Steady-state pharmacokinetics of controlled release oral morphine sulphate in healthy subjects.

Abstract:

:The pharmacokinetics of oral morphine sulphate as controlled release tablets ('MS-Contin') and solution were compared at steady-state. Plasma morphine concentrations were determined over 24 hours following the last dose of each drug when given in a randomised, crossover fashion to healthy subjects. Radioimmunoassay was used, which was sensitive yet provided good specificity relative to high-performance liquid chromatography. Controlled release tablets had 86% the bioavailability of the solution. Although each dose of controlled release tablets was double that of the solution, their peak plasma concentrations were the same. Time to maximum concentration was 3 times longer for controlled release tablets with an absorption half-life twice that of the solution. Elimination of both drugs was similar and biphasic with the minor terminal portion at 10 times the half-life of the major early process. These data explain the analgesic duration of 12 hours observed in clinical studies and the lack of accumulation with morphine compared with methadone.

journal_name

Clin Pharmacokinet

authors

Savarese JJ,Goldenheim PD,Thomas GB,Kaiko RF

doi

10.2165/00003088-198611060-00006

subject

Has Abstract

pub_date

1986-11-01 00:00:00

pages

505-10

issue

6

eissn

0312-5963

issn

1179-1926

journal_volume

11

pub_type

临床试验,杂志文章,随机对照试验
  • Ofloxacin pharmacokinetics in chronic renal failure and dialysis.

    abstract::Data on the pharmacokinetics of ofloxacin in chronic renal failure, in patients who were not dialysed or were receiving haemodialysis or continuous ambulatory peritoneal dialysis (CAPD), are reviewed. In addition, a large pool of data obtained in patients with a wide range of renal dysfunction is provided. The good ab...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.2165/00003088-199121050-00004

    authors: Lameire N,Rosenkranz B,Malerczyk V,Lehr KH,Veys N,Ringoir S

    更新日期:1991-11-01 00:00:00

  • Pharmacokinetics of cetirizine in tear fluid after a single oral dose.

    abstract:BACKGROUND:Antihistamines (histamine H(1) receptor antagonists) are effective and convenient drugs for the treatment of allergic conjunctivitis. Because of the short duration of action generally observed for drugs administered topically to the eye, the oral route is often preferred. However, the presence of a selective...

    journal_title:Clinical pharmacokinetics

    pub_type: 临床试验,杂志文章

    doi:10.2165/00003088-200241070-00006

    authors: Grumetto L,Cennamo G,Del Prete A,La Rotonda MI,Barbato F

    更新日期:2002-01-01 00:00:00

  • Pharmacokinetic considerations in the treatment of inflammatory bowel disease.

    abstract::This review describes the pharmacokinetics of the major drugs used for the treatment of inflammatory bowel disease. This information can be helpful for the selection of a particular agent and offers guidance for effective and well tolerated regimens. The corticosteroids have a short elimination half-life (t1/2beta) of...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.2165/00003088-200140100-00003

    authors: Schwab M,Klotz U

    更新日期:2001-01-01 00:00:00

  • Development of a Whole-Body Physiologically Based Pharmacokinetic Approach to Assess the Pharmacokinetics of Drugs in Elderly Individuals.

    abstract:BACKGROUND:Because of the vulnerability and frailty of elderly adults, clinical drug development has traditionally been biased towards young and middle-aged adults. Recent efforts have begun to incorporate data from paediatric investigations. Nevertheless, the elderly often remain underrepresented in clinical trials, e...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/s40262-016-0422-3

    authors: Schlender JF,Meyer M,Thelen K,Krauss M,Willmann S,Eissing T,Jaehde U

    更新日期:2016-12-01 00:00:00

  • Lack of Clinical Pharmacokinetic Studies to Optimize the Treatment of Neglected Tropical Diseases: A Systematic Review.

    abstract:INTRODUCTION:Neglected tropical diseases (NTDs) affect more than one billion people, mainly living in developing countries. For most of these NTDs, treatment is suboptimal. To optimize treatment regimens, clinical pharmacokinetic studies are required where they have not been previously conducted to enable the use of ph...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.1007/s40262-016-0467-3

    authors: Verrest L,Dorlo TPC

    更新日期:2017-06-01 00:00:00

  • Reduction of saquinavir exposure by coadministration of loperamide: a two-way pharmacokinetic interaction.

    abstract:OBJECTIVE:To assess any pharmacokinetic interactions between loperamide and saquinavir. DESIGN:Double-blind, double-dummy, randomised, placebo-controlled, three-way crossover trial. PARTICIPANTS:Twelve healthy male and female volunteers, aged 24-46 years. METHODS:Saquinavir and loperamide pharmacokinetics were deter...

