Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0011570 (depression)
 172,036 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Butorphanol, a new, totally synthetic morphinan, which is chemically related to naloxone, has been demonstrated to have both analgesic and narcotic antagonist properties. In rodent antiwrithing analgesic tests, butorphanol was 4 to 30 times more potent than morphine and dl-pentazocine, respectively. As an antagonist, butorphanol was about equivalent to nalorphine and 30 times more potent than dl-pentazocine. On the basis of the naloxone-induced mouse jumping test and the lack of substitution in withdrawn morphine-dependent mice, it is estimated that the potential for physical dependence of butorphanol will be less than that of dl-pentazocine but greater than that of nalorphine and dl-cyclazocine. Animal data also show that agonistic actions of butorphanol, such as respiratory depression and miosis, reach ceiling effects which are lower than those seen with morphine with an increase in dosage. Thus, butorphanol differed from morphine which exhibited agonist effects in a dose-related manner. Butorphanol showed weak to moderate central depressant properties at doses which were considerably higher (greater than 100 X) than those producing analgesia. Minimal cardiovascular and respiratory effects were seen with butorphanol in conscious dogs.
 ...
PMID:The pharmacology of butorphanol, a 3,14-dihydroxymorphinan narcotic antagonist analgesic. 6 89

Butorphanol tartrate 1 mg and 2 mg were compared in 80 normal mothers at term in a double-blind study with meperidine hydrochloride 40 mg and 80 mg for the relief of pain in labour. Butorphanol was found to be as effective as meperidine in relieving pain in labour. The foetal condition, as measured by ECG monitoring, Apgar scores, time to sustained respiration, umbilical venous H+ (pH) and PCO2, and a general nursery survey were comparable for meperidine and butorphanol. No psychomimetic phenomena were seen. Assays indicated that both butorphanol and meperidine crossed the placenta. The mean concentration of butorphanol in neonatal serum was 0.84 times maternal serum at 1.5 to 3.5 hours after intramuscular administration of a single or two successive doses of butorphanol 1 mg or 2 mg to the mother. The mean concentrations for meperidine in neonatal serum was 0.89 times maternal serum at 0.85 to 3.6 hours after intramuscular administration of meperidine 40 mg or 80 mg to the mother. Neither analgesic caused severe depression of the infant except for one meperidine-treated case.
 ...
PMID:A double-blind comparison of butorphanol and meperidine in labour: maternal pain relief and effect on the newborn. 35 9

Butorphanol tartrate (Stadol; Anaquest, Madison, WI/Bristol-Meyers Squibb, Evansville, IN) is an analgesic possessing mixed agonist-antagonist activity at opiate receptors. Receptor specificity has been used to limit respiratory depression, gastrointestinal side effects, and reduce the risk of dependency. Theoretically it offers an advantage over traditional opiates such as morphine and meperidine in the treatment of moderate pain. Butorphanol has been used as a preoperative sedative and analgesic, as a supplement to balanced anesthesia, and for suppression of postanesthesia shaking. Other recognized uses include obstetric analgesia during labor and relief of moderate postpartum pain. In addition, butorphanol has been used effectively for conscious sedation. Its lack of euphoric effects may be useful in emergency medicine for clinical populations prone to drug-seeking behavior. Butorphanol has been used more recently for epidural analgesia or for intravenous patient-controlled analgesia when allergies to opiates exist. Since butorphanol is not a controlled substance, its use can reduce administrative liability for abuse and can lower the number of distribution records associated with Schedule II narcotics.
 ...
PMID:Butorphanol tartrate (stadol): a review. 184 91

The optimum doses according to age of butorphanol tartrate as a supplemental drug during epidural and spinal anesthesia were investigated in 60 patients without complications. We classified patients into 4 groups by age as A, B, C and D-group. A-group consisting of patients between 20 to 40 years received 1.5mg of butorphanol. B-group 41-60, C-group 61-75 and D-group over 76 years received 1.0mg, 0.5mg and 0.25mg respectively. After operation was started without pain, and during the stable period, we determined by age, doses of butorphanol injected intravenously in one minute. HRs, mean BPs, respiratory rates (RRs) and so on were obtained at the preinjection point and 5 minutes after injection. In addition, in 15 patients, arterial blood gas analysis was performed at the same times. Butorphanol injections decreased HRs, mean BPs and RRs significantly. But there was no one whose PaCO2 increased more than 50 mmHg and no difference was found in degree of side effects between the groups. In conclusion, this study suggests that the decision to administer doses depending on the age is useful to decrease frequency of the grave side effects, especially respiratory depression which the elderly people frequently fall into.
 ...
PMID:[Optimum dose of intravenous butorphanol as a supplemental drug during regional anesthesia]. 272 13

Butorphanol tartrate is a highly effective opioid agonist-antagonist analgesic with qualitative as well as quantitative differences from the pure agonists. These differences are thought to be due to interaction with a distinct subset of opioid receptors. Although it relieves severe pain, the drug does not usually elevate mood, and it may occasionally cause dysphoria. Counterbalancing its disadvantages is a wealth of clinical experience with the drug showing an impressive record of safety. Butorphanol produces limited respiratory depression and smooth muscle spasm, and both effects are reversible with naloxone. The most prominent side effect is sedation, a property that is generally quite useful in the perioperative period. Butorphanol is a weak morphine antagonist, so it may interact with agonists like morphine or fentanyl. The chief advantages of this agent are its low toxicity and very low potential for abuse.
 ...
PMID:Butorphanol in perspective. 283 Jul 56

