Review Article

Designing Opioids That Deter Abuse

Table 1

A very short modern history of opioid analgesia [19].

YearEvent

1804Morphine isolated from opium (Germany)
1827Morphine commercially available (Merck)
1832Codeine isolated (France)
1857Hypodermic needle invented
1890First USA law regulating narcotics, a tax on opium and morphine. Narcotics can be freely bought and sold
1903Heroin addiction is recognized as a major public health crisis in USA
1905USA bans opium
1914Harrison Narcotics Act requires registration of physicians, pharmacists, and others associated with narcotics prescribing and distribution
1914Oxymorphone synthesized (Germany)
1916Oxycodone synthesized (Germany)
1923First US federal drug agency (US Treasury Department’s Narcotics Division) bans sale of all narcotics in USA
1930Federal Bureau of Narcotics established in the Treasury Department
1939Oxycodone available in USA
1959Oxymorphone available in USA
1960Fentanyl synthesized
1964World Health Organization introduces concept of opioid dependence
1965USA estimates that 750,000 citizens are addicted to heroin
1967Talwin (pentazocine) approved for pain relief and is described as having no known potential for abuse
1968First reports of Talwin dependence
1968Bureau of Narcotics and Dangerous Drugs established in the Justice Department
1970Congress passes Controlled Substances Act
1973Drug Enforcement Administration (DEA) is set up under the Justice Department
1979Schedule IV controlled substance act, labeling changes to include postmarketing events of addiction
1982Talwin is reformulated to include naloxone and marketed commercially the following year
1983The original formulation of Talwin (without naloxone) is withdrawn from market and reports of abuse decreased in next few years
1999Veterans Health Administration launches the “Pain as the 5th Vital Sign” initiative. JCAHO and other regulatory bodies incorporate into their guidelines, which was initial start of increased opioid prescriptions
2000Congress declares decade 2001–2010 “Decade of Pain Control and Research”
2002Suboxone (buprenorphine/naloxone) approved
2004Consumer lawsuit against Purdue Pharma regarding OxyContin
2004First “around-the-clock” product approved for opioid-tolerant pain patients (Palladone, Purdue Pharma)
2005Palladone pulled from the USA market (still available in UK)
2005Majority of single-agent oxycodone sold in US is extended release (64%)
2007Reports of Suboxone abuse nationally as abusers figured out how to extract buprenorphine
2007USA consumes 82% of world’s supply of oxycodone annually
2009Embeda (morphine with sequestered naltrexone) approved
2009Majority of single-agent oxycodone sold in US is immediate release (54%)
2010Safe use Initiative launched by FDA