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MANNITOL(甘露醇25% IV溶液)

2013-05-01 23:17:31  作者:新特药房  来源:互联网  浏览次数:199  文字大小:【】【】【
简介: 部分中文甘露醇处方资料(仅供参考)甘露醇Mannitol 中文别名:甘露醇、甘露糖醇、六己醇、水蜜醇 英文别名:Isotol、Manicol、Manita、Manna Sugar、Mannistol、Mannite、Osmitrol、Osmofundin、Osm ...

 部分中文甘露醇处方资料(仅供参考)
甘露醇Mannitol 
中文别名:甘露醇、甘露糖醇、六己醇、水蜜醇
英文别名:Isotol、Manicol、Manita、Manna Sugar、Mannistol、Mannite、Osmitrol、Osmofundin、Osmosal、Resectisol、V-Mannitol
药品类别:脱水药 
药理药动
药效学
甘露醇为单糖,在体内不被代谢,经肾小球滤过后在肾小管内甚少被重吸收,起到渗透利尿作用。
(1) 组织脱水作用。提高血浆胶体通透压,导致组织内(包括眼、脑、脑脊液等)水分进入血管内,从而减轻组织水肿,降低眼内压、颅内压和脑脊液容量及其压力。1g甘露醇可产生渗透浓度为5.5mOsm,注射100g甘露醇可使2000ml细胞内水转移至细胞外, 尿钠排泄50g。
(2) 利尿作用。甘露醇的利尿作用机制分两个方面。
①甘露醇增加血容量,并促进前列腺素I2分泌, 从而扩张肾血管,增加肾血流量包括肾髓质血流量。肾小球入球小动脉扩张, 肾小球毛细血管压升高, 皮质肾小球滤过率升高。
②本药自肾小球滤过后极少(<10%)由肾小管重吸收,故可提高肾小管内液渗透浓度,减少肾小管对水及Na+、CI-、K+、Ca2+、Mg2+和其他溶质的重吸收。
过去认为本药主要作用于近端小管,但经穿刺动物实验发现,应用大剂量甘露醇后,通过近端小管的水和Na+仅分别增多10~20%和4~5%;而到达远端小管的水和Na+则分别增加40%和25%。揭示亨氏袢重吸收水和Na+减少在甘露醇利尿作用中占重要地位。此可能是由于肾髓质血流量增加,髓质内尿素和Na+流失增多,从而破坏了髓质渗透压梯度差。
由于输注甘露醇后肾小管液流量增加,当某些药物毒物中毒时,这些物质在肾小管内浓度下降,对肾脏毒性减小,而且经肾脏排泄加快。
药动学
甘露醇口服吸收很少。静脉注射后迅速进入细胞外液而不进入细胞内。利尿作用于静注后0.5~1小时出现, 维持3小时。降低眼内压和颅内压作用于静注后15分钟内出现, 达峰时间为30~60分钟, 维持3~8小时。本药可由肝脏生成糖原,但由于静脉注射后迅速经肾脏排泄, 故一般情况下经肝脏代谢的量很少。本药半衰期为100分钟, 当存在急性肾功能衰竭时可延长至6小时。肾功能正常时,静脉注射甘露醇100g, 3小时内80%经肾脏排出。
适 应 症
(1) 组织脱水药。用于治疗各种原因引起的脑水肿,降低颅内压,防止脑疝。
(2) 降低眼内压。可有效降低眼内压,应用于其他降眼内压药无效时或眼内手术前准备。
