左卡尼汀口服液属口服溶液剂。可用于防治左卡尼汀缺乏,如慢性肾衰病人因血液透析所致的左卡尼汀缺乏;改善心肌缺血,抗心绞痛等。临床表现如心肌病、骨骼肌病(痛)、心律失常、高脂血症,以及低血压和透析中肌痉挛等。
英文药名: Carnitor (Levocarnitine)
中文药名: 左卡尼汀
药品名称 通用名称:左卡尼汀口服液 英文名称:Levocarnitine 成份: 左卡尼汀
药理毒理 左卡尼汀是哺乳动物能量代谢中必需的体内天然物质,其主要功能是促进脂类代谢。在缺血、缺氧时,脂酰-CoA堆积,线粒体内的长链脂酰卡尼汀也堆积,游离卡尼汀因大量消耗而降低。缺血、缺氧导致ATP水平下降,细胞膜和亚细胞膜通透性升高,堆积的脂酰CoA可致膜结构改变,膜相崩解而导致细胞死亡。另外,缺氧时以糖无氧酵解为主,脂肪酸等堆积导致酸中毒,离子紊乱,细胞自溶死亡。足够量的游离卡尼汀可以使堆积的脂酰-CoA进入线粒体内,减少其对腺嘌呤核苷酸转位酶的抑制,使氧化磷酸化得以顺利进行。左卡尼汀是肌肉细胞尤其是心肌细胞的主要能量来源,脑、肾等许多组织器官亦主要靠脂肪酸氧化供能。卡尼汀还能增加NADH细胞色素C还原酶、细胞色素C氧化酶的活性、加速ATP的产生,参与某些药物的解毒作用。对于各种组织缺氧缺血,左卡尼汀通过增加能量产生而提高组织器官的供能。 左卡尼汀其他功能有:中等长链脂肪酸的氧化作用;脂肪酸过氧化物酶的氧化作用;对结合性辅酶A和游离辅酶A二者比率的缓冲作用;从酮类物质、丙酮酸、氨基酸(包括支链氨基酸)中产生能量,去除过高辅酶A的毒性,调节血中氨浓度。 致突变试验表明:用组胺酸缺陷型鼠伤寒沙门氏菌,啤酒酵母菌和繁殖酵母菌没有发现左卡尼汀致突变。用以评价该化合物致癌作用的长期动物试验尚未进行。 生殖力毒性研究表明,对大鼠和兔子给予人的剂量的3.8倍,本品对胎儿繁殖力无损害或毒性。
药代动力学 一次口服0.5g,健康受试者血浆最大浓度为48.5μmol/L。单一口服或静脉给予左卡尼汀0.5-2g,对健康受试者,其生物半衰期为2-15小时。左卡尼汀不与血浆蛋白结合。 左卡尼汀的排泄途径取决于给药的途径,静脉注射12小时内从尿中回收大约70%,24小时内大约80%。口服给药,尿中回收10%。
适应症 用于防治左卡尼汀缺乏。如慢性肾衰病人因血透析所致的左卡尼汀缺乏;改善心肌缺血,抗心绞痛等。临床表现如心肌病、骨骼肌病(痛)、心律失常、高脂血症,以及低血压和透析中肌痉挛等。
规格 口服溶液:10ml:1g 片剂:330mg
用法用量 口服,用餐时服用。 成人每日1-3g,分1-3次服用; 儿童起始剂量每公斤体重50mg,根据需要和耐受性缓慢加大剂量,通常剂量为每公斤体重50-100mg(最大剂量一天不超过3g)。 任何疑问,请遵医嘱!
不良反应 偶有口干、胃肠道轻度不适,停药后可自行消失。
禁忌 对本品过敏者禁用。
注意事项 用胰岛素或口服降糖药物治疗的糖尿病患者,由于改善葡萄糖的利用,在服用本品时,可能引起低血糖现象,因此,这些患者在接受治疗中血糖应当保持在经常控制的数值以内。 本品含有少量乙醇,对乙醇过敏的病人慎用。
孕妇及哺乳期妇女用药 妊娠期间,只有在明显需要时才使用本剂。尚不清楚这种药是否能进入母乳,应根据该药对母亲的重要性,决定是停止哺乳还是停止用药。
药物过量 目前尚无左卡尼汀过量毒性方面的报导,口服左卡尼汀小鼠LD50为19.2g/kg,左卡尼汀可引起腹泻,过量时可进行辅助治疗,需小心护理。
Carnitor Generic Name: levocarnitine (Oral route, Intravenous route) lee-voe-KAR-ni-teen
Commonly used brand name(s): In the U.S. Carnitine Carnitor
Available Dosage Forms: Capsule Tablet Solution Wafer Powder
Therapeutic Class: Amino Acid Supplement
Uses For Carnitor Levocarnitine is used to prevent and treat a lack of carnitine. It is used to prevent and treat this condition in patients with kidney disease on dialysis. It is given to people whose body cannot properly use carnitine from their diet. Lack of carnitine can lead to liver, heart, and muscle problems. Your doctor may treat lack of carnitine by prescribing levocarnitine for you.
