Drugs

Which opioids are hepatically activated or inactivated? Almost all opioids are metabolized in the liver. Some are metabolized to inactive compounds, some to active compounds, and some to both. For example, hydrocodone is metabolized to the more active hydromorphone by cytochrome 2D6 (CYP2D6) and by CYP3A4 to inactive norhydrocodone. Likewise, oxycodone is metabolized to the …

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What is the difference among a pure agonist partial agonist and an agonist? Pure agonists are opioid drugs that bind to mu-opioid receptors in the body. That binding then produces naturally occurring endorphins, analgesia, euphoria, and other well-known opioid properties. Examples of full agonists include morphine, oxycodone, hydrocodone, fentanyl, methadone, and several others. Partial agonists …

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Are poppies the only naturally occurring source for opiates? Historically, poppies have been thought to be the only naturally occurring source of opiates, specifically opium and derived products morphine and codeine. Recently kratom has become a popular designer drug of abuse. Kratom is indigenous to areas of Southeast Asia. Although the US Drug Enforcement Administration …

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Narcotics The word “narcotic” refers to an agent capable of inducing sleep, which includes opioids. Over time the term “narcotic” has become a derogatory term for opioids and other drugs of abuse. Naming police units that deal with illicit drugs “narcotics divisions” and the name of the group “narcotics anonymous” both place negative implications on …

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Is opioid induced constipation readily treatable in the majority of patients using OTC laxatives? In many patients, OIC can be treated with OTC stimulant laxatives, with or without emollient laxatives (stool softeners). OIC is caused when opioid agonists combine with and activate mu-opioid receptors within the gastric mucosa. This results in reduced peristalsis, decreased fluid …

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What is the most common side effect of opioids? The most common side effect of opioids is opioid-induced constipation (OIC). The rate of constipation with chronic use of opioids for noncancer pain may be as high as 90%, and remains an issue even with intermittent regular use. Prevalence is no doubt elevated, because OIC is …

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Role of the atypical antidepressants in the treatment of chronic pain Buprorion, trazadone, and mirtazapine are among the atypical antidepressants that have shown benefit in limited studies to support their use in chronic, primarily neuropathic, pain.