(3) 渗透性利尿药。应用于预防各种原因起的急性肾小管球死,并用于鉴别肾前性因素或急性肾功能衰竭引起的少尿。
(4) 作为辅助性利尿措施治疗肾病综合征、肝硬化腹水,尤其是当伴有低蛋白血症时。
(5) 对某些药物逾量或药物中毒(如巴比妥类药物、锂、水杨酸盐和溴化物等),本药可促进上述物质的排泄,并防止肾毒性。
(6) 作为冲洗剂,应用于经尿道内作前列腺切除术。
(7) 术前肠道准备。
用法用量
1.成人常用量
(1)利尿。常用量为按体重 1—2g/kg,一般用 20%溶液250ml静脉滴注,并调整剂量使尿量维持在每小时 30—50ml。
(2)治疗脑水肿、颅内高压和青光眼。按体重 1.5—2g/kg,配制为 15—25%浓度于 20—60分钟内静脉滴注。每日可给3次。当病人衰弱时,剂量应减小至 0.5g/kg。
(3)鉴别肾前性少尿和肾性少尿。按体重 0.2g/kg,以 20%浓度于 3—5分钟内静脉滴注,如用药后 2~3小时以后每小时尿量仍低于30—50ml,最多再试用一次,如仍无反应则应停药。已有心功能减退或心力衰竭者慎用或不宜使用。
(4)预防急性肾小管坏死。先给予 12.5—25g,10分钟内静脉滴注,若无特殊情况,再给50g 1小时内静脉滴注,若尿量能维持在每小时50ml以上,则可继续应用 5%溶液静滴;若无效则立即停药。
(5)治疗药物、毒物中毒。50g以20%溶液静滴,调整剂量使尿量维持在每小时 100—500ml。
(6)肠道准备。术前 4—8小时,10%溶液 1000ml于 30分钟内口服完毕;
2.小儿常用量
(1)利尿。按体重 2g/kg或按体表面积60g/平方米,以 15—20%溶液 2~6小时内静脉滴注。
(2)治疗脑水肿、颅内高压和青光眼。按体重 1—2g/kg或按体表面积 30~60g/平方米,以15—20%浓度溶液于30—60分钟内静脉滴注。病人衰弱时剂量减至 0.5g/kg。
(3)鉴别肾前性少尿和肾性少尿。按体重 0.2g/kg或按体表面积 6g/平方米,以 15—25%浓度静脉滴注 3—5分钟,如用药后2—3小时尿量无明显增多,可再用 1次,如仍无反应则不再使用。
(4)治疗药物、毒物中毒。按体重 2g/kg或按体表面积60g/平方米以 5—10%溶液静脉滴注。
[制剂与规格]
甘露醇注射液(1)50ml:10g(2)100ml:20g(3)250ml:50g
静脉滴注,按1-4.5g/kg计,用20%溶液250-500ml,滴速10ml/分.不能注入过快。
不良反应
(1)水和电解质紊乱。最为常见。
①快速大量静注甘露醇可引起体内甘露醇积聚,血容量迅速大量增多,导致心力衰竭(尤其有心功能损害时),稀释性低钠血症,偶可致高钾血症。
②不适当的过度利尿导致血容量减少,加重少尿。
(2)寒战、发热。
(3)排尿困难。
(4)血栓性静脉炎。
(5)甘露醇外渗可致组织水肿、皮肤坏死。
(6)过敏引起皮疹、荨麻疹、呼吸困难、过敏性休克。
(7)头晕、视力模糊。
(8)高渗引起口渴。
(9)渗透性肾病(或称甘露醇肾病),主要见于大剂量快速静脉滴注时。其机理尚未完全阐明,可能与甘露醇引起肾小管液渗透压上升过高,导致肾小管上皮细胞损伤。病理表现为肾小管上皮细胞肿胀,空泡形成临床上出现尿量减少,甚至急性肾功能衰竭。渗透性肾病常见于老年肾血流量减少及低钠、脱水患者。
