药品信息:
英文药名：Lipuro（propofoL）
中文药名：丙泊酚注射液
药品介绍
丙泊酚(propofol), 其化学名为2,6-双异丙基苯酚，是目前临床上普遍用于麻醉诱导、麻醉维持、ICU危重病人镇静的一种新型快速、短效静脉麻醉药。它具有麻醉诱导起效快、苏醒迅速且功能恢复完善，术后恶心呕吐发生率低等优点。
药理毒理
该品为烷基酚类的短效静脉麻醉药，通过激活GABA受体—氯离子复合物，发挥镇静催眠作用。临床剂量时，丙泊酚增加氯离子传导，大剂量时使GABA受体脱敏感，从而抑制中枢神经系统，产生镇静、催眠效应，其麻醉效价是硫喷妥钠的1.8倍。起效快，作用时间短，以 2.5mg/kg静脉注射时，起效时间为30-60秒，维持时间约10分钟左右，苏醒迅速。能抑制咽喉反射，有利于插管，很少发生喉痉挛。对循环系统有抑制作用，该品作全麻诱导时，可引起血压下降，心肌血液灌注及氧耗量下降，外周血管阻力降低，心率无明显变化。丙泊酚可抑制二氧化碳的通气反应，表现为潮气量减少，清醒状态时可使呼吸频率增加，静脉注射常发生呼吸暂停，对支气管平滑肌无明显影响。丙泊酚能降低颅内压及眼压，减少脑耗氧量和脑血流量，镇痛作用很微弱。与其他中枢神经抑制药并用时有协同作用。应用丙泊酚可使血浆皮质激素浓度下降，但肾上腺皮质对外源性皮质激素反应正常。丙泊酚诱导麻醉时产生不自主的肌肉运动、抽搐，浅麻时更为明显。
【药代动力学】
该品是一种起效迅速（约50秒）、短效的全身麻醉药，通常是在麻醉中迅速复苏。像所有全身麻醉一样，对该品的作用机理了解较少。 该品一次冲击剂量后或输注终止后，可用三室开放模型来描述。首相具有迅速分布（半衰期2～4分钟）及迅速消除（半衰期30～60分钟）的特点。丙泊酚分布广泛，并迅速从机体消除（总体消除率1.5～2升/分钟）。
主要通过肝脏代谢，形成丙泊酚和相应的无活性的醌醇结合物，该结合物从尿中排泄。当用丙泊酚维持麻醉时，血药浓度逐渐接近已知给药速率稳态值。当丙泊酚的输注速率在推荐范围内，其药物动力学是线性的。
适 应 症
适用于麻醉诱导和静脉全身麻醉的维持，也可用于加强监护病人接受机械通气时的镇静，及无痛人工流产手术等。
用法用量
使用丙泊酚通常需要配合使用止痛药。丙泊酚可辅助用于脊髓和硬膜外麻醉。并与常用的术前用药，神经肌肉阻断药，吸入麻醉药和止痛药配合使用。
作为全身麻醉以辅助区域麻醉技术，所需的剂量较低。
麻醉给药：建议应在给药时[一般健康成年人每10秒约给药4ml(40mg）] 调节剂量，观察病人反应直至临床体征表明麻醉起效。大多数年龄小于55岁的成年病人，大约需要2.0～2.5毫克/公斤的丙泊酚；超过该年龄需要量一般将减少；ASAⅢ级和Ⅳ级病人的给药速率应更低，每10秒约2ml(20mg）。
麻醉维持：通过持续输注或重复单次注射给予丙泊酚都能够较好的达到维持麻醉所需要的浓度。持续输注所需的给药速率在个体之间有明显的不同，通常4～12毫克/公斤/小时的速率范围能保持令人满意的麻醉。用重复单次注射给药，应根据临床需要，每次给予2.5ml(25mg）至 5.0ml(50mg）的量。 ICU镇静：当作为对正在强化监护而接受人工通气病人的镇静药物使用时，建议持续输注丙泊酚。输注速率应根据所需要的镇静深度进行调节，通常 0.3～0.4毫克/公斤/小时的输注速率范围，应能获得令人满意的镇静效果。
人工流产手术：
术前以2.0mg/kg剂量实行麻醉诱导，术中若因疼痛病人有肢体动时，以0.5mg/kg剂量追加，应能获得满意的效果。
给药方式：
未稀释的丙泊酚注射液能直接用于输注。当使用未稀释的丙泊酚注射液直接输注时，建议使用微量泵或输液泵，以便控制输注速率。丙泊酚注射液也可以稀释后使用，但只能用5%葡萄糖注射液稀释，存放于 PVC输液袋或输液瓶中。稀释度不超过1∶5(2mg/ml）。用于麻醉诱导部分的丙泊酚注射液，可以以大于20∶1的比例与0.5%或1%的利多卡因注射液混合使用。稀释液应无菌制备，给药前配制。该稀释液在6小时内是稳定的。
不良反应
全身副作用 麻醉诱导通常是平稳的，极少出现兴奋。在麻醉诱导期间，由于剂量、使用的术前用药和其他药物，可能会发生低血压和短暂性呼吸暂停。可采用静脉输液和降低维持麻醉期间丙泊酚输注的速率来纠正低血压。在麻醉诱导、维持、复苏期间，其他负作用很少见。在复苏期间，只有少部分病人出现恶心、呕吐和头疼。惊厥和角弓长的癫痫样运动、肺部水肿和手术后发热偶有出现。当于其他麻醉药物合用时，可能出现性欲抑制解除。 局部副作用 在丙泊酚麻醉诱导期可能出现局部疼痛，可通过和用利多卡因或通过使用前臂或肘前窝较粗的静脉来减轻疼痛。血栓形成和静脉炎罕见。事故性临床外渗和动物实验表明丙泊酚的组织反应极小，给动物动脉内注射，不诱导组织反应。
禁忌症
对已知丙泊酚或其中的乳化剂成分过敏者禁用。
English drug name: Lipuro (propofoL)
Chinese drug name: Propofol Injection
