[Properties and features of nabumetone].

Abstract:

:Nabumetone is a nonsteroidal anti-inflammatory drug (NSAID) of the 2,6-disubstituted naphthylalkanone class. It is a prodrug metabolised to an active metabolite, 6-methoxy-2-naphthylacetic acid (6-MNA), which preferentially inhibits cyclo-oxygenase-2 (COX-2) and has both anti-inflammatory and analgesic properties. The efficacy of nabumetone is comparable to that of other NSAIDs currently marketed in France for the treatment of rheumatoid arthritis and osteoarthritis. Nabumetone is metabolised to 6-MNA by extensive first-pass metabolism. This active metabolite is subsequently conjugated and excreted in urine. 6-MNA does not undergo enterohepatic recirculation, which may have implications for comparative gastrointestinal toxicity. Substantial concentrations of 6-MNA are achieved and maintained in synovial fluid, which is close to the proposed site of action in chronic arthropathies. The long plasma half-life of 6-MNA (20 to 24 hours) and its persistence in synovial fluid facilitate a once-daily dosage regimen. Nabumetone compares favourably with other NSAIDs with respect to its renal and gastrointestinal adverse effect profile, although increased clinical vigilance of drug-related adverse events relating to these organ systems is still recommended. In addition, in vitro experiments have shown this drug to have a good cartilage tolerability profile. Whether nabumetone has clinical utility in cardiovascular disorders remains to be determined. The unique pharmacokinetic and pharmacodynamic properties of nabumetone make it a welcome addition to the growing arsenal of drugs used in the treatment of chronic arthropathies. There may be clinical advantages in terms of the relative tolerability profile of nabumetone, given that this drug has a low COX-2/COX-1 ratio compared with other nonselective NSAIDs.

journal_name

Drugs

journal_title

Drugs

authors

Davies NM,McLachlan AJ

subject

Has Abstract

pub_date

2000-01-01 00:00:00

pages

25-33

eissn

0012-6667

issn

1179-1950

journal_volume

59 Spec No 1

pub_type

杂志文章,评审

相关文献

DRUGS文献大全
  • Alectinib: a review of its use in advanced ALK-rearranged non-small cell lung cancer.

    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

    authors: McKeage K

    更新日期:2015-01-01 00:00:00

  • Darunavir: a review of its use in the management of HIV infection in adults.

    abstract:UNLABELLED:Darunavir is an oral nonpeptidic HIV-1 protease inhibitor (PI) that is used, together with a low boosting dose of ritonavir, as part of an antiretroviral therapy (ART) regimen in treatment-experienced and -naive patients with HIV-1 infection. Compared with early-generation PIs, boosted darunavir has a high g...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-200969040-00007

    authors: McKeage K,Perry CM,Keam SJ

    更新日期:2009-01-01 00:00:00

  • Dapoxetine: in premature ejaculation.

    abstract::Dapoxetine, a selective serotonin reuptake inhibitor, is the first oral pharmacological agent indicated for the treatment of men aged 18-64 years with premature ejaculation. In four randomized, double-blind, placebo-controlled, multicentre studies of 12-24 weeks' duration, oral dapoxetine 30 or 60 mg (administered as ...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/11204750-000000000-00000

    authors: Hoy SM,Scott LJ

    更新日期:2010-07-30 00:00:00

  • [The kidney as a target organ in diabetic patients with arterial hypertension].

    abstract::Diabetes mellitus has become the most common single cause of end-stage renal disease in the Western world. Diabetic nephropathy, as most forms of renal disease leading to end-stage renal failure, is frequently complicated by arterial hypertension. In type 1 diabetes mellitus the reported excess in arterial hypertensio...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:

    authors: Viberti G

    更新日期:2003-01-01 00:00:00

  • Telavancin.

    abstract::Telavancin is the first available lipoglycopeptide antibacterial agent. It is active against Gram-positive bacteria, including meticillin/oxacillin-resistant Staphylococcus aureus (MRSA) strains associated with complicated skin and skin structure infections (cSSSIs). In randomized, double-blind trials, intravenous tel...

    journal_title:Drugs

    pub_type: 杂志文章

    doi:10.2165/10481380-000000000-00000

    authors: Lyseng-Williamson KA,Blick SK

    更新日期:2009-01-01 00:00:00

  • Drugs affecting the inner ear. A review of their clinical efficacy, mechanisms of action, toxicity, and place in therapy.

    abstract::Many drugs have a site of action within the inner ear. The list includes therapeutic, diagnostic and ototoxic agents. Therapeutic agents are most useful in cases of infections, endolymphatic hydrops, vascular insufficiency, vertigo of peripheral origin, autoimmune disease, otosclerosis (otospongiosis), sudden hearing ...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-198836060-00005

    authors: Norris CH

    更新日期:1988-12-01 00:00:00

  • Management of insomnia in patients with chronic obstructive pulmonary disease.