注入过快可引起头痛,视物模糊,眩晕,畏寒,注射部位疼痛.可有接触性皮炎,皮疹,急性肾衰。对于肾功能不全的病人,会造成低血钠症和结肠内氢离子浓度过高。
本品可以引起皮肤过敏和全身性荨麻疹。主要的不良反应和毒性反应是造成电解质紊乱和急性的肾功能衰竭。
注射过快时有一过性头痛、视力模糊、眩晕、畏寒等,甚至出现神志不清、抽搐。这些可能是中枢神经系统疾病本身表现,也可能由于脱水过多,诱发高渗透压症群的表现,可有硬脑膜下或蛛网膜下出血,需要作出鉴别,测血浆渗透压可有帮助。在剂量较大如8小时内超过200g时。则可出现胸闷、胸痛、心律不齐或过速、咳嗽、呼吸时有哮鸣音或肺基部出现罗音、颈静脉怒张等,这些可由于心功能不全或注射甘露醇过速、用量过多、肾排泄功能不佳,以致心脏负荷过重所引起,严重时可导致急性肺水肿。
甘露醇静脉输入还可有肌力软弱、行动不便、手脚麻木、有刺痛感或肌痉挛等,这可能因甘露醇应用后导致利尿、脱水、失钠从而引起水、电解质紊乱,若患者原来存在失水或血容不足,则症状更易出现。
在注射甘露醇的同时应纠正上述紊乱。持续大剂量应用甘露醇还可引起高渗性肾病(有称甘露醇性肾病),患者尿量减少甚至达少尿程度(每日排尿少于400ml),可出现浮肿,高渗性昏迷等症状,肾穿针活组织检查可发现肾小管上皮细胞肿胀,应即停用,给予葡萄糖注射液或葡萄糖氯化钠注射液,以降低血浆渗透压。
其急性肾衰的发生与使用大剂量甘露醇有关。使用大剂量甘露醇后,在致密斑部位造成一个异常强烈的传入刺激,导致肾单位滤过率明显下降,而发生急性肾衰。
其急性肾衰的发生与使用大剂量甘露醇有关。使用大剂量甘露醇后,在致密斑部位造成一个异常强烈的传入刺激,导致肾单位滤过率明显下降,而发生急性肾衰。
高敏反应的人注射甘露醇后可发生过敏反应,在滴注药物的3~5分钟后出现喷嚏、流鼻涕、舌肿、呼吸困难、意识丧失等,应立即停药,对症处理。
高渗甘露醇注射时可引起静脉炎,局部出现红肿及疼痛,注射处有渗漏时可引起局部皮肤坏死。
本品也可致有所谓的糖贮存肾伴有草酸钙沉淀。
禁忌症
(1)甘露醇能透过胎盘屏障。
(2)是否能经乳汁分泌尚不清楚。
(3)小儿应用本药无特殊注意事项。
(4)老年人应用本药较易出现肾损害,且随年龄增长,发生肾损害的机会增多。
(5)下列情况慎用:
①明显心肺功能损害者,因本药所致的突然血容量增多可引起充血性心力衰竭;
②高钾血症或低钠血症;
③低血容量,应用后可因利尿而加重病情,或使原来低血容量情况被暂时性扩容所掩盖;
④严重肾功能不全而排泄减少使本药在体内积聚,引起血容量明显增加,加重心脏负荷,诱发或加重心力衰竭;
⑤对甘露醇不能耐受者。
(6)下列情况禁用:
①已确诊为急性肾小管坏死的无尿患者,包括对试用甘露醇无反应者,因甘露醇积聚引起血容量增多,加重心脏负担;
②严重失水者;
③颅内活动性出血者,因扩容加重出血,但颅内手术时除外;
④急性肺水肿,或严重肺瘀血。
心功能不全,脱水少尿者慎用。对于肾功能不全的病人,会造成低血钠症和结肠内氢离子浓度过高。
药物相互作用
(1)可增加洋地黄毒性作用,与低钾血症有关。
(2)增加利尿药及碳酸酐酶抑制剂的利尿和降眼内压作用,与这些药物合并时应调整剂量。