    journal_title:Clinical pharmacokinetics

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.2165/00003088-200443140-00004

    authors: Mikus G,Schmidt L,Burhenne J,Ding R,Riedel KD,Tayrouz Y,Weiss J,Haefeli WE

    更新日期:2004-01-01 00:00:00

  • Pharmacodynamic, pharmacokinetic and pharmacogenetic aspects of drugs used in the treatment of Alzheimer's disease.

    abstract::With the aging population and its rapidly increasing prevalence, dementia has become an important public health concern in developed and developing countries. To date, the pharmacological treatment is symptomatic and based on the observed neurotransmitter disturbances. The four most commonly used drugs are donepezil, ...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.1007/s40262-013-0038-9

    authors: Noetzli M,Eap CB

    更新日期:2013-04-01 00:00:00

  • Drugs and Diseases Interacting with Cigarette Smoking in US Prescription Drug Labelling.

    abstract::The US Food and Drug Administration (FDA) draft guidance for industry on drug interaction studies recommends, but does not mandate, that both cigarette smokers and non-smokers can be used to study drug metabolism in clinical trials, and that important results related to smoking should be included in drug labelling to ...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.1007/s40262-015-0246-6

    authors: Li H,Shi Q

    更新日期:2015-05-01 00:00:00

  • Prediction of the Effect of Renal Impairment on the Pharmacokinetics of New Drugs.

    abstract:INTRODUCTION:Renal impairment may have a significant impact on the pharmacokinetics of drugs. Ad hoc studies in subjects with renal impairment are required by the regulatory authorities to propose dose adjustments in these subjects, to find a dosing regimen able to provide a systemic exposure similar to those in subjec...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/s40262-017-0574-9

    authors: Borella E,Poggesi I,Magni P

    更新日期:2018-04-01 00:00:00

  • Reliability of antiarrhythmic drug plasma concentration monitoring.

    abstract::Measurement of drug levels is becoming increasingly popular to optimise the dosage of various drugs. In the case of antiarrhythmic drugs, the narrow therapeutic margin of most of these agents and a direct relationship between their pharmacological effects and plasma concentrations would justify more widespread use of ...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.2165/00003088-198308010-00004

    authors: Follath F,Ganzinger U,Schuetz E

    更新日期:1983-01-01 00:00:00

  • Elucidating the Plasma and Liver Pharmacokinetics of Simeprevir in Special Populations Using Physiologically Based Pharmacokinetic Modelling.

    abstract::The disposition of simeprevir (SMV) in humans is characterised by cytochrome P450 3A4 metabolism and hepatic uptake by organic anion transporting polypeptide 1B1/3 (OATP1B1/3). This study was designed to investigate SMV plasma and liver exposure upon oral administration in subjects infected with hepatitis C virus (HCV...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/s40262-016-0476-2

    authors: Snoeys J,Beumont M,Monshouwer M,Ouwerkerk-Mahadevan S

    更新日期:2017-07-01 00:00:00

  • Comparison of the pharmacokinetics of cephradine and cefazolin in pregnant and non-pregnant women.

    abstract::The pharmacokinetics of cephradine, a cephalosporin with a low degree of protein binding, was studied in 12 women after oral and intravenous administration of the drug during and after pregnancy. Six of the 12 women also received a cephalosporin with a high degree of protein binding, cefazolin, intravenously during an...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章

    doi:10.2165/00003088-198712020-00004

    authors: Philipson A,Stiernstedt G,Ehrnebo M

    更新日期:1987-02-01 00:00:00

  • The fentanyl HCl patient-controlled transdermal system (PCTS): an alternative to intravenous patient-controlled analgesia in the postoperative setting.

    abstract::Inadequate pain control in the postoperative period not only contributes to patient discomfort, but also causes physiological changes that may result in increased risk of myocardial ischaemia, deep vein thrombosis and pulmonary embolism. These events complicate postoperative recovery and may lead to longer hospital st...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.2165/00003088-200544001-00002

    authors: Sinatra R

    更新日期:2005-01-01 00:00:00

  • Clarithromycin clinical pharmacokinetics.

    abstract::Clarithromycin is a semisynthetic macrolide antibiotic, structurally related to erythromycin. It has a more favourable pharmacokinetic profile than erythromycin, thus allowing twice-daily administration and possibly increasing compliance among outpatients. Clarithromycin is well absorbed from the gastrointestinal trac...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.2165/00003088-199325030-00003

    authors: Fraschini F,Scaglione F,Demartini G

    更新日期:1993-09-01 00:00:00

  • Pharmacokinetics of Hydroxychloroquine in Pregnancies with Rheumatic Diseases.

