Abstral

Abstral is a formulation of fentanyl citrate available as a sublingual tablet.[1] It dissolves quickly[1] and is absorbed through the sublingual mucosa to provide rapid analgesia. In the UK, Abstral is licensed for the treatment of breakthrough cancer pain (BTcP) in patients with otherwise stable, baseline persistent pain that is managed with conventional opioids.[1]

The active constituent of Abstral is fentanyl, which is classified as a controlled Class A drug under the Misuse of Drugs Act 1971 in the UK.[2]

When used under license, fentanyl is a highly lipophilic compound,[1][3] which is well absorbed sublingually[1] and generally well tolerated.[1] Other pharmaceutical preparations licensed for breakthrough cancer pain in the UK, which contain fentanyl are: Actiq, Effentora, Instanyl and PecFent.[4] Abstral is manufactured and marketed by Galena Biopharma, Inc..

Currently, patients receive conventional oral opioids (e.g. morphine) to treat their breakthrough cancer pain episodes. However, the pharmacokinetic profile of conventional opioids does not fit the profile of breakthrough cancer pain. A breakthrough cancer pain episode is rapid in onset, short in duration and severe in intensity,[5] while an opioid such as morphine is slow in onset and long in duration. This necessitated the development of specialised, fast-acting fentanyl preparations.

Administration

Approximately 100 times more potent than morphine, Abstral is licensed for opioid-tolerant individuals who require relief from a breakthrough cancer pain episode.[1] An Abstral tablet is administered by placing it beneath the tongue, and allowing it to dissolve.[6] Abstral is rapidly absorbed through the oral mucosa over approximately 30 minutes following administration. The bioavailability of Abstral has not been studied but is estimated to be about 70%. Mean maximal plasma concentrations of Abstral range from 0.2 to 1.3 ng/ml (after administration of 100 to 800 µg Abstral) and are reached within 22.5 to 240 minutes.[1]

FDA risk evaluation and mitigation strategies (REMS)

Distributors of Abstral are required to implement an FDA-approved risk evaluation and mitigation strategy (REMS) program.[7][8]

Efficacy

Much like any other pharmaceutical drug, Abstral has been thoroughly tested in clinical trials. These have identified several characteristics:

Recent studies have suggested that Abstral may work less than 10 minutes after administration.

Side effects

Like all medicines, Abstral has a range of associated adverse effects.[1]

Very common side effects (affects more than 1 user in 10) include:

Common side effects (affects 1 to 10 users in 100) include:

References

  1. 1 2 3 4 5 6 7 8 9 10 11 12 Abstral Summary of Product Characteristics. February 2010. http://www.medicines.org.uk/emc/medicine/21371/SPC/Abstral+Sublingual+Tablets/
  2. ↑ http://www.legislation.gov.uk/ukpga/1971/38/schedule/2
  3. ↑ "Abstral (Fentanyl Sublingual Tablets for Breakthrough Cancer Pain)". P T 36 (2): 2–28. February 2011. PMC 3086091. PMID 21560267.
  4. ↑ http://bnf.org/bnf/bnf/current/3530.htm
  5. ↑ http://spcare.bmj.com/content/1/Suppl_1/A24.1.abstract
  6. ↑ http://www.mims.co.uk/Drugs/pain/pain-fever/abstral/
  7. ↑ "RelayHealth's pharmacy connectivity network and reach, aligned with McKesson Specialty Care Solutions' REMS expertise, expands cancer patients' access to pain therapy". Atlanta. 20 January 2011. Retrieved 5 November 2015.
  8. ↑ Shelley, Suzanne (22 April 2011). "With a Few Stumbles, REMS Begins to Hit Its Stride". Pharmaceutical Commerce. Retrieved 5 November 2015.

External links

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