morphinans and Nausea

Butorphanol (Stadol) is a synthetic agonist-antagonist analgesic from the 14-hydroxymorphinan series. Animal studies display analgesia, antitussive effects, low gastrointestinal activity, limited respiratory depression, some cardiovascular and skeletal muscle actions, diuresis, slight miosis and opiate antagonism. Butorphanol is metabolized in the liver with renal excretion, yielding a half-life of 3-4 h. Pain relief is good to excellent with parenteral administration in 90% of patients with moderate to severe pain. Surgical anesthetic indications involve preoperative and preinduction supplementation, balanced anesthesia and postoperative pain. Side effects are sedation, nausea, elevated pulmonary vascular pressures and rarely CNS excitation. Limited respiratory depression exists. Butorphanol is a potent analgesic agent with a favorable side effect profile.

Topics: Anesthesia; Animals; Antitussive Agents; Butorphanol; Chemical Phenomena; Chemistry; Depression, Chemical; Diuretics; Dose-Response Relationship, Drug; Humans; Morphinans; Morphine; Naloxone; Nausea; Oxymorphone; Pain; Pulmonary Wedge Pressure; Rats; Respiration; Substance-Related Disorders

Topics: Analgesics; Blood Circulation; Fentanyl; Humans; Intestines; Levallorphan; Meperidine; Methadone; Methotrimeprazine; Morphinans; Morphine; Nalorphine; Narcotic Antagonists; Nausea; Pain; Pentazocine; Psychopharmacology; Respiration; Substance-Related Disorders; Urinary Tract; Vomiting

We prospectively investigated the efficacy of opioid rotation from oral morphine to oral oxycodone in cancer patients who had difficulty in continuing oral morphine treatment because of inadequate analgesia and/or intolerable side effects.. Twenty-seven patients were enrolled and 25 were evaluated. The rate of patients who achieved adequate pain control, which provided an indication of treatment success, was evaluated as primary endpoint. The acceptability and pharmacokinetics of oxycodone were evaluated in addition to the assessment of analgesic efficacy and safety during the study period.. In spite of intense pain, the morphine daily dose could not be increased in most patients before the study because of intolerable side effects. However, switching to oral oxycodone allowed approximately 1.7-fold increase as morphine equivalent dose. Consequently, 84.0% (21/25) of patients achieved adequate pain control. By the end of the study, all patients except one had tolerated the morphine-induced intolerable side effects (i.e. nausea, vomiting, constipation, drowsiness). Common side effects (>10%) that occurred during the study were typically known for strong opioid analgesics, and most were mild to moderate in severity. A significant negative correlation between creatinine clearance (CCr) value and the trough concentrations of the morphine metabolites was observed. On the other hand, no significant correlation was found between CCr value and the pharmacokinetic parameters of oxycodone or its metabolites.. For patients who had difficulty in continuing oral morphine treatment, regardless of renal function, opioid rotation to oral oxycodone may be an effective approach to alleviate intolerable side effects and pain.

Topics: Administration, Oral; Aged; Analgesics, Opioid; Constipation; Drug Administration Schedule; Female; Humans; Linear Models; Male; Middle Aged; Morphinans; Morphine; Morphine Derivatives; Nausea; Neoplasms; Oxycodone; Pain; Prospective Studies; Renal Insufficiency, Chronic; Sleep Stages; Treatment Outcome; Vomiting

The frequency of postanesthesia side effects and times to reach "benchmarks" in the recovery process for IV preinduction doses of 20 micrograms/kg butorphanol, 40 micrograms/kg butorphanol, or a 2 micrograms/kg dose of fentanyl were compared in a double-blinded study involving ambulatory surgical patients. The authors hypothesized that all drugs would perform equally well in all study areas. Sixty ASA physical status I and II women undergoing laparoscopic tubal sterilization were randomly assigned to one of three groups: Group I (n = 20) received 20 micrograms/kg butorphanol as a preinduction agent; Group II (n = 20) received 40 micrograms/kg butorphanol; Group III (n = 20) received 2 micrograms/kg fentanyl. Anesthesia management for all groups was the same. Statistically significant variance was found in time to discharge-ready status and duration of nausea (p less than 0.05) between 40 micrograms/kg butorphanol and 2 micrograms/kg fentanyl, but no significant difference was found between 20 micrograms/kg butorphanol and 2 micrograms/kg fentanyl in these areas. Statistically significant variance was found in duration of dizziness and time to obtain a 10 on the Aldrete Post Anesthesia Recovery Score (APARS) between 40 micrograms/kg butorphanol and 20 micrograms/kg butorphanol and 40 micrograms/kg butorphanol and 2 micrograms/kg fentanyl. From the study, 20 micrograms/kg butorphanol appears to be as suitable as 2 micrograms/kg fentanyl for use as a preinduction narcotic analgesic, whereas 40 micrograms/kg butorphanol appears to be unsuitable due to increased duration of nausea, dizziness, and time to score 10 on APARS and reach discharge-ready status.

