Pharmacokinetics of dinalbuphine sebacate and nalbuphine in human after intramuscular injection of dinalbuphine sebacate in an extended‐release formulation

@article{Tien2017PharmacokineticsOD,
  title={Pharmacokinetics of dinalbuphine sebacate and nalbuphine in human after intramuscular injection of dinalbuphine sebacate in an extended‐release formulation},
  author={Yu-En Tien and Wen-Chuan Huang and Hui-Yuan Kuo and Li Ling Tai and Yow Shieng Uang and Wendy H Chern and Jin‐ding Huang},
  journal={Biopharmaceutics \& Drug Disposition},
  year={2017},
  volume={38},
  pages={494–497}
}
Nalbuphine is a semi-synthetic opioid indicated for the relief of moderate to severe pain. Its short half-life requires frequent injections in clinical practice, resulting in a greater incidence of adverse events. A prodrug of nalbuphine has been developed, dinalbuphine sebacate (DNS), dissolved in a simple oil-based injectable formulation, which could deliver and maintain an effective blood level of nalbuphine. An open-label, prospective, two-period study was performed in healthy volunteers to… 

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References

SHOWING 1-10 OF 14 REFERENCES
IN VITRO AND IN VIVO EVALUATION OF THE METABOLISM AND PHARMACOKINETICS OF SEBACOYL DINALBUPHINE
TLDR
SDN fulfilled the original pro-soft drug design in which the prodrug can rapidly metabolize to nalbuphine, and no other unexpected compounds were apparent in the blood.
Evaluation of nalbuphine hydrochloride.
  • R. Miller
  • Medicine, Biology
    American journal of hospital pharmacy
  • 1980
TLDR
On the basis of presently available evidence, nalbuphine appears to have fewer disadvantages than any other parenteral strong analgesic, and the frequency of psychotomimetic reactions apparently is very low.
Simultaneous determination of nalbuphine and its prodrug sebacoly dinalbuphine ester in human plasma by ultra-performance liquid chromatography-tandem mass spectrometry and its application to pharmacokinetic study in humans.
TLDR
The UPLC-MS/MS method was applied successfully to determine nalbuphine concentration in human plasma samples obtained from four Taiwanese volunteers receiving intramuscularly administration of sebacoyl dinal Buphine ester.
A comparison of morphine and nalbuphine for intraoperative and postoperative analgesia.
  • F. Minai, F. Khan
  • Medicine
    JPMA. The Journal of the Pakistan Medical Association
  • 2003
TLDR
Nalbuphine provides better haemodynamic stability and better analgesia, recovery profile and postoperative pain relief compared to morphine in patients undergoing total abdominal hysterectomy.
Evaluation of nalbuphine for abuse potential
TLDR
It is concluded that nalbuphine has an abuse potential which approximates that of pentazocine, but equianalgesic doses of nal Buphine produce less nalorphine‐like effects than does pentazOCine.
Clinical Significance of Esterases in Man
TLDR
The concentration of aspirin relative to salicylate in the circulation may be affected by individual variation in esterase levels and the relative roles of the different esterases, and this may influence the overall pharmacological effect.
Analgesics and ENT surgery. A clinical comparison of the intraoperative, recovery and postoperative effects of buprenorphine, diclofenac, fentanyl, morphine, nalbuphine, pethidine and placebo given intravenously with induction of anaesthesia.
TLDR
Nalbuphine and pethidine are the most efficacious analgesics for routine in-patient ENT surgery and provide sedation with analgesia during recovery, a prolonged time to re-medication and a mild emetic effect.
Possible physiological roles of carboxylic ester hydrolases.
(1987). Possible Physiological Roles of Carboxylic Ester Hydrolases. Drug Metabolism Reviews: Vol. 18, No. 4, pp. 379-439.
Nalbuphine
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