The Experts below are selected from a list of 306 Experts worldwide ranked by ideXlab platform

Geoffrey K. Gourlay - One of the best experts on this subject based on the ideXlab platform.

  • Sustained Relief of Chronic Pain
    Clinical Pharmacokinetics, 1998
    Co-Authors: Geoffrey K. Gourlay
    Abstract:

    There are a number of modified release formulations of morphine with recommended dosage intervals of either 12 or 24 hours, including tablets (MS Contin®, Oramorph SR®), capsules (Kapanol®, Skenan®), suspension and suppositories. Orally administered solid dosage forMS are most popular but significant differences exist in the resultant pharmacokinetics and bioequivalence status of morphine after both single doses and at steady state. Following single doses, the plasma morphine concentrations showed pronounced differences in the 0- to 12-hour period with a 4- to 5-fold difference in the mean peak concentration (C_max) for morphine and the time to C_max(t_max) The area under the concentration-time curve (AUC) from 0 to 24 hours for the 4 formulations show greater similarity. None of the formulations were shown to be bioequivalent according to US Food and Drug Administration (FDA) criteria. At steady state, fluctuations in plasma morphine concentrations throughout a 12-hour dosage interval were greatest for MS Contin and least for Kapanol. In fact, the relatively small fluctuations in plasma morphine concentrations following Kapanol administration suggested the same formulation could successfully be used with a 24-hour dosage interval. The pharmacokinetic parameters of morphine following Kapanol once daily were similar to MS Contin (12 hours) with the obvious exception of the longer t_max. There is also another once daily oral morphine preparation (MXL) which has been shown to be bioequivalent to Kapanol under fasting conditions only in a single dose study in volunteers. Food has been shown to have an effect on the pharmacokinetics of morphine following doses of immediate release solution and the modified release preparations. However, bioequivalence is generally maintained between the fed and fasting states for most preparations. MS Contin tablets have been administered rectally, but morphine pharmacokinetic parameters show greater variability compared with oral administration and the 2 routes are not bioequivalent. The results suggest a slower rate but greater extent of morphine adsorption. Somwhat similar results were obtained when Kapanol granules are administered rectally. The morphine pharmacokinetics following administration of a specifically formulated controlled release suppository showed less variability (rectal bioavailability was 42%). The pronounced differences in morphine pharmacokinetics between the various formulations are not translated into measurable differences in the pharmaco-dynamic effects of pain relief and adverse effects. The lack of bioequivalence between some of the formulations suggests that care should be exercised if physicians change modified release formulations as dosage adjustments may be necessary in some patients.

  • Sustained Relief of Chronic Pain Pharmacokinetics of Sustained Release Morphine
    Clinical pharmacokinetics, 1998
    Co-Authors: Geoffrey K. Gourlay
    Abstract:

    There are a number of modified release formulations of morphine with recommended dosage intervals of either 12 or 24 hours, including tablets (MS Contin, Oramorph SR), capsules (Kapanol, Skenan), suspension and suppositories. Orally administered solid dosage forMS are most popular but significant differences exist in the resultant pharmacokinetics and bioequivalence status of morphine after both single doses and at steady state. Following single doses, the plasma morphine concentrations showed pronounced differences in the 0- to 12-hour period with a 4- to 5-fold difference in the mean peak concentration (Cmax) for morphine and the time to Cmax (tmax) The area under the concentration-time curve (AUC) from 0 to 24 hours for the 4 formulations show greater similarity. None of the formulations were shown to be bioequivalent according to US Food and Drug Administration (FDA) criteria. At steady state, fluctuations in plasma morphine concentrations throughout a 12-hour dosage interval were greatest for MS Contin and least for Kapanol. In fact, the relatively small fluctuations in plasma morphine concentrations following Kapanol administration suggested the same formulation could successfully be used with a 24-hour dosage interval. The pharmacokinetic parameters of morphine following Kapanol once daily were similar to MS Contin (12 hours) with the obvious exception of the longer tmax. There is also another once daily oral morphine preparation (MXL) which has been shown to be bioequivalent to Kapanol under fasting conditions only in a single dose study in volunteers. Food has been shown to have an effect on the pharmacokinetics of morphine following doses of immediate release solution and the modified release preparations. However, bioequivalence is generally maintained between the fed and fasting states for most preparations. MS Contin tablets have been administered rectally, but morphine pharmacokinetic parameters show greater variability compared with oral administration and the 2 routes are not bioequivalent. The results suggest a slower rate but greater extent of morphine adsorption. Somewhat similar results were obtained when Kapanol granules are administered rectally. The morphine pharmacokinetics following administration of a specifically formulated controlled release suppository showed less variability (rectal bioavailability was 42%). The pronounced differences in morphine pharmacokinetics between the various formulations are not translated into measurable differences in the pharmacodynamic effects of pain relief and adverse effects. The lack of bioequivalence between some of the formulations suggests that care should be exercised if physicians change modified release formulations as dosage adjustments may be necessary in some patients.

