Naltrexone nausea

Administration of naltrexone may result in anxiety, dif-ficully sleeping, abdominal cramps, nasal congestion, joint and muscle pain, nausea, vomiting, dizziness, irritability, depression, fatigue, and drowsiness. 

The therapeutic dose of acamprosate is 666 mg orally three times daily, and it is supplied as a 333 mg tablet. It can be started at the full dose in most patients without titration. It differs from disulfiram and naltrexone in that it is excreted by the kidneys without liver metabolism. Consequently, it is contraindicated in patients with severe renal impairment (creatinine clearance less than or equal to 30 mL/minute), and dose reduction is necessary when the creatinine clearance is between 30 and 50 mL/minute. The most common side effects are gastrointestinal and include nausea and diarrhea. Rates of suicidal thoughts were also increased in patients treated for 1 year with acamprosate (2.4%) versus placebo (0.8%). If necessary the total daily dose maybe decreased by 1 to 3 tablets (333-999 mg) per day to alleviate side effects. 

Naltrexone is hepatotoxic and contraindicated in patients with hepatitis or liver failure. LFTs should be monitored monthly for the first 3 months, then every 3 months. Side effects include nausea, headache, dizziness, nervousness, insomnia, and somnolence. 

Potential side effects of naltrexone include anxiety, drowsiness, and nausea. In addition, it rarely causes a chemical hepatitis. For this reason, blood testing of liver enzymes should be conducted periodically. If any signs of naltrexone-induced hepatitis appear, it should be discontinued. Furthermore, patients should be advised that they must be totally abstinent from opiates for at least 2 weeks before using naltrexone or it can precipitate severe withdrawal symptoms. 

Naltrexone can induce hepatotoxicity at doses only five times the therapeutic dose and should be used with care in patients with poor hepatic function or liver damage. Side effects of the use of naltrexone are more frequently observed than following naloxone administration. Such side effects include headache, difficulty sleeping, lethargy, increased blood pressure, nausea, sneezing, delayed ejaculation, blurred vision, and increased appetite. 

An excellent brief article on buprenorphine treatment has been provided by Taikato et al. (2005), which notes the common possible side-effects (headaches, nausea and vomiting, sweating, constipation, etc.) and drug interactions. The limited central depressant effect of buprenorphine may be compounded by alcohol and antidepressants, while the metabolism of buprenorphine can be enhanced by anticonvulsants, with therefore possibly reduced efficacy. There have been some case reports of liver toxicity from buprenorphine that is reversible if the medication is stopped (Herve et al. 2004), and often clinical guidelines will recommend that liver function tests are included in buprenorphine treatment, as they definitely should be with naltrexone. 

In 1951, disulfiram was the first medication approved by the U.S. Food and Drug Administration (FDA) for the treatment of alcohol dependence other than detoxification. Disulfiram inhibits a key enzyme, aldehyde dehydrogenase, involved in breakdown of ethyl alcohol. After drinking, the alcohol-disulfiram reaction produces excess blood levels of acetaldehyde, which is toxic in that it produces facial flushing, tachycardia, hypotension, nausea and vomiting, and physical discomfort. Opioid receptors antagonists, such as naloxone and naltrexone (see Chapter 47) that block opioid receptors have been found to decrease alcohol consumption (Cornish et al 2004). 

In an open, single-blind, randomized study, naltrexone (50 mg/day) and acamprosate (1665-1998 mg/day) were used for 1 year by 157 recently detoxified alcohol-dependent men with moderate dependence (4). The time to first relapse was 63 days (naltrexone) and 42 days (acamprosate) after 1 year, 41% of those given naltrexone and 17% of those given acamprosate had not relapsed. Adverse effects were more common with naltrexone and were worse during the first 2 weeks of treatment. They included nausea (25 versus 4%), abdominal pain (23 versus 4%), drowsiness (35 versus 2%), headache (13 versus 6%), and nasal congestion (23 versus 7%). 

The Health Technology Board of Scotland has concluded that in people with alcohol dependence, naltrexone reduces drinking (5). In a multicenter, double-blind, placebo-controlled, 12-week study of naltrexone 50 mg/day in 202 patients with alcohol dependence naltrexone was well tolerated, with few adverse effects abdominal pain (8.6%), headache (7.5%), nausea (6.5%), and dizziness (5.4%) there were no changes in liver function tests (6). However, those who took naltrexone did not have significant improvements in drinking history or fewer relapses. 

Naltrexone 50 mg/day has been used to relieve pruritus in cholestatic liver disease in five patients (7). Pruritus scores fell, but two patients developed severe nausea, vomiting, light-headedness, or tremor, requiring withdrawal of treatment. The reviewers commented that these reactions may or may not have been related to opioid withdrawal and that the trial had had several design limitations. They pointed out that one concern relating to the chronic use of high-dose naltrexone is an asymptomatic rise in serum transaminases, although the doses used in this study have not been reported to produce liver function abnormalities. 

