英文药名：Palux inj(alprostadil) 中文药名：前列地尔注射剂 生产厂家：大正制药 治疗类别名称 前列腺素E1製剤 商標名 Palux inj 一般名 アルプロスタジル（JAN） alprostadil（JAN, INN） 化学名 7-{(1R, 2R, 3R)-3-Hydroxy-2-[(1E, 3S)-3-hydroxyoct-1-en-1-yl]-5-oxocyclopentyl}heptanoic acid 構造式 分子式 C20H34O5 分子量 354.48 性状 它是一种结晶性粉末或白色结晶。它是易溶于四氢呋喃或乙醇（99.5），微溶于乙腈中，并在水中几乎不溶。 熔点 114〜118℃ 适应症为 1．治疗慢性动脉闭塞症(血栓闭塞性脉管炎、闭塞性动脉硬化症等)引起的四肢溃疡及微小血管循环障碍引起的四肢静息疼痛，改善心脑血管微循环障碍。 2．脏器移植术后抗栓治疗，用以抑制移植后血管内的血栓形成。 3．动脉导管依赖性先天性心脏病，用以缓解低氧血症，保持导管血流以等待时机手术治 4．用于慢性肝炎的辅助治疗。 用法用量 成人一日一次，1-2ml（前列地尔5-10μg）+10ml生理盐水（或5％的葡萄糖）缓慢静注，或直接入小壶缓慢静脉滴注。 不良反应 1．休克：偶见休克。要注意观察，发现异常现象时，立刻停药，采取适当的措施。 2．注射部位：有时出现血管疼、血管炎、发红，偶见发硬，瘙痒等。 3．循环系统：有时出现加重心衰，肺水肿，胸部发紧感，血压下降等症状，一旦出现立即停药。另外，偶见脸面潮红、心悸。 4．消化系统：有时出现腹泻、腹胀、不愉快感，偶见腹痛、食欲不振、呕吐、便秘、转氨酶升高等。 5．精神和神经系统：有时头晕、头痛、发热、疲劳感，偶见发麻。 6．血液系统：偶见嗜酸细胞增多、白细胞减少。 7．其他：偶见视力下降、口腔肿胀感、脱发、四肢疼痛、浮肿、荨麻疹。 禁忌 以下患者禁用： 1．严重心衰(心功能不全)患者。 2．妊娠或可能妊娠的妇女。 3．既往对本制剂有过敏史的患者。 注意事项 包装规格 5μg： 1毫升×1管，1毫升×5管，1毫升×10管 10μg：2毫升×1管，2毫升×5管，2毫升×10管 制造及销售 大正制药有限责任公司 http://www.info.pmda.go.jp/go/pack/2190406A1055_1_13/  http://medical.taishotoyama.co.jp/data/tenp/htm/px/tenpu.htm Therapeutic category name Prostaglandin E1 preparation Brand Name Palux Note disposable 10μg [Kit formulation] Composition Capacity in one syringe 2mL Component-content Sun stations alprostadil 10μg Additive-content Purified soybean oil 200mg Highly purified egg yolk lecithin 36mg Oleic acid 4.8mg Concentrated glycerin 44.2mg Sodium hydroxide qs Contraindication There is a severe heart failure patients [reported that enhancement of heart failure appear. ] Hemorrhage (intracranial hemorrhage, gastrointestinal bleeding, hemoptysis, etc.) is likely to be conducive to patient [bleeding to have. ] Women [that might have pregnant women or pregnant reference section of "pregnant women, maternal, administration to lactating women, etc.". ] Patients with a history of hypersensitivity to components of this drug. Efficacy or effect ○ chronic arterial occlusive disease (Buerger's disease, arteriosclerosis obliterans) improvement of limb ulcers and pain at rest in Improvement of skin ulcers in ○ following disease Progressive systemic sclerosis Systemic lupus erythematosus Improvement of skin ulcers in ○ diabetes ○ improvement of subjective symptoms associated with peripheral blood circulation disorders in vibration disease as well as the recovery of the peripheral circulation and nervous-motor dysfunction Normal, adult once a day 1~2mL IV the (5~10μg as alprostadil) slowly by mixing directly or infusion, or intravenous infusion. In addition, it will be adjusted according to the symptoms. Patency of the ductus arteriosus in ○ ductus arteriosus-dependent congenital heart disease The mixed infusion refers continuous intravenous as starting alprostadil 5ng / kg / min, thereafter it is an effective minimum amount is increased or decreased as appropriate according to the symptoms. That it does not mix use with other drugs other than transfusion this drug. However the incorporation of a plasma expander (dextran, gelatin formulation, etc.) should be avoided. Incidentally, in the case of continuous administration, in order to prevent agglomeration in the line, it can be administered alone always line. Careful administration Sometimes appear enhancement tendency of heart failure patients [heart failure. ] Glaucoma, there is a possibility that enhances the patient [intraocular pressure with eye hypertension. ] To a patient in the patient [history with complications and a history of stomach ulcer there is a risk of stomach bleeding. ] Which may exacerbate the patient [interstitial pneumonia of interstitial pneumonia. ] Patients with renal failure [sometimes exacerbate renal failure. ] Patients with bleeding tendency [is likely to contribute to bleeding. ] Anticoagulant (warfarin potassium, etc.) or platelet function to inhibit drug (aspirin, ticlopidine hydrochloride, cilostazol, etc.), see the section of the patient during the administration thrombolytic agent (urokinase, etc.) ["interaction". ] Clinically significant adverse reactions Shock, anaphylactoid symptoms Both incidence unknown Shock, because it may appear anaphylaxis-like symptoms, carefully monitored, urticaria, laryngeal edema, dyspnea, cyanosis, administration should be discontinued if the drop in blood pressure, etc. are observed, to take appropriate measures . Loss of consciousness Frequency unknown Since there is that transient loss of consciousness appears due to decreased blood pressure, carefully observed, administration should be discontinued if any abnormality is observed, be carried out and appropriate measures should be taken. Heart failure, pulmonary edema Both incidence unknown Heart failure (including enhanced), pulmonary edema, because it may pleural effusion appears, palpitations, chest tightness, stop the administration breathing difficulty, if the edema, etc. are observed, is carried out ("important appropriate action see the section of basic care "). Interstitial pneumonia Frequency unknown Since the interstitial (including exacerbations) pneumonia is that it appears, fever, cough, breathing difficulty, if the chest X-ray abnormality was observed to discontinue administration, and proper administration of corticosteroids performing the action. Myocardial infarction Frequency unknown Since it may MI appears carefully monitored, chest pain, chest tightness, discontinue administration if ECG abnormalities such as are observed, carrying out the appropriate action. Cerebral hemorrhage, gastrointestinal bleeding Both incidence unknown Cerebral hemorrhage, because it may appear gastrointestinal bleeding, carefully monitored, and should be discontinued administration if any abnormality is observed. Agranulocytosis, leukopenia, thrombocytopenia Both incidence unknown Agranulocytosis, leukopenia, because it may thrombocytopenia appears, carefully observed, administration should be discontinued if any abnormality is observed, to take appropriate measures. Liver dysfunction, jaundice Both incidence unknown Since there is that AST (GOT) · ALT liver dysfunction or jaundice associated with the rise of such (GPT) · Al-P · γ-GTP appears, carefully monitored, and the administration if any abnormalities are observed such as discontinuation, doing the appropriate action. Apneic attack 12.23% When administered to newborns, since it may apnea may occur, sufficiently carried out and observed. Note that when expressed, weight loss, slowing the infusion rate, and to take appropriate action such as discontinuation of administration. Pharmacology Vasodilating action 8) to 10) Blood flow increasing action, the results were compared with the PGE1-CD vasodilation action to index the blood pressure lowering effects are as follows. In normal rats and streptozotocin-induced diabetic rats, showed a strong blood flow increasing effect than PGE1-CD, the effect was more pronounced in diabetic rats. In the dog, it showed a strong blood flow increasing effect than PGE1-CD at a dose that does not show significant blood pressure lowering effect. In streptozotocin-induced diabetic rats and spontaneously hypertensive rats, it showed a significant strong blood pressure lowering effect than PGE1-CD. This became more pronounced with the progress or chronic disease states. For rat neonatal ductus arteriosus, it showed a persistent ductus arteriosus extended action stronger than PGE1-CD. Platelet aggregation inhibiting action 11) to 13) For the ADP-induced thrombus formation in hamster cheek pouch microvessels and showed strong thrombus formation inhibitory effect and persistence than PGE1 in either the normal or damaged blood vessels. In peripheral arterial occlusive disease model by lauric acid in rats showed suppression of strong pathology progression than PGE1-CD. In rat ex vivo system, and showed a strong platelet aggregation inhibitory effect than PGE1-CD increased the cyclic-AMP amount. Mechanism of action 1), 2), 11) While the active ingredient of the present agent is alprostadil (PGE1), by the fat particles and the drug carrier, the following characteristics were observed. After damage the hamster cheek pouch microvessels, who upon administration of this drug has showed significant and sustained thrombosis inhibitory effect than when administered prior to injury. Mesenteric artery of fat particles as a drug carrier is normal and diabetic rats, attached to the chest lesions aortic endothelial cells of capillary endothelial cells and spontaneously hypertensive rats, and endocytosis that has been, it is electron microscopy observed It has been. This drug labeled with 3H showed high radioactivity distribution in diseased blood vessels in spontaneously hypertensive rats as compared to 3H-PGE1. In rats, plasma PGE1 unchanged concentration after intravenous administration of this drug labeled with 3H was significantly higher as compared to when 3H-PGE1-CD administration. The physicochemical knowledge of active ingredient Generic name Alprostadil (JAN) alprostadil (JAN, INN) Chemical name 7 - {(1R, 2R, 3R) -3-Hydroxy-2 - [(1E, 3S) -3-hydroxyoct-1-en-1-yl] -5-oxocyclopentyl} heptanoic acid Molecular formula C20H34O5 Molecular weight 354.48 Behavior It is a white crystal or crystalline powder. Ethanol (99.5) or freely soluble in tetrahydrofuran, and slightly soluble in acetonitrile, and practically insoluble in water. Melting point 114~118 ℃