Articles: narcotic-antagonists.
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Arzneimittel Forsch · Jul 1999
Randomized Controlled Trial Comparative Study Clinical TrialBioavailability investigation of a new tilidine/naloxone liquid formulation compared to a reference formulation.
An oral solution available as ethanol-free droplets of the fixed drug combination tilidine-HCl 50 mg/naloxone-HCl 4 mg (CAS 27107-79-5 and CAS 465-65-6, respectively; Tilidin-ratiopharm plus Tropfen) was investigated in 12 healthy volunteers together with an ethanol-containing reference preparation for comparable bioavailability. The study was conducted in an open, randomized, two-way cross-over design applying single doses of 20 droplets (equivalent to 50 mg tilidine-HCl/4 mg naloxone-HCl) of either formulation in the fasting state. The drug plasma profiles were monitored for a period of 48 h by means of LC-MS/MS for tilidine and its active metabolite nortilidine, whereas GC-MS was employed in order to determine naloxone and its phase I metabolite, 6-beta-naloxole. ⋯ In conclusion, single doses of two different tilidine/naloxone 50 mg/4 mg liquid formulations revealed well comparable bioavailability for all 4 analytes investigated. Both treatments were fairly well tolerated. Most frequently reported adverse events were dizziness, headache and nausea, which all recovered without sequelae and necessity of concomitant treatment.
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J. Obstet. Gynaecol. Res. · Jun 1999
Randomized Controlled Trial Clinical TrialOptimal dose of nalbuphine for treatment of intrathecal-morphine induced pruritus after caesarean section.
To search for the optimal dosage of nalbuphine relief of intrathecal-morphine induced pruritus after caesarean section. ⋯ Nalbuphine of 2 to 3 mg was considered to be adequate in treatment of intrathecal morphine induced pruritus after caesarean section without increasing pain scores or causing other side effects.
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Randomized Controlled Trial Clinical Trial
The effect of naloxone on ketamine-induced effects on hyperalgesia and ketamine-induced side effects in humans.
The (NMDA) receptor plays a significant role in wind-up and spinal hypersensitivity and is involved in the occurrence of secondary hyperalgesia. Ketamine is an NMDA-receptor antagonist and has proven effective in alleviating secondary hyperalgesia in humans. Although it is disputed, the actions of ketamine have been ascribed not only to NMDA receptor antagonism, but also to opioid receptor agonism. A study therefore was designed in which the abolishment of a previously demonstrated effect of ketamine on secondary hyperalgesia was sought by pretreatment with naloxone. ⋯ In this experimental setting, opioid receptor blockade does not inhibit ketamine-induced reductions of secondary hyperalgesia.
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We report the case of a 30-year-old male, heroin dependent, receiving methadone treatment, who, while staying at home, ingested 50 mg of naltrexone. He immediately developed serious withdrawal symptoms and was admitted to the hospital. In the emergency department the drugs given to counteract the agitation were ineffective, and the patient developed respiratory distress. ⋯ Afterwards he did not attend his scheduled outpatient follow-up visits. Treatment with propofol is effective in the case of a patient with a serious withdrawal syndrome secondary to naltrexone overdose during methadone therapy. Despite the actual possibility of getting through the withdrawal symptoms the patient failed to return for follow-up visits, which might be related to a lack of motivation.
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J. Pharmacol. Exp. Ther. · May 1999
Spinal blockade of opioid receptors prevents the analgesia produced by TENS in arthritic rats.
Transcutaneous electrical nerve stimulation (TENS) is commonly used for relief of pain. The literature on the clinical application of TENS is extensive. However, surprisingly few reports have addressed the neurophysiological basis for the actions of TENS. ⋯ Spinal blockade of delta opioid receptors dose-dependently prevented the antihyperalgesia produced by high-frequency TENS. In contrast, blockade of kappa opioid receptors had no effect on the antihyperalgesia produced by either low- or high-frequency TENS. Thus, low-frequency TENS produces antihyperalgesia through mu opioid receptors and high-frequency TENS produces antihyperalgesia through delta opioid receptors in the spinal cord.