Opioid

Understanding Opioids: A Class of Drugs with a Complex History

Opioids are a class of drugs derived from or mimicking natural substances found in the opium poppy plant. They work on opioid receptors to produce morphine-like effects, primarily for pain relief and anesthesia. But their journey through history is as complex as their molecular structure, with both life-saving benefits and dangerous pitfalls.

The Evolution of Opioids

Have you ever wondered about the origins of opioids? The earliest known evidence of Papaver somniferum dates back to the Neolithic period around 5,700–5,500 BCE. Use of opium poppy can be traced to the fourth century BC in Sumerian clay tablets and was valued by Hippocrates (460-370 BC) for its sleep-inducing properties.

From ancient times to modern pharmaceuticals, opioids have played a significant role in medicine. The term ‘opioid’ was first used in the 1950s, combining ‘opium’ and ‘-oid’. Research found that opiate effects are mediated by activation of specific molecular receptors in the nervous system, which were termed ‘opioid receptors.’

Medical Uses and Misuses

Medically, opioids are used for pain relief, suppression of diarrhea, replacement therapy for opioid use disorder, and suppressing cough. However, they can also be used recreationally for their euphoric effects or to prevent withdrawal.

The global number of people using opioids illicitly has increased, attributed to over-prescription of opioid medications and inexpensive illicit heroin. As an American legal term, narcotic refers to cocaine and opioids, and their source materials, with pejorative connotations. The term can also be loosely applied to any illegal or controlled psychoactive drug.

Types of Opioids

Narcotics are used to treat various types of pain, including acute pain, chronic cancer pain, and chronic non-cancer pain. They are also used for cough suppression, diarrhea relief, and other conditions like shortness of breath and severe restless legs syndrome.

Side Effects and Risks

The side effects of opioids include itchiness, sedation, nausea, respiratory depression, constipation, and euphoria. Long-term use can lead to tolerance, physical dependence, and addiction. An overdose or concurrent use with other depressant drugs like benzodiazepines can result in death from respiratory depression.

Opioids act by binding to opioid receptors, which mediate both psychoactive and somatic effects. They are addictive and controlled substances due to their potential for fatal overdose. The global number of people using opioids illicitly has increased, attributed to over-prescription of opioid medications and inexpensive illicit heroin.

Legal and Social Implications

The U.S. Food and Drug Administration launched an education campaign ‘Remove the Risk’ to help Americans understand the importance of removing and properly disposing of unused prescription opioids from their homes. The target group is women aged 35-64 who oversee household health care decisions.

Pharmacology and Development

The individual molecular structure also affects the duration of action, with unique binding affinities to various classes of opioid receptors (μ, κ, and δ), allowing for a wide class of opioids with different effect profiles due to their unique molecular structure.

A new strategy in drug development aims to increase the activation of desirable signaling pathways while reducing the impact on undesirable pathways through functional selectivity or biased agonism. Oliceridine is an example of a biased agonist that displays analgesic activity with reduced adverse effects.

Historical Context and Modern Challenges

The earliest known evidence of Papaver somniferum dates back to the Neolithic period around 5,700–5,500 BCE. Use of opium poppy can be traced to the fourth century BC in Sumerian clay tablets and was valued by Hippocrates (460-370 BC) for its sleep-inducing properties.

The term ‘opioid’ was first used in the 1950s, combining ‘opium’ and ‘-oid’. Research found that opiate effects are mediated by activation of specific molecular receptors in the nervous system, which were termed ‘opioid receptors.’

Conclusion

The journey of opioids from ancient remedies to modern pharmaceuticals is a tale of both healing and harm. Understanding their complex nature, side effects, and risks can help us navigate this challenging landscape more effectively.