Constipation oxycodone

Derived from the alkaloid thebaine, oxycodone is a highly effective pain-reliever and prescribed to postsurgical patients, cancer patients, and others with severe pain. Oxycodone is sold under various trade names in combination with aspirin, including Per-codan , Endodan, and Roxipirin with acetaminophen it is marketed as Percocet , Endocet, and Roxicet. Oxycodone is also the main ingredient in OxyContin. The most frequent side effect of oxycodone is constipation, but naseua is also common. Oxycodone is highly abused in the United States. 

Evidence suggests that oxycodone has the ability to lock onto a special cell receptor found primarily in the brain, spinal cord, and intestines. When the drug connects to the receptors in the spinal cord, it causes the nerves that are sending pain signals to be temporarily blocked. Similarly, when the drug connects to the receptors in the brain, it causes an overall sense of well-being and relaxation. However, when the drug connects to the receptors in the intestines, the result is often constipation. 

Oxycodone s effects on the central nervous system produce pain relief, euphoria, and slowed breathing. It also decreases the activity of the intestinal tract, often leading to constipation. To combat this, patients are advised to drink six to eight full glasses of water per day and increase the amount of dietary fiber they eat. 

In a randomized, double-bUnd, crossover study, previous findings on the adverse effects of oxycodone among sufferers of postherpetic neuralgia were confirmed (4). Oxycodone was analgesic in this group, although 76% of the sample reported adverse effects compared with 49% of the placebo group. Constipation, nausea, and sedation were the most frequently reported adverse effects. 

Oxycodone Metabolized to oxymorphone 3-4h Less nausea/constipation than codeine Rapid CNS dysphoria or euphoria... 

Codeine is an analgesic that is effective in the treatment of mild to moderate pain. It is often combined with other analgesic products and enjoys a popularity that makes it the standard for other oral opioids. Unfortunately, codeine has the same propensity to produce tolerance, dependence, and constipation as morphine. Hydrocodone, a derivative of codeine, also is seen most often in combination products and has pharmacologic properties similar to those of morphine. Oxycodone has a similar potency to morphine and is an excellent oral analgesic for moderate to severe pain. This is especially trne when the product is used in combination with nonopioids however, its predilection for causing tolerance and dependence, along with its basic opioid characteristics, likens it to morphine. It shonld be noted that sustained-release oxycodone is also available. 

Methadone is frequently used to treat heroin, codeine, hydrocodone, oxycodone, and morphine addictions. Methadone when used as prescribed, is safe and effective and does not cause euphoric sensations but does relieve physical withdrawal symptoms and reduces physiologic cravings. Methadone does have side effects which may be intolerable to some patients. They include constipation, water retention, drowsiness, skin rash, excessive sweating, and change in sex drive. Methadone has been used successfully in the treatment of opioid addiction for over 30 years. 

Administration of opioids for chronic arthritic pain in elderly people is effective but can be associated with problematic adverse reactions, particularly morphine and related compounds in those with chronic renal insufficiency [53 ]. There is a higher frequency of nausea, constipation, and cognitive impairment. Pethidine, dextro-propoxyphene, and pentazocine should also be avoided because they have toxic metabolites. Preferred alternatives are hydro-morphone, oxycodone, and oxymorphone. 

Comparative studies Tapentadol, a centrally acting p opioid receptor agonist and a noradrenaline reuptake inhibitor, has been compared with oxycodone in the management of moderate to severe chronic osteoarthritis in 1030 patients who were randomized to tapentadol ER 100-250 mg bd, oxycodone CR 20-50 mg bd, or placebo [181. Tapentadol ER was associated with less nausea and vomiting (23% versus 41%) and constipation (19% versus 37%) than oxycodone CR. Dropouts were also more conunon with oxycodone CR (43% versus 19%), mainly because of gastrointestinal effects. Tapentadol ER was better tolerated than oxycodone CR. 

Gastrointestinal constipation and nausea are common. Nausea may be treated with antiemetics, and frequently improves with ongoing therapy. Virtually all patients taking opioids become constipated and do not become tolerant to this side effect. Activation of mu receptors in the gastrointestinal tract slows peristalsis, which promotes further absorption of water and electrolytes in the colon. Patients should be treated prophylactically with stool softeners and/ or laxatives. There is an oral oxycodone/naloxone prolonged-release tablet in clinical trials to counteract opioid-induced constipation, which is often debilitating. 

Better gastrointestinal tolerability than oxycodone CR, specifically, less nausea and vomiting and constipation in the osteoarthritis and CLBP efficacy trials and 1-year safety trial [6,8,10]. 

Observational studies In patients with moderate to severe cancer pain taking OxyContin (controlled-release oxycodone hydrochloride), adverse reactions occurred in 25% in the first week and the incidence gradually fell with time, to 12% in the 8th week [132 ]. The most common adverse effects reported in the first week were constipation (26%), nausea (13%), vomiting (6.2%), dizziness (5%), and lethargy (3.7%). Other effects included dysuria, fatigue, headache, pruritus, and thirst. There was a similar pattern at 8 weeks. Five patients had delusions after dosage reduction or withdrawal, and another had delirium on days 2 and 3. The authors suggested that the adverse effects of OxyContin could be reduced with preventive medication. 

Gastroiutestiual In a randomized study, 87 patients with pain due to herpes zoster infection taking famciclovir were allocated to controlled-release oxycodone, gabapentin, or placebo eight patients withdrew, in four cases because of constipation, and of the others, 15 also had constipation [138, 139. ... 

Naloxone The combination of rectal oxycodone 40, 60, or 80 mg/day and rectal naloxone 10, 20, or 40 mg/day has been studied in a randomized, placebo-con-trolled 202 patients with chronic pain [142 ]. The addition of naloxone reduced opioid-induced constipation. 

Meissner W, Leyendecker P, Mueller-Lissner S, Nadstawek J, Hopp M, Ruckes C, Wirz S, Fleischer W, Reimer K. A randomised controlled trial with prolonged-release oral oxycodone and naloxone to prevent and reverse opioid-induced constipation. Eur J Pain 2009 13(1) 56-64. 

The combination oxycodone/naloxone is an opioid analgesic which may also be used for severe pain in CKD patients. Oxycodone is responsible for the pain-relieving effects, while naloxone reduces opioid-induced constipation. 

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