  • Pharmacokinetics and pharmacodynamics of twenty-four-hourly Kapanol compared to twelve-hourly MS Contin in the treatment of severe cancer pain.
    Pain, 1997
    Co-Authors: Geoffrey K. Gourlay, David A. Cherry, Margaret M. Onley, Simon G Tordoff, David A Conn, Gillian M Hood, John L. Plummer
    Abstract:

    Twenty-four patients with severe pain related to cancer completed a randomised, double-blind, double-dummy, crossover study examining morphine pharmacokinetics and pharmacodynamics when the same 24-h morphine dose was administered using two modified release oral morphine formulations; either one dose of Kapanol (a new sustained release polymer coated pellet formulation administered in capsule form, Glaxo Wellcome group of companies) per 24 h, or MS Contin (Purdue Frederick Company, Connecticut, USA) administered at 12-h intervals. The morphine dose was optimised for each patient using an immediate release morphine solution in the lead-in period to provide the most favourable balance between pain relief and side-effects. Patients were then randomly allocated to receive their 24-h morphine dose as either Kapanol or MS Contin in period 1. Patients recorded daily measures of pain relief and morphine related side-effects (morphine pharmacodynamics) in a diary. Patients were admitted to the Pain Management Unit on the morning of day 7 (+/- 1 day) and frequent blood samples were collected for 24 h following the 10:00 h dose to fully characterise the pharmacokinetic profile for morphine and its metabolites at steady state. Morphine pharmacodynamics and the amount and timing of rescue medication (dextromoramide) were also recorded during this time. Period 2, which commenced at 10:00 h on day 8, was identical to period 1 except the modified release formulations were changed. The pharmacokinetic profile of Kapanol exhibited a significantly higher Cmin (minimum plasma morphine concentration), less fluctuation in plasma morphine concentration throughout the dosing interval, a longer Tmax (time associated with the maximum morphine concentration) and a greater time that the plasma morphine concentration was > or = 75% of Cmax (an index of the control the formulation exerts over the morphine release rate) compared to that of MS Contin. Some of these pharmacokinetic differences (e.g., Cmin and fluctuation in plasma morphine concentration) were surprising given that the dosing interval for Kapanol (24 h) was double that of MS Contin (12 h). There was no significant difference between the Kapanol and MS Contin treatment phases in any of the pharmacodynamic parameters, morphine related side-effects, the percentage of patients taking rescue medication as well as the amount or time to the first dose of rescue analgesia on day 7 in periods 1 and 2, patient or investigator assessments of global efficacy at the end of periods 1 and 2, or patient treatment preference at the end of the study. Once a day Kapanol provided the same degree of pain relief and morphine related side-effects as 12-h MS Contin.

  • 897 Once a day (i.e. 24 hourly) kapanolTM, a new sustained release morphine formulation, in the treatment of cancer pain: Pharmacokinetic aspects
    European Journal of Cancer, 1995
    Co-Authors: Geoffrey K. Gourlay, David A. Cherry, Margaret M. Onley, Simon G Tordoff, David A Conn, John L. Plummer
    Abstract:

    Sustained release morphine formulations are now generally accepted as the formulations of choice in the treatment of severe cancer pain. Kapanol™/Kadian™ (Glaxo/Faulding), a new sustained release formulation consisting of polymer coated pellets in a capsule, has recently been shown to have a superior morphine release profile compared to the standard tablet, MS Contin. If fact, the release characteristics of morphine from Kapanol suggested the possibility that one oral dose of Kapanol per 24 hours could effectively treat severe cancer pain. Twenty four patients completed a randomised, double-blind, two period, crossover study comparing 24-hourly Kapanol to 12-hourly MS Contin. The morphine dose per 24 hours was identical for the two formulations and morphine pharmacokinetics were determined over 24 hours at steady state for each formulation (i.e. after 7 days). The Cmax, Cmin, AUC and fluctuations in plasma morphine concentrations were not significantly different between the two formulations ( P  > 0.05, repeated measures ANOVA). Kapanol had significantly longer Tmax values (P

