Abstract:
:Since their introduction 15 years ago, retinoids have been increasingly used for topical and systemic treatment of psoriasis and other hyperkeratotic and parakeratotic skin disorders, keratotic genodermatoses, severe acne and acne-related dermatoses, and also for therapy and/or chemoprevention of skin cancer and other neoplasia. Oxidative metabolites of vitamin A (retinol) are natural retinoids present at low levels in the peripheral blood. Synthetic retinoids are classified into 3 generations including nonaromatic, monoaromatic and polyaromatic compounds. They are detectable in plasma 30-60 minutes after systemic administration, and reach maximum concentrations 2 to 4 hours later. Elimination half-life is 10 to 20 hours for isotretinoin, 80 to 175 days for etretinate and 2 to 4 days for, trans-acitretin; the latter, however, partially converts into etretinate. Retinoid concentrations in skin are rather low in contrast to subcutaneous fat tissue. Intracellularly, retinoids interact with cytosolic proteins and specific nuclear receptors. Two classes of nuclear receptors have been suggested to mediate retinoid activity at the molecular level, RARs and RXRs. The expression of retinoid receptors is tissue specific; skin mainly espresses RAR gamma and RXR alpha. Retinoids affect epidermal cell growth and differentiation as well as sebaceous gland activity and exhibit immunomodulatory and anti-inflammatory properties. Current retinoid research targets the development of receptor-selective retinoids for tailoring and/or improving their therapeutic profile. Currently, tretinoin is used systemically for acute promyelocytic leukaemia, etretinate and acitretin for psoriasis and related disorders, as well as other disorders of keratinisation and isotretinoin for seborrhoea, severe acne, rosacea and acneiform dermatoses. Systemic retinoids are also applied for chemoprevention of epithelial skin cancer and cutaneous T cell lymphoma. The major adverse effect of retinoids is teratogenicity; all other adverse effects are dose-dependent and controllable. Contraception is, therefore, essential during retinoid treatment in women of child-bearing age. Clinical monitoring requires physical examination for adverse effects every 3 to 4 weeks and proper laboratory investigations, also including analysis of retinoid bioavailability in selected cases. Topical retinoids are rapidly developing at present and seem promising for the future; their clinical application includes acne, aging, photodamage, precanceroses, skin cancer and disorders of skin pigmentation. The development of receptor-specific retinoids for topical treatment of psoriasis and/or acne may lead to interesting new compounds based on our current concepts of retinoid function.
journal_name
Drugsjournal_title
Drugsauthors
Orfanos CE,Zouboulis CC,Almond-Roesler B,Geilen CCdoi
10.2165/00003495-199753030-00003subject
Has Abstractpub_date
1997-03-01 00:00:00pages
358-88issue
3eissn
0012-6667issn
1179-1950journal_volume
53pub_type
杂志文章,评审相关文献
DRUGS文献大全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::Asthmatic patients during sympton-free periods almost invariably have abnormalities in lung mechanics and gas exchange. Tentacious secretions and mucosal thickening exaggerate maldistribution of ventilation and cause flow limitation in small airways. Hence, the maximal expiratory flow volume loop in these patients wil...
journal_title:Drugs
pub_type: 杂志文章
doi:10.2165/00003495-197816030-00007
更新日期:1978-09-01 00:00:00
abstract::The cardiovascular and cardiorenal disease continuum comprises the transition from cardiovascular risk factors to endothelial dysfunction and atherosclerosis, to clinical complications such as myocardial infarction (MI) and stroke, to the development of persistent target-organ damage and, ultimately, to chronic conges...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/11537910-000000000-00000
更新日期:2010-07-09 00:00:00
abstract::Lung tissue remodelling in chronic inflammatory lung diseases has long been regarded as a follow-up event to inflammation. Recent studies have indicated that, although airway and lung tissue remodelling is often independent of inflammation, it precedes or causes inflammation. None of the available therapies has a sign...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.1007/s40265-014-0319-0
更新日期:2015-01-01 00:00:00
abstract::Goserelin is a gonadotrophin-releasing hormone (GnRH) analogue which, during continuous administration, down-regulates the pituitary-ovarian gonadal axis and reduces levels of the gonadotrophins, luteinising hormone and follicle-stimulating hormone. In women, this results in suppression of ovarian steroidogenesis and ...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-199651020-00009
更新日期:1996-02-01 00:00:00
abstract::Azimilide is a potassium channel antagonist that, in contrast to existing class III antiarrhythmic agents, blocks both the rapidly (I(Kr)) and slowly (I(Ks)) activating components of the delayed rectifier potassium current. In animal and clinical studies, azimilide prolonged repolarisation by increasing the action pot...
