Opioids (2)

Prescription Opioid

As a treatment: Prescription opioids can be used to treat moderate-to-severe pain and are often prescribed following surgery or injury, or for health conditions such as cancer.

In recent years, there has been a dramatic increase in the acceptance and use of prescription opioids for the treatment of chronic, non-cancer pain, such as back pain or osteoarthritis, despite serious risks and the lack of evidence about their long-term effectiveness.

Image result for Prescription opioid volume peaked in 2011 at 240 billion milligrams of morphine equivalents and have declined by 29% to 171 billion
Source: IQVIA

Prescription opioid usage in the United States increased considerably from the mid 1990’s to its peak in 2011, at 240 billion MMEs (morphine milligram equivalents). It is now declining rapidly with the largest single year change in 2017 with a decline of 23.3 billion MMEs or 12.0%.

The most common drugs involved in prescription opioid overdose deaths include:

    • Methadone
    • Oxycodone (such as OxyContin®)
    • Hydrocodone (such as Vicodin®)

Abuse Deterrent

What is an Abuse Deterrent Opioid: with abuse-deterrent formulation properties that are expected to meaningfully deter certain types of abuse and/or make abuse more difficult or less rewarding.

As a general framework, abuse-deterrent formulations can currently be categorized as follows:

  1. Physical/chemical barriers – Physical barriers can prevent chewing, crushing, cutting, grating, or grinding of the dosage form. Chemical barriers, such as gelling agents, can resist extraction of the opioid using common solvents like water, simulated biological media, alcohol, or other organic solvents. Physical and chemical barriers can limit drug release following mechanical manipulation, or change the physical form of a drug, rendering it less amenable to abuse.
  2. Agonist/antagonist combinations – An opioid antagonist can be added to interfere with, reduce, or defeat the euphoria associated with abuse. The antagonist can be sequestered and released only upon manipulation of the product. For example, a drug product can be formulated such that the substance that acts as an antagonist is not clinically active when the product is swallowed, but becomes active if the product is crushed and injected or snorted.
  3. Aversion – Substances can be added to the product to produce an unpleasant effect if the dosage form is manipulated or is used at a higher dosage than directed. For example, the formulation can include a substance irritating to the nasal mucosa if ground and snorted.
  4. Delivery System (including use of depot injectable formulations and implants) – Certain drug release designs or the method of drug delivery can offer resistance to abuse. For example, sustained-release depot injectable formulation or a subcutaneous implant may be difficult to manipulate.
  5. New molecular entities and prodrugs– The properties of a new molecular entity (NME) or prodrug could include the need for enzymatic activation, different receptor binding profiles, slower penetration into the central nervous system, or other novel effects. Prodrugs with abuse-deterrent properties could provide a chemical barrier to the in vitro conversion to the parent opioid, which may deter the abuse of the parent opioid. New molecular entities and prodrugs are subject to evaluation of abuse potential for purposes of the Controlled Substances Act (CSA).
  6. Combination – Two or more of the above methods could be combined to deter abuse.
  7. Novel approaches – This category encompasses novel approaches or technologies that are not captured in the previous categories.

Opioids with FDA-Approved Labeling Describing Abuse-Deterrent Properties

FDA has approved these opioids with labeling describing abuse-deterrent properties consistent with the FDA’s Guidance for Industry: Abuse-Deterrent Opioids – Evaluation and Labeling:

There are currently NO generic opioids with FDA-approved abuse-deterrent labeling.