dezocine and ciramadol

The hemodynamic and respiratory effects of dezocine and ciramadol, two agonist-antagonist analgesics, were compared with those of morphine in 30 patients undergoing diagnostic cardiac catheterization. Each subject received a single intravenous dose of dezocine (0.125 mg/kg), ciramadol (0.6 mg/kg), or morphine (0.125 mg/kg) in a double-blind fashion. Hemodynamic and respiratory parameters were measured at baseline and 5, 10, and 20 minutes after dosing. Dezocine increased the cardiac index (CI; 2.67 to 2.92 L/min/m2), stroke volume index (SVI; 43.6 to 47.6 ml/beat/m2), left ventricular stroke work index (LVSWI; 57.4 to 64.7 gm-m/m2), and pulmonary vascular resistance (PVR; 105.6 to 154.0 dynes X sec/cm5). Ciramadol increased the CI (2.78 to 3.22 L/min/m2), SVI (40.9 to 48.2 ml/beat/m2), LVSWI (51.1 to 57.9 gm-m/m2), and mean pulmonary arterial pressure (PA; 14.7 to 18.9 mm Hg). Morphine had no effect on CI, SVI, LVSWI, PA, or PVR, but it significantly lowered systolic and diastolic blood pressures. There were no appreciable changes in heart rate, left ventricular end-diastolic pressure, mean arterial pressure, or mean pulmonary capillary wedge pressure after any of the drugs. All three drugs significantly decreased systemic vascular resistance. There were no clinically significant changes in respiratory parameters. We conclude that dezocine, ciramadol, and morphine have no clinically important adverse effects on cardiac performance.

Topics: Adult; Aged; Amines; Analysis of Variance; Benzylamines; Bridged Bicyclo Compounds, Heterocyclic; Cardiac Catheterization; Cycloparaffins; Double-Blind Method; Drug Evaluation; Hemodynamics; Humans; Male; Middle Aged; Morphine; Random Allocation; Respiration; Tetrahydronaphthalenes

The effects of two novel synthetic narcotic agonist/antagonists dezocine and ciramadol were examined at the ileocecal sphincter (ICS) in the intact anesthetized cat. Changes in blood pressure were seen with higher doses of both dezocine and ciramadol. No ICS pressure changes were seen in the ICS to dezocine and an increase in ICS pressure was seen only to the highest dose of ciramadol examined (10 mg/kg). The antagonist action of the two drugs were examined against submaximal doses of the mu receptor agonist morphine sulfate, delta receptor agonist methionine enkephalin and the k-receptor agonist dynorphin. Both drugs inhibit the ICS response to morphine sulfate. No inhibition of the responses to methionine enkephalin or dynorphin were seen with dezocine and only partial inhibition of the ICS response to dynorphin was seen with ciramadol.

Topics: Analgesics; Animals; Benzylamines; Blood Pressure; Bridged Bicyclo Compounds, Heterocyclic; Cats; Cycloparaffins; Dynorphins; Enkephalin, Methionine; Ileocecal Valve; Male; Morphine; Muscle Contraction; Narcotic Antagonists; Pressure; Receptors, Opioid, mu; Tetrahydronaphthalenes

Topics: Amines; Analgesics; Benzylamines; Bridged Bicyclo Compounds, Heterocyclic; Chromatography, Gas; Chromatography, High Pressure Liquid; Cycloparaffins; Electrochemistry; Humans; Kinetics; Male; Tetrahydronaphthalenes

The effects of bolus and infusion of ciramadol, dezocine, morphine and pentazocine were examined in anesthetized dogs. Cardiopulmonary parameters, blood PCO2, PO2 and pH and plasma histamine determinations were made. Ciramadol (2 and 8 mg/kg) did not exhibit any major activity. Dezocine produced slight respiratory depression at 2 mg/kg but no cardiopulmonary effects were observed at this dose. At 8 mg/kg there were also reductions in pulmonary compliance (Cdyn) and resistance (RL), tidal volume (VT) and a marked arterial hypotension. Morphine (2 mg/kg) elicited significant effects on all parameters examined: marked bronchoconstriction, increased arterial PCO2 and pH and corresponding decrease in PO2, slight increase in heart rate and dramatic arterial hypotension. Morphine was the only agent studied to elevate plasma histamine. Histamine (0.015 mg/kg) mimicked the cardiopulmonary actions of morphine but was virtually devoid of effect on blood gases and pH. Pentazocine (8 mg/kg) did not produce bronchoconstriction but did increase VT and reduce respiratory frequency. It produced increases in arterial PCO2 and reductions in pH and PO2. There was a slight bradycardia and hypotension within this dose. These results demonstrate that both ciramadol and dezocine possess less potential than either morphine or pentazocine for producing bronchoconstriction, respiratory depression, hypotension and histamine release.

Topics: Analgesics, Opioid; Anesthesia; Animals; Benzylamines; Bridged Bicyclo Compounds, Heterocyclic; Bridged-Ring Compounds; Cyclohexanols; Cycloparaffins; Depression, Chemical; Dogs; Female; Gases; Heart; Histamine; Male; Morphine; Pentazocine; Respiratory System; Tetrahydronaphthalenes