Carnitine comes in two forms. Levocarnitine (L-carnitine) should not be confused with the D,L-carnitine form (labeled as “vitamin B T”'). Only the L-form of carnitine is used by the body to treat serious carnitine deficiency. The D,L-form does not help the body use fat and can actually interfere with and cause a lack of levocarnitine.
Certain levocarnitine products have been specifically approved by the U.S. Food and Drug Administration for medical use and are available only with your doctor's prescription.
Once a medicine has been approved for marketing for a certain use, experience may show that it is also useful for other medical problems. Although this use is not included in product labeling, levocarnitine is used in certain patients with the following medical condition: Carnitine deficiency that results from treatment with valproic acid
Before Using Carnitor In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:
Allergies Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.
Pediatric Although there is no specific information comparing use of levocarnitine in children with use in other age groups, this dietary supplement is not expected to cause different side effects or problems in children than it does in adults.
Geriatric There is no specific information comparing use of levocarnitine in the elderly with use in other age groups; however, this medicine is not expected to cause different side effects or problems in older people than it does in younger adults.
Breast Feeding There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.
Interactions with Medicines Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.
Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines. Acenocoumarol
Interactions with Food/Tobacco/Alcohol Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.
Other Medical Problems The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:
Seizures—occur more often and are more severe in patients with a history of seizure activity Severe renal dysfunction—administration of high doses of oral levocarnitine for long periods of time may build up in the body of patients with severe kidney disease Proper Use of levocarnitine This section provides information on the proper use of a number of products that contain levocarnitine. It may not be specific to Carnitor. Please read with care.
Take levocarnitine with or just after meals. Also, if you are taking it in liquid form, drink it slowly. It will be less likely to upset your stomach if you take it this way. The liquid form may be taken alone or dissolved in drink or other liquid food.
This medicine is also less likely to cause unwanted effects when there is a constant amount in the blood. If you are taking more than one dose a day, take the doses at evenly spaced times throughout the day. Doses should be spaced at least 3 to 4 hours apart. If you need help in planning the best times to take your medicine, check with your health care professional.
Dosing The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.
The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.
Do NOT change brands or dosage forms of levocarnitine without first checking with your doctor. Different products may not work in the same way. If you refill your medicine and it looks different, check with your pharmacist.
For oral dosage form (solution): To prevent or treat carnitine deficiency: Adults and teenagers—At first, 1 gram taken once a day with food. Your doctor may change the dose if needed. Children—The dose is based on body weight and must be determined by your doctor. The usual dose at first is 50 mg per kg (22.7 mg per pound) of body weight a day, divided into smaller amounts with meals. Your doctor may change the dose if needed.
For oral dosage form (tablets): To prevent or treat carnitine deficiency: Adults and teenagers—990 milligrams taken two or three times a day with meals. Children—The dose is based on body weight and must be determined by your doctor. The usual dose at first is 50 mg per kg (22.7 mg per pound) of body weight a day, divided into smaller amounts with meals. Your doctor may change the dose if needed.
For injection dosage form: To treat carnitine deficiency: Adults and children—The dose is based on body weight and must be determined by your doctor. The usual dose is 50 mg per kg (22.7 mg per pound) of body weight a day injected into a vein. Your doctor may change the dose if needed.
To prevent and treat carnitine deficiency in kidney disease patients on hemodialysis: Adults and children—10 to 20 mg per kg of body weight a day, after dialysis. The dose may be reduced based on laboratory test results, after 3 to 4 weeks of therapy.
Missed Dose If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.
Taking doses too close together may increase stomach upset.
Storage Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.
Keep out of the reach of children.
Do not keep outdated medicine or medicine no longer needed.
Precautions While Using Carnitor Do not change brands or dosage forms of levocarnitine without first checking with your doctor. Different products may not work in the same way. If you refill your medicine and it looks different, check with your pharmacist
Carnitor Side Effects Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.
Check with your doctor as soon as possible if any of the following side effects occur:
More common High blood pressure
Less common Fast heartbeat fever
Rare Seizures
Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:
More common Abdominal or stomach cramps diarrhea headache nausea or vomiting
Less common Abdominal discomfort body odor depression dizziness impaired vision loss of appetite or weight swelling in hands, lower legs, and feet tingling sensation weakness
Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.
Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.
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