    abstract:BACKGROUND:Hydroxychloroquine is an oral drug prescribed to pregnant women with rheumatic disease to reduce disease activity and prevent flares. Physiologic changes during pregnancy may substantially alter drug pharmacokinetics. However, the effect of pregnancy on hydroxychloroquine disposition and the potential need f...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/s40262-018-0712-z

    authors: Balevic SJ,Green TP,Clowse MEB,Eudy AM,Schanberg LE,Cohen-Wolkowiez M

    更新日期:2019-04-01 00:00:00

  • Population pharmacokinetics of losmapimod in healthy subjects and patients with rheumatoid arthritis and chronic obstructive pulmonary diseases.

    abstract:BACKGROUND AND OBJECTIVE:Losmapimod is an orally available, potent p38 mitogen-activated protein kinase inhibitor. It is in development as an anti-inflammatory drug in different therapeutic areas. Clinical studies have shown that losmapimod is well tolerated and safe in humans and several studies have shown its pharmac...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,随机对照试验

    doi:10.1007/s40262-012-0025-6

    authors: Yang S,Lukey P,Beerahee M,Hoke F

    更新日期:2013-03-01 00:00:00

  • Population pharmacokinetic analysis of tesamorelin in HIV-infected patients and healthy subjects.

    abstract:BACKGROUND AND OBJECTIVES:Tesamorelin is a synthetic analogue of growth hormone-releasing factor (GRF), which increases basal and pulsatile growth hormone (GH) secretion and subsequently increases insulin-like growth factor (IGF)-1. Limited information is available about the pharmacokinetics of this compound. Consequen...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,随机对照试验

    doi:10.1007/s40262-014-0202-x

    authors: González-Sales M,Barrière O,Tremblay PO,Nekka F,Mamputu JC,Boudreault S,Tanguay M

    更新日期:2015-03-01 00:00:00

  • The relationship between fluticasone furoate systemic exposure and cortisol suppression.

    abstract:INTRODUCTION:The inhaled corticosteroid (ICS) fluticasone furoate is in development, in combination with the long-acting beta2-agonist vilanterol for the once-daily treatment of asthma and chronic obstructive pulmonary disease and as a monotherapy treatment for asthma. Corticosteroids, including ICSs, have the potentia...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,meta分析

    doi:10.1007/s40262-013-0078-1

    authors: Allen A

    更新日期:2013-10-01 00:00:00

  • Physiologic Indirect Response Modeling to Describe Buprenorphine Pharmacodynamics in Newborns Treated for Neonatal Opioid Withdrawal Syndrome.

    abstract:BACKGROUND AND OBJECTIVE:Buprenorphine has been shown to be effective in treating infants with neonatal opioid withdrawal syndrome. However, an evidence-based buprenorphine dosing strategy has not been established in the treatment of neonatal opioid withdrawal syndrome because of a lack of exposure-response data. The a...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/s40262-020-00939-2

    authors: Mizuno T,McPhail BT,Kamatkar S,Wexelblatt S,Ward L,Christians U,Akinbi HT,Vinks AA

    更新日期:2020-09-17 00:00:00

  • Covariance analysis of laboratory variance in steady-state serum phenytoin concentrations.

    abstract::Inpatients (n = 57) on long term prophylaxis with 2 oral phenytoin preparations were followed up via monthly checks of serum drug concentrations. Duplicate serum aliquots were submitted to 2 laboratories, and covariance analysis was used to estimate laboratory error. The laboratory-associated variance of examinations ...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章

    doi:10.2165/00003088-199120040-00007

    authors: Costeff H,Groswasser Z,Soroker N,van Belle G

    更新日期:1991-04-01 00:00:00

  • Clinical pharmacokinetics of intranasal sumatriptan.

    abstract::A substantial proportion of migraine patients have gastric stasis and suffer severe nausea and/or vomiting during their migraine attack. This may lead to erratic absorption from the gastrointestinal tract and make oral treatment unsatisfactory. For such patients, an intranasal formulation may be advantageous. Sumatrip...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.2165/00003088-200241110-00002

    authors: Fuseau E,Petricoul O,Moore KH,Barrow A,Ibbotson T

    更新日期:2002-01-01 00:00:00

  • Pharmacokinetics of metformin in girls aged 9 years.

    abstract:BACKGROUND AND OBJECTIVE:Metformin is a biguanide used in the treatment of type 2 diabetes mellitus. In girls with a low birth weight, and early-normal and rapidly progressive puberty, metformin therapy is capable of modifying this outcome, prolonging pubertal growth, increasing height gain, delaying the age at menarch...

    journal_title:Clinical pharmacokinetics

    pub_type: 临床试验,杂志文章

    doi:10.2165/11593970-000000000-00000

    authors: Sánchez-Infantes D,Díaz M,López-Bermejo A,Marcos MV,de Zegher F,Ibáñez L

    更新日期:2011-11-01 00:00:00

  • Clinical pharmacokinetics of leflunomide.

