Hospice, Cancer Pain Management, and Symptom Control
Mark V. Boswell, B. Eliot Cole in Weiner's Pain Management, 2005
Whether or not patients experience significant toxicity with morphine therapy, there may be times to consider changing to a semisynthetic opioid. Many of these are currently available (or soon to become available) as controlled-release preparations. Hydromorphone is frequently selected, as the duration of analgesic action and plasma half-life are the same as morphine (Pasero et al., 1999). Perhaps relatively less nauseating and CNS “toxic” than morphine, hydromorphone is available in immediate-release oral tablets (controlled-release tablets are available outside the United States and are in clinical trials in the United States), oral solutions, suppositories, and an injectable solution (10 mg/ml). The parenteral form can be quite useful for end-stage cancer pain management, especially when higher doses may be needed (Miller et al., 1999). Hydromorphone’s metabolites (primarily hydromor-phone-3-glucuronide) are not thought to be pharmacologically active, although myoclonus and mental status changes have been reported with high doses of hydromor-phone, potentially making it particularly useful for patients with renal failure after dosage reduction and careful titration (Kuczynska, 2004; Kurella et al., 2003).
Pain and Its Management in Older Adults
K. Rao Poduri in Geriatric Rehabilitation, 2017
As a rule, the basal infusion should not exceed 20%–30% of the total available hourly dose. The most common opioid used is morphine followed by hydromorphone and fentanyl. The usual dose for morphine is a loading dose of 0.1–0.3 mg/kg in divided doses. One-tenth of the total loading dose can be used as a bolus every 10–15 minutes on an as-needed basis. For example, if a patient needed 10 mg of morphine to be comfortable, the prn bolus should be set at 1 mg every 10–15 minutes. Dosing for hydromorphone or fentanyl can be extrapolated using equianalgesic charts. Intravenous PCA is a safe and effective modality for use in cognitively intact older adults albeit they are able to understand and participate in their care, hence appropriate selection is very important.23
Treating Pain
Ronald Schleifer in Pain and Suffering, 2014
Unlike anesthetics, analgesics are drugs that relieve pain without affecting consciousness or sensory perception. There are two types of analgesic drugs: anti-inflammatory drugs that alleviate pain by reducing local inflammation; and the opioids, which act on the brain and the central nervous system. Anti-inflammatory drugs are used for short-term pain relief for such conditions as headaches, muscle strain, arthritis. Opioid analgesics are used for relief of severe pain (both short term and long term). The most widely known anti-inflammatory is aspirin—a trade name for acetylsalicylic acid—that is a derivative of salicylic acid. Aspirin was marketed by Friedrich Bayer and Company in the 1890s—it was the first “block buster” pharmaceutical that commanded worldwide sales. Although aspirin has been remarkably effective, it was not until recently that the physiological basis of its effects were discovered: aspirin acts by inhibiting the production of prostaglandins, body chemicals that are necessary for blood clotting and are noted for sensitizing nerve endings to pain. Around 1960 the FDA approved a new anti-inflammatory, acetaminophen, marketed under the brand name Tylenol. Unlike aspirin, Tylenol does not create irritation of the stomach and gastrointestinal tract. Still, the most common cause of acute liver failure in the west is toxicity from acetaminophen, and the vast majority of people suffering from this condition in the United States are women (Thernstrom 2010: 147; see also Fishman 2000: 41).
Designing safer analgesics: a focus on μ-opioid receptor pathways
Published in Expert Opinion on Drug Discovery, 2018
Joseph V. Pergolizzi, Jo Ann LeQuang, Robert Taylor, Michael H. Ossipov, Daniel Colucci, Robert B. Raffa
Typical opioids act as agonists at the µ-opioid receptors and sometimes have activity at δ- and κ- opioid receptors. Newer centrally acting drugs introduced to market or in development activate MOR, but exhibit characteristics atypical of conventional opioids. To date, four such analgesics have been developed (in alphabetical order): buprenorphine, cebranopadol, tapentadol, and tramadol. These agents rely on unique and synergistic mechanisms of action. Thus, they do not work like conventional opioids, yet they are often simply categorized as ‘opioids.’ Such categorization is partly true, of course, since they do have opioid effects, but it is misleading to consider them as typical opioids in that they possess many different attributes. These four drugs are sometimes rightly termed ‘atypical opioids,’ because while they possess properties typical of opioids, they are also different from conventional opioids in clinically important ways.
Current and emerging pharmacotherapies for opioid dependence treatments in adults: a comprehensive update
Published in Expert Opinion on Pharmacotherapy, 2022
Jonna M. Leyrer-Jackson, Amanda M. Acuña, M. Foster Olive
Opium is a naturally occurring substance derived from the opium poppy Papaver somniferum, and contains various bioactive opioid alkaloids, such as morphine, codeine, thebaine, papaverine, and others. Recorded history of use of opium for relief of pain and a variety of other medical ailments date back more than six millennia. In the latter half of the 19th century, chemical isolation of morphine from opium, the discovery of its conversion to diacetylmorphine (heroin) by boiling in acetic anhydride, and the invention of the hypodermic syringe, collectively led to widespread intravenous opioid use which revealed the high abuse dependence of these otherwise therapeutic compounds [1]. Over the next century, a multitude of synthetic and semisynthetic opioids were developed for use in the treatment of chronic pain, cough, and diarrhea, the most commonly prescribed being hydrocodone, hydromorphone, oxycodone, oxymorphone, fentanyl, tramadol, and meperidine.
Research progress of p38 as a new therapeutic target against morphine tolerance and the current status of therapy of morphine tolerance
Published in Journal of Drug Targeting, 2023
Xiao Fu, Yanhong Zhang
As a powerful opioid analgesic, morphine is widely used in intraoperative anaesthesia, postoperative analgesia, severe pain treatment and the third step pain relief of malignant tumours. Between 2004 (25,644 S-DDD (defined daily doses for statistical purposes) and 2019, (27,957 S-DDD), the global trend in morphine usage stayed relatively consistent, but grew to 31,824 S-DDD in 2020, the greatest consumption in over a decade. In 2020, 35.3 tons (11.4%, up from 9.4% in 2019) of morphine were used directly, primarily for palliative care [1]. Morphine tolerance is becoming increasingly common as a result of long-term and extensive usage, resulting in poor effectiveness, hyperalgesia, and even adverse effects such as low mood, nausea or vomiting, respiratory suppression, and so on [2]. Morphine tolerance is the main reason for the weakening of pain control and the increase of dose [3,4]. Seriously affect the safety and comfort of patients.
Related Knowledge Centers
- Anesthesia
- Carfentanil
- Drug Withdrawal
- Morphine
- Pain Management
- Diarrhea
- Euphoria
- Opioid Receptor
- Opioid Use Disorder
- Opioid Overdose