Topics: Adult; Anesthesia Recovery Period; Anesthesia, Intravenous; Butorphanol; Dizziness; Double-Blind Method; Female; Fentanyl; Humans; Morphinans; Nausea; Postoperative Period; Random Allocation; Sterilization, Reproductive; Time Factors

Drug dosages, length of stay (LOS), and incidence of psychological side effects of fentanyl and nalbuphine were compared in a randomized, double-blind study using unpremedicated female day-surgery patients undergoing diagnostic laparoscopy. Patients received either fentanyl 1.5 micrograms/kg (F group; n = 142), low-dose nalbuphine 300 micrograms/kg (LN group; N = 103), or high-dose nalbuphine 500 micrograms/kg (HN group; n = 41), intravenously (IV) before anesthesia consisting of thiopental, N2O, O2, and a succinylcholine infusion. Additional IV intraoperative and IM postoperative opioids were given if required for signs of inadequate anesthesia or postoperative pain. The patients' clinical and psychological status was evaluated at 20-min intervals postoperatively by a team of trained interviewers. The low- and high-dose nalbuphine groups clinically resembled the fentanyl group in terms of dosing frequency and patients' self-ratings of postoperative analgesia. Length of stay and postoperative sedation were significantly greater with nalbuphine. The incidence of psychological side effects, including dreaming and postoperative anxiety, was also greater with nalbuphine. However, patient acceptance of nalbuphine was high and was similar to that observed in patients given fentanyl.

Topics: Ambulatory Care; Anxiety; Clinical Trials as Topic; Double-Blind Method; Dreams; Female; Fentanyl; Humans; Laparoscopy; Length of Stay; Morphinans; Nalbuphine; Nausea; Random Allocation

In a randomized double-blind placebo-controlled trial involving 80 patients nalbuphine 10 mg and 20 mg were compared with pethidine 100 mg and a placebo given i.m. at least 90 min before minor gynaecological surgery. Nalbuphine proved a suitable alternative to pethidine, producing beneficial sedation which was maximum at 60 min after injection. Both nalbuphine and pethidine reduced the excitatory sequelae of methohexitone induction. Increasing the dose of nalbuphine from 10 mg to 20 mg produced no significant additional sedation or intraoperative benefit. Short-lived pain at the injection site was a feature of the use of nalbuphine in either dose. The main disadvantage of nalbuphine was nausea and vomiting of delayed onset, the frequency of which was similar after either dose.

Topics: Adult; Clinical Trials as Topic; Female; Humans; Meperidine; Morphinans; Nalbuphine; Nausea; Postoperative Complications; Preanesthetic Medication; Vomiting

The safety and efficacy of single intramuscular doses of dezocine (10 or 15 mg) were compared with butorphanol (2 mg) and placebo in 157 patients with moderate to severe postoperative pain. A verbal pain intensity scale, an analog pain intensity scale, and a verbal pain relief scale were used to record the patients' subjective assessments. The results of this study indicate that a single 10 or 15 mg intramuscular injection of dezocine is safe and more effective than placebo for four to six hours, respectively, in the treatment of moderate to severe postoperative pain (P less than .05). During the first hour of treatment the pain relief afforded by 2 mg of butorphanol was significantly greater than that afforded by 10 mg of dezocine (P less than .05), but both doses of dezocine provided long-lasting relief. The scores on all three efficacy scales were highest with the 15 mg dose of dezocine after the first hour, while the 10 mg dose of dezocine and butorphanol were compared during this period. Nausea and vomiting were the most commonly reported side effects; injection site reactions were reported more frequently in the butorphanol group.

Topics: Acute Disease; Adolescent; Adult; Bridged Bicyclo Compounds, Heterocyclic; Butorphanol; Clinical Trials as Topic; Consumer Behavior; Cycloparaffins; Double-Blind Method; Female; Humans; Injections, Intramuscular; Male; Middle Aged; Morphinans; Nausea; Pain, Postoperative; Placebos; Tetrahydronaphthalenes; Time Factors; Vomiting

A randomized double-blind cross-over study was performed to evaluate the possible anti-emetic effect of the partial opiate antagonist buprenorphine in comparison to domperidone in chemotherapy-induced nausea and vomiting. Emesis was of significantly shorter duration on domperidone treatment. Most patients preferred domperidone, mainly due to adverse side-effects of buprenorphine. Nevertheless, emesis in buprenorphine treatment was less disabling. Therefore, it might be useful to search for new alternatives in this group of drugs or to use them in a combination regimen of anti-emetic agents.

Topics: Adult; Aged; Antiemetics; Antineoplastic Agents; Buprenorphine; Clinical Trials as Topic; Domperidone; Double-Blind Method; Female; Humans; Male; Middle Aged; Morphinans; Nausea; Pilot Projects; Random Allocation; Vomiting

Buprenorphine was used as an analgesic medication for patients at the pain clinic. Clinical observations on its long term administration for intractable pain are reported. A good analgesic activity was noted in most of the patients. Nausea and vomiting was the mean reason for cancellation of the therapy.

