Opiate
[4] Most opiates are considered drugs with moderate to high abuse potential and are listed on various "Substance-Control Schedules" under the Uniform Controlled Substances Act of the United States of America.
Papaverine, noscapine, and approximately 24 other alkaloids are also present in opium but have little to no effect on the human central nervous system.
Very small quantities of hydrocodone and hydromorphone are detected in assays of opium on rare occasions; it appears to be produced by the plant under circumstances and by processes that are not understood at this time.
[citation needed] Dihydrocodeine, oxymorphol, oxycodone, oxymorphone, metopon Possibly other derivatives of morphine and/or hydromorphone also are found in trace amounts in opium.
A significant population are rapid, or ultra-rapid metabolizers and can quickly develop fatal toxicity from even the small amount present in breast milk or from a few doses.
Once scaled for commercial use, the process would cut production time from a year to several days and could reduce costs by 90%.
Conversely, individuals with rapid or ultra-rapid CYP2D6 activity may metabolize the drug too quickly and experience dose-related side effects such as sedation and fatal respiratory depression.
[14] Heroin, the common name for diacetylmorphine, is the first of several semi-synthetic opioids to be derived from morphine, a component of natural opium.
Normeperidine may accumulate to toxic levels in patients with renal impairment with repeated doses, and can cause CNS excitation and seizures.
[21] In addition, there is an increase risk of mortality in patients who are treated with methadone compared to other opioids, thought to be due to QTc prolongation and cardiac arrhythmias.
M6G has potent analgesic activity, binds to opioid receptors, and is a main contributor to the therapeutic benefit of morphine.
[25] Another indication is symptomatic relief of shortage of breath, both in the acute setting (for example, pulmonary edema) and in terminally ill patients.
Given the abuse potential, the frequent GI side effects, and several studies showing no discernable benefit, recommendations are against use of opioids for cough in children.
Generally, parenteral (IV or IM) morphine is used as the standard for converting between opiates to achieve equivalent analgesic effects.
[28] Calculating total daily dose using morphine milligram equivalents is used to identify patients at risk of overdose.
[29] Common side effects associated with opioid use include: sedation, nausea, dizziness, vomiting, constipation, physical dependence, tolerance, and potentially fatal respiratory depression.
Less common side effects include: delayed gastric emptying, hyperalgesia, immunologic and hormonal dysfunction (hypogonadism is often seen in men taking chronic opioids, but is not always clinically evident), muscle rigidity, and myoclonus.
However, long-term treatment for chronic pain is controversial as there is a high risk of addiction associated with its use leading to abuse and diversion to others even when taken properly.
[33] Those addicted to opiates will prioritize acquiring these drugs over other activities in their lives, negatively impacting their professional and personal relationships.
Concentration-dependence adverse effects may vary based on the user's genetic polymorphisms which can alter drug metabolism.
Other clinically important roles of mu are its involvement in respiratory and cardiovascular functions, gastrointestinal peristalsis, feeding, and mood.
[38] These other pathways are important because they explain the side effects of opiate use like respiratory depression at high doses, constipation with chronic use, and addicting properties.