journal_title:Drugs
pub_type: 杂志文章
doi:10.2165/00003495-200059020-00016
更新日期:2000-02-01 00:00:00
abstract:UNLABELLED:5-Methoxypsoralen, a naturally occurring linear furocoumarin, has been successfully used in combination with ultraviolet (UV) A irradiation [psoralen plus UV (PUVA)] to manage psoriasis and vitiligo. In patients and volunteers, PUVA 5-methoxypsoralen causes a dose-related increase in cutaneous photosensitivi...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-199856040-00015
更新日期:1998-10-01 00:00:00
abstract::Alirocumab (Praluent®) is a fully human monoclonal antibody developed by Regeneron Pharmaceuticals and Sanofi that has been approved in the US as an adjunct to diet and maximally tolerated statin therapy for the treatment of adults with heterozygous familial hypercholesterolaemia (HeFH) or clinical atherosclerotic car...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.1007/s40265-015-0469-8
更新日期:2015-09-01 00:00:00
abstract::Mild to moderate hypertension still remains poorly controlled. This relates to multiple factors including low antihypertensive efficacy of single drug therapies reluctance of primary care physicians to modify/titrate initially chosen therapy to obtain target blood pressure, and poor compliance with medication. Several...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200161070-00004
更新日期:2001-01-01 00:00:00
abstract::The Diabetes Control and Complications Trial and the Stockholm Study have conclusively demonstrated that improving the blood glucose control in patients with insulin-dependent diabetes mellitus (IDDM) reduces the risk of developing retinopathy, nephropathy and neuropathy. Each patient with IDDM should be carefully eva...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-199447040-00005
更新日期:1994-04-01 00:00:00
abstract::Coronary arterial thrombolysis is becoming an established treatment of acute myocardial infarction. If given early enough, it recanalises occluded coronary arteries, salvages myocardial function and reduces mortality. A reduction of mortality in patients with acute myocardial infarction has now been demonstrated for s...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-198938030-00003
更新日期:1989-09-01 00:00:00
abstract::The use of digitalis in congestive heart failure with normal sinus rhythm is still debated. While older uncontrolled, withdrawal studies from 1969 to 1983 provided incomplete data, with poorly documented clinical status and poor haemodynamic and exercise data, some patients did improve clinically when digitalis treatm...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-199855060-00002
更新日期:1998-06-01 00:00:00
abstract::Transdermal nicotine delivery systems are a cigarette smoking cessation aid designed to deliver nicotine into the systemic circulation via the skin. The partial replacement of plasma nicotine, which would have otherwise been obtained from cigarettes, reduces the severity of nicotine withdrawal symptoms, and so allows ...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-199244030-00011
更新日期:1992-09-01 00:00:00
abstract::The pathogenesis of postoperative ileus (PI) is multifactorial, and includes activation of inhibitory reflexes, inflammatory mediators and opioids (endogenous and exogenous). Accordingly, various strategies have been employed to prevent PI. As single-modality treatment, continuous postoperative epidural analgesia incl...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200262180-00004
更新日期:2002-01-01 00:00:00
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
更新日期:2019-06-01 00:00:00
abstract::Brexpiprazole (Rexulti®) is an atypical antipsychotic that has been developed by Otsuka Pharmaceutical Co. Ltd and H. Lundbeck A/S as an oral treatment for several psychiatric disorders. Brexpiprazole is a novel serotonin-dopamine activity modulator that acts as a partial agonist of serotonin 1A (5-HT1A) and dopamine ...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.1007/s40265-015-0462-2
更新日期:2015-09-01 00:00:00
abstract::When to treat the patient who presents with ocular hypertension has been a question that has 'stumped' the ophthalmic community for decades. Population-based studies and intervention trials have provided the basis for understanding why we consider treating such patients. Although the EGPS (European Glaucoma Prevention...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200666080-00001
更新日期:2006-01-01 00:00:00
abstract::The popularity of antidepressants in the treatment of insomnia is not supported by a large amount of convincing data, but rather by opinions and beliefs of the prescribing physicians on the advantages of these agents compared with drugs acting on the benzodiazepine receptor or other drugs used for the treatment of ins...
