[Pharmacokinetics of buprenorphine in subcutaneous administration]. 1995

I Gralow, and W F von Hornstein, and E Schleyer, and W Hiddemann
Schmerzambulanz und -Tagesklinik der Klinik, Westfälischen Wilhelms-Universität Münster.

In this study investigations were carried out on pharmacokinetics of buprenorphine after it had been applied subcutaneously. Up to now no pharmacokinetic data exist using this kind of application with relevant clinical doses. METHODS With 6 patients, who had major general surgery under balanced anaesthesia, buprenorphine was given in a single subcutaneous injection of 5 micrograms/kg bodyweight for postoperative pain relief. Over a period of 48 hours the level of buprenorphine in blood plasma was measured. The analyses were done with a modified HPLC method with electrochemical detection which is able to achieve measurements as low as 40 pg/ml of plasma. The pharmacokinetic values were calculated with the "Topfit" pharmacokinetic computerised programme. RESULTS Whereas the period of time (tmax) to reach peak plasma concentration (Cmax) after subcutaneous application is much longer than with other parenteral application forms, the plasma concentration levels tend to be similar after 20 minutes. The most important finding of this study is that the mean terminal half-life (t1/2c) of buprenorphine is 23 hours. However, the presently available data for other application forms in respect to terminal half-life did not produce the same results. This can be explained by the use of insufficiently sensitive analytical procedures and by too short periods of observation of 3 and 13 hours respectively, leading to values of t1/2c of 2 and 5 hours. CONCLUSIONS These results indicate that the terminal half-life (t1/2c) of buprenorphine is much longer than had been supposed. It confirms clinical findings of sufficient pain relief by showing measurable uptake of buprenorphine after subcutaneous application.

UI MeSH Term Description Entries
D007279 Injections, Subcutaneous Forceful administration under the skin of liquid medication, nutrient, or other fluid through a hollow needle piercing the skin. Subcutaneous Injections,Injection, Subcutaneous,Subcutaneous Injection
D008297 Male Males
D008657 Metabolic Clearance Rate Volume of biological fluid completely cleared of drug metabolites as measured in unit time. Elimination occurs as a result of metabolic processes in the kidney, liver, saliva, sweat, intestine, heart, brain, or other site. Total Body Clearance Rate,Clearance Rate, Metabolic,Clearance Rates, Metabolic,Metabolic Clearance Rates,Rate, Metabolic Clearance,Rates, Metabolic Clearance
D008875 Middle Aged An adult aged 45 - 64 years. Middle Age
D010147 Pain Measurement Scales, questionnaires, tests, and other methods used to assess pain severity and duration in patients or experimental animals to aid in diagnosis, therapy, and physiological studies. Analgesia Tests,Analogue Pain Scale,Formalin Test,McGill Pain Questionnaire,Nociception Tests,Pain Assessment,Pain Intensity,Pain Severity,Tourniquet Pain Test,Visual Analogue Pain Scale,Analog Pain Scale,Assessment, Pain,McGill Pain Scale,Visual Analog Pain Scale,Analgesia Test,Analog Pain Scales,Analogue Pain Scales,Formalin Tests,Intensity, Pain,Measurement, Pain,Nociception Test,Pain Assessments,Pain Intensities,Pain Measurements,Pain Questionnaire, McGill,Pain Scale, Analog,Pain Scale, Analogue,Pain Scale, McGill,Pain Severities,Pain Test, Tourniquet,Questionnaire, McGill Pain,Scale, Analog Pain,Scale, Analogue Pain,Scale, McGill Pain,Severity, Pain,Test, Analgesia,Test, Formalin,Test, Nociception,Test, Tourniquet Pain,Tests, Nociception,Tourniquet Pain Tests
D010149 Pain, Postoperative Pain during the period after surgery. Acute Post-operative Pain,Acute Postoperative Pain,Chronic Post-operative Pain,Chronic Post-surgical Pain,Chronic Postoperative Pain,Chronic Postsurgical Pain,Pain, Post-operative,Persistent Postsurgical Pain,Post-operative Pain,Post-operative Pain, Acute,Post-operative Pain, Chronic,Post-surgical Pain,Postoperative Pain, Acute,Postoperative Pain, Chronic,Postsurgical Pain,Postoperative Pain,Acute Post operative Pain,Chronic Post operative Pain,Chronic Post surgical Pain,Chronic Postsurgical Pains,Pain, Acute Post-operative,Pain, Acute Postoperative,Pain, Chronic Post-operative,Pain, Chronic Post-surgical,Pain, Chronic Postoperative,Pain, Chronic Postsurgical,Pain, Persistent Postsurgical,Pain, Post operative,Pain, Post-surgical,Pain, Postsurgical,Post operative Pain,Post operative Pain, Acute,Post operative Pain, Chronic,Post surgical Pain,Post-operative Pains,Post-surgical Pain, Chronic,Postsurgical Pain, Chronic,Postsurgical Pain, Persistent
D002047 Buprenorphine A derivative of the opioid alkaloid THEBAINE that is a more potent and longer lasting analgesic than MORPHINE. It appears to act as a partial agonist at mu and kappa opioid receptors and as an antagonist at delta receptors. The lack of delta-agonist activity has been suggested to account for the observation that buprenorphine tolerance may not develop with chronic use. 6029-M,Buprenex,Buprenorphine Hydrochloride,Buprex,Prefin,RX-6029-M,Subutex,Temgesic,Temgésic,6029 M,6029M,Hydrochloride, Buprenorphine,RX 6029 M,RX6029M
D005260 Female Females
D006207 Half-Life The time it takes for a substance (drug, radioactive nuclide, or other) to lose half of its pharmacologic, physiologic, or radiologic activity. Halflife,Half Life,Half-Lifes,Halflifes
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man

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