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Randomized Controlled Trial
. 2021 Feb 1;132(2):456-464.
doi: 10.1213/ANE.0000000000005108.

Pharmacokinetics and Pharmacodynamics of 3 Doses of Oral-Mucosal Dexmedetomidine Gel for Sedative Premedication in Women Undergoing Modified Radical Mastectomy for Breast Cancer

Sahar Abdel-Baky Mohamed  1 , Hala Saad Abdel-Ghaffar  2 , Nivin Abdel-Azim Hassan  3 , Fatma Adel El Sherif  1 , Samia Abdelsamie Shouman  4 , Mervat Mostafa Omran  4 , Sahar Badr Hassan  5 , Ayat Ahmed Abd El-Monsef Allam  5 , Doaa Gomaa Sayed  1
Affiliations
Randomized Controlled Trial

Pharmacokinetics and Pharmacodynamics of 3 Doses of Oral-Mucosal Dexmedetomidine Gel for Sedative Premedication in Women Undergoing Modified Radical Mastectomy for Breast Cancer

Sahar Abdel-Baky Mohamed et al. Anesth Analg. .

Abstract

Background: Buccal dexmedetomidine (DEX) produces adequate preoperative sedation and anxiolysis when used as a premedication. Formulating the drug as a gel decreases oral losses and improves the absorption of buccal DEX. We compared pharmacokinetic and pharmacodynamic properties of 3 doses of buccal DEX gel formulated in our pharmaceutical laboratory for sedative premedication in women undergoing modified radical mastectomy for breast cancer.

Methods: Thirty-six patients enrolled in 3 groups (n = 12) to receive buccal DEX gel 30 minutes before surgery at 0.5 µg/kg (DEX 0.5 group), 0.75 µg/kg (DEX 0.75 group), or 1 µg/kg (DEX 1 group). Assessments included plasma concentrations of DEX, and pharmacokinetic variables calculated with noncompartmental methods, sedative, hemodynamic and analgesic effects, and adverse effects.

Results: The median time to reach peak serum concentration of DEX (Tmax) was significantly shorter in patients who received 1 µg/kg (60 minutes) compared with those who received 0.5 µg/kg (120 minutes; P = .003) and 0.75 µg/kg (120 minutes; P = .004). The median (first quartile-third quartile) peak concentration of DEX (maximum plasma concentration [Cmax]) in plasma was 0.35 ng/mL (0.31-0.49), 0.37 ng/mL (0.34-0.40), and 0.54 ng/mL (0.45-0.61) in DEX 0.5, DEX 0.75, and DEX 1 groups (P = .082). The 3 doses did not produce preoperative sedation. The 1 µg/kg buccal DEX gel produced early postoperative sedation and lower intraoperative and postoperative heart rate values. Postoperative analgesia was evident in the 3 doses in a dose-dependent manner with no adverse effects.

Conclusions: Provided that it is administered 60-120 minutes before surgery, sublingual administration of DEX formulated as an oral-mucosal gel may provide a safe and practical means of sedative premedication in adults.

Trial registration: ClinicalTrials.gov NCT03120247.

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Conflict of interest statement

The authors declare no conflicts of interest.

Comment in

  • Pharmacokinetics Police.
    Fisher DM, Shafer SL. Fisher DM, et al. Anesth Analg. 2022 Feb 1;134(2):e7-e8. doi: 10.1213/ANE.0000000000005813. Anesth Analg. 2022. PMID: 35030129 No abstract available.
  • In Response.
    Mohamed SA, Abdel-Ghaffar HS, Hassan NA, El Sherif FA, Shouman SA, Omran MM, Hassan SB, Allam AAAE. Mohamed SA, et al. Anesth Analg. 2022 Feb 1;134(2):e9-e11. doi: 10.1213/ANE.0000000000005815. Anesth Analg. 2022. PMID: 35030131 No abstract available.

References

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    1. Chandra A, Ranjan R, Kumar J, Vohra A, Thakur VK. The effects of intravenous dexmedetomidine premedication on intraocular pressure and pressor response to laryngoscopy and intubation. J Anaesthesiol Clin Pharmacol. 2016;32:198–202.
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    1. Fan W, Xue H, Sun Y, et al. Dexmedetomidine improves postoperative patient-controlled analgesia following radical mastectomy. Front Pharmacol. 2017;8:250.

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