journal_title:Drugs
pub_type: 杂志文章
doi:10.2165/0003495-200868170-00001
更新日期:2008-01-01 00:00:00
abstract:OBJECTIVE:The aim of this article is to review data on the efficacy and safety of montelukast in the treatment of children with asthma. METHODOLOGY:Available published literature, including published abstracts, is reviewed. RESULTS:In patients aged 6 to 14 years with asthma (n = 27), montelukast 5mg demonstrated a si...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200059001-00005
更新日期:2000-01-01 00:00:00
abstract::Allergic rhinitis represents a global health burden. The disease can seriously affect quality of life and is associated with multiple co-morbidities. Histamine and leukotrienes are important pro-inflammatory mediators in nasal allergic inflammation. Their actions on target cells are mediated through specific receptors...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200767180-00006
更新日期:2007-01-01 00:00:00
abstract::Rapid progress has recently been encountered in pharmacologically treating the unborn baby. This unique area of drug therapy raises new methodological and ethical questions. This article is a systematic review of known modalities of fetal pharmacotherapy, and aims to highlight essential principles, difficulties and co...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200262050-00004
更新日期:2002-01-01 00:00:00
abstract::Alectinib (Alecensa(®)) is a second-generation, orally active, potent and highly selective inhibitor of anaplastic lymphoma kinase (ALK). Alectinib is approved for the treatment of ALK fusion-gene positive, unresectable, advanced or recurrent non-small cell lung cancer (NSCLC) in Japan, where it has been given orphan ...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.1007/s40265-014-0329-y
更新日期:2015-01-01 00:00:00
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
更新日期:2006-01-01 00:00:00
abstract::Results from the United Kingdom Prospective Diabetes Study showed that intensive treatment of type 2 (non-insulin-dependent) diabetes mellitus, with sulphonylureas or insulin, significantly reduced microvascular complications but did not have a significant effect on macrovascular complications after 10 years. Insulin ...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200060050-00004
更新日期:2000-11-01 00:00:00
abstract::Trimetrexate is a folinic acid analogue structurally related to methotrexate, whose primary mechanism of action is believed to be inhibition of dihydrofolate reductase. This reduces the production of DNA and RNA precursors and leads to cell death. Trimetrexate is lipophilic and can passively diffuse across cell membra...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-199549040-00007
更新日期:1995-04-01 00:00:00
abstract::MenB-FHbp (bivalent rLP2086; Trumenba®) is a recombinant protein-based vaccine targeting Neisseria meningitidis serogroup B (MenB), which has recently been licensed in the EU for active immunization to prevent invasive disease caused by MenB in individuals ≥ 10 years of age. The vaccine, which contains a variant from ...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.1007/s40265-018-0869-7
更新日期:2018-02-01 00:00:00
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
更新日期:1977-11-01 00:00:00
abstract::Stroke is the third most common cause of death in the US. Primary prevention of stroke can be achieved by control of risk factors including hypertension, diabetes mellitus, elevated cholesterol levels and smoking. Approximately one-third of all ischaemic strokes occur in patients with a history of stroke or transient ...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200565040-00003
更新日期:2005-01-01 00:00:00
abstract::As a consequence of disparities in access to and utilization of preventative healthcare, the incidence and death rates from cervical cancer remain substantial in the face of indisputable evidence that screening saves lives. While disparities persist, there will be an urgent need for research into the treatment of adva...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.1007/s40265-015-0481-z
更新日期:2015-11-01 00:00:00
abstract::HMG-CoA reductase inhibitors (statins) have been shown to reduce mortality and cardiovascular morbidity in patients with hyperlipidaemia and those with coronary artery disease. However, evidence for statin treatment in patients with chronic heart failure (CHF) remains a subject of debate. Patients with heart failure w...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200666020-00002
更新日期:2006-01-01 00:00:00