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Pharmacological characteristics of sufentanil and Application-controlled analgesia_0
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Pharmacological characteristics of sufentanil and Application-controlled analgesia
[Keywords:] sufentanil; pharmacology; controlled analgesia
Sufentanil is a phenyl piperidine is N-4-substituted fentanyl derivatives, their chemical and pharmacological effect was first reported in 1976, is currently in the analgesic effects of opiates in the strongest, has been widely used in anesthesia induction, anesthesia was maintained, analgesia, postoperative analgesia and sedation, etc., the paper on its pharmacological characteristics and the application of advances in analgesia were reviewed.
Pharmacological characteristics of 1
1.1 The pharmacokinetics and plasma protein binding rate, 92.5%, and @ l acid glycoprotein with a rate of 84%, plasma free fraction and a @ l acid glycoprotein, albumin, a negative correlation. Lipophilic about is 2 times of fentanyl, can rapidly penetrate the biofilm, in the brain to achieve effective blood concentration, it produces faster clinical response than fentanyl. Meuldermans [1] reported that rats with intravenous sufentanil 2.5g / kg after 2min in the brain, lung, liver, kidney, heart and muscle to reach maximum concentration, 8 ~ 15min in the spleen, gastrointestinal tract, thymus, testis, 30min in the pancreas, fat, up to maximum concentration. TCI 4ng / ml sufentanil or 6ng/ml clinical study found that the pharmacokinetics can be described as a three compartmental models [2], the central compartment capacity is 5.4L, steady-state volume of distribution (Vdss222.6L, metabolic clearance rate (CI0.84L / min, elimination half-life (t1/2y389min. sufentanil and fentanyl and opioid receptor affinity stronger than that, it is not only the analgesic potency large, the duration of action is also longer, about 2 to 6 of fentanyl times, and morphine close. a small volume of distribution (1.7L/kg, short elimination half-life (160min and the clearance rate (12.7ml/kg min, so no significant accumulation in th
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