Topics: Administration, Oral; Adult; Aged; Analgesics; Clinical Trials as Topic; Confusion; Depression; Drug Evaluation; Female; Humans; Male; Middle Aged; Morphinans; Nausea; Pain; Sleep; Sweating; Time Factors; Vomiting

Topics: Adolescent; Adult; Aged; Blood Pressure; Cholecystectomy; Female; Humans; Isonipecotic Acids; Male; Meperidine; Middle Aged; Morphinans; Nausea; Nitriles; Pain; Piperidines; Pulse; Respiration; Vomiting

Topics: Administration, Oral; Adolescent; Adult; Aged; Analgesia; Clinical Trials as Topic; Female; Headache; Humans; Male; Middle Aged; Morphinans; Nausea; Pentazocine; Placebos; Time Factors; Vomiting

The new paradigm of precision medicine in oncology questions today the respective place of evidence-based medicine and doctor-patient relationship. Based on the results of a randomized study comparing the efficacy of a homeopathic molecule in the prevention of nausea and vomiting induced by chemotherapy in non-metastatic breast cancer, this article extends and develops the discussion of maintaining an unresolved tension between medical art and medical science, between care and cure. This tension sets a base for the authors of the therapeutic alliance in medicine, defined as a dialectic constantly adjourned between the alliance of the doctor with the patient and his therapy, and the therapeutic effect of this alliance. Because if a policy or a public opinion were to promote an exclusively rational medicine deprived of the field of relation to care, or on the contrary a medicine based only on clinical sense and intuition, then respectively the ethics of care and the progress of therapy would be threatened. It is advisable to be aware of erring from the truth, amplified today by social networks, as much due to a tide of scientific positivism, as an excess of the "good caring soul". Taking into account the therapeutic alliance makes it possible to no longer oppose scientific medicine and care relationship.

Topics: Breast Neoplasms; Delivery of Health Care; Evidence-Based Medicine; Female; Humans; Materia Medica; Medicine; Metaphor; Morphinans; Nausea; Online Social Networking; Physician-Patient Relations; Precision Medicine; Proof of Concept Study; Randomized Controlled Trials as Topic; Science; Therapeutic Alliance; Vomiting

Topics: Adult; Advance Care Planning; Aged; Antiemetics; Baclofen; Benzodiazepines; Constipation; Depressive Disorder, Major; Dyspnea; Female; Hiccup; Humans; Male; Methylphenidate; Middle Aged; Morphinans; Morphine; Nausea; Olanzapine; Palliative Medicine; Polyethylene Glycols; Prochlorperazine; Pruritus; Sertraline; Terminal Care; Walkers

Topics: Adult; Female; Heart Rate; Humans; Infant, Newborn; Male; Middle Aged; Morphinans; Morphine; Nalbuphine; Nausea; Pain; Postoperative Complications; Respiration

A therapeutic regimen is described for sedative, analgesic, and anti-emetic effect in patients receiving intra-arterial carmustine (BCNU) for malignant gliomas. This regimen consists of nalbuphine, 30 mg, i.v., and droperidol, 2.5 mg, i.v., given immediately prior to intra-carotid BCNU infusion. Droperidol, 2.5 mg, i.v., is then administered on four hour intervals for sixteen hours post-procedure. This combination provided excellent effect in nine patients treated for twelve intra-carotid infusions. None of the nine patients experienced vomiting, one experienced mild nausea several hours post-infusion, and non complained of severe pain or discomfort. Thirteen additional patients received diazepam, 10 mg, P.O., prior to the intra-carotid BCNU infusion, with fentanyl, 100 mcg, i.v., and prochlorperazine, 10 mg, i.m. at the onset of infusion. All thirteen patients suffered from severe nausea, vomiting, and orbital pain. The nalbuphine/droperidol combination is thought to provide a superior alternative to the traditional narcotic/pheonothiazine/benzodiazepine combination for carotid BCNU infusion. This combination has theoretical advantages for the patient with intracranial mass lesions by providing analgesia and sedation with minimal potential for respiratory depression and carbon dioxide retention.

Topics: Adult; Aged; Brain Neoplasms; Carmustine; Carotid Arteries; Diazepam; Droperidol; Drug Therapy, Combination; Fentanyl; Glioma; Humans; Injections, Intra-Arterial; Middle Aged; Morphinans; Nalbuphine; Nausea; Prochlorperazine; Vomiting

Topics: Adult; Anesthesia, Epidural; Aspirin; Blood Pressure; Butorphanol; Caffeine; Cesarean Section; Codeine; Drug Combinations; Female; Humans; Morphinans; Nausea; Oxycodone; Phenacetin; Pregnancy; Reoperation; Substance Withdrawal Syndrome

Buprenorphine, a partial opiate-receptor agonist with potent analgesic properties, was given to 7548 patients in the immediate postoperative period. Ninety per cent of patients had good or adequate pain relief for at least 4 hours; there were few adverse effects and the incidence of drug-associated respiratory depression was estimated at less than 1%. There were no other side-effects of clinical note.

Topics: Adolescent; Adult; Aged; Buprenorphine; Child; Child, Preschool; Drug Evaluation; Female; Humans; Male; Middle Aged; Morphinans; Nausea; Pain, Postoperative; Respiratory Insufficiency; Time Factors; Vomiting