    abstract::Chronic obstructive pulmonary disease (COPD) is a common medical disorder, which causes considerable morbidity and mortality. Given the chronic and symptomatic nature of the disease, the patient is often seen in the physician's office with complaints of dyspnea. However, more than 50% of COPD patients also have sleep ...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-200363040-00004

    authors: George CF,Bayliff CD

    更新日期:2003-01-01 00:00:00

  • Current, new and future treatments in dyslipidaemia and atherosclerosis.

    abstract::The new therapeutic options available to clinicians treating dyslipidaemia in the last decade have enabled effective treatment for many patients. The development of the HMG-CoA reductase inhibitors (statins) have been a major advance in that they possess multiple pharmacological effects (pleiotropic effects) resulting...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-200060010-00005

    authors: Chong PH,Bachenheimer BS

    更新日期:2000-07-01 00:00:00

  • Drug-induced hypertension: pathogenesis and management.

    abstract::Estrogenic compounds are the most important group of drugs that can induce hypertension. Studies have shown an incidence of significant hypertension amounting to less than 1% after 1 year of taking oral contraceptives and about 2% after 5 years. The ratio of the incidence of hypertension among ''takers'' to that of ...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-197612030-00005

    authors: Stokes GS

    更新日期:1976-01-01 00:00:00

  • Pharmacokinetics of cefoperazone: a review.

    abstract::The pharmacokinetics of cefoperazone in normal subjects, and in patients with hepatic and renal dysfunction are reviewed. After intravenous administration of 2 g of cefoperazone, levels in serum ranged from 202 to 375 microgram/ml depending on the period of drug administration. After intramuscular injection of 2 g of ...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-198100221-00010

    authors: Craig WA,Gerber AU

    更新日期:1981-01-01 00:00:00

  • Goserelin. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in benign gynaecological disorders.

    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

    authors: Perry CM,Brogden RN

    更新日期:1996-02-01 00:00:00

  • Tolerability of nimesulide. Epidemiological data.

    abstract::This review describes the tolerability profile of nimesulide as documented in a global assessment of the clinical data available to Helsinn for this drug. Data from 151 trials were considered and the relevant case report forms and study reports were used as source information. The analysis was conducted using between-...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-199300461-00070

    authors: Fusetti G,Magni E,Armandola MC

    更新日期:1993-01-01 00:00:00

  • Liposomal drug formulations. Rationale for development and what we can expect for the future.

    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

    authors: Allen TM

    更新日期:1998-11-01 00:00:00

  • Comparison of nimesulide and diclofenac in the prevention and treatment of painful inflammatory postoperative complications of general surgery.

    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

    authors: Ramella G,Costagli V,Vetere M,Capra C,Casella G,Sogni A,Scaricabarozzi I

    更新日期:1993-01-01 00:00:00

  • Bezafibrate. An update of its pharmacology and use in the management of dyslipidaemia.

    abstract::The lipid-modifying profile of bezafibrate is characterised by marked decreases in elevated triglyceride levels, increases in high density lipoprotein (HDL) cholesterol levels and decreases in total and low density lipoprotein (LDL) cholesterol levels. Bezafibrate also reduces elevated levels of lipoprotein(a) [Lp(a)]...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-199652050-00008

    authors: Goa KL,Barradell LB,Plosker GL

    更新日期:1996-11-01 00:00:00

  • Budesonide MMX(®): a review of its use in patients with mild to moderate ulcerative colitis.

    abstract::Budesonide MMX(®) (Cortiment(®); Uceris(®)) is a novel once-daily oral formulation of budesonide using Multi Matrix (MMX(®)) colonic delivery technology to permit the release of budesonide at a controlled rate throughout the colon. It is available in the USA for the induction of remission in patients with active, mild...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.1007/s40265-015-0396-8

    authors: Hoy SM

    更新日期:2015-05-01 00:00:00

  • Assessment of the risk-benefit ratio for antiarrhythmic drug use.

    abstract::Arrhythmia treatment has always been difficult, particularly as there are no good indicators of the optimal management strategy. The introduction of new antiarrhythmic agents has forced reappraisal of how these drugs are used. Dynamic electrocardiography and invasive electrophysiological studies are important tools fo...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-198836050-00005

    authors: Campbell RW

    更新日期:1988-11-01 00:00:00

  • Androgen replacement therapy in androgen-deficient women with hypopituitarism.

