更新日期:1993-01-01 00:00:00
abstract::Hypopituitarism is a rare disorder, but its prevalence has increased as a result of an increase in secondary causes of hypopituitarism such as traumatic brain injury and cranial irradiation. Estrogen with or without progestogen (progestin) treatment is conventional therapy in women with hypopituitarism. Recent data de...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200868150-00001
更新日期:2008-01-01 00:00:00
abstract::The pharmacokinetics of different formulations of glyceryl trinitrate, isosorbide dinitrate, isosorbide 5-mononitrate and isosorbide 2-mononitrate are reviewed. ...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-198700334-00004
更新日期:1987-01-01 00:00:00
abstract::Several antihypertensive agents such as thiazide diuretics and some beta-blockers have recently been shown to adversely affect lipid metabolism. Moreover, there is a growing suspicion that the adverse effect on plasma lipids might outweigh the favourable effect of lowering blood pressure. The effect of ketanserin tart...
journal_title:Drugs
pub_type: 临床试验,杂志文章
doi:10.2165/00003495-198800361-00006
更新日期:1988-01-01 00:00:00
abstract::The occurrence of late side effects of long term levodopa therapy (fluctuations in motor performance, abnormal movements, and symptoms unresponsive to dihydroxyphenylalanine) led to the search for novel anti-Parkinsonian drugs. Dopamine agonists are one of the newer families of anti-Parkinsonian agents, and they inclu...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-199346030-00005
更新日期:1993-09-01 00:00:00
abstract::This review considers recent pharmacological and biochemical studies of sulphasalazine and its colonic metabolites, 5-aminosalicylic acid and sulphapyridine, in relation to the use of the parent drug for the treatment of ulcerative colitis and, more recently, rheumatoid arthritis. Several factors make it difficult to ...
journal_title:Drugs
pub_type: 临床试验,杂志文章,评审
doi:10.2165/00003495-198600321-00005
更新日期:1986-01-01 00:00:00
abstract::Meloxicam is a new nonsteroidal anti-inflammatory drug (NSAID) developed for the treatment of rheumatoid arthritis and osteoarthritis. It has greater in vitro and in vivo inhibitory action against the inducible isoform of cyclo-oxygenase (COX-2), which is implicated in the inflammatory response, than against the const...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-199651030-00007
更新日期:1996-03-01 00:00:00
abstract::The potential beneficial effects of antihypertensive drugs on cardiovascular morbidity and mortality may be compromised by their adverse effects on serum lipid levels. In our study we compared verapamil and captopril and evaluated their effects on blood pressure and on serum lipid and lipoprotein levels, with particul...
journal_title:Drugs
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.2165/00003495-199200441-00016
更新日期:1992-01-01 00:00:00
abstract::Patients frequently come to the emergency department for pain. For decades, ketamine has been used in the emergency department for procedural sedation but is now receiving attention as a potential alternative to opioids because of its unique analgesic effects. Additionally, ketamine's dissociative properties have made...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.1007/s40265-018-0904-8
更新日期:2018-05-01 00:00:00
abstract::Ondansetron is a selective 5-HT3 receptor antagonist which has previously been reported in the Journal to be a promising new agent for use as prophylaxis against nausea and vomiting caused by chemotherapy and radiotherapy. Since the publication of this original review, further studies have been published that show ond...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-199345060-00006
更新日期:1993-06-01 00:00:00
abstract::In a double-blind study, 40 patients scheduled for saphenectomy or inguinal hernioplasty were randomly assigned to treatment with nimesulide (200mg 3 times daily) or diclofenac (100mg 3 times daily) administered rectally. Therapy with either drug resulted in significantly less pain, oedema and hyperaemia, and resoluti...
journal_title:Drugs
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.2165/00003495-199300461-00038
更新日期:1993-01-01 00:00:00
abstract::Alzheimer's disease (AD) is the most common age-related neurodegenerative disease and has become an urgent public health problem in most areas of the world. Substantial progress has been made in understanding the basic neurobiology of AD and, as a result, new drugs for its treatment have become available. Cholinestera...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200161010-00005
更新日期:2001-01-01 00:00:00
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
更新日期:2000-01-01 00:00:00
abstract::The treatment of a variety of inflammatory skin diseases was greatly changed by the introduction, in the early 1950s, of corticosteroids for topical use. Topical corticosteroids are still the most widely used drugs in dermatology, and many preparations with quite different potencies are now available. However, attempt...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-198800365-00008
更新日期:1988-01-01 00:00:00
abstract::Drug-drug interactions (DDIs) occur commonly and may lead to severe adverse drug reactions if not handled appropriately. Considerable information to support clinical decision making regarding potential DDIs is available in the literature and through various systems providing electronic decision support for healthcare ...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.1007/s40265-017-0729-x
更新日期:2017-05-01 00:00:00
abstract::A new formulation of paclitaxel, 130-nanometre albumin-bound paclitaxel (nab-paclitaxel), solubilises hydrophobic paclitaxel and may increase paclitaxel delivery to tumour cells. Intravenous nab-paclitaxel 260 mg/m(2) had a higher maximum whole-blood concentration, shorter time to peak concentration, larger distributi...
journal_title:Drugs
pub_type: 杂志文章
doi:10.2165/00003495-200666070-00007
更新日期:2006-01-01 00:00:00
abstract::Macitentan (Opsumit(®)) is an orally active, dual endothelin receptor antagonist (ERA) with tissue targeting properties. Macitentan was approved recently in the EU (as monotherapy or combination therapy) for the long-term treatment of pulmonary arterial hypertension (PAH) in adults of WHO functional class II or III, a...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.1007/s40265-014-0266-9
更新日期:2014-09-01 00:00:00
abstract::Novartis has developed oral and intravenous formulations of panobinostat (Farydak(®)), a histone deacetylase (HDAC) inhibitor, for the treatment of cancer. HDACs have important roles in maintaining chromatin structure and in regulating gene expression, including that of tumour suppressor genes, and thus represent vali...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.1007/s40265-015-0388-8
更新日期:2015-04-01 00:00:00
abstract::Because platelets are so important in thrombus formation, drugs which inhibit platelet function (the 'antiplatelet drugs') have considerable potential as antithrombotic agents. Among the antiplatelet drugs, only aspirin, sulphinpyrazone, dipyridamole, hydroxychloroquine, and clofibrate have had wide clinical trial. Th...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-197918060-00002
更新日期:1979-12-01 00:00:00
abstract::Liposomes are versatile drug carriers which can be used to solve problems of drug solubility, instability and rapid degradation. Both hydrophilic and hydrophobic drugs can be associated with liposomes and special techniques have been developed for the efficient loading of weak acids and weak bases into liposomes. Lipo...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-199856050-00001
更新日期:1998-11-01 00:00:00
abstract::Intravenous minocycline (Minocin®) is approved in the USA for use in patients with infections due to susceptible strains of Gram-positive and Gram-negative pathogens, including infections due to Acinetobacter spp. Minocycline is a synthetic tetracycline derivative that was originally introduced in the 1960s. A new int...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.1007/s40265-016-0636-6
更新日期:2016-10-01 00:00:00
abstract::Hypertension affects 65 million people in the US, and is a major cause of morbidity and mortality, but less than one-third of patients with hypertension are treated to goal blood pressure. Multiple factors have been cited, and include suboptimal adherence to treatment and lifestyle modifications, limited access to hea...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200666090-00006
更新日期:2006-01-01 00:00:00