  • Pharmacological management of chronic pain: a clinician's perspective.
    Inflammation Research, 1994
    Co-Authors: David A. Cherry, Geoffrey K. Gourlay
    Abstract:

    Of the currently available mu agonist drugs, the following are relatively contraindicated: Morphine remains the drug of choice for chronic pain when administered in a sustained release preparation. MS Contin, a slow release oral formulation of morphine, is available and has a predictable duration of action lasting from 8–12 h, while improved formulations are about to be released in the near future in some countries. Prescribers need to take into account the relatively poor oral bioavailability of morphine when calculating the daily morphine dose.

John L. Plummer - One of the best experts on this subject based on the ideXlab platform.

  • Pharmacokinetics and pharmacodynamics of twenty-four-hourly Kapanol compared to twelve-hourly MS Contin in the treatment of severe cancer pain.
    Pain, 1997
    Co-Authors: Geoffrey K. Gourlay, David A. Cherry, Margaret M. Onley, Simon G Tordoff, David A Conn, Gillian M Hood, John L. Plummer
    Abstract:

    Twenty-four patients with severe pain related to cancer completed a randomised, double-blind, double-dummy, crossover study examining morphine pharmacokinetics and pharmacodynamics when the same 24-h morphine dose was administered using two modified release oral morphine formulations; either one dose of Kapanol (a new sustained release polymer coated pellet formulation administered in capsule form, Glaxo Wellcome group of companies) per 24 h, or MS Contin (Purdue Frederick Company, Connecticut, USA) administered at 12-h intervals. The morphine dose was optimised for each patient using an immediate release morphine solution in the lead-in period to provide the most favourable balance between pain relief and side-effects. Patients were then randomly allocated to receive their 24-h morphine dose as either Kapanol or MS Contin in period 1. Patients recorded daily measures of pain relief and morphine related side-effects (morphine pharmacodynamics) in a diary. Patients were admitted to the Pain Management Unit on the morning of day 7 (+/- 1 day) and frequent blood samples were collected for 24 h following the 10:00 h dose to fully characterise the pharmacokinetic profile for morphine and its metabolites at steady state. Morphine pharmacodynamics and the amount and timing of rescue medication (dextromoramide) were also recorded during this time. Period 2, which commenced at 10:00 h on day 8, was identical to period 1 except the modified release formulations were changed. The pharmacokinetic profile of Kapanol exhibited a significantly higher Cmin (minimum plasma morphine concentration), less fluctuation in plasma morphine concentration throughout the dosing interval, a longer Tmax (time associated with the maximum morphine concentration) and a greater time that the plasma morphine concentration was > or = 75% of Cmax (an index of the control the formulation exerts over the morphine release rate) compared to that of MS Contin. Some of these pharmacokinetic differences (e.g., Cmin and fluctuation in plasma morphine concentration) were surprising given that the dosing interval for Kapanol (24 h) was double that of MS Contin (12 h). There was no significant difference between the Kapanol and MS Contin treatment phases in any of the pharmacodynamic parameters, morphine related side-effects, the percentage of patients taking rescue medication as well as the amount or time to the first dose of rescue analgesia on day 7 in periods 1 and 2, patient or investigator assessments of global efficacy at the end of periods 1 and 2, or patient treatment preference at the end of the study. Once a day Kapanol provided the same degree of pain relief and morphine related side-effects as 12-h MS Contin.

  • 897 Once a day (i.e. 24 hourly) kapanolTM, a new sustained release morphine formulation, in the treatment of cancer pain: Pharmacokinetic aspects
    European Journal of Cancer, 1995
    Co-Authors: Geoffrey K. Gourlay, David A. Cherry, Margaret M. Onley, Simon G Tordoff, David A Conn, John L. Plummer
    Abstract:

    Sustained release morphine formulations are now generally accepted as the formulations of choice in the treatment of severe cancer pain. Kapanol™/Kadian™ (Glaxo/Faulding), a new sustained release formulation consisting of polymer coated pellets in a capsule, has recently been shown to have a superior morphine release profile compared to the standard tablet, MS Contin. If fact, the release characteristics of morphine from Kapanol suggested the possibility that one oral dose of Kapanol per 24 hours could effectively treat severe cancer pain. Twenty four patients completed a randomised, double-blind, two period, crossover study comparing 24-hourly Kapanol to 12-hourly MS Contin. The morphine dose per 24 hours was identical for the two formulations and morphine pharmacokinetics were determined over 24 hours at steady state for each formulation (i.e. after 7 days). The Cmax, Cmin, AUC and fluctuations in plasma morphine concentrations were not significantly different between the two formulations ( P  > 0.05, repeated measures ANOVA). Kapanol had significantly longer Tmax values (P

Jacques R Caldwell - One of the best experts on this subject based on the ideXlab platform.