Mannitol InjectionPronunciation.
Dosage Form: injection, solution
Mannitol Injection USP
.25%
For Intravenous Use and Urologic Irrigation
Mannitol Injection Description
Mannitol is a 6-carbon sugar alcohol and has the following structure:

C6H14O6                                                             182.17

Mannitol occurs naturally in fruits and vegetables, and is metabolically inert in humans.
Mannitol Injection, USP, 25%, an osmotic diuretic, is a sterile, nonpyrogenic solution of mannitol in Water for Injection.  It is a supersaturated solution at room temperature.
Each mL contains: Mannitol 250 mg; Water for Injection q.s. The osmolar concentration is 1372 mOsmol/L (calc.).  It contains no antimicrobial agents.  The pH of a 5% solution is between 4.5 and 7.0.
Mannitol Injection - Clinical Pharmacology
Mannitol is an osmotic diuretic.  After intravenous injection it is confined to the extracellular space, metabolized only slightly and excreted rapidly by the kidneys.  Approximately 80% of a 100 g dose appears in the urine in three hours.  Mannitol is freely filtered by the glomeruli with less than 10% tubular reabsorption.  It is not secreted by tubular cells.  It induces diuresis by elevating the osmolarity of the glomerular filtrate and thereby hinders tubular reabsorption of water.  Urinary output of water and excretion of sodium and chloride are enhanced.  Mannitol is poorly absorbed from the gastrointestinal tract.
Mannitol Injection is free of electrolytes and is used in urology as a nonhemolytic irrigant.  The amount of mannitol absorbed intravascularly during transurethral prostatic surgery is variable and depends primarily on the extent of the surgery.  Such mannitol is excreted by the kidneys and produces osmotic diuresis.
Indications and Usage for Mannitol Injection
For Intravenous Injection
Mannitol Injection, USP is indicated for the following therapeutic uses:
• The promotion of diuresis, in the prevention and/or treatment of the oliguric phase of acute renal failure before irreversible renal failure becomes established.
• The reduction of intracranial pressure and treatment of cerebral edema by reducing brain mass.
• The reduction of elevated intraocular pressure when it cannot be lowered by other means.
• The promotion of urinary excretion of toxic substances.
For Urologic Irrigation
Mannitol solution, 2.5% is indicated as an irrigation solution in transurethral prostatic resection or other transurethral surgical procedures.
Contraindications
• Well established anuria due to severe renal disease.
• Severe pulmonary congestion or frank pulmonary edema.
• Active intracranial bleeding except during craniotomy.
• Severe dehydration.
• Progressive renal damage or dysfunction after institution of mannitol therapy, including increasing oliguria and azotemia.
• Progressive heart failure or pulmonary congestion after mannitol therapy is started.
Warnings
In severe impairment of renal function a test dose should be given (see DOSAGE AND ADMINISTRATION).  A second test dose may be given if there is an inadequate response.   No more than two test doses should be attempted.
Excessive loss of water and electrolytes may lead to serious imbalances.  Serum sodium and potassium should be carefully monitored during mannitol therapy.
The diuresis after rapid infusion of mannitol may increase preexisting hemoconcentration.  With continued use of mannitol a loss of water in excess of electrolytes can cause hypernatremia.
Shift of sodium-free intracellular fluid into the extracellular compartment after mannitol infusion may lower serum sodium concentration and aggravate preexisting hyponatremia.
Closely monitor the urine output and discontinue mannitol infusion promptly if output is low.  Inadequate urine output results in accumulation of mannitol, expansion of extracellular fluid volume and could result in water intoxication or congestive heart failure.  Renal function must be closely monitored during mannitol infusion.
Mannitol solution must be used with caution in patients with significant cardiopulmonary or renal dysfunction.
Irrigating solutions used in transurethral prostatectomy have been shown to enter the systemic circulation in relatively large volumes, exert a systemic effect and may significantly alter cardiopulmonary and renal dynamics.
Precautions
General
Crystals, if present in Mannitol Injection, 25%, may be dissolved by placing the vial in a hot water bath maintained at 60° to 80°C with occasional shaking.  The resulting solution should be allowed to cool to body temperature before injection.
An administration set with a filter should be used for intravenous infusions of solutions containing 20% or more of mannitol.
NOTE: Use of any other method to heat the vial may result in its explosion.
The cardiovascular status should be carefully evaluated before mannitol is administered by rapid intravenous injection or before and during transurethral resection since expansion of extracellular fluid may lead to fulminating congestive heart failure.
By sustaining diuresis, mannitol may obscure and intensify inadequate hydration or hypovolemia.
Unless it is essential, electrolyte-free mannitol solutions should not be combined with blood.  When it is essential to give the combination, at least 20 mEq of sodium chloride should be added to each liter of mannitol solution to avoid pseudoagglutination.  The contents of opened containers should be used promptly and unused contents should be discarded.
A white flocculant mannitol precipitate may result from contact with PVC surfaces which act as nuclei for rapid rate crystallization of small crystals.  This condition has also been reported to occur when mannitol has come in contact with other plastic and rough glass surfaces.  Attempting to resolubilize the white flocculant precipitate with the aid of heat is not useful because crystallization may recur in a short period of time.
Carcinogenesis, Mutagenesis, Impairment of Fertility
