丙氧氨酚与酮咯酸治疗癌痛的比较

晚期肿瘤疼痛病人３１例（男性１７例，女性１４例，年龄５０±５１４ａ），用丙氧氨酚２片，ｐｏ，ｔｉｄ，共７ｄ。相似病人３０例（男性１６例，女性１４例，年龄５１±１３ａ），用酮咯酸１０ｍｇ，ｐｏ，ｑｉｄ，共７ｄ。结果：疼痛强度（标尺法）２组均有降低；显效时间前组（丙氧氨酚）快于后组（酮咯酸）；药效维持时间后组长于前组；不良反应前组嗜睡多于后组，而胃肠道不适少于后组。     

Effects of prenalterol on central hemodynamics and myocardial metabolism in experimental propoxyphene-induced shock

The hemodynamic and cardiometabolic effects of prenalterol were evaluated in propoxyphene-induced circulatory shock in 10 pentobarbital-anesthetized pigs. Circulatory shock (i.e. a systolic arterial blood pressure below 60 mmHg (8 kPa) and/or a cardiac index of less than 2.0 1 X min-1 X m-2) was induced by intravenous propoxyphene chloride 15 mg X min-1. Circulatory shock occurred after 26 +/- 3 mg X kg-1 of propoxyphene. During continuous infusion of propoxyphene, consecutive doses of prenalterol 0.5, 1.0, 2.0 and 4.0 mg i.v. were injected with an interval between increments of 8 min. The maximum effect of prenalterol was seen following the 2 mg dose. Increases were observed in mean arterial blood pressure, cardiac index, stroke volume index, left ventricular stroke work index, right ventricular stroke work index, maximum rate of rise of ventricular pressure, and total body oxygen consumption. Decreases were observed in pulmonary artery occlusion pressure, mean right atrial pressure and systemic vascular resistance, whereas heart rate and pulmonary vascular resistance remained unchanged. The cardiometabolic parameters: coronary sinus flow, coronary vascular resistance, myocardial oxygen consumption and extraction, remained low. Due to profound vasodilation, normal perfusion pressures were not reestablished. In conclusion, prenalterol improved cardiac performance by a significant positive inotropic action. However, pure inotropic stimulation was not sufficient to counteract the circulatory shock state during severe propoxyphene intoxication.     

The Effects of Naloxone on Central Hemodynamics and Myocardial Metabolism in Experimental Propoxyphene-Induced Circulatory Shock

The courses of the hemodynamic and cardiometabolic effects of naloxone were evaluated in propoxyphene-induced shock in eight pentobarbital-anesthetized pigs. Circulatory shock was induced by an infusion of propoxyphene chloride 15 mg . min-1 i.v. At shock, i.e. MAP less than 60 mmHg and/or CI less than 2.0 l . min-1 . m-2, naloxone was administered at 0.75, 1.5 and 3.0 mg . kg-1 with an interval between increments of 8 min. The propoxyphene infusion of 15 mg . min-1 was continued throughout the study. Following the injection of naloxone 0.75 mg . kg-1, increases were observed (% of baseline value) in MAP (41%), i.e. deficit to baseline 59%, HR (66%), CI (67%) and SVI (108%), whereas MPAP and MPAOP were unchanged. dP/dt increased (34%). In the coronary circulation naloxone initiated the following changes: CSF increased (69%) as did MVO2 (48%) with unchanged MO2-extraction, but CVR decreased further (36%). The maximum effects of naloxone were registered 2-3 min after 0.75 mg . kg-1. Following 1.5 and 3.0 mg . kg-1, no changes in hemodynamics were observed other than those caused by progressing propoxyphene intoxication.     

A controlled clinical comparison of the analgesic efficacy of ethoheptazine,propoxyphene and placebo

Summary In a double-blind crossover study performed at Wood Veterans Administration Center and Milwaukee County General Hospital, the efficacy of ethoheptazine (Zactane®) as an analgesic agent was compared to dextropropoxyphene (65 mg) and placebo. Single oral doses of 150 mg ethoheptazine citrate were administered to 76 patients with chronic pain of various etiologies. The analgesia score obtained for 150 mg ethoheptazine was not significantly different from that obtained for 65 mg dextropropxyphene HCl. Both active medications demonstrated significant analgesic activity compared to placebo. Side effects were minor and did not interfere with the course of therapy.     