  • Avinza® – 24-h sustained-release oral morphine therapy
    Expert opinion on pharmacotherapy, 2004
    Co-Authors: Jacques R Caldwell
    Abstract:

    Avinza is a once-daily, extended-release oral morphine preparation. It has a pharmacokinetic profile that exhibits less peak-to-trough fluctuations in plasma concentration whilst providing analgesia statistically identical to that produced by MS Contin (controlled-release morphine sulfate), OxyContin (oxycodone HCl controlled-release) and six doses of oral morphine sulfate administered every 4 h. Avinza improves quality of sleep by several measures but interestingly gives the best sleep improvement when given in the morning rather than at night. It causes the same side effects of other opioids: constipation, nausea, vomiting, somnolence and mood swings. Doses of 30 - 60 mg/day have been shown to be well tolerated by patients with osteoarthritis (even in the elderly), who have failed other medications.

  • efficacy and safety of a once daily morphine formulation in chronic moderate to severe osteoarthritis pain results from a randomized placebo controlled double blind trial and an open label extension trial
    Journal of Pain and Symptom Management, 2002
    Co-Authors: Jacques R Caldwell, Ronald J Rapoport, Jeffrey C Davis, Howard Offenberg, Howard W Marker, Sanford H Roth, William Yuan, Lise Eliot, Najib Babul, Pia Mikkelsen Lynch
    Abstract:

    Abstract A randomized, 4-week, double-blind trial followed by an open-label extension trial assessed the efficacy and safety of a once-daily, extended-release morphine formulation (Avinza™ (previously referred to as Morphelan™)) in 295 patients with chronic, moderate-to-severe osteoarthritis pain who had failed to obtain adequate pain relief with NSAIDs and acetaminophen. Participants received one of four treatments: Avinza 30 mg once daily (QAM or QPM), MS Contin® 15 mg twice daily, or placebo twice daily. Patients (n =181) received Avinza QAM or QPM during the 26-week open-label extension trial and could increase their dose to optimize pain control. Avinza and MS Contin reduced pain and improved several sleep measures versus placebo. Analgesic efficacy was comparable between Avinza and MS Contin; however, Avinza QAM demonstrated greater improvements in overall quality of sleep. The most common adverse events were constipation and nausea. The majority of AEs occurred at a similar incidence among the active treatment groups.

R Mahmoud - One of the best experts on this subject based on the ideXlab platform.

  • quality of life and cancer pain satisfaction and side effects with transdermal fentanyl versus oral morphine
    Journal of Clinical Oncology, 1998
    Co-Authors: Richard Payne, Susan D Mathias, David J Pasta, L A Wanke, R Williams, R Mahmoud
    Abstract:

    PURPOSETo compare pain-related treatment satisfaction, patient-perceived side effects, functioning, and well-being in patients with advanced cancer who were receiving either transdermal fentanyl (Duragesic, Janssen Pharmaceuticals, Titusville, NJ) or sustained-release oral forMS of morphine (MS Contin, Perdue Frederick Co, Norwalk, CT, or Oramorph SR, Roxanne Laboratories, Columbus, OH).PATIENTS AND METHODSA total of 504 assessable cancer patients participated in this cross-sectional, quality-of-life study. Relevant elements of four validated scales were used--the Functional Assessment of Cancer Therapy-General (FACT-G) scale, the Brief Pain Inventory (BPI), the Medical Outcomes Study (MOS) questionnaire, and the Memorial Symptom Assessment Scale (MSAS)--as well as original scales that were developed and validated for this study.RESULTSThe majority of patients in both treatment groups had late-stage (IV/D) cancer. Patients who received transdermal fentanyl were more satisfied overall with their pain medic...

Zhang Rui-l - One of the best experts on this subject based on the ideXlab platform.