Dataset Information

Pharmacokinetics of transdermal buprenorphine patch in the elderly.

ABSTRACT:

Purpose

Transdermal buprenorphine patches provide comparable pain relief to that of low-potency opioids in elderly individuals. However, specific data on their use in elderly individuals is limited. This study investigated and compared the PK of buprenorphine transdermal patches in elderly (? 75 years) versus younger (50-60 years) individuals.

Methods

This was a multiple-dose, open-label, parallel-group study in healthy volunteers split into two age groups (younger, 50-60 years; elderly, ? 75 years) with 37 individuals in each. Study participants received two consecutive 7-day buprenorphine 5 ?g/h transdermal patch applications, and blood samples were collected on the week of the second patch application [day 7 (predose), days 8, 9, 10, 12, and 14] to determine PK at steady state. Pharmacokinetic parameters were determined for buprenorphine and norbuprenorphine. Safety was assessed by analyzing adverse events, hematology, clinical chemistry, urine analysis, vital signs, electrocardiogram (ECG), and physical examinations.

Results

The area under the plasma concentration-time curve at steady state (AUC(tau)), measured over one dosing interval, was similar for elderly [mean ± standard deviation (SD) 9,940 pg/h/ml (4,827 pg/h/ml] and younger [mean ± SD 11,309 (3,670 pg/h/ml] individuals. Bioequivalence was not demonstrated between groups, which may be attributable to the relatively high level of variability in individual plasma profiles. More adverse events were reported by younger (216) than elderly (164) study participants.

Conclusions

No dosage alterations are necessary for PK reasons when treating elderly people with buprenorphine transdermal patches.

SUBMITTER: Al-Tawil N

PROVIDER: S-EPMC3548110 | biostudies-literature | 2013 Feb

REPOSITORIES: biostudies-literature

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Publications

Pharmacokinetics of transdermal buprenorphine patch in the elderly.

Al-Tawil Nabil N Odar-Cederlöf Ingegerd I Berggren Anna-Carin AC Johnson Helen E HE Persson Jan J

European journal of clinical pharmacology 20120617 2

<h4>Purpose</h4>Transdermal buprenorphine patches provide comparable pain relief to that of low-potency opioids in elderly individuals. However, specific data on their use in elderly individuals is limited. This study investigated and compared the PK of buprenorphine transdermal patches in elderly (≥ 75 years) versus younger (50-60 years) individuals.<h4>Methods</h4>This was a multiple-dose, open-label, parallel-group study in healthy volunteers split into two age groups (younger, 50-60 years; e ...[more]

PMID: 22706617

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Project description:Background and objectivesRotigotine is a dopamine receptor agonist with activity across the D1 through to D5 receptors as well as select serotonergic and adrenergic sites; continuous transdermal delivery of rotigotine with replacement of the patch once daily maintains stable plasma concentrations over 24 h. Rotigotine is indicated for the treatment of early and advanced-stage Parkinson's disease and moderate-to-severe idiopathic restless legs syndrome. The pharmacokinetics and pharmacodynamics of a drug may vary between subjects of different ethnic origin. This study evaluated the pharmacokinetics, safety, and tolerability of single-dose treatment with rotigotine transdermal patch in Japanese and Caucasian subjects.MethodsIn this open-label, parallel-group study, healthy male and female subjects of Japanese or Caucasian ethnic origin were matched by sex, body mass index, and age. A single transdermal patch delivering 2 mg/24 h rotigotine (patch content 4.5 mg) was applied to the ventral/lateral abdomen for 24 h. The main outcome measures were the plasma concentrations of unconjugated and total rotigotine and its desalkyl metabolites and derived pharmacokinetic parameters (area under the concentration-time curve from time zero to last quantifiable concentration [AUClast], maximum plasma concentration [Cmax], and body weight- and dose-normalized values).ResultsThe pharmacokinetic analysis included 48 subjects (24 Japanese, 24 Caucasian). The mean apparent dose of rotigotine was 2.0±0.5 mg for Japanese subjects and 2.08±0.58 mg for Caucasians. Plasma concentration-time profiles of unconjugated rotigotine and of the main metabolites were similar for both ethnic groups. Parameters of model-independent pharmacokinetics, Cmax, time to Cmax (tmax), and AUClast, for unconjugated rotigotine showed no statistically significant differences between Japanese and Caucasian subjects. Values of concentration-dependent pharmacokinetic parameters were higher in female subjects; this difference was minimized after correction for body weight. A statistically significant difference between ethnic groups was observed for total rotigotine concentrations (total rotigotine=unconjugated rotigotine+conjugated rotigotine), with slightly lower values in Caucasians after correction for body weight and apparent dose. No relevant differences were observed between males and females. Inter-individual variability was high. The terminal half-life for unconjugated rotigotine was 5.3 h in Japanese subjects and 5.7 h in Caucasians; corresponding values for total rotigotine were 8.6 h and 9.6 h. Less than 0.1% of the apparent dose was renally excreted as the parent compound. Renal elimination of total rotigotine covers 11.7% of absorbed dose in Japanese subjects and 10.8% of the absorbed dose in Caucasians, whereas the renal elimination via total despropyl rotigotine was 8.2 and 7.1%, respectively. The corresponding values for total desthienylethyl rotigotine were 3.5% in Japanese subjects and 4.2% Caucasians. Most adverse events were mild in intensity and typical for dopamine agonists or for transdermal therapeutics.ConclusionAdministration of a single patch delivering 2 mg/24 h rotigotine resulted in comparable pharmacokinetic profiles in Japanese and Caucasian subjects. The rotigotine transdermal patch was generally well-tolerated. Our findings suggest similar dose requirements for Japanese and Caucasian populations.

Project description:IntroductionPain management in patients with hip fractures can be challenging. Poor pain control is associated with reduced mobility and increased morbidity. Inadequate analgesia in patients with dementia is a concern. After using several different alternatives, transdermal buprenorphine was chosen as a standardised approach for analgesia in patients with fragility fracture in our hospital. There is limited evidence on the use of buprenorphine in this population. Our aim was to investigate the safety and effectiveness of transdermal buprenorphine in patients with hip fractures.MethodsA review of consecutive patients presenting with a hip fracture from June 2018 to December 2018 was conducted using medical records. Our primary outcome was the incidence of complications as a consequence of transdermal buprenorphine. Our secondary outcome was adequate analgesia measured by reviewing the requirement for analgesia during the first week following the patient's admission. Analgesia demands were considered adequate if patients required less than 20 mg of oral morphine in total during the first week following injury.ResultsIn total, 148 patients presented with a hip fracture during the study period. 128 patients had documented evidence of buprenorphine patch application. Complete data was available for the primary outcome of complications in all cases. Data was available for the secondary outcome in 124 patients. Buprenorphine was discontinued in 24 patients (19%), most commonly due to due to concerns about contribution to hypoactive delirium (9%), and when strong analgesia was no longer required (4%). There were no severe complications. Adequate analgesia was achieved using this regime in 68% patients. 38 patients (32%) required more than 20 mg of oral morphine sulphate solution in the first week post-admission.ConclusionThis series suggests that transdermal buprenorphine is safe and effective in the management of pain following a neck of femur fragility fracture.

Dataset Information

Pharmacokinetics of transdermal buprenorphine patch in the elderly.

Purpose

Methods

Results

Conclusions

Publications

Pharmacokinetics of transdermal buprenorphine patch in the elderly.

Similar Datasets

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