Opioids side effects

Tramadol a weak opioid that also blocks the reuptake of NA and 5-HT—these combined actions synergise to give a good analgesia that lacks some of the typical opioid side-effects. 

Managing Opioid Side Effects and Drug Interactions... 

Tramadol is an opioid analgesic, which acts by exerting an opioid effect and through the stimulation of adrenergic and serotonin pathways. Compared with the other opioids, tramadol is less likely to cause the typical opioid side-effects, such as respiratory depression, and constipation. It is also less likely to cause addiction. 

Bates JJ, Foss JF, Murphy DB. Are peripheral opioid antagonists the solution to opioid side effects Anesth Anaig 2004 98 116-22. 

The intestinal inhibitory action of opioids can be used for treatment of diarrhea (De Luca and Coupar, 1996). The clinically most important anti-diarrheal opioid is loperamide (Heel et al., 1978). After oral administration, loperamide acts locally within the gastro-intestinal tract. After parenteral administration, the compound is rapidly inactivated and does not reach the CNS. Therefore loperamide does not show the typical central opioid side-effects, has no analgesic action and has no abuse potential. 

Side-effects Typical side-effects of tramadol are nausea, sweating and dizziness. In rare cases seizures after high i.v. doses are reported, mostly in combination with other proconvulsant componds or in patients with reduced seizure theshold (Gardner et al., 2000). Tramadol shows a reduced level of opioid side-effects, especially respiratory depression and constipation are less frequent and severe than with standard opioids such as morphine. Tramadol has a very limited abuse potential and is not subject to narcotic control (Cossmann et al., 1997). 

Agents used as adjuncts or adjunctive therapies to opioid analgesics in total management of moderate-to-severe pain. They can directly diminish pain, counteract opioid side effects, or help manage concurrent psychiatric symptoms. 

Within the last 10, years several new compounds were launched in the field of non-steroidal antiinflammatory drugs (NSAIDs) with a clear focus on cyclooxygenase type 2 selective compounds. In the field of opioids on the other hand no new drugs have passed phase III clinical trials. In this field innovation has been achieved through new pharmaceutical formulations of known drugs such as transdermal systems, e.g. buprenorphine patch, transmucosal systems, e.g. fentanyl lollipop, or rectal delivery systems containing e.g. morphine. These were developed in order to reduce opioid side effects, but also to overcome pharmacokinetical limitations, in particular to prolong compliance and duration of action. 

McNicol E, Horowicz-Mehler N, Fisk RA, et al. Management of opioid side effects in cancer-related and chronic noncancer pain a systematic review. J Pain. 2003 4 231-256. 

Cepeda MS, Alvarez H, Morales O, Carr DB. Addition of ultralow dose naloxone to postoperative morphine PCA unchanged analgesia and opioid requirement but decreased incidence of opioid side effects. Pain. 2004 107 41-46. 

If additional analgesia is required beyond that afforded by the nonnarcotic analgesics, an opioid such as oxycodone, hydrocodone, or codeine should be used. If opioid side effects are unacceptable or become problematic, the narcotic dose is reduced or an alternative opioid is selected. 

The pure opioid antagonist naloxone binds competitively to opioid receptors but does not produce an analgesic or opioid side-effect response. Therefore, it is used most often to reverse the toxic effects of agonist- and agonist-antagonist-derived opioids. 

Oxycodone compounds that are combined with aspirin, acetaminophen, or ibuprofen are limited in dose by the amount of the non-opioid component. These combination products provide enhanced analgesic effect with fewer opioid side effects, and possibly better compliance because the patient does not need two separate medications. Use of oxycodone alone may be advantageous in those patients who are at risk for toxicity from NSAIDs or acetaminophen. The maximum daily dose of acetaminophen is 4000 mg in a person with no liver impairment. 

The most common adverse events seen with fentanyl buccal tablets and fentanyl lozenges are typical of opioid side effects. The most serious adverse reactions with all opiods include respiratory depression, circulatory depression, hypotension, and shock. Other common opioid side effects include nausea, vomiting, fatigue, dizziness, drowsiness, constipation, and headache. Dental caries has been reported with the use of fentanyl oralet. A minor adverse event with fentanyl buccal tablets is mouth ulcer. 

Opioid side effects may occur with intrathecal morphine just as with any opioid administration. 

Pruritus is the most common opioid side effect of intrathecal morphine. It may occur even with small doses and can be effectively treated with either intermittent intravenous nalbuphine or an infusion of low-dose intravenous naloxone. Pruritus due to intrathecal morphine does not respond well to diphenhydramine. 

CR845 offers the potential advantage of opioid-like analgesia in the absence of classical opioid side effects. Due to CR845 s lack of central nervous system activity... 

Ruiz G, Orts A, Monsalve J, Aliste P, Ross A, Monsalve B. Downbeat nystagmus related with epidural opioid side effect. Acute Pain 2008 10(2) 93-5. 

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