    abstract::Leflunomide is the first disease-modifying antirheumatic drug to be approved for rheumatoid arthritis in the past 10 years. Orally administered leflunomide is almost completely converted into its active metabolite A77 1726 (hereafter referred to as M1). M1 displays linear pharmacokinetics at the dosages of leflunomide...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章

    doi:10.2165/00003088-200241060-00003

    authors: Rozman B

    更新日期:2002-01-01 00:00:00

  • Geographical/interracial differences in polymorphic drug oxidation. Current state of knowledge of cytochromes P450 (CYP) 2D6 and 2C19.

    abstract::The isoenzymes which catalyse the polymorphic hydroxylations of debrisoquine/sparteine and S-mephenytoin are cytochromes P450 2D6 and P450 2C19 (CYP2D6 and CYP2C19), respectively. CYP2D6 is involved in the stereospecific metabolism of several important groups of drugs, for example antiarrhythmics, antidepressants and ...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.2165/00003088-199529030-00005

    authors: Bertilsson L

    更新日期:1995-09-01 00:00:00

  • Antiretroviral therapy : pharmacokinetic considerations in patients with renal or hepatic impairment.

    abstract::Hepatic and renal insufficiency due to co-infection, alcoholism, diabetes mellitus, family history, adverse effects of antiretrovirals and other factors are commonly seen in HIV-infected patients. Therefore, the use of antiretrovirals in this patient setting requires attention to the pharmacokinetic issues that clinic...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.2165/00003088-200847030-00002

    authors: McCabe SM,Ma Q,Slish JC,Catanzaro LM,Sheth N,DiCenzo R,Morse GD

    更新日期:2008-01-01 00:00:00

  • Interchangeability and predictive performance of empirical tolerance models.

    abstract::Models of tolerance are commonly derived on empirical grounds, because of lack of knowledge about the mechanism of tolerance or because of the difficulty of appropriately simplifying complex physiological processes. The present study was performed to evaluate the interchangeability of tolerance models used in the lite...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.2165/00003088-199936020-00005

    authors: Gårdmark M,Brynne L,Hammarlund-Udenaes M,Karlsson MO

    更新日期:1999-02-01 00:00:00

  • Blockade of the High-Affinity Interleukin-2 Receptors with Daclizumab High-Yield Process: Pharmacokinetic/Pharmacodynamic Analysis of Single- and Multiple-Dose Phase I Trials.

    abstract:BACKGROUND AND OBJECTIVE:Daclizumab high-yield process (DAC HYP) is a humanized monoclonal antibody that selectively blocks the α-subunit (CD25) of the high-affinity interleukin-2 receptors, and has shown robust efficacy as a treatment for multiple sclerosis (MS). This work quantitatively characterized the relationship...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,随机对照试验

    doi:10.1007/s40262-015-0305-z

    authors: Minocha M,Tran JQ,Sheridan JP,Othman AA

    更新日期:2016-01-01 00:00:00

  • Clinical Pharmacokinetics and Pharmacodynamics of the Epidermal Growth Factor Receptor Inhibitor Panitumumab in the Treatment of Colorectal Cancer.

    abstract::Despite progress in the treatment of metastatic colorectal cancer (mCRC) in the last 15 years, it is still a condition with a relatively low 5-year survival rate. Panitumumab, a fully human monoclonal antibody directed against the epidermal growth factor receptor (EGFR), is able to prolong survival in patients with mC...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.1007/s40262-017-0590-9

    authors: Ketzer S,Schimmel K,Koopman M,Guchelaar HJ

    更新日期:2018-04-01 00:00:00

  • Pharmacokinetics of the Soluble Guanylate Cyclase Stimulator Riociguat in Healthy Young Chinese Male Non-Smokers and Smokers: Results of a Randomized, Double-Blind, Placebo-Controlled Study.

    abstract:BACKGROUND AND OBJECTIVES:The aim of this study was to investigate the pharmacokinetics, safety, and tolerability of riociguat after single and multiple oral doses of 1 or 2 mg three times daily (tid), and to determine the effect of smoking on riociguat pharmacokinetics in Chinese men. METHODS:In a randomized, double-...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,随机对照试验

    doi:10.1007/s40262-015-0337-4

    authors: Zhao X,Wang Z,Wang Y,Zhang H,Blode H,Yoshikawa K,Becker C,Unger S,Frey R,Cui Y

    更新日期:2016-05-01 00:00:00

  • Drug, meal and formulation interactions influencing drug absorption after oral administration. Clinical implications.

    abstract::Drug-drug, drug-formulation and drug-meal interactions are of clinical concern for orally administered drugs that possess a narrow therapeutic index. This review presents the current status of information regarding interactions which may influence the gastrointestinal (GI) absorption of orally administered drugs. Abso...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.2165/00003088-199936030-00004

    authors: Fleisher D,Li C,Zhou Y,Pao LH,Karim A

    更新日期:1999-03-01 00:00:00