Seventy institutionalized severely and profoundly retarded patients were administered intramuscular butorphanol, 1.0 to 4.0 mg, for premedication prior to dental procedures. These patients had been refractory to previous combined chloral hydrate and diphenhydramine treatment. Clinical efficacy was categorized according to the extent that adjunctive restraints were required to accomplish the dental procedure. A total of 151 butorphanol trials were recorded. Butorphanol was observed to be clinically effective in 74.8% of the administrations and sedation was observed in 28.2% of the trials. Dosage titration increased efficacy to 85.0%. Contribution of concurrent central nervous system depressant medication to clinical efficacy and dose requirements lacked statistical significance; however, a strong trend (p = 0.068) was found in the medication-free group with higher dosage. Vomiting (2.6%) was the most frequent adverse effect observed. One patient had marked cardiorespiratory depression that was promptly reversed by intravenous naloxone. Two patients experienced mild hypotensive episodes immediately following injection, but they recovered uneventfully. Butorphanol was shown to be a safe and effective agent for dental premedication in this difficult patient population.
 ...
PMID:Butorphanol as a dental premedication in the mentally retarded. 295 29

The agonist/antagonist analgesics, butorphanol (Stadol) and nalbuphine (Nubain), are being increasingly employed as intravenous sedation agents; nalbuphine will be available in the future as an oral analgesic. The drugs possess numerous pharmacologic similarities and some dissimilarities. Both are equianalgesic (and nalbuphine is equipotent) with morphine parenterally and codeine orally. Their pharmacokinetics are similar; nalbuphine has a longer duration of action. Both may precipitate an abstinence syndrome in narcotic-dependent persons and will probably be associated with low-level drug abuse potential. They are both agonists of the kappa opioid receptor and partial agonists of the mu receptor. Butorphanol is a partial agonist of the sigma receptor responsible for psychotomimetic effects. The incidence of adverse effects is low, sedation being the most common. In cardiac-risk patients, nalbuphine does not increase cardiac work or oxygen requirements; nor do increasing doses of nalbuphine increase the duration of respiratory depression. Both drugs possess plateau respiratory depressant actions.
 ...
PMID:Butorphanol and nalbuphine: a pharmacologic comparison. 298 81

The effect of butorphanol on respiratory drive was assessed using a carbon dioxide response test (CRT). Eight male volunteers received 3 mg/70 kg of intravenous butorphanol every 30 min to a cumulative dose of 15 mg/70 kg (5 doses). Thirty minutes before the first butorphanol dose, each subject received normal saline to establish a baseline CRT. After each butorphanol dose, a CRT was repeated at 15 min to assess respiratory depression. Minute ventilation was plotted against PaCO2 to generate a regression line for saline and each dose. Slopes and intercepts for each line were calculated by least squares linear regression, and CRT displacement from saline was determined at each dose. The mean slope for each dose was not significantly different from the saline slope (p = 0.23-0.91). The mean displacement (+/- SEM) of the CRT from saline was greatest after the second dose (7.29 +/- 1.94 mm Hg) but not significantly different from the first or subsequent doses (p greater than 0.05). Butorphanol in doses of up to 15 mg/70 kg may have a 'ceiling effect' in respiratory depression.
 ...
PMID:Respiratory effects of high-dose butorphanol. 312 14

Cardiohemodynamic and respiratory effects of eptazocine, a new analgesic agent, were studied and compared with those of pentazocine and butorphanol in anesthetized dogs. Eptazocine (1 mg/kg, i.v.) increased the heart rate (HR), left ventricular dP/dt (LVdP/dt) and cardiac output (CO), and scarcely affected the blood pressure (BP), left ventricular end-diastolic pressure (LVEDP), right atrial pressure, pulmonary arterial pressure (PAP) and pulmonary capillary wedge pressure. On the other hand, eptazocine (3 mg/kg, i.v.) decreased BP, LVdP/dt, CO and LVEDP and did not influence the pulmonary circulation. Pentazocine (1 mg/kg and 3 mg/kg, i.v.) increased BP, LVdP/dt and CO, while HR was not altered. Pentazocine also increased PAP. Butorphanol (0.1 mg/kg and 0.3 mg/kg, i.v.) decreased BP, HR and LVdP/dt, while other hemodynamic parameters were not changed. In spontaneously breathing anesthetized dogs, eptazocine (1 mg/kg and 3 mg/kg, i.v.) caused a decrease of respiratory minute volume. The fall in PO2 and pH, and a rise in PCO2 were simultaneously observed in blood gas analysis. These respiratory depressant effects of eptazocine were short-lasting, and they were less potent than those of pentazocine. Butorphanol scarcely affected the respiration. These results suggest that eptazocine has different cardiohemodynamic effects than other analgesics and produces mild respiratory depression.
 ...
PMID:[Cardiohemodynamic and respiratory effects of eptazocine, a new analgesic agent, in anesthetized dogs]. 337 99

A double-blind, randomized study was conducted in 16 patients who were anesthetized with 50% nitrous oxide in oxygen and given either 0.17 mg/kg butorphanol or 0.86 mg/kg nalbuphine, and whose respiratory depression was assessed by the response of minute ventilation to increasing carbon dioxide concentrations. The slopes of the carbon dioxide ventilatory response curves [delta VE/delta PCO2(L.min-1 X %CO2(-1)] were 7.45 +/- 1.17 with nalbuphine and 2.42 +/- 0.56 with butorphanol. Butorphanol caused significantly (P less than 0.025) greater respiratory depression than nalbuphine. The results of this study caution against the indiscriminate use of butorphanol in the perianesthetic setting.
 ...
PMID:Respiratory effects of nalbuphine and butorphanol in anesthetized patients. 361 95


1 2 Next >>