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At least 19 recordsLinked to original sources
PubMed1980

A comparison of alphaprodine and meperidine pharmacokinetics.

We have developed a gas-liquid chromatographic analysis for measuring plasma alphaprodine. The analysis is sufficiently sensitive for studying therapeutic-dose pharmacokinetics in man. Single intravenous bolus injections of either alphaprodine or meperidine were given to volunteer subjects. Plasma concentration data were fitted to a biexpoential equation and pharmacokinetic parameters were calculated. Consistent with alphaprodine's shorter clinical duration compared to meperidine, we found that plasma levels of alphaprodine decline at a more rapid rate. Plasma clearances for the two narcotics are nearly identical (1.04 l./kg/min for alphaprodine and 1.01 l./kg/min for meperidine). The apparent volume of distribution for alphaprodine is smaller than for meperidine (1.90 l./kg for alphaprodine and 3.37 l./kg for meperidine).

Adult↗
PubMed1978

Comparing the effects of anileridine, alphaprodine and fentanyl on schedule-controlled responding by pigeons.

The effects of anileridine, alphaprodine and fentanyl were studied on responding by pigeons under a multiple fixed-ratio, fixed-interval schedule of food presentation. Generally, all three drugs produced dose-related decreases in responding under both components of the multiple schedule, but rate increases were observed after low doses of anileridine and alphaprodine in some birds. Naloxone (1 mg/kg) antagonized the rate-increasing and rate-decreasing effects of doses of anileridine and alphaprodine of 10 mg/kg or less, whereas the effects of higher doses were not antagonized by naloxone. Likewise, chronic methadone or morphine (120 mg/kg/day p.o.) dosing produced only a slight cross-tolerance to the rate-decreasing effects of anileridine and alphaprodine. In contrast, naloxone (0.01, 0.1 and 1 mg/kg) and chronic methadone or morphine administration shifted the dose-effect curve for fentanyl to the right, indicating narcotic antagonism and methadone and morphine-induced cross-tolerance. These data indicate that the rate-decreasing effects of anileridine and alphaprodine are related only slightly to narcotic effects, whereas the rate-decreasing effects of fentanyl are primarily narcotic effects.

Alphaprodine↗
PubMed1986

Neonatal responses to alphaprodine administered during labor.

The effect of intravenously administered alphaprodine on newborn Apgar scores, neonatal acid-base status, and the Neurologic and Adaptive Capacity Scoring System (NACS) were compared in 30 parturients. Patients in group 1 (n = 15) received 20-40 mg increments of alphaprodine, with a total dose of 39.3 +/- 3.7 mg (mean +/- SEM). Group 2 patients (n = 15) received no medication during labor. Apgar scores, neonatal acid-base status, and the NACS were equally good in the two groups. The concentrations of alphaprodine in maternal vein, umbilical vein, and umbilical artery at delivery were measured using a gas-chromographic mass spectrophotometric technique. The results showed an umbilical vein-to-maternal vein ratio of 0.52 +/- 0.09. It is concluded that when administered as in this study, alphaprodine has no adverse effects on the neonate.

Adult↗
PubMed1982

Maternal and fetal response to alphaprodine during labor. A preliminary study.

Alphaprodine is a synthetic narcotic, structurally similar to meperidine. Respiratory depression has been reported as a not-infrequent side effect when larger doses of alphaprodine were used, particularly intravenously. In this study, the maternal respiratory rate and tissue pO2 and pCO2 were determined in patients receiving alphaprodine, 0.4 mg/kg of prepregnancy weight, for first-stage analgesia. Statistically significant falls in maternal tcpO2 and increases in tcpCO2 were observed. The baseline fetal heart rate decreased significantly 20 minutes after the injection (139 to 132 bpm). There was no increase in abnormal fetal heart rate patterns. The variability of the baseline fetal heart rate was unchanged until 25 minutes following alphaprodine administration, when a significant reduction occurred. The changes seen in the parameters monitored in this study were not associated with any clinically adverse effects on the mother or fetus.

Alphaprodine↗
PubMed1980

Comparison of haemodynamic effects of anaesthetic doses of alphaprodine and sulfentanil in the dog.