Manufacturer: Germany BRAUN
Drug Introduction
Propofol (propofol), whose chemical name is 2,6-bis-isopropyl-phenol, is currently widely used in clinical anesthesia, anesthesia was maintained, ICU sedation in critically ill patients a new type of fast, short-acting intravenous anesthetic. It has a rapid onset of anesthesia, recovery quickly and improve functional recovery, low incidence of postoperative nausea and vomiting, etc..
Pharmacology and Toxicology
The product is a short-acting intravenous anesthetic alkylphenols by activating GABA receptors - sedative and hypnotic effects of chloride complexes play. When the clinical dose, the increase of chloride ion propofol conduction, so that large doses of GABA receptor desensitization, thereby suppressing the central nervous system, resulting in sedation, hypnotic effect, thiopental anesthetic potency 1.8 times. Rapid onset, short duration of action to 2.5mg / kg intravenous injection, the onset time of 30-60 seconds duration of about 10 minutes or so, wake up quickly. Can inhibit the throat reflection conducive intubation, laryngospasm rarely occurs. Inhibition of the circulatory system, when the goods for induction of anesthesia, can cause decreased blood pressure, decreased myocardial blood perfusion and oxygen consumption, reduce peripheral vascular resistance, heart rate did not change significantly. Propofol inhibits the ventilatory response to carbon dioxide, performance reduced tidal volume, respiratory frequency during wakefulness can increase intravenous apnea often occurs, no significant effect on bronchial smooth muscle. Propofol can reduce intracranial pressure and intraocular pressure, reduction of cerebral blood flow and cerebral oxygen consumption, the analgesic effect is very weak. And there is a synergistic effect when used with other CNS depressants. Propofol can decrease plasma concentrations of corticosteroids, but adrenocortical response to exogenous corticosteroids normal. Propofol induction of anesthesia produce involuntary muscle movements, convulsions, more obvious superficial anesthesia.