A 29-year-old woman with bulimia nervosa and a family history of anxiety was enrolled in a trial of naltrexone (100 mg/day). She had no history of opioid use. Within hours of her first dose she experienced alarm, anxiety, chest discomfort, shortness of breath, a fear of dying, sweating, nausea, and derealization. She was unable to remain at home or to go out alone. For 3 days she continued to take naltrexone, with an increasing frequency of panic attacks. On day 4 she was treated with alprazolam (0.5 mg) but relapsed after further naltrexone. Withdrawal of naltrexone led to complete remission of symptoms. 

The risk factors for naltrexone-induced nausea have been studied in 120 alcohol-dependent patients in an open trial (14). After 5-30 days of abstinence, they received a bolus dose of naltrexone 25 mg followed by 50 mg/day for 10 weeks. Moderate to severe nausea was reported in 15%. The risk of nausea was significantly predicted by poor medication compliance, intensity of drinking during... 

Reversible hepatocellular injury has been reported with naltrexone in doses of up to 300 mg/day, which is five times that usually used for opioid blockade (SED-11, 147) (17). Five of twenty-six patients treated with naltrexone for obesity developed raised serum transaminase activities after 3-8 weeks of treatment. In another study in which 60 obese subjects received naltrexone for 8 weeks, there were abnormal liver function tests in six patients. Three patients failed to complete the course. Nausea and vomiting occurred within the first 24 hours of treatment but responded to a reduction in dose. There were also changes in mentation such as decreased mental acuity, depression, and anxiety, all of which resolved after withdrawal. This is significant, as adverse effects from naltrexone have previously been attributed to mild physical withdrawal syndromes. 

O Malley SS, Krishnan-Sarin S, Farren C, O Connor PG. Naltrexone-induced nausea in patients treated for alcohol dependence clinical predictors and evidence for opioid-mediated effects. J Clin Psychopharmacol 2000 20(l) 69-76. 

Naltrexone 25-50 mg/day Oral 2.7 Adjunct to prevent relapse in Nausea, vomiting, abdominal pain. 

Nausea is the most common side effect of naltrexone, occurring in about 10% of patients. Other side effects are headache, dizziness, nervousness, fatigue, insomnia, vomiting, anxiety, and somnolence. 

Opiates Pupillary constriction, constipation, drowsiness, coma, slurred speech, respiratory depression, Flu-like muscle aches, nausea or vomiting, yawning, piloerection, [animation, rhinorrhea, fever, insomnia, pupillary dilation Opiates receptors, locus cereleus pathway (noradrenergic) Naloxone (short half-life), naltrexone (longer half-life), donidine (ease withdrawal), methadone, LAMM (Levo-ac-aretyl-methadol) substitute addictions,longer withdrawal period Males > Females 3 1 TB, AIDS, hepatitis, pulmonary hypertension, pneumonia... 

Observational studies The use of naltrexone implants in 23 prison inmates before release from prison reduced the frequency of benzodiazepine and/or heroin use and criminality at 6 months after release but was associated with adverse reactions [18. Pruritus and rash at the implantation site were reported by two patients. Headache, nausea, reduced appetite, sleep disorders, restlessness, and irritability were reported by more than half of the patients. Constipation, diarrhea, and muscle/joint pains were uncommon. There were no serious adverse events. 

Naltrexone in the management of alcohol dependence has been reviewed [210 ]. The most common adverse reaction was nausea. Hepatotoxicity was a concern with doses of naltrexone over 50 mg/day. 

The most common adverse event was nausea, typically of early onset, transient, and dose related. The NNTb and NNTh were discussed in an editorial comment on this study [212. Nausea, the most common adverse event, was observed in 30% of those who took naltrexone 32 mg/day (NNTh = 5) and in 27% of those who took 16 mg/day (NNTh = 5). Withdrawal occurred in 20% and 21% respectively (NNTh = 11 and 9). 

The adverse reactions associated with the use of naltrexone in patients with alcohol dependence tend to be mild gastrointestinal reactions (nausea, vomiting, and abdominal pain or discomfort) and they occur early in treatment [204 ]. Hepatotoxicity has been reported with high doses (100-300 mg/ day) and especially in obese individuals. Naltrexone can also precipitate opioid withdrawal and may not be suitable for those requiring future opioids, such as those requiring surgery. 

In 12 subjects with kleptomania the most common adverse reaction to naltrexone 50-150 mg/day was nausea (in five subjects, one of whom withdrew as a result) [205 ]. Other events included dry mouth and... 

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