The haemodynamic effects of equi-anaesthetic doses of alphaprodine and sulfentanil were evaluated in mongrel dogs ventilated mechanically. The effects of the addition of atropine were assessed for each drug, as were the effects of breathing nitrous oxide 60 per cent with oxygen and nitrogen 60 per cent with oxygen and the administration of naloxone. The results of this study demonstrate that anaesthetic doses of sulfentanil produce little change in cardiovascular dynamics in atropinized dogs and only small changes in dogs without atropine premedication, irrespective of the infusion rate. In contrast alphaprodine causes a significant cardiovascular depression irrespective of the presence or absence of atropine premedication. Naloxone reversed the anaesthetic effects in all dogs anaesthetized with alphaprodine but did not reverse the anaesthetic state in any dog given sulfentanil. Our data suggest that sulfentanil deserves evaluation as a narcotic anaesthetic in man.

Alphaprodine↗
PubMed1989

Obstetrical medication and the human newborn: the influence of alphaprodine hydrochloride on visual behaviour.

The visual habituation of two groups of newborn infants was tested at a mean age of 2.9 days with large achromatic squares of varying luminance. Mothers of the infants in one group received no medication during labour; mothers in the second group received a single dose of the synthetic narcotic alphaprodine hydrochloride. The two groups did not differ in the number of trials to reach the criterion, but newborns in the no-medication group fixated the stimuli for much longer periods than did infants in the alphaprodine group. First-fixation times of babies in the alphaprodine group were shorter when drug-to-delivery intervals were longer. These results, although tentative, imply that babies of medicated and unmedicated mothers differ in the manner in which they respond to visual stimuli.

Alphaprodine↗
PubMed1979

Relative potencies and durations of action with respect to respiratory depression of intravenous meperidine, fentanyl and alphaprodine in man.

Fentanyl, 0.7 and 1.4 microgram/kg, alphaprodine, 0.135 and 0.270 mg/kg meperidine, 0.564 and 1.127 mg/kg, and placebo were administered intravenously over 2.6 min by infusion to five healthy adult males. The crossover study was of incomplete Latin square design with at least 1 week between administrations of each study drug. The subjects breathed from a mixing chamber the gas composition of which was servo-controlled so as to produce CO2 ramps in the end-tidal gases. Each experiment was composed of: 1) control CO2 ramps, 2) a 25-min isocarbic run during which the drug was infused and 3) CO2 ramps at half-hour intervals for 3 hr postinfusion. The 20-liter intercept (the PETCO2 at which ventilation was 20 liters/min) was used as the measure of respiratory drive; the change in 20-liter intercept measured drug effect. The potency ratios at peak effect were: fentanyl/meperidine, 679; alphaprodine/meperidine, 3.68; fentanyl/alphaprodine, 179. With the area under the time-effect curves, the potency ratios of mean effect were: fentanyl/meperidine, 45c; alphaprodine/meperidine, 3.00; fentanyl/alphaprodine, 141. Thus, both fentanyl and alphaprodine are shorter-acting than meperidine, and fentanyl is shorter-acting than alphaprodine. The time-effect curves were fitted to linear and mono- and bi-exponential models. The time constants were compatible with the above relative durations of action.

Adult↗
PubMed1986

Cyanosis of the hands following the use of alphaprodine in dental anaesthesia.

A case is presented of asymptomatic cyanosis of the hands, seen four hours after dental surgery under intravenous, local and inhalational anaesthesia. Alphaprodine hydrochloride, a synthetic opiate and one of the agents used, may produce dilatation of the venous bed with passive venous pooling. Such a mechanism is thought to have occurred in this case, manifesting as cyanosis. A weakly positive intradermal skin test to alphaprodine suggests immediate type hypersensitivity as a possible underlying cause.

Adolescent↗
PubMed1980

Comparison of morphine, meperidine, anileridine, and alphaprodine on schedule-controlled responding and analgesia.

The effects of morphine, meperidine, alphaprodine, and anileridine were studied alone and in the presence of 1 mg/kg of naloxone in rats on level pressing under a fixed-ratio 20-response schedule of food presentation and on tail-withdrawal latency from warm water (55 degrees C) as a measure of analgesia. All four narcotics decreased rates of lever pressing and increased tail-withdrawal latencies. Naloxone antagonized the effects of all four narcotics on tail-withdrawal, but did not antagonize the rate-decreasing effect of meperidine on lever pressing. Naloxone shifted the morphine dose-effect for lever-pressing by a factor of 4-8; the alphaprodine dose-effect curve by a factor of 4-8; and the anileridine dose-effect curve by a factor of 2. These results strengthen the interpretation that meperidine's effect on schedule-controlled responding is not mediated by a narcotic action whereas the analgesic effect is. The results also suggest that anileridine has significant non-narcotic actions like meperidine.