Pharmacokinetics]
This product is a rapid onset of action (approximately 50 seconds), short-acting general anesthetic, usually rapid recovery in anesthesia. Like all general anesthesia, as the poorly understood mechanism of action items. After the goods after the first dose or infusion termination shock, can be described in three-compartment open model. Prime with a rapid distribution (half-life of 2 to 4 minutes), and rapid elimination (half-life of 30 to 60 minutes) characteristics. Propofol is widely distributed, and rapid elimination (total elimination rate of 1.5 to 2 liters / min) from the body.
Mainly metabolized by the liver, the formation of propofol and the corresponding non-active quinone alcohol conjugates, the conjugates excreted in the urine. When anesthesia was maintained with propofol plasma concentration gradually approaching a known dose rate steady-state value. When propofol infusion rates within the recommended range, its pharmacokinetics are linear.
Indications
Suitable for induction and maintenance of general anesthesia intravenous anesthesia, sedation can also be used to strengthen the monitoring of patients receiving mechanical ventilation, and induced abortion surgery.
Dosage
Usually requires the use of propofol in conjunction with painkillers. Propofol can assist for spinal and epidural anesthesia. And with the usual premedication, neuromuscular blocking drugs, inhalation anesthetics and analgesics used in conjunction.
As a general anesthesia to assist regional anesthesia techniques, the lower the required dose.
Administration of anesthesia: proposals should be administered at the time of [the general administration of healthy adults about every 10 seconds 4ml (40mg)] to adjust the dose response of the patient until the clinical signs show the onset of anesthesia. Most adult patients younger than 55 years of age, about 2.0 to 2.5 mg / kg of propofol; over the age requirement will generally decrease; ASAⅢ Ⅳ grade level and the patient's dose rate should be lower, about every 10 seconds 2ml (20mg).
Anesthesia was maintained: are able to better achieve the desired concentration of anesthesia was maintained by continuous infusion or repeated bolus administered propofol. Desired continuous infusion dose rate between individuals are quite different, usually from 4 to 12 mg / kg / hr to maintain a satisfactory range of anesthesia. Repeat injection with a single dose, according to clinical need be, per dose 2.5ml (25mg) to 5.0ml (50mg) of the amount. ICU sedation: When using as being enhanced monitoring of patients underwent artificial ventilation sedative drugs, we recommend continuous infusion of propofol. Infusion rate should be adjusted according to the desired depth of sedation is usually 0.3 to 0.4 mg / kg / hr infusion rate range, should be able to obtain satisfactory sedation.
Abortion:
Preoperative to 2.0mg / kg dose induction of anesthesia practice, surgery patients with limb Ruoyin pain when moving to 0.5mg / kg dose added, should be able to obtain satisfactory results.
Administration:
Undiluted propofol injection can be directly used for infusion. When using undiluted direct injection of propofol infusion, we recommend using micro-pump or infusion pump to control the infusion rate. Propofol injection can also be diluted after use, but only with a 5% dextrose injection diluted, stored in PVC infusion bag or infusion bottle. Dilution of not more than 1:5 (2mg / ml). Propofol injection parts for induction of anesthesia, can be mixed in a ratio of greater than 20:1 with 0.5% or 1% lidocaine injection use. A sterile diluent to be prepared, formulated prior to administration. The dilutions are stable within 6 hours.
Adverse reactions
Anesthesia was induced systemic side effects are usually smooth, very rare excitement. During induction of anesthesia, due to dose, premedication and other drug use, may be hypotension and transient apnea occur. Can be used during intravenous infusion and reduce maintenance of anesthesia with propofol infusion rate to correct hypotension. Anesthesia induction, maintenance, recovery period, other negative effects are very rare. During recovery, only a small number of patients experience nausea, vomiting, and headache. Convulsions and epileptic long horn bow movement, fever, pulmonary edema and occasionally after surgery. When combined with other narcotic drugs, sexual disinhibition may occur. Local side effects may occur localized pain in propofol induction of anesthesia, and the use of lidocaine or by using the forearm or elbow fossa thick vein to relieve pain. Thrombosis and phlebitis rare. Accidental clinical extravasation and animal experiments show that tissue reaction propofol is extremely small, given the animal arterial injection, do not induce tissue reaction.
Contraindications
Known propofol or one emulsifier ingredient allergy. |
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