丙氧氨酚身体依赖性潜力的实验研究

采用小鼠自然戒断和催促实验评价丙氧氨酚的身体依赖性潜力。丙氧氨酚ｉｇ３００—６００ｍｇ·ｋｇ－１·ｄ－１连续３０ｄ，或ｉｇ总量为３．２７ｇ·ｋｇ－１的丙氧氨酚，ｉｐ环丙羟丙吗啡（Ｍ５０５０）３ｍｇ·ｋｇ－１催促，体重明显下降。丙氧氨酚２．０－３．０ｇ·ｋｇ－１·ｄ－１连续ｉｇ６ｄ后，ｉｐＭ５０５０３ｍｇ·ｋｇ－１催促，大鼠体重明显下降并出现了与吗啡相似的戒断症状。当大鼠吗啡掺食５ｄ产生身体依赖之后，用丙氧氨酚０８－１．６ｇ·ｋｇ－１·ｄ－１ｉｇ替代，可减轻其戒断后的体重下降。恒河猴丙氧氨酚６０－９０ｍｇ·ｋｇ－１·ｄ－１８ｗｋ后，ｓｃＭ５０５０１ｍｇ·ｋｇ－１催促或ｉｇ６０－９０ｍｇ·ｋｇ－１·ｄ－１１１ｗｋ后断然停药，恒河猴出现明显戒断症状。上述实验说明丙氧氨酚具有一定的身体依赖性潜力。     

The Effects of Dopamine on Central Hemodynamics and Myocardial Metabolism in Experimental Propoxyphene-Induced Shock

The hemodynamic and cardiometabolic effects of dopamine were evaluated in propoxyphene-induced circulatory shock in eight pentobarbital anesthetized pigs. Circulatory shock was induced by an infusion of propoxyphene chloride 15 mg . min-1 i.v. At shock, i.e. CI less than or equal to 2.0 l . min-1 . m-2 and/or MAP less than or equal to 60 mmHg, dopamine was infused at 10, 20, 40, 80 and 160 micrograms . kg-1 . min-1 with an interval between increments of 8 min. After 30 min at 160 micrograms . kg-1 . min-1, the infusion rate was reversibly decreased. The propoxyphene infusion of 15 mg . min-1 was continued throughout the study. Dopamine improved the circulation in seven animals; one animal died in refractory shock during dopamine infusion. Dopamine infusion at shock level resulted in an increase of the following variables (% of baseline value): MAP (69%), HR (109%), CI (138%) and SVI (129%). Normalisation was seen in MRAP (120%) and in MPAOP (100%). A profound decrease in systemic vascular resistance was unchanged. Increases were seen in left and right ventricular stroke work index, to 88% and 176% of baseline, respectively. Left ventricular dP/dt increased (170%). In the coronary circulation myocardial blood flow increased (133%) as did myocardial oxygen consumption (65%) concomitant with a decrease in myocardial oxygen uptake (41%), but coronary vascular resistance progressively decreased (38%). The myocardial propoxyphene extraction changed from +54% to -86% during peak dopamine infusion. In conclusion, dopamine reversed cardiac failure in propoxyphene overdose by a marked positive inotropic stimulation restoring contractility. A marked positive chronotropic stimulation maintained a sufficient cardiac index and a normal blood pressure in spite of a profound vasodilatation which was unresponsive to dopamine.     

Propoxyphene use by community-dwelling and institutionalized elderly Medicare beneficiaries

OBJECTIVES: To provide the first comparable national prevalence estimates on use of propoxyphene, a potentially inappropriate drug, by elderly Medicare beneficiaries living in the community and institutions and to determine whether institutionalized beneficiaries are at a greater risk for receiving propoxyphene than community-dwelling beneficiaries. DESIGN: Cross-sectional study. SETTING: U.S. representative sample of elderly using Medicare database. PARTICIPANTS: Nationally representative sample of community-dwelling (n = 9,851, weighted n = 32.5 million) and institutionalized (n = 1,099, weighted n = 2.3 million) Medicare beneficiaries aged 65 and older. MEASUREMENTS: National estimates on prevalence of propoxyphene use and the odds of receiving propoxyphene were the two main outcome measures. RESULTS: Annual prevalence of propoxyphene use in 1998 was 6.8% by all community-dwelling elderly beneficiaries and 15.5% by institutionalized elderly beneficiaries. Beneficiaries in long-term care facilities had almost 40% higher odds of receiving propoxyphene (odds ratio = 1.38, 95% confidence interval = 1.1-1.8) than beneficiaries in the community even after controlling for other factors in a logistic regression. Other risk factors include female, rural residence, poor health, and history of osteoporosis or hip fracture. Beneficiaries residing in regions in the midwest and south were more than twice as likely to receive propoxyphene as those in the mid-Atlantic area. CONCLUSION: These results show that propoxyphene use by U.S. community-dwelling seniors is high but is much higher in the institutionalized population. These findings suggest that prescribing for older adults with pain could be improved, especially for vulnerable long-term care residents.