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Review
. 2012 Jun 1;26(6):509-35.
doi: 10.2165/11630580-000000000-00000.

A comprehensive review of rapid-onset opioids for breakthrough pain

Howard Smith  1
Affiliations
Review

A comprehensive review of rapid-onset opioids for breakthrough pain

Howard Smith. CNS Drugs. .

Abstract

Breakthrough pain (BTP) is a transitory pain (reaching maximum severity in ~15 minutes and lasting ~60 minutes in patients with cancer) that occurs despite the management of chronic pain with long-term around-the-clock analgesia. BTP occurs in 33-65% of patients with chronic cancer pain and in ~70% of patients with chronic noncancer pain. BTP has historically been managed with short-acting opioids; however, these medications have a pharmacokinetic profile that does not correlate with the sudden onset and short time to maximum severity of BTP. Interest in rapid-onset opioids to relieve BTP has therefore been growing. This comprehensive review aims to summarize the currently available clinical data for the approved rapid-onset opioids, which comprise different formulations of fentanyl, a μ-opioid receptor agonist with anaesthetic and analgesic properties. Administration routes for fentanyl in the management of BTP currently include the transmucosal and intranasal routes; an intrapulmonary formulation is also in development. The findings of this review suggest that the efficacy and safety of the approved rapid-onset opioids are comparable.

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Figures

Fig. 1
Fig. 1
Categorization of breakthrough pain (BTP).
Fig. 2
Fig. 2
Timeline of rapid-onset opioid approval in the US and EU. = European Medicines Agency; FBSF = fentanyl buccal soluble film; FBT = fentanyl buccal tablet; FPNS = fentanyl pectin nasal spray; INFS = intranasal fentanyl spray; OTFC = oral transmucosal fentanyl citrate; SLF = sublingual fentanyl.
Table I
Table I
Studies included in this review
Table II
Table II
Characteristics of the various administration routes used for opioid medications with a particular focus on breakthrough pain[2,34]
Table III
Table III
Summary pharmacokinetic dataa for fentanyl formulations
Table IV
Table IV
Clinically meaningful improvements with fentanyl vs comparators (placebo or other opioids)
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