Alphaprodine↗
PubMedDate not supplied

Effects of variable alphaprodine dose levels on arterial blood gases in rhesus monkeys.

The administration of alphaprodine submucosally in doses of 0.5, 1.0, and 1.5 mg/kg to ketaminized rhesus monkeys resulted in Po(2) levels significantly lower than those observed for controls (ketamine only) at the 10 min level. There was a significant increase in Po(2) levels between the 10 and 20 min intervals, thereafter, Po(2) levels returned toward normal and were not statistically different from baseline. Higher alphaprodine doses (1.0 and 1.5 mg/kg) resulted in a non-significant increase in Pco(2) values. Monitoring Po(2) levels during sedation seems preferable to monitoring Pco(2) in view of the findings of this study.

Alphaprodine↗
PubMed1982

The clinical significance of a sinusoidal fetal heart rate pattern associated with alphaprodine administration.

A prospective analysis of 34 patients in active labor who were given alphaprodine for analgesia revealed a 32% incidence of sinusoidal fetal heart rate patterns (SFHRP). In a control group of 27 patients who did not receive narcotic analgesia, 1 patient (3.7%) showed a sinusoidal pattern. All study infants, with one exception, who developed SFHRP had a one-minute Apgar score of 7 or greater. Alphaprodine is believed to affect the fetal cardioregulatory center in such a manner as to cause the SFHRP but seems to cause no increase in perinatal morbidity or mortality when given in nontoxic doses.

Alphaprodine↗
PubMed1978

Sinusoidal fetal heart rate pattern associated with alphaprodine administration.

Sinusoidal fetal heart rate patterns were observed in 42.5% of a group of 40 women who had received alphaprodine (Nisentil) for relief of labor pain. Analysis showed that the pattern appeared approximately 19 minutes following alphaprodine administration and persisted for approximately 60 minutes. In a control group of 18 patients who did not receive narcotic analgesia, and intermittent sinusoidal pattern was observed in one patient. All babies with sinusoidal heart rate during labor had 1-minute Apgar scores of 7 or greater except two in the study group. Both these neonates had low Apgar scores directly associated with complications at delivery. All 5-minute Apgar scores were 7 or greater, and there were no perinatal deaths.

Alphaprodine↗
PubMed1978

Electric shock titration: effects of meperidine, anileridine and alphaprodine.

The effects of meperidine, anileridine and a alphaprodine were studied in the squirrel monkey whose behavior was maintained under a 2.0-sec schedule of shock increment. Low doses of all three drugs had no effect, whereas higher doses decreased responding at the zero shock intensity. Slightly higher doses of meperidine and anileridine increased responding at the zero shock intensity and produced convulsions.

Alphaprodine↗
PubMed1985

Evaluation of an alphaprodine-hydroxyzine combination as a sedative agent in the treatment of the pediatric dental patient.

This investigation proposed and evaluated a submucosally administered standard dose drug combination containing .6 mgm/kgm alphaprodine hydrochloride and .3 mgm/kgm hydroxyzine hydrochloride, in conjunction with nitrous oxide, oxygen, and lidocaine with epinephrine, in the sedation and treatment of uncooperative pediatric dental patients. Observations from this study include: The technique was successful in attaining a desirable, conscious sedation level that was characterized by rapid onset, maintenance throughout treatment, and rapid reversibility with naloxone and 100% oxygen. The protective airway reflexes remained intact during the procedures. Vital signs remained fairly constant throughout the treatment. Respiratory rate was slightly depressed during the sedation, but hemoglobin oxygen saturation levels remained constant. There were no incidences of respiratory depression, hypoxia, or apnea either during or after treatment, and no emergency medical or resuscitative efforts were necessary. Twenty-four hours after the appointment, few patients complained of the experience and more than half stated that they looked forward to returning. In view of these findings, the techniques and drug combination described in this investigation appear to provide a safe and effective means for the sedation and treatment of uncooperative pediatric dental patients. It should be emphasized, however, that the dentist using these methods should have a thorough knowledge of the agents involved, the ability to monitor patients and recognize possible adverse reactions, and the capacity to respond to any emergency situations should they arise. Consequently, only practitioners who have had extensive training and experience in all forms of anesthesia, especially pediatric anesthesia, should consider the use of these agents in their practices. It should be emphasized further that the agents and techniques should be used only for conscious sedation, the light level of sedation during which the patient retains the ability present before sedation to independently maintain an airway and respond appropriately to verbal command, and not for any deeper forms of anesthesia.

Alphaprodine↗