Pharmacokinetics and -dynamics of intramuscular and intranasal naloxone: an explorative study in healthy volunteers
| Autor: | Trond Sand, Ida Tylleskar, Øyvind Salvesen, Turid Nilsen, Ola Dale, Arne Kristian Skulberg, Sissel Skarra, Thorsteinn Loftsson |
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| Jazyk: | angličtina |
| Rok vydání: | 2018 |
| Předmět: |
Adult
Male Narcotic Antagonists Remifentanil Pain Drug overdose 030226 pharmacology & pharmacy Injections Intramuscular Models Biological 03 medical and health sciences Young Adult 0302 clinical medicine Pharmacokinetics Piperidines Naloxone Medicine Humans Pharmacology (medical) 030212 general & internal medicine Administration Intranasal Pharmacology Cross-Over Studies business.industry Opioid overdose Pupil General Medicine Miosis medicine.disease Healthy Volunteers Analgesics Opioid Opioid Anesthesia Pharmacodynamics Female business Pupillometry medicine.drug |
| Zdroj: | European Journal of Clinical Pharmacology |
| Popis: | This study aimed to develop a model for pharmacodynamic and pharmacokinetic studies of naloxone antagonism under steady-state opioid agonism and to compare a high-concentration/low-volume intranasal naloxone formulation 8 mg/ml to intramuscular 0.8 mg. Two-way crossover in 12 healthy volunteers receiving naloxone while receiving remifentanil by a target-controlled infusion for 102 min. The group were subdivided into three different doses of remifentanil. Blood samples for serum naloxone concentrations, pupillometry and heat pain threshold were measured. The relative bioavailability of intranasal to intramuscular naloxone was 0.75. Pupillometry showed difference in antagonism; the effect was significant in the data set as a whole (p |
| Databáze: | OpenAIRE |
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