    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

    authors: Zang H,Davis SR

    更新日期:2008-01-01 00:00:00

  • Effects of alpha-adrenoceptor blockers on renal function and blood pressure adjustment in human hypertension.

    abstract::In this paper the different aspects of the role played by alpha-adrenoceptors in the control of renin secretion from the juxtaglomerular apparatus and renal sodium and water reabsorption, and the effects of alpha-adrenoceptor antagonists on systemic haemodynamics, will be investigated. Animal experiments suggest that ...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-198800356-00007

    authors: Leonetti G

    更新日期:1988-01-01 00:00:00

  • Treatment of Kaposi's sarcoma. Current guidelines and future perspectives.

    abstract::Kaposi's sarcoma is the most common malignancy associated with HIV infection, and the morbidity and mortality attributable to AIDS-related Kaposi's sarcoma (AIDS-KS) may be increasing. No curative therapy is available for AIDS-KS, but palliative therapy can eliminate or reduce cosmetically unacceptable lesions, reduce...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-199448040-00006

    authors: Northfelt DW

    更新日期:1994-10-01 00:00:00

  • Updated national and international hypertension guidelines: a review of current recommendations.

    abstract::Despite the availability of effective pharmacological treatments to aid the control of blood pressure, the global rate of uncontrolled blood pressure remains high. As such, further measures are required to improve blood pressure control. Recently, several national and international guidelines for the management of hyp...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.1007/s40265-014-0306-5

    authors: Kjeldsen S,Feldman RD,Lisheng L,Mourad JJ,Chiang CE,Zhang W,Wu Z,Li W,Williams B

    更新日期:2014-11-01 00:00:00

  • Drug-induced agranulocytosis.

    abstract::An unexpected precipitous fall in peripheral leucocyte count may occur during treatment of certain sensitised individuals with drugs usually well tolerated by most people. Three basic mechanisms for drug sensitivity have been found. One is characterised by sudden destruction of large numbers of leucocytes in periphera...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-197815020-00003

    authors: Pisciotta V

    更新日期:1978-02-01 00:00:00

  • The role of proton pump inhibitors in gastro-oesophageal reflux disease.

    abstract::The proton pump inhibitors (PPIs) are the most successful class of drugs that have been introduced for the treatment of gastro-oesophageal reflux disease (GORD) because of their profound and consistent effect on gastric acid secretion. The PPIs have demonstrated an excellent adverse effect profile after approximately ...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-200464030-00004

    authors: Dekel R,Morse C,Fass R

    更新日期:2004-01-01 00:00:00

  • 5-Methoxypsoralen. A review of its effects in psoriasis and vitiligo.

    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

    authors: McNeely W,Goa KL

    更新日期:1998-10-01 00:00:00

  • Risk factors for the spread of antibiotic-resistant bacteria.

    abstract::The emergence of antibiotic resistance is primarily due to excessive and often unnecessary use of antibiotics in humans and animals. Risk factors for the spread of resistant bacteria in hospitals and the community can be summarised as over-crowding, lapses in hygiene or poor infection control practices. Increasing ant...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-199855030-00001

    authors: Rao GG

    更新日期:1998-03-01 00:00:00

  • Lemborexant: First Approval.

    abstract::Lemborexant (DAYVIGO™) is an orally administered, dual orexin receptor (OXR) antagonist that exhibits reversible competitive antagonism at OXR1 and OXR2 (> affinity at OXR2) that was discovered and developed by Eisai Inc. for the treatment of adult patients with insomnia. In December 2019, lemborexant received its fir...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.1007/s40265-020-01276-1

    authors: Scott LJ

    更新日期:2020-03-01 00:00:00

  • A comparison of nimesulide vs paracetamol in the treatment of pyrexia in the elderly.

    abstract::The efficacy and safety of rectally administered nimesulide 200mg and paracetamol 500mg were assessed in a double-blind study. The study was conducted in 39 elderly inpatients with infections of the upper or lower respiratory tract associated with fever; 18 patients received nimesulide and 21 received paracetamol. Bot...

    journal_title:Drugs

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.2165/00003495-199300461-00026

    authors: Cunietti E,Monti M,Viganò A,D'Aprile E,Saligari A,Scafuro E,Scaricabarozzi I

    更新日期:1993-01-01 00:00:00

  • Dofetilide: a review of its use in atrial fibrillation and atrial flutter.

    abstract:UNLABELLED:Dofetilide is a 'pure' class III antiarrhythmic agent which has demonstrated efficacy in the conversion of atrial fibrillation or flutter to sinus rhythm and the maintenance of sinus rhythm. By blocking the rapid component of the cardiac delayed rectifier potassium current (I(Kr)), dofetilide prolongs the ca...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-199958060-00007

    authors: McClellan KJ,Markham A

    更新日期:1999-12-01 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

  • Atorvastatin efficacy in the prevention of cardiovascular events in patients with diabetes mellitus and/or metabolic syndrome.

    abstract::Several large-scale clinical trials have assessed the efficacy of atorvastatin in the primary and secondary prevention of cardiovascular events in patients with diabetes mellitus and/or metabolic syndrome. In primary prevention, CARDS (Collaborative Atorvastatin Diabetes Study) showed that atorvastatin 10 mg/day (vs p...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-200767001-00005

    authors: Arca M

    更新日期:2007-01-01 00:00:00