In an early study of 1, 5 or 10% mannitol, given for 94 weeks in the diet of Wistar rats, a low incidence of benign thymomas occurred in females which was apparently treatment related.  A subsequent life-time study at similar dose levels in Spraque-Dawley, Fischer and Wistar rats revealed no carcinogenic effect in the thymus.
Mannitol had no mutagenic activity in a series of in vitro and in vivo test systems.
Adequate studies measuring the effects of mannitol on fertility have not been done.
Pregnancy
Pregnancy Category B–Teratogenic studies in the mouse, rat and rabbit at oral doses up to 1600 mg/kg did not reveal harm to the fetus or adverse effects on reproduction due to mannitol.  There are, however, no adequate and well-controlled studies in pregnant women.  Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.
Nursing Mothers
It is not known whether this drug is excreted in human milk.  Because many drugs are excreted in human milk, caution should be exercised when mannitol is given to a nursing mother.
Pediatric Use
Dosage requirements in children below the age of 12 years have not been established.
Adverse Reactions
Reactions are infrequent and may include:
Metabolic: fluid and electrolyte imbalance, acidosis, dehydration.
Gastrointestinal: dryness of mouth, nausea, vomiting, diarrhea.
Genitourinary: osmotic nephrosis, urinary retention.
Central Nervous System: headache, convulsions, dizziness.
Special Senses: Blurred vision, rhinitis.
Cardiovascular: pulmonary edema, edema, hypotension, hypertension, tachycardia, angina-like chest pains.
Dermatologic: skin necrosis, thrombophlebitis.
Hypersensitivity: urticaria.
Miscellaneous: thirst, arm pain, chills, fever.
Mannitol Injection Dosage and Administration
For Intravenous Injection
General Recommendations–Give Mannitol Injection only intravenously.  The total dosage, concentration and rate of administration should be governed by the nature and severity of the condition being treated, fluid requirement and urinary output.  Usual adult dosage ranges from 50 to 200 g in 24 hours but in most instances an adequate response will be achieved at a dosage of approximately 100 g in 24 hours.  The rate is usually adjusted to maintain an adequate urine flow (at least 30 to 50 mL/hr).
Test Dose–In marked oliguria or inadequate renal function a test dose of mannitol should be given.  The test dose may be approximately 0.2 g/kg (about 50 mL of a 25% solution) infused in three to five minutes to produce an adequate urine flow (at least 30 to 50 mL/hr).  If urine flow does not increase within two or three hours a second test dose may be given.  If there is an inadequate response the patient should be reevaluated.
Prevention of Acute Renal Failure (Oliguria)–When used during surgery, immediately postoperatively or following trauma, 50 to100 g of mannitol as a 5 to 25% solution maybe given.  The concentration and amount will depend upon the fluid requirements of the patient.  Following suspected or actual hemolytic transfusion reactions 20 g of mannitol may be given intravenously over a five minute period to provoke diuresis.  If diuresis does not occur the 20 g dose may be repeated.  If there is an adequate urine flow (30 to 50 mL/hr) then intravenous fluids containing not more than 50 to 75 mEq of sodium per liter should be given in sufficient volume to match the desired urine flow (100 mL/hr) until fluids can be taken orally.
Treatment of Oliguria–The usual dose for treatment of oliguria is 50 to 100 g as a 15 to 25% solution.
Reduction of Intracranial Pressure, Cerebral Edema or Intraocular Pressure–A 25% solution of mannitol is recommended since its effectiveness depends on establishing intravascular hyperosmolarity.  When used before or after surgery, a total dose of 1.5 to 2 g/kg can be given over a period of 30 to 60 minutes.  Careful evaluation must be made of the circulatory and renal reserve prior to and during use of mannitol at this relatively high dose and rapid infusion rate.  Careful attention must be paid to fluid and electrolyte balance, body weight, and total input and output before and after infusion of mannitol.  Evidence of reduced cerebral spinal fluid pressure may be observed within 15 minutes after starting infusion.
Maximal reduction of intraocular pressure occurs 30 to 60 minutes after injection.
Urinary Excretion of Toxic Substances–Mannitol in 5 to 25% solutions is used as an infusion as long as indicated if the level of urinary output remains high.  The concentration will depend upon the fluid requirement and urinary output.  Intravenous water and electrolytes must be given to replace the loss of these substances in the urine, sweat and expired air.  If benefits are not observed after 200 g of mannitol are given, discontinue it.
For Urologic Irrigation
A 2.5% solution is used.  The use of 2.5% mannitol solution minimizes the hemolytic effect of water alone, the entrance of hemolyzed blood into the circulation, and the resulting hemoglobinemia which is considered a major factor in producing serious renal complications.
INSTRUCTIONS FOR PROPER USE OF VIALS WITH FLIP-TEAR TOP SEALS
Read instructions carefully.  Use proper aseptic technique.
CAUTION: IF IT IS NECESSARY TO INTRODUCE FILTERED AIR INTO THE VIAL, THIS MUST BE DONE SLOWLY AND WITH CAUTION.  IF THE VIAL HAS BEEN WARMED, ALLOW VIAL TO COOL TO ROOM TEMPERATURE BEFORE USE.
The flip-tear top seal may be used in two ways:
METHOD A
METHOD B
Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.
How is Mannitol Injection Supplied
Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature].

---------------------------------------------------------------
产地国家: 美国
原产地英文商品名:
MANNITOL 25% 50ML/VIAL 25VIALS/BOX
原产地英文药品名:
MANNITOL
中文参考商品译名:
甘露醇25% 50毫升/瓶 25瓶/盒
中文参考药品译名:
甘露醇


该药品相关信息网址1:
http://www.drugs.com/cdi/mannitol.html
该药品相关信息网址2:
http://www.rxlist.com/mannitol_iv-